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((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
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((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
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(+)-usnic acid
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90.7% inhibition, the most active compound and could be used as a lead compound in developing novel anti-HCV agents. The major amino acid residues of NS3 protease likely involved in the interaction with (+)-usnic acid are Gln41, Ser42, Phe43, His57, Arg10
(-)-epicatechin-3-O-gallate
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(-)-epigallocatechin-3-O-gallate
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(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
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(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
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(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
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(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
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(10R,13R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10-cyclohexyl-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
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(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-oxo-2,7-dioxa-8-thia-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide 8,8-dioxide
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(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
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(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
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(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
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(11R,14R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-2-oxa-10,13-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-14-carboxamide
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(11S,14S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-1,10,13,17-tetraazabicyclo[14.2.1]nonadeca-16(19),17-diene-14-carboxamide
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(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-15-oxo-1,2,3,7,8,9,10,12a,13,14,15,15a-dodecahydrocyclopropa[f]pyrrolo[1,2-b][1,2,5]thiadiazacyclotetradecine-13a(6H)-carboxamide 5,5-dioxide
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most potent inhibitor of the series with sulfonamide linkage. The microsomally predicted clearance numbers is 0.17/0.7 L/h/kg (h/r)
(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-5,15-dioxo-1,2,3,5,6,7,8,9,10,12a,13,14,15,15a-tetradecahydro-13aH-cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclotetradecine-13a-carboxamide
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inhibitor with proline amide linkage, slightly more potent than inhibitors with sulfonamide linkage. The microsomally predicted clearance number is 0.17/0.82 L/h/kg (h/r)
(1aR,5S,10R,22aR)-5-tert-butyl-9-cyclopropyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-9-propyl-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10R,22aR)-9-(butan-2-yl)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,10S,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-9-phenoxy-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,19E,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,21,22,22a-dodecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,21aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-14-methoxy-3,6-dioxo-1a,3,4,5,6,9,10,17b,18,18a,19,20,21,21a-tetradecahydro-1H,8H-7,10-methanodicyclopropa[13,14:18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(difluoromethyl)cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethylcyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-methylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18-fluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(2,2-difluoroethyl)cyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(2-fluoroethyl)cyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
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(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
(1R)-2-but-3-en-1-yl-1-[[(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]hept-6-enoyl]-4-(quinolin-4-yloxy)-L-prolyl]amino]cyclopropanecarboxylic acid
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(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
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(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
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(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
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(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
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(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
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(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
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(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
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(1R,2S)-1-[([(1R,2R,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopentyl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-cyclopentylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-tert-butylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyldimethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethylpropylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-methyl-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl](methyl)carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,5S)-3-(N-[[(1S)-1-cyclohexyl-2-cyclopropyl-2-oxoethyl]carbamoyl]-3-methyl-L-valyl)-N-[1-(cyclopropylamino)-1,2-dioxohept-6-yn-3-yl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1R,5S)-3-[2(S)-[[[[1-[(1-azetidinylsulfonyl)methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-3-[2(S)-[[[[1-[[[cyclobutyl(methyl)amino]sulfonyl]methyl]cyclohexyl]amino] carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[N-(tert-butylcarbamoyl)-3-methyl-L-valyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyll]-butyl]-3-[2(S)-[[[[1-[[(dimethylamino)sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-2-[[[[1-[1(R)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-[[[[1-[1(S)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-(2-cyclopropyl-1,1-dioxido-5(R)-isothiazolidinyl)cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(2-fluoro-1,1-dimethylethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(cyclopropylmethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(1-methylethyl)amino]-sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[ethyl(methyl)amino]sulfonyl]methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[(4-morpholinylsulfonyl)-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[(methylamino)sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[[methyl(1-me5thylethyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-pemtyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(2-cyclopropylethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cycloppropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(cyclopropylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
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Boceprevir: EC50 and EC90 values, determined in a bicistronic, subgenomic, cell-based replicon assay run over 72 h using Huh-7 hepatoma cells, are 200 and 400 nM, respectively. Preclinical, metabolism and pharmacokinetics data are very promising. Currently ongoing phase II clinical trials demonstrate the compound to be well tolerated
(1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide
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(1S,5R)-6,6-dichloro-3-[cyclohexyl[[[(1,1-dimethylethyl)amino]carbonyl]amino]acetyl]-N-[1-[1,2-dioxo-2-(2-propenylamino)ethyl]butyl]-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
