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Information on EC 5.3.99.3 - prostaglandin-E synthase
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EC Tree
5.3.99.3 prostaglandin-E synthaseIUBMB Comments
Brings about the opening of the epidioxy bridge. Requires glutathione.
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Word Map
- 5.3.99.3
- cox-2
-
cyclooxygenase
-
arachidonic
- synthases
-
prostanoids
- lipopolysaccharide
- tnf
- lps
- phospholipase
-
eicosanoids
-
lps-induced
- pain
- endometrium
-
leukotriene
- prostacyclin
-
thromboxane
-
nsaids
- indomethacin
-
pgf2alpha
-
5-lipoxygenase
- il-1beta
- celecoxib
-
nonsteroidal
- interleukin-1beta
-
luteolysis
- luteal
- platinum
- 15-pgdh
-
estrous
-
postictal
- medicine
-
rhodium
-
pencil
- palladium
- drug development
-
6-keto-pgf1alpha
-
automobile
- pghs-2
-
prostaglandin-endoperoxide
-
e-prostanoid
-
ictal
-
pge2-dependent
- l-pgds
- 15-hydroxyprostaglandin
-
lipocalin-type
- akr1b1
-
cox-2-dependent
-
6-keto
-
coxibs
-
6-keto-pgf1
- ptgds
-
cox-derived
The expected taxonomic range for this enzyme is: Eukaryota, Bacteria, Archaea
Reaction Schemes
=
Synonyms
mpges-1, pges, microsomal prostaglandin e synthase-1, mpges, pge synthase, ptges, prostaglandin e synthase, mpges-2, cpges, mpges1, 
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
CPGES
cPGES/p23
cytosolic prostaglandin E synthase
cytosolic prostaglandin E(2) synthase-2
endoperoxide isomerase
-
-
-
-
Isomerase, prostaglandin R2 E-
-
-
-
-
microsomal PGE2 synthase-1
microsomal prostaglandin E synthase 1
microsomal prostaglandin E synthase-1
microsomal prostaglandin E synthase-2
microsomal prostaglandin E(2) synthase-1
microsomal prostaglandin E(2) synthase-2
microsomal prostaglandin E2 synthase-1
mPGES
mPGES-1
mPGES-2
MPGES1
MPGES2
p23
PGE isomerase
-
-
-
-
PGE synthase
PGE2
PGE2 isomerase
-
-
-
-
PGES
PGES-2
PGH-PGE isomerase
-
-
-
-
PGH2/PGE2 isomerase
-
-
-
-
prostagandin-E synthetase
-
-
-
-
Prostaglandin E synthase
prostaglandin E synthase 1
prostaglandin E synthase-1
prostaglandin E synthase-2
Prostaglandin E2 isomerase
-
-
-
-
prostaglandin E2 synthase
Prostaglandin endoperoxide E isomerase
-
-
-
-
Prostaglandin endoperoxide E2 isomerase
-
-
-
-
Prostaglandin endoperoxide-E isomerase
-
-
-
-
Prostaglandin H-E isomerase
-
-
-
-
Prostaglandin H-prostaglandin E isomerase
-
-
-
-
Prostaglandin R-prostaglandin E isomerase
-
-
-
-
Prostaglandin-H2 E-isomerase
-
-
-
-
PTGES
microsomal prostaglandin E synthase-1
-
-
microsomal prostaglandin E synthase-1
-
microsomal prostaglandin E synthase-1
-
-
microsomal prostaglandin E synthase-1
-
-
microsomal prostaglandin E2 synthase-1
-
-
mPGES-1
-
-
mPGES-1
-
mPGES-1
-
-
Prostaglandin E synthase
-
-
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
(13E)-(15S)-15-hydroxy-9-oxoprosta-10,13-dienoate = (13E)-(15S)-15-hydroxy-9-oxoprosta-11,13-dienoate
-
-
-
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
catalytic mechanism of mPGES-2, hydrogen bond-forming residues Y107, C113, C110, and F112 are involved, substrate binding and catalytic sites
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate = (5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
intramolecular oxidation
-
-
-
-
isomerization
isomerization
-
-
-
-
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PATHWAY SOURCE
PATHWAYS
BRENDA
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SYSTEMATIC NAME
IUBMB Comments
(5Z,13E)-(15S)-9alpha,11alpha-Epidioxy-15-hydroxyprosta-5,13-dienoate E-isomerase
Brings about the opening of the epidioxy bridge. Requires glutathione.
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CAS REGISTRY NUMBER
COMMENTARY
52227-79-9
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + reduced glutathione
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + oxidized glutathione
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
1-chloro-2,4-dinitrobenzene + GSH
?
-
glutathione S-transferase activity
-
?
5-hydroperoxyeicosatetraenoic acid + 2 GSH
5-hydroxyeicosatetraenoic acid + GSSG + H2O
-
-
-
?
Prostaglandin G1
15-Hydroperoxy-prostaglandin E1
-
at 50% of the activity relative to prostaglandin H
major product
?
Prostaglandin H
?
-
involved in prostaglandin synthesis, which in the case of prostaglandin E is likely to be associated with the subversion or suppression of host immunity
-
-
?
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
-
-
-
-
?
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11a,15-dihydroxyprosta-5,13-dienoate + GSSG
-
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
PGH2
PGE2
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
-
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate + GSH
(5Z,13E)-(15S)-11alpha,15-dihydroxyprosta-5,13-dienoate + GSSG
i.e. prostaglandin H2
i.e. prostaglandin E2
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
reaction of heme-free isozyme mPGES2
-
-
?
prostaglandin G2
15-hydroperoxy-prostaglandin E2
-
at 50% of the activity relative to prostaglandin H
major product
?
prostaglandin G2
15-hydroperoxy-prostaglandin E2
-
at pH 7.5, 2.5 mM glutathione and 10 microM substrate
-
-
?
Prostaglandin H1
Prostaglandin E1
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-13-enoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
-
660669, 662071, 667959, 668886, 670732, 702158, 702165, 702622, 703593, 706521, 714421, 714468, 715100, 715541, 715856, 715865, 747278, 748368, 748441, 748542, 748846
-
-
?
Prostaglandin H2
Prostaglandin E2
-
at pH 7.5, 2.5 mM glutathione and 10 microM substrate
-
-
?
Prostaglandin H2
Prostaglandin E2
-
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
Prostaglandin H2
Prostaglandin E2
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
Prostaglandin H2
Prostaglandin E2
-
-
662071, 667830, 702146, 702949, 703978, 705284, 706576, 713719, 714401, 714944, 716081, 716814, 746707, 747229, 748296
-
-
?
Prostaglandin H2
Prostaglandin E2
-
isozyme mPEGS-2 has an important role in urogenital function
-
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
Prostaglandin H2
Prostaglandin E2
-
-
660669, 660677, 660973, 662071, 663277, 667165, 702165, 702949, 705284, 715541, 716814, 747229, 749371
-
-
?
Prostaglandin H2
Prostaglandin E2
-
i.e. 15-hydroxy-9alpha,11alpha-peroxidoprosta-5,13-dienoic acid
-
?
additional information
?
-
-
the enzyme also shows glutathione transferase activity with 1-chloro-2,4-dinitrobenzene
-
-
?
additional information
?
-
-
platelet-derived growth factor-induced increase in enzyme activity occurs within min after exposure to the growth factor
-
-
?
additional information
?
-
-
glutathione-heme-complex bound enzyme catalyzes formation of 12(S)-hydroxy-5(Z),8(E),10(E)-heptadecatrienoic acid and malonaldehyde from prostaglandin H2, i.e. shows lyase activity
-
-
?
additional information
?
-
heme-free isozyme mPGES2 and heme-bound isozyme mPGES2 catalyze isomerization of prostaglandin H2 to prostaglandin E2 and conversion of prostaglandin H2 to to (12S)-hydroxy-(5Z,8E,10E)-heptadecatrienoic acid and malondialdehyde, respectively
-
-
?
additional information
?
-
-
concordant induction of terminal prostaglandin E2 synthase with cyclooxygenase-2 leads to the preferred production of prostaglandin E2 over thromboxane B2 and prostaglandin D2, by lipopolysaccharide-stimulated macrophages
-
-
?
additional information
additional information
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate, PGH2, mutation R126A/Q creates a glutathione-dependent reductase which is able to convert prostaglandin H2 to prostaglandin F2alpha
(5Z,13E)-(15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dienoate, PGF2alpha
-
?
additional information
additional information
-
-
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate, PGH2, mutation R126A/Q creates a glutathione-dependent reductase which is able to convert prostaglandin H2 to prostaglandin F2alpha
(5Z,13E)-(15S)-9alpha,11alpha,15-trihydroxyprosta-5,13-dienoate, PGF2alpha
-
?
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
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
Prostaglandin H
?
-
involved in prostaglandin synthesis, which in the case of prostaglandin E is likely to be associated with the subversion or suppression of host immunity
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
PGH2
PGE2
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E)-(15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
-
-
-
-
?
(5Z,13E,15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
(5Z,13E,15S)-11alpha,15-dihydroxy-9-oxoprosta-5,13-dienoate
reaction of heme-free isozyme mPGES2
-
-
?
Prostaglandin H2
Prostaglandin E2
-
-
667959, 670732, 702158, 702622, 703593, 706521, 715541, 715856, 747278, 748368, 748441, 748542, 748846
-
-
?
Prostaglandin H2
Prostaglandin E2
-
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
Prostaglandin H2
Prostaglandin E2
mPGES-1 is a gonadotropin-regulated enzyme
-
-
?
Prostaglandin H2
Prostaglandin E2
-
-
-
-
?
Prostaglandin H2
Prostaglandin E2
-
isozyme mPEGS-2 has an important role in urogenital function
-
-
?
additional information
?
-
-
platelet-derived growth factor-induced increase in enzyme activity occurs within min after exposure to the growth factor
-
-
?
additional information
?
