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Information on EC 3.4.22.27 - cathepsin S
for references in articles please use BRENDA:EC3.4.22.27
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EC Tree 3 Hydrolases
3.4 Acting on peptide bonds (peptidases)
3.4.22 Cysteine endopeptidases
3.4.22.27 cathepsin S
IUBMB Comments
A lysosomal cysteine endopeptidase that is unusual amongst such enzymes for its stability to neutral pH. In peptidase family C1 (papain family)
The enzyme appears in viruses and cellular organisms
- 3.4.22.27
- cathepsins
- lysosomal
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point-of-care
- cystatins
- dendritic
- atherosclerosis
- proteinases
- elastin
- papain
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antigen-presenting
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histocompatibility
- autoimmune
- drug development
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lacrimal
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papain-like
- diagnostics
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ii-associated
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elastolytic
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resource-limited
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s-deficient
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procathepsins
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l-like
- pharmacology
- endostatin
- microglial
- fractalkine
- medicine
- par2
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collagenolytic
- syphilis
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ii-restricted
Reaction Schemes
showsimilar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
Synonyms
cathepsin s, pocts, cat s, cat-s, pfctssa, socats, cath s, rs1136774, rs7534124, rs16827671, more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
C01.034
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Cat S
Cat-S
cathepsin S
CatS
CTSS
Cat S
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cathepsin S
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cathepsin S
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cathepsin S
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
similar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
similar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
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similar to cathepsin L, but with much less activity on Z-Phe-Arg-/-NHMec, and more activity on the Z-Val-Val-Arg-/- compound
the catalytic triad is formed by Cys25, His164, and Asn184, the substrate binding site lies between the N-terminal and the C-terminal domain, cysteine protease mechanism, overview
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY
71965-46-3
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(4-methyl-7-[[(2S)-2-(4-[(1S)-1-(4-methylcyclohexyl)-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
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Substrates: -
Products: -
Products: -
?
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMGAPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWHPMG + APWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: specific substrate for CatS
Products: -
Products: -
?
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMGLPWEK(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: specific substrate for CatS
Products: -
Products: -
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(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
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Substrates: -
Products: -
Products: -
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(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(thiophen-3-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
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Substrates: -
Products: -
Products: -
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(phenylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
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Substrates: -
Products: -
Products: -
?
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid + H2O
?
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Substrates: -
Products: -
Products: -
?
10 kDa fragment of the lysosomal MHCII-bound invariant chain + H2O
class II associated invariant chain peptide fragments
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Substrates: li p10
Products: -
Products: -
?
Ac-His-Pro-Val-Lys-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Ac-His-Pro-Val-Lys + 7-amino-3-carbamoylmethyl-4-methylcoumarin
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Substrates: assay at pH 5.5, 37°C
Products: -
Products: -
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-L-Val-L-Val-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Leu-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Lys-4-nitrophenyl ester + H2O
benzyloxycarbonyl-Lys + 4-nitrophenol
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Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-4-nitroanilide + H2O
benzyloxycarbonyl-Phe-Arg + 4-nitroaniline
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
?
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Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
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benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
Boc-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
Boc-Val-Leu-Lys + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
?
butyloxycarbonyl-L-Phe-L-Phe-L-Arg-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-L-Phe-L-Phe-L-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
cathepsin K + H2O
?
Substrates: cathepsin S cleaves cathepsin K (cathepsin cannibalism) which reduces the total elastin- and collagen-degradative activity in the multiple cathepsin system
Products: -
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CBZ-Val-Val-Arg- 7-amino-4-trifluoromethyl coumarin + H2O
?
Substrates: -
Products: -
Products: -
?
Cbz-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Cbz-Val-Val-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
?
CX3CL1 + H2O
?
Substrates: cathepsin S is able to cleave membrane-anchored CX3CL1, releasing a 55-kDa fragment to the medium
Products: -
Products: -
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elastin + H2O
elastin fragments
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Substrates: -
Products: catS generates soluble elastin peptides
Products: catS generates soluble elastin peptides
?
GRWH-norleucine-VGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWH-norleucine-VG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHDVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHDVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHFVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHFVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHGVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHGVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHIVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHIVGL + RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHKVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHKVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHPVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHPVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHT-norleucine-GLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHT-norleucine-G + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTDGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTDG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTFGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTFG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTGGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTGG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTIGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTIG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTKGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTKG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
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?
GRWHTMGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTMG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTPGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTPG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTTGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTTG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTV-norleucine-LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTV-norleucine + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVDLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVD + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVFLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVF + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVG-citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVG-norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGFRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + FRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGIRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + IRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGKRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + KRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGLRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVGLRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + LRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHTVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
GRWHTVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: specific substrate for CatS
Products: -
Products: -
?
GRWHTVGRRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + RRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
GRWHTVGVRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVG + VRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVILRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVI + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVKLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVK + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVPLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVP + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVQLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVQ + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
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GRWHTVTLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHTVT + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
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Substrates: -
Products: -
Products: -
?
GRWHVVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2 + H2O
GRWHVVG + LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
Substrates: -
Products: -
Products: -
?
Ii-p10 + H2O
?
-
Substrates: i.e. MHC classe-associated invariant chain, cathepsin S is the only human cysteine protease able to efficiently degrade the Ii-p10 fragment in epithelial cells
Products: -
Products: -
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invariant chain + H2O
?
-
Substrates: invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM
Products: -
Products: -
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L-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
L-Leu-Leu-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
laminin alpha5-chain + H2O
?
Substrates: the laminin-alpha5-chain is cleaved by CatS specifically at the Ser-Val bond
Products: -
Products: -
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MCA-GRWPPMG-LPWEK(Dnp)-D-Arg-NH2 + H2O
?
Substrates: internally quenched peptide substrate, spans the entire Schechter-Berger subsite area between subsites S4 and S2' and beyond of the enzyme
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MG101 + H2O
?
Substrates: MG101: BHQ3-EEEEEAAGRWHPMGAPWEAARRRRRC-1-ethylpyrrolidine-2,5-dione-AF680, substrate-based probe for monitoring extracellular CatS activity. The fused peptide hairpin loop-structure, combines a CatS recognition domain, an electrostatic zipper, as well as a N- and C-terminal Foerster resonance energy transfer pair
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MG73 + H2O
?
Substrates: MG73: Abz-EEEEEAAGRWHPMGAPWEAARRRRRC-1-ethylpyrrolidine-2,5-dione-Dnp, substrate-based probe for monitoring extracellular CatS activity. The fused peptide hairpin loop-structure, combines a CatS recognition domain, an electrostatic zipper, as well as a N- and C-terminal Abz/Tyr(NO2)
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MHCII-class assosciated invariant chain li + H2O
class II invariant chain peptide fragments
-
Substrates: -
Products: -
Products: -
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N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-L-Phe-Arg + 7-amino-4-methylcoumarin
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Substrates: -
Products: -
Products: -
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N-benzyloxycarbonyl-Phe-Arg-4-nitroanilide + H2O
N-benzyloxycarbonyl-Phe-Arg + 4-nitroaniline
Substrates: -
Products: -
Products: -
?
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide + H2O
?
-
Substrates: -
Products: -
Products: -
?
nidogen-1 + H2O
?
Substrates: protein of basement membrane architecture
Products: -
Products: -
?
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu + Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 80% cleavage site, 20% cleavage site: o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 80% cleavage site, 20% cleavage site: o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Gly-Arg-Leu-Asp-Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Arg-Leu-Asp + Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Gly-Phe-Phe-Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Gly-Phe-Phe + Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-His-Leu-Val-Glu + Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 56% cleavage site, 44% cleavage site: o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu + Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 56% cleavage site, 44% cleavage site: o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu + Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Leu-Arg-Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Arg-Met-Lys + Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 74% cleavage site, 26% cleavage site: o-aminobenzoic acid-Leu-Arg + Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 74% cleavage site, 26% cleavage site: o-aminobenzoic acid-Leu-Arg + Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Leu-Gln-Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Gln + Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 57% cleavage site, 42% cleavage site: o-aminobenzoic acid-Leu-Gln-Leu-Glu + Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 57% cleavage site, 42% cleavage site: o-aminobenzoic acid-Leu-Gln-Leu-Glu + Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Leu-Tyr-Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Leu-Tyr-Leu + Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 70% cleavage site, 30% cleavage site: o-aminobenzoic acid-Leu-Tyr + Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 70% cleavage site, 30% cleavage site: o-aminobenzoic acid-Leu-Tyr + Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu-Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu + Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Lys-Pro-Val-Ser-Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Lys-Pro-Val-Ser + Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Phe-Val-Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Phe-Val-Asn + Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: 69% cleavage site, 31% cleavage site: o-aminobenzoic acid-Glu-Val + Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
Products: 69% cleavage site, 31% cleavage site: o-aminobenzoic acid-Glu-Val + Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
?
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine) + H2O
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu + Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe + Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
Substrates: -
Products: -
Products: -
?
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr-Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine + H2O
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr + Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
Substrates: -
Products: -
Products: -
?
Oxidized insulin B-chain + H2O
?
-
Substrates: major cleavage sites: Glu13-Ala14, Leu17-Val18 and Phe25-Tyr26. Minor cleavage sites: Asn3-Gln4, Ser9-His10 and Leu15-Tyr16
Products: -
Products: -
?
plasminogen + H2O
?
-
Substrates: -
Products: cleavage occurs at the Leu469-Leu470 peptide bond resulting in 2 fragments: 60000 Da and 38000 Da
Products: cleavage occurs at the Leu469-Leu470 peptide bond resulting in 2 fragments: 60000 Da and 38000 Da
?
prion protein 94-233 + H2O
prion protein 135-233 + prion protein 117-233 + prion protein 114-233
-
Substrates: in vitro, enzyme causes specific and limited N-terminal truncation of prion protein 94-233
Products: major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
Products: major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
?
pro-dipeptidyl peptidase I + H2O
?
-
Substrates: i.e. cathepsin C, less efficient activation than with cathepsin L
Products: -
Products: -
?
tert-butyloxycarbonyl-Phe-Leu-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Z-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
Z-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Arg-7-amido-4-methylcoumarin + H2O
Arg + 7-amino-4-methylcoumarin
-
Substrates: no activity detected
Products: -
Products: -
?
azocasein + H2O
?
-
Substrates: high activity in presence of urea at pH 5.5
Products: -
Products: -
?
azocasein + H2O
?
-
Substrates: reaction only in presence of urea
Products: -
Products: -
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzoyl-Phe-Val-Arg-7-amido-4-methylcoumarin + H2O
benzoyl-Phe-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-L-Val-L-Val-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-L-Val-L-Val-L-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-L-Val-L-Val-L-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-4-methyl-coumaryl-7-amide + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: 73% of the activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin + H2O
butyloxycarbonyl-Val-Leu-Lys + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Collagen type I + H2O
?
-
Substrates: degradation in plasma membranes
Products: -
Products: -
?
Elastin + H2O
?
-
Substrates: can hydrolyze insoluble elastin at acid and neutral pH
Products: -
Products: -
?
Elastin + H2O
?
-
Substrates: elastolytic enzyme activity of cathepsin S in artherosclerotic lesions, degradation of aortic elastin contributing to atherosclerosis and diabetes
Products: -
Products: -
?
Elastin + H2O
?
-
Substrates: degradation, elastolytic enzyme activity of cathepsin S
Products: -
Products: -
?
Elastin + H2O
?
-
Substrates: the enzyme shows distinctive preferences in degrading elastins from bovine neck ligament, aorta, and lung
Products: -
Products: -
?
Elastin + H2O
?
Substrates: i.e. CongoRed elastin or bovine neck elastin
Products: -
Products: -
?
Ii protein + H2O
Ii fragments
-
Substrates: inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
Products: -
Products: -
?
Ii protein + H2O
Ii fragments
-
Substrates: inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
Products: -
Products: -
?
Ii protein + H2O
Ii fragments
-
Substrates: Ii invariant chain
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: bioactive gamma2-fragments of 100 kDa, 80 kDa, and 50 kDa
Products: bioactive gamma2-fragments of 100 kDa, 80 kDa, and 50 kDa
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
MHC class II-associated invariant chain Ii + H2O
?
-
Substrates: degradation, cathepsin S and MHC class II-associated invariant chain Ii are responsible for in vivo control of endosomal size and multivesicular morphology
Products: -
Products: -
?
MHC class II-associated invariant chain Ii + H2O
?
-
Substrates: degradation
Products: -
Products: -
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
tert-butyloxycarbonyl-Phe-Phe-Arg-7-amido-4-methylcoumarin + H2O
tert-butyloxycarbonyl-Phe-Phe-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
-
Substrates: -
Products: -
Products: -
?
Z-Leu-Leu-Arg-7-amido-4-methylcoumarin + H2O
Z-Leu-Leu-Arg + 7-amino-4-methylcoumarin
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme prefers small neutral amino acid residues in the subsites S2 and S3
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is considered crucial for normal presentation of major histocompatibility complex class II-restricted antigens by antigen presenting cells to CD4+ T cells. It is a key enzyme for the degradation of the class II-associated invariant chain, a process that is required for effective antigen loading of class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme may contribute to the contact-dependent elastase activity of live human alveolar macrophages
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is involved in obesity and development of adiposity, enzyme regulation in subcutaneous adipose tissue, cathepsin S is upregulated in obesity, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: Cat S is involved in degradtion of extracellular matrix and smooth muscle cell invasion, but not in adhesion and migration, overview, the enzyme shows elastolytic and collagenolytic activities on smooth muscle cell plasma membranes, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: serum cathepsin S is increased in patients with atherosclerosis and diabetes, the cystatin C level might play a role in disease development, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview, Cat S might be involved in psoriasis induction due to an increased interferon gamma level in the epidermis, Cat S is increased in neurons of Alzheimer's disease and Down's syndrome patients, where Cat S facilitates the formation of amyloidbeta from its precursor protein, Cat S might also be involved in asthma, Sjörgren's syndrome, allergen-specific T-cell proliferation in autoimmune processes, and atherosclerosis, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: active Cat S co-localizes with integrins, e.g. integrin alphanubeta3
Products: -
Products: -
?
additional information
?
-
-
Substrates: Cat S forms an alpha-beta-CLIP complex, unlike CatB or CatD, from an alpha-beta-Ii molecule in vitro
Products: -
Products: -
?
additional information
?
-
Substrates: does not cleave GRWHKISVRWE
Products: -
Products: -
?
additional information
?
-
-
Substrates: does not cleave GRWHKISVRWE
Products: -
Products: -
?
additional information
?
-
Substrates: CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
Products: -
Products: -
?
additional information
?
-
-
Substrates: CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is capable of degrading a range of extracellular matrix macromolecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is identified as a compound involved in MHC class II maturation and trafficking within antigen presentation pathways, as well as in the control of processing antigens and the formation of peptide-receptive class II dimers
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme mediates degradation of the MHC class II invariant chain and participates in antigen processing
Products: -
Products: -
?
additional information
?
-
-
Substrates: protease is implicated in the development of atherosclerotic lesions in both animal
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is one of the major proteases involved in antigen processing
Products: -
Products: -
?
additional information
?
-
-
Substrates: the cysteine protease cathepsin S is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity
Products: -
Products: -
?
additional information
?
-
-
Substrates: in the case of atherosclerotic lesions, the local extracellular matrix is degraded either by CatS secreted by smooth muscle cells and macrophages or by circulating CatS produced by adipose tissue, this elastolytic activity of CatS causes the migration of blood monocytes and smooth muscle cells into the vascular wall which leads to the progression of atherosclerotic lesions
Products: -
Products: -
?
additional information
?
-
Substrates: cathepsin S is putatively involved in the pathogenesis of COPD
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is putatively involved in the pathogenesis of COPD
Products: -
Products: -
?
additional information
?
-
Substrates: this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
Products: -
Products: -
?
additional information
?
-
Substrates: in antigen presenting cells Cat S plays an essential role in the proteolytic events that lead to antigen presentation at the cells surface for recognition by T cells
Products: -
Products: -
?
additional information
?
-
Substrates: major role of Cat S in these cells is the processing of the major histocompatibility complex class II associated invariant chain, which is essential for the normal functioning of the immune system, Cat S is largely responsible for the last proteolytic cleavage step of the invariant chain that produces class II-associated leupeptin induced peptide
Products: -
Products: -
?
additional information
?
-
-
Substrates: the function of cathepsin S within antigen presenting cells relates to its pivotal role in major histocompatibility class II restricted antigen presentation to CD4+ T-lymphocytes, cathepsin S mediates the final proteolytic cleavage of the invariant chain chaperone molecule 2 thereby facilitating the subsequent presentation of MHC-II associated peptides to CD4+ T-cells
Products: -
Products: -
?
additional information
?
-
-
Substrates: the major role of CAT S is the processing of the major histocompatibility complex (MHC) class II associated invariant chain, which is essential for the normal functioning of the immune system
Products: -
Products: -
?
additional information
?
-
Substrates: cathepsin S-dependent activation of PAR-2 activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S-dependent activation of PAR-2 activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S, a cysteine protease, plays an important role in generating peptides for the vacuolar, TAP-independent MHC class I cross-presentation in vivo
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: Cat S forms an alpha-beta-CLIP complex, unlike CatB or CatD, from an alpha-beta-Ii molecule in vitro
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is a potent regulator of both cell and matrix turnover in advanced atherosclerosis
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is an elastolytic enzyme
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is implicated in the regulation of intracellular cholesterol metabolism
Products: -
Products: -
?
additional information
?