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(1S,5R)-N-((S)-5-cyclopropyl-1-(cyclopropylamino)-1,2-dioxopentan-3-yl)-3-((S)-2-(3-(1-((N-cyclopropyl-N-methylsulfamoyl)methyl)cyclohexyl)ureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-6,6,6-trifluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-7,7,7-trifluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-((1s,3S)-3-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(1-fluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(1-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(2,2-difluorocyclopropyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(3,3-difluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(5-amino-1,1,1-trifluoro-4,5-dioxopentan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
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(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2-(3-((12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,-13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
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(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2,10-dioxa-13-azatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[16.2.2.13,7]tricosa-1(20),3(23),4,6,18,21-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-2-(acetylamino)-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
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(2R)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-2-(4-methoxyphenyl)-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(6-methylpyridin-2-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-3-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-4-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(morpholin-4-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-[(2-phenylquinazolin-4-yl)oxy]-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,4S,7S,14Z)-7-tert-butyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-6,9-dioxo-3,4,6,7,8,9,12,13-octahydro-2H,11H-16,18-etheno-2,5-methanopyrido[2,3-k][1,10,3,6]dioxadiazacyclononadecine-4-carboxamide
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(2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14-carboxylic acid
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(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-5,16-dioxo-2-(quinolin-4-yloxy)-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
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(2R,6S,10Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
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(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine
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(2R,6S,12Z,14aR,16aS)-2-[(8-chloro-2-ethoxyquinolin-4-yl)oxy]-6-[[(cyclopentyloxy)carbonyl]amino]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-([7-methoxy-2-[2-(methylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxyquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[(4-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[2-(1H-imidazol-1-yl)-7-methoxyquinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrrol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(4-methyl-1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(5-methyl-1,3,4-oxadiazol-2-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[(5-ethoxythieno[3,2-b]pyridin-7-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
(2S)-([N-[3-([[(10S,13S)-10-cyclohexyl-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-trien-13-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
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(2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[17.2.2.13,7]tetracosa-1(21),3(24),4,6,19,22-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
(2S)-2-[([(1R,4R)-2-[[(1R)-1-[[(1R)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]butanoic acid
-
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(2S)-2-[[(2-[[(1S)-1-(methoxycarbonyl)-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
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(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoic acid
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-([7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(3-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxyquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-([2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
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-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
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(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
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(2S,4S)-1-((S)-2-(furan-2-carboxamido)-3,3-dimethylbutanoyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,4S)-1-((S)-2-benzamido-2-cyclohexylacetyl)-N-((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,4S)-1-((S)-2-benzamido-2-cyclohexylacetyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,4S)-1-((S)-2-cyclohexyl-2-(thiophene-2-carboxamido)acetyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,4S)-1-((S)-2-cyclohexyl-2-isobutyramidoacetyl)-N-((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,4S)-1-((S)-2-isobutyramido-3-phenylpropanoyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
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(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,15-trioxo-1,4,10-triazacyclopentadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,16-trioxo-1,4,10-triazacyclohexadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,17-trioxo-1,4,10-triazacycloheptadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,18-trioxo-1,4,10-triazacyclooctadecane-5-carboxamide
-
-
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
comparison of binding affinity with human neutrophil elastase, selectivity of 420
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
comparison of binding affinity with human neutrophil elastase, selectivity of 35
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
-
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
-
(3R,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
(3S)-3-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
(3S,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
(3S,18S)-18-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinoline-3-carboxamide
-
-
(3S,6S)-6-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-3-carboxamide
-
-
(4-acetylphenoxy)acetic acid
-
(4-aminophenyl)(2-aminopyridin-3-yl)methanone
-
(4-aminophenyl)(phenyl)methanone
-
(4-methoxyphenyl)(1H-pyrrol-2-yl)methanone
-
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-([(1S)-1-(4-bromophenyl)ethyl]carbamoyl)-2-propylhydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.000072 mM
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-([(1S)-2,3-dihydro-1H-inden-1-yl]carbamoyl)-2-propylhydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.0001 mM
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2R,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-butyl-2-([(1S)-1-phenylethyl]carbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.000099 mM, over 400fold selectivity for enzyme over human leukocyte elastase
(4R)-4-([(2S)-2-acetamido-3-carboxypropanoyl]amino)-5-([(2S,3S)-1-([(2S)-1-[(2S,4R)-4-(benzyloxy)-2-(2-ethyl-2-([(1S)-1-phenylethyl]carbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino)-3-methyl-1-oxopentan-2-yl]amino)-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.000085 mM
(4R)-4-[[(2S)-2-(acetylamino)-3-carboxypropanoyl]amino]-5-[(1-[[(1R)-1-([(2S,4R)-4-(benzyloxy)-2-[(2-[[(1S)-1-phenylethyl]carbamoyl]-2-propylhydrazino)carbonyl]pyrrolidin-1-yl]carbonyl)-2-methylpropyl]carbamoyl]-2-methylbutyl)amino]-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.000078 mM
(4R,6S,7Z,15S,17S)-17-[((7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl)oxy)methyl]-13-methyl-N-[(1-methylcyclopropyl)sulfonyl]-2,14-dioxo-1,3,13-triazatricyclo[13.2.0.0-4,6-]heptadec-7-ene-4-carboxamide