-
-
concordant induction of terminal prostaglandin E2 synthase with cyclooxygenase-2 leads to the preferred production of prostaglandin E2 over thromboxane B2 and prostaglandin D2, by lipopolysaccharide-stimulated macrophages
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
heme
-
crystallization data of red-coloured protein purified after growth of recombinant Escherichia coli in LB medium containing delta-aminolevulinate and Fe(NO3)3. Heme is complexed with bound glutathione forming a S-Fe coordination bond with no polar interaction with enzyme. Heme dissociation constant is 0.00053 mM
additional information
mutants R126A/Q possess glutathione-dependent reductase activity
-
additional information
-
mutants R126A/Q possess glutathione-dependent reductase activity
-
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid
-
35% inhibition at 0.001 mM
(2E)-2-(2,5-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]benzylidene)hexanoic acid
-
-
(2E)-2-(2,5-bis[[4-(trifluoromethyl)benzyl]oxy]benzylidene)hexanoic acid
-
55.1% residual activity at 0.01 mM
(2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid
-
28.3% residual activity at 0.01 mM
(2E)-2-[5-(2-cyclohexylethoxy)-2-[[4-(trifluoromethyl)benzyl]oxy]benzylidene]hexanoic acid
-
74% residual activity at 0.01 mM
(3R)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
-
(3S)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
-
(4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)acetic acid
-
22% inhibition at 0.001 mM
(4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)acetic acid
-
17% inhibition at 0.001 mM
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
(4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
-
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
-
(4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
-
-
(4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
-
(4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
-
(4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
-
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid
-
-
([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid
-
75.4% residual activity at 0.01 mM
1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
-
-
1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)-N-methylpiperidine-4-carboxamide
76% inhibition at 0.01 mM
1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid
-
65% inhibition at 0.001 mM
1-[2-(2-methylphenyl)ethyl]-4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazole
-
90% residual activity at 0.03 mM
1-[4-[2-(2-carboxy-2-methylpropyl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-4-yl]-2-fluorophenyl]pyridinium
-
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
1-[6-(4-chlorophenyl)-5-methyl-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-(2-chloro-6-fluorophenyl)-7-phenyl-1,5-dihydro-4H-naphtho[1,2-d]imidazol-4-one
-
2-(2-chloro-6-fluorophenyl)-9-fluoro-3,6-dihydro-7H-benzo[h]imidazo[4,5-f]isoquinolin-7-one
-
-
2-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)acetic acid
-
23% inhibition at 0.001 mM
2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
-
-
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
-
2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
-
-
2-(trifluoromethyl)-N-(3-[[5-(trifluoromethyl)pyridin-2-yl]carbamoyl]phenyl)benzamide
-
2-([4,6-bis[2-(4-methoxyphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
-
63.7% residual activity at 0.01 mM
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid
-
-
2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
88.3% residual activity at 0.01 mM
2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
59.1% residual activity at 0.01 mM
2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
58% residual activity at 0.01 mM
2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
-
-
2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
-
CEP-32496
2-chloro-4-[(2,2-dimethylpropanamido)methyl]-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
-
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-[4-oxo-3-[4-(trifluoromethyl)phenyl]-3,4-dihydrophthalazin-6-yl]benzamide
-
2-chloro-6-fluoro-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
-
2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
-
-
2-methyl-2-(cis-4-[[1-(3-methyl-5-phenylfuro[2,3-b]pyridin-6-yl)piperidine-4-carbonyl]amino]cyclohexyl)propanoic acid
-
-
2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
2-[(4,6-bis[2-[4-(trifluoromethoxy)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
-
88.3% residual activity at 0.01 mM
2-[(4,6-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
-
-
2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
-
-
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid
-
-
2-[2,4-bis(2-phenylethoxy)benzyl]hexanoic acid
-
90.1% residual activity at 0.01 mM
2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
-
-
2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazoline-7-carboxamide
16% inhibition at 0.01 mM
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
-
2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
-
2-[3-(aminooxy)-2,2-dimethyl-3-oxopropyl]-3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indole
-
IC50: 0.01 mM
2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
-
-
2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid
-
licofelone, ML3000
2-[6-bromo-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-chloro-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
-
-
2-[[4,6-bis(2-cycloheptylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
62.4% residual activity at 0.01 mM
2-[[4,6-bis(2-cyclopentylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
90% residual activity at 0.01 mM
2-[[4,6-bis(3-methylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
-
54.5% residual activity at 0.01 mM
2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
-
81.9% residual activity at 0.01 mM
3-(1,3,5-trimethyl-4-octadecanoyl-1H-pyrrol-2-yl)propanoic acid
-
97% inhibition at 0.001 mM
3-(1,3,5-trimethyl-4-tetradecanoyl-1H-pyrrol-2-yl)propanoic acid
-
91% inhibition at 0.001 mM
3-(1-benzyl-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid
-
62% inhibition at 0.001 mM
3-(1-benzyl-4-dodecanoyl-5-methyl-3-phenylpyrrol-2-yl)propionic acid
-
64% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid
-
54% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(benzenesulfonyl)propanamide
-
77% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)-N-(methanesulfonyl)propanamide
-
52% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanamide
-
39% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanehydrazide
-
35% inhibition at 0.001 mM
3-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)propanenitrile
-
22% inhibition at 0.001 mM
3-(4-dodecanoyl-3,5-dimethyl-1-phenylpyrrol-2-yl)propionic acid
-
65% inhibition at 0.001 mM
3-(4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl)propanoic acid
-
38% inhibition at 0.001 mM
3-(4-hexadecanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid
-
97% inhibition at 0.001 mM
3-[(5E)-3-(4-butylbenzyl)-1-(4-chlorobenzyl)-4-methylidene-5-[(2E)-4-methylpent-2-en-1-ylidene]-4,5-dihydro-1H-pyrrol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00029 mM
3-[1-(4-carbamoylbenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
28% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00025 mM
3-[1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0032 mM
3-[1-(4-chlorobenzyl)-3-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0011 mM
3-[1-(4-chlorobenzyl)-3-methyl-5-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00060 mM
3-[1-(4-chlorobenzyl)-3-methyl-7-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0043 mM
3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid
-
MK-886
3-[1-(4-chlorobenzyl)-4-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
78% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenoxy-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00065 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0064 mM
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-[(2-methylphenyl)carbonyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00090 mM
3-[1-(4-chlorobenzyl)-5-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000004 mM
3-[1-(4-chlorobenzyl)-5-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000008 mM
3-[1-(4-chlorobenzyl)-5-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000022 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000005 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000003 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-3'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000033 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-4'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000031 mM
3-[1-(4-chlorobenzyl)-5-(2-fluoro-5-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
3-[1-(4-chlorobenzyl)-5-(3-fluoro-4-pyridin-3-ylphenyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000012 mM
3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0026 mM
3-[1-(4-chlorobenzyl)-5-[2-fluoro-2'-(phenylcarbonyl)biphenyl-4-yl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000006 mM
3-[1-(4-chlorobenzyl)-5-[3-fluoro-4-(pyrimidin-5-ylmethyl)phenyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000032 mM
3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid
-
i.e. 3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid or FLAP, formerly designated L-663,536, a lipoxygenase inhibitor, IC50: 0.0016 mM
3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
3-[3-(tert-butylsulfanyl)-1-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.01 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-(3-phenylpropyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0032 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-prop-2-en-1-yl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.0067 mM
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.01 mM
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00026 mM
3-[4-(2'-acetyl-2-fluorobiphenyl-4-yl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[4-(4-butoxybenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid
-
32% inhibition at 0.001 mM
3-[4-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[4-dodecanoyl-1-(4-hydroxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
53% inhibition at 0.001 mM
3-[4-dodecanoyl-1-(4-methoxybenzyl)-3,5-dimethyl-1H-pyrrol-2-yl]propanoic acid
-
72% inhibition at 0.001 mM
3-[4-dodecanoyl-3,5-dimethyl-1-(4-methylbenzyl)-1H-pyrrol-2-yl]propanoic acid
-
52% inhibition at 0.001 mM
3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid
-
83.9% residual activity at 0.01 mM
3-[5-biphenyl-3-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00016 mM
3-[5-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000016 mM
3-[5-tert-butyl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.00033 mM
3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
-
73.6% residual activity at 0.03 mM
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-3-ol
-
60.1% residual activity at 0.03 mM
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
-
89% residual activity at 0.03 mM
4'-[1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-amine
-
98.2% residual activity at 0.03 mM
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
91.9% residual activity at 0.03 mM
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazole
-
87.9% residual activity at 0.03 mM
4-(3-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole-5-carboxylic acid
-
-
4-(4'-phenoxybiphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
88.7% residual activity at 0.03 mM
4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
-
-
4-(4-dodecanoyl-1,3,5-trimethylpyrrol-2-yl)butanoic acid
-
70% inhibition at 0.001 mM
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
-
-
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
-
-
4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
-
4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
-
4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
-
4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
-
4-dodecanoyl-1,3,5-trimethyl-1H-pyrrole-2-carboxylic acid
-
37% inhibition at 0.001 mM; 59% inhibition at 0.001 mM
4-dodecanoyl-3,5-dimethyl-1-phenylpyrrole-2-carboxylic acid
-
99% inhibition at 0.001 mM
4-dodecanoyl-3,5-dimethyl-1H-pyrrole-2-carboxylic acid
-
62% inhibition at 0.001 mM
4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