-
-
Substrates: catS is a potent elastolytic protease and accelerates calcification in atherosclerotic mice with chronic renal disease induced by 5/6 nephrectemy
Products: -
Products: -
?
additional information
?
-
-
Substrates: catS has proinflammatory effects
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsins are primarily involved in general protein turnover, CATS belongs to the cathepsins with a distinct substrate specificity
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS participates in inflammatory processes accompanying aging and pathologies of the central nervous system
Products: -
Products: -
?
additional information
?
-
-
Substrates: it degrades the invariant chain Ii, which is crucial to the immune response since it acts as an essential step in MHC class II antigen presentation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S substrate Leu-Arg and a poly(ethylene glycol) chain in dendritic arms
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: no activity with benzyloxycarbonyl-Arg-Arg-7-amido-4-methylcoumarin and benzoyl-Gly-Gly-7-amido-4-methylcoumarin
Products: -
Products: -
?
additional information
?
-
-
Substrates: proteolysis of prion protein by cathepsin S generates a soluble-structured intermediate oligomeric form, with potential implications for neurotoxic mechanisms
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: primary role of the enzyme in heterophagocytosis of proteins from the ultrafiltrate
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is possibly involved in thyroid hormone biosynthesis
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS is an important player in the spinal mechanisms involved in chronic pain induction and maintenance
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS is widely expressed in the brain and is implicated in several neurological conditions such as Alzheimer's disease, amyotrophic lateral sclerosis and age-related inflammation, CATS is also implicated in neuropathic hyperalgesia and allodynia
Products: -
Products: -
?
additional information
?
-
-
Substrates: key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
Collagen type I + H2O
?
-
Substrates: degradation in plasma membranes
Products: -
Products: -
?
CX3CL1 + H2O
?
Substrates: cathepsin S is able to cleave membrane-anchored CX3CL1, releasing a 55-kDa fragment to the medium
Products: -
Products: -
?
elastin + H2O
elastin fragments
-
Substrates: -
Products: catS generates soluble elastin peptides
Products: catS generates soluble elastin peptides
?
Ii-p10 + H2O
?
-
Substrates: i.e. MHC classe-associated invariant chain, cathepsin S is the only human cysteine protease able to efficiently degrade the Ii-p10 fragment in epithelial cells
Products: -
Products: -
?
invariant chain + H2O
?
-
Substrates: invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM
Products: -
Products: -
?
laminin alpha5-chain + H2O
?
Substrates: the laminin-alpha5-chain is cleaved by CatS specifically at the Ser-Val bond
Products: -
Products: -
?
MHC class II-associated invariant chain Ii + H2O
?
-
Substrates: degradation, cathepsin S and MHC class II-associated invariant chain Ii are responsible for in vivo control of endosomal size and multivesicular morphology
Products: -
Products: -
?
prion protein 94-233 + H2O
prion protein 135-233 + prion protein 117-233 + prion protein 114-233
-
Substrates: in vitro, enzyme causes specific and limited N-terminal truncation of prion protein 94-233
Products: major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
Products: major soluble fragments, the region of prion protein between S135 and N146 is a major target for selective cleavage cathepsins S
?
Elastin + H2O
?
-
Substrates: elastolytic enzyme activity of cathepsin S in artherosclerotic lesions, degradation of aortic elastin contributing to atherosclerosis and diabetes
Products: -
Products: -
?
Ii protein + H2O
Ii fragments
-
Substrates: inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
Products: -
Products: -
?
Ii protein + H2O
Ii fragments
-
Substrates: inhibition of Ii degradation in enzyme-deficient cells leads to accumulation of Ii degradation intermediates in endosomal/lysosomal compartments
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
laminin-5 + H2O
laminin-5 gamma-2 fragments
-
Substrates: degradation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is considered crucial for normal presentation of major histocompatibility complex class II-restricted antigens by antigen presenting cells to CD4+ T cells. It is a key enzyme for the degradation of the class II-associated invariant chain, a process that is required for effective antigen loading of class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme may contribute to the contact-dependent elastase activity of live human alveolar macrophages
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme is involved in obesity and development of adiposity, enzyme regulation in subcutaneous adipose tissue, cathepsin S is upregulated in obesity, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: Cat S is involved in degradtion of extracellular matrix and smooth muscle cell invasion, but not in adhesion and migration, overview, the enzyme shows elastolytic and collagenolytic activities on smooth muscle cell plasma membranes, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: serum cathepsin S is increased in patients with atherosclerosis and diabetes, the cystatin C level might play a role in disease development, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview, Cat S might be involved in psoriasis induction due to an increased interferon gamma level in the epidermis, Cat S is increased in neurons of Alzheimer's disease and Down's syndrome patients, where Cat S facilitates the formation of amyloidbeta from its precursor protein, Cat S might also be involved in asthma, Sjörgren's syndrome, allergen-specific T-cell proliferation in autoimmune processes, and atherosclerosis, overview
Products: -
Products: -
?
additional information
?
-
Substrates: CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
Products: -
Products: -
?
additional information
?
-
-
Substrates: CTSS is a cysteine protease that has a central role in remodeling the extracellular matrix and it is implicated in the etiology of cardiovascular disease
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is capable of degrading a range of extracellular matrix macromolecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is identified as a compound involved in MHC class II maturation and trafficking within antigen presentation pathways, as well as in the control of processing antigens and the formation of peptide-receptive class II dimers
Products: -
Products: -
?
additional information
?
-
-
Substrates: enzyme mediates degradation of the MHC class II invariant chain and participates in antigen processing
Products: -
Products: -
?
additional information
?
-
-
Substrates: protease is implicated in the development of atherosclerotic lesions in both animal
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is one of the major proteases involved in antigen processing
Products: -
Products: -
?
additional information
?
-
-
Substrates: the cysteine protease cathepsin S is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity
Products: -
Products: -
?
additional information
?
-
-
Substrates: in the case of atherosclerotic lesions, the local extracellular matrix is degraded either by CatS secreted by smooth muscle cells and macrophages or by circulating CatS produced by adipose tissue, this elastolytic activity of CatS causes the migration of blood monocytes and smooth muscle cells into the vascular wall which leads to the progression of atherosclerotic lesions
Products: -
Products: -
?
additional information
?
-
Substrates: cathepsin S is putatively involved in the pathogenesis of COPD
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is putatively involved in the pathogenesis of COPD
Products: -
Products: -
?
additional information
?
-
Substrates: this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: this enzyme serves a crucial role in MHC class II mediated immune systems, resulting in CD4+ T cell activation
Products: -
Products: -
?
additional information
?
-
Substrates: in antigen presenting cells Cat S plays an essential role in the proteolytic events that lead to antigen presentation at the cells surface for recognition by T cells
Products: -
Products: -
?
additional information
?
-
Substrates: major role of Cat S in these cells is the processing of the major histocompatibility complex class II associated invariant chain, which is essential for the normal functioning of the immune system, Cat S is largely responsible for the last proteolytic cleavage step of the invariant chain that produces class II-associated leupeptin induced peptide
Products: -
Products: -
?
additional information
?
-
-
Substrates: the function of cathepsin S within antigen presenting cells relates to its pivotal role in major histocompatibility class II restricted antigen presentation to CD4+ T-lymphocytes, cathepsin S mediates the final proteolytic cleavage of the invariant chain chaperone molecule 2 thereby facilitating the subsequent presentation of MHC-II associated peptides to CD4+ T-cells
Products: -
Products: -
?
additional information
?
-
-
Substrates: the major role of CAT S is the processing of the major histocompatibility complex (MHC) class II associated invariant chain, which is essential for the normal functioning of the immune system
Products: -
Products: -
?
additional information
?
-
Substrates: cathepsin S-dependent activation of PAR-2 activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S-dependent activation of PAR-2 activation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S, a cysteine protease, plays an important role in generating peptides for the vacuolar, TAP-independent MHC class I cross-presentation in vivo
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is a potent regulator of both cell and matrix turnover in advanced atherosclerosis
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is an elastolytic enzyme
Products: -
Products: -
?
additional information
?
-
-
Substrates: CatS is implicated in the regulation of intracellular cholesterol metabolism
Products: -
Products: -
?
additional information
?
-
-
Substrates: catS is a potent elastolytic protease and accelerates calcification in atherosclerotic mice with chronic renal disease induced by 5/6 nephrectemy
Products: -
Products: -
?
additional information
?
-
-
Substrates: catS has proinflammatory effects
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsins are primarily involved in general protein turnover, CATS belongs to the cathepsins with a distinct substrate specificity
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS participates in inflammatory processes accompanying aging and pathologies of the central nervous system
Products: -
Products: -
?
additional information
?
-
-
Substrates: it degrades the invariant chain Ii, which is crucial to the immune response since it acts as an essential step in MHC class II antigen presentation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S controls angiogenesis and tumor growth via matrix-derived angiogenic factors, the enzyme is required for neoplastic progression, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S in professional antigen-presenting cells, APC, controls MHC class II-mediated antigen presentation by epithelial cells in vivo, and plays a critical role in invariant chain degradation
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is responsible for murine autoimmune myasthenia gravis pathogenesis, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: proteolysis of prion protein by cathepsin S generates a soluble-structured intermediate oligomeric form, with potential implications for neurotoxic mechanisms
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is implicated as a key enzyme in the processing of major histocompatability complex class II molecules
Products: -
Products: -
?
additional information
?
-
-
Substrates: primary role of the enzyme in heterophagocytosis of proteins from the ultrafiltrate
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S is possibly involved in thyroid hormone biosynthesis
Products: -
Products: -
?
additional information
?
-
-
Substrates: cathepsin S catalyzes a key step in antigen presentation, detailed overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS is an important player in the spinal mechanisms involved in chronic pain induction and maintenance
Products: -
Products: -
?
additional information
?
-
-
Substrates: CATS is widely expressed in the brain and is implicated in several neurological conditions such as Alzheimer's disease, amyotrophic lateral sclerosis and age-related inflammation, CATS is also implicated in neuropathic hyperalgesia and allodynia
Products: -
Products: -
?
additional information
?
-
-
Substrates: key protease responsible for the removal of the invariant chain from MHC class II molecules, the enzyme plays a major role in antigen presentation
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
-
-
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-2-[(4-bromobenzene-1-sulfonyl)amino]-3-phenylpropyl N-benzoyl-D-phenylalaninate
inhibitory against both cathepsin L and S, not inhibitory to cathepsin B, K
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1991 nM
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 8340 nM
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
IC50: 1427 nM
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
-
-
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-(1-cyanocyclopropyl)-3-((4-(pyridin-2-yl)-piperazin-1-yl)sulfonyl)-2-(2-(thiophen-2-yl)acetamido)-propanamide
inhibitor dispalys poor cell membrane permeability
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
-
IC50: 609 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 2010 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50 above 0.01 mM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3931 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1365 nM
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 2364 nM
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
IC50: 658 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
-
-
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
-
-
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-(1-cyanocyclopropyl)-2-[(pyridin-3-yl)amino]-2-[4-(pyridin-2-yl)piperazine-1-sulfonyl]acetamide
inhibitor dispalys poor cell membrane permeability
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
-
-
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
-
-
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 42 nM
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 12 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
-
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 49 nM
(4'-fluorobiphenyl-4-yl)sulfonyl-(S)-phenylalanyl-aminocyclopropane-nitrile
most selective cathepsin S inhibitor synthesized, selectivity ratio for cathepsin S/K is 57, for cathepsin S/L is 31
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
-
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
-
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
-
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
-
IC50 above 0.01 mM
(biphenyl-3-yl)sulfonyl-(S)-leucyl-aminocyclopropane-nitrile
selectivity ratio for cathepsin S/K is 5.8; for cathepsin S/L is 67
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
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1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
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1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
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1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
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-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
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-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
-
-
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 350 nM
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 190 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 10 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
-
-
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 210 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 90 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 140 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 310 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 500 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 460 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 120 nM
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 230 nM
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
-
-
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
-
-
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
1-[(3R)-4-(methylsulfonyl)-2-oxo-3-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]butyl]cyclopropanecarbonitrile
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
-
-
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 130 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 100 nM
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 110 nM
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 180 nM
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 200 nM
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
IC50: 50 nM
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
-
-
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
-
-
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
-
-
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
-
-
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 0.020 mM
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
-
-
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
-
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
-
IC50: 120 nM
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
-
-
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
-
-
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
-
-
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
-
-
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 35 nM
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
-
-
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
-
-
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
-
-
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
-
-
2-[3-(4-chloro-3-[4-[(4-chloro-benzylamino)-methyl]-phenylethynyl]-phenyl)-1-[3-(3-methyl-morpholin-4-yl)-propyl]-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-2-oxo-acetamide
-
-
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
-
-
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
-
-
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
-
IC50: 20 nM
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
-
-
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
-
-
2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
-
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
-
IC50: 1373 nM
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
-
-
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 33 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
-
IC50: 5.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
-
IC50: 3.3 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 8.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
-
IC50: 4.0 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
-
IC50: 17 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
-
IC50: 34 nM
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
-
IC50: 26 nM
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 197 nM
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 43 nM
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.0 nM
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
-
-
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-(((S)-3-cyclohexyl-1-(((S,E)-1-fluoro-1-(phenoxysulfonyl)-5-phenylpent-1-en-3-yl)amino)-1-oxopropan-2-yl)carbamoyl)benzenaminium chloride
compound allows the attachment of various functionalities, such as linkers or nanodelivery systems
-
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 123 nM
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-bromo-N-[(2R)-1-[(2R)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]benzene-1-sulfonamide
inhibitory against both cathepsin L and S, not inhibitory to cathepsin B, K
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 16 nM
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
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4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
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4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl]
-
previously reported as 05141, ihbitor-dosed mice are protected against ozone-induced airway hyperresponsiveness
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
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4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
-
-
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
-
-
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
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4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
-
-
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 150 nM
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 80 nM
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 60 nM
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 30 nM
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
-
-
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
-
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
-
-
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyloxycarbonyl Phe-Ala-CH2F
-
very potent time-dependent inhibitor, inhibits proteinase 30times more efficiently than it does cathepsin L and about 300times better than it does cathepsin B
benzyloxycarbonyl-((CH3)3C-CH2-CH(NH2)-COOH)-Leu-Tyr-CHN2
-
t1/2 at 0.0004 mM is 3.85 min
benzyloxycarbonyl-Phe-Leu-COCHO
-
potent, reversible cathepsin S inhibitor, the inhibitor is 400fold more selective for cathepsin S than for cathepsin B
benzyloxycarbonyl-Phe-Lys(benzyloxycarbonyl)-CH3
-
inhibition in the micromolar range, competitive
benzyloxycarbonyl-Phe-Tyr(tert-butyl)CHN2
-
t1/2 at 0.02 mM is 19.25 min, about 10000times more effective against cathepsin L than against cathepsin S
benzyloxycarbonyl-Val-Val-Nle-CHN2
-
t1/2 at 0.000001 is 2.5 min, 300times more effective in inactivating cathepsin S than cathepsin L
benzyloxycarbonyl-Val-Val-Phe-CH3
-
inhibition in the micromolar range, competitive
BMV083
a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells
BMV117
a near-infrared quenched activity-based probe (qABP) that selectively targets cathepsin S in immune cells
BMV157
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
cathepsin S propeptide
-
0.0002 mM, blocks gelatinase, collagenase and elastinase activities of mature cathepsin S
-
CLIK60
-
selective CatS inhibitor, CatS inhibition increases macrophage cholesterol accumulation and efflux
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 71 nM
LO143
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
LO219
a near-infrared quenched activity-based probe (qABP) that targets cathepsin S in immune cells
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
-
-
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
-
-
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
-
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
-
-
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
-
-
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 2-amino-4-([(1S)-2-(1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropylamino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)benzoate
-
-
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
-
IC50: 43 nM
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
-
-
