Information on EC 3.4.23.15 - renin

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The expected taxonomic range for this enzyme is: Tetrapoda

EC NUMBER
COMMENTARY
3.4.23.15
-
RECOMMENDED NAME
GeneOntology No.
renin
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cleavage of Leu-/- bond in angiotensinogen to generate angiotensin I
show the reaction diagram
inhibits vasorelaxation induced by nitroso albumin
-
SYNONYMS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
angiotensin-forming enzyme
-
-
-
-
angiotensinogenase
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
9015-94-5
-
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
healthy persons and hypertensive patients
-
-
Manually annotated by BRENDA team
healthy persons, hypertensive patients, and patients with aldosterone- and/or cortisol secreting adenomas
-
-
Manually annotated by BRENDA team
patients with biopsy-confirmed post-transplant glomerulonephritis
-
-
Manually annotated by BRENDA team
patients with hypertension
-
-
Manually annotated by BRENDA team
recombinant
-
-
Manually annotated by BRENDA team
male
-
-
Manually annotated by BRENDA team
transgenic expression in rat
-
-
Manually annotated by BRENDA team
transgenic expression in Ren2 rat
-
-
Manually annotated by BRENDA team
wild-type BPN and hypertensive BPH mice
-
-
Manually annotated by BRENDA team
Watanabe heritable hyperlipidemic rabbit
-
-
Manually annotated by BRENDA team
male sprague-dawley rats
-
-
Manually annotated by BRENDA team
transfected with human kidney renin RNA
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
metabolism
-
renin is the first rate-limiting enzymatic step in the renin-angiotensin-aldosterone system pathway
metabolism
-
renin is the rate-limiting step in angiotensin II generation
physiological function
-
renin is a key regulator of the renin-angiotensin system which is important for blood pressure and electrolyte regulation. High renin angiotensin system activity results in over-activation of the angiotensin AT1-receptor by its substrate, angiotensin II, leading to increases in blood pressure and direct growth-promoting effects on tissues that result in end-organ damage
physiological function
-
renin-catalyzed conversion of angiotensinogen to angiotensin i is the rate-limiting step in the event cascade that activates the renin-angiotensin system. Renin directly increases the production of the fibrogenic cytokine transforming growth factor beta1 in the kidney
physiological function
-
the intrarenal renin-angiotensin-aldosterone system is activated and plays a critical role in the pathogenesis of chronic kidney disease
physiological function
-
the renin-angiotensin-aldosterone system plays a key role in the regulation of blood volume, blood pressure, and cardiovascular and renal function
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
4-(4'-(dimethylaminophenylazo))-benzoyl-gamma-aminobutyryl-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS + H2O
4-(4'-(dimethylaminophenylazo))-benzoyl-gamma-aminobutyryl-Ile-His-Pro-Phe-His-Leu + Val-Ile-His-Thr-EDANS
show the reaction diagram
Q6DYE7
-
-
-
?
4-(4-dimethylaminophenylazo)benzoic acid-IHPFHLVIHT-5-[(e-amino-ethyl)amino]naphthalene-1-sulfonic acid + H2O
4-(4-dimethylaminophenylazo)benzoic acid-IHPFHL + VIHT-5-[(e-amino-ethyl)amino]naphthalene-1-sulfonic acid
show the reaction diagram
-
fluorogenic peptide
-
-
?
acetyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser + H2O
acetyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu + Leu-Val-Tyr-Ser
show the reaction diagram
Q6DYE7
-
-
-
?
aliskiren + H2O
?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + ?
show the reaction diagram
-
highly specific for Leu10-Leu11 bond in horse or rat angiotensinogen or Leu10-Val11 bond in human angiotensinogen, minimum sequence required: His-Pro-Phe-His-Leu-Leu-Val-Tyr
-
-
?
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
Q8IYK8
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
enzyme activity is increased in hypertensive mice
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
high glucose concentration stimulates intracellular renin activity and angiotensin II generation in mesangial cells, mechanism, the renin-angiotensin system is involved in diabetic nephropathy, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin is an active component of the local synovial renin-angiotensin system in rheumatoid arthritis, renin-angiotensin system in synovial fluid, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary aldosteronism, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary hyperaldosteronism, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the renin-angiotensin system is responsible for regulation of blood pressure and electrolytic balance
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the His-Pro-Phe motif of angiotensinogen is a crucial determinant of the substrate specificity of renin. Mutant angiotensinogens in which the Ile-His-Pro-Phe-His-Leu sequence at positions 5-10 of wild-type angiotensinogen is replaced by either His-Pro-Phe-His-Leu-Leu or Ala-Ile-His-Pro-Phe-His are cleaved by renin at the C-terminal side of residues 9 and 11, respectively, while wild-type angiotensinogen is cleaved at residue 10. A triple Ala substitution for the His-Pro-Phe motif of angiotensinogen prevents its cleavage by renin. In contrast, triple Ala substitution for residues 9-11, including the natural site of cleavage by renin, allows cleavage between the two Ala residues at positions 10 and 11
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin catalyses the rate-limiting step in the system and has unique specificity for its substrate angiotensinogen
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin cleaves the Leu10-Leu11 bond
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin is a highly specific enzyme for angiotensinogen
-
-
?
Arg-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(4-(4-dimethylaminophenylazo)-benzoic acid)-Arg + H2O
?
show the reaction diagram
-
commercial renin peptide substrate 1
-
-
?
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide + H2O
benzyloxycarbonyl-Pro-Phe-His-Leu + Leu-Val-Tyr-Ser-beta-naphthylamide
show the reaction diagram
-
-
-
?
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide + H2O
?
show the reaction diagram
-
-
-
-
?
DABCYL-c-Abu-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS + H2O
?
show the reaction diagram
-
-
-
-
?
H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Glu + H2O
H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu + Val-Ile-His-Thr-Glu
show the reaction diagram
-
-
-
?
N-methylanthranyl-Ile-His-Pro-Phe-His-Leu-Val-Ile-Thr-His-Lys-2,4-dinitrophenyl-D-Arg-D-Arg-NH2 + H2O
N-methylanthranyl-Ile-His-Pro-Phe-His-Leu + Val-Ile-Thr-His-Lys-2,4-dinitrophenyl-D-Arg-D-Arg-NH2
show the reaction diagram
-
-
-
-
?
tetradecapeptide + H2O
?
show the reaction diagram
-
-
-
-
?
megsin + H2O
?
show the reaction diagram
-
the protein which carries a naturally occurring His-Pro-Phe sequence, is cleaved by renin at the C-terminal side of the His-Pro-Phe-Leu-Phe sequence
-
-
?
additional information
?
-
-
the main role of the enzyme is the intracellular generation of angiotensin
-
?
additional information
?
-
-
possible binding mechanism of prorenin and renin to the renin/prorenin receptor, overview
-
-
-
additional information
?
-
Q8IYK8
tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
-
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
?
show the reaction diagram
-
role in regulating blood pressure
-
-
-
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
Q8IYK8
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
-
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
enzyme activity is increased in hypertensive mice
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
high glucose concentration stimulates intracellular renin activity and angiotensin II generation in mesangial cells, mechanism, the renin-angiotensin system is involved in diabetic nephropathy, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin is an active component of the local synovial renin-angiotensin system in rheumatoid arthritis, renin-angiotensin system in synovial fluid, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary aldosteronism, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary hyperaldosteronism, overview
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
the renin-angiotensin system is responsible for regulation of blood pressure and electrolytic balance
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin catalyses the rate-limiting step in the system and has unique specificity for its substrate angiotensinogen
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin cleaves the Leu10-Leu11 bond
-
-
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
show the reaction diagram
-
renin is a highly specific enzyme for angiotensinogen
-
-
?
additional information
?
-
-
the main role of the enzyme is the intracellular generation of angiotensin
-
?
additional information
?
-
-
possible binding mechanism of prorenin and renin to the renin/prorenin receptor, overview
-
-
-
additional information
?