-
4-[(4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazol-1-yl)sulfonyl]benzoic acid
-
59.8% residual activity at 0.03 mM
4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
96.8% residual activity at 0.03 mM
4-[4-(phenanthren-9-yl)phenyl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
-
78.2% residual activity at 0.03 mM
4-[4-benzyl-1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-5-yl]benzaldehyde
-
72.1% residual activity at 0.03 mM
4-[[2-(2-carboxyethyl)-4-dodecanoyl-3,5-dimethyl-1H-pyrrol-1-yl]methyl]benzoic acid
-
27% inhibition at 0.001 mM
4-[[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]methyl]-3-nitrobenzoic acid
-
most efficient inhibitor of mPGES-1, 12% residual activity at 0.03 mM
5-(4-cyclohexylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
-
5-(4-tert-butylphenyl)-1-[4-(1-methylethoxy)benzyl]-1H-indole-2-carboxylic acid
-
-
5-(4-tert-butylphenyl)-3-[4-(1-methylethoxy)phenyl]-1-[4-[(1-methylethyl)amino]benzyl]-1H-indole-2-carboxylic acid
-
-
5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
5-(dimethylamino)-N-[4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-yl]naphthalene-1-sulfonamide
-
85% residual activity at 0.03 mM
5-hydroxy-3-naphthalen-2-yl-4-(3-naphthalen-2-yl-phenyl)-5H-furan-2-one
-
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
-
-
5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
ethyl 2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
-
ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate
-
83.9% residual activity at 0.01 mM
heme
heme is bound to the enzyme subunits and alters the enzyme catalytic specificity, overview. Heme is attached to the bound GSH by an iron-sulfur bond, but heme cannot bind to mPGES2 in the absence of GSH, other sulfhydryl compounds, such as DTT and 2-mercaptoethanol, are unable to promote heme binding to isozyme mPGES2. Bound heme is oxidized by H2O2, but it does not dissociate from mPGES2
imidazole
imidazole stacks on the bound heme and inhibits heme oxidation by H2O2, heme dissociation by DTT, and catalytic activity
methyl 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoate
-
IC50: 0.0072 mM
methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
-
-
methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
-
-
N-(2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-7-yl)cyclopropanecarboxamide
74% inhibition at 0.01 mM
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
N-(3-chloro-2-methylphenyl)-6-[2-chloro-6-(trifluoromethyl)benzamido]-2-(methoxymethyl)-1H-benzimidazole-4-carboxamide
-
N-(4-bromophenyl)-2-[2-chloro-5-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
-
N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
-
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-([3-[(4-chlorophenyl)ethynyl]phenyl]methyl)-N'-propan-2-yl-N-([3-[(pyridin-4-yl)ethynyl]phenyl]methyl)urea
-
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-4-oxo-6-(3-oxopiperazin-1-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
79% inhibition at 0.01 mM
N-([4-chloro-3-[7-chloro-4-oxo-6-(pyridin-4-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-6-(4-hydroxypiperidin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-([4-chloro-3-[7-chloro-6-(4-methylpiperazin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
75% inhibition at 0.01 mM
N-([4-chloro-3-[7-chloro-6-(morpholin-4-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
-
N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
-
N-cyclopentyl-1-[5,6-diamino-1-(3-amino-4-fluorophenyl)-1H-benzimidazol-2-yl]piperidine-4-carboxamide
-
-
N-tert-butyl-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)azetidine-3-carboxamide
-
N-[(4-chloro-3-[4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)piperidin-1-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[4-oxo-7-[6-(trifluoromethyl)pyridin-3-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[7-chloro-4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(4-chloro-3-[7-chloro-6-[(3R)-3-hydroxypyrrolidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
95% inhibition at 0.01 mM
N-[(4-chloro-3-[7-chloro-6-[(3S)-3-hydroxypyrrolidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
91% inhibition at 0.01 mM
N-[(4-chloro-3-[7-chloro-6-[4-(difluoromethyl)piperidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
-
N-[(6-chloro-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl)methyl]-2-methylpropanamide
-
N-[3-(4-bromophenyl)-4-oxo-3,4-dihydrophthalazin-6-yl]-2-chloro-6-fluorobenzamide
-
N-[3-[(4-bromophenyl)carbamoyl]-4-(2,2-difluoroethoxy)phenyl]-2-chloro-5-[(2,2-dimethylpropanamido)methyl]benzamide
-
N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
-
-
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
-
-
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
-
N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
-
-
N-[[3-(7-amino-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
70% inhibition at 0.01 mM
N-[[3-(7-bromo-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
67% inhibition at 0.01 mM
N-[[4-chloro-3-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-chloro-6-cyclopropyl-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-chloro-6-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-fluoro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
98% inhibition at 0.01 mM
N-[[4-chloro-3-(7-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[4-chloro-3-(7-nitro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
-
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
-
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
-
SB-203580
-
blocks the association of cPGES with casein kinase II and Hsp90, as well as cPGES phosphorylation
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
-
-
[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]methyl benzoate
-
76.1% residual activity at 0.03 mM
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]acetic acid
-
66.4% residual activity at 0.01 mM
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
-
(4E)-4-[2-(3-bromophenyl)hydrazin-1-ylidene]-1-ethanethioyl-3-methyl-4,5-dihydro-1H-pyrazol-5-one
-
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
PF-4693627
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
PF-4693627
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
MF-63
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
-
fludrocortisone
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
-
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
-
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
-
selective for human over rat MPGES1
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
-
inhibitor of mutant enzyme V131T/F135L/F138A, but not of the wild type enzyme
3-(4-dodecanoyl-1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)propanoic acid
-
90% inhibition at 0.001 mM
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
IC50: 0.000007 mM
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
-
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
12% residual activity at 0.03 mM
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
-
75% inhibition at 0.01 mM
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
-
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
-
dexamethasone
-
inhibition of cytokine-induced expression of isoform mPGES-1, while isoforms mPGES-2 and cPGES remain unaffected
MF63
i.e. 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile
MK-886
-
inhibition of cytokine-induced expression of isoform mPGES-1, while isoforms mPGES-2 and cPGES remain unaffected
MK-886
-
i.e. 3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-isopropyl-1H-indol-2-yl)-2,2-dimethylpropanoic acid
MK-886
-
glutamate-induced PGE2 production is suppressed almost completely by MK-886 at a concentration of 0.003 mM or higher
MK-886
-
glutamate-induced PGE2 production is suppressed almost completely by MK-886 at a concentration of 0.003 mM or higher
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
PF-1984
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
-
PF-9184
-
potent, competitive and reversible mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
PF-9184
-
poor mPGES-1 inhibitor, i.e. N-(3',4'-dichlorobiphenyl-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
additional information
-
structure-activity relationship analysis of inhibitors
-
additional information
-
not inhibited by BWA4C, i.e. (E)-N-hydroxy-N-(3-(3-phenoxyphenyl)-allyl)acetamide
-
additional information
-
synthesis and inhibitory potency of a series of 6-nitro-3-(m-tolylamino) benzo[d]isothiazole 1,1-dioxide analogues against microsomal prostaglandin E2 synthase. No inhibition by Zileuton
-
additional information
-
pyrrole alkanoic acid derivatives as nuisance inhibitors of microsomal prostaglandin E2 synthase-1, overview. No inhibition at 0.001 mM by 3-(4-butanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-(4-heptanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-(1,3,5-trimethyl-4-octanoyl-1H-pyrrol-2-yl)propanoic acid, 3-(4-decanoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-[1,3,5-trimethyl-4-[2-(octyloxy)benzoyl]-1H-pyrrol-2-yl]propanoic acid, 3-[4-(3-heptyloxybenzoyl)-1,3,5-trimethylpyrrol-2-yl]propionic acid, 3-(4-benzoyl-1,3,5-trimethyl-1H-pyrrol-2-yl)propanoic acid, 3-[1,3,5-trimethyl-4-(naphthalen-1-ylcarbonyl)-1H-pyrrol-2-yl]propanoic acid, 3-[1,3,5-trimethyl-4-(naphthalen-2-ylcarbonyl)-1H-pyrrol-2-yl]propanoic acid, 3-[4-(2-ethylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 3-[4-(4-ethylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 3-[4-(4-benzylbenzoyl)-1,3,5-trimethyl-1H-pyrrol-2-yl]propanoic acid, 4-dodecanoyl-1-methyl-1H-pyrrole-2-carboxylic acid, (4-dodecanoyl-1-methyl-1H-pyrrol-2-yl)acetic acid, and 3-(4-dodecanoyl-1-methyl-1H-pyrrol-2-yl)propanoic acid
-
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
angiotensin II
-
angiotension II infusion induces mRNA expression of mPGES-1, mPGES-2 and cytosolic PGE synthase
epigallocatechin gallate
-
enhances COX-2 and isoform mPGES-1 gene expression and production of prostaglandin E2. Induction of mPGES-1 is mediated by active ERK1/2MAP kinases and early growth response gene 1
Hsp90
-
maximal activity is achieved when the three components (cPGES, casein kinase II and Hsp90) are mixed at a molar proportion of 1:1:1
-
lipopolysaccharide
-
lipopolysaccharide binds to receptor TLR4 on osteoblasts that directly induces isoform mPGES-1 expression for prostaglandin E2 synthesis, leading to subsequent bone resorption
Tumor necrosis factor alpha
-
increase in protein expression and activity of isoform mPGES-1, accompanied by increased COX-2 expression and production of prostaglandin E2
-
dithiothreitol
leads to dissociation of the bound heme which is hindered by imidazole
GSH
the enzyme activity is increased in the presence of reduced glutathione
GSH
the enzyme activity is increased in the presence of reduced glutathione
GSH
mPGES2 has a GSH-binding motif, the GSH molecule binds at the predicted amino acid residues 148VPxL to 164DSxxI. GSH is essential for heme binding to isozyme mPGES2, structures of GSH-heme complex-binding cavity in isozyme mPGES2, overview
GSH
-
concentrations below 0.5 mM are required for maximal activity of IgG1(hei-26)-reactive protein
GSH
-
two different types of prostaglandin E synthase: 1. GSH-dependent enzyme, 2. GSH-independent enzyme. The genitally organs, especially the deferent duct have mainly GSH-dependent prostaglandin E synthase activity. Heart, spleen and uterus have only the GSH-independent activity. In absence of reduced glutathione the enzyme from deferent duct shows only 3% of the activity in presence of reduced glutathione
interleukin 1beta
-
increase in protein expression and activity of isoform mPGES-1, accompanied by increased COX-2 expression and production of prostaglandin E2
-
interleukin 1beta
induces isoform mPGES-1 and subsequent production of prostaglandin E2, while production of prostaglandin I2 is reduced by increased expression of mPGES-1
-
interleukin 1beta
stimulates release of prostaglandin E2 by myometrical smooth muscle cells and increases COX-2 and mPGES-1 mRNA and protein expression
-
additional information
-
IL-1 administration into the mouse cortex leads to elevated expression of cPGES and an increase in prostaglandin E2
-
additional information
-
mPGES-1 expression is upregulated in COX-1 and COX-2 knock-out cells
-
additional information
-