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4-([(1S)-2-((1S)-1-[(benzyloxy)methyl]-3-[(2-ethoxy-2-oxoethyl)amino]-2,3-dioxopropyl amino)-1-(cyclohexylmethyl)-2-oxoethyl]aminocarbonyl)-2-[(tert-butoxycarbonyl)amino]benzoate
-
-
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
-
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 565 mM
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
-
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.011 mM
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 387 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
-
IC50: 0.107 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
-
IC50: 1400 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 130 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
-
IC50: 0.076 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
-
IC50: 5 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
-
IC50: 0.006 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
-
IC50: 173 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
-
IC50: 23 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
-
IC50: 84 nM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
-
IC50: 0.134 mM
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
-
IC50: 41 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
-
IC50: 82 nM
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 142 nM
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 19 nM
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
-
IC50: 124 nM
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 114 nM
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
-
IC50: 51 nM
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 11 nM
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
-
IC50: 56 nM
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 7 nM
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
IC50: 35 nM
morpholine-4-carboxylic acid [1S-[2-(2-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(3-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
9 nM
morpholine-4-carboxylic acid [1S-[2-(4-chlorobenzyloxy)-1R-cyanoethylcarbamoyl]-3-methylbutyl]amide
-
27 nM
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
-
IC50: 0.097 m
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
-
IC50 above 0.339 mM
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
-
IC50 above 0.028 mM
morpholineurea-leucyl-homophenylalanine-vinylsulfone phenyl
-
LHVS, CatS-specific inhibitor at a concentration of 10 nM, other cathepsins are not inhibited
morpholinurea-leucine-homophenylalanine-vinyl sulfone-phenyl
-
irreversible inhibitor
morpholinurea-leucinehomophenylalanine-vinyl phenyl sulfone
-
irreversible CatS inhibitor
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-((S)-3-cyclohexyl-1-(((S,E)-1-fluoro-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl)amino)-1-oxopropan-2-yl)isonicotinamide
-
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 2310 nM
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
-
IC50: 6597 nM
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
-
IC50 above 0.01 nM
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
-
IC50: 1748 nM
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 521 nM
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 3368 nM
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50 above 0.01 mM
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 652 nM
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1245 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1695 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 9422 nM
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
-
IC50: 1421 nM
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
-
IC50: 6623 nM
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
-
-
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
-
-
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
-
-
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 29 nM
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 62 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 0.020 mM
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
-
IC50: 23 nM
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
-
IC50: 16 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 0.065 mM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 3707 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
-
IC50: 6769 nM
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
-
IC50: 285 nM
N-[(1S)-2-[(1-cyanocyclopropyl)amino]-2-oxo-1-[4-(pyridin-2-yl)piperazine-1-sulfonyl]ethyl]-3,3-dimethylbutanamide
inhibitor dispalys poor cell membrane permeability
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
-
-
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
-
IC50: 38 nM
N-[(1S)-3-methyl-1-(((4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(2R)-1-[(2S)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]-4-(trifluoromethyl)benzene-1-sulfonamide
inhibitory against both cathepsin L and S, not inhibitory to cathepsin B, K
N-[(2S)-1-([4-cyano-1-[3-(morpholin-4-yl)propyl]piperidin-4-yl]amino)-5,5-dimethyl-1-oxoheptan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-1-[(2S)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]pyridine-4-carboxamide
inhibitory against both cathepsin L and S, not inhibitory to cathepsin B, K
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-oxopropan-2-yl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(2S)-3-cyclohexyl-1-[[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]amino]-1-oxopropan-2-yl]morpholine-4-carboxamide
-
-
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
N-[(3S)-4-benzyloxy-(2S)-4-methyl-[[[2-[(9-oxo-9H-1-fluorenyl)carbonyl]amino]propaneyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-amino-4-chlorobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[(2S)-2-[(3-[(tert-butoxycarbonyl)amino]-4-chlorobenzoyl amino)]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ester
-
-
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((1-methylcyclopropyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((2,2-dimethyl-4-oxo-3,4-dihydro-2H-6-pyranyl)carbonyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((5-nitro-2-thienyl)carbonyl)amino]cyclo-hexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[((E)-3-(2,5-dimethoxyphenyl)-2-propenoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2,3-dioxo-3-(2-thienyl)propanoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-(2-thienyl)acetyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(2-chloro-5-(methylsulfanyl)benzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-chloro-3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(4-methoxybenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-chloro-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[(3S)-4-benzyloxy-3-[[[2-[(5-methoxy-2-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
-
-
N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
-
-
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
-
-
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 46 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 27 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
-
IC50: 62 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
-
IC50: 19 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
-
IC50: 29 nM
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
-
IC50: 66 nM
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
-
-
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
-
-
N-[[(2S)-1-[[(1S)-1-cyano-3-phenylpropyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]carbamoyl]morpholine-4-carboxamide
-
-
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 173 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
-
IC50: 21 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 151 nM
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 93 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 26 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
-
IC50: 11 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 15 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 12.3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 3 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 19 nM
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
-
IC50: 1 nM
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 2.9 nM
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.1 nM
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
-
IC50: 26 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
-
IC50: 222 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
-
IC50: 94 nM
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 29 nM
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
-
IC50: 5 nM
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.4 nM
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 9.4 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 49 nM
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 107 nM
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
-
IC50: 7.1 nM
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
-
-
neohesperidin dihydrochalcone
a potent, competitive, and selective inhibitor, impairs hydrolysis of nidogen-1, as well elastin, collagens I and IV
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
phenyl (1E,3S)-3-[[3-cyclohexyl-N-(morpholine-4-carbonyl)-L-alanyl]amino]-1-fluoro-5-phenylpent-1-ene-1-sulfonate
-
phenyl (1E,3S)-3-[[3-cyclohexyl-N-(phenylcarbamoyl)-L-alanyl]amino]-1-fluoro-5-phenylpent-1-ene-1-sulfonate
-
phenyl (S,E)-1-fluoro-3-((S)-2-(isonicotinamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
-
phenyl (S,E)-1-fluoro-3-((S)-2-(morpholine-4-carboxamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
-
phenyl (S,E)-3-((S)-3-cyclohexyl-2-(morpholine-4-carboxamido)propanamido)-1-fluoro-5-phenylpent-1-ene-1-sulfonate
most effective inhibitor synthesized, high selectivity over cathepsins B and L
-
squamous cell carcinoma antigen 1
-
99% inhibition at 1 mM, interacts with cathespin S at 1:1 stoichiometry, t1/2 of the cathepsin-squamous cell carcinoma antigen 1 complex is above 1155 min
-
tanshinone IIA sulfonate
reduces the degradation of CongoRed elastin by about 80% at a 1:20 enzyme/inhibitor molar ratio and reduces the binding of CatS on insoluble bovine neck elastin by about 80%. Inhibitor does not block the hydrolysis of macromolecular protein substrates such as gelatin and thyroglobulin
-
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
-
IC50: 730 nM
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
-
-
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
-
IC50: 1298 nM
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
-
-
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
-
-
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
-
-
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
-
-
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
-
IC50 above 0.02 mM
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
-
-
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
-
-
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 18 nM
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
IC50: 53 nM
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
-
-
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
IC50: 27 nM
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
IC50: 50 nM
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
-
-
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
brain-penetrating cathepsin S inhibitors
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
-
-
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
0.0005 mM: 51-58% inhibition after 10 min. 0.005 mM: 86-90% inhibition after 10 min
cathespin S propeptide
-
more selective for inhibition of cathepsin L than cathepsin S
-
cystatin C
-
specific endogenous inhibitor, potency against smooth muscle cell invasion, overview
-
cystatin C
-
endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogene sis and tumor cell proliferation
-
cystatin C
-
endogenous specific enzyme inhibitor, absence of cystatin C results in increased angiogenesis and tumor cell proliferation
-
JNJ 10329670
-
CAS: 400797-24-2, the inhibitor blocks the presentation of tetanus toxoid and giant ragweed by human PBMCs, the inhibitor is a candidate for immunosuppressive therapy of allergies and autoimmune diseases, completely reversible inhibition
JNJ 10329670
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
-
-
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
i.e. LHVS, specific inhibitor, potency against smooth muscle cell invasion, overview
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
specific inhibitor
N-morpholinurea-leucine-homophenylalanine-vinylsulfone-phenyl
-
specific inhibitor
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
-
i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site, in vitro and in vivo inhibition
N-morpholinurea-leucyl-homophenylalanyl-vinylsulfone-phenyl
-
i.e. LHVS, irreversible inhibition, the inhibitor binds covalently to the active site
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
IC50: 17 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
IC50: 34 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
IC50: 47 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
IC50: 6 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
IC50: 213 nM
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
IC50: 11 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
IC50: 12 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
-
-
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
IC50: 21 nM
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
-
-
RO5461111
inhibits Cat-S activity and reduces podocyte loss, proteinuria, glomerulosclerosis, and renal inflammation in T2D db/db mice
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
IC50: 12 nM
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
-
-
additional information
-
inhibitory potential in vivo on Ii degradation in JY cells
-
additional information
-
analysis of inhibition mechanisms and binding to the active site; design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S, overview
-
additional information
-
synthesis and evaluation of heterocyclic arylaminoethyl amides as noncovalent inhibitors of cathepsin S, binding specificities of positions P1-P3 and of subsite S3, overview
-
additional information
-
reversible inhibition by a dipeptide-nitrile inhibitor
-
additional information
design of inhibitory antibodies targeting human CTSS by genetically fusing the propeptide of procathepsin S with antibodiesin IgG and Fab format. The resulting antibody fusions can be stably expressed and potently inhibit CTSS proteolytic activity in high specificity, reaching Ki value in nanomlolar range
-
additional information
-
diverse arylaminoethyl amides as noncovalent inhibitors of cathepsin S with IC50 in the nanomolar range, optimization of P1 and N-aryl, binding specificities of positions P1 and P2, and of subsite S1, overview
-
additional information
-
effect of cathepsin S inhibition on bronchoalveolar lavage fluid cytokines: inhibition reduces ozone-induced interleukin-6 levels at 3 h and 20-24 h and TNF-alpha levels are inhibited at 20-24 h
-
additional information
design and synthesis of a near-infrared quenched activity-based probes (qABP) that selectively target cathepsin S which is highly expressed in immune cells, green-fluorescent pan-reactive cysteine cathepsin qABP in dual color labeling studies in bone marrow-derived immune cells, and identification of vesicles containing exclusively cathepsin S activity, method optimization and evaluation, overview. The high degree of selectivity is retained both in vitro and in vivo
-
additional information
-
synthesis and inhibitory effects of diverse arylaminoethyl carbamate inhibitors possessing a substrate peptidomimetic scaffold, structue-activity relationship, pharmacokinetics, overview
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
kainate
kainate treatment (15 mg/kg) induces a 3.3fold increased cathepsin S expression
Ozone
-
cathepsin S levels peak 3 h after ozone exposure in bronchoalveolar lavage cells
radiation
-
radiation induced production of CatS at both the mRNA and protein level and increased its protease activity, that IFN regulatory factor-1 is the critical transcriptional mediator of interferon-gamma-dependent CatS production after radiation, treatment with as little as 0.5 Gy of radiation induces CatS mRNA, the highest levels are induced in response to treatment with 10 Gy of radiation
-
TNF-alpha
-
cathepsin S can be upregulated by TNF-alpha in endothelial cells and cathepsin S induces endothelial cell motility, invasion and migration
-
dithiothreitol
-
the presence of 0.2 mM dithiothreitol is required to maintain cathepsin activity
additional information
-
IFN-gamma and interleukin-1beta induce cathepsin S expression in smooth muscle plasma membranes
-
additional information
-
treatment with taxol and cisplatin do not induces CatS expression
-
additional information
-
recombinant CatS is activated in 100 mM sodium acetate, pH 5.5 containing 1 mM EDTA and 2 mM dithiothreitol for 30 min at 37°C
-
additional information
cathepsin expression is not increased by nicotin treatment (10 mg/kg)
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.017
(4-methyl-7-[[(2S)-2-(4-[(1S)-1-(4-methylcyclohexyl)-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.00556
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMGLPWEK(2,4-dinitrophenyl)-D-Arg-NH2
-
-
0.41
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.3
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(thiophen-3-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.057
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(phenylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.13
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.0016
GRWH-norleucine-VGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00188
GRWHDVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00142
GRWHFVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00514
GRWHGVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00048
GRWHIVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.17
GRWHKFSVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
0.04
GRWHKISVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
0.09
GRWHKLSVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
0.00194
GRWHKVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00324
GRWHPVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00418
GRWHT-norleucine-GLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01237
GRWHTDGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0021
GRWHTFGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01286
GRWHTGGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00395
GRWHTIGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00782
GRWHTKGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00779
GRWHTMGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00591
GRWHTPGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0093
GRWHTTGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01047
GRWHTV-norleucine-LRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0028
GRWHTVDLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00258
GRWHTVFLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00171
GRWHTVG-citrulline-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00073
GRWHTVG-norleucine-RWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0048
GRWHTVGFRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00198
GRWHTVGIRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00525
GRWHTVGKRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00314
GRWHTVGLDWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00527
GRWHTVGLFWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00312
GRWHTVGLHWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0015
GRWHTVGLIWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00105
GRWHTVGLKWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00131
GRWHTVGLPWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00259
GRWHTVGLQWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01668
GRWHTVGLRDE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0082
GRWHTVGLRFE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01648
GRWHTVGLRGE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01493
GRWHTVGLRHE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0082
GRWHTVGLRIE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.03787
GRWHTVGLRKE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01154
GRWHTVGLRRE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00237
GRWHTVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00244
GRWHTVGRRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00237
GRWHTVGVRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00512
GRWHTVILRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.02747
GRWHTVKLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.01998
GRWHTVPLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0249
GRWHTVQLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00506
GRWHTVTLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.00276
GRWHVVGLRWE-Lys(2,4-dinitrophenyl)-D-Arg-NH2
-
0.02 mM substrate, 1.3 nM CatS, 50 mM sodium acetate, 4 mM dithiothreitol, pH 5.5, 37°C
0.0015
o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
0.0171
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L,, pH 5.5, 25°C
0.0198
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L plus mutation Y118A, pH 5.5, 25°C
0.0267
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
wild-type, pH 5.5, 25°C
0.0315
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant Y118A, pH 5.5, 25°C
0.0343
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant DeltaG119, pH 5.5, 25°C
0.0534
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutation of exosite 1, pH 5.5, 25°C
0.0125
benzyloxycarbonyl-Phe-Val-Arg-7-amido-4-methylcoumarin
-
in 50 mM sodium phosphate buffer, pH 6.5, containing 2.5 mM EDTA and 0.1% PEG-6000
0.006
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
0.011
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
0.013
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
0.014
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
0.0184
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
at pH 6.5 and 37°C
0.024
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
0.288
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 7.5, 37°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.46
(4-methyl-7-[[(2S)-2-(4-[(1S)-1-(4-methylcyclohexyl)-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-2-oxo-2H-chromen-3-yl)acetic acid
-
-
5.666
(7-methoxycoumarin-4-yl)-acetyl-GRWPPMGLPWEK(2,4-dinitrophenyl)-D-Arg-NH2
-
-
0.45
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(phenylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.77
(7-[[(2S)-2-(4-[(1S)-1,2-dimethyl-1-[(thiophen-3-ylcarbonyl)amino]propyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.2
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(phenylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
0.22
(7-[[(2S)-2-(4-[(1S)-1-cyclohexyl-1-[(thiophen-3-ylcarbonyl)amino]ethyl]-1H-1,2,3-triazol-1-yl)hexanoyl]amino]-4-methyl-2-oxo-2H-chromen-3-yl)acetic acid
-
-
3.3
butyloxycarbonyl-L-Phe-L-Phe-L-Arg-7-amido-4-methylcoumarin
-
pH 6.5, 25°C
-
11
GRWHKFSVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
3
GRWHKISVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
44
GRWHKLSVRWE
in 0.1 M citrate buffer, pH 5.5 containing 4 mM dithiothreitol, at 37°C
15.1
benzyloxycarbonyl-L-Val-L-Val-L-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
1.57
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L,, pH 5.5, 25°C
1.72
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L plus mutation Y118A, pH 5.5, 25°C
2.57
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant DeltaG119, pH 5.5, 25°C
