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Information on EC 3.4.23.15 - renin
for references in articles please use BRENDA:EC3.4.23.15
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EC Tree 3 Hydrolases
3.4 Acting on peptide bonds (peptidases)
3.4.23 Aspartic endopeptidases
3.4.23.15 renin
IUBMB Comments
Formed from prorenin in plasma and kidney. In peptidase family A1 (pepsin A family).
The enzyme appears in viruses and cellular organisms
- 3.4.23.15
- hypertension
- aldosterone
- arterial
- urinary
- cardiovascular
- cardiac
-
antihypertensive
-
normotensive
- gastric
- glomerular
-
natriuretic
-
hemodynamic
-
systolic
-
diastolic
-
sympathetic
- ras
-
angiotensin-converting
- norepinephrine
- output
- adrenal
-
blocker
- prostaglandin
- ventricular
- catecholamine
-
diuretic
- creatinine
- hg
-
electrolyte
-
placebo
- vasopressin
- captopril
-
vasodilator
- cortisol
-
supine
-
intrarenal
-
renovascular
-
conscious
-
pressor
-
posture
- acth
- noradrenaline
- losartan
-
hypotensive
-
mineralocorticoid
-
vasoconstriction
- enalapril
- furosemide
- anp
- medicine
-
macula
- pharmacology
-
aceis
- diagnostics
showSynonyms
renin, prorenin, angiotensinogenase, angiotensin-forming enzyme, more
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SYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
angiotensin-forming enzyme
-
-
-
-
angiotensinogenase
EC 3.4.4.15
-
-
formerly
-
EC 3.4.99.19
-
-
formerly
-
REN
angiotensinogenase
-
-
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
cleavage of Leu-/- bond in angiotensinogen to generate angiotensin I
inhibits vasorelaxation induced by nitroso albumin
-
cleavage of Leu-/- bond in angiotensinogen to generate angiotensin I
-
-
-
-
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
endopeptidase
-
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CAS REGISTRY NUMBER
COMMENTARY
9015-94-5
-
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
4-(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
Substrates: -
Products: -
Products: -
?
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
-
Substrates: fluorogenic peptide
Products: -
Products: -
?
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
Substrates: -
Products: -
Products: -
?
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
?
-
Substrates: commercial renin peptide substrate 1
Products: -
Products: -
?
Arg-Glu(EDANS)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Leu-Val-Ile-His-Thr-Lys(Dabcyl)-Arg + H2O
?
Substrates: -
Products: -
Products: -
?
Arg-Glu(EDANS)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(DABCYL)-Arg + H2O
?
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide + H2O
?
-
Substrates: -
Products: -
Products: -
?
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide + H2O
benzyloxycarbonyl-Pro-Phe-His-Leu + Leu-Val-Tyr-Ser-beta-naphthylamide
-
Substrates: -
Products: -
Products: -
?
DABCYL-c-Abu-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-EDANS + H2O
?
Substrates: -
Products: -
Products: -
?
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
human angiotensinogen + H2O
angiotensin I + VIHN
-
Substrates: DRVYIHPFHLVIHN
Products: -
Products: -
?
megsin + H2O
?
-
Substrates: 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
Products: -
Products: -
?
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
-
Substrates: -
Products: -
Products: -
?
porcine angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: DRVYIHPFHLLVYS
Products: -
Products: -
?
recombinant ovine angiotensinogen from CHO cells + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
recombinant ovine angiotensinogen from Escherichia coli + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + ?
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + ?
-
Substrates: 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
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + ?
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary hyperaldosteronism, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary aldosteronism, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin is an active component of the local synovial renin-angiotensin system in rheumatoid arthritis, renin-angiotensin system in synovial fluid, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: 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
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
711396, 711686, 711767, 711766, 711778, 711793, 710784, 711797, 711802, 711814, 711896, 711895, 711901, 711919, 712135, 712254
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin is a highly specific enzyme for angiotensinogen
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin catalyses the rate-limiting step in the system and has unique specificity for its substrate angiotensinogen
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin cleaves the Leu10-Leu11 bond
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
Substrates: DRVYIHPFHLVIHNESTC
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the renin-angiotensin system is responsible for regulation of blood pressure and electrolytic balance
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: enzyme activity is increased in hypertensive mice
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: 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
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
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
-
Substrates: -
Products: -
Products: -
?