compound displays high mean clearance of 150 micro per minand mg protein in rat, cynomolgus monkey and human liver microsomes, along with a short half life of less than 10 min
(4R,6S,7Z,15S,17S)-17-[((8-chloro-7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl)oxy)methyl]-13-methyl-N-[(1-methylcyclopropyl)sulfonyl]-2,14-dioxo-1,3,13-triazatricyclo[13.2.0.0-4,6-]heptadec-7-ene-4-carboxamide
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
-
(4S,7S,9R)-4-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2,5-dioxo-10,15-dioxa-3,6-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-7-carboxamide
-
-
(5R,7S,10S)-10-cyclopentyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo(prop-2-en-1-ylamino)acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(1-phenylethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(pyridin-2-ylmethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclobutylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopentylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-1,6,7,9,10,11,12,14,15,16,17,18-dodecahydro-5H-2,22:5,8-dimethano-4,13,2,8,11-benzodioxatriazacycloicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[[(1-methylpropyl)amino](oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-N-[(1S)-1-[(benzylamino)(oxo)acetyl]butyl]-10-tert-butyl-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-methyl-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5R,8S,10R)-5-tert-butyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-2,11,15-trioxa-4,7-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.2.2]icosa-1(18),16,19-triene-8-carboxamide
-
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.3.1]icosa-1(20),16,18-triene-8-carboxamide
-
-
(5S,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-8-carboxamide
-
-
(6R,8S,11R)-11-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(6R,8S,11S)-11-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-8-carboxamide
-
-
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
-
(6S,11S,20S)-11-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-20-carboxamide
-
-
(6S,8S,9R,10S,13S)-13-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-triene-10-carboxamide
-
-
(7R,9S)-12-(2,3-dihydro-1H-inden-1-yl)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-15-methyl-11,14-dioxo-2,6-dioxa-10,13,15-triazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methoxy-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-19-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-6-(phenylsulfonyl)-2-oxa-6,10,13-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[[4-(dimethylamino)-2,4-dioxo-3-phenylbutyl]amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
50% inhibition at 400 nM
(7R,9S,12S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(1-methylethyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(2-methylpropyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(S)-cyano(phenyl)methyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7S,12S,21S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-21-carboxamide
-
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
-
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid
-
-
(R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
-
-
(R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(S)-((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
-
(S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(R)-1-[((R)-cyclohexylmethoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-butyric acid
-
21% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
35% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((R)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
37% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-butyric acid
-
65% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
100% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-4,4-difluoro-butyric acid
-
-
(S)-2-[[(1R,4R)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1S,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonylmethyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
(S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(Z)-(1R,4R,6S,14R,16R)-12-tert-butoxycarbonylamino-16-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,13-dioxo-3,12-diaza-tricyclo[12.3.0. 04, 6]heptadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-13-tert-butoxycarbonylamino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo-[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,16R,18R)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,16R,18R)-14-tert-butoxycarbonylamino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R) and (1S,4R,6S,17S)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadeca-7,15-diene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R,19R)-15-amino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R,19R)-15-tert-butoxycarbonylamino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,18R) and (1S,4R,6S,18S)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadeca-7,16-diene-4-carboxylic acid
-
-
1,1-dimethylethyl [1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[1,2-dioxo-2-(2-propenylamino) ethyl]butyl]-amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl [2-[(1S,5R)-2(S)-[[[1-(2-amino-1,2-dioxoethyl)butyl]amino]carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]-carbamate
-
-
1,1-dimethylethyl[1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[2-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxoethyl]amino]-1,2-dioxoethyl]-butyl]amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[ [1-(cyclopropyl-methyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl]amino]-2,3-dioxopropyl]-amino]carbonyl]-3-azabicyclo[3.1.0]-hexan-3-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[1-(cyclobutylmethyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxomethyl]amino]-2,3-dioxopropylamino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxomethyl]carbamate
-
-
1,2,3,4-tetrahydroacridin-9-amine
-
inhibitor binding to Zn2+-free enzyme, dissociation constant 0.0017 mM, EC50 value 0.060 mM
1,3,4-tri-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
1,3,6-tri-O-galloyl-beta-D-glucose
-
from Terminalia chebula
1-(2-(6-Benzyl-3-(3-(tert-butyl)ureido)-2-oxopyrazin-1(2H)-yl)acetamido)-3-hydroxy-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
-
1-(2-(6-benzyl-3-(3-(tert-butyl)ureido)-5-chloro-2-oxopyrazin-1(2H)-yl)acetamido)-3-(benzyloxy)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
-
1-(4-aminophenyl)-2-phenylethane-1,2-dione
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
-
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-2-vinyl-cyclopropanecarboxylic acid
IC50: 0.0097 mM
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
IC50: 0.33 mM
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-hydroxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 1 mM
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-phenoxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 0.08 mM
1-([4-(3'-Acetylamino-biphenyl-3-yloxy)-1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-4'-hydroxyphenyl-5-phenyl-2(E)-en-1-pentanone
-
56.5% inhibition
-
1-aminocyclopropane-1-carboxylic acid ketoacid
-
electrophilic and acidic compound
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
electrophilic and acidic compound
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
electrophilic and non-acidic compound
1-aminocyclopropanecarboxylic acid
-
non-electrophilic and acidic compound
1-benzofuran-2-carboxylic acid
-
1-benzothiophene-2-carboxylic acid
-
1-methyl-1H-indole-2-carboxylic acid
-