-
Q8IYK8
tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
-
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1R,5S)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-oxa-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3,3-dioxide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3-oxide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3-oxa-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3,3-dioxide
-
-
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3-oxide
-
-
(2R)-1-methoxy-3-([(3S,4R,5R)-4-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)-5-[(4-methoxynaphthalen-2-yl)methoxy]piperidin-3-yl]oxy)propan-2-ol
-
-
(2R)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]-N-[3-(2-methoxyethoxy)-5-(3-methoxypropyl)benzyl]propanamide
-
-
(2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
-
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide
-
-
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-methylhexanamide
-
-
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[[4-methoxy-3-(3-methoxypropoxy)phenyl]sulfonyl](propan-2-yl)amino]-2-methylhexanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-methyl-2-morpholin-4-ylpropyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-morpholin-4-ylethyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-piperidin-1-ylethyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-pyridin-2-ylethyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-thiomorpholin-4-ylethyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(3-morpholin-4-ylpropyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(4-morpholin-4-yl-4-oxobutyl)nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(1H-tetrazol-5-yl)propyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[4-(methylamino)-4-oxobutyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[2-(piperidin-1-yl)ethyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[2-(pyridin-2-yl)ethyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[3-(1H-tetrazol-5-yl)propyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[3-(morpholin-4-yl)propyl]nonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-(3-methoxypropyl)-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-(4-methoxypiperidin-1-yl)ethyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(3-hydroxypropyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(4-hydroxybutyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[(4-hydroxypiperidin-1-yl)methyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[2-(4-hydroxypiperidin-1-yl)ethyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[3-(1H-imidazol-4-yl)propyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[4-[(2-methoxyethyl)amino]-4-oxobutyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-tert-butylbenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(2-aminoethyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(3-aminopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(3-cyanopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pyridin-4-ylmethoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[(methylsulfonyl)methoxy]benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-[2,2-dimethyl-3-(methylamino)-3-oxopropoxy]-4-methoxybenzyl]-4-hydroxy-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(1,1-dioxidothiomorpholin-4-yl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylsulfamoyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(ethylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-(tert-butylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-N-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-N-[2-(acetylamino)ethyl]-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(2S)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
-
(2S,4S,5S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-(propan-2-yl)hexanamide
-
-
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-methyl-1-(morpholin-4-yl)propan-2-yl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-methyl-3-(methylamino)-3-oxopropyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[4-(methylamino)-4-oxobutyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(1-amino-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(1-amino-2-methyl-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(1-amino-3-hydroxy-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(2-amino-2-oxoethyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(3-amino-2-methyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(2S,4S,5S,7S)-5-amino-N-[2,2-dimethyl-3-(methylamino)-3-oxopropyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
-
(3R)-3-[(1S)-1-(2-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-bromophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chloro-2-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chloro-5-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(propanoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(sulfamoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylcarbamoyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylsulfonyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-[(2,2,2-trifluoroethyl)amino]propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(cyclopropylcarbonyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(dimethylcarbamoyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-1-(3-cyanophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-4-(acetylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-4-(butanoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(1S)-4-(carbamoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(R)-(3-chloro-2-fluorophenyl)(3-methoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-3-[(R)-(3-chlorophenyl)(3-hydroxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-methoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2,3-difluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2-fluoro-5-methylphenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-ethylphenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methoxyphenyl)pentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methylphenyl)pentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethoxy)phenyl]pentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethyl)phenyl]pentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(3-fluorophenyl)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-fluorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
-
(3R)-N-[(2S)-1-[(chloromethyl)amino]-3-cyclohexylpropan-2-yl]-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
-
1,2-epoxy-3-(p-nitrophenoxy)propane
-
-
2'-O-beta-D-glucopyranosyl momordin Ic
-
-
2'-O-beta-D-glucopyranosyl momordin IIc
-
-
2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
-
-
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
-
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
-
-
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
-
3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-[3-(dimethylamino)propyl]benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[[5-chloro-2-(3-methoxypropyl)-1-oxidopyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[[5-chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butyl acetate
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butanoic acid
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butyl acetate
-
-
4-amino-N-[2-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]phenyl]-3-methoxybenzamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-5,5-difluoro-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-difluoro-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
5-amino-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)pentanamide
-
-
5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine
-
-
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
-
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
-
-
6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
-
-
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
the (+)- and (-)-enantiomers are almost equally potent as renin inhibotrs in buffer and in plasma. crystallization data
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
8-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5-azaspiro[2.5]oct-7-ene-7-carboxamide
-
-
8-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-5-azaspiro[2.5]oct-7-ene-7-carboxamide
-
-
A 62198
-
-
-
A 65317
-
-
-
A 74273
-
-
-
aliskiren
-
the renin inhibitor prevents atherosclerosis progression
aliskiren
Q6DYE7
-
aliskiren
-
depending on incubation conditions, circulating renin inhibitors interfere with the recognition of active renin molecules by the monoclonal antibodies used in commercial available assaysCareful considerations must therefore by given to the methodology used for quantifying immunoreactive plasma active renin when patients are treated with renin inhibitors, to avoid an overestimation of the magnitude of active renin release attributable to conformational changes in plasma prorenin
aliskiren
-
non-peptide orally active renin inhibitor
aliskiren
-
treatment of young heterozygous male Ren2 and age-matched control rats with renin inhibitor aliskiren leads to significantly increased blood pressure, NADPH oxidase activity and subunit immunostaining, 3-nitrotyrosine, perivascular fibrosis, mitochondrial content and markers of activity in Ren2 rats
aliskiren
-
co-administration of aliskiren results in changes below 30% in pharmacokinetic parameters AUC and Cmax of digoxin, atorvastatin, o-hydroxyatorvastatin, and p-hydroxyatorvastatin, indicating no clinically significant interaction with P-glycoprotein or CYP3A4 substrates. Aliskiren AUC is significantly increased by coadministration with atorvastatin or ketoconazole
aliskiren
-
renal vasodilation in healthy people with aliskiren exceeds responses seen with angiotensin-converting enzyme inhibitors and angiotensin receptor blockers. The effects are longer lasting and are associated with significant natriuresis. Aliskiren may provide more complete and more effective blockade of the renin-angiotensin system
aliskiren
-
aliskiren produces a parallel, dose-related, sustained decrease in plasma renin activity, angiotensin I, and angiotensin II levels and a slightly delayed increase in active renin. The effect is described by an indirect stimulatory response model in conjunction with an empirical submodel of functional adaptation. Estimated concentration of aliskiren necessary for producing 50% inhibition of plasma renin activity is 0.66 ng/ml
aliskiren
-
treatment of transgenic Ren2 rat results in systemic insulin resistance with decreased skeletal muscle insulin metabolic signaling and glucose uptake. Effects are associated with increased angiotensin II, mineralocorticoid receptor, angiotensin type I receptor, oxidative stress, and reduced tyrosine insulin receptor substrate phosphorylation, protein kinase B/(Akt) phosphorylation and GLUT-4 immunostaining
aliskiren
-
study on long-term safety, tolerability, and antihypertensive efficacy on Japanese patients with mild to moderate essential hypertension. Aliskiren alone or in combination with a diuretic or a calcium channel blocker is well tolerated. The incidence of suspected study-related adverse events was 25.3%. The overall responder efficacy was 73.3% at the endpoint. A clinically meaningful reduction of 17.6/12.8 m Hg from baseline was achieved in the mean sitting blood pressure at the endpoint
aliskiren
-
treatment of Watanabe heritable hyperlipidemic rabbits with aliskiren or aliskiren plus valsartan leads to greater increases in plasma nitric oxide concentration in response to intra-aortic acetylcholine infusion than in control. Aliskiren plus valsartan treatment increases acetylcholine-induced nitric oxide by 6.2 nmol/l, which is significantly higher than with either aliskiren or valsartan alone. Vascular superoxide and peroxynitrite levels are both significantly higher in controls and significantly lower in the aliskiren plus valsartan group than in the aliskiren or valsartan group
aliskiren
-
aliskiren at the highest approved dose of 300 mg once daily for 7 days and a 4-fold higher dose has no effect on cardiac repolarization or conduction in healthy volunteers
aliskiren
-