2.66
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant Y118A, pH 5.5, 25°C
2.8
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
wild-type, pH 5.5, 25°C
3.5
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutation of exosite 1, pH 5.5, 25°C
12.4
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
20.3
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
20.3
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
33.1
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
-
pH 5.0, room temperature
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
1248
o-aminobenzoic acid-Ala-Thr-Pro-Leu-Leu-Met-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
312
o-aminobenzoic acid-Gly-Arg-Leu-Asp-Lys-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
98
o-aminobenzoic acid-Gly-Phe-Phe-Val-Thr-Thr-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
1083
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
866
o-aminobenzoic acid-His-Leu-Val-Glu-Ala-Leu-Tyr-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
2000
o-aminobenzoic acid-Leu-Arg-Met-Lys-Leu-Pro-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
706
o-aminobenzoic acid-Leu-Gln-Leu-Glu-Asn-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
135
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
141
o-aminobenzoic acid-Leu-Tyr-Leu-Val-Cys-Gly-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
5599
o-aminobenzoic acid-Lys-Pro-Pro-Val-Val-Leu-Leu-Pro-Asp-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
923
o-aminobenzoic acid-Lys-Pro-Val-Ser-Thr-Glu-Gln-Leu-Ala-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
66
o-aminobenzoic acid-Phe-Val-Asn-Gln-His-Leu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
1920
o-aminobenzoic acid-Ser-Arg-His-Ser-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
-
-
198
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
1733
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Lys-Val-Tyr-Leu-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
-
67
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutation of exosite 1, pH 5.5, 25°C
75
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant DeltaG119, pH 5.5, 25°C
84
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant Y118A, pH 5.5, 25°C
87
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L plus mutation Y118A, pH 5.5, 25°C
105
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
wild-type, pH 5.5, 25°C
111
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin
mutant with replaced residues 94-177 and introduction of residues 174-180 of cathepsin L,, pH 5.5, 25°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000095
(2R)-2-(2-cyclohexylethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000002
(2R)-2-(2-cyclopentylethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000011
(2R)-2-(2-cyclopentylethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000194
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)butanamide
-
-
0.000013
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000016
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000062
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000018
(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1R)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.000028
(2R)-2-(cyclohexylmethyl)-N-[(1R)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000011
(2R)-2-(cyclohexylmethyl)-N-[(1R)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.1
(2R)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.000012
(2R)-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxo-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)butyl]butanamide
-
-
0.000031
(2R)-2-(cyclopentylmethyl)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000038
(2R)-2-(cyclopentylmethyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.024
(2R)-2-benzyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.024 mM
0.000408
(2R)-4-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)pentanamide
-
-
0.00006
(2R)-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)-N-[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.00007
(2R)-5-dimethyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-2-(2-morpholin-4-yl-2-oxoethyl)hexanamide
-
-
0.000014
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-2-(2-morpholin-4-yl-2-oxoethyl)-5-phenylpentanamide
-
-
0.000027
(2R)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-(2-phenylethyl)butanamide
-
-
0.000021
(2S)-2-(4-chlorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000024
(2S)-2-(4-fluorophenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000105
(2S)-2-(4-methoxyphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000134
(2S)-2-(4-methylphenyl)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.001368
(2S)-2-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000019
(2S)-3-cyclohexyl-1-(morpholin-4-yl)-1-oxopropan-2-yl [(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]carbamate
-
-
0.000261
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-1-phenyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]butanamide
-
-
0.000037
(2S)-4-morpholin-4-yl-4-oxo-2-phenyl-N-[(1S)-3-phenyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]butanamide
-
-
0.0156
(2S)-4-morpholin-4-yl-4-oxo-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000616
(2S)-N-[(1S)-1-cyclopropyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00159
(2S)-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000025
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-phenylbutanamide
-
-
0.1
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[2-(trifluoromethyl)phenyl]butanamide
-
Ki above 0.1 mM
0.01853
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[3-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(1S)-2-methyl-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]-4-morpholin-4-yl-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.000043
(2S)-N-[(2S)-3-methyl-1-[[4-(trifluoromethoxy)phenyl]amino]butan-2-yl]-4-(morpholin-4-yl)-4-oxo-2-[4-(trifluoromethyl)phenyl]butanamide
-
-
0.00844
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.1
(3R)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
Ki above 0.1 mM
0.001721
(3S)-3-(cyclohexylmethyl)-N-[2-[(4-fluorophenyl)amino]ethyl]-4-morpholin-4-yl-4-oxobutanamide
-
-
0.000071
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
-
-
0.00298
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000136
(4'-fluorobiphenyl-3-yl)sulfonyl-(S)-leucyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.0000355
(4'-fluorobiphenyl-4-yl)sulfonyl-(S)-phenylalanyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.00000402
(biphenyl-3-yl)sulfonyl-(S)-leucyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.0000268
(biphenyl-3-yl)sulfonyl-(S)-phenylalanyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.00031
(S)-[1-[1-cyano-pyrrolidin-3(R)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.00097
(S)-[1-[1-cyano-pyrrolidin-3(S)-ylcarbamoyl]-3-methyl-butyl]-carbamic acid benzyl ester
-
pH 6.5, 23°C
0.4377
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]benzoyl)amino]propanoyl]amino)-L-erythro-hex-2-ulose
-
-
0.00003
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000049
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000004
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000021
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000027
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000023
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00011
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000063
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000056
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([4-[(ethylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000053
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose ammoniate (1:1)
-
-
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-fluorophenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[(4-[[(3-methoxyphenyl)sulfonyl]amino]benzoyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000016
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000038
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000001
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000002
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000033
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([3-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(methylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000008
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(phenylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([4-[(pyridin-4-ylsulfonyl)amino]benzoyl]amino)propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.00019
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000057
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000045
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000029
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000083
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000039
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000013
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000009
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000086
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00014
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[4-(methylsulfamoyl)benzoyl]amino]propanoyl]amino]-L-erythro-hex-2-ulose
-
-
0.000031
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-([4-[(cyclohexylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000024
1,4-anhydro-3-[[(2S)-2-([4-[(cyclopropylsulfonyl)amino]benzoyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-erythro-hex-2-ulose
-
-
0.0000056
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000012
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000031
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000034
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000024
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000059
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000008
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000006
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000011
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00018
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.01458
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide]
-
in 0.5 M MES, 2 mM DTT at pH 6.0
146.3
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.05686
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0109
2-[[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl]-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000297
3-chlorophenylsulfonyl-(S)-leucyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.000026
3-chlorophenylsulfonyl-(S)-phenylalanyl-aminocyclopropane-nitrile
pH 6.0, 25°C
0.000057
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000013
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00000064
4-morpholinecarboxamide, N-[(1R)-2-[[(1S)-1-(2-benzoxazolylcarbonyl) propyl] amino]-1-[[(cyclopropylmethyl)-sulfonyl]methyl]-2-oxoethyl]
-
excellent selectivity and activity for cathepsin S over the other cathepsin family members L, K and B
3.39
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000004
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
with Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.001
CLIK60
-
CatS activity in RAW264.7 cells or peritoneal macrophages from C57Bl/6 or LDLr-/-mice is completely repressed
0.01663
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000005
methyl (3R)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.000069
methyl (3S)-3-[[(2R)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanoyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
-
-
0.00278
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.00005
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.000033
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.00011
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
pH 4.5
0.0000059
N-((S)-3-cyclohexyl-1-(((S,E)-1-fluoro-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl)amino)-1-oxopropan-2-yl)isonicotinamide
pH 6.5, 24°C
0.1982
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000055
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
0.00889
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0012
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]benzamide
-
-
0.00042
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1,2-dimethylpropyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.000015
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-(trans-4-methylcyclohexyl)ethyl]thiophene-3-carboxamide
-
-
0.0002
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]benzamide
-
-
0.000018
N-[(1S)-1-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-1-cyclohexylethyl]thiophene-3-carboxamide
-
-
0.00042
N-[(2S)-2-[1-[(1S)-1-cyanopentyl]-1H-1,2,3-triazol-4-yl]-3-methylbutan-2-yl]thiophene-3-carboxamide
-
-
0.000009
N-[(2S)-3-methyl-2-[1-[(2S)-1-oxohexan-2-yl]-1H-1,2,3-triazol-4-yl]butan-2-yl]thiophene-3-carboxamide
-
-
0.01948
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.01527
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.000068
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(3-methylbenzoyl)-L-leucinamide
-
-
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(2S)-1-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)propan-2-yl]-L-alaninamide
-
-
0.025
o-aminobenzoic acid-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.02
o-aminobenzoic acid-Val-Leu-Phe-Glu-Lys-Gln-N-(2,4-dinitrophenyl)ethylendiamine
-
substrate N-benzyloxycarbonyl-L-Phe-Arg-7-amido-4-methylcoumarin
0.00000009
phenyl (1E,3S)-3-[[3-cyclohexyl-N-(morpholine-4-carbonyl)-L-alanyl]amino]-1-fluoro-5-phenylpent-1-ene-1-sulfonate
pH 6.5, 24°C
0.000009
phenyl (1E,3S)-3-[[3-cyclohexyl-N-(phenylcarbamoyl)-L-alanyl]amino]-1-fluoro-5-phenylpent-1-ene-1-sulfonate
pH 6.5, 24°C
0.0000008 - 0.0000079
phenyl (S,E)-1-fluoro-3-((S)-2-(isonicotinamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
0.0000009
phenyl (S,E)-1-fluoro-3-((S)-2-(morpholine-4-carboxamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
pH 6.5, 24°C
0.02817
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile
-
in 0.5 M MES, 2 mM DTT at pH 6.0
0.0000096
[[2',3'-difluoro-4'-(2-methylpropyl)biphenyl-2-yl]oxy]acetaldehyde
-
-
0.0000025
cathepsin S propeptide
-
using benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin as a substrate
-
0.0000008
phenyl (S,E)-1-fluoro-3-((S)-2-(isonicotinamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
pH 6.5, 24°C
0.0000079
phenyl (S,E)-1-fluoro-3-((S)-2-(isonicotinamido)-3-phenylpropanamido)-5-phenylpent-1-ene-1-sulfonate
pH 6.5, 24°C
additional information
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
value above 0.01
additional information
additional information
-
Ki-value for wild-type cystatin C, and the mutant cystatins V10F, V10W, V10R, and L9W are below 0.01 nM
-
additional information
additional information
-
Ki-values above 0.15 mM: 1-iminomethyl-(D)-Pro-Leu benzyl ester, 1-formyl-(D)-Pro-Leu benzyl ester
-
additional information
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
value below 0.0000001
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000395
(2R)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0001
(2R)-2-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)-2-phenylethanol
Homo sapiens
-
-
0.00603
(2R)-2-[(4-bromobenzene-1-sulfonyl)amino]-3-phenylpropyl N-benzoyl-D-phenylalaninate
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.001991
(2R)-2-[4'-(1-azabicyclo[2.2.2]oct-4-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1991 nM
0.00834
(2R)-2-[4'-(4-tert-butylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 8340 nM
0.001427
(2R)-2-[4'-[1-(2-amino-2-methylpropyl)piperidin-4-yl]-1,1'-biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1427 nM
0.00008
(2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-N-(1-cyanocyclopropyl)-3-(methylsulfanyl)propanamide
Homo sapiens
-
-
0.000135
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.01
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxy-2-methylpropyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000609
(2R)-N-(cyanomethyl)-2-[4'-[4-(2-hydroxyethyl)-1-piperazinyl][1,1'-biphenyl]-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50: 609 nM
0.00201
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 2010 nM
0.01
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1H-tetraazol-5-yl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.003931
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3931 nM
0.001365
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-pyrimidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1365 nM
0.002364
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-[4-(2-oxopropyl)-piperazin-1-yl]-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 2364 nM
0.000037
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000062
(2R)-N-[(1R)-2-[(4-chlorobenzyl)oxy]-1-cyanoethyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000658
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 658 nM
0.000018 - 0.000053
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
0.000171
(2R)-N-[(1S)-1-cyano-3-phenylpropyl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000207
(2R)-N-[(3R)-1-benzyl-3-cyanopiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000066
(2R)-N-[(3R)-3-cyano-1-(1-methylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000039
(2R)-N-[(3R)-3-cyano-1-(2-methylpropyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(2-phenylethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000022
(2R)-N-[(3R)-3-cyano-1-(cyclopropylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000042
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(2,3-dihydro-1H-inden-2-ylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000023
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000063
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclopentylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000047
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000014
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-(morpholin-4-yl)-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.0000019
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-(1,2,3,4-tetrahydronaphthalen-2-ylmethyl)butanamide
Homo sapiens
-
-
0.003136
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-4-morpholin-4-yl-4-oxo-2-[(4-phenylcyclohexyl)methyl]butanamide
Homo sapiens
-
-
0.000075
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000251
(2R)-N-[(3R)-3-cyano-1-methylpiperidin-4-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000155
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
-
0.000141
(2R)-N-[(3R)-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000029
(2R)-N-[(3S)-1-benzyl-3-cyanopyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.000041
(2R)-N-[(3S)-3-cyano-1-(cyclohexylmethyl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
-
0.00003
(2S)-1-(4,4'-bipiperidin-1-yl)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000245
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxypropan-1-one
Homo sapiens
-
-
0.000058
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00035
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propan-2-ylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.0003
(2S)-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(propylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
(2S)-1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(1'-methyl-4,4'-bipiperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000658
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000018 - 0.000053
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
0.00033
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(furan-2-yl)methanone
Homo sapiens
-
-
0.00014
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(pyridin-2-yl)methanone
Homo sapiens
-
-
0.00031
(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(tetrahydrofuran-2-yl)methanone
Homo sapiens
-
-
0.000006
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000042
(3R)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 42 nM
0.000012
(3S)-3-[(N-1,3-benzoxazol-2-yl-3-cyclohexyl-L-alanyl)amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 12 nM
0.000027
(3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoic acid
Homo sapiens
-
IC50: 27 nM
0.000049
(3S)-tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 49 nM
0.0000043
(4R)-1-acetyl-N-[(2R)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[(2S)-1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxo-3-phenylpropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(ethylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000207
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfanyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000837
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfinyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.001
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-phenoxy-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000023
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(2-chlorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[(4-fluorophenyl)sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-[[4-(1H-pyrazol-1-yl)phenyl]sulfonyl]-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000181
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-1-oxopropan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000246
(4R)-1-acetyl-N-[1-(1,3-benzoxazol-2-yl)-3-methyl-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000024
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-methylpropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000454
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(2-oxopropyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000011
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(3-methoxypropanoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000002
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(4-chlorobenzoyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000041
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(biphenyl-4-ylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-(methylsulfinyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-benzoyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000124
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-1-phenyl-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-3-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000033
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyridin-4-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(pyrrolidin-1-ylcarbonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000027
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-(trifluoroacetyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000031
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-1-propanoyl-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.000156
(4R)-N-[1-(1,3-benzoxazol-2-yl)-1-oxobutan-2-yl]-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000366
(4R)-N-[2-(1,3-benzoxazol-2-yl)-2-oxoethyl]-1-(cyclohexylcarbonyl)-4-(phenylsulfonyl)-L-prolinamide
Homo sapiens
pH and temperature not specified in the publication
0.01
(4S)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]hexanamide
Homo sapiens
-
IC50 above 0.01 mM
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002 - 0.000015
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0017
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00031
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00015
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.000062
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.0014
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
Homo sapiens
-
effect of R1 substituent on the Ii p10 cell assay at 37°C
0.00001
1-(1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidin-1-yl)ethanone
Homo sapiens
-
-