phosphorylation is crucial for the enzyme's function, phosphorylation by casein kinase II enhances cPGES activity 3fold
-
additional information
-
lipopolysaccharide significantly increases the mRNA level of mPGES-1
-
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.13
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
wild-type, 0°C, pH 7.2
0.734
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
mutant Q134E, 0°C, pH 7.2
1.61
(5Z,13E)-(15S)-9a,11a-epidioxy-15-hydroxyprosta-5,13-dienoate
-
mutant Q36E, 0°C, pH 7.2
0.0024
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
-
0.014
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
-
0.1
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
in the presence of 0.3 mM dodecylmaltoside
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TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
7
(5Z,13E)-(15S)-9alpha,11alpha-epidioxy-15-hydroxyprosta-5,13-dienoate
dodecylmaltoside activated
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0035
(2E)-2-(2,5-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]benzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
(2E)-2-(2,5-bis[[4-(trifluoromethyl)benzyl]oxy]benzylidene)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0034
(2E)-2-[2,5-bis(2-cyclohexylethoxy)benzylidene]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0015
(2E)-2-[2,5-bis(2-phenylethoxy)benzylidene]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
(2E)-2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzylidene]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
(2E)-2-[5-(2-cyclohexylethoxy)-2-[[4-(trifluoromethyl)benzyl]oxy]benzylidene]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0042
(2R)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0046
(2S)-2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000248
(3R)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
Homo sapiens
pH and temperature not specified in the publication
0.000243
(3S)-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)pyrrolidin-3-yl acetate
Homo sapiens
pH and temperature not specified in the publication
0.00372
(4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.000504
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
0.000004
(4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000007
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000012
(4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003
(4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
(4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0051
([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)(5,8-dihydronaphthalen-1-yl)acetic acid
Homo sapiens
-
-
0.01
([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)acetic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000002
1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
Homo sapiens
-
pH and temperature not specified in the publication
0.03
1-[2-(2-methylphenyl)ethyl]-4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.000012
1-[4-[2-(2-carboxy-2-methylpropyl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-4-yl]-2-fluorophenyl]pyridinium
Homo sapiens
-
-
0.000003
1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0022
2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0011
2-(2,3-diphenethoxybenzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000023
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,2-trifluoroethyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000062
2-(2,6-dichloroanilino)-7,7-dimethyl-N-(2,2,3,3,3-pentafluoropropyl)-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000041
2-(2,6-dichloroanilino)-7,7-dimethyl-N-phenyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000017
2-(2,6-dichloroanilino)-7,7-dimethyl-N-[6-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000046
2-(2,6-dichloroanilino)-7-methyl-N-[3-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000094
2-(2,6-dichloroanilino)-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000013
2-(2,6-dichloroanilino)-N-(2,6-dimethylpyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
2-(2,6-dichloroanilino)-N-(2-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000047
2-(2,6-dichloroanilino)-N-(4,4-difluorocyclohexyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000035
2-(2,6-dichloroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000067
2-(2,6-dichloroanilino)-N-(6-methoxypyridin-3-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
2-(2,6-dichloroanilino)-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000039
2-(2-chloro-6-fluoroanilino)-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000077
2-(2-chloro-6-fluoroanilino)-N-(3-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000042
2-(2-chloro-6-fluoroanilino)-N-(4-cyanophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000028
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000022
2-(2-chloro-6-fluoroanilino)-N-(4-fluorophenyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000021
2-(2-chloro-6-fluoroanilino)-N-(5-chloropyridin-2-yl)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000011
2-(2-chloro-6-fluoroanilino)-N-(cyclohexylmethyl)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000008
2-(2-chloro-6-fluoroanilino)-N-[3-fluoro-5-(trifluoromethyl)phenyl]-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2,3-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00002
2-(2-chloro-6-fluoroanilino)-N-[6-(difluoromethoxy)pyridin-3-yl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00066
2-(2-chloro-6-fluorophenyl)-4-(4-chlorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00032
2-(2-chloro-6-fluorophenyl)-4-(4-phenoxyphenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00015
2-(2-chloro-6-fluorophenyl)-4-[4-(2-phenylethyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000008
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylethynyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00018
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0014
2-(2-chloro-6-fluorophenyl)-4-[4-(phenylsulfonyl)phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
2-(2-chloro-6-fluorophenyl)-4-[4-[(E)-2-phenylethenyl]phenyl]-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0024
2-(3,5-diphenethoxybenzyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0028
2-(3,5-diphenethoxybenzylidene)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0037
2-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.0000053
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
0.000676
2-(difluoromethyl)-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000009
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000009
2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00112
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-([[(2R)-2-methylbutanoyl]amino]methyl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00246
2-(difluoromethyl)-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000103
2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]-5-(propanamidomethyl)pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0059
2-([4,6-bis[2-(4-cyanophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-([4,6-bis[2-(4-methoxyphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0009
2-([4,6-bis[2-(4-methylphenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0037
2-([4,6-bis[2-(4-nitrophenyl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0065
2-([4,6-bis[2-(thiophen-3-yl)ethoxy]pyrimidin-2-yl]sulfanyl)hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0039
2-([4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0017
2-([4-chloro-6-[(4'-cyanobiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0021
2-([4-chloro-6-[(5-methoxy-2-methylbiphenyl-4-yl)amino]pyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0013
2-([4-[(biphenyl-4-ylmethyl)amino]-6-chloropyrimidin-2-yl]sulfanyl)nonanoic acid
Homo sapiens
-
-
0.0029
2-([4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0088
2-([4-[3-(2-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(3-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(3-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0094
2-([4-[3-(4-chloro-2-methoxyphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0093
2-([4-[3-(4-methylphenoxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0022
2-([4-[3-(5,6,7,8-tetrahydronaphthalen-1-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.01
2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.000198
2-bromo-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00367
2-chloro-4-fluoro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
2-chloro-4-[(2,2-dimethylpropanamido)methyl]-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-[4-oxo-3-[4-(trifluoromethyl)phenyl]-3,4-dihydrophthalazin-6-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000385
2-chloro-5-[(3,3-dimethylbutanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000157
2-chloro-6-fluoro-N-[3-[4-(trifluoromethyl)anilino][1,2]thiazolo[4,5-b]pyridin-7-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00232
2-chloro-N-(1H-imidazol-2-yl)-4-methyl-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000885
2-chloro-N-(1H-imidazol-2-yl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.0000058
2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-N-[4-(trifluoromethyl)phenyl]-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000082
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-(3-methylbutyl)-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000065
2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-N-[4-(trifluoromethyl)phenyl]-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000157
2-[(3,5-dichloropyridin-4-yl)amino]-N-[(4-fluorophenyl)methyl]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000037
2-[(3,5-dichloropyridin-4-yl)amino]-N-[2-fluoro-4-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000047
2-[(3,5-dichloropyridin-4-yl)amino]-N-[4-fluoro-3-(trifluoromethyl)phenyl]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0046
2-[(3,5-diphenethoxyphenyl)thio]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[(4,6-bis[2-[4-(trifluoromethoxy)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0019
2-[(4,6-bis[2-[4-(trifluoromethyl)phenyl]ethoxy]pyrimidin-2-yl)sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0012
2-[(4,6-diphenethoxypyrimidin-2-yl)thio]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0041
2-[(4-[3-[2-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0027
2-[(4-[3-[3-(propan-2-yl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.002
2-[(4-[3-[3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0017
2-[(4-[3-[4-chloro-3-(trifluoromethyl)phenoxy]propoxy]phenyl)sulfanyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0026
2-[(4-[[3,5-bis(2,2,2-trifluoroethoxy)phenyl]amino]-6-chloropyrimidin-2-yl)sulfanyl]nonanoic acid
Homo sapiens
-
-
0.0039
2-[2,3-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[2,4-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0024
2-[2,5-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.00018
2-[2-(2-chloro-6-fluorophenyl)-4-[6-(phenylethynyl)pyridin-3-yl]-1H-imidazol-5-yl]ethanol
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethoxy)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000006
2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]pyridine-3-carboxylic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
2-[2-[(1S,2S)-2-([1-[5-(trifluoromethyl)pyridin-2-yl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
2-[2-[(1S,2S)-2-[[1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.0027
2-[3,4-bis(2-phenylethoxy)benzyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0006
2-[3,5-bis(2-phenylethoxy)phenoxy]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[3-(aminooxy)-2,2-dimethyl-3-oxopropyl]-3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indole
Homo sapiens
-
IC50: 0.01 mM
0.0014
2-[4-(4-bromophenyl)-1H-imidazol-2-yl]benzonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
2-[4-(4-chlorophenyl)-1H-imidazol-2-yl]-3-fluorobenzonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.005
2-[4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)phenyl]propan-2-ol
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.0071
2-[4-[3-(2,3-dimethylphenoxy)propoxy]benzyl]hexanoic acid
Homo sapiens
-
in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0000009
2-[6-(2-cyclopropylethoxy)-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.006