after 12 weeks of treatment in patients with hypertension, aliskiren, atenolol and aliskiren/atenolol lower systolic and diastolic blood pressure from baseline by 14.3/11.3, 14.3/13.7 and 17.3/14.1 mmHg, respectively. Systolic blood pressure reductions with aliskiren/atenolol are significantly greater than those with aliskiren or atenolol alone, and diastolic blood pressure reductions are greater than with aliskiren alone. Diastolic blood pressure changes are larger with atenolol than with aliskiren. Aliskiren, atenolol and aliskiren/atenolol reduce geometric mean plasma renin activity from baseline by 65%, 52% and 61%, respectively. In patients with moderate or high baseline plasma renin activity, plasma renin activity is reduced to low levels at week 12 endpoint in a greater proportion of patients receiving aliskiren or aliskiren/atenolol than with atenolol. Aliskiren treatment is associated with numerically lower rates of adverse events and discontinuations due to adverse events compared with atenolol or combination treatment, and unlike atenolol is not associated with bradycardia
aliskiren
-
low molecular weight, orally active renin inhibitor
aliskiren
-
potent direct renin inhibitor
aliskiren
-
SPP-100, formerly CGP-60539
aliskiren
-
highly potent selective inhibitor of human renin
aliskiren
-
direct renin inhibitor, aliskiren has the potential to reduce end organ damage in chronic kidney disease
aliskiren
-
oral direct renin inhibitor
aliskiren
-
orally active direct renin inhibitor
aliskiren
-
orally effective, nonpeptide, low-molecular-weight, direct renin inhibitor
aliskiren
-
nonpeptide, orally active, direct renin inhibitor
aliskiren
-
orally effective direct renin inhibitor, aliskiren inhibits the renin-angiotensin-aldosterone system by blocking the enzymatic activity of renin
aliskiren
-
targets the renin enzyme directly
aliskiren
-
a renin inhibitor used in the treatment of hypertension. Rifampicin reduces the renin-inhibiting effect of aliskiren (plasma renin activity 24 h after aliskiren intake is 61% higher after treatment with rifampicin (600 mg once daily for 5 days))
aliskiren
-
renin inhibition is more than 99% at 5 h after the 300 and 600 mg aliskiren doses
aliskiren
-
non-peptide, orally active, selective renin inhibitor
aliskiren
-
direct renin inhibitor for the treatment of hypertension
aliskiren
-
direct renin inhibitor, aliskiren is useful for antihypertensive treatment in patients with severe arterial hypertension, in patients with an already long-lasting course of disease, and in the presence of comorbidities such as diabetes mellitus
aliskiren
-
direct renin inhibitor
aliskiren
-
renin inhibitor in clinical practice for hypertension
BILA 2157 BS
-
-
-
Bromoisocaproyl peptides
-
-
-
BW 633C
-
-
-
BW-175
-
-
-
CGP 29287
-
-
-
CGP 38560A
-
-
CGP 44099
-
-
-
CGP 60536
-
automated quantitative determination of the inhibitor by high-performance liquid chromatography
CGP 60536
-
-
CGP-29,287
-
-
-
CGP-44099A
-
-
-
CGP38560A
-
-
CH-66
-
-
chikusetsusaponin IV
-
-
chitooligosaccharide
-
chitooligosaccharides are competitive inhibitors of renin. Chitololigosaccharides from 90% deacetylated chitosan and with molecular weight of 1000-5000 Da exhibit the highest activity with IC50 value of 0.51 mg/ml and Km value of 0.28 mg/ml. Chitooligosaccharides from 90% deacetylated chitosan and with molecular weight below 1000 Da show an IC50 value of 0.59 mg/ml. Main binding sites of chitooligosaccharides are not S3-S1 pockets of renin. Interactions could be formed by the hydrogen bonding and/or the electrostatic interaction between the positively charged amide group at C2 postition and the carboxylates of the catalytic resiudues
-
CI 992
-
-
-
CI-992
-
-
-
ciprokiren
-
Ro 44-9375
CP 71362
-
-
-
CP 81282
-
-
CP-72,647
-
-
CP-80,794
-
-
CP-81,198
-
-
CP-81,282
-
-
cyclothiazomycin
-
-
decanoyl acetal sodium sulfite
-
IC50: 0.273 mM
diazoacetyl methyl ester derivatives of glycine, norleucine, leucine
-
in presence of Cu2+
-
diisopropylfluorophosphate
-
gamma-renin only
ditekren
-
U 71038
dodecanoyl acetal sodium sulfite
-
IC50: 0.195 mM
EMD 51921
-
-
-
EMD 52297
-
-
-
EMD 56133
-
-
-
EMD 58265
-
-
-
enalkiren
-
-
enalkiren
-
A 64662
ES 1005
-
-
-
ES 6864
-
-
-
ES-8891
-
-
-
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
-
-
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alaninate
-
-
ethyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
-
FK906
-
-
-
glycyrrhizin
-
-
GR 70982
-
-
-
H-141
-
-
-
H-142
-
-
-
H-142-08
-
-
-
H-189
-
-
H-261
-
-
H-77
-
-
-
H-77-77
-
-
-
hexanoyl acetal sodium sulfite
-
-
houttuynin
-
from the volatile oil of Houttuynia cordata
Isoamylamine
-
-
Kallikrein
-
-
-
KR1-1314
-
-
-
KRI 1177
-
-
-
L 363714
-
-
-
L-Ile-L-Trp
-
70% inhibition at 3.2 mM
-
L-Leu-L-Trp
-
37% inhibition at 3.2 mM
methyl (2-[(R)-(3-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chloro-5-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(5-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
-
-
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
-
-
methyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
-
methyl [2-(5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxyphenyl)ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-chlorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,3-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,5-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,4-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,5-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-methylphenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](phenyl)methoxy]ethyl]carbamate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-methoxyphenoxy]methanesulfinate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]acetate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]methanesulfinate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
-
-
momordin Ic
-
-
momordin IIc
-
-
N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
N-acetyl-D-glucosamine-2-epimerase
-
-
-
N-alpha-carbobenzoxy-Arg-Arg-Pro-Phe-His-Sta-Ile-His-Nepsilon-butyloxycarbonyl-Lys
-
-
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
inhibitor is well absorbed and reduces the blood pressure by about 30 mm Hg at 10 mg/kg in vivo
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
-
N-cyclopropyl-N-[[1-(3-methoxypropyl)-1H-indol-3-yl]methyl]morpholine-2-carboxamide
-
-
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alanine
-
-
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alanine
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-3-(3-methoxypropoxy)-4-methyl-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-bromo-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethynyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(4-methoxybutyl)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-[(1E)-4-methoxybut-1-en-1-yl]-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5S)-2-amino-5-(butylcarbamoyl)-3-hydroxy-6-methylheptyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]benzamide
-
-
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
-
-
N-[2-[6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl]acetamide
-
-
N-[2-[7-([[(3R,4R)-4-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperidin-3-yl]oxy]methyl)-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[7-[[(2R)-1-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperazin-2-yl]methoxy]-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
-
octanoyl acetal sodium sulfite
-
-
PD 132002
-
-
-
PD 133,450
-
-
PD-129,541
-
-
Pepstatin
-
-
pepstatin A
Q6DYE7
-
pepstatin A
-
SR 42128
Phenylethylamine
-
-
R-PEP-27
-
-
-
remikiren
-
-
remikiren
-
RO 42-5892
renin inhibitory peptide
-
-
-
Renin-binding protein
-
from hog kidney
-
RI 78
-
-
-
Ro 42-5892
-
-
Ro 44-9378
-
-
-
S-2864
-
-
-
SC 46944
-
-
-
SC 56525
-
-
-
soyasaponin I
-
i.e. soybean renin inhibitor. Significant inhibition of recombinant renin, partially noncompetitive
soyasaponin I
-
-
soyasaponin II
-
-
-
SQ 32970
-
-
-
SQ 33800
-
-
-
SR 42128
Q6DYE7
-
SR 43845
-
-
-
terlakiren
-
CP 80794
tert-butyl [(3S,5S,6S,8S)-8-(butylcarbamoyl)-6-hydroxy-3-(4-methoxybenzyl)-2,9-dimethyldecan-5-yl]carbamate
-
potent low nanomolar inhibitor of renin
tetradecanoyl acetal sodium sulfite
-
complex formation with the enzyme, mixed inhibition type, IC50: 0.044 mM
tetrahydro-2H-pyran-4-yl cyclopropyl[[(3S,4S)-4-[(2R)-2-[4-methoxy-3-(3-methoxypropoxy)benzyl]-3-methylbutyl]pyrrolidin-3-yl]methyl]carbamate
-
-
Transition state analogues
-
-
-
Transition state analogues
-
energy calculation for transition state complex
-
Transition state analogues
-
angiotensinogen modified in P1 or P1' position by e.g. statine, statine-derivatives, keto-groups, hydroxyethylene; in vivo effect
-
Transition state analogues
-
in vivo effect
-
Transition state analogues
-
reduced analogous, keto- or hydroxyisosteres
-
Transition state analogues
-
regulation of blood pressure
-
U-62168E
-
-
U-71909E
-
-
U-72407E
-
-
U-72408E
-
-
-
U-72409E
-
-
U-73777E
-
-
U-76780E
-
-
U-77451E
-
-
U-77455E
-
-
U-77646E
-
-
U-77647E
-
-
U-80215E
-
-
U-80631E
-
-
YM-21095
-
-
-
YM-26365
-
-
-
YY
-
dipeptide derived from royal jelly proteins. YY inhibits the renin activity only at acidic pH values below 8.0
zankiren
-
-
zankiren
-
A 72517
monoglucuronyl glycyrrhetic acid
-
-
additional information
-
development of oral renin inhibitors and their pharmacokinetic and pharmacodynamic properties
-
additional information
-
renin is not inhibited by soyasapogenol B glycyrrhetic acid, saikosaponin b2, saikosaponin c and ginsenoside Rb1
-
additional information
-
not inhibited by L-Val-L-Trp and L-Ala-L-Trp
-
additional information
-
-
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
-
high glucose concentration stimulates intracellular renin activity and angiotensin II generation in mesangial cells
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0036
4-(4-dimethylaminophenylazo)benzoic acid-IHPFHLVIHT-5-[(e-amino-ethyl)amino]naphthalene-1-sulfonic acid
-
-
-
0.00029
angiotensinogen
-
porcine substrate, activated enzyme
0.00031
angiotensinogen
-
porcine substrate, non-activated enzyme
0.00077
angiotensinogen
-
-
0.00154
angiotensinogen
-
human substrate and enzyme
0.00204
angiotensinogen
-
-
0.0033
angiotensinogen
-
recombinant, immobilized renin and prorenin
0.0035
angiotensinogen
-
-
0.017 - 0.105
angiotensinogen
-
depending on form of enzyme
0.0064
Arg-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(4-(4-dimethylaminophenylazo)-benzoic acid)-Arg
-
pH 8.0, 37C
0.03 - 0.041
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-2-naphthylamide
-
depending on isoenzyme
0.12
acetyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser
Q6DYE7
-
additional information
aliskiren
-
estimated Km1 value is 0.516 ng/ml, Km2 value is 135 ng/ml
0.03 - 0.041
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-2-naphthylamide
-
depending on isoenzyme
additional information
additional information
-
kinetics of plasma renin, overview
-
additional information
additional information
-
binding affinities of recombinant prorenin and renin to the recombinant renin/prorenin receptor, kinetics, overview
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.00717
angiotensinogen
-
isoenzyme R-III
0.00817
angiotensinogen
-
isoenzyme R-II
0.00867
angiotensinogen
-
isoenzyme R-I
1.35
angiotensinogen
-
pH 6.0, 37C, maleate buffer
1.5
angiotensinogen
-
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000021
(3R)-3-[(1S)-1-(3-chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000015
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(propanoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000046
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(sulfamoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000046
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylcarbamoyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000177
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylsulfonyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000047
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000017
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(cyclopropylcarbonyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00226