0.00035
1-(1-[(2R)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 350 nM
0.00019
1-(1-[(2S)-3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 190 nM
0.00001
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 10 nM
0.00005
1-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00005
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00014
1-(1-[3-[3-(4-bromophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00006
1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.0002
1-(1-[3-[3-[3-[(2-hydroxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00022
1-(1-[3-[5-(methylsulfonyl)-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)pyrrolidin-2-one
Homo sapiens
-
-
0.00008
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00011
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5,6-dichloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methoxy-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00021
1-(1-[3-[5-acetyl-3-(4-bromophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-7-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 210 nM
0.00013
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.00009
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 90 nM
0.00014
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 140 nM
0.00031
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 310 nM
0.0005
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 500 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-3-tert-butyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0001
1-(1-[3-[5-acetyl-3-(4-chloro-3-methylphenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-5-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00046
1-(1-[3-[5-acetyl-3-(4-chlorophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 460 nM
0.00012
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 120 nM
0.00023
1-(1-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-6-fluoro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 230 nM
0.000565
1-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperidin-4-ol
Homo sapiens
-
-
0.00022
1-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-hydroxyethanone
Homo sapiens
-
-
0.00029
1-(4-cyclopropylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00115
1-(4-methylpiperazin-1-yl)-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.0001
1-(ethenylideneamino)-3-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.0000002 - 0.000044
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0000002 - 0.000066
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
0.0000141
1-methyl-6-[4-(piperidin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000316
1-methyl-6-[4-(piperidin-4-yloxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
1-methyl-6-[4-(pyridin-2-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000126
1-methyl-6-[4-(pyridin-3-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
1-methyl-6-[4-(pyridin-4-ylmethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[(3-oxopiperazin-1-yl)oxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
1-methyl-6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
1-methyl-6-[4-[2-(6-methylpyridin-2-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000083
1-methyl-6-[4-[2-(piperidin-4-yl)ethoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000095
1-methyl-6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
1-methyl-6-[4-[3-(pyrrolidin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000627
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-([[1-(4-fluorophenyl)-1-methylethoxy]sulfinyl]methyl)-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(2-methylpropoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000004
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(4-fluorophenoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000005 - 0.000759
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
0.0000003 - 0.000021
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000005
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)methyl]-4-fluorobenzene
Homo sapiens
-
-
0.00004
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00201
1-[1-(3-[3-[3-([2-[benzyl(methyl)amino]ethyl]sulfanyl)-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0001
1-[1-(3-[3-[3-[[2-(2-methylpyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00009
1-[1-(3-[3-[3-[[2-(3-hydroxypyrrolidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00034
1-[1-(3-[3-[3-[[2-(4-hydroxypiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00074
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00106
1-[1-(3-[3-[3-[[2-(4-methylpiperazin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00021
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00011
1-[1-(3-[3-[3-[[2-(4-methylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00016
1-[1-(3-[3-[3-[[2-(4-tert-butylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0007
1-[1-(3-[3-[3-[[2-(benzylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00128
1-[1-(3-[3-[3-[[2-(dimethylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0008
1-[1-(3-[3-[3-[[2-(methylamino)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00012
1-[1-(3-[3-[3-[[3-hydroxy-2-oxo-3-(piperidin-4-yl)propyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.0002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(4-phenylpiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00002
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00027
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.000055
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(octahydroisoquinolin-2(1H)-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00017
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00041
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00007
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00006
1-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-oxo-2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]pyrrolidin-2-one
Homo sapiens
-
-
0.00005
1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00013
1-[1-(3-[5-acetyl-3-[4-(trifluoromethoxy)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 130 nM
0.0001
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 100 nM
0.00011
1-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-3-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 110 nM
0.00018
1-[1-[(2R)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 180 nM
0.0002
1-[1-[(2S)-3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl]-6-chloro-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 200 nM
0.000032
1-[2-(dimethylamino)ethyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000027
1-[3-(dimethylamino)propyl]-6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00113
1-[3-[3-[(2-aminoethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00011
1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxamide
Homo sapiens
-
-
0.00031
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-(methylsulfanyl)ethanone
Homo sapiens
-
-
0.000235
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-hydroxyethanone
Homo sapiens
-
-
0.00047
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-methoxyethanone
Homo sapiens
-
-
0.000385
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.00069
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]propan-1-one
Homo sapiens
-
-
0.0096
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000149
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.009
1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-5-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00005
1-[3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropyl]-3-(4-iodophenyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
IC50: 50 nM
0.000058
1-[3-[4-(5-methyl-1H-indol-3-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00014
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.00038
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperazin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00008
1-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.001035
1-[4-(2-[[5-[1-[2-hydroxy-3-(piperidin-1-yl)propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]ethyl)piperazin-1-yl]ethanone
Homo sapiens
-
-
0.00071
1-[4-(dimethylamino)piperidin-1-yl]-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propan-2-ol
Homo sapiens
-
-
0.00008
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(3,4-dichlorobenzyl)methanamine
Homo sapiens
-
-
0.00023
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methoxybenzyl)methanamine
Homo sapiens
-
-
0.00035
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-(4-methylbenzyl)methanamine
Homo sapiens
-
-
0.0013
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00049
1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00042
1-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000325
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(morpholin-4-yl)propan-2-ol
Homo sapiens
-
-
0.000204
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.000595
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(propylamino)propan-2-ol
Homo sapiens
-
-
0.000335
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(pyrrolidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.00001
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyridin-2-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000218
1-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propan-2-ol
Homo sapiens
-
-
0.000712
1-[5-(methylsulfonyl)-3-[3-[[2-(pyrrolidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-3-(piperidin-1-yl)propan-2-ol
Homo sapiens
-
-
0.02
2,3,4,5,6-pentafluoro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 0.020 mM
0.001578
2-(1,1'-biphenyl-3-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 1578 nM
0.003343
2-(1,1'-biphenyl-4-yl)-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: 3343 nM
0.00028
2-(3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)-2-oxoethyl acetate
Homo sapiens
-
-
0.00012
2-(4-[3-[5-acetyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazin-1-yl)benzonitrile
Homo sapiens
-
IC50: 120 nM
0.0003
2-([5-[1-[2-hydroxy-3-[(3S)-3-methylmorpholin-4-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00002
2-([5-[1-[2-hydroxy-3-[4-(3-methyl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(piperidin-1-yl)ethanone
Homo sapiens
-
-
0.000001
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3R)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.000007
2-([5-[1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-[(3S)-3-hydroxypyrrolidin-1-yl]ethanone
Homo sapiens
-
-
0.00004
2-([5-[1-[2-hydroxy-3-[4-(pyrrolidin-1-ylcarbonyl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00001
2-([5-[1-[3-[4-(2-fluorophenyl)piperazin-1-yl]-2-hydroxypropyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.000005
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-1,3-thiazolidine
Homo sapiens
-
-
0.0000013
2-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)-2,3-dihydro-1,3-benzothiazole
Homo sapiens
-
-
0.00081
2-amino-1-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]ethanone
Homo sapiens
-
-
0.000035
2-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 35 nM
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.000031
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000026
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000032
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000093
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000024
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000005
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000003
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
0.000003
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000004
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000003
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00001
2-hydroxy-1-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)ethanone
Homo sapiens
-
-
0.00096
2-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)sulfanyl]ethanol
Homo sapiens
-
-
0.0000007
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-1,3-difluorobenzene
Homo sapiens
-
-
0.0000018
2-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]biphenyl
Homo sapiens
-
-
0.00001
2-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]benzonitrile
Homo sapiens
-
-
0.00006
2-[3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
2-[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]-2-oxoacetamide
Homo sapiens
-
-
0.0000045
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-(2-hydroxyethyl)-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9-ethyl-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000039
2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
2-[4-methoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
2-[5-carbamoyl-3-(4-iodophenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-1-[[4-(2-cyanophenyl)piperazin-1-yl]methyl]ethyl carbamate
Homo sapiens
-
IC50: 20 nM
0.000016
2-[N-(3-chlorophenyl)-L-leucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000035
2-[N-(4-fluorophenyl)-L-valyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.000019
2-[N-[3-(trifluoromethyl)phenyl]-L-isoleucyl]tetrahydropyridazine-1(2H)-carbonitrile
Homo sapiens
-
-
0.00019
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00011
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00006
2-[[5-(1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00015
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-hydroxypropan-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00002
2-[[5-(5-acetyl-1-[2-hydroxy-3-[4-(2-methoxyphenyl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(morpholin-4-yl)ethanone
Homo sapiens
-
-
0.00025
2-[[5-(5-ethyl-1-[2-hydroxy-3-[4-(pyridin-2-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.00018
2-[[5-[5-acetyl-1-[2-hydroxy-3-(4-methylpiperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl]-1-(pyrrolidin-1-yl)ethanone
Homo sapiens
-
-
0.001373
3'-[1-[[(cyanomethy)amino]carbonyl]-3-methylbutyl]-1,1'biphenyl-4-carboxamide
Homo sapiens
-
IC50: 1373 nM
0.0079
3-(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)prop-2-yn-1-ol
Homo sapiens
-
-
0.0074
3-(4-chloro-3-ethynylphenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00087
3-(4-chloro-3-[[2-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-(4-chloro-3-[[3-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-(4-chloro-3-[[4-(trifluoromethyl)phenyl]ethynyl]phenyl)-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000033
3-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 33 nM
0.000005
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-(naphthalen-2-ylacetyl)-L-alaninamide
Homo sapiens
-
IC50: 5.0 nM
0.0000033
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-([5-[3-(trifluoromethyl)phenyl]furan-2-yl]acetyl)-L-alaninamide
Homo sapiens
-
IC50: 3.3 nM
0.000008
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 8.0 nM
0.000004
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-morpholin-4-ylphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 4.0 nM
0.000017
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(4-phenoxyphenyl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 17 nM
0.000034
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(5-methyl-1-phenyl-1H-pyrazol-4-yl)acetyl]-L-alaninamide
Homo sapiens
-
IC50: 34 nM
0.000026
3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[[4-(1H-1,2,4-triazol-1-yl)phenyl]acetyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000197
3-cyclohexyl-N2-(5-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 197 nM
0.000043
3-cyclohexyl-N2-(6-fluoro-1,3-benzoxazol-2-yl)-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 43 nM
0.000002
3-cyclohexyl-N2-([4-[(4,6-dimethylpyrimidin-2-yl)amino]phenyl]acetyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.0 nM
0.00003
3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,5-dimethyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.00165
3-[3-(benzylsulfanyl)-4-chlorophenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000235
3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxamide
Homo sapiens
-
-
0.0083
3-[4-chloro-3-(4-methylpent-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0067
3-[4-chloro-3-(cyclohexylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.011
3-[4-chloro-3-(hept-1-yn-1-yl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00061
3-[4-chloro-3-(phenylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0036
3-[4-chloro-3-(propylsulfanyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00079
3-[4-chloro-3-(thiophen-2-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0015
3-[4-chloro-3-(thiophen-3-ylethynyl)phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00072
3-[4-chloro-3-[(2-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00055
3-[4-chloro-3-[(2-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0011
3-[4-chloro-3-[(2-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0006
3-[4-chloro-3-[(2-phenoxyethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00147
3-[4-chloro-3-[(2-phenylethyl)sulfanyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00032
3-[4-chloro-3-[(3,4-dichlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0007
3-[4-chloro-3-[(3-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.0002 - 0.00069
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
0.00048
3-[4-chloro-3-[(4-methoxyphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00028
3-[4-chloro-3-[(4-methylphenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000007
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000447
4-(3-acetylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000174
4-(3-bromophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000148
4-(3-chlorophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
4-(3-cyclobutylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
4-(3-cyclopropylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000083
4-(3-ethylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00095
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000191
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000123
4-(acetylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 123 nM
0.00053
4-(dimethylamino)-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.0041
4-bromo-N-[(2R)-1-[(2R)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]benzene-1-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000016
4-chloro-N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 16 nM
0.00036
4-fluoro-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00039
4-hydroxy-N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.000093
4-methyl-N-[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]-N2-(morpholin-4-ylcarbonyl)-L-leucinamide
Rattus norvegicus
-
-
0.00022
4-methyl-N2-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-leucinamide
Rattus norvegicus
-
-
0.01
4-phenyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00041
4-propyl-6-(3-propylphenyl)pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000115
4-propyl-6-[3-(trifluoromethoxy)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000032
4-propyl-6-[4-(trifluoromethoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001259
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00043
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]aniline
Homo sapiens
-
-
0.00051
4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzoic acid
Homo sapiens
-
-
0.001925
4-[1-(2-hydroxy-3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00001
4-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(morpholin-4-yl)-2-oxoethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0018
4-[1-(3-[3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00003
4-[1-(3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.00012
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0001
4-[1-(3-[5-acetyl-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000826
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.0009
4-[1-(3-[5-tert-butoxy-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000022
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.001047
4-[2-chloro-5-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000051
4-[3,5-bis(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000224
4-[3-(2-methylpropyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000093
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000195
4-[3-(propan-2-yl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000045
4-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
4-[4-(propan-2-yloxy)-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000028
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
4-[4-ethoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
4-[4-fluoro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
4-[4-methoxy-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[4-methyl-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000013
4-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00074
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[(2-phenoxyethyl)sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00081
5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000058
5-(methylsulfonyl)-1-[3-[4-(1H-pyrrolo[3,2-c]pyridin-3-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00038
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(piperidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00052
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-(pyrrolidin-1-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00056
5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[3-[4-(pyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.000002
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00015
5-chloro-3-(1-[3-[3-(3,4-dichlorophenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl]piperidin-4-yl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 150 nM
0.00008
5-chloro-3-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 80 nM
0.00045
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000033
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000099
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000007
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00032
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00019
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000019
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, pyrrolopyrimidine inhibitor by modification of the P2 moieties
0.00005
6-chloro-1-(1-[3-[3-(4-chloro-3-methylphenyl)-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidin-4-yl)-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 50 nM
0.00006
6-chloro-1-[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 60 nM
0.00003
6-chloro-1-[1-(3-[5-(methylsulfonyl)-3-[4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
IC50: 30 nM
0.001047
6-[3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002884
6-[3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000071
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000145
6-[4-(2-hydroxyethoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000024
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000063
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000155
6-[4-(3-hydroxypropoxy)-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0002
6-[4-(3-oxopropyl)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000105
6-[4-(ethylamino)-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000037
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[2-(morpholin-4-yl)ethyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1-[3-(morpholin-4-yl)propyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000025
6-[4-ethoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00166
6-[4-ethoxy-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000339
6-[4-methoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000676
6-[4-phenoxy-3-(trifluoromethyl)phenyl]-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