2-[6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl] acetic acid
Homo sapiens
-
-
0.0000009
2-[6-bromo-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.0000009
2-[6-chloro-9-(3-hydroxy-3-methylbut-1-yn-1-yl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.0000007
2-[6-chloro-9-(3-hydroxy-3-methylbutyl)-1H-phenanthro[9,10-d]imidazol-2-yl]benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.01
2-[[4,6-bis(2-cycloheptylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0024
2-[[4,6-bis(2-cyclohexylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4,6-bis(2-cyclopentylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0096
2-[[4,6-bis(2-cyclopropylethoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0073
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]butanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.002
2-[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]octanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4,6-bis(3-methylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0022
2-[[4,6-bis(3-phenylpropoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0009
2-[[4,6-bis(4-phenylbutoxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.0038
2-[[4,6-bis(benzyloxy)pyrimidin-2-yl]sulfanyl]hexanoic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
2-[[4-(3-phenoxypropoxy)phenyl]sulfanyl]hexanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0016
2-[[4-(biphenyl-4-ylamino)-6-chloropyrimidin-2-yl]sulfanyl]nonanoic acid
Homo sapiens
-
-
0.00323
3,4-bis-(3-benzo[b]thiophen-3-yl-phenyl)-5-hydroxy-5H-furan-2-one
Mus musculus
-
0.00011
3-(4-bromophenyl)-5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazole
Homo sapiens
-
pH and temperature not specified in the publication
0.0021
3-(naphthalen-1-ylamino)-6-nitrobenzo[d]isothiazole 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.00029
3-[(5E)-3-(4-butylbenzyl)-1-(4-chlorobenzyl)-4-methylidene-5-[(2E)-4-methylpent-2-en-1-ylidene]-4,5-dihydro-1H-pyrrol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00029 mM
0.00025
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00025
3-[1-(4-chlorobenzyl)-3-(3,3-dimethylbutanoyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00025 mM
0.0032
3-[1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0032 mM
0.0011
3-[1-(4-chlorobenzyl)-3-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0011 mM
0.0006
3-[1-(4-chlorobenzyl)-3-methyl-5-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00060 mM
0.0043
3-[1-(4-chlorobenzyl)-3-methyl-7-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0043 mM
0.002
3-[1-(4-chlorobenzyl)-3-t-butyl-thio-5-isopropylindol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000004
3-[1-(4-chlorobenzyl)-4-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000008
3-[1-(4-chlorobenzyl)-4-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000022
3-[1-(4-chlorobenzyl)-4-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000005
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000003
3-[1-(4-chlorobenzyl)-4-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000007
3-[1-(4-chlorobenzyl)-4-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00065
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenoxy-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00065 mM
0.0064
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-phenyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0064 mM
0.0009
3-[1-(4-chlorobenzyl)-5-(1-methylethyl)-3-[(2-methylphenyl)carbonyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00090 mM
0.000004
3-[1-(4-chlorobenzyl)-5-(2'-chloro-2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000004 mM
0.000008
3-[1-(4-chlorobenzyl)-5-(2,2'-difluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000008 mM
0.000022
3-[1-(4-chlorobenzyl)-5-(2-chlorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000022 mM
0.000005
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methoxybiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000005 mM
0.000003
3-[1-(4-chlorobenzyl)-5-(2-fluoro-2'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000003 mM
0.000033
3-[1-(4-chlorobenzyl)-5-(2-fluoro-3'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000033 mM
0.000031
3-[1-(4-chlorobenzyl)-5-(2-fluoro-4'-methylbiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000031 mM
0.000007
3-[1-(4-chlorobenzyl)-5-(2-fluorobiphenyl-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000007 mM
0.000012
3-[1-(4-chlorobenzyl)-5-(3-fluoro-4-pyridin-3-ylphenyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000012 mM
0.0026
3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0026 mM
0.000006
3-[1-(4-chlorobenzyl)-5-[2-fluoro-2'-(phenylcarbonyl)biphenyl-4-yl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000006 mM
0.000032
3-[1-(4-chlorobenzyl)-5-[3-fluoro-4-(pyrimidin-5-ylmethyl)phenyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000032 mM
0.0016
3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
i.e. 3-[1-(p-chlorobenzvl)-5-isopropyl-3-tert-butylthioindol-2-yl]-2,2-dimethylpropanoic acid or FLAP, formerly designated L-663,536, a lipoxygenase inhibitor, IC50: 0.0016 mM
0.00006
3-[3-(benzylsulfanyl)-1-(4-chlorobenzyl)-5-[4-[(4-chloro-2-fluorophenyl)ethynyl]phenyl]-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.0021
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.0024
3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(propan-2-yl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.01
3-[3-(tert-butylsulfanyl)-1-methyl-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.01 mM
0.0032
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-(3-phenylpropyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0032 mM
0.0067
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1-prop-2-en-1-yl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.0067 mM
0.01
3-[3-(tert-butylsulfanyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.01 mM
0.00026
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-4-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.00026
3-[3-[(tert-butylsulfanyl)acetyl]-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00026 mM
0.000006
3-[4-(2'-acetyl-2-fluorobiphenyl-4-yl)-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.000016
3-[4-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
-
0.01
3-[4-[3-(2,3-dimethylphenoxy)propoxy]phenyl]propanoic acid
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.00016
3-[5-biphenyl-3-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00016 mM
0.000016
3-[5-biphenyl-4-yl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.000016 mM
0.00033
3-[5-tert-butyl-1-(4-chlorobenzyl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
-
IC50: 0.00033 mM
0.000007
3-[6-([1,1'-biphenyl]-4-yl)-1-[(4-chlorophenyl)methyl]-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoic acid
Homo sapiens
pH and temperature not specified in the publication
0.03
4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-3-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-ol
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4'-[1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazol-4-yl]biphenyl-4-amine
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-(2'-[[2-chloro-5-(trifluoromethyl)phenoxy]methyl]biphenyl-4-yl)-1-[2-(2-methylphenyl)ethyl]-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.00459
4-(4'-butyl-biphenyl-4-yl)-3-(4-butyl-phenyl)-5-hydroxy-5H-furan-2-one
Mus musculus
-
0.03
4-(4'-phenoxybiphenyl-4-yl)-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.00057
4-(4-benzylphenyl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.00039
4-(4-chlorobenzyl)-2,6-bis[4-(trifluoromethoxy)phenyl]-4H-thieno[3,2-b]pyrrole
Homo sapiens
-
-
0.00011
4-(biphenyl-4-yl)-2-(2-chloro-6-fluorophenyl)-1H-imidazole
Homo sapiens
-
pH and temperature not specified in the publication
0.005
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzamide
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.005
4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzoic acid
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.000043
4-chloro-2-([[(1S,2S)-2-(2,2-dimethylpropanamido)cyclopentyl]methyl]amino)benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000004
4-chloro-2-([[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methyl]amino)benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
4-chloro-2-[([(1S,2S)-2-[(1-phenylpiperidine-4-carbonyl)amino]cyclopentyl]methyl)amino]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-chloro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000002
4-chloro-2-[[(1R,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]methoxy]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-fluoro-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.000001
4-methyl-2-[2-[(1S,2S)-2-([1-[4-(trifluoromethyl)phenyl]piperidine-4-carbonyl]amino)cyclopentyl]ethyl]benzoic acid
Homo sapiens
pH and temperature not specified in the publication
0.03
4-[(4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1H-1,2,3-triazol-1-yl)sulfonyl]benzoic acid
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[2'-[(naphthalen-1-yloxy)methyl]biphenyl-4-yl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[4-(phenanthren-9-yl)phenyl]-1-(3-phenylpropyl)-1H-1,2,3-triazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.03
4-[4-benzyl-1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-5-yl]benzaldehyde
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.0032
4-[[4-(biphenyl-4-yl)-1H-1,2,3-triazol-1-yl]methyl]-3-nitrobenzoic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.03
5-(4-bromophenyl)-3-(2-chloro-6-fluorophenyl)-1,2,4-oxadiazole
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.000074
5-(acetamidomethyl)-2-(difluoromethyl)-N-[4-methyl-5-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.03
5-(dimethylamino)-N-[4'-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]biphenyl-4-yl]naphthalene-1-sulfonamide
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.00084
5-hydroxy-3-naphthalen-2-yl-4-(3-naphthalen-2-yl-phenyl)-5H-furan-2-one
Mus musculus
-
0.00108
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-(trifluoromethyl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00311
5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)-2-methylbenzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.00094
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(1,3-thiazol-2-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000013
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohex-1-en-1-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclohexylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00017
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(cyclopropylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000023
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00048
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(pyridin-3-ylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-ethynylpyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(2-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(3-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000031
5-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-[(4-chlorophenyl)ethynyl]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.00002
5-[2-(2-chloro-6-fluorophenyl)-5-methyl-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000016
5-[5-(2-chloro-6-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
5-[5-bromo-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000005
5-[5-chloro-2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]-2-(phenylethynyl)pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.0067
6-nitro-3-(m-tolylamino) benzo[d]isothiazole 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0236
6-nitro-N-phenyl-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
6-nitro-N-[3-(propan-2-yl)phenyl]-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0011
7-hydroxy-N,N'-bis(2,4,6-trimethylphenyl)naphthalene-1,3-disulfonamide
Homo sapiens
-
-
0.005
aminomethyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.01
ethyl 2-([4-[3-(quinolin-6-yloxy)propoxy]phenyl]sulfanyl)hexanoate
Homo sapiens
-
IC50 above 0.01 mM, in 0.1 M potassium phosphate buffer, pH 7.4, at 4°C
0.0056
ethyl 2-[[4-chloro-6-(quinolin-6-ylamino)pyrimidin-2-yl]sulfanyl]nonanoate
Homo sapiens
-
-
0.0072
methyl 3-[3-(tert-butylsulfanyl)-1-(4-chlorobenzyl)-5-(1-methylethyl)-1H-indol-2-yl]-2,2-dimethylpropanoate