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(dimethylcarbamoyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000013
(3R)-3-[(1S)-4-(acetylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000057
(3R)-3-[(1S)-4-(butanoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000031
(3R)-3-[(1S)-4-(carbamoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000014
ethyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000061
methyl (2-[(R)-(3-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000053
methyl (2-[(R)-(3-chloro-5-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000087
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000048
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000062
methyl (2-[(R)-(5-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000018
methyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000048
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-chlorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000058
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000021
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000017
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,3-difluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000062
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,5-difluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000025
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,4-difluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000023
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,5-difluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000059
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000047
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-methylphenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0375
soyasaponin I
-
pH 6.5, 37C
0.00004
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
additional information
chitooligosaccharide
-
chitooligosaccharides from 90% deacetylated chitosan and with molecular weight of 1000-5000 Da exhibit an Km value of 0.28 mg/ml
-
0.00000117
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](phenyl)methoxy]ethyl]carbamate
-
50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
additional information
additional information
-
inhibition kinetics
-
0.045
tetradecanoyl acetal sodium sulfite
-
pH 8.0, 37C
additional information
YY
-
Ki value is estimated 4.6 micromol per l at pH 6.0
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000004
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
pH and temperature not specified in the publication
0.00000068
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-oxa-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide
-
pH and temperature not specified in the publication
0.0000064
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3,3-dioxide
-
pH and temperature not specified in the publication
0.00000137
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
pH and temperature not specified in the publication
0.00000049
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3-oxa-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide
-
pH and temperature not specified in the publication
0.000064
(1S)-7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-3-thia-9-azabicyclo[3.3.1]non-6-ene-6-carboxamide 3-oxide
-
pH and temperature not specified in the publication
0.00000002
(2R)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]-N-[3-(2-methoxyethoxy)-5-(3-methoxypropyl)benzyl]propanamide
-
at pH 7.4 and 37C
0.000132
(2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
-
0.1
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide
-
IC50 above 0.1 mM, at pH 7.4, temperature not specified in the publication
0.000013
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-methylhexanamide
-
at pH 7.4, temperature not specified in the publication
0.0003
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[[4-methoxy-3-(3-methoxypropoxy)phenyl]sulfonyl](propan-2-yl)amino]-2-methylhexanamide
-
at pH 7.4, temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-methyl-2-morpholin-4-ylpropyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000004
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-methyl-2-morpholin-4-ylpropyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-morpholin-4-ylethyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000007
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-morpholin-4-ylethyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000022
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-piperidin-1-ylethyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000008
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-pyridin-2-ylethyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000016
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-pyridin-2-ylethyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-thiomorpholin-4-ylethyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000012
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(2-thiomorpholin-4-ylethyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000007
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(3-morpholin-4-ylpropyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000011
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(3-morpholin-4-ylpropyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(4-morpholin-4-yl-4-oxobutyl)nonanamide
-
pH 7.2, 37C, purified enzyme
0.000004
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-(4-morpholin-4-yl-4-oxobutyl)nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000003
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(1H-tetrazol-5-yl)propyl]nonanamide
-
pH 7.2, 37C, purified enzyme
0.000007
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(1H-tetrazol-5-yl)propyl]nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]nonanamide
-
pH 7.2, 37C, purified enzyme
0.000015
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000003
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[4-(methylamino)-4-oxobutyl]nonanamide
-
pH 7.2, 37C, purified enzyme
0.000011
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethyl-N-[4-(methylamino)-4-oxobutyl]nonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000022
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[2-(piperidin-1-yl)ethyl]nonanamide
-
pH and temperature not specified in the publication
0.000008
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[2-(pyridin-2-yl)ethyl]nonanamide
-
pH and temperature not specified in the publication
0.000003
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[3-(1H-tetrazol-5-yl)propyl]nonanamide
-
pH and temperature not specified in the publication
0.000011
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methyl-N-[3-(morpholin-4-yl)propyl]nonanamide
-
pH and temperature not specified in the publication
0.0000004
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-(3-methoxypropyl)-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-(3-methoxypropyl)-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000005
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-(4-methoxypiperidin-1-yl)ethyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000049
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-(4-methoxypiperidin-1-yl)ethyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(3-hydroxypropyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000003
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(3-hydroxypropyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.0000008
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(4-hydroxybutyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000017
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(4-hydroxybutyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.00001
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[(4-hydroxypiperidin-1-yl)methyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.00001
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[2-(4-hydroxypiperidin-1-yl)ethyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000052
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[2-(4-hydroxypiperidin-1-yl)ethyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[3-(1H-imidazol-4-yl)propyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000007
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[3-(1H-imidazol-4-yl)propyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[4-[(2-methoxyethyl)amino]-4-oxobutyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.00001
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-[4-[(2-methoxyethyl)amino]-4-oxobutyl]-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.00004
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000092
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000092
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
-
pH and temperature not specified in the publication
0.00002
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-tert-butylbenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
-
pH and temperature not specified in the publication
0.0000006
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000015
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000016
(2R,4S,5S,7S)-5-amino-N-(2-aminoethyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000007
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000013
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000007
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000016
(2R,4S,5S,7S)-5-amino-N-(3-aminopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000001
(2R,4S,5S,7S)-5-amino-N-(3-cyanopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000003
(2R,4S,5S,7S)-5-amino-N-(3-cyanopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000011
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000009
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000006
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000018
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000006
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000011
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000031
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000001
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
at pH 7.4, temperature not specified in the publication
0.000025
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.00007
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000005
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pyridin-4-ylmethoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000005
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pyridin-4-ylmethoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000021
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[(methylsulfonyl)methoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.00005
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[(methylsulfonyl)methoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000019
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.00014
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000019
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000042
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.00009
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000042
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000003
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000003
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000009
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000005
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-[2,2-dimethyl-3-(methylamino)-3-oxopropoxy]-4-methoxybenzyl]-4-hydroxy-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-N-[2-(1,1-dioxidothiomorpholin-4-yl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000011
(2R,4S,5S,7S)-5-amino-N-[2-(1,1-dioxidothiomorpholin-4-yl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000018
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000053
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000018
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
-
pH and temperature not specified in the publication
0.000002
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylsulfamoyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000009