6-[4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000209
6-[4-[2-(dimethylamino)ethoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000031
6-[4-[3-(2-ethyl-1H-imidazol-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000072
6-[4-[3-(4-ethylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000058
6-[4-[3-(4-methylpiperazin-1-yl)propoxy]-3-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000041
6-[4-[3-(dimethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000015
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000015
6-[[4-(1-acetylpiperidine-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012 - 0.000014
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009 - 0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000005
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001 - 0.000028
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000017
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000009
6-[[4-(4-acetylpiperazine-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.00044
7-(2-cyclohexylethyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000011
7-(2-cyclohexylethyl)-6-[(pyridine-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
7-(2-cyclohexylethyl)-6-[(pyridine-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000052
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00046
7-tert-butyl-6-(4-chlorobenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000069
9-[3-(dimethylamino)propyl]-2-[4-ethoxy-3-(trifluoromethyl)phenyl]-9H-purine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00004
benzyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
42
benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
Homo sapiens
at pH 6.5 and 37°C
0.000071
ethyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 71 nM
0.0001
JNJ 10329670
Homo sapiens
-
competitive, reversible inhibition, 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl derivative, IC50: 100 nM
0.0001
methyl (2R)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.01
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-4-[(1S)-1-[(1R)-2-[(1-cyanocyclopropyl)amino]-1-(methoxysulfinyl)methyl]-2-oxoethyl]amino)-2,2,2-trifluoroethyl]-4'-fluorobiphenyl
Homo sapiens
-
-
0.002173
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfenate
Homo sapiens
-
-
0.00000016 - 0.001051
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
0.0000064
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(3-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.000096 - 0.01
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
0.0000006 - 0.000426
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
0.0000025
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.00012
methyl (2S)-([4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]amino)(phenyl)ethanoate
Homo sapiens
-
-
0.00004
methyl (3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-1-[3-(morpholin-4-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl)(oxo)acetate
Homo sapiens
-
-
0.000005
methyl (3S)-3-[[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino]-4-[[4-(trifluoromethoxy)phenyl]amino]butane-1-sulfinate
Rattus norvegicus
-
-
0.0017
methyl 1-[2-hydroxy-3-(4-quinolin-4-ylpiperazin-1-yl)propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000163
methyl 1-[2-hydroxy-3-[4-(2-oxo-2,3-dihydro-4,1-benzoxazepin-1(5H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000088
methyl 1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000023
methyl 1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000028
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00008
methyl 1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00002
methyl 1-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperidine-4-carboxylate
Homo sapiens
-
-
0.000023
methyl 1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000145
methyl 1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00003
methyl 1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000013
methyl 1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000016
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-3-[4-(trifluoromethyl)phenyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000043
methyl 2-[[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-fluorophenyl)amino]ethyl]amino)-2-oxoethyl]amino]-1,3-benzoxazole-6-carboxylate
Homo sapiens
-
IC50: 43 nM
0.000133
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000065
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000032
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000068
methyl 3-(4-bromophenyl)-1-[2-hydroxy-3-[4-(3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.001775
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroisoquinolin-2(1H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000322
methyl 3-(4-bromophenyl)-1-[3-[4-(3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00006
methyl 3-(4-bromophenyl)-1-[3-[4-(3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.0017
methyl 3-(4-bromophenyl)-1-[3-[4-(5-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000075
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2,2-dioxido-3,4-dihydro-1H-2,1,3-benzothiadiazin-1-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000033
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinazolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000018
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000048
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]-2-hydroxypropyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.00013
methyl 3-(4-bromophenyl)-1-[3-[4-(6-chloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)piperidin-1-yl]propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-sulfinate
Homo sapiens
-
-
0.000265
methyl 4'-[(1S)-1-([(1S)-1-[(1-cyanocyclopropyl)carbamoyl]pentyl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
Homo sapiens
-
-
565
morpholine-4-carboxylic acid [1-[1S-(N-benzoyl-hydrazinomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 565 mM
0.011
morpholine-4-carboxylic acid [1R-(1S-cyano-3-phenyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.011 mM
0.000387
morpholine-4-carboxylic acid [1S-(1R-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 387 nM
0.107
morpholine-4-carboxylic acid [1S-(1S-cyano-2,2-dimethylpropylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 0.107 mM
0.0014
morpholine-4-carboxylic acid [1S-(1S-cyano-2-methyl-propylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 1400 nM
0.00013
morpholine-4-carboxylic acid [1S-(1S-cyano-2-phenylethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 130 nM
0.076
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenyl-propylcarbamoyl)-1,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 0.076 mM
5
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-cyclohexyl-ethyl]-amide
Homo sapiens
-
IC50: 5 mM
0.006
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-methyl-propyl]-amide
Homo sapiens
-
IC50: 0.006 mM
173
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-2-phenyl-ethyl]-amide
Homo sapiens
-
IC50: 173 mM
0.000023
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-3,3-dimethyl-butyl]-amide
Homo sapiens
-
IC50: 23 nM
0.000084
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-cyclohexyl-R-methyl]-amide
Homo sapiens
-
IC50: 84 nM
0.134
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-ethyl]-amide
Homo sapiens
-
IC50: 0.134 mM
0.000041
morpholine-4-carboxylic acid [1S-(1S-cyano-3-phenylpropylcarbamoyl)-pentyl]-amide
Homo sapiens
-
IC50: 41 nM
0.000082
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 82 nM
0.000056
morpholine-4-carboxylic acid [1S-(1S-cyanobutylcarbamoyl)-3-methylpentyl]amide
Homo sapiens
-
IC50: 56 nM
0.000142
morpholine-4-carboxylic acid [1S-(1S-cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 142 nM
0.000019
morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 19 nM
0.000124
morpholine-4-carboxylic acid [1S-(cyanomethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50: 124 nM
0.000114
morpholine-4-carboxylic acid [1S-[(1-cyano-1-methyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 114 nM
0.000051
morpholine-4-carboxylic acid [1S-[(cyano-phenyl-S-methyl)carbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 51 nM
0.000011
morpholine-4-carboxylic acid [1S-[1S-(benzoyl-hydrazonomethyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 11 nM
0.000056
morpholine-4-carboxylic acid [1S-[1S-cyano-2-(3,4-dichlorophenyl)ethylcarbamoyl]-3-methylbutyl]amide
Homo sapiens
-
IC50: 56 nM
0.000007
morpholine-4-carboxylic acid [1S-[1S-[(2-hydroxy-benzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 7 nM
0.000035
morpholine-4-carboxylic acid [1S-[1S-[(4-hydroxybenzoyl)-hydrazonomethyl]-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
Homo sapiens
-
IC50: 35 nM
0.097
morpholine-4-carboxylic acid [3-methyl-1S-(1-prop-2-ynylcarbamoyl)butyl]amide
Homo sapiens
-
IC50: 0.097 mM
0.339
morpholine-4-carboxylic acid [3-methyl-1S-(1R-methyl-3-phenylpropylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.339 mM
0.028
morpholine-4-carboxylic acid [3-methyl-1S-(3-phenyl-propylcarbamoyl)butyl]amide
Homo sapiens
-
IC50 above 0.028 mM
0.00052
N,N-dimethyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000729
N-(1-cyanocyclopropyl)-3-(methylsulfinyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.00001
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4'-fluorobiphenyl-4-yl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000018
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000025
N-(1-cyanocyclopropyl)-3-(methylsulfonyl)-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000002
N-(1-cyanocyclopropyl)-3-[(3,4-dichlorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.0000005
N-(1-cyanocyclopropyl)-3-[(4-fluorobenzyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-phenylethyl]-L-alaninamide
Homo sapiens
-
-
0.0000004
N-(1-cyanocyclopropyl)-3-[(4-fluorophenyl)sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000627
N-(1-cyanocyclopropyl)-3-[[2-(4-fluorophenyl)propan-2-yl]sulfonyl]-N2-[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]-L-alaninamide
Homo sapiens
-
-
0.000265
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000002
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00014
N-(4-chlorobenzyl)-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
-
0.000008
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000012
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000922
N-(cyanomethyl)-2-[3-(1H-indol-5-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 922 nM
0.001257
N-(cyanomethyl)-2-[3-(1H-indol-6-yl)phenyl]-4-methylpentanamide
Homo sapiens
-
IC50: 1257 nM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]-3-phenylpropanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]acetamide
Homo sapiens
-
IC50 above 0.01 mM
0.00231
N-(cyanomethyl)-3-cyclobutyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 2310 nM
0.006597
N-(cyanomethyl)-3-cyclopropyl-2-[4'-(4-methylpiperazin-1-yl)-1,1'-biphenyl-3-yl]propanamide
Homo sapiens
-
IC50: 6597 nM
0.01
N-(cyanomethyl)-4-methyl-2-(2-phenyl-1,3-thiazol-4-yl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(3'-piperazin-1-yl-1,1'-biphenyl-3-yl)pentanamide methanesulfonate
Homo sapiens
-
IC50 above 0.01 mM
0.00000001
N-(cyanomethyl)-4-methyl-2-(3-pyridin-3-ylphenyl)-pentanamide
Homo sapiens
-
IC50 above 0.01 nM
0.001748
N-(cyanomethyl)-4-methyl-2-(3-pyridin-4-ylphenyl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50: 1748 nM
0.01
N-(cyanomethyl)-4-methyl-2-(3-pyrimidin-5-ylphenyl)pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.01
N-(cyanomethyl)-4-methyl-2-(5-phenylpyridin-3-yl)-pentanamide trifluoroacetate
Homo sapiens
-
IC50 above 0.01 mM
0.000521
N-(cyanomethyl)-4-methyl-2-[2'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 521 nM
0.003368
N-(cyanomethyl)-4-methyl-2-[2'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 3368 nM
0.01
N-(cyanomethyl)-4-methyl-2-[3'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50 above 0.01 mM
0.000652
N-(cyanomethyl)-4-methyl-2-[4'-(1,2,3,6-tetrahydro-4-pyridinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 652 nM
0.001245
N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1245 nM
0.001695
N-(cyanomethyl)-4-methyl-2-[4'-(4-methyl-1-piperazinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1695 nM
0.009422
N-(cyanomethyl)-4-methyl-2-[4'-(4-morpholinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 9422 nM
0.001421
N-(cyanomethyl)-4-methyl-2-[4'-(4-piperidinyl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC50: 1421 nM
0.006623
N-(cyanomethyl)-4-methyl-2-[4'-(methylsulfonyl)-1,1'-biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: 6623 nM
0.0006
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]-N-methylmethanamine
Homo sapiens
-
-
0.00042
N-benzyl-1-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]phenyl]methanamine
Homo sapiens
-
-
0.00037
N-benzyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000001
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00115
N-methyl-2-([5-[5-(methylsulfonyl)-1-[3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)acetamide
Homo sapiens
-
-
0.000021
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000029
N-[(1S)-1-(1H-indol-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 29 nM
0.000034
N-[(1S)-1-(biphenyl-4-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 34 nM
0.000062
N-[(1S)-1-(cyclohexylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 62 nM
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
0.000099
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[[(1S)-1-([[4-(trifluoromethoxy)phenyl]amino]methyl)propyl]amino]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
0.000111
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000087
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000049
N-[(1S)-1-(cyclopentylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.02
N-[(1S)-1-(furan-2-ylmethyl)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.020 mM
0.000023
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000023
N-[(1S)-1-cyclohexyl-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 23 nM
0.000016
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-1-(naphthalen-2-ylmethyl)-2-oxoethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 16 nM
0.065
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(1,3-thiazol-5-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 0.065 mM
0.003707
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-3-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 3707 nM
0.006769
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-(pyridin-4-ylmethyl)ethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 6769 nM
0.000285
N-[(1S)-2-([2-[(4-methoxyphenyl)amino]ethyl]amino)-2-oxo-1-phenylethyl]-3-methylbenzamide
Homo sapiens
-
IC50: 285 nM
0.000012
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfanyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000032
N-[(1S)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxo-1-[(2-phenylethyl)sulfonyl]ethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000038
N-[(1S)-3-cyclohexyl-1-([2-[(4-methoxyphenyl)amino]ethyl]carbamoyl)propyl]-3-methylbenzamide
Homo sapiens
-
IC50: 38 nM
0.0075
N-[(2R)-1-[(2S)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]-4-(trifluoromethyl)benzene-1-sulfonamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00547
N-[(2S)-1-[(2S)-3-[4-(2-cyanophenyl)piperazin-1-yl]-2-hydroxypropoxy]-3-phenylpropan-2-yl]pyridine-4-carboxamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000055
N-[(2S)-1-[[(1R)-2-(benzyloxy)-1-cyanoethyl]amino]-3-cyclohexyl-1-oxopropan-2-yl]morpholine-4-carboxamide
Homo sapiens
-
pH 6.5, 37°C
0.0000044
N-[(3S)-4-benzyloxy-3-[[[1-[(4-morpholinylcarbonyl)-amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.0000019
N-[(3S)-4-benzyloxy-3-[[[2-[(3-nitrobenzoyl)amino]cyclohexyl-L-alanyl]carbonyl]amino]-1,2-dioxobutyl]glycine ethyl ester
Homo sapiens
-
pH 6.5, 37°C
0.00013
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]-2-phenylacetamide
Homo sapiens
-
-
0.00038
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]benzamide
Homo sapiens
-
-
0.00042
N-[2-([5-[1-[2-hydroxy-3-[4-(2-oxopyrrolidin-1-yl)piperidin-1-yl]propyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]-2-(trifluoromethyl)phenyl]sulfanyl)ethyl]piperidine-3-carboxamide
Homo sapiens
-
-
0.000046
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 46 nM
0.000027
N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 27 nM
0.000062
N-[2-[(4-methoxyphenyl)amino]ethyl]-N2-[(3-methylphenyl)carbonyl]-L-leucinamide
Homo sapiens
-
IC50: 62 nM
0.000019
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-4-(trifluoromethyl)-L-phenylalaninamide
Homo sapiens
-
IC50: 19 nM
0.000029
N-[2-[(4-methoxyphenyl)amino]ethyl]-Na-[(3-methylphenyl)carbonyl]-L-phenylalaninamide
Homo sapiens
-
IC50: 29 nM
0.000066
N-[2-[(4-methoxyphenyl)amino]ethyl]-O-methyl-Na-[(3-methylphenyl)carbonyl]-L-tyrosinamide
Homo sapiens
-
IC50: 66 nM
0.003236
N-[4-(4-cyano-1H-imidazo[4,5-c]pyridin-6-yl)-2-(trifluoromethyl)phenyl]formamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00019
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-1-phenylethanamine
Homo sapiens
-
-
0.00058
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]-2-phenylethanamine
Homo sapiens
-
-
0.00035
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzamide
Homo sapiens
-
-
0.00016
N-[4-[(2-chloro-5-[5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl]phenyl)ethynyl]benzyl]benzenesulfonamide
Homo sapiens
-
-
0.000173
N2-(5-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 173 nM
0.000021
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]-3-(methylsulfonyl)propyl]-L-alaninamide
Homo sapiens
-
IC50: 21 nM
0.000151
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 151 nM
0.000093
N2-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 93 nM
0.000026
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[3-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000011
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-(1-methyl-2-[[4-(methylsulfonyl)phenyl]amino]ethyl)-L-alaninamide
Homo sapiens
-
IC50: 11 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,2-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.000015
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 15 nM
0.0000123
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-2-oxo-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 12.3 nM
0.000003
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-(5-fluoro-3,3-dimethyl-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 3 nM
0.000019
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 19 nM
0.000001
N2-(7-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 1 nM
0.0000029
N2-(biphenyl-3-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 2.9 nM
0.0000091
N2-(biphenyl-4-ylacetyl)-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.1 nM
0.000026
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[(1S)-2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)-1-methylethyl]-L-alaninamide
Homo sapiens
-
IC50: 26 nM
0.000222
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-(5-fluoro-2,3-dihydro-1H-indol-1-yl)ethyl]-L-alaninamide
Homo sapiens
-
IC50: 222 nM
0.000094
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-fluorophenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 94 nM
0.000029
N2-1,3-benzoxazol-2-yl-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 29 nM
0.000005
N2-1,3-benzoxazol-2-yl-N-[(1R)-2-(benzyloxy)-1-[(5-fluoro-2,3-dihydro-1H-indol-1-yl)methyl]ethyl]-3-cyclohexyl-L-alaninamide
Homo sapiens
-
IC50: 5 nM
0.0000074
N2-[(3'-chlorobiphenyl-4-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.4 nM
0.0000094
N2-[(5-chloro-1-benzofuran-2-yl)acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 9.4 nM
0.000049
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-3-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 49 nM
0.000107
N2-[[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 107 nM
0.0000071
N2-[[5-(4-chlorophenyl)furan-2-yl]acetyl]-3-cyclohexyl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-alaninamide
Homo sapiens
-
IC50: 7.1 nM
0.0114
Na-(morpholin-4-ylcarbonyl)-N-(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)-L-phenylalaninamide
Rattus norvegicus
-
-
0.00073
tert-butyl (3S)-3-[[N-(6-chloro-1,3-benzoxazol-2-yl)-3-cyclohexyl-L-alanyl]amino]-4-(5-fluoro-2,3-dihydro-1H-indol-1-yl)butanoate
Homo sapiens
-
IC50: 730 nM
0.00001
tert-butyl 1'-[(2S)-3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]-4,4'-bipiperidine-1-carboxylate
Homo sapiens
-
-
0.001298
tert-butyl 4-[3'-[1-[[(cyanomethyl)amino]carbonyl]-3-methylbutyl]-1,1'-biphenyl-4-yl]piperazine-1-carboxylate
Homo sapiens
-
IC50: 1298 nM
0.00015
tert-butyl 4-[3-[3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]-2-hydroxypropyl]piperazine-1-carboxylate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-1-oxo-3-phenylpropan-2-yl]carbamate
Homo sapiens
-
-
0.000023
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000003
tert-butyl [(2S)-1-(2-cyanopyrazolidin-1-yl)-4-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
-
0.000004
tert-butyl [(2S)-1-(2-cyanotetrahydropyridazin-1(2H)-yl)-3-methyl-1-oxobutan-2-yl]carbamate
Homo sapiens
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
0.000042 - 0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
0.0000006
[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]benzene
Homo sapiens
-
-
0.00009
[1-(2-hydroxy-3-[5-(methylsulfonyl)-3-[3-[[2-(piperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-1-yl]propyl)piperidin-4-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000042
[1S-(1S-cyano-3-phenylpropylcarbamoyl)-3-methylbutyl]-amide
Homo sapiens
-
IC50: 42 nM
0.02
[1S-(2-cyano-1S-phenethyl-ethylcarbamoyl)-3-methylbutyl]amide
Homo sapiens
-
IC50 above 0.02 mM
0.000205
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](1H-1,2,4-triazol-3-yl)methanone
Homo sapiens
-
-
0.00119
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](pyrrolidin-1-yl)methanone
Homo sapiens
-
-
0.000355
[3-[3-[[2-(4-fluoropiperidin-1-yl)ethyl]sulfanyl]-4-(trifluoromethyl)phenyl]-1-[(2S)-2-hydroxy-3-(piperidin-1-yl)propyl]-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl](thiophen-2-yl)methanone
Homo sapiens
-
-
additional information
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
0.000018
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 18 nM
0.000053
(2R)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000018
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Rattus norvegicus
-
-
0.000053
(2S)-N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-2-carboxamide
Homo sapiens
-
IC50: 53 nM
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
IC50 less than 0.2 mM
0.000015
1,2-dichloro-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.0000002
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.0000002
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
IC50 less than 0.2 mM
0.000044
1-bromo-3-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
IC50 less than 0.2 mM
0.0000002
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Mus musculus
-
-
0.0000003
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Homo sapiens
-
-
0.000066
1-bromo-4-([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-phenylethyl]amino]propyl]sulfinyl]oxy)benzene
Rattus norvegicus
-
-
0.0000005
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Homo sapiens
-
-
0.0000009
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Mus musculus
-
-
0.000759
1-[(1S)-1-[[(1R)-2-[(1-cyanocyclopropyl)amino]-1-[[(cyclopropylmethoxy)sulfinyl]methyl]-2-oxoethyl]amino]-2,2,2-trifluoroethyl]-4-fluorobenzene
Rattus norvegicus
-
-
0.0000003
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Homo sapiens
-
-
0.0000008
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Mus musculus
-
-
0.000021
