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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(2R)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]-N-[3-(2-methoxyethoxy)-5-(3-methoxypropyl)benzyl]propanamide
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(2R)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
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(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[(4-methoxyphenyl)sulfonyl](propan-2-yl)amino]-2-methylhexanamide
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(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[4-methoxy-3-(3-methoxypropoxy)benzyl](propan-2-yl)amino]-2-methylhexanamide
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(2R,4S,5S)-5-amino-N-butyl-4-hydroxy-6-[[[4-methoxy-3-(3-methoxypropoxy)phenyl]sulfonyl](propan-2-yl)amino]-2-methylhexanamide
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(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
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(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
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(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
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(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
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(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
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(2R,4S,5S,7S)-5-amino-7-[3-(2-amino-2-oxoethoxy)-4-tert-butylbenzyl]-N-butyl-4-hydroxy-2-methylnonanamide
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(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
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(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
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(2R,4S,5S,7S)-5-amino-N-(3-aminopropyl)-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanamide
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(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
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(3R)-3-[(1S)-1-(3-bromophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(3R)-3-[(1S)-1-(3-chloro-2-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(3R)-3-[(1S)-1-(3-chloro-5-fluorophenyl)-1-hydroxy-5-methoxypentyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(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
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(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
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(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
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(3R)-3-[(1S)-4-(acetylamino)-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-(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
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(3R)-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(3R)-3-[(R)-(3-chlorophenyl)(3-hydroxypropoxy)methyl]-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]piperidine-1-carboxamide
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(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
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(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
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(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-chlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
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(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
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(3R)-N-[(2S)-1-amino-3-cyclohexylpropan-2-yl]-3-[(R)-(3-methoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
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(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
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(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
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(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-(3-fluorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methoxyphenyl)pentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-(3-methylphenyl)pentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-phenylpentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethoxy)phenyl]pentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-1-hydroxy-5-methoxy-1-[3-(trifluoromethyl)phenyl]pentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(1S)-5-ethoxy-1-hydroxy-1-phenylpentyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-ethoxypropoxy)methyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(2,3-dichlorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(3-fluorophenyl)methyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-ethoxypropoxy)(phenyl)methyl]piperidine-1-carboxamide
(3R)-N-[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]-3-[(R)-(3-fluorophenyl)(3-methoxypropoxy)methyl]piperidine-1-carboxamide
-
(3R)-N-[(2S)-1-[(chloromethyl)amino]-3-cyclohexylpropan-2-yl]-3-[(1S)-1-(3-chlorophenyl)-1-hydroxy-5-methoxypentyl]piperidine-1-carboxamide
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
-
(5R)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-9-azabicyclo[3.3.1]non-2-ene-2-carboxamide
-
-
1,2-epoxy-3-(p-nitrophenoxy)propane
-
-
2'-O-beta-D-glucopyranosyl momordin Ic
-
-
2'-O-beta-D-glucopyranosyl momordin IIc
-
-
2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
-
-
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
-
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
-
-
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
-
3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[2-chloro-5-[3-(dimethylamino)propyl]benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[[5-chloro-2-(3-methoxypropyl)-1-oxidopyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
3-amino-N-[[5-chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoic acid
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butyl acetate
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butanoic acid
-
-
4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]amino)butyl acetate
-
-
4-amino-N-[2-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]phenyl]-3-methoxybenzamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-5,5-difluoro-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-difluoro-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