Homo sapiens
-
IC50: 0.0072 mM
0.005
methyl 4-([4-[2-(2-chloro-6-fluorophenyl)-1H-imidazol-4-yl]phenyl]ethynyl)benzenesulfinate
Homo sapiens
-
IC50 above 0.005 mM, pH and temperature not specified in the publication
0.0000017
methyl 4-[6-bromo-2-(2-chloro-6-fluorophenyl)-1H-phenanthro[9,10-d]imidazol-9-yl]but-3-ynoate
Homo sapiens
-
-
0.05
N-(1,3-benzodioxol-4-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(2-methylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.000016
N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-1,1-dioxo-1,2-dihydro-1lambda~6~,2-benzothiazine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.05
N-(3,4-dimethoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(3-bromobenzyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°Cn
0.0073
N-(3-bromophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0057
N-(3-chlorophenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0088
N-(3-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(3-tert-butylphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.000004
N-(4-chloro-2-fluorophenyl)-2-[2,6-dichloro-3-[(2,2-dimethylpropanamido)methyl]anilino]-6-(2,2-difluoroethoxy)-1-methyl-1H-benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0169
N-(4-methoxyphenyl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(5-bromonaphthalen-1-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.00015
N-(6-nitro-1,1-dioxido-1,2-benzothiazol-3-yl)quinolin-5-amine
Homo sapiens
-
0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.05
N-(biphenyl-3-yl)-6-nitro-1,2-benzothiazol-3-amine 1,1-dioxide
Homo sapiens
-
above, 0.1 M potassium phosphate buffer, pH 7.4, 4°C
0.0000022
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000013
N-(cyclohexylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000023
N-(cyclopentylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
N-(cyclopropylmethyl)-2-(2,6-dichloroanilino)-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000025
N-(cyclopropylmethyl)-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000026 - 0.000058
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
0.000481
N-([4-chloro-3-[7-chloro-4-oxo-6-(pyridin-4-yl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000713
N-([4-chloro-3-[7-chloro-6-(4-hydroxypiperidin-1-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000261
N-([4-chloro-3-[7-chloro-6-(morpholin-4-yl)-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000026
N-cyclohexyl-2-(2,6-dichloroanilino)-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000063
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7,7-dimethyl-7,8-dihydro-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000012
N-cyclohexyl-2-[(3,5-dichloropyridin-4-yl)amino]-7-methyl-1H-furo[3,2-e]benzimidazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
N-tert-butyl-1-(7-chloro-2-[2-chloro-5-[(2-methylpropanamido)methyl]phenyl]-4-oxo-3,4-dihydroquinazolin-6-yl)azetidine-3-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000055
N-[(4-chloro-3-[4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005 - 0.000007
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
0.000074
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)piperidin-1-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000016
N-[(4-chloro-3-[4-oxo-7-[6-(trifluoromethyl)pyridin-3-yl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000036
N-[(4-chloro-3-[7-chloro-4-oxo-6-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000024
N-[(4-chloro-3-[7-chloro-6-[4-(difluoromethyl)piperidin-1-yl]-4-oxo-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
N-[(6-chloro-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000179
N-[3-(4-bromophenyl)-4-oxo-3,4-dihydrophthalazin-6-yl]-2-chloro-6-fluorobenzamide
Homo sapiens
pH and temperature not specified in the publication
0.0013
N-[4-chloro-3-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-2-(trifluoromethyl)benzamide
Homo sapiens
-
-
0.000003
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
N-[5-(4-chlorophenyl)-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000003
N-[5-(4-chlorophenyl)-4-methyl-1H-imidazol-2-yl]-2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]pyridine-3-carboxamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000036
N-[[3-(7-bromo-4-oxo-3,4-dihydroquinazolin-2-yl)-4-chlorophenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000042
N-[[4-chloro-3-(7-chloro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000032
N-[[4-chloro-3-(7-chloro-6-cyclopropyl-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000111
N-[[4-chloro-3-(7-chloro-6-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000304
N-[[4-chloro-3-(7-methoxy-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000063
N-[[4-chloro-3-(7-nitro-4-oxo-3,4-dihydroquinazolin-2-yl)phenyl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000004
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydropyrido[4,3-d]pyrimidin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000006
N-[[6-(difluoromethyl)-5-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]pyridin-3-yl]methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.0000195
sodium 3-[1-[(4-chlorophenyl)methyl]-5-(2-fluoro[1,1'-biphenyl]-4-yl)-3-methyl-1H-indol-2-yl]-2,2-dimethylpropanoate
Homo sapiens
-
at pH 7.0 and 25°C
0.03
[1-[(phenylsulfanyl)methyl]-1H-1,2,3-triazol-4-yl]methyl benzoate
Homo sapiens
-
IC50 above 0.03 mM, pH and temperature not specified in the publication
0.0012
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl](phenyl)acetic acid
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.01
[[4,6-bis(2-phenylethoxy)pyrimidin-2-yl]sulfanyl]acetic acid
Homo sapiens
-
IC50 above 0.01 mM, in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000001
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000504
(4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
-
-
0.000001
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0000053
2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile
Homo sapiens
-
at pH 7.0 and 25°C
0.000241
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
-
at pH 7.0 and 25°C
0.000241
2-chloro-5-[(2,2-dimethylpropanamido)methyl]-N-(1H-imidazol-2-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
Homo sapiens
-
wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.00059
2-chloro-N-[3-(naphthalen-1-ylcarbamoyl)phenyl]benzamide
Rattus norvegicus
-
mutant enzyme V131T/F135L/F138A, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.0024
MK-886
Homo sapiens
-
in potassium phosphate buffer (0.1 M, pH 7.4) containing 2.5 mM glutathione, at 4°C
0.000026
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000058
N-([4-chloro-3-[4-oxo-7-(trifluoromethyl)-3,4-dihydroquinazolin-2-yl]phenyl]methyl)-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000005
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
0.000007
N-[(4-chloro-3-[4-oxo-7-[4-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-2-yl]phenyl)methyl]-2-methylpropanamide
Homo sapiens
pH and temperature not specified in the publication
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.054
-
mutant enzyme T131V/L135F/A138F, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.059
-
wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.086
-
mutant enzyme V131T/F135L/F138A, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
0.214
-
wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4, 2.5 mM glutathione, at 4°C
100 - 200
-
in the presence of 0.4 mM prostaglandin H2 or prostaglandin G2 and 2.5 mM glutatione
510
-
in the presence of 10 microM prostaglandin H2 or prostaglandin G2 and 2.5 mM glutatione
additional information
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.2
7.4
7.4
-
microsomal membranes are incubated with PGH2, enzyme activity assay
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5 - 10
-
pH 5: about 75% of maximal activity, pH 10: about 70% of maximal activity, GSH-dependent enzyme from deferent duct
5 - 12
-
pH 5: about 60% of maximal activity, pH 9: about 75% of maximal activity, pH 12: about 90% of maximal activity, GSH-independent enzyme from heart
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
microsomal suspension is incubated on ice with PGH2, enzyme activity assay
additional information
-
microsomal suspension is incubated on ice with PGH2, enzyme activity assay
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TEMPERATURE RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
660669, 662071, 662700, 662768, 663051, 670732, 677444, 678094, 678432, 678584, 681868, 690320, 690622, 691476, 692090
-
-
brenda
women undergoing treatment for infertility, isozymes mPGES-2, mPGES-1, and cPGES
-
-
brenda
cPGES; cynomologus macaque, adult female, isozyme cPGES
SwissProt
brenda
mPGES-1; cynomologus macaque, adult female, isozyme mPGES-1
SwissProt
brenda
mPGES-2, truncated form; cynomologus macaque, adult female, isozyme mPGES-2
SwissProt
brenda
-
691635, 692588, 693501, 694941, 694942, 702146, 702949, 703978, 705284, 706576, 713719, 714401, 714944, 716081, 716814, 746707, 747229, 748296
-
-
brenda
at least 2 different proteins with PGE-PGH isomerase activity: IgG1(hei-7)-reactive protein and IgG1(hei-26)-reactive protein
-
-
brenda
-
3133, 3134, 3135, 660669, 660973, 662071, 663277, 702165, 702949, 705284, 715541, 716814, 747229, 749371
-
-
brenda
after induction of acid reflux oesophagitis. Expression of COX-2 and enzyme isoform mPGES-1 are markedly increased in oesophagitis and co-localize in epithelial cells of the basal layer, as well as inflammatory and mesenchymal cells in the lamina propria and submucosa
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
-
brenda
-
in normal breast the enzyme is seen in myoepithelial cells and in stromal fibroblasts and vascular smooth muscle, in breast disease, the enzyme is observed in epithelial cells adjacent to cancer, in scattered foci of fibrocystic disease, in ductal carcinoma in situ and in invasive cancers, in addition to myoepithelial cells
brenda
-
extravillous cytotrophoblast is strongly posistive for enzyme protein in the basal plate
brenda
expression of the primary form of PGES, mPGES-1
brenda
-
mesenchymal cells of the basal layer, co-localization of isoform mPGES-1 and COX-2 after induction of oesophagitis
brenda
-
peripheral blood monocyte, no basal expression of enzyme, but strong induction of expression by proinflammatory stimulation via LPS. In alternatively activated M2 monocytes-macrophages, interleukins IL-4, IL-13, and to a lesser extent, IL-10 or interferon IFN-gamma inhibit LPS-induced expression of enzyme. Induction of enzyme expression correlates with changes at the protein level and production of prostaglandin E2
brenda
-
only isoform mPGES-1 can be found in neutrophils, it co-localizes with COX-2 and its expression is mainly constitutive
brenda
at 24 h after fertilization, endothelial cells of the pharyngeal arch vasculature
brenda
-
enzyme protein is prominent in vesicles separating from syncytiotrophoblast into the intervillous space
brenda
-
constitutive expression of enzyme is associated with increased prostaglandin E2 production and stimulation of growth. Inhibition of enzyme activity and expression block the release of prostaglandin E2 and decrease cellular proliferation. Antiproliferative effects may be overcome by exogenous prostaglandin E2
brenda
-
enzyme protein is elevated in the endometrium during spontaneous term labour and after estradiol treatment. Enzyme is localized to endometrial stromal cells
brenda
additional information
-
in brain mPGES-2 is detected in neurons, activated microglia, and endothelium, but not in resting microglia, astrocytes, or smooth muscle cells
brenda
-
weak enzyme expression, in the tubular epithelial cells of the caput and cauda
brenda
-
from women undergoing treatment for infertility, expression of mPGES-2, mPGES-1, and cPGES
brenda
-
in the tubular epithelial cells of the caput and cauda
brenda
-
epithelial cells of the basal layer, co-localization of isoform mPGES-1 and COX-2 after induction of oesophagitis
brenda
both microsomal enzyme immunostaining and mRNA, enzyme is induced by equine and human chorionic gonadotropin treatment
brenda
-
mPGES-2 colocalizedswith microglia in activated (amoeboid-shaped) cells
brenda