1-O-(3-O-galloylgalloyl)-2,3,4-tri-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-phenyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-phenyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-thiophen-3-yl-pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3'-nitro-biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-morpholin-4-yl-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.032 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.04 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-chloro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-fluoro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-iodo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.01 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(5-chloro-quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(6-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.016 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-chloro-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.002 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.009 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-1-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.008 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.004 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2,2-diethyl-cyclopropanecarboxylic acid
IC50: 0.31 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-ethyl-cyclopropanecarboxylic acid
IC50: 0.0048 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
IC50: 0.00063 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
IC50: 0.014 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.19 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.17 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.005 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.25 mM
12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)-methyl)aminooxalyl)butyl)amide
-
50% inhibition at 130 nM
12-tert-butyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
50% inhibition at 700 nM
12-tert-butyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)-aminooxalyl)butyl)amide
-
50% inhibition at 200 nM
1H-indole-2-carboxylic acid
-
2'-[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-5-(1-carboxy-cyclopropylcarbamoyl)-pyrrolidin-3-yloxy]-biphenyl-4-carboxylic acid
-
IC50: above 0.2 mM
2,2,2-trifluoro-1,1-dimethylethyl[2-[(1S,5R)-2(S)-[[[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]amino]-carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]carbamate
-
-
2,2-Dihydroxy-indan-1,3-dione
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-(pyrimidin-5-yl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-fluoro-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((2-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((3-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)-4-vinylbenzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-Nmethyl-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-Ntosylbenzamide
-
-
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoic acid
-
-
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: above 0.1 mM
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.054 mM
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
-
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
lead compound
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-[(naphthalen-1-yl)methyl]-2-oxopyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
-
2-(2-[6-benzyl-3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
-
2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)-N-(4-(2-oxo-2-(4-(trifluoromethyl)phenylsulfonamido)ethyl)phenyl)acetamide
-
-
2-(3-chlorobenzoyl)benzoic acid
-
2-(4-Butyl-phenyl)-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.0017 mM
2-(4-carboxybenzoyl)benzoic acid
-
2-(4-chlorobenzoyl)-6-(methoxycarbonyl)benzoic acid
-
2-(4-chlorobenzoyl)-6-[(dimethylamino)carbonyl]benzoic acid
-
2-(4-chlorobenzoyl)benzoic acid
-
2-(4-chlorobenzyl)benzoic acid
-
2-(4-chlorophenoxy)benzoic acid
-
2-(4-fluorobenzoyl)benzoic acid
-
2-(4-fluorophenoxy)benzoic acid
-
2-(4-hydroxybenzoyl)-4-methylbenzoic acid
-
2-(4-hydroxybenzoyl)benzoic acid
-
2-(4-hydroxybenzyl)benzoic acid
-
2-(4-methoxybenzoyl)benzoic acid
-
2-(4-methylbenzoyl)benzoic acid
-
2-(4-[3-[1-Carboxy-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid
competitive
2-(4-[3-[1-tert-Butoxycarbonyl-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid tert-butyl ester
competitive
2-(6-benzyl-3-(3-(tert-butyl)ureido)-5-chloro-2-oxopyrazin-1(2H)-yl)acetate
-
-
2-(carboxymethyl)-6-(4-chlorobenzoyl)benzoic acid
-
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-pentanoic acid
IC50: 0.53 MM
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbony]}-amino)-3-mercapto-propionic acid
IC50: 0.14 mM
2-chloro-6-(4-chloro-benzoyl)-benzoic acid
-
2-Hydroxy-2-(1-nitro-ethyl)-indan-1,3-dione
-
-
2-Hydroxy-2-(2-nitro-cyclopentyl)-indan-1,3-dione
-
-
2-Methyl-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.0036 mM
2-O-(4-O-galloylgalloyl)-1,3,4-tri-O-galloyl-beta-D-glucose
-
from Rhodiola kirilowii
2-Phenyl-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.012 mM
2-Phenylsulfanyl-2-p-tolyl-indan-1,3-dione
-
IC50: 0.0031 mM
2-[1-[1-(1-Carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
-
IC50: 0.015 mM, wild-type enzyme, IC50: 0.017 mM, mutant enzyme K136R, IC50: 0.027 mM, mutant enzyme K136M, IC50: 0.05 mM, mutant enzyme K136S, IC50: above 0.3 mM, mutant enzyme R109Q
2-[1-[2-Carboxy-1-(1-ethylcarbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
-
IC50: 0.032 mM
2-[4-(3-carboxypropyl)benzoyl]benzoic acid
-
2-[4-(trifluoromethyl)benzoyl]benzoic acid
-
2-[[(2,3-dimethylphenoxy)acetyl]amino]-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxamide
Hepatitis C virus genotype 4a
an inhibitor identified due to its activity against genotype 4d
3,3'-digalloylprocyanidin B2
-
-
3,3'-digalloylproprodelphinidin B2
-
rhodisin
3,4-dichloroisocoumarin
-
0.03 mM, 50% inhibition
3,6-di-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
3-(2-(3-(3-(tert-b-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-5-(trifluoromethyl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
3-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: 0.0092 mM
3-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.025 mM
3-(4-acetylphenoxy)propanoic acid
-
3-(4-hydroxy-3,5-diiodophenyl)-2-phenylpropanoic acid
-
3-(4-hydroxy-3,5-diiodophenyl)-3-phenylpropanoic acid
-
3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
3-(benzyloxy)-1-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
-
3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)-henicosa-13(21),14,16(20)-triene-18-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
inhibitor adopts a donutlike conformation and has close contact to A156 methyl group of enzyme
3-[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]propanoic acid
-
-
3-[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]propanoic acid
-
-
3-[2-(2-Benzyloxycarbonylamino-3-methyl-pentanoylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(2-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-carboxy-butyrylamino)-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(3-tert-butyl-ureido)-2-indan-2-yl-acetyl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
3-[2-(3-tert-butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
3-[2-[2-(2-Acetylamino-3,3-diphenyl-propionylamino)-4-tert-butoxycarbonyl-butyrylamino]-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3beta-O-acetyl-olean-12-en
-
29.0% inhibition
4-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
0.45 mM, 50% inhibition
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
highly specific
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
reversible competitive inhibitor, highly specific
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid
-
IC50: 0.0007 mM
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid methyl ester
-
IC50: 0.0032 mM
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: 0.002 mM
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.017 mM
4-(4-hydroxy-3,5-diiodophenyl)butanoic acid
-
4-(amidinophenyl)-methanesulfonyl fluoride
-
1.89 mM, 50% inhibition
4-(trifluoroacetyl)benzoic acid
-
4-Benzyloxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.04 mM