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylsulfamoyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-N-[2-(ethylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000006
(2R,4S,5S,7S)-5-amino-N-[2-(tert-butylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000025
(2R,4S,5S,7S)-5-amino-N-[2-(tert-butylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-N-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000029
(2R,4S,5S,7S)-5-amino-N-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.0000003
(2R,4S,5S,7S)-N-[2-(acetylamino)ethyl]-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, purified enzyme
0.000018
(2R,4S,5S,7S)-N-[2-(acetylamino)ethyl]-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
pH 7.2, 37C, plasma enzyme assay
0.000007
(2S,4S,5S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-(propan-2-yl)hexanamide
-
at pH 7.4, temperature not specified in the publication
0.000016
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-methyl-1-(morpholin-4-yl)propan-2-yl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000001
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[2-methyl-3-(methylamino)-3-oxopropyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.0000008
(2S,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-[4-(methylamino)-4-oxobutyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000004
(2S,4S,5S,7S)-5-amino-N-(1-amino-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000013
(2S,4S,5S,7S)-5-amino-N-(1-amino-2-methyl-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000002
(2S,4S,5S,7S)-5-amino-N-(1-amino-3-hydroxy-1-oxopropan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000003
(2S,4S,5S,7S)-5-amino-N-(2-amino-2-oxoethyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.0000006
(2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.0000009
(2S,4S,5S,7S)-5-amino-N-(3-amino-2-methyl-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000006
(2S,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutan-2-yl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.0000007
(2S,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.0000004
(2S,4S,5S,7S)-5-amino-N-[2,2-dimethyl-3-(methylamino)-3-oxopropyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-(propan-2-yl)nonanamide
-
pH and temperature not specified in the publication
0.000007
(3R)-3-[(1S)-1-(2-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000013
(3R)-3-[(1S)-1-(3-bromophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000001
(3R)-3-[(1S)-1-(3-chloro-2-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000009
(3R)-3-[(1S)-1-(3-chloro-5-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000021
(3R)-3-[(1S)-1-(3-chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000047
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000046
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-[(2,2,2-trifluoroethyl)amino]propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000037
(3R)-3-[(1S)-1-(3-cyanophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000039
(3R)-3-[(R)-(3-chloro-2-fluorophenyl)(3-methoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000004
(3R)-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000764
(3R)-3-[(R)-(3-chlorophenyl)(3-hydroxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000021
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000038
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000055
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000055
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000308
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-methoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000014
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2,3-difluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000035
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2-fluoro-5-methylphenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000004
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000009
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-ethylphenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000003
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000013
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methoxyphenyl)pentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.0000025
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methylphenyl)pentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000007
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000069
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethoxy)phenyl]pentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000007
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethyl)phenyl]pentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000016
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000125
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000609
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000011
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(3-fluorophenyl)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00004
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000058
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-fluorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.000006
(3R)-N-[(2S)-1-[(chloromethyl)amino]-3-cyclohexylpropan-2-yl]-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25C
0.00000055
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
pH and temperature not specified in the publication
0.0000011
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
pH and temperature not specified in the publication
0.00000074
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
pH and temperature not specified in the publication
0.00000092
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
pH and temperature not specified in the publication
0.0194
2'-O-beta-D-glucopyranosyl momordin Ic
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0384
2'-O-beta-D-glucopyranosyl momordin IIc
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0000019
2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
-
at pH 7.4 and 37C
0.00000055
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.00056
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.00026
3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
at pH 7.4 and 37C
0.00021
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
-
at pH 7.4 and 37C
0.00000079
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
at pH 7.4 and 37C
0.0000004
3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000026
3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000027
3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000011
3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000009
3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000021
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000019
3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000026
3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.0000015
3-amino-N-[2-chloro-5-[3-(dimethylamino)propyl]benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.0000003
3-amino-N-[[5-chloro-2-(3-methoxypropyl)-1-oxidopyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.00000019
3-amino-N-[[5-chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.000003
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
-
pH 7.2, 37C, purified enzyme
0.000013
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
-
pH 7.2, 37C, plasma enzyme assay
0.000006
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butyl acetate
-
pH 7.2, 37C, purified enzyme
0.000009
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butyl acetate
-
pH 7.2, 37C, plasma enzyme assay
0.000003
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butanoic acid
-
pH and temperature not specified in the publication
0.000006
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butyl acetate
-
pH and temperature not specified in the publication
0.000336
4-amino-N-[2-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]phenyl]-3-methoxybenzamide
-
-
0.00033
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-5,5-difluoro-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.0000012
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.0008
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-difluoro-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.000031
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.000002
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.00017
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
pH and temperature not specified in the publication
0.00065
5-amino-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)pentanamide
-
at pH 7.4 and 37C
0.00656
5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine
-
-
0.0000071
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
-
0.000095
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
-
-
0.000691
6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
0.000058
6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
0.000173
6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
-
-
0.0000004
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.00036
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.000034
8-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5-azaspiro[2.5]oct-7-ene-7-carboxamide
-
pH and temperature not specified in the publication
0.0000005
aliskiren
-
in 50 mM BES, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, temperature not specified in the publication
0.0000006
aliskiren
Q6DYE7
-
0.0000006
aliskiren
-
-
0.0000006
aliskiren
-
temperature not specified in the publication, at pH 7.4
0.0000006
aliskiren
-
at pH 7.4, temperature not specified in the publication
0.0000006
aliskiren
-
pH and temperature not specified in the publication
0.0000033
BW-175
-
temperature not specified in the publication, at pH 7.4
-
0.000001
CGP-29,287
-
temperature not specified in the publication, at pH 7.4
-
0.0000003
CGP-44099A
-
temperature not specified in the publication, at pH 7.4
-
0.0000007
CGP38560A
-
-
0.00000058
CI-992
-
temperature not specified in the publication, at pH 7.4
-
0.000005
CP-72,647
-
temperature not specified in the publication, at pH 7.4
0.00001
CP-81,198
-
temperature not specified in the publication, at pH 7.4
0.000005
CP-81,282
-
temperature not specified in the publication, at pH 7.4
0.273
decanoyl acetal sodium sulfite
-
IC50: 0.273 mM
0.0000004
ditekren
-
temperature not specified in the publication, at pH 7.4
0.195
dodecanoyl acetal sodium sulfite
-
IC50: 0.195 mM
0.000014
enalkiren
-
-
0.0000073
ES 6864
-
temperature not specified in the publication, at pH 7.4
-
0.0000007
ES-8891
-
temperature not specified in the publication, at pH 7.4
-
0.000004
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
-
pH 7.2, 37C, purified enzyme
0.000013
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
-
pH 7.2, 37C, plasma enzyme assay
0.000004
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alaninate
-
pH and temperature not specified in the publication
0.0000006
FK906
-
temperature not specified in the publication, at pH 7.4
-
0.0571
glycyrrhizin
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0000069
GR 70982
-
temperature not specified in the publication, at pH 7.4
-
0.00001
H-141
-
temperature not specified in the publication, at pH 7.4
-
0.000001
H-77
-
temperature not specified in the publication, at pH 7.4
-
0.0000006
KR1-1314
-
temperature not specified in the publication, at pH 7.4
-
2.3
L-Ile-L-Trp
-
recombinant enzyme, in 50 mM Tris-HCl buffer containing 100 mM NaCl (pH 8.0), at 37C
-
0.000003
methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
-
at pH 7.4, temperature not specified in the publication
0.000001
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
-
pH 7.2, 37C, purified enzyme
0.000003
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
-
pH 7.2, 37C, plasma enzyme assay
0.0001
methyl [2-(5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxyphenyl)ethyl]carbamate
-
at pH 7.4, temperature not specified in the publication
0.00005
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-methoxyphenoxy]methanesulfinate
-
pH and temperature not specified in the publication
0.000006
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]acetate
-
pH and temperature not specified in the publication