4-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(3-methoxy-2-methylbenzyl)-5,5-dimethyl-1,2,5,6-tetrahydropyridine-3-carboxamide
-
-
5-amino-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)pentanamide
-
-
5-[4-[(3,5-difluorobenzyl)amino]phenyl]-6-ethylpyrimidine-2,4-diamine
-
-
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2H-1,4-benzoxazin-3(4H)-one
-
-
6-ethyl-5-[1-(3-methoxypropyl)-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
6-ethyl-5-[1-(3-methoxypropyl)-2-phenyl-1,2,3,4-tetrahydroquinolin-7-yl]pyrimidine-2,4-diamine
-
-
6-ethyl-5-[9-(3-methoxypropyl)-9H-carbazol-2-yl]pyrimidine-2,4-diamine
-
-
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
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
-
-
Bromoisocaproyl peptides
-
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
-
decanoyl acetal sodium sulfite
-
IC50: 0.273 mM
diazoacetyl methyl ester derivatives of glycine, norleucine, leucine
-
in presence of Cu2+
-
diisopropylfluorophosphate
-
gamma-renin only
dodecanoyl acetal sodium sulfite
-
IC50: 0.195 mM
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
-
-
hexanoyl acetal sodium sulfite
-
-
houttuynin
-
from the volatile oil of Houttuynia cordata
L-Ile-L-Trp
-
70% inhibition at 3.2 mM
L-Leu-L-Trp
-
37% inhibition at 3.2 mM
methyl (2-[(R)-(3-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chloro-5-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(3-chlorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (2-[(R)-(5-chloro-2-fluorophenyl)[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]methoxy]ethyl)carbamate
-
-
methyl (5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxybenzyl)carbamate
-
-
methyl 4-([(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]amino)butanoate
methyl [(4S)-4-(3-chlorophenyl)-4-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl]-4-hydroxybutyl]carbamate
-
-
methyl [2-(5-[[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl](propan-2-yl)carbamoyl]-2-methoxyphenyl)ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-chlorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-amino-3-cyclohexylpropan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(ethylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,3-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](2,5-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,4-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3,5-difluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-fluorophenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](3-methylphenyl)methoxy]ethyl]carbamate
-
-
methyl [2-[(R)-[(3R)-1-[[(2S)-1-cyclohexyl-3-(methylamino)propan-2-yl]carbamoyl]piperidin-3-yl](phenyl)methoxy]ethyl]carbamate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-methoxyphenoxy]methanesulfinate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]acetate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-2-ethyl-5-hydroxy-7-methyl-8-oxooctyl]-2-tert-butylphenoxy]methanesulfinate
-
-
methyl [5-[(2S,4S,5S,7R)-4-amino-8-(butylamino)-5-hydroxy-7-methyl-2-(1-methylethyl)-8-oxooctyl]-2-methoxyphenoxy]acetate
monoglucuronyl glycyrrhetic acid
-
-
N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
-
N-acetyl-D-glucosamine-2-epimerase
-
-
-
N-alpha-carbobenzoxy-Arg-Arg-Pro-Phe-His-Sta-Ile-His-Nepsilon-butyloxycarbonyl-Lys
-
-
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
N-cyclopropyl-N-[[1-(3-methoxypropyl)-1H-indol-3-yl]methyl]morpholine-2-carboxamide
-
-
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alanine
N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2-methylnonanoyl]-beta-alanine
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-3-(3-methoxypropoxy)-4-methyl-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-bromo-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-ethynyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-(4-methoxybutyl)-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5R)-2-amino-6-(butylamino)-3-hydroxy-5-methyl-6-oxohexyl]-4-methoxy-3-[(1E)-4-methoxybut-1-en-1-yl]-N-(propan-2-yl)benzamide
-
-
N-[(2S,3S,5S)-2-amino-5-(butylcarbamoyl)-3-hydroxy-6-methylheptyl]-4-ethyl-3-(3-methoxypropoxy)-N-(propan-2-yl)benzamide
-
-
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]benzamide
-
-
N-[2-([2-amino-6-ethyl-5-[4-(3-methoxypropyl)-2,2-dimethyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl]pyrimidin-4-yl]amino)ethyl]naphthalene-2-sulfonamide
-
-
N-[2-[6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl]acetamide
-
-
N-[2-[7-([[(3R,4R)-4-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperidin-3-yl]oxy]methyl)-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[7-[[(2R)-1-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperazin-2-yl]methoxy]-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
-
octanoyl acetal sodium sulfite
-
-
Pro-Arg-Tyr
mixed-type inhibition
renin inhibitory peptide
-
-
-
Renin-binding protein
-
from hog kidney
-
tert-butyl [(3S,5S,6S,8S)-8-(butylcarbamoyl)-6-hydroxy-3-(4-methoxybenzyl)-2,9-dimethyldecan-5-yl]carbamate
-
potent low nanomolar inhibitor of renin
tetradecanoyl acetal sodium sulfite
-
complex formation with the enzyme, mixed inhibition type, IC50: 0.044 mM
tetrahydro-2H-pyran-4-yl cyclopropyl[[(3S,4S)-4-[(2R)-2-[4-methoxy-3-(3-methoxypropoxy)benzyl]-3-methylbutyl]pyrrolidin-3-yl]methyl]carbamate
-
-
transition state analogues
-
Trp-Gly
mixed-type inhibition
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
-
aliskiren
-
depending on incubation conditions, circulating renin inhibitors interfere with the recognition of active renin molecules by the monoclonal antibodies used in commercial available assaysCareful considerations must therefore by given to the methodology used for quantifying immunoreactive plasma active renin when patients are treated with renin inhibitors, to avoid an overestimation of the magnitude of active renin release attributable to conformational changes in plasma prorenin
aliskiren
-
non-peptide orally active renin inhibitor
aliskiren
-
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
-
low molecular weight, orally active renin inhibitor
aliskiren
-
SPP-100, formerly CGP-60539
aliskiren
-
highly potent selective inhibitor of human renin
aliskiren
-
direct renin inhibitor, aliskiren has the potential to reduce end organ damage in chronic kidney disease