4-bromo-2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
-
4-chloro-1H-indole-2-carboxylic acid
-
4-hydroxy-2-(4-hydroxybenzoyl)benzoic acid
-
4-hydroxy-3,5-diiodobenzoic acid
-
4-Isobutoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.019 mM
4-methoxy-2-(4-methoxybenzoyl)benzoic acid
-
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
IC50: 0.0065 mM
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
-
4-tert-Butoxycarbonylamino-4-[1-(1-carboxy-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: above 0.2 mM
4-tert-Butoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.027 mM
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
4-[1-(1-Benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-4-tert-butoxycarbonylamino-butyric acid
-
IC50: above 0.2 mM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl)-butyric acid
-
IC50: 2 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[1-(1-benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-2-cyclohexyl-ethylcarbamoyl]-butyric acid
-
IC50: 250 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-ethylcarbamoyl]-butyric acid
-
IC50: 7 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(2-cyclohexyl-ethylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1540 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(indan-2-ylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1700 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(2-phenyl-cyclopropylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1500 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(3-phenyl-propylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 210 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(methyl-phenethyl-carbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 0.07 mM
4MeBu-P-norvaline-(CO)-GMSYS-NH2
-
CVS4440
5-bromo-1H-indole-2-carboxylic acid
-
5-bromo-2-(4-hydroxybenzoyl)benzoic acid
-
5-chloro-1-benzofuran-2-carboxylic acid
-
5-chloro-1H-indole-2-carboxylic acid
-
5-cyclohexyl-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo(15.3.1.17,10)-docosa-1(21),17,19-triene-8-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
-
5-fluoro-1H-indole-2-carboxylic acid
-
5-methoxy-1-benzothiophene-2-carboxylic acid
-
5-methoxy-1H-indole-2-carboxylic acid
-
5-methyl-1H-indole-2-carboxylic acid
-
6,6-dichloro-3-[2-cyclohexyl-2-(3-cyclohexyl-ureido)-acetyl]-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
6-(2-ethoxyphenyl)-3-(2-methylfuran-3-yl)[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole
Hepatitis C virus genotype 4a
an inhibitor identified due to its activity against genotype 4d
6-chloro-1H-indole-2-carboxylic acid
-
7-bromo-1H-indole-2-carboxylic acid
-
7-chloro-1H-indole-2-carboxylic acid
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
-
Ac-DDIVPC-OH
-
0.04 mM, 50% inhibition
Ac-DVIVPC-OH
-
0.0075 mM, 50% inhibition
Ac-FASGKR-arginylaldehyde
-
competitive, 50% inhibition at about 0.001 mM
acetyl-3,3-diphenylalanine-beta-cyclohexylalanine-Cys-OH
-
0.3 mM, 50% inhibition
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-D-(gamma-carboxyglutamic acid)-Leu-Ile-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-D-Glu-Leu-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
-
IC50: 0.0006 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Asp-Glu-(3,3-diphenylalanine)-Glu-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
-
IC50: 0.0034 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-Glu-3,3-diphenylalanine-Glu-beta-cyclohexylalanine-Cys-OH
-
0.00005 mM, 50% inhibition
acetyl-Asp-Glu-3,3-diphenylalanine-Ile-beta-cyclohexylalanine-OH
-
0.046 mM, 50% inhibition
acetyl-Asp-Glu-Leu-Glu-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
0.0026 mM, 50% inhibition
acetyl-Asp-Glu-Leu-Ile-beta-cyclohexylalanine-Cys-OH
-
0.00006 mM, 50% inhibition
acetyl-Asp-Glu-Met-Glu-beta-cyclohexylalanine-Cys-OH
-
0.00035 mM, 50% inhibition
acetyl-Asp-Glu-Met-Glu-Glu-Cys
-
-
acetyl-Asp-Glu-Met-Glu-Glu-Cys-OH
-
0.001 mM, 50% inhibition
acetyl-Asp-Glu-Val-Val-Pro-boroAlg-OH
-
the inhibitor binds in an antiparrallel manner to beta-strand E2 and interacts with the unprimed sites of the substrate binding pocket. In the NS3/NS4 inhibitor complex, the inhibitor behaves like a reaction intermediate analog. In the absence of the cofactor, inhibitor binding is an order of magnitude weaker
acetyl-EEVVP-norvaline-(CO)-GMSYS-NH2
-
CVS4437
acetyl-EEVVP-norvaline-(CO)-phenethylamide
-
CVS4442
acetyl-Glu-3,3-diphenylalanine-Glu-beta-cyclohexyalanine-Cys-OH
-
0.0014 mM, 50% inhibition
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
-
IC50: 0.0019 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(Me)Ala-Nle-Ser-Tyr-NH2
-
IC50: 0.0035 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-Asp-Val-Val-Leu-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
-
IC50: 0.001 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-beta-cyclohexylalanine-Cys-OH
-
0.46 mM, 50% inhibition
acetyl-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
5 mM, 50% inhibition
acetyl-P-norvaline-(CO)-GMSYS-NH2
-
CVS4441
acetyl-VVP-norvaline-(CO)-G-NH2
-
SCH212986
acetyl-VVP-norvaline-(CO)-S(Bzl)-NH2
-
SCH215426
antibody Fv fragment
-
specific for the HCV NS3 protease domain, IC50: 71.3 nM
-
Asp-Glu-Leu-Ile-L-cyclohexylalanine-aminobutyryl-(Me)Ala-Ser-His-Leu
-
IC50: 5 mM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
IC50: 15 nM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-L-cyclohexylalanine-Asp-Leu
-
IC50 below 0.2 nM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-Nle-Ser-Leu
-
IC50: 10 nM
benzyl 1-([[(2S)-1-[(1R,5S)-2-[(4-amino-1-cyclopropyl-3,4-dioxobutan-2-yl)carbamoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hex-3-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]amino)cyclohexanecarboxylate
-
-
benzyl((S)-1-cyclohexyl-2-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-2-oxoethyl)carbamate
Hepatitis C virus genotype 1b
-
benzyloxycarbonyl-L-Ile-L-Leu-L-(difluoro)aminobutyric acid
-
-
bis(4-aminophenyl)methanone
-
Bz-D-Nle-Lys-Arg-Arg-H
-
-
Bz-N-Me-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-D-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Arg-(p-Cl)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-CN)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-guanidinyl)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-Ph)-Phe-H
-
-
Bz-Nle-Lys-Arg-D-Arg-H
-
-
Bz-Nle-Lys-D-Arg-Arg-H
-
-
Bz-Nle-Lys-Lys(Z)-Arg-H
-
-
Bz-Nle-Lys-Lys-Arg-B(OH)2
-
-
Bz-Nle-Lys-N-Me-Arg-Arg-H
-
-
Bz-Nle-N-Me-Lys-Arg-Arg-H
-
-
chymostatin
-
0.71 mM, 50% inhibition
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
high potency, lacks the P4 substituent
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0. 04,6]octadec-7-ene-4-carbonyl]-amide
-
-
cyclopropyl(4-methoxyphenyl)methanone
-
daphneolon
-
63.6% inhibition
-
daphneticin
-
69.9% inhibition
-
daphnetin
-
79.5% inhibition
daphnoretin
-
36.5% inhibition
DDIVPC-OH
-
0.071 mM, 50% inhibition
EGTA
-
1.6 mM, 50% inhibition
fluorescein-L-Asp-D-Glu-L-Leu-L-Ile-L-beta-cyclohexylalanine-L-Cys-L-Pro-L-beta-cyclohexylalanine-L-Asp-L-Leu-NH2
-
i.e. PepInh-1, noncleavable decapeptidyl inhibitor
glecaprevir
Hepatitis C virus genotype 1b
-
GS-9132
-
an acylthiourea with in vitro activity against Hepatitis C virus genotype 1, inhibits the formation of a functional replication complex. Reversible nephrotoxicity in clinical trials
hydrangetin
-
72.5% inhibition
iodoacetamide
-
0.26 mM, 50% inhibition
ITMN-C
-
active site inhibitor of the NS3-4A protease
-
L-aminobutyric acid carboxylic acid
-
non-electrophilic and acidic compound
L-aminobutyric acid pentafluoroethyl ketone
-
electrophilic and non-acidic compound
L-norvaline carboxylic acid
-
non-electrophilic and acidic compound
L-norvaline ketotetrazole
-
electrophilic and acidic compound
L-norvaline pentafluoroethyl ketone
-
electrophilic and non-acidic compound
