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Literature summary for 3.4.23.15 extracted from

  • Yamaguchi, Y.; Menear, K.; Cohen, N.C.; Mah, R.; Cumin, F.; Schnell, C.; Wood, J.M.; Maibaum, J.
    The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin (2009), Bioorg. Med. Chem. Lett., 19, 4863-4867.
    View publication on PubMed
Search for more literature for 3.4.23.15

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide
-
 Homo sapiens
(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-methylhexanamide
-
 Homo sapiens
(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
(2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
-
 Homo sapiens
(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
aliskiren highly potent selective inhibitor of human renin Homo sapiens
methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
-
 Homo sapiens
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
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
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
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
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
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
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
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
N-[(2S,3S,5S)-2-amino-5-(butylcarbamoyl)-3-hydroxy-6-methylheptyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
angiotensinogen + H2O Homo sapiens
-
 angiotensin I + angiotensinogen propeptide
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
angiotensinogen + H2O
-
 Homo sapiens angiotensin I + angiotensinogen propeptide
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000006
-
 at pH 7.4, temperature not specified in the publication Homo sapiens aliskiren
0.000001
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2R,4S,5S,7S)-5-amino-N-butyl-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
0.000001
-
 at pH 7.4, temperature not specified in the publication Homo sapiens 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
0.000001
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5S)-2-amino-5-(butylcarbamoyl)-3-hydroxy-6-methylheptyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
0.000001
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(4-methoxybutyl)-N-(propan-2-yl)benzamide
0.000002
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
0.000002
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
0.000003
-
 at pH 7.4, temperature not specified in the publication Homo sapiens methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
0.000006
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethynyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
0.000007
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (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
0.000008
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-bromo-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
0.000008
-
 at pH 7.4, temperature not specified in the publication Homo sapiens N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-3-(3-methoxypropoxy)-4-methyl-N-(propan-2-yl)benzamide
0.000013
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-methylhexanamide
0.0001
-
 at pH 7.4, temperature not specified in the publication Homo sapiens methyl [2-(5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxyphenyl)ethyl]carbamate
0.0003
-
 at pH 7.4, temperature not specified in the publication Homo sapiens (2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[[4-methoxy-3-(3-methoxypropoxy)phenyl]sulfonyl](propan-2-yl)amino]-2-methylhexanamide
0.1
-
 IC50 above 0.1 mM, at pH 7.4, temperature not specified in the publication Homo sapiens (2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide