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Literature summary for 3.4.23.15 extracted from

  • Xu, Z.; Cacatian, S.; Yuan, J.; Simpson, R.D.; Jia, L.; Zhao, W.; Tice, C.M.; Flaherty, P.T.; Guo, J.; Ishchenko, A.; Singh, S.B.; Wu, Z.; McKeever, B.M.; Scott, B.B.; Bukhtiyarov, Y.; Berbaum, J.; Mason, J.; Panemangalore, R.; Cappiello, M.G.; Bentley, R.; Doe, C.P.; Harrison, R.K.; McGeehan, G.M.; Dillard, L.W.
    Optimization of orally bioavailable alkyl amine renin inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 694-699.
    View publication on PubMed
Search for more literature for 3.4.23.15

Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-[(1S)-1-(3-chlorophenyl)-1,5-dihydroxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(propanoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-(sulfamoylamino)butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylcarbamoyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-4-[(methylsulfonyl)amino]butyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(cyclopropylcarbonyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-1-(3-chlorophenyl)-4-[(dimethylcarbamoyl)amino]-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-4-(acetylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-4-(butanoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-3-[(1S)-4-(carbamoylamino)-1-(3-chlorophenyl)-1-hydroxybutyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
-
 Homo sapiens
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
-
 Homo sapiens
aliskiren
-
 Homo sapiens
ethyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
 Homo sapiens
methyl (2-[(R)-(3-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
 Homo sapiens
methyl (2-[(R)-(3-chloro-5-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
 Homo sapiens
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
 Homo sapiens
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
 Homo sapiens
methyl (2-[(R)-(5-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
 Homo sapiens
methyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-chlorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,3-difluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,5-difluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,4-difluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,5-difluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-methylphenyl)methoxy]ethyl]carbamate
-
 Homo sapiens
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](phenyl)methoxy]ethyl]carbamate
-
 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
-
-
-

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
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens
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 Homo sapiens