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, 1,1-dimethylethyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, methyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, phenylmethyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]sulfonyl]-, 1,1-dimethylethyl ester
-
-
methyl 2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoate
-
-
methyl [5-(thiophen-2-ylcarbonyl)-1H-benzimidazol-2-yl]carbamate
-
inhibitor binding to Zn2+-free enzyme, dissociation constant 0.0019 mM, EC50 value 0.00003 mM
MK-5172
Hepatitis C virus genotype 1b
-
MK-7009
-
i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,70.06,11]heptacosa-6,8,10-triene-24-carboxamide, potent and selective inhibitor of hepatitis C virus NS3/4A protease
N-((2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
-
N-((3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
-
N-((4-(2-(3-(3-(tert-butyl)ureido)-5-chloro- 6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
-
N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)-2-(naphthalen-2-yloxy)acetamide
Hepatitis C virus genotype 4a
i.e. BE114
N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thien-2-yl)-2-phenoxyacetamide
Hepatitis C virus genotype 4a
i.e. BE113
N-(cyclohexylacetyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000037 mM
N-(cyclohexylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000009 mM
N-(cyclopentylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000005 mM
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-[[7-(acetylamino)-2-phenylquinolin-4-yl]oxy]-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-L-prolinamide
-
50% inhibition at 0.000029 mM
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-4-[(6-methoxyisoquinolin-1-yl)oxy]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000029 mM
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(4-methoxybenzamido)-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-[(naphthalene-2-carbonyl)amino]-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-[2-(2,3-dimethylanilino)benzamido]-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
N-(tert-butoxycarbonyl)-D-valyl-(4S)-N-(1-carboxy-2-ethenylcyclopropyl)-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolinamide
-
50% inhibition of processing of substrate SEAP-1 at 0.00026 mM
N-(tert-butylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
inhibitor derived from peptide DDIVPC applying rigidification of the peptide scaffold to the bioactive conformation
N-(tert-butylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000008 mM
N-([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
N-([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-b-phenyl-L-phenylalanyl-L-alpha-glutamyl-N-[1-(carboxycarbonyl)-3,3-difluoropropyl]-3-cyclohexyl-L-alaninamide
-
50% inhibition of processing of substrate SEAP-1 at 0.0067 mM
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-beta-phenyl-L-phenylalanyl-L-alpha-glutamyl-3-cyclohexyl-L-alanine
-
1.17 mM, 50% inhibition
N-acetyl-L-alpha-aspartyl-N-[(1S)-2-[[(1S)-1-([(2S,4R)-2-[[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]carbamoyl]-4-[(2-phenylquinolin-4-yl)oxy]pyrrolidin-1-yl]carbonyl)-2,2-dimethylpropyl]amino]-1-cyclohexyl-2-oxoethyl]-D-alpha-glutamine
-
-
N-acetyl-L-aspartyl-L-glutamyl-L-isoleucyl-L-valyl-(3R)-3-(benzyloxy)-L-prolyl-N-[(1S)-1-phenylethyl]-L-norleucinamide
-
-
N-tosyl-Phe chloromethyl ketone
N-[(1S)-1-cyclohexyl-2-[[(2S)-1-(2-{[1-cyclopropyl-4-(cyclopropylamino)-3,4-dioxobutan-2-yl]carbamoyl]-1',3'-dihydrospiro[cyclobutane-1,2'-inden]-3-yl)-3,3-dimethyl-1-oxobutan-2-yl]amino}-2-oxoethyl]pyrazine-2-carboxamide
-
compound displays an EC50 of 0.8 microM against hepatitis C virus with no toxicity in Huh7 and Vero cells at concentration up to 10 and 100 microM, respectively. Unfortunately, overall cytotoxicity in cell based systems discourages further development
N-[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]-L-norvaline
-
-
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000001 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000013 mM, no inhibition of human leukocyte elastase, cathepsin B
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(6-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000041 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7,8-dimethoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000013 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000002 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(8-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000005 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[[2-(3-methoxyphenyl)quinolin-4-yl]oxy]-L-prolinamide
-
50% inhibition at 0.000010 mM
N-[(2S)-2-amino-2-cyclohexylacetyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000018 mM
N-[(2S)-2-cyclohexylpropanoyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000037 mM
N-[(2S)-2-[(N-acetyl-L-alpha-aspartyl-D-alpha-glutamyl)amino]-2-cyclohexylacetyl]-L-valyl-(4S)-4-(naphthalen-2-ylmethoxy)-D-prolyl-D-norvaline
-
-
N-[(cyclobutyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000024 mM
N-[(cyclohexyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000030 mM
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000014 mM
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
-
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3R)-2-carboxy-3-ethenylcyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
-
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3S)-2-ethenyl-3-phosphonocyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
N-[2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chlorobenzene-1-sulfonyl]-4-(trifluoromethyl)benzamide
-
-
N-{17-[8-chloro-2-(4-isopropylthiazol-2-yl)-7-methoxy-quinolin-4-yloxy]-2,14-dioxo-3,15-diazatricyclo [13.3.0.0]octadec-7-ene-4-carbonyl}-(1-methylcyclo propyl)-(1-methylcyclopropyl)sulfonamide
-
EC50 = 3.76 nM, non-cytotoxic (CC50 above 0.020 nM), and metabolically stable HCV inhibitor. Compound exhibits advantageous drug metabolism and pharmacokinetic properties in rat and dog, with a high liver exposure after oral administration, but limited heart exposure observed in rat
Nalpha-p-tosyl-Lys chloromethyl ketone
narlaprevir
Hepatitis C virus genotype 1b
-
nona-D-Arg-NH2
-
reduces infection in primary neurons
peptidyl-alpha ketoamides
-
-
-
phenylmethanesulfonyl fluoride
-
0.6 mM, 50% inhibition
RNA aptamer G9-I
-
noncompetitive inhibition, Arg161 as well Arg130 of the NS3 protease domain are essential for interaction with the G9-I aptamer
-
SCH6
-
active site inhibitor of the NS3-4A protease
sofosbuvir
-
approved drug for HCV treatment
sovaprevir
Hepatitis C virus genotype 1b
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[(ethylamino)carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[[(cyclopropylmethyl)amino]carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[[[3-(dimethylamino)propyl]methylamino]carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
IC50: 0.00066 mM
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-2-[[[[(1S)-1-(hydroxymethyl)-2-methylpropyl]amino]carbonyl]amino]-3-methyl-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[(2-propenylamino)carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[(propylamino)carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[[(2,2,2-trifluoroethyl)amino]carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-2-[[[(1-methylethyl)amino]carbonyl]amino]-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-2-[[[[(1S)-2-methyl-1-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]propyl]amino]carbonyl]amino]-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4',4'''-[sulfonylbis[imino[(2S)-2-(1-methylethyl)-1-oxo-2,1-ethanediyl]]]bis[1'-(cyclopropylcarbonyl)hexahydro]-, (3'aR,3'''aR,6'aS,6'''aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-amino-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, monohydrochloride, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[(aminocarbonyl)amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclohexylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclopentylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclopropylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