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
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
-
Substrates: the enzyme possesses no general protease activity
Products: -
Products: -
?
additional information
?
-
Substrates: tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: the main role of the enzyme is the intracellular generation of angiotensin
Products: -
Products: -
?
additional information
?
-
-
Substrates: the main role of the enzyme is the intracellular generation of angiotensin
Products: -
Products: -
?
additional information
?
-
-
Substrates: possible binding mechanism of prorenin and renin to the renin/prorenin receptor, overview
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
?
-
Substrates: role in regulating blood pressure
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary hyperaldosteronism, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the ratio of plasma renin activity to plasma aldosterone concentration is a screening test for primary aldosteronism, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin is an active component of the local synovial renin-angiotensin system in rheumatoid arthritis, renin-angiotensin system in synovial fluid, overview
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
711396, 711686, 711767, 711766, 711778, 711793, 710784, 711797, 711802, 711814, 711896, 711895, 711901, 711919, 712135, 712254
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin is a highly specific enzyme for angiotensinogen
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin catalyses the rate-limiting step in the system and has unique specificity for its substrate angiotensinogen
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: renin cleaves the Leu10-Leu11 bond
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: the renin-angiotensin system is responsible for regulation of blood pressure and electrolytic balance
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: enzyme activity is increased in hypertensive mice
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: 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
Products: -
Products: -
?
angiotensinogen + H2O
angiotensin I + angiotensinogen propeptide
-
Substrates: -
Products: -
Products: -
?
additional information
?
-
Substrates: tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: tissue-specific renin-angiotensin system in pulmonary lymphangioleiomyomatosis in LAM cells promotes cell proliferation and migration together with LAM nodules, overview
Products: -
Products: -
?
additional information
?
-
-
Substrates: the main role of the enzyme is the intracellular generation of angiotensin
Products: -
Products: -
?
additional information
?
-
-
Substrates: the main role of the enzyme is the intracellular generation of angiotensin
Products: -
Products: -
?
additional information
?
-
-
Substrates: possible binding mechanism of prorenin and renin to the renin/prorenin receptor, overview
Products: -
Products: -
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
INHIBITOR
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
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-
(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
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-
(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-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
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-
(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
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-
(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
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-
(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
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-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(sulfamoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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-
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylcarbamoyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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-
(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
-
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(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(dimethylcarbamoyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(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
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(3R)-3-[(1S)-4-(carbamoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(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
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(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
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(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
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(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methoxyphenyl)pentyl]piperidine-1-carboxamide
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(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
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(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethoxy)phenyl]pentyl]piperidine-1-carboxamide
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(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
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(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
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(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
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(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
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(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
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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
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3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
-
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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
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3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
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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
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-
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
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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
-
-
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
-
-
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
-
-
AGVTVS
1 mg/ml, about 82% inhibition. Peptide derived from pigeon pea, exhibits the strongest activity against angiotensin-converting enzyme, renin as well as superoxide and hydroxyl radicals
-
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
-
cod protein hydrolysate
-
non-competitive inhibition, 43% renin-inhibitory activity at 1 mg/ml
-
cod protein hydrolysate fraction CF3
-
non-competitive inhibition, 63% renin-inhibitory activity at 1 mg/ml
-
diazoacetyl methyl ester derivatives of glycine, norleucine, leucine
-
in presence of Cu2+
-
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
-
-
GRIST
1 mg/ml, about 25% inhibition. Peptide derived from pigeon pea, exhibits activity against angiotensin-converting enzyme, renin as well as superoxide and hydroxyl radicals
-
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
N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
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
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
-
-
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
-
-
TKDIG
1 mg/ml, about 20% inhibition. Peptide derived from pigeon pea, exhibits activity against angiotensin-converting enzyme, renin as well as superoxide and hydroxyl radicals
-
YY
-
dipeptide derived from royal jelly proteins. YY inhibits the renin activity only at acidic pH values below 8.0
(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-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-morpholin-4-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-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-(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-(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-(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-(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-[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]-2,8-dimethyl-N-[4-(methylamino)-4-oxobutyl]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-(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-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-(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-hydroxybutyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(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-[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-[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-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-2,8-dimethylnonanamide
-
-
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
-
-
(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-(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]-2,8-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-(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]-2,8-dimethylnonanamide
-
-
(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]-2,8-dimethylnonanamide
-
-
(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]-2,8-dimethylnonanamide
-
-
(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-(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-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
-
-
(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]-2,8-dimethylnonanamide
-
-
(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-(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-[(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]-2,8-dimethylnonanamide
-
-
(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]-2,8-dimethylnonanamide
-
-
(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-(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-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
-
-
(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-(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]-2,8-dimethylnonanamide
-
-
(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-(dimethylsulfamoyl)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-(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)-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
-
-
(2R,4S,5S,7S)-N-[2-(acetylamino)ethyl]-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
-
(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)-1,5-dihydroxypentyl]-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-(methylamino)propan-2-yl]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-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
-
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-(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
-
-
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)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]-2,8-dimethylnonanoyl]amino)butyl acetate
-
-
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)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
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
-
-
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
-
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
-
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
-
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
-
direct renin inhibitor, aliskiren has the potential to reduce end organ damage in chronic kidney disease
aliskiren
-
orally effective, nonpeptide, low-molecular-weight, direct renin inhibitor
aliskiren
-
orally effective direct renin inhibitor, aliskiren inhibits the renin-angiotensin-aldosterone system by blocking the enzymatic activity of renin
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
-
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
-
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
-
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
-
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
CGP 60536
-
automated quantitative determination of the inhibitor by high-performance liquid chromatography
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]-2,8-dimethylnonanoyl]-beta-alaninate
-
-
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
-
-
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
-
-
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-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-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-[(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]-2,8-dimethylnonanoyl]-beta-alanine
-
-
soyasaponin I
-
i.e. soybean renin inhibitor. Significant inhibition of recombinant renin, partially noncompetitive
transition state analogues
-
angiotensinogen modified in P1 or P1' position by e.g. statine, statine-derivatives, keto-groups, hydroxyethylene; in vivo effect
-
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
additional information
-
high glucose concentration stimulates intracellular renin activity and angiotensin II generation in mesangial cells
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0036
4-(4-dimethylaminophenylazo)benzoic acid-IHPFHLVIHT-5-[(e-amino-ethyl)amino]naphthalene-1-sulfonic acid
-
-
0.12
acetyl-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser
-
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, 37°C
0.01937
Arg-Glu(EDANS)-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Thr-Lys(DABCYL)-Arg
at pH 8.0 and 37°C
0.000072
recombinant ovine angiotensinogen from CHO cells
-
at pH 7.2 and 37°C
-
0.000071
recombinant ovine angiotensinogen from Escherichia coli
-
at pH 7.2 and 37°C
-
0.03 - 0.041
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-2-naphthylamide
-
depending on isoenzyme
0.03 - 0.041
benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-2-naphthylamide
-
depending on isoenzyme
additional information
aliskiren
-
estimated Km1 value is 0.516 ng/ml, Km2 value is 135 ng/ml
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.59
recombinant ovine angiotensinogen from Escherichia coli
-
at pH 7.2 and 37°C
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
8300
recombinant ovine angiotensinogen from Escherichia coli
-
at pH 7.2 and 37°C