isoform mPGES-1 localizes mostly in myometrial and vascular smooth muscle cells of pregnant women. Isoform cPGES is diffusely located throughout the myometrium. Expression of COX-2 and isoform mPGES-1 mRNA with term labour, whereas cPGES expression does not change. Interleukin 1beta stimulates release of prostaglandin E2 by myometrical smooth muscle cells and increases COX-2 and mPGES-1 mRNA and protein expression
brenda
isoform mPGES-2 protein is largely in stromal cells surrounding smooth vascular muscle. Expression of mPGES-2 mRNA increases with term labour and preterm labour
brenda
exclusive localization of cytosolic enzyme, no obvious effect of treatment with equine chorionic gonadotropin on mRNA or protein level
brenda
prostaglandin E synthases are mostly concentrated in the oviductal epithelial layer and primarily expressed in the ampulla section of the oviduct and to a lesser extent in the isthmus and the isthmic-ampullary junction
brenda
prostaglandin E synthases are mostly concentrated in the oviductal epithelial layer and primarily expressed in the ampulla section of the oviduct and to a lesser extent in the isthmus and the isthmic-ampullary junction, the mPGES-1 protein is highly expressed in the contralateral oviduct
brenda
prostaglandin E synthases are mostly concentrated in the oviductal epithelial layer and primarily expressed in the ampulla section of the oviduct and to a lesser extent in the isthmus and the isthmic-ampullary junction, the mPGES-2 is mostly expressed in the ipsilateral oviduct
brenda
-
immunolocalized in extravillous trophoblasts and macrophages, in early gestation also in cytotrophoblasts and syncytiotrophoblasts
brenda
-
immunolocalized to the fibroblasts and macrophages in villous stroma, also in apoptotic early gestational syncytiotrophoblasts
brenda
-
application of glucocorticoids to mother or fetus significantly stimulate enzyme isoform mPGES1 in placenta. Enzyme is localized to placental trophoblast cells
brenda
-
weak enzyme expression, Leydig cells, Sertoli cells, seminiferous tubules
brenda
-
in the epithelium from the proximal segment to the distal portion of the vas deferens and ampulla
brenda
-
strong enzyme expression, in the epithelium from the proximal segment to the distal portion of the vas deferens and ampulla
brenda
cells express both microsomal isoforms mPGES-1 and mPGES-2 and cytosolic isoform cPGES
brenda
cells express both microsomal isoforms mPGES-1 and mPGES-2 and cytosolic isoform cPGES. Isoform mPGES-1 contributes most to total activity and is induced by interleukin IL-1beta, which in turn reduces the ability of cells to produce prostaglandin I2
brenda
additional information
-
endometrium, located in epithelial, glandular and stromal cells
brenda
additional information
endometrium, located in epithelial, glandular and stromal cells
brenda
additional information
endometrium, located in epithelial, glandular and stromal cells
brenda
additional information
-
in patients with rheumatoid arthritis, the protein is overexpressed in synovial tissue, particularly by macrophages and fibroblasts in the synovial lining layer
brenda
additional information
tissue distribution of isozme expression, overview
brenda
additional information
tissue distribution of isozme expression, overview
brenda
additional information
tissue distribution of isozme expression, overview
brenda
additional information
tissue distribution of isozyme expression, overview
brenda
additional information
tissue distribution of isozyme expression, overview
brenda
additional information
tissue distribution of isozyme expression, overview
brenda
additional information
abundant tissue distribution of isozyme mPGES2
brenda
additional information
protein expression occurs in luminal epithelial and stromal cells around the implanting blastocyst on day 5 of pregnancy, with the progression of implantation to day 6, the protein is mainly expressed in the cells of the primary decidual zone
brenda
additional information
no microsomal enzyme immunostaining or mRNA in thecal cell or oocyte
brenda
additional information
-
no microsomal enzyme immunostaining or mRNA in thecal cell or oocyte
brenda
additional information
-
the enzyme expression is altered in rats with nephrogenic and central diabetes insipidus, expression overview
brenda
additional information
endometrium, mainly in luminal and glandular epithelium, higher levels of PGES-1 mRNA occur during pregnancy on days 10-11 when compared with days 12-17, intermediate levels of PGES-1 protein are observed on days 10-13, afterwards, PGES-1 mRNA and protein expression decrease, followed by an increase from days 18-19 or 22-23 of pregnancy, highest mRNA and protein levels are reached on days 24-25
brenda
additional information
-
endometrium, mainly in luminal and glandular epithelium, higher levels of PGES-1 mRNA occur during pregnancy on days 10-11 when compared with days 12-17, intermediate levels of PGES-1 protein are observed on days 10-13, afterwards, PGES-1 mRNA and protein expression decrease, followed by an increase from days 18-19 or 22-23 of pregnancy, highest mRNA and protein levels are reached on days 24-25
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
cPGES is directly associated with and phosphorylated by casein kinase 2, cPGES, casein kinase 2 and Hsp90 form a stoichiometric complex of 1:1:1 immediately after cell activation, Hsp90 acts as an essential scaffold protein that brings cPGES and casein kinase 2 in proximity, thereby allowing their efficient functional interaction under physiological condition
-
brenda
membrane-associated prostaglandin E synthase-2
brenda
-
-
-
652244, 652399, 662768, 663051, 667959, 668886, 670732, 678444, 678584, 681044, 690320, 690622, 693823, 702165, 702622, 706521, 715541, 715856, 715865, 747278, 748368, 748441, 748542, 748846
brenda
-
-
-
brenda
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
evolution
microsomal prostaglandin E2 synthase belongs to the MAPEG superfamily
malfunction
-
baseline blood pressures are significantly higher in mPGES1-deficientanimals than wild type controls
malfunction
-
mPGES-1-deficient mice exhibit significantly less neuronal loss induced by kainic acid
malfunction
-
small interfering RNA silencing of mPGES-1 in Lewis lung carcinoma cells decreases prostaglandin E2 synthesis markedly, accompanied by reduced cell proliferation, attenuated Matrigel invasiveness and increased extracellular matrix adhesion, while mPGES-1-overexpression shows increased proliferating and invasive capacities
malfunction
-
the deletion of mPGES-1 in mice results in increased prostacyclin I2 formation and marginal effects on the circulatory prostaglandin E2 level. Loss of mPGES-1 results in increased prostacyclin I2 formation, and in contrast to inhibition of prostacyclin I2, without worsening acute cardiac ischemic injury
malfunction
-
embryonic fibroblasts deficient in cPGES/p23 decrease the expression of the prostaglandin E2 degrading enzyme, 15-hydroxyprostaglandin dehydrogenase, which catalyzes the inactivating conversion of the PGE2 15-OH to a 15-keto group
malfunction
-
fibroblasts deficient in cPGES/p23 decrease the expression of the prostaglandin E2 degrading enzyme, 15-hydroxyprostaglandin dehydrogenase, which catalyzes the inactivating conversion of the PGE2 15-OH to a 15-keto group
malfunction
-
mPGES-1 knockdown delays tumor formation and reduced tumor weight in human cholangiocarcinoma tissue
malfunction
-
PGES-1-deficient mice exhibit reduced tumor growth in bone marrow and significantly fewer spontaneous flinches and their onset is several days later compared to wild type mice
malfunction
-
the expression of vascular endothelial growth factor A is significantly reduced in mPGES-1-deficient endometrial tissues implanted into mPGES-1-deficient mice at days 14 and 28
malfunction
-
the healing of acetic acid-induced gastric ulcers is significantly delayed in mPGES-1 knockout mice compared with wild type. This is accompanied with reduced angiogenesis in ulcer granulation tissues. The mRNA levels of proangiogenic growth factors, such as transforming growth factor-beta, basic fibroblast growth factor, and connective tissue growth factor are reduced in mPGES-1 knockout mice compared with wild type
metabolism
-
mPGES-1 is a rate-limiting enzyme that is coupled with cyclooxygenase-2 in the synthesis of prostaglandin E2
metabolism
-
the prostaglandin E2-inactivating pathway is controlled by cPGES/p23
metabolism
-
the prostaglandin E2-inactivating pathway is controlled by cPGES/p23
metabolism
-
the enzyme is involved in the activation of extracellular signal regulated kinase to promote c-Fos expression
metabolism
-
the enzyme is involved in the activation of extracellular signal regulated kinase to promote c-Fos expression
physiological function
-
microsomal prostaglandin E synthase-1 and cyclooxygenase-2 are co-induced by excess glutamate in ischaemic brain. mPGES-1 activity is required for cyclooxygenase-2 to cause neuronal damage in ischaemic injury
physiological function
-
microsomal prostaglandin E synthase-1 and cyclooxygenase-2 are co-induced by excess glutamate in ischaemic brain. mPGES-1 activity is required for cyclooxygenase-2 to cause neuronal damage in ischaemic injury
physiological function
-
the enzyme is responsible for prostaglandin E2 synthesis in inflammation-associated pathologies
physiological function
-
the enzyme is responsible for prostaglandin E2 synthesis in inflammation-associated pathologies
physiological function
-
microsomal prostaglandin E synthase-1 enhances bone cancer growth and bone cancer-related pain behaviors in mice
physiological function
-
mPGES-1 enhances the gastric ulcer-healing processes and the angiogenesis indispensable to gastric ulcer healing
physiological function
-
mPGES-1 regulates growth of endometrial tissues and angiogenesis
physiological function
-
overexpression of mPGES-1 in human cholangiocarcinoma cells increases tumor cell proliferation, migration, invasion, and colony formation. mPGES-1 inhibits the expression of phosphatase and tensin homologue deleted on chromosome 10 (PTEN), leading to activation of the epidermal growth factor/phosphoinositide 3-kinase/AKT/mammalian target of rapamycin signaling pathways in cholangiocarcinoma cells
physiological function
-
microsomal prostaglandin E synthase-1 protects against Fas-induced liver injury and enhances epidermal growth factor receptor/Akt signaling
physiological function
-
the enzyme plays a critical role in the continuous suppression of motor function in the post-bowel obstruction state
additional information
-
the electron-sharing network of the Bombyx mori enzyme includes Asn95, Asp96, and Arg98, the residues contribute to catalytic activity. The C-terminal domain contains the binding site for hydrophobic substrate and PGH2, active site and substrate binding site structures, overview
additional information
the isozyme mPGES-1 structure reveals three well-defined active site cavities within the membrane-spanning region in each monomer interface of the trimeric structure. An important determinant of the active site cavity is a small cytosolic domain inserted between transmembrane helices I and II. A a 16-A-deep cone-shaped cavity extending from the cytosolic side into the membrane-spanning region might have a potential role in substrate access. Serine 127 plays a role in the catalytic mechanism, active site structure, overview
additional information
-
the isozyme mPGES-1 structure reveals three well-defined active site cavities within the membrane-spanning region in each monomer interface of the trimeric structure. An important determinant of the active site cavity is a small cytosolic domain inserted between transmembrane helices I and II. A a 16-A-deep cone-shaped cavity extending from the cytosolic side into the membrane-spanning region might have a potential role in substrate access. Serine 127 plays a role in the catalytic mechanism, active site structure, overview
Show AA Sequence and Transmembrane Helices (1790 entries)
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
16000
17000
17500
18000
215000
-
gradient centrifugation, density equilibrium centrifugation, gel filtration
33000
45000
-
trimer, determined by SDS-PAGE and Western blot analysis, crosslinked subunits
33000
-
dimer, determined by SDS-PAGE and Western blot analysis, crosslinked subunits
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
dimer
homotrimer
trimer
additional information
?
-
8 different subunits detected by SDS-PAGE, activity resides mainly in subunit H, MW 25700
?
x * 39000, N-terminally truncated His6-tagged enzyme, SDS-PAGE
?