tert-butyl (1-cyclohexyl-2-[(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl)carbamate
-
-
tert-butyl (1-[[(3R)-3-([1-(2-cyclobutylethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
non-preferred name
tert-butyl (1-[[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
non-preferred name
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
tert-butyl (2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoate
-
-
tert-butyl [(2R,6S,12Z,14aR,16aS)-14a-[(cyclopropylsulfonyl)carbamoyl]-2-[(6-methoxyisoquinolin-1-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,11,13a,14,14a,15,16,16a-tetradecahydro-5H-cyclopropa[e]pyrrolo[2,1-i][1,7,10]oxadiazacyclopentadecin-6-yl]carbamate
-
-
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]-4-methylpentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
non-preferred name
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
-
tert-butyl [1-cyclohexyl-2-[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl]carbamate
-
-
tert-butyl [2-[(3R)-3-([1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxo-3-phenylpropan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxo-3-phenylpropan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-1-cyclohexyl-2-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-2-oxoethyl)-carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-3,3-dimethyl-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxobutan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyl((S)-3-(1H-indol-3-yl)-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamate
Hepatitis C virus genotype 1b
-
tert-butyloxacrybonyl-L-Glu-L-Leu-L-(difluoro)aminobutyric acid
-
-
TMC 435350
-
rapidly reversible inhibitor
TMC435
-
small-molecule reversible noncovalent inhibitor of the NS3/4A serine protease
trans-1,2-cyclohexanediamine-N,N,N',N'-tetraacetic acid
-
0.007 mM, 50% inhibition
[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]acetic acid
-
-
[(2R,6R,12Z,13aS,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl]phosphonic acid
-
-
[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]acetic acid
-
-
[(Z)-(1R,4R,6S,15R,17R)-4-cyclopropanesulfonylaminocarbonyl-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-en-13-yl]-carbamic acid tert-butyl ester
-
-
[1-(6-Ethyl-4-methanesulfonyl-5-oxo-hexahydro-pyrrolo[3,2-b]pyrrole-1-carbonyl)-2-methyl-propyl]-carbamic acid tert-butyl ester
-
IC50: 0.0005 mM
[1-[1-(2-Mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-2-methyl-propyl]-carbamic acid benzyl ester
-
IC50: 0.4 mM
[1-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-3-carbonyl]-2,2-dimethyl-propyl]-carbamic acid tert-butyl ester
-
is the most promising of all the inhibitors. With tert-leucine as P3 residue, extremely potent with single digit nanomolar potency in enzymatic assay. Excellent selectivity against elastase. Bioavailability above 10% in rat, monkey, and dog
[2-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hex-3-yl]-1-indan-2-yl-2-oxo-ethyl]-carbamic acid tert-butyl ester
-
-
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
50% inhibition at 0.0000004 mM, NMR and molecular dynamics analysis
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
-
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000077 mM, NMR and molecular dynamics analysis
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000011 mM, NMR and molecular dynamics analysis
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000027 mM, NMR and molecular dynamics analysis
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
1,10-phenanthroline
inhibits NS2/3 auto-cleavage and NS3 protease activity
1,10-phenanthroline
-
0.26 mM, 50% inhibition
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.0008 mM
Aprotinin
-
-
asunaprevir
-
-
asunaprevir
hepatitis C virus genotype 1a
-
-
asunaprevir
hepatitis C virus genotype 1a
-
asunaprevir
Hepatitis C virus genotype 1b
-
asunaprevir
Hepatitis C virus genotype 1b
-
asunaprevir
Hepatitis C virus genotype 2a
-
asunaprevir
Hepatitis C virus genotype 4a
-
asunaprevir
Hepatitis C virus genotype 5a
-
BILN 2061
significantly less active on genotype 2 and 3 enzyme
BILN 2061
-
potent inhibitor
BILN-2061
-
used in clinical trials. Potently inhibits Hepatitis C virus replication in human hepatoma cells, but causes cardiac toxicity in experimental animals
BILN-2061
-
about 90% inhibition at 40 nM
BILN-2061
-
rapidly reversible NS3 inhibitor
BILN-2061
Hepatitis C virus genotype 2a
a NS3 serine protease inhibitor
BILN2061
-
NS3 protease inhibitor, fully restores MAVS/IPS-1-dependent IFN-alpha promoter activity in Hepatitis C virus-infected cells
BMS-605339
hepatitis C virus genotype 1a
-
BMS-605339
Hepatitis C virus genotype 1b
-
boceprevir
-
-
boceprevir
-
SCH 503034, slowly reversible covalent inhibitor
boceprevir
hepatitis C virus genotype 1a
-
-
boceprevir
Hepatitis C virus genotype 1b
-
boceprevir
Hepatitis C virus genotype 2a
-
boceprevir
Hepatitis C virus genotype 4a
-
boceprevir
Hepatitis C virus genotype 5a
-
Bz-Ala-Lys-Arg-Arg-H
-
-
Bz-Nle-Ala-Arg-Arg-H
-
-
Bz-Nle-Lys-Ala-Arg-H
-
-
Bz-Nle-Lys-Arg-Ala-H
-
-
Bz-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Arg-Lys-H
-
-
Bz-Nle-Lys-Arg-Phe-H
-
-
Bz-Nle-Lys-Lys-Arg-H
-
-
Bz-Nle-Lys-Phe-Arg-H
-
-
Bz-Nle-Phe-Arg-Arg-H
-
-
Bz-Phe-Lys-Arg-Arg-H
-
-
danoprevir
-
-
danoprevir
-
approved drug for HCV treatment
danoprevir
Hepatitis C virus genotype 1b
-
deldeprevir
hepatitis C virus genotype 1a
-
-
deldeprevir
Hepatitis C virus genotype 2a
-
deldeprevir
Hepatitis C virus genotype 4a
-
deldeprevir
Hepatitis C virus genotype 5a
-
EDTA
inhibits NS2/3 auto-cleavage and NS3 protease activity
EDTA
-
0.007 mM, 50% inhibition
faldaprevir
-
-
faldaprevir
hepatitis C virus genotype 1a
-
-
faldaprevir
Hepatitis C virus genotype 1b
-
faldaprevir
Hepatitis C virus genotype 2a
-
faldaprevir
Hepatitis C virus genotype 4a
-
faldaprevir
Hepatitis C virus genotype 5a
-
grazoprevir
-
-
grazoprevir
hepatitis C virus genotype 1a
-
-
grazoprevir
Hepatitis C virus genotype 1b
-
grazoprevir
Hepatitis C virus genotype 2a
-
grazoprevir
Hepatitis C virus genotype 4a
-
grazoprevir
Hepatitis C virus genotype 5a
-
ITMN-191
-
high in vitro potency and specificity
ITMN-191
-
rapidly reversible inhibitor
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-4-[(6-methoxyisoquinolin-1-yl)oxy]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R)-2-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-4-[(6-methoxyisoquinolin-1-yl)oxy]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
Hepatitis C virus genotype 1b
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
hepatitis C virus genotype 1a
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
Hepatitis C virus genotype 1b
-
N-tosyl-Phe chloromethyl ketone
-
-
N-tosyl-Phe chloromethyl ketone
-
0.03 mM, 50% inhibition
N-tosyl-Phe chloromethyl ketone
-
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
-
HCV replication in a cellular assay (subgenomic 1b replicon) is inhibited with a half-maximal effective concentration (EC50) of 8 nM. The compound is synergistic with alpha interferon and an NS5B inhibitor in the replicon model and additive with ribavirin. In rats, the compound is extensively distributed to the liver and intestinal tract, and the absolute bioavailability is 44% after a single oral administration. Compound concentrations detected in both plasma and liver at 8 h postdosing are above the EC99 value measured in the replicon
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
hepatitis C virus genotype 1a
-
HCV replication in a cellular assay (subgenomic 1b replicon) is inhibited with a half-maximal effective concentration (EC50) of 8 nM. The compound is synergistic with alpha interferon and an NS5B inhibitor in the replicon model and additive with ribavirin. In rats, the compound is extensively distributed to the liver and intestinal tract, and the absolute bioavailability is 44% after a single oral administration. Compound concentrations detected in both plasma and liver at 8 h postdosing are above the EC99 value measured in the replicon