1-[([[(2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propyl]sulfinyl]oxy)methyl]-2,3-difluorobenzene
Rattus norvegicus
-
-
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.00013
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000014
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000022
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000015
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000005
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat S
0.000002
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000004
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.0002
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Homo sapiens
-
-
0.00069
3-[4-chloro-3-[(4-chlorophenyl)ethynyl]phenyl]-5-(methylsulfonyl)-1-[3-(morpholin-4-yl)propyl]-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine
Mus musculus
-
-
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000021
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000064
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00015
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00011
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000012
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.000014
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.000009
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.00001
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00002
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Mus musculus
-
mus Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as substrate
0.000028
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat Cat S, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00014
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00001
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000024
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00000016
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Mus musculus
-
-
0.000011
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Homo sapiens
-
-
0.001051
methyl (2R)-2-[[(1S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl]amino]-3-[(1-cyanocyclopropyl)amino]-3-oxopropane-1-sulfinate
Rattus norvegicus
-
-
0.000096
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Mus musculus
-
-
0.000729
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Homo sapiens
-
-
0.01
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfenate
Rattus norvegicus
-
IC50 above 0.01 mM
0.0000006
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Mus musculus
-
-
0.0000018
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Homo sapiens
-
-
0.000426
methyl (2R)-3-[(1-cyanocyclopropyl)amino]-3-oxo-2-[[(1S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethyl]amino]propane-1-sulfinate
Rattus norvegicus
-
-
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Homo sapiens
-
IC50: 17 nM
0.000017
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-1-benzofuran-2-carboxamide
Rattus norvegicus
-
-
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Homo sapiens
-
IC50: 34 nM
0.000034
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-(3-fluorophenyl)furan-2-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]-5-[3-(trifluoromethyl)phenyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Homo sapiens
-
IC50: 47 nM
0.000047
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-2-carboxamide
Rattus norvegicus
-
-
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Homo sapiens
-
IC50: 6 nM
0.000006
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]furan-3-carboxamide
Rattus norvegicus
-
-
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 213 nM
0.000213
N-[(1S)-1-(cyclohexylmethyl)-2-oxo-2-[(2-[[4-(trifluoromethoxy)phenyl]amino]ethyl)amino]ethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Homo sapiens
-
IC50: 11 nM
0.000011
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]morpholine-4-carboxamide
Rattus norvegicus
-
-
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Homo sapiens
-
IC50: 12 nM
0.000012
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydro-2H-pyran-4-carboxamide
Rattus norvegicus
-
-
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Homo sapiens
-
IC50: 21 nM
0.000021
N-[(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]tetrahydrofuran-3-carboxamide
Rattus norvegicus
-
-
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Homo sapiens
-
IC50: 12 nM
0.000012
tetrahydro-2H-pyran-4-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000042
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
0.000049
tetrahydrofuran-3-yl [(1S)-1-(cyclohexylmethyl)-2-[[(1S)-1-methyl-2-[[4-(trifluoromethoxy)phenyl]amino]ethyl]amino]-2-oxoethyl]carbamate
Rattus norvegicus
-
-
additional information
(2R)-N-(1-benzyl-4-cyanopiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 207 - 347 nM
additional information
(2R)-N-(1-cyanocyclopropyl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 135 - 154 nM
additional information
(2R)-N-(4-cyano-1-methylpiperidin-4-yl)-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 251 - 641 nM
additional information
(2R)-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 37 - 63 nM
additional information
(2R)-N-[(3R)-3-cyano-1-(propan-2-yl)pyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 66 - 82 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cycloheptylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 35 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 23 - 49 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(1-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 47 - 62 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclohexylpyrrolidin-3-yl]-2-[(4-methylcyclohexyl)methyl]-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 14 - 17 nM
additional information
(2R)-N-[(3R)-3-cyano-1-cyclopentylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 75 -78 nM
additional information
(2R)-N-[(3R)-3-cyano-1-methylpyrrolidin-3-yl]-2-(cyclohexylmethyl)-4-(morpholin-4-yl)-4-oxobutanamide
Homo sapiens
-
IC50: 155 - 172 nM
additional information
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
Homo sapiens
-
IC50 above 20 microM, effect of R1 substituent on the Ii p10 cell assay at 37°C
additional information
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, determined by a fluorometric assay with recombinant catS employing L-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
-
IC50: below 1 nM
additional information
6-(4-chlorobenzyl)-7-(2-piperidine-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT S employing Z-Leu-Leu-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
rat mutant G137C Cat S, IC50 is above 0.01 mM, Z-Leu-Leu-Arg-7-amido-4-methylcumarin as substrate
additional information
Chlorella powder
Homo sapiens
-
chlorella powder inhibits peptidase cathepsin S in a dose-concentration manner with 50% inhibitory concentration of 3.46 mg/l
-
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
additional information
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is below 0.001 M, inhibition is determined by a fluorometric assay with recombinant Cat S
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
-
Cat S activity quantification in serum of healthy persons and atherosclerosis and/or diabetes patients, non-atheroma, and atheroma patients with myocardial infarction, overview
additional information
CTSS sequence variations are associated with two human metabolic risk factors for cardiovascular diseases: plasma Apo-A1 and HDL-C concentrations
additional information
-
CTSS sequence variations are associated with two human metabolic risk factors for cardiovascular diseases: plasma Apo-A1 and HDL-C concentrations
additional information
CTSS circulating levels are increased in obese individuals and decreased following weight loss induced by gastric surgery
additional information
-
CTSS circulating levels are increased in obese individuals and decreased following weight loss induced by gastric surgery
additional information
an independent obese adult population, associations between 3 CTSS variants (rs10888390, rs10888394 and rs1136774) and plasma Apo-A1 levels in women are found
additional information
-
an independent obese adult population, associations between 3 CTSS variants (rs10888390, rs10888394 and rs1136774) and plasma Apo-A1 levels in women are found
additional information
-
dendritic and B-cells show significantly lower endosomal CatS activity compared with macrophages, the CatS activity in endosomal extracts from macrophages is 10times higher than in the corresponding extracts from B-cell line and even 30times higher than in endosomal fractions from dendritic cells, CatS activity differs not only between the different types of antigen presenting sells but also between endosomal and lysosomal compartments of one cell type
additional information
-
macrophage endosomal extracts even show a 600fold higher CatS activity compared with lysosomal extracts
additional information
in a lean cohort, which corresponds to a general French population, significant associations between the rs11576175 variant and the plasma Apo-A1 and HDL-C in women and men are identified
additional information
-
in a lean cohort, which corresponds to a general French population, significant associations between the rs11576175 variant and the plasma Apo-A1 and HDL-C in women and men are identified
additional information
cathepsin S genotypes are associated with Apo-A1 and HDL-cholesterol in lean and obese French populations
additional information
-
cathepsin S genotypes are associated with Apo-A1 and HDL-cholesterol in lean and obese French populations
additional information
CTSS sequence variations are associated with two human metabolic risk factors for cardiovascular diseases, plasma Apo-A1 and HDL-C concentrations
additional information
-
CTSS sequence variations are associated with two human metabolic risk factors for cardiovascular diseases, plasma Apo-A1 and HDL-C concentrations
additional information
CTSS contributes independently to plasma Apo-A1 and HDL-Clevels in both healthy and obese populations, with the most prominent CTSS polymorphism (rs10888390) explaining 3.8% of the variance in plasma Apo-A1 phenotype levels in obese women
additional information
-
CTSS contributes independently to plasma Apo-A1 and HDL-Clevels in both healthy and obese populations, with the most prominent CTSS polymorphism (rs10888390) explaining 3.8% of the variance in plasma Apo-A1 phenotype levels in obese women
additional information
the median tear CTSS activity in patients with Sjögren's syndrome is 4.1fold higher than that in patients with other autoimmune diseases, 2.1fold higher than that in patients with nonspecific dry eye disease, and 41.1fold higher than that in healthy control subjects
additional information
-
the median tear CTSS activity in patients with Sjögren's syndrome is 4.1fold higher than that in patients with other autoimmune diseases, 2.1fold higher than that in patients with nonspecific dry eye disease, and 41.1fold higher than that in healthy control subjects
additional information
up-regulation of cathepsin S transcript during the early stage of Edwardsiella ictaluri infection, leading to speculate that CTSS may play a role in infection
additional information
-
up-regulation of cathepsin S transcript during the early stage of Edwardsiella ictaluri infection, leading to speculate that CTSS may play a role in infection
additional information
-
leucocyte CatS deficiency leads to a markedly altered plaque morphology and composition, which can in part be attributed to fewer elastic lamina ruptures and a higher resistance of macrophages to apoptosis and necrosis
additional information
-
osteogenic activity decreases in apolipoprotein-/-/catS-/- mouse aortas with chronic renal disease
additional information
-
CATS protein expression increases in the cerebral cortex, the cerebellum and the hippocampus, the proform is the predominant enzymatic form in all analyzed age groups
additional information
-
the number of CATS immunopositive cells with glial morphology clearlyincreases in 4-week- and 26-30-month old mice
additional information
-
in a transgenic mouse model of amyotrophic lateral sclerosis expressing mutant superoxide dismutase 1, CATS transcript and protein levels are significantly upregulated in spinal cord and lower brain regions displaying neuronal degeneration
additional information
-
CATS transcript and protein are strongly increased between 3 and 5 months of age in the central nervous system of SOD1-G93A transgenic mice with amyotrophic lateral sclerosis
additional information
-
cathepsin S, a cellular enzyme shows enhanced expression in pathogenic conditions
additional information
-
expression and activity of CATS is upregulated in the spinal cord during the development and progression of neuropathic pain in the CNS of the rat 5th lumbar spinal nerve transection model after the lesion, the strongest increase in protein content is found in the thoracic segment (63.6%)
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5.5
6 - 6.5
6.5
5.5
-
hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
6.5
-
maximum kcat/Km, substrate: o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
6.5
-
reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin or benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
6.5
-
hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
3.5 - 8
-
pH 3.5: about 60% of maximal activity, pH 7.0: about 50% of maximal activity, pH 8.0: about 60% of maximal activity, hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
3.5 - 8.5
3.5 - 9
-
pH profiles of autocatalytic processing activity in presence or absence of dermatan sulfate, overview
4.5 - 8
4.5 - 9
-
substrate: o-aminobenzoic acid-Leu-Glu-Gln-(N-[2,4-dinitrophenyl]ethylenediamine)
5 - 7.5
-
pH 5.0: about 20% of maximal activity, pH 7.5: about 40% of maximal activity, reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin or benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
5.5 - 8.5
-
pH 5.5: about 45% of maximal activity, pH 8.5: about 50% of maximal activity, reaction with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
3.5 - 8.5
-
pH 3.5: about 50% of maximal activity, pH 7.5: about 40% of maximal activity, pH 8.0: about 85% of maximal activity, pH 8.5: about 30% of maximal activity, hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
3.5 - 8.5
-
pH 3.5: about 55% of maximal activity, pH 7.5: about 50% of maximal activity, pH 8.0: about 70% of maximal activity, pH 8.5: about 35% of maximal activity, hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
4.5 - 8
-
pH 4.5: about 55% of maximal activity, pH 8.0: about 65% of maximal activity
4.5 - 8
-
pH 4.5: about 35% of maximal activity, pH 7.5: about 40% of maximal activity, pH 8.0: about 50% of maximal activity, hydrolysis of benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
4.5 - 8
-
pH 4.5: about 60% of maximal activity, pH 8.0: about 40% of maximal activity, reaction with benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
50
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TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
cathepsin S is a cysteine protease that is able to work outside the lysosome and in a wide range of pH
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pI VALUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
647947, 647957, 647970, 647973, 647976, 647978, 647979, 647983, 647984, 647987, 647988, 647989, 647991, 647992, 668394
-
-
brenda
i.e. Pimelodus fulvidraco or Pelteobagrus fulvidraco
UniProt
brenda
-
30359, 647947, 647948, 647949, 647950, 647951, 647952, 647953, 647954, 647955, 647956, 647958, 647959
-
-
brenda
-
647961, 647962, 647963, 647964, 647965, 647966, 647969, 647970, 647971, 647972, 647977, 647980, 647981, 647985, 647986, 647990, 647993, 667140, 667363, 667952, 667963, 667971, 668394, 668538, 668602, 669514, 677874
-
-
brenda
-
-
-
brenda
-
696743, 698325, 698859, 699142, 699442, 707626, 707684, 707685, 707699, 707700, 707701, 707715, 708138, 708159, 708259, 708426, 708567, 709364, 709479, 709657, 709658, 710217, 717159, 717328, 717329, 717330
-
-
brenda
-
733231, 733448, 733485, 733993, 734187, 753917, 753981, 768884, 769122, 769357, 769630, 769642, 770435, 773461, 773914
UniProt
brenda
reference no. rs7534124, A/G type single strand conformation polymorphism
UniProt
brenda
tag single polymorphism at location 147,540,467, intronic A/G exchange
UniProt
brenda
tag single polymorphism at location 147,540,612, exon 4 A/G exchange
UniProt
brenda
tag single polymorphism at location 147,551,270, location at 5'-UTR, T/C exchange
UniProt
brenda
tag single polymorphism at location 147,562,986, genomic C/T exchange
UniProt
brenda
tag single polymorphism at location 47,560,484, genomic T/G exchange
UniProt
brenda
C57BL/6 mice and SOD1-G93A transgenic mice (model of amyotrophic lateral sclerosis)
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brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
hypoxia increases the levels of CatS gene and protein in cultured HUVECs
brenda
-
increased serum cathepsin S in patients with atherosclerosis and diabetes
brenda
additional information
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subcutaneous, of obese and lean individuals, adipocytes and stromal vascular fraction, the enzyme level in obese tissue is increased, genetic profiling and expression analysis, overview
brenda
specific localization of cathepsin S activity in dendritic cells
brenda
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in nephron segments microdissected from lyophilized renal sections, highest cathepsin S activity is found in the proximal convoluted tubules followed by proximal straight tubules of the superficial cortex. In the remaining segments cathepsin S activity is hardly detectable
brenda
bone marrow-derived immune cells, cathepsin S expression is mainly restricted to antigen-presenting cells (APCs)
brenda
cathepsin S is expressed by macrophages infiltrating the human kidney
brenda
additional information
in human type 2 diabetic nephropathy, only CD68+ intrarenal monocytes express Cat-S mRNA, whereasCat-S protein is present along endothelial cells and inside proximal tubular epithelial cells also
brenda
additional information
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in human type 2 diabetic nephropathy, only CD68+ intrarenal monocytes express Cat-S mRNA, whereasCat-S protein is present along endothelial cells and inside proximal tubular epithelial cells also
brenda
additional information
in mouse type 2 diabetic nephropathy, only CD68+ intrarenal monocytes express Cat-S mRNA, whereasCat-S protein is present along endothelial cells and inside proximal tubular epithelial cells also. Transcriptome analysis
brenda
additional information
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in mouse type 2 diabetic nephropathy, only CD68+ intrarenal monocytes express Cat-S mRNA, whereasCat-S protein is present along endothelial cells and inside proximal tubular epithelial cells also. Transcriptome analysis
brenda
additional information
-
the enzyme is expressed in antigen presenting cells
brenda
additional information
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cathepsin S is not expressed in HeLa-CIITA and MeIJuSo cells
brenda
additional information
SoCatS expression is detected in various tissues
brenda
additional information
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SoCatS expression is detected in various tissues
brenda
additional information
expression is detected in all the examined tissues
brenda
additional information
highest enzyme expression levels are seen in head kidney, fin, skin, spleen, and gill and the lowest levels are seen in the muscle, blood, liver, heart, intestine, and back kidney. Quantitative expression analysis in tissues, overview
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
of vascular smooth muscle cells, by association with integrin alphanybeta3, surface distribution
brenda
additional information
the enzyme contains a signal peptide (residues 1-17)
brenda
additional information
-
the enzyme is highly expressed in artherosclerotic and neointimal lesions, active Cat S co-localizes with integrins
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brenda
additional information
design and synthesis of a near-infrared quenched activity-based probes (qABP) that selectively target cathepsin S which is highly expressed in immune cells, green-fluorescent pan-reactive cysteine cathepsin qABP in dual color labeling studies in bone marrow-derived immune cells, and identification of vesicles containing exclusively cathepsin S activity. The high degree of selectivity is retained both in vitro and in vivo
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Highest Expressing Human Cell Lines
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
cathepsin S homologues are papain-like proteases. SoCatS is evolutionally close to the cathepsin S of other teleost fish (with 60-90% overall sequence identities), especially to Miichthys miiuy (Sciaena miiuy), a member of Sciaenidae family like red drum
malfunction
metabolism
cathepsin S cleaves cathepsin K (cathepsin cannibalism) which reduces the total elastin- and collagen-degradative activity in the multiple cathepsin system. Cathepsin cannibalism protects type I collagen through a reduction in the amount of highly collagenolytic cathepsin K available due to cathepsin S degradation of cathepsin K
physiological function
additional information
malfunction
cathepsin S deficiency as shown in knockout mice induces a high bone turnover, leading to less dense bone and trabecular thinning despite normal bone mass
malfunction
CatS knockdown leads to defective endothelial cell invasion, proliferation, and tube formation as shown in CatS knockout mice and CatS silincing in HUVEC cells
malfunction
silencing of CatS impairs the HUVEC invasion, proliferation and tubulogenesis
malfunction
the population of CD11c+ dendritic cells is significantly increased in the splenic marginal zone (MZ) locally of wild-type (DBA/2) mice with splenomegaly but not in that of CatS deficient (CatS-/-) mice after systemic exposure to lipopolysaccharide from Porphyromonas gingivalis (PgLPS) for 7 consecutive days
malfunction
cathepsin S (CTSS) activity is increased in tears of Sjögren's syndrome patients. This elevated CTSS may contribute to ocular surface inflammation. Cells with reduced PAR-2 expression show reduced ability of chronic CTSS to induce gene expression of pro-inflammatory cytokines and proteases. Acute exposure to heat-inactivated CTSS does not induce pro-inflammatory cytokines
malfunction
in vitro transcriptome analysis and experiments using siRNA or specific Cat-S and PAR2 antagonists revealed that Cat-S specifically impaired the integrity and barrier function of glomerular endothelial cells selectively through PAR2. Extrinsic and intrinsic Cat-S triggers endothelial cell injury and microvascular permeability through PAR2 in vivo. Cat-S-induced monolayer disruption is prevented by Cat-S. Extrinsic and intrinsic Cat-S triggers endothelial cell injury and microvascular permeability through PAR2 in vivo
malfunction
in vitro transcriptome analysis and experiments using siRNA or specific Cat-S and PAR2 antagonists revealed that Cat-S specifically impaired the integrity and barrier function of glomerular endothelial cells selectively through PAR2
physiological function
by cleaving membrane-anchored CX3CL1 cathepsin S regulates the adhesion of vascular smooth muscle cells and the capture of monocytes to the sites of atherogenesis
physiological function
CatS activity controls ischemia-induced neovascularization partially via the modulation of PPAR-gamma and VEGF/Akt signaling activation
physiological function
CatS activity controls ischemia-induced neovascularization partially via the modulation of PPAR-gamma and VEGF/Akt signaling activation
physiological function