0.000013
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]methanesulfinate
-
pH and temperature not specified in the publication
0.000004
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
-
pH 7.2, 37C, purified enzyme
0.00019
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
-
pH 7.2, 37C, plasma enzyme assay
0.0259
momordin Ic
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0468
momordin IIc
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0422
monoglucuronyl glycyrrhetic acid
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0000029
N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
at pH 7.4 and 37C
0.0000002
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.00019
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
in buffer
0.000012
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alanine
-
pH 7.2, 37C, purified enzyme
0.000023
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alanine
-
pH 7.2, 37C, plasma enzyme assay
0.000012
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alanine
-
pH and temperature not specified in the publication
0.000008
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-3-(3-methoxypropoxy)-4-methyl-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000008
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-bromo-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000002
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000006
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethynyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000002
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000001
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(4-methoxybutyl)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000001
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-[(1E)-4-methoxybut-1-en-1-yl]-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000001
N-[(2S,3S,5S)-2-amino-5-(butylcarbamoyl)-3-hydroxy-6-methylheptyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
at pH 7.4, temperature not specified in the publication
0.000027
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
-
-
0.000222
N-[2-[6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl]acetamide
-
-
0.0000001
PD 133,450
-
temperature not specified in the publication, at pH 7.4
0.0008
pepstatin A
Q6DYE7
-
0.0000008
remikiren
-
-
0.0336
soyasaponin I
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
0.0303
soyasaponin II
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
-
0.00000035
SQ 33800
-
temperature not specified in the publication, at pH 7.4
-
0.0000023
SR 42128
Q6DYE7
-
0.0000001
SR 43845
-
temperature not specified in the publication, at pH 7.4
-
0.0000011
terlakiren
-
temperature not specified in the publication, at pH 7.4
0.044
tetradecanoyl acetal sodium sulfite
-
complex formation with the enzyme, mixed inhibition type, IC50: 0.044 mM
0.00000047
YM-21095
-
temperature not specified in the publication, at pH 7.4
-
0.0000029
YM-26365
-
temperature not specified in the publication, at pH 7.4
-
0.0000011
zankiren
-
-
0.00021
8-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-5-azaspiro[2.5]oct-7-ene-7-carboxamide
-
pH and temperature not specified in the publication
additional information
aliskiren
-
estimated concentration of aliskiren necessary for producing 50% inhibition of plasma renin activity is 0.66 ng/ml
0.0774
chikusetsusaponin IV
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37C
additional information
chitooligosaccharide
-
chitololigosaccharides from 90% deacetylated chitosan and with molecular weight of 1000-5000 Da exhibit an IC50 value of 0.51 mg/ml. Chitooligosaccharides from 90% deacetylated chitosan and with molecular weight below 1000 Da show an IC50 value of 0.59 mg/ml
-
0.0000005
Ro 42-5892
-
temperature not specified in the publication, at pH 7.4
additional information
soyasaponin I
-
IC50 value 30 microg/ml at pH 6.5, 37C
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
-
-
additional information
-
-
additional information
-
renin activity in conscious hindlimb-unloaded rats
additional information
Q8IYK8
enzyme activity in lymphangioleiomyomatosis nodules and cells, overview
additional information
-
activity in submandibular gland tissue of wild-type BPN and hypertensive BPH mice
additional information
-
ratio of plasma aldosterone concentration to plasma renin activity
additional information
-
plasma renin activity, PRA, and active renin concentration, ARC, of healthy persons, hypertensive patients, and patients with aldosterone- and/or cortisol secreting adenomas, overview
additional information
-
mass spectrometric methods for evaluation of plasma renin activity applicable for quantitative proteomics, overview
additional information
-
renin activity in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
additional information
-
renin content and activity in serum and synovial fluid from healthy persons, and from patients with osteoarthritis or rheumatism, overview
additional information
-
1072 Goldblatt units/mg, 1 Goldblatt unit: generation of 120000 ng angiotensin I per h
additional information
-
1123 Goldblatt units/mg, 1 Goldblatt unit: generation of 120000 ng angiotensin I per h; 1 Goldblatt unit: generation of 120000 ng angiotensin I per h
additional information
-
-
additional information
-
-
additional information
-
2000 Golblatt units/mg; bioassay; fluorimetric assay; radioimmunoassy
additional information
-
bioassay; fluorimetric assay; radioimmunoassy
additional information
-
-
additional information
-
-
additional information
-
1675 Goldblatt units/mg, 1 Goldblatt unit: generation of 120000 ng angiotensin I per h
additional information
-
-
additional information
-
-
additional information
-
-
additional information
-
-
additional information
-
-
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4 - 4.5
-
substrate benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide
4 - 5.5
-
-
5.5 - 6.5
-
hog plasma angiotensinogen as substrate
5.5 - 6.8
-
-
5.5 - 7
-
kidney
6 - 6.5
-
rat plasma angiotensinogen as substrate
6 - 7.5
-
-
6.5 - 7.5
-
-
7 - 7.5
-
-
7.5
-
assay at
8
-
assay at
additional information
-
-
pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
5
-
no activity below
5
-
no activity below
6 - 8.5
-
more than 30% activity
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
-
assay at
37
-
assay at
37
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
determination of plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
Manually annotated by BRENDA team
-
plasma renin activity, PRA, and active renin concentration, ARC, overview
Manually annotated by BRENDA team
-
plasma renin activity is markedly reduced in preeclampsia
Manually annotated by BRENDA team
-
placental
Manually annotated by BRENDA team
-
from recombinant expression
Manually annotated by BRENDA team
-
of mesangial cells, active renin is significantly higher in the cell lysate than in culture medium. Inactive prorenin is similar for the intracellular and extracellular compartments. Free active renin is the predominant form found in both cell compartments. Mesangial cells in culture are able to synthesize and translate renin mRNA probably as inactive prorenin which is mostly processed to active renin inside the cells. The cells secrete both forms of the enzyme but at lower level compared with intracellular content
Manually annotated by BRENDA team
-
renin is present in the vascular endothelium and intensely expressed in the epithelial basal layer of periodontally affected gingival tissue
Manually annotated by BRENDA team
-
renin activity in conscious hindlimb-unloaded rats compared to untreated rats
Manually annotated by BRENDA team
-
enzymatically inactive prorenin is primarily synthesized in the kidney and accounts for 70% to 90% of the renin in the circulation
Manually annotated by BRENDA team
-
renin is released as an active enzyme in the juxtaglomerular apparatus of the kidney
Manually annotated by BRENDA team
Q8IYK8
lymphangioleiomyomatosis cell
Manually annotated by BRENDA team
Q8IYK8
lymphangioleiomyomatosis nodule, i.e. LAM nodule
Manually annotated by BRENDA team
-
podocytes express a functional intrinsic renin-angiotensin system characterized by neprilysin, aminopeptidase A, ACE2, and renin activities, which predominantly lead to angiotensin(1-7) and angiotensin(1-9) formation, as well as angiotensin II degradation
Manually annotated by BRENDA team
-
enzyme activity is increased in hypertensive mice compared to wild-type mice
Manually annotated by BRENDA team
-
active renin is significantly higher in the cell lysate than in culture medium. Inactive prorenin is similar for the intracellular and extracellular compartments. Free active renin is the predominant form found in both cell compartments. Mesangial cells in culture are able to synthesize and translate renin mRNA probably as inactive prorenin which is mostly processed to active renin inside the cells. The cells secrete both forms of the enzyme but at lower level compared with intracellular content
Manually annotated by BRENDA team
additional information
-
not in cerebrospinal fluid
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
active renin is significantly higher in the cell lysate than in culture medium. Inactive prorenin is similar for the intracellular and extracellular compartments. Free active renin is the predominant form found in both cell compartments. Mesangial cells in culture are able to synthesize and translate renin mRNA probably as inactive prorenin which is mostly processed to active renin inside the cells. The cells secrete both forms of the enzyme but at lower level compared with intracellular content
-
Manually annotated by BRENDA team
-
serum and synovial fluid
-
Manually annotated by BRENDA team
-
active renin is significantly higher in the cell lysate than in culture medium. Inactive prorenin is similar for the intracellular and extracellular compartments. Free active renin is the predominant form found in both cell compartments. Mesangial cells in culture are able to synthesize and translate renin mRNA probably as inactive prorenin which is mostly processed to active renin inside the cells. The cells secrete both forms of the enzyme but at lower level compared with intracellular content
Manually annotated by BRENDA team
-
renin is stored in secretory granules and is released in response to decreases in renal perfusion pressure, decreases in Cl- in the distal tubule fluid or increased sympathetic nerve stimulation via beta1-adrenoceptors
Manually annotated by BRENDA team
additional information
-
subcellular distribution
-
Manually annotated by BRENDA team
PDB
SCOP
CATH
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
26000
-
mouse, gamma-renin, non-denaturing SDS-PAGE
29366
31000 - 44000
-
SDS-PAGE, different values with and without reducing agents
29366
31000 - 44000
-
gel filtration
36933
31000 - 44000
-
active renin, gel filtration HPLC
95754
31000 - 44000
-
gel filtration
95770
31000 - 44000
-
gel filtration
95773
31000 - 44000
-
SDS-PAGE
95779
31000 - 44000
-
gel filtration; sedimentation equilibrium centrifugation
95780
31000 - 44000
-
gel filtration
95785
31000 - 44000
-
gel electrophoresis; gel filtration
95786
31000 - 44000
-
gel filtration
95787
31000 - 44000
-
gel filtration; sedimentation equilibrium centrifugation
95795
31000 - 44000
-
-
95798
31000 - 44000
-
gel filtration
95798
36490
-
submaxillary gland, amino acid sequence
95811
38000
-
gel filtration
95798
41000
-
non-denaturing SDS-PAGE
95802
42000
-
gel filtration
95798
44000
-
gel filtration, renal active renin
95781
45000 - 59000
-
prorenin, activation by trypsin, or acidification, or pepsin, immunoprecipitation
95751
45000 - 59000
-
gel filtration
95777
45000 - 59000
-
gel filtration
95785, 95788
46000
-
gel filtration, plasma active renin
95781
48000
-
gel filtration, plasma inactive renin
95781
48000
-
gel filtration, plasma inactive renin
95808
additional information
-
conformation of flexible region
95749, 95750
additional information
-
comparison with other proteases
95763
additional information
-
-
95763
additional information
-
comparison of amino acid sequences with other aspartate proteinases
95768
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
?