Nalpha-p-tosyl-Lys chloromethyl ketone
-
-
Nalpha-p-tosyl-Lys chloromethyl ketone
-
0.15 mM, 50% inhibition
Nalpha-p-tosyl-Lys chloromethyl ketone
-
-
paritaprevir
-
approved drug for HCV treatment
paritaprevir
hepatitis C virus genotype 1a
-
-
paritaprevir
Hepatitis C virus genotype 1b
-
paritaprevir
Hepatitis C virus genotype 2a
-
paritaprevir
Hepatitis C virus genotype 4a
-
paritaprevir
Hepatitis C virus genotype 5a
-
SCH-503034
-
used in clinical trials. Orally bioavailable, covalent, reversible alpha-keto amide inhibitor. Displays potent and time-dependent inhibition of the NS3-4A protease. Inhibitor dissociation constant in the low nanomolar range. Ability to effectively inhibit Hepatitis C virus RNA synthesis in the human hepatoma cells harboring the hepatitis C virus replicon
simeprevir
-
approved drug for HCV treatment
simeprevir
hepatitis C virus genotype 1a
-
-
simeprevir
Hepatitis C virus genotype 1b
-
simeprevir
Hepatitis C virus genotype 2a
-
simeprevir
Hepatitis C virus genotype 4a
-
simeprevir
Hepatitis C virus genotype 5a
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
-
telaprevir
-
-
telaprevir
-
VX-950, slowly reversible covalent inhibitor
telaprevir
hepatitis C virus genotype 1a
-
-
telaprevir
Hepatitis C virus genotype 1b
-
telaprevir
Hepatitis C virus genotype 2a
-
telaprevir
Hepatitis C virus genotype 4a
-
telaprevir
Hepatitis C virus genotype 5a
-
vaniprevir
-
MK-7009, i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
vaniprevir
hepatitis C virus genotype 1a
-
-
vaniprevir
Hepatitis C virus genotype 1b
-
vaniprevir
Hepatitis C virus genotype 2a
-
vaniprevir
Hepatitis C virus genotype 4a
-
vaniprevir
Hepatitis C virus genotype 5a
-
vedroprevir
-
-
vedroprevir
Hepatitis C virus genotype 1b
-
VX-950
equally active on enzyme from all three genotypes
VX-950
-
used in clinical trials. Orally biovailable tetrapeptide alpha-ketoamide, binds slowly and reversibly to the protease, with an affinity for the genotype 1 Hepatitis C virus NS4-4A protease in the low nanomolar range and a half life of nearly an hour. Moderately potent inhibitor of Hepatitis C virus replication. Achieves a more than a 10000fold suppression of hepatitis C virus RNA in replicon cells treated for 14 days in the presence of relatively low concentrations of the compound
additional information
-
alpha-ketoacids incorporating difluoroaminobutyric acid in the p1 position are potent slow binding inhibitors
-
additional information
-
many NS3 protease inhibitors have taken advantage of an unusual product inhibition by N-terminal products of cleavage at the polyprotein processing sites
-
additional information
-
solid-phase synthesis of peptidomimetic inhibitors
-
additional information
-
the effect of prime-site occupancy on the enzyme structure
-
additional information
-
inhibitors with electrophilic C-terminal residues are generally non-selective while compounds with non-electrophilic C-terminal residues are more selective. Compounds with P1 aminobutyric acid residues are non-selective, while 1-aminocyclopropanecarboxylic acid and norvaline-based inhibitors are generally selective. Most potent and selective inhibitors contain a non-electrophilic phenyl acyl sulfonamide C-terminal residue
-
additional information
-
human leukocyte antigen A2restricted epitope in which substitutions at 5 of 9 residues destroy the protease
-
additional information
EGTA and zinc metalloprotease inhibitors bestatin, phosphoramidon and thiorphan have no effect on NS2/3 auto-cleavage and NS3 protease activity. No inhibitory effect of the NS4A peptide on NS2/3 auto-cleavage, additionally the NS4A peptide does not significantly affect the sensitivity of NS2/3 autocleavage to zinc chelation, but has a marked effect on NS3 protease activity, rendering this activity approximately 3fold more resistant to zinc chelation
-
additional information
-
methylated 3,3'-digalloylproprodelphinidin B2, hexanoylated (-)-epigallocatechin-3-O-gallate, (-)-epigallocatechin, (-)-epicatechin, gallic acid, luetolin, tyrosol and salidroside show no activity up to 100 micromol
-
additional information
-
two galloyl residues at 3 and 4 positions of the glucopyranose ring of the plant inhibitors interact with SER139, GLY137, ALA157, and ASP81 by hydrogen bond interaction and with ALA156 and HIE57 by hydrophobic interaction and are essential for the activities of the inhibitors
-
additional information
-
compounds with urea cappings are more potent and selective than their carbamate counterparts
-
additional information
-
protease is susceptible to feedback inhibition by the N-terminal products released from the polyprotein substrate after enzymatic cleavage
-
additional information
-
14-membered ring system is the most potent.The corresponding 13-, 15-, and 16-membered macrocyclic rings deliver less potent inhibitors. Corresponding P1 acylsulfonamides have superior potencies over the corresponding P1 carboxylic acids. Highly potent protease inhibitors lack the P4 substituent
-
additional information
-
macrocyclic peptidic inhibitors, are less susceptible to hydrolytic degradation by proteases, have markedly improved oral absorption, and pharmacokinetic properties compared to corresponding acyclic analogs
-
additional information
-
electrophilic compounds with a pentafluoroethyl ketone group show stronger inhibition at pH 8 than pH 6, the difference is only significant at high ionic strength. Electrophilic compounds with an acidic C-terminal group or a cyclic P1 residue show a lower inhibitory effect at pH 8 than at pH 6, inconsistent with a mechanism-based inhibition. All electrophilic compounds have a strong inhibition at pH 6, when mechanism-based inhibition is unlikely
-
additional information
-
decrease in the efficiency of expression of NS3/4A protease, as the concentration of Hepatitis C virus-infected cells increases
-
additional information
-
not inhibited by BMS-858
-
additional information
-
in the absence of Zn+2, the NS3 protease adopts a partially-folded inactive conformation. Identification of ligands binding to the Zn+2-free NS3 protease, that trap the inactive protein, and block the viral life cycle. Ligands show a new inhibition mechanism simultaneously blocking substrate and cofactor interactions in a non-competitive fashion, appropriate for combination therapy, low impact of known resistance-associated mutations and inhibition of NS4A binding, thus blocking its several effects on NS3 protease
-
additional information
-
discovery and synthesis of pyrazinone-based compounds that potently inhibit the drug-resistant enzyme variant R155K of the hepatitis C virus NS3 protease, molecular docking and modeling, overview. The compounds, that are very different to the approved drugs and clinical candidates, have potential in the development of inhibitors less sensitive to drug resistance
-
additional information
-
screening for NS3/4A protease inhibitors with pan-genotypic antiviral activity, improved coverage of resistance associated substitutions, and a decreased risk of hepatotoxicity. The natural peptide substrates of the HCV NS3/4A protease contain a cysteine or threonine at P1, highlighting the small nature of the S1 pocket. While replacing the P1 vinyl with an ethyl on the 3-methyl pyrrolidine series improveds the predicted clearance, the larger ethyl group results in an approximate 5fold loss in both biochemical and cellular GT3 potency. Significantly improved metabolic stability can be realized by adding a fluoro or difluoro to the P1 ethyl group, but at the expense of further compromised GT3 potency. The P1 difluoromethyl substituent appears to be a viable replacement for the reactive vinyl group wherein GT3 potency is maintained and metabolic stability is improved with compound. Compound synthesis and evaluation, detailed overview
-
additional information
-
the ethyl acetate