x * 39000, N-terminally truncated His6-tagged enzyme, SDS-PAGE
trimer
-
3 * ?, gradient centrifugation, density equilibrium centrifugation, gel filtration
trimer
-
trimeric state characterized by chemical cross-linking with glutaraldehyde
additional information
-
the N-terminal domain contains the GSH-binding site (G-site), and the C-terminal domain contains the binding site for hydrophobic substrate and PGH2
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CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purified enzyme in complex with glutathione sulfonic acid, sitting drop vapor diffusion method, mixing of 10 mg/ml protein in 20 mM Tris-HCl , pH 8.5, and 0.2 M NaCl with 0.1 M HEPES, pH 7.5, 30% PEG 400 w/v, and 20% 1,2-propanediol v/v, in a 1:1 or 1:2 ratio, X-ray diffraction structure determination and analysis at 1.37 A resolution, molecular replacement
-
purified recombinant microsomal isozyme PGE2 synthase-1, in presence of beta-octyl-glycoside and GSH or 1-(4-phenylphenyl)-2-(S-glutathionyl)-ethanone (bis-phenyl-GSH), hanging drop vapor diffusion method, the reservoir solutions used contain 100 mM CAPSO, pH 9.5, 30% PEG 400, 100 mM NaCl, and 100 mM Li2SO4 (mersalyl acid soak and bis-phenyl-GSH complex) or 100 mM Tris, pH 8.0-8.5, 30% PEG400, 100 mM NaCl, and 1 mM TCEP (native GSH complex), 4°C, X-ray diffraction structure determination and analysis at 1.2 A resolution
red-coloured protein purified after growth of Escherichia coli in LB medium containing delta-aminolevulinate and Fe(NO3)3. Enzyme contains bound glutathione and heme
-
the structure of human MPGES1 is determined in complex with the tripeptide gamma-L-glutamyl-L-cysteinyl-glycine, glutathione, at 3.5 A in-plane resolution using electron crystallography
three-dimensional model of substrate-domain and its binding with subsrtates prostaglandin H2 and glutathione. Residue Y130 plays a key role in binding with prostaglandin H2 and in the catalytic process. R110 and T114 interact intensively with the carbonyl tail of prostaglandin H2, whereas Q36 and Q134 only enhance the prostaglandin H2 binding affinity. Prostaglandin H2 interacts with glutathione through hydrogen binding between the peroxy group of prostaglandin H2 and the -SH group of glutathione
-
threedimensional structural model of binding with inhibitors, quantitative structure-activity correlation
-
purified recombinant His-tagged truncated mPGES-2, complexed with anti-inflammatory drug IMN, 10 mg/ml protein in 1.7 M ammonium sulfate, 0.1 M sodium acetate-HCl, pH 5.5, and 1.5 mM indomethacin, sitting drop vapour diffusion method, 3 days, 22°C, X-ray diffraction structure determinationand analysis at 2.6 A resolution, modeling
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
N96A
-
site-directed mutagenesis, the mutant shows reduced isomerase activity compared to the wild-type enzyme
D49N
the mutant shows severely reduced activity compared to the wild type enzyme
H72A
R126A
R126K
the mutant shows severely reduced activity compared to the wild type enzyme
R126Q
R70A
R70A/R122A
the mutant shows increased Km compared to the wild type enzyme, the double mutant of the mPGES-1 significantly reduces the binding affinity of GSH
S127A
T131V/L135F/A138F
-
the mutant shows bout 4fold reduced specific activity towards prostaglandin H2 compared to the wild type enzyme and is not inhibited by 1-C-(2-chlorobenzene)-3-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide
Y117A
Y117F
Y130I
C-delta-35
-
35-amino acid COOH-terminal deletion, diminishes association of the enzyme with membranes
V131T/F135L/F138A
-
the mutant shows bout 4fold increased specific activity towards prostaglandin H2 compared to the wild type enzyme and is inhibited by 1-C-(2-chlorobenzene)-3-N-(naphthalen-1-yl)benzene-1,3-dicarboxamide
C-delta-35
-
35-amino acid COOH-terminal deletion, diminishes association of the enzyme with membranes
additional information
R126A
mutant, exhibits a glutathione-dependent reductase activity, which allows conversion of prostaglandin H2 into prostaglandin F2alpha
R126A
-
the mutation of the enzyme abolishes its PGES activity to exhibit a novel glutathione-dependent reductase activity
R126Q
mutant, exhibits a glutathione-dependent reductase activity, which allows conversion of prostaglandin H2 into prostaglandin F2alpha
R126Q
-
the mutation of the enzyme abolishes its PGES activity to exhibit a novel glutathione-dependent reductase activity
R126Q
the mutant shows severely reduced activity compared to the wild type enzyme
Y117F
the mutant still maintains full catalytic activity relative to the wild type
additional information
-
knockdown of isoform mPGES-1 by siRNA results in downregulation of cytokine-induced mPGES-1 protein expression and activity. siRNA does not affect the cytokine-stimulated production of prostaglandin E2, whereas prostaglandin F2alpha levels are enhanced. Neither isoform mPGES-2 nor cPGES expression are affected by siRNA silencing of mPGES-1
additional information
-
in enzyme knock-out mice, the infarction, edema, apoptotic cell death, and caspase-3 activation in the cortex ischemia cell are all reduced. the behavioral neurological dysfunctions observed after ischemia in wild-type animals are significantly ameliorated in knock-out animals
additional information
-
in mice with targeted disruption of isoform mPGES-1 gene, basal excretion of prostaglandin E2 in urine is decreased by 50%. In female enzyme-deficient mice, there is a reciprocal increase in basal excretion of other prostanoids. Urinary osmolalities are similar in wild-type and enzyme deficient animals at baseline and after 12 h of water deprivation, and there are no differences in blood pressure on control or high- or low-salt diet. Furesemide-associated diuresis is reduced in male enzyme-deficient animals
additional information
-
isoform mPGES-1 knockout mice. Contrary to wild-type, in knock-out animals no prostaglandin E2 production is found in osteoblast after administration of LPS. While in wild-type, LPS reduces the bone volume in femur associated with an increased number of osteoclasts, this loss is reduced in knock-out mice. LPS induces the loss of alveolar bone in wild-type, but not in the mutants
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7 - 8
-
pH-range of highest stability, 35°C, 7.5 min, either in presence or absence of glutathione
3129
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TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
thiol compounds, glutathione, dithiothreitol, 2-mercaptoethanol or cysteine markedly protect from thermal inactivation
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
activity in solubilized membranes remains stable for a prolonged time in the presence of reduced glutathione and glycerol
-
the enzyme stability is increased in the presence of reduced glutathione
thiol compounds, glutathione, dithiothreitol, 2-mercaptoethanol or Cys markedly protect from thermal inactivation
-
the enzyme stability is increased in the presence of reduced glutathione
the enzyme stability is increased in the presence of reduced glutathione
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
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PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
Ni-NTA column chromatography, and Superdex 200 gel filtration
purification after expression of N-terminally truncated enzyme in recombinant Escherichia coli growing in LB medium containing delta-aminolevulinate and Fe(NO3)3 gives a protein of red colour. Purification after growth of Escherichia coli on minimal medium gives a colourless protein
-
recombinant active isozyme mPGES-1 from Spodoptera frugiperda Sf9 cell microsomes by hydroxylapatite chromatography
recombinant enzyme by ammonium sulfate fractionation, ion exchange chromatography, and gel filtration
-
recombinant His-tagged truncated mPGES-2 from Escherichia coli strain BL21 by nickel affinity chromatography
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in A-549 cells, HeLa cells, HEK-293 cells, RAW 264.7 cells, Pichia pastoris strain KM71H, and Sf9 insect cells
-
expressed in Escherichia coli BL21(DE3)RP cells
expressed in Escherichia coli BL21Star (DE) pLysS cells
expressed in Escherichia coli BL21Star (DE) pLysS cells and SF9 insect cells
expression in Escherichia coli
into the TA vector and subsequently into pET-28a for expression in various Escherichia coli strains, the expression rate is enhanced by modifying the utility of specific codons
-
into the vector pET30 for expression in Escherichia coli BL21Star DE3 cells
isozyme mPGES-1, recombinant functional expression in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method
overexpression of truncated mPGES-2, comprising residues 1-87, with an extended His-tag in Escherichia coli strain BL21 by nickel affinity chromatography
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
1 mM glutamate up-regulates the expression of mPGES-1 to about 3fold that in the controls
100 units/ml interleukin-1beta induces the expression of COX-2 and mPGES-1 in osteoarthritic chondrocytes
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inhibition of NADPH-oxidase negatively modulates mPGES-1 expression induced by tobacco smoke/interleukin-1beta. The activation of mPGES-1 is negatively regulated by prostaglandin I2
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interleukin-1beta does not change expression of MPGES-1 in the prostate cancer cell lines
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microinjection of kainic acid induces mPGES-1 in venous endothelial cells but not in neurons or astrocytes
mPGES-2 immunoreactivity is particularly elevated in the pyramidal neurons of brains from three of five sporadic and four of five familial Alzheimer's disease patients compared with four of five age-matched control brains that showed minimal immunoreactivity
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the enzyme expression increases in the distended bowel during obstruction
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the enzyme shows elevated levels in the cartilages and chondrocytes of patients suffering from osteoarthritis. The enzyme is overexpressed in 80% of several cancer cells
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the expression of mPGES-1 in wild type mice is markedly upregulated in the gastric ulcer tissues compared with normal gastric tissues without ulcers
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tobacco smoke (EC50 about 5 puffs/l) interacting with IL-1beta (0.002 mg/l) upregulates PGE2 production and mPGES-1 expression, reaching a plateau at 4-6 h
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1 mM glutamate up-regulates the expression of mPGES-1 to about 3fold that in the controls
-
1 mM glutamate up-regulates the expression of mPGES-1 to about 3fold that in the controls
-
microinjection of kainic acid induces mPGES-1 in venous endothelial cells but not in neurons or astrocytes
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microinjection of kainic acid induces mPGES-1 in venous endothelial cells but not in neurons or astrocytes
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
drug development
medicine
drug development
-
the enzyme constitues an attractive drug target for treatment of inflammatory diseases
drug development
-
the enzyme is a potential target for therapy of breast cancer
drug development
-
the enzyme represents a novel target for anti-inflammatory and anti-cancer drugs
medicine
-
a considerable increase of mPGES-2 expression is observed in human colorectal cancer
medicine
antiinflammatory drug target, deletion of microsomal mPGES-1 abrogates inflammation
medicine
-
mPGES-1 is involved in various types of pathology including inflammation, pain hyperalgesia, fever, and cancer
medicine
-
in enzyme knock-out mice, the infarction, edema, apoptotic cell death, and caspase-3 activation in the cortex ischemia cell are all reduced. the behavioral neurological dysfunctions observed after ischemia in wild-type animals are significantly ameliorated in knock-out animals. Microsomal enzyme mPGES-1 may be a critical determinant of postischemic neurological dysfunctions and a therapeutic target for treatment of stroke
medicine
-
prostaglandin E2 derived from COX-2 and isoform mPGES-1 plays a significant role in the pathogenesis of chronic acid reflux oesophagitis, and possibly in basal hyperplasia and persistent inflammatory cell infiltration
medicine
-
use of isoform mPGES-1 as a target for the treatment of inflammatory bone disease
medicine
-
17beta-estradiol and proinflammatory cytokines can act together to up-regulate PTGES, the finding supports a model whereby estrogens and inflammatory factors orchestrate a complex network of cross talk and feedback mechanisms that can contribute to hormone-dependent breast tumor growth and progression
medicine
-
induction of various inflammatory cytokines in addition to overexpression of COX-2 and mPGES-1 could be risk factors of gastric carcinogenesis and may serve as a better gastric carcinogenesis model
medicine
-
licofelone suppresses inflammatory PGE2 formation preferentially by inhibiting mPGES-1 at concentrations that do not affect COX-2
medicine
-
mPGES-1 could be a potential therapeutic target of novel inhibitors for treatment of inflammatory diseases
medicine
-
mPGES-1 expression is significantly elevated in Alzheimer's disease tissue
medicine
-
mPGES-1 inhibitors have therapeutic potential in syndromes of cardiovascular inflammation, cancer and perhaps neurodegenerative disease
medicine
-
mPGES-1 is a potential target for inhibitors, pathological conditions, such as inflammation, pain, fever, anorexia, atherosclerosis, stroke, and tumorigenesis are related to elevated levels of PGE2
medicine
mPGES-1 is a promising target for the development of anti-inflammatory drugs
medicine
-
mPGES-1 plays a role in atherosclerosis, stroke, inflammation, pain and fever
medicine
MPGES1 has been implicated in a number of human diseases or pathological conditions, such as rheumatoid arthritis, fever, and pain, and is therefore regarded as a primary target for development of novel antiinflammatory drugs
medicine
-
the selective inhibition of mPGES-1 generates anti-inflammatory effects without unwanted side effects involving homeostasis
medicine
-
MPGES-1 is an alternative therapeutic target in cancer cells expressing this enzyme
medicine
-
inhibition of mPGES-1 may have clinical utility in the management of bone cancer pain
medicine
-
enzyme inhibition can be useful for treating pain, fever, and anorexia
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EXTERNAL LINKS (specific for EC-Number 5.3.99.3)
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Release 2023.1 (January 2023)
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