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000021
(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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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 25°C
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
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0000004
(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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
at pH 7.4 and 37°C
0.000132
(2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.1
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
at pH 7.4, temperature not specified in the publication
0.000002 - 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
0.000002 - 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
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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000008 - 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
0.000002 - 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
0.000007 - 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
0.000002 - 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
0.000003 - 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
0.000002 - 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
0.000003 - 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
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004 - 0.000002
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-(3-methoxypropyl)-2,8-dimethylnonanamide
0.000005 - 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
0.000002 - 0.000003
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(3-hydroxypropyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.0000008 - 0.000017
(2R,4S,5S,7S)-5-amino-4-hydroxy-N-(4-hydroxybutyl)-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
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
Homo sapiens
-
pH and temperature not specified in the publication
0.00001 - 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
0.000004 - 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
0.000002 - 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
0.00004 - 0.000092
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
0.000092
(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
Homo sapiens
-
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
Homo sapiens
-
pH and temperature not specified in the publication
0.0000006 - 0.000015
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
0.000016
(2R,4S,5S,7S)-5-amino-N-(2-aminoethyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000007 - 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
0.000007
(2R,4S,5S,7S)-5-amino-N-(3-amino-3-oxopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000001 - 0.000003
(2R,4S,5S,7S)-5-amino-N-(3-cyanopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.000001 - 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
0.000001
(2R,4S,5S,7S)-5-amino-N-(4-amino-4-oxobutyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 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
0.000002
(2R,4S,5S,7S)-5-amino-N-(5-amino-5-oxopentyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000006 - 0.000018
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
0.000006
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000011 - 0.000031
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
0.000001 - 0.000025
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.000001 - 0.000002
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
0.000002 - 0.00007
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
0.000002 - 0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2-methylnonanamide
Homo sapiens
-
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
0.000021 - 0.00005
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[(methylsulfonyl)methoxy]benzyl]-2,8-dimethylnonanamide
0.000019 - 0.00014
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2,8-dimethylnonanamide
0.000019
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(2-methoxyethoxy)ethoxy]benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000042 - 0.00009
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2,8-dimethylnonanamide
0.000042
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000003 - 0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
0.000003 - 0.000009
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
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
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 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
0.000018 - 0.000053
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.000018
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylamino)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000002 - 0.000009
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylsulfamoyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.000004
(2R,4S,5S,7S)-5-amino-N-[2-(ethylsulfonyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000006 - 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
0.000002 - 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
0.0000003 - 0.000018
(2R,4S,5S,7S)-N-[2-(acetylamino)ethyl]-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.00000013
(3R)-3-[(1S)-1-(3-bromophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000021
(3R)-3-[(1S)-1-(3-chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.00000047
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000037
(3R)-3-[(1S)-1-(3-cyanophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000039
(3R)-3-[(R)-(3-chloro-2-fluorophenyl)(3-methoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000004
(3R)-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000764
(3R)-3-[(R)-(3-chlorophenyl)(3-hydroxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000021
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000038
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.0000055
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000055
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000308
(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-methoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000004
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(2-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000009
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-ethylphenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000003
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000007
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000016
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000125
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000609
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000011
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(3-fluorophenyl)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.00004
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000058
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-fluorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
0.000006
(3R)-N-[(2S)-1-[(chloromethyl)amino]-3-cyclohexylpropan-2-yl]-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
Homo sapiens
in 50 mM BES buffer, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, at 25°C