cathepsin S (CatS) is involved in Th17 differentiation through the upregulation of interleukin-6 by activating PAR-2 after systemic exposure to lipopolysaccharide from Porphyromonas gingivalis (PgLPS). Lysosomal proteinase CatS is known to be involved in dendritic cell functions. CatS is essential for the production of interleukin-6 by splenic CD11cC dendritic cells after systemic exposure to PgLPS
physiological function
cathepsin S alters the expression of pro-inflammatory cytokines and MMP-9, partially through protease-activated receptor-2, in human corneal epithelial cells. Acute CTSS exposure significantly increased HCE-T cell gene and protein expression of interleukin 6 (IL-6), interleukin 8 (IL-8), tumor necrosis factor-alpha (TNF-alpha), and interleukin-1beta (IL-1beta) from 2 to 4 h, while matrix metalloproteinase 9 (MMP-9), CTSS, and protease-activated receptor-2 (PAR-2) are increased by chronic CTSS exposure
physiological function
cathepsin S expression is mainly restricted to antigen-presenting cells (APCs) where it contributes to antigen presenting capacity by controlling trafficking and maturation of major histocompatibility complex (MHC) class II molecules
physiological function
cathepsin S (Cat-S) is a cysteine protease that degrades elastic fibers and activates the protease-activated receptor-2 (PAR2) on endothelial cells. Cathepsin S cleavage of protease-activated receptor-2 on endothelial cells promotes microvascular diabetes complications. Cat-S is a monocyte/macrophage-derived circulating PAR2 agonist and mediator of endothelial dysfunction-related microvascular diabetes complications. Extrinsic and intrinsic Cat-S triggers endothelial cell injury and microvascular permeability through PAR2 in vivo, Cat-S specifically induces GEnC dysfunction through PAR2 in vitro
physiological function
cathepsin S (Cat-S) is a cysteine protease that degrades elastic fibers and activates the protease-activated receptor-2 (PAR2) on endothelial cells. Cathepsin S cleavage of protease-activated receptor-2 on endothelial cells promotes microvascular diabetes complications. Cat-S is a monocyte/macrophage-derived circulating PAR2 agonist and mediator of endothelial dysfunction-related microvascular diabetes complications. In vitro transcriptome analysis and experiments using siRNA or specific Cat-S and PAR2 antagonists revealed that Cat-S specifically impaired the integrity and barrier function of glomerular endothelial cells selectively through PAR2. Delayed treatment of type 2 diabetic db/db mice with Cat-S or PAR2 inhibitors attenuates albuminuria and glomerulosclerosis (indicators of diabetic nephropathy) and attenuates albumin leakage into the retina and other structural markers of diabetic retinopathy
physiological function
knockdown of CatS attenuates the ability of fish to eliminate pathogenic bacteria. Recombinant CatS shows strong binding ability to lipopolysaccharide and peptidoglycan and is able to agglutination to different bacteria
additional information
catalytic residues are Gln132, Cys138, His274, and Asn294
additional information
enzyme SoCatS possesses a peptidase domain with four catalytically essential residues, Gln140, Cys146, His285, and Asn305, Asn305, and a characteristic ERWNI/VN motif of cathepsin L family. The catalytic residue is Cys146. Enzyme structure homology modelling, the enzyme structure displays a typical papain-type fold, overview
additional information
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enzyme SoCatS possesses a peptidase domain with four catalytically essential residues, Gln140, Cys146, His285, and Asn305, Asn305, and a characteristic ERWNI/VN motif of cathepsin L family. The catalytic residue is Cys146. Enzyme structure homology modelling, the enzyme structure displays a typical papain-type fold, overview
additional information
Cys25, His162, and Asn183 are catalytical residues
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UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). CATS_SAIBB
330
0
37346
Swiss-Prot
other Location (Reliability: 3)
O18456_HETGL
353
1
38769
TrEMBL
Secretory Pathway (Reliability: 4)
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
24000
25000
26000
36700
calculated from 329-amino acid sequence, the complete CTSS cDNA comprises 1530 nucleotides including a 96-nucleotide 5'-untranslated region, a 990-nucleotide open reading frame and a 444-nucleotide 3'-untranslated region
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
monomer
additional information
monomer
-
enzyme has 217 amino acids, the structure of CatS is composed of 2 domains
additional information
-
most of the loss of procathepsin S occurs during folding, probably because of aggregation. Concentrations lower than 0.02 mg/ml of procathepsin S are necessary to minimise such aggregation
additional information
enzyme SoCatS possesses the typical cathepsin S domain architecture, i.e. a signal peptide (residues 1-21), an N-terminal proregion known as protease inhibitor I-29 (residues 34-94), and a C-terminal C1-peptidase domain (residues 122-337)
additional information
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enzyme SoCatS possesses the typical cathepsin S domain architecture, i.e. a signal peptide (residues 1-21), an N-terminal proregion known as protease inhibitor I-29 (residues 34-94), and a C-terminal C1-peptidase domain (residues 122-337)
additional information
the enzyme contains a signal peptide (1-17 aa), a propeptide inhibitor domain (18-113 aa), and a mature peptide (114-326 aa). The mature peptide consists of four catalytic residues (Gln132, Cys138, His274, and Asn294), four N-glycosylation sites, eight conserved cysteine sites, and six dominant subsites for the binding of specific substrates
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
proteolytic modification
glycoprotein
potential N-glycosylation site at the Asn98 residue, important for CTSS transportation into lysosomes
glycoprotein
cahepsin Sa has four N-glycosylation sites, it contains more N-glycosylation sites than cathepsin S
proteolytic modification
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structural stability and the folding of procathepsin S are considerably dependent on an aromatic stack built by the residue Trp28, Trp31 and Trp52
proteolytic modification
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optimization of the in vitro folding conditions for cathepsin S
proteolytic modification
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identification of internal autoproteolytic cleavage sites within the prosegment of procathepsin S. Contribution of a plausible unimolecular autoproteolytic event for the processing of the zymogen
proteolytic modification
-
the propeptide domain of procathepsin S shows chaperone function
proteolytic modification
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the folding of cathepsin S depends on ist proregion, the prodomain core and the hairpin region are important for the foldase function
proteolytic modification
-
the proenzyme is autocatalytically processed to active cathepsin S at pH 4.5 in the presence of an excess of cysteine and catalytic amounts of dextran sulfate
proteolytic modification
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the precursor can be activated in vitro at ph 4.5 and 40°C under reducing conditions. The in vitro activated enzyme has a NH2-terminal extension when compared with the native bovine enzyme. The precursor of cathepsin S can also be efficiently transformed into the mature enzyme by treatment with subtilisin BPN. The MW of the nonglycosylated precursor is 35900 Da
proteolytic modification
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the cDNA predicts a 331-amino acid prepro-cathepsin S
proteolytic modification
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autocatalytic activation of procathepsin S, recombinant procathepsin S is capable of autocatalytic processing at neutral pH in the presence of about 20fold activating glycosaminoglycans, or polysaccharides, such as dextran sulfate, chondroitin sulfates A and E, and dermatan sulfate, activation via electrostatic interaction with procathepsin S, heparin, heparan sulfate, and hyaluronic acid have poor or no effect
proteolytic modification
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the prepeptide of CATS is removed during the passage to the endoplasmic reticulum and the procathepsin undergoes proteolytic processing to the mature enzyme in the lysosomal compartment
proteolytic modification
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the cDNA encodes a 330-residue protein with a 17-amino acid putative signal sequence, 95-residue ürpregion, and 216-residue mature protein
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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
2.5 A structure of a complex between human cathepsin S and a potent irreversible inhibitor, vapor diffusion methods at 17°C, where the reservoir contains 1.25 M ammonium sulfate, 70 mM MES, pH 6.5, and 7 mM CoCl2
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cathepsin S mixed with morpholine-4-carboxylic acid [1S-(2-benzyloxy-1R-cyano-ethylcarbamoyl)-3-methylbutyl]amide, crystals are grown by vapor diffusion at room temperature in hanging drops
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cathepsin S-inhibitor complex with the mechanism-based inhibitor Mu(morpholine urea)-Phe-homoPhe-vinylsulfonyl-benzene, vapor diffusion with hanging drops, optimization of parameters results in diffraction-quality crystals produced in 0.2 M (NH4)3PO4, 0.1 M Na3-citrate, pH 5.6 at 17°C. The best crystals to date have been obtained by feeding the crystal drop with 0.0003 ml of protein solution every 5 days for approximately 2 months
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crystal complex of cathepson S with potent covalent inhibitors, microcrystals are grown at 22°C by hanging drop vapor diffusion method
crystallization of the enzyme in complex with an heterocyclic arylaminoethyl amide inhibitor, crystallization in presence of 0.2 M zinc acetate, X-ray diffraction structure determination and analysis at 1.8 A resolution
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determination of the crystal structure of the enzyme cocrystallized with the irreversible vinyl-sulfone inhibitor APC-2848 or with a reversible dipeptide-nitrile inhibitor, crystal structure determination of the C25S mutant cathepsin S
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
C25S
DELTAW52-N63
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the mutant procathepsin S is expressed in HEK 293 cells as a stable protein. However it is not processed to mature cathepsin S as is the wild-type procathepsin S
Y118A
mutation of exosite 2, mutant shows a highly reduced elastolytic activity
G137C
recombinant rat Cat S mutant shows no inhibition by 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile or 6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile or 6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
additional information
additional information
mutation of the putative exosite 1, i.e. replacement of residues 94-104 by corresponding residues of cathepsin L, does not affect elastolytic activity. Replacement of residues 94-177 and introduction of residues 174-180 of cathepsin L, i.e. mutation of the site A of CatS by its CatL counterpart results in a 72% reduction in CongoRed elastin degradation. Additional introduction of mutation Y11A leads to 82% less degradation of CongoRed
additional information
-
addition of a carboxy-terminal hexahistidine purification tag has no effect on the kinetic characterization of any of the enzyme forms against butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin substrate
additional information
-
cathepsin S-deficient mutant mice lack the TAP-independent vacuolar pathway of MHC class I crosspresentation, and have reduced crosspriming to particulate and cell-associated antigens as well as to influenza virus, overview
additional information
-
generation of enzyme-deficient mutant murine splenocytes, which show enlarged endosome forms lacking the multivesicular morphology due to accumulation of MHC class II-associated invariant chain Ii, cells lacking both CatS and MHC class II-associated invariant chain Ii show normal endosome size but absence of endosomal membranes
additional information
-
generation of Cat S-deficient mutant mice, the mutant mice demonstrate impaired angiogenesis and tumor cell proliferation
additional information
-
cathepsin S-deficient mutant mice show impaired degradation of the invariant chain in antigen presenting cells alng with resistance to collagen-induced arthritis and autoimmune myasthenia gravis
additional information
-
generation of Cat S-deficient knockout mice mutants showing accumulation of MHC class II molecules bound to the 10 kDa fragment of Ii, knockout mice phenotype, overview
additional information
-
generation of Cat S null mutant mice showing increased resistance to the development of experimental autoimmune myasthenia gravis with reduced responses of B- and T-cells to acetylcholine receptor antigen compared to wild-type mice
additional information
-
generation of Cat S-deficient mutant mice, the mutant mice demonstrate impaired angiogenesis and tumor cell proliferation
-
additional information
-
generation of Cat S null mutant mice showing increased resistance to the development of experimental autoimmune myasthenia gravis with reduced responses of B- and T-cells to acetylcholine receptor antigen compared to wild-type mice
-
additional information
-
addition of a carboxy-terminal hexahistidine purification tag has no effect on the kinetic characterization of any of the enzyme forms against butyloxycarbonyl-Val-Leu-Lys-7-amido-4-methylcoumarin substrate
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4
-
10-12% loss of activity after 60 min in presence of dithiothreitol and EDTA, 70% inactivation after 60 min in absence of dithiothreitol and EDTA
7.5
additional information
-
CatS is markedly more stable at extracellular pH, which indicates that it may play a role in extracellular proteolysis
7.5
-
40°C, 10-12% loss of activity after 60 min in presence of dithiothreitol and EDTA
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
26
at temperatures above 26°C activity rapidly declines after short initial increase
37
40
-
pH 5.5-7.0, in presence for dithiothreitol and EDTA stable for 240 min. 10-12% of the enzyme activity is lost after 60 min at pH 7.5 or pH 4.0. In absence of dithiothreitol and EDTA the enzyme is inactivated at pH 4.0 by 70% after 60 min
37
-
15 min, retention of more than 80% enzyme activity at pH 7.0, about 40% retention at pH 4.7 and about 50% retention at pH 8.5
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-10°C, 0.012-0.04 mM cathepsin S, 100 mM sodium acetate buffer, pH 5.5, 1 mM EDTA, stable for 8 months. In presence of 0.5 mM Hg2+ and 1 mM EDTA rapid decrease of about 50% of the activity which then remains unchanged for 3 months
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
a method of zymography (substrate gel electrophoresis) is described to detect the activity of cathepsins K, L, S, and V from one cell extract/preparation
-
ammonium sulfate precipitation and phenyl-Sepharose column chromatography
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
apolipoprotein-deficient with minus or plus catS are assigned to chronic renal disease
-
chimeric LDLr-/-mice deficient in leucocyte cathepsin S are generated by bone marrow transplantation
-
DELTAW52-N63 mutant procathepsin S is expressed in HEK 293 cells as a stable protein. However it is not processed to mature cathepsin S as is the wild-type procathepsin S
-
DNA and amino acid sequence determination and analysis, sequence comparisons and phylogenetic analysis
expressed in Escherichia coli
expression in baby hamster kidney cells and transport to lysosomes via the mannose 6-phosphate receptor pathway
-
expression in baculovirally infected Sf9 insect cells along with humanized forms truncated by eight residues at the amino-terminus
gene PfCTSSa, DNA and amino acid sequence determination and analysis, sequence comparisons and phylogenic analysis, quantitative expression analysis, recombinant expression in Escherichia coli strain BL21(DE3)
genetic profiling and expression analysis of CatS in adipose tissue of non-obese and obese individuals
-
human CatS is obtained by autocatalytic processing of the zymogene expressed in Escherichia coli
-
the cDNA encoding proenzyme of PoCtS is expressed in Escherichia coli as a fusion protein with glutathione S-transferase in a pGEX-4T-1 vector. The recombinant proPoCtS protein is overexpressed in Escherichia coli BL21(DE3) as a 60 kDa fusion protein
-
wild type human CatS is cloned into pcDNA3, CatS overexpression is involved in radioresistance
-
expression in baculovirally infected Sf9 insect cells along with humanized forms truncated by eight residues at the amino-terminus
-
expression in baculovirally infected Sf9 insect cells along with humanized forms truncated by eight residues at the amino-terminus
-
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
both expression and activity of Cat S are significantly reduced in neohesperidin dihydrochalcone-treated keratinocytes
CTSS gene expression is increased after cells have been treated with recombinant CTSS for 24 h. CTSS protein expression in cell lysates measured using the human CTSS ELISA kit also reveal that the protein increases after 8 h CTSS treatment
expression in immune-related tissues is upregulated in a time-dependent manner upon bacterial pathogen infection
PoCtS expression increased significantly in muscle 6 h post-injection of bacterial lipopolysaccharide
-
SoCatS expression is enhanced by bacterial infection with fish pathogenic Edwardsiella tarda, a fish pathogen. In kidney, significant induction of SoCatS occurs at 4 h (2.31fold) and 8 h (2.55fold) post-infection. In liver, significant induction of SoCatS (3.0fold) is only observed at 24 h post-infection. In spleen, SoCatS expression is significantly upregulated at 12 h post-infection (5.46fold) and at 24 h post-infection (4.23fold)
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RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
folding is initiated by 100fold dilution of denatured-reduced proenzymes into folding buffers, generally containing 1-2 mM EDTA, most effective in promotion of procathepsin S folding is arginine (1 M)
recombinant procathepsin S from inclusion bodies produced in Escherichia coli is renatured at pH 7.6 by a two-step dilution
-
solubilization of recombinant enzyme from inclusion bodies after expression in Escherichia coli, refolding and reoxidizing
-
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
analysis
design of near-infrared fluorescent substrate-based probe MG101 for monitoring extracellular CatS activity. The fused peptide hairpin loop-structure, combines a CatS recognition domain, an electrostatic zipper, as well as a N- and C-terminal Foerster resonance energy transfer pair. The probe is selective for CatS at pH 7 and sensitive to concentrations of CatS below 1 nM. In a similar probe MG73, the AlexaFluor680/BHQ3 couple is substituted by Abz/Tyr(NO2). At pH 5.5, both prpbes are poosr substrates for cathepsin L
diagnostics
drug development
medicine
pharmacology
-
the enzyme might be a good target for development of inhibitors in treatment of collagen-induced arthritis and autoimmune myasthenia gravis
diagnostics
-
cathepsin S is a biomarker for adiposity and has relevance to atherogenesis
diagnostics
-
an increased serum level of cathepsin S may serve as a biomarker for atherosclerosis and diabetes
drug development
-
enzyme may be a potential target in rheumatoid arthritis and obesity with its associated cardiovascular risks
drug development
-
CatS is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity, therefore, it represents a promising pharmacological target for drug development
drug development
-
important role for cathepsin S in the regulation of ozone-induced airway hyperresponsiveness and neutrophil cell recruitment, cathepsin S may be a target in the treatment of oxidative stress-induced airway hyperresponsiveness and inflammation
drug development
brain-penetrating cathepsin S inhibitors demonstrate potential clinical utility for the treatment of multiple sclerosis and neuropathic pain
drug development
Cat S is an attractive therapeutic target and selective Cat S inhibitors may also modulate a number of other diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, asthma, atherosclerosis and neuropathic pain
drug development
-
discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain, cathepsin S inhibitors are attractive targets as immunological therapeutic agents
drug development
discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain, cathepsin S inhibitors are attractive targets as immunological therapeutic agents
drug development
-
discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain, cathepsin S inhibitors are attractive targets as immunological therapeutic agents
drug development
-
inhibition of the proteolytic activity of cathepsin S is an attractive target for drug development with such inhibitors having potential for modulation and regulation of autoimmune diseases such as multiple sclerosis and rheumatoid arthritis, and allergic disorders, such as asthma
drug development
-
cat S is an attractive therapeutic target for the treatment of autoimmune disorders
drug development
-
increased risk of mortality and morbidity associates with cardiovascular calcification drives the development of new therapeutic strategies to prevent and potentially reverse this process, new therapeutic options may also include selective inhibition of catS
drug development
-
importance of CATS in inflammatory processes, which has generated much interest in the development of CATS inhibitors as immunomodulatory therapeutics for immune disorders such as bronchial asthma, rheumatoid arthritis and psoriasis, CATS may also be an attractive target in neurodegenerative disorders associated with inflammation
medicine
-
cathepsin S is a potential therapeutic target for regulation of major histocompatibility complex class II immune responses, possibly resulting in treatments for autoimmune diseases and allergic asthma
medicine
-
cathepsin S is a potential therapeutic target for regulation of major histocompatibility complex class II immune responses, possibly resulting in treatments for autoimmune diseases and allergic asthma
medicine
-
cathepsin S is a potential therapeutic target for regulation of major histocompatibility complex class II immune responses, possibly resulting in treatments for autoimmune diseases and allergic asthma
medicine
-
the inhibitor JNJ 10329670 is a candidate for immunosuppressive therapy of allergies and autoimmune diseases, completely reversible inhibition
medicine
tear cathepsin S serves as a candidate biomarker for Sjögren's Syndrome
medicine
cathepsin S activation of PAR-2 may represent a potential therapeutic target for amelioration of ocular surface inflammation in Sjögren's syndrome patients
medicine
Cat-S or PAR2 inhibition might be a strategy to prevent microvascular disease in diabetes and other diseases
medicine
design of inhibitory antibodies targeting human CTSS by genetically fusing the propeptide of procathepsin S with antibodiesin IgG and Fab format. The resulting antibody fusions can be stably expressed and potently inhibit CTSS proteolytic activity in high specificity, reaching Ki alue in nanomlolar range
medicine
Cat L and S are expressed concurrently in metastatic pancreatic cancer cells. Asperphenamate analog ASPER-29, exhibits dual Cat L and S inhibitory potency, and show an antimetastatic effect on pancreatic cancer BxPC-3 and PANC-1 cells
EXTERNAL LINKS (specific for EC-Number 3.4.22.27)
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Release 2026.1 (March 2026)
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