-
x * 46000, recombinant prorenin, SDS-PAGE, x * 42000, recombinant renin, SDS-PAGE
monomer
-
-
monomer
-
-
monomer
-
heavy chain: 31036 Da, 288 amino acids, light chain: 5458 Da, 48 amino acids, linked by disulfide bridge, SDS-PAGE, gel filtration after reducing and carboxymethylation, amino acid sequence
monomer
-
isoenzymes A0, A, C, E: 30000 Da, isoenzyme D: 33000 Da, SDS-PAGE
monomer
-
1 * 36000-38000 Da, SDS-PAGE
monomer
-
1 * 36000 Da, SDS-PAGE
monomer
-
1 * 40000-50000 Da, SDS-PAGE
monomer
-
42000 Da and 32500 Da, held together by a disulfide bond
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
side-chain modification
-
glycoprotein
glycoprotein
-
-
proteolytic modification
-
the inactive prorenin needs to be proteolytically activated to the mature active renin
side-chain modification
-
glycoprotein
proteolytic modification
-
the inactive prorenin needs to be proteolytically activated to the mature active renin, activation in vitro by trypsin at 37C
proteolytic modification
-
the inactive prorenin needs to be proteolytically activated to the mature active renin, activation of the recombinant prorenin in vitro by trypsin at 25C and pH 6.5
side-chain modification
-
glycoprotein
side-chain modification
-
glycoprotein, phosphorylation
additional information
-
no glycoprotein
side-chain modification
-
glycoprotein
additional information
-
-
side-chain modification
-
glycoprotein
additional information
-
pituitary renin
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
hanging drop vapor diffusion method, recombinant renin. Crystal structure of recombinant renin in complex with 5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine, 6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine, and N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
-
in complex with the (+)- and (-)-enantiomer of inhibitor 7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide. The hydrophobic interactions dominate the positioning of the inhibitors with the pseudosymmetry of the central template being able to establish the necessary hydrogen bonds in either orientation. Substitution of either of the two nitrogen atoms abolishes this pseudosymmetry and completely abrogates this observed effect
-
modeling of stereo strucuture of the complex of human renin with dipeptide YY. The loss of inhibitory activiy at basic pH values may be due to a local shift of YY from the center of the renin cleft into the N-domain side
-
pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
3.3
-
20 min, 50% activity
95791
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
bovine serum albumin, stabilization
-
dilution below 1 mg/ml, inactivation
-
freezing/thawing, inactivation
-
dilution below 1 mg/ml, inactivation
-
freezing/thawing, inactivation
-
bovine serum albumin, stabilization
-
freezing/thawing, inactivation
-
freezing/thawing, inactivation
-
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20C, 0.02 M sodium phosphate buffer, pH 6.2, 0.025 M NaCl, 6 months, 90% activity
-
-70C, 1 mg/ml protein, at least 1 year
-
-70C, or -20C, or 4C, neutral pH
-
-90C, or -10C, 10 months
-
0.02M potassium phosphate buffer, pH 7.5, 1 year
-
4C, inactive renin, 0.1 M phosphate buffer, 1 week
-
-20C, 50 mM sodium acetate buffer, pH 5.38, 6 months
-
-20C, 1 month, 70% activity
-
4C, pH 4.6, at least 4 months
-
-20C, pH 7.0, 8 weeks
-
-20C, prorenin, pH 6.5, 0.05% bovine serum albumin, at least 10 days
-
4C, pH 5. 0 or 7.0, 8 weeks
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
full-length prorenin is expressed in HEK 293 cells, purified and converted to its active form by trypsin-mediated cleavage of the 43 residue propeptide
Q6DYE7
2 forms
-
3 forms
-
inactive renin, activated by trypsin
-
prorenin
-
2 isoenzymes
-
5 forms
-
post-transitionally modified forms
-
renin and gamma-renin
-
2 components
-
3 isoenzymes
-
prorenin activated by trypsin
-
recombinant renin
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
full-length prorenin is expressed in HEK 293 cells
Q6DYE7
expression in CHO cells
-
expression in CHO cells; expression in Sf9/baculovirus cells
-
expression in COS cells
-
expression in Cos-1 cells
-
expression in DAMP cells
-
expression in human kidney cell line 293
-
expression in transgenic mice
-
transgenic expression in Ren2 rat
-
expression in COS-7 and CHO cells
-
expression of prorenin in CHO cells
-
expression of prorenin in CHO cells, expression of the FLAG-tagged renin/prorenin receptor in the cytoplasm of Trichoplusia ni Tn-5B1-4 insect cells using the baculovirus transfection system, subcloning in Escherichia coli strain DH10
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
angiotensin II inhibits renin release from the juxtaglomerular cells in the kidney
-
angiotensin II inhibits the release of renin from the kidney
-
renin-angiotensin-aldosterone system blockade with angiotensin-converting enzyme inhibitors and/or angiotensin receptor blockers leads to exacerbated renin release through loss of negative-feedback inhibition
-
the angiotensin type I receptor 1166C allele in homozygous form is characterized by low plasma renin levels
-
treatment with 16 mg azelnidipine for 4 weeks does not affect plasma renin activity
-
diuretics increase plasma renin concentration and plasma renin activity, as volume depletion stimulates the release of renin from the kidney
-
renin inhibitors like aliskiren increase the plasma concentration of renin because they attenuate the negative feedback effect of angiotensin II on renin release
-
renin release from juxtaglomerular cells is inhibited by Ca2+ and calcium-dependent phosphodiesterase 1C
-
renin release from juxtaglomerular cells is stimulated by cAMP
-
tubular renin protein is increased by angiotensin II (400 ng/kg/min infusion for 12 days) and angiotensin-converting enzyme inhibitor (lisinopril, 100 mg/l), but not by the combination of angiotensin II plus angiotensin-converting enzyme inhibitor
-
chronic sympatho-inhibition with rilmenidine (2.5 mg/kg/day) reduces basal plasma renin activity
-
after 5 weeks of renal artery stenosis, plasma renin activity is 3fold greater than in sham-operated rabbits
-
treatment with 0.05 mg urocortin 2 or 0.05 mg urocortin 2 plus 20 mg furosemide markedly reduces plasma renin activity
-
20 mg furosemide induces activation of renin
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
G149S/S150T
Q6DYE7
mutant enzyme shows lower specific activities than native renin. 50% loss in specific activity with 4-(4'-(dimethylaminophenylazo))-benzoyl-gamma-aminobutyryl-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS and 4-(4'-(dimethylaminophenylazo))-benzoyl-gamma-aminobutyryl-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS. Mutation has no effect on substrate specificity of canine renin
G149S/S150T/V286L
Q6DYE7
mutant enzyme shows lower specific activities than native renin
V286L
Q6DYE7
mutant enzyme shows lower specific activities than native renin
additional information
-
transgenic expression in Ren2 rat results in hypertension, insulin resistance, and cardiovascular damage. Treatment of young heterozygous male Ren2 and age-matched control rats with renin inhibitor aliskiren leads to significantly increased blood pressure, NADPH oxidase activity and subunit immunostaining, 3-nitrotyrosine, perivascular fibrosis, mitochondrial content and markers of activity in Ren2 rats. Both renin inhibition and blockade of the Ang I type receptor significantly attenuate cardiac functional and structural alterations
additional information
-
treatment of transgenic Ren2 rat results in systemic insulin resistance with decreased skeletal muscle insulin metabolic signaling and glucose uptake. Effects are associated with increased angiotensin II, mineralocorticoid receptor, angiotensin type I receptor, oxidative stress, and reduced tyrosine insulin receptor substrate phosphorylation, protein kinase B/(Akt) phosphorylation and GLUT-4 immunostaining
APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
diagnostics
-
comparison of active renin concentration and plasma renin activity for the diagnosis of primary hyperaldosteronism in patients with an adrenal mass, the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary hyperaldosteronism
diagnostics
-
the plasma aldosterone-to-renin ratio measuring plasma renin activity, PRA, is used for screening of primary aldosteronism
diagnostics
-
the ratio of plasma aldosterone concentration to plasma renin activity is used for screening for primary aldosteronism in hypertension, development of a test method, overview
medicine
-
depending on incubation conditions, circulating renin inhibitors interfere with the recognition of active renin molecules by the monoclonal antibodies used in commercial available assays. Careful considerations must therefore by given to the methodology used for quantifying immunoreactive plasma active renin when patients are treated with renin inhibitors, to avoid an overestimation of the magnitude of active renin release attributable to conformational changes in plasma prorenin
medicine
-
hypertension is a pathophysiologically heterogeneous condition in which renin-angiotensin system activity is an important determinant of the blood pressure response to antihypertensive drug treatment. The pretreatment plasma renin activity level is a significant predictor of treatment efficacy despite the different experimental designs employed and the ethnically diverse populations evaluated. These observations support the case that pathophysiologic markers such as plasma renin activity should be incorporated into the design of studies that assess antihypertensive treatment strategies
medicine
-
plasma active renin concentration is superior to plasma renin activity and a high plasma active renin concentration is an independent prognostic predictor in heart failure patients who are already receiving angiotensin-converting enzyme inhibitors or angiotensin-receptor blockers
medicine
-
in patients with biopsy-confirmed post-transplant glomerulonephritis, statins and renal reini-angiotensin system blockers prolong graft survival. The effect persists after adjustment for presentation with nephrotic syndrome, graft dysfunction, mean arterial pressure, immunosuppression enhancement with mycophenolate mofetil
medicine
-
direct renin inhibition with aliskiren represents an effective option for the long-term treatment of essential hypertension
medicine
-
inhibition of the renin-angiotensin-aldosterone system plays a pivotal role in preventing and treating diabetic nephropathy. Inhibition of renin with aliskiren decreases blood pressure in patients with hypertension. Direct renin inhibition with aliskiren has antiproteinuric effects in type 2 diabetic patients with nephropathy and additive proteinuric effects when used in diabetic patients already treated with the maximal dose of angiotensin type 1 receptor blockers
medicine
-
plasma renin activity is an independent predictor of morbidity and mortality in patients with hypertension
medicine
-
renin inhibition is the preferred pharmacologic approach to blockade of the renin-angiotensin system. Renin inhibition offers substantial promise for cardioprotection and renoprotection
medicine
-
renin inhibition with aliskiren is useful for antihypertensive treatment in patients with severe arterial hypertension, in patients with an already long-lasting course of disease, and in the presence of comorbidities such as diabetes mellitus
medicine
-
renin is a target to prevent hypertension
medicine
-
renin-angiotensin system inhibition is used as treatment for the primary and secondary prevention of atrial fibrillation
medicine
-
there is an association of polymorphisms of renin-angiotensin-aldosterone system genes with the risk of non-control of hypertension in angiotensin-converting enzyme inhibitor drugs-treated patients
pharmacology
Q8IYK8
the renin-angiotensin system is a potential target for lymphangioleiomyomatosis therapy
pharmacology
-
after 12 weeks of treatment in patients with hypertension, aliskiren, atenolol and aliskiren/atenolol lower systolic and diastolic blood pressure from baseline by 14.3/11.3, 14.3/13.7 and 17.3/14.1 mmHg, respectively. Systolic blood pressure reductions with aliskiren/atenolol are significantly greater than those with aliskiren or atenolol alone, and diastolic blood pressure reductions are greater than with aliskiren alone. Diastolic blood pressure changes are larger with atenolol than with aliskiren. Aliskiren, atenolol and aliskiren/atenolol reduce geometric mean plasma renin activity from baseline by 65%, 52% and 61%, respectively. In patients with moderate or high baseline plasma renin activity, plasma renin activity is reduced to low levels at week 12 endpoint in a greater proportion of patients receiving aliskiren or aliskiren/atenolol than with atenolol. Aliskiren treatment is associated with numerically lower rates of adverse events and discontinuations due to adverse events compared with atenolol or combination treatment, and unlike atenolol is not associated with bradycardia
pharmacology
-
aliskiren at the highest approved dose of 300 mg once daily for 7 days and a 4-fold higher dose has no effect on cardiac repolarization or conduction in healthy volunteers
pharmacology
-
co-administration of aliskiren results in changes below 30% in pharmacokinetic parameters AUC and Cmax of digoxin, atorvastatin, o-hydroxyatorvastatin, and p-hydroxyatorvastatin, indicating no clinically significant interaction with P-glycoprotein or CYP3A4 substrates. Aliskiren AUC is significantly increased by coadministration with atorvastatin or ketoconazole
pharmacology
-
detailed pharmacodynamic analysis of aliskiren in humans. Development of an integrated pharmacokinetik/pharmacodynamic model for aliskiren, including an empirical submodel to account for additional complexities arising from multiple dosing
pharmacology
-
renal vasodilation in healthy people with renin inhibitor aliskiren exceeds responses seen with angiotensin-converting enzyme inhibitors and angiotensin receptor blockers. The effects are longer lasting and are associated with significant natriuresis. Aliskiren may provide more complete and more effective blockade of the renin-angiotensin system
pharmacology
-
study on long-term safety, tolerability, and antihypertensive efficacy on Japanese patients with mild to moderate essential hypertension. Aliskiren alone or in combination with a diuretic or a calcium channel blocker is well tolerated. The incidence of suspected study-related adverse events was 25.3%. The overall responder efficacy was 73.3% at the endpoint. A clinically meaningful reduction of 17.6/12.8 m Hg from baseline was achieved in the mean sitting blood pressure at the endpoint
medicine
-
renin inhibition improves systemic insulin sensitivity, insulin metabolic signaling and glucose transport, along with normalization of angiotensin II, angiotensin type I receptor and mineralocorticoid receptor levels, oxidative stress markers, fibrosis and mitochondrial structural abnormalities
pharmacology
-
treatment of Watanabe heritable hyperlipidemic rabbits with aliskiren or aliskiren plus valsartan leads to greater increases in plasma nitric oxide concentration in response to intra-aortic acetylcholine infusion than in control. Aliskiren plus valsartan treatment increases acetylcholine-induced nitric oxide by 6.2 nmol/l, which is significantly higher than with either aliskiren or valsartan alone. Vascular superoxide and peroxynitrite levels are both significantly higher in controls and significantly lower in the aliskiren plus valsartan group than in the aliskiren or valsartan group
medicine
-
renin angiotensin system inhibition improves diabetic nephropathy at several levels, independently of its effects on blood pressure and glycemic control, via mechanisms depending of renal oxidative stress
medicine
-
blockade of renin activation is a therapeutic target to prevent glomerular injury and associated proteinuria