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
pH and temperature not specified in the publication
0.0194
2'-O-beta-D-glucopyranosyl momordin Ic
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.0384
2'-O-beta-D-glucopyranosyl momordin IIc
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.0000019
2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000055 - 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
0.00026
3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00021
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000079
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.0000004
3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
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
Homo sapiens
-
at pH 7.4 and 37°C
0.00000027
3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000011
3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000009
3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000021
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000019
3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
0.00000026
3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
Homo sapiens
-
at pH 7.4 and 37°C
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
Homo sapiens
-
at pH 7.4 and 37°C
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
Homo sapiens
-
at pH 7.4 and 37°C
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
Homo sapiens
-
at pH 7.4 and 37°C
0.000003 - 0.000013
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
0.000006 - 0.000009
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butyl acetate
0.000003
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butanoic acid
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
at pH 7.4 and 37°C
0.00656
5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine
Homo sapiens
-
-
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
Homo sapiens
-
-
0.000095
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
Homo sapiens
-
-
0.000691
6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
Homo sapiens
-
-
0.000058
6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
Homo sapiens
-
-
0.000173
6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
Homo sapiens
-
-
0.0000004 - 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
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
Homo sapiens
-
pH and temperature not specified in the publication
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
Homo sapiens
-
pH and temperature not specified in the publication
0.0774
chikusetsusaponin IV
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.000004 - 0.000013
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
0.000004
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alaninate
Homo sapiens
-
pH and temperature not specified in the publication
0.0571
glycyrrhizin
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
2.3
L-Ile-L-Trp
Homo sapiens
-
recombinant enzyme, in 50 mM Tris-HCl buffer containing 100 mM NaCl (pH 8.0), at 37°C
0.000003
methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
Homo sapiens
-
at pH 7.4, temperature not specified in the publication
0.000001 - 0.000003
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
pH and temperature not specified in the publication
0.000004 - 0.00019
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
0.0259
momordin Ic
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.0468
momordin IIc
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.0422
monoglucuronyl glycyrrhetic acid
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
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
Homo sapiens
-
at pH 7.4 and 37°C
0.0000002 - 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
0.000012 - 0.000023
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alanine
0.000012
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alanine
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
-
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
Homo sapiens
-
-
0.0336
soyasaponin I
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
0.0303
soyasaponin II
Homo sapiens
-
in 50 mM sodium phosphate, pH 6.5, 0.1 M NaCl, 0.02% (v/v) Tween 20, at 37°C
-
0.044
tetradecanoyl acetal sodium sulfite
Homo sapiens
-
complex formation with the enzyme, mixed inhibition type, IC50: 0.044 mM
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.0000004
(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-N-(3-methoxypropyl)-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.0000006
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000015
(2R,4S,5S,7S)-5-amino-7-[3-(benzyloxy)-4-methoxybenzyl]-N-butyl-4-hydroxy-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, 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]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-(3-cyanopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000006
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000018
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[3-(3-hydroxypropoxy)-4-methoxybenzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000011
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000031
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(2-methoxyethoxy)benzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000001
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000001
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanamide
Homo sapiens
-
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
Homo sapiens
-
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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.00007
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(4-methoxybutoxy)benzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pentyloxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000005
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(pyridin-4-ylmethoxy)benzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000021
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[(methylsulfonyl)methoxy]benzyl]-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000042
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-[2-(methylamino)-2-oxoethoxy]benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000003
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000004
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(2-ethoxyethoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000003
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, purified enzyme
0.000009
(2R,4S,5S,7S)-5-amino-N-butyl-7-[3-(3-ethoxypropoxy)-4-methoxybenzyl]-4-hydroxy-2,8-dimethylnonanamide
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000002
(2R,4S,5S,7S)-5-amino-N-[2-(dimethylsulfamoyl)ethyl]-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
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
Homo sapiens
in buffer
0.000003
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, 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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
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
Homo sapiens
in buffer
0.0000005
aliskiren
Homo sapiens