aliskiren
-
oral direct renin inhibitor
aliskiren
-
orally active direct renin inhibitor
aliskiren
-
orally effective, nonpeptide, low-molecular-weight, direct renin inhibitor
aliskiren
-
nonpeptide, orally active, direct renin inhibitor
aliskiren
-
orally effective direct renin inhibitor, aliskiren inhibits the renin-angiotensin-aldosterone system by blocking the enzymatic activity of renin
aliskiren
-
targets the renin enzyme directly
aliskiren
-
direct renin inhibitor for the treatment of hypertension
aliskiren
-
a renin inhibitor used in the treatment of hypertension. Rifampicin reduces the renin-inhibiting effect of aliskiren (plasma renin activity 24 h after aliskiren intake is 61% higher after treatment with rifampicin (600 mg once daily for 5 days))
aliskiren
-
renin inhibition is more than 99% at 5 h after the 300 and 600 mg aliskiren doses
aliskiren
-
non-peptide, orally active, selective renin inhibitor
aliskiren
-
direct renin inhibitor for the treatment of hypertension
aliskiren
-
direct renin inhibitor
aliskiren
-
direct renin inhibitor, aliskiren is useful for antihypertensive treatment in patients with severe arterial hypertension, in patients with an already long-lasting course of disease, and in the presence of comorbidities such as diabetes mellitus
aliskiren
-
direct renin inhibitor
aliskiren
-
renin inhibitor in clinical practice for hypertension
aliskiren
-
the renin inhibitor prevents atherosclerosis progression
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
aliskiren
-
potent direct renin inhibitor
Bromoisocaproyl peptides
-
-
-
Bromoisocaproyl peptides
-
-
-
Bromoisocaproyl peptides
-
-
-
CGP 60536
-
automated quantitative determination of the inhibitor by high-performance liquid chromatography
enalkiren
-
-
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
-
-
pepstatin
-
-
pepstatin A
-
pepstatin A
-
almost complete inhibition at 0.01 mM
remikiren
-
-
soyasaponin I
-
i.e. soybean renin inhibitor. Significant inhibition of recombinant renin, partially noncompetitive
transition state analogues
-
regulation of blood pressure
-
transition state analogues
-
regulation of blood pressure
-
transition state analogues
-
-
-
transition state analogues
-
energy calculation for transition state complex
-
transition state analogues
-
angiotensinogen modified in P1 or P1' position by e.g. statine, statine-derivatives, keto-groups, hydroxyethylene; in vivo effect
-
transition state analogues
-
in vivo effect
-
transition state analogues
-
reduced analogous, keto- or hydroxyisosteres
-
transition state analogues
-
regulation of blood pressure
-
transition state analogues
-
regulation of blood pressure
-
zankiren
-
-
additional information
-
development of oral renin inhibitors and their pharmacokinetic and pharmacodynamic properties
-
additional information
-
renin is not inhibited by soyasapogenol B glycyrrhetic acid, saikosaponin b2, saikosaponin c and ginsenoside Rb1
-
additional information
-
not inhibited by L-Val-L-Trp and L-Ala-L-Trp
-
additional information
-
-
-
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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
0.0000005 - 0.0000006
aliskiren
0.0000033
BW-175
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.000001
CGP-29,287
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000003
CGP-44099A
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000007
CGP38560A
Homo sapiens
-
-
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
0.00000058
CI-992
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.000005
CP-72,647
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.00001
CP-81,198
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.000005
CP-81,282
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.273
decanoyl acetal sodium sulfite
Homo sapiens
-
IC50: 0.273 mM
0.0000004
ditekren
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.195
dodecanoyl acetal sodium sulfite
Homo sapiens
-
IC50: 0.195 mM
0.000014
enalkiren
Homo sapiens
-
-
0.0000073
ES 6864
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000007
ES-8891
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
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
0.0000006
FK906
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
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
0.0000069
GR 70982
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.00001
H-141
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
-
0.000001
H-77
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000006
KR1-1314
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
-
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
-
-
0.0000001
PD 133,450
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0008
pepstatin A
Canis lupus familiaris
-
0.09533
Pro-Arg-Tyr
Homo sapiens
at pH 8.0 and 37°C
0.0000008
remikiren
Homo sapiens
-
-
0.0000005
Ro 42-5892
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
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
-
0.00000035
SQ 33800
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000023
SR 42128
Canis lupus familiaris
-
0.0000001
SR 43845
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000011
terlakiren
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.044
tetradecanoyl acetal sodium sulfite
Homo sapiens
-
complex formation with the enzyme, mixed inhibition type, IC50: 0.044 mM
0.11234
Trp-Gly
Homo sapiens
at pH 8.0 and 37°C
0.00000047
YM-21095
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000029
YM-26365
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.0000011
zankiren
Homo sapiens
-
-
additional information
aliskiren
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
0.0000006
aliskiren
Homo sapiens
-
-
0.0000006
aliskiren
Canis lupus familiaris
-
0.0000006
aliskiren
Homo sapiens
-
pH and temperature not specified in the publication
0.0000006
aliskiren
Homo sapiens
-
at pH 7.4, temperature not specified in the publication
0.0000006
aliskiren
Homo sapiens
-
temperature not specified in the publication, at pH 7.4
0.000004
ethyl N-[(2R,4S,5S,7S)-5-amino-4-hydroxy-7-[4-methoxy-3-(3-methoxypropoxy)benzyl]-2,8-dimethylnonanoyl]-beta-alaninate
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
-
additional information
soyasaponin I
Homo sapiens
-
IC50 value 30 microg/ml at pH 6.5, 37°C
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