in 50 mM BES, 150 mM NaCl, 0.25 mg/ml bovine serum albumin, pH 7.0, temperature not specified in the publication
0.000004
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000001
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
0.000004
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
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
Homo sapiens
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
Homo sapiens
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
Homo sapiens
-
pH 7.2, 37°C, 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
Callithrix sp.
-
pH 7.2, 37°C, plasma enzyme assay
additional information
aliskiren
Homo sapiens
-
estimated concentration of aliskiren necessary for producing 50% inhibition of plasma renin activity is 0.66 ng/ml
additional information
chitooligosaccharide
Homo sapiens
-
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
-
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SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
0.000064
-
enzyme from kidney of TGM (rTon) transgenic mice that express rat tonin, at pH 7.5 and 37°C
additional information
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
additional information
-
1 Goldblatt unit: generation of 120000 ng angiotensin I per h
additional information
-
1675 Goldblatt units/mg, 1 Goldblatt unit: generation of 120000 ng angiotensin I per h
additional information
-
renin activity in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
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
-
ratio of plasma aldosterone concentration to plasma renin activity
additional information
-
renin content and activity in serum and synovial fluid from healthy persons, and from patients with osteoarthritis or rheumatism, overview
additional information
enzyme activity in lymphangioleiomyomatosis nodules and cells, overview
additional information
-
enzyme activity in lymphangioleiomyomatosis nodules and cells, overview
additional information
-
mass spectrometric methods for evaluation of plasma renin activity applicable for quantitative proteomics, overview
additional information
-
activity in submandibular gland tissue of wild-type BPN and hypertensive BPH mice
additional information
-
renin activity in conscious hindlimb-unloaded rats
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pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
4 - 4.5
-
substrate benzyloxycarbonyl-Pro-Phe-His-Leu-Leu-Val-Tyr-Ser-beta-naphthylamide
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pH RANGE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
37
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ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
95749, 95750, 95751, 95753, 95754, 95755, 95757, 95758, 95759, 95761, 95762, 95763, 95764, 95766, 95772, 95776, 95779, 95780, 95781, 95783, 95785, 95786, 95788, 95798, 95799, 95800, 95802, 95803, 95804, 95807, 95809, 95810, 95812, 652615
-
-
brenda
-
668017, 669705, 670872, 677442, 677527, 678986, 679245, 681186, 681314, 681706, 696615, 696833, 697155, 697360, 697430, 698064, 699192
-
-
brenda
-
711389, 711396, 711406, 711431, 711686, 711766, 711767, 711778, 711793, 711797, 711802, 711814, 711895, 711896, 711901, 711919, 712135, 712254, 712265, 712634, 712874, 712875, 712922, 712931, 713093, 713103, 713104, 713170, 717078, 717093, 717506, 717688, 753084, 753638
-
-
brenda
healthy persons, hypertensive patients, and patients with aldosterone- and/or cortisol secreting adenomas
-
-
brenda
-
29366, 95756, 95760, 95763, 95765, 95768, 95770, 95771, 95775, 95776, 95792, 95795, 95798, 95811, 650745, 677495, 680100, 707920, 710820, 710822, 754490, 769473
-
-
brenda
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SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
-
renin is present in the vascular endothelium and intensely expressed in the epithelial basal layer of periodontally affected gingival tissue
brenda
-
renin activity in conscious hindlimb-unloaded rats compared to untreated rats
brenda
-
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
brenda
additional information
-
determination of plasma aldosterone-to-renin ratio thresholds in plasma of healthy persons, patients with hypertension and those with additional adrenal adenomas, overview
brenda
-
plasma renin activity, PRA, and active renin concentration, ARC, overview
brenda
-
-
679245, 677442, 681186, 711396, 711686, 711778, 711793, 711797, 711802, 711896, 711895, 712135, 712265, 712634, 712874, 712875, 712922, 712931, 711431, 711389, 717688, 717093, 717506
brenda
-
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
brenda
-
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
brenda
-
renin is released as an active enzyme in the juxtaglomerular apparatus of the kidney
brenda
-
enzymatically inactive prorenin is primarily synthesized in the kidney and accounts for 70% to 90% of the renin in the circulation
brenda
-
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
brenda
-
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
brenda
-
enzyme activity is increased in hypertensive mice compared to wild-type mice
brenda
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LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
-
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
brenda
-
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
-
brenda
-
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
-
brenda
-
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
brenda
-
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
brenda
Highest Expressing Human Cell Lines
Cell Line LinksPlease wait a moment until the data is sorted. This message will disappear when the data is sorted.
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
metabolism
physiological function
metabolism
-
renin is the first rate-limiting enzymatic step in the renin-angiotensin-aldosterone system pathway
physiological function
-
the intrarenal renin-angiotensin-aldosterone system is activated and plays a critical role in the pathogenesis of chronic kidney disease
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
-
the renin-angiotensin-aldosterone system plays a key role in the regulation of blood volume, blood pressure, and cardiovascular and renal function
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
Show AA Sequence and Transmembrane Helices (987 entries)
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
Please use the AA Sequence and Transmembrane Helices Search for a specific query.
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PDB
SCOP
CATH
UNIPROT
ORGANISM
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MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
31000 - 44000
42000
45000 - 59000
46000
48000
additional information
42000
-
x * 46000, recombinant prorenin, SDS-PAGE, x * 42000, recombinant renin, SDS-PAGE
45000 - 59000
-
prorenin, activation by trypsin, or acidification, or pepsin, immunoprecipitation
46000
-
x * 46000, recombinant prorenin, SDS-PAGE, x * 42000, recombinant renin, SDS-PAGE
additional information
-
comparison of amino acid sequences with other aspartate proteinases
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SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
monomer
?
-
x * 46000, recombinant prorenin, SDS-PAGE, x * 42000, recombinant renin, SDS-PAGE
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
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POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
glycoprotein
proteolytic modification
side-chain modification
additional information
proteolytic modification
-
the inactive prorenin needs to be proteolytically activated to the mature active renin
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 25°C and pH 6.5
proteolytic modification
-
the inactive prorenin needs to be proteolytically activated to the mature active renin, activation in vitro by trypsin at 37°C
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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 angiotensinogen, sitting drop vapor diffusion method, using 1.74 M (NH4)2SO4 and 0.1 M Tris, pH 7.6
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 structure 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
-
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PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
G149S/S150T
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
mutant enzyme shows lower specific activities than native renin
V286L
mutant enzyme shows lower specific activities than native renin
additional information
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
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pH STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
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GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
bovine serum albumin, stabilization
dilution below 1 mg/ml, inactivation
freezing/thawing, inactivation
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STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
-20°C, 0.02 M sodium phosphate buffer, pH 6.2, 0.025 M NaCl, 6 months, 90% activity
-
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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
recombinant renin
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CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
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
-
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
after 5 weeks of renal artery stenosis, plasma renin activity is 3fold greater than in sham-operated rabbits
-
angiotensin II inhibits renin release from the juxtaglomerular cells in the kidney
-
chronic sympatho-inhibition with rilmenidine (2.5 mg/kg/day) reduces basal 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-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
-
the enzyme exhibits low mRNA expression levels in all stages of pre-adipocyte differentiation with no significant transcriptional increase up to day 21
-
there are no significant differences in mRNA abundance between salinities or time for the enzyme gene
-
there is an increase of renin activity in the kidney of TGM(rTon) mice when compared to control animals
-
treatment with 0.05 mg urocortin 2 or 0.05 mg urocortin 2 plus 20 mg furosemide markedly reduces plasma renin activity
-
treatment with 16 mg azelnidipine for 4 weeks does not affect plasma renin activity
-
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
-
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APPLICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
diagnostics
medicine
pharmacology
diagnostics
-
the plasma aldosterone-to-renin ratio measuring plasma renin activity, PRA, is used for screening of primary aldosteronism
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
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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
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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
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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
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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
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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
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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
medicine
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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
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direct renin inhibition with aliskiren represents an effective option for the long-term treatment of essential hypertension
medicine
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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
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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
medicine
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renin-angiotensin system inhibition is used as treatment for the primary and secondary prevention of atrial fibrillation
medicine
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renin inhibition is the preferred pharmacologic approach to blockade of the renin-angiotensin system. Renin inhibition offers substantial promise for cardioprotection and renoprotection
medicine
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plasma renin activity is an independent predictor of morbidity and mortality in patients with hypertension
medicine
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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
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blockade of renin activation is a therapeutic target to prevent glomerular injury and associated proteinuria
medicine
elevated renin concentrations are associated with cardiovascular instability and increased cases of acute kidney injury after cardiac surgery. Elevated renin concentrations may be used to identify high-risk patients for cardiovascular instability and acute kidney injury
medicine
soluble (pro)renin receptor s(P)RR levels are positively correlated with plasma renin activity of symptomatic heart failure with reduced ejection fraction patients
medicine
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in normotensive mice with dilated cardiomyopathy (DCM) and symptomatic heart failure with reduced ejection fraction (HFrEF), without renal dysfunction, plasma soluble (pro)renin receptor (s(P)RR) levels positively correlate with plasma renin activity and systemic edema, but not with ejection fraction. In female DCM mice with elevated plasma renin activity levels and plasma s(P)RR levels, direct renin inhibition normalizes plasma renin activity, lowers s(P)RR, and prevents symptomatic HFrEF
medicine
blood samples from patients with chronic renal failure show a considerable rise in the level of renin enzyme compared to healthy volunteers. Chronic renal failure affects several electrolytes and liver functions and causes a considerable increase in renin levels
pharmacology
the renin-angiotensin system is a potential target for lymphangioleiomyomatosis therapy
pharmacology
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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
pharmacology
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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
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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
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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
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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
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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
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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
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Release 2026.1 (March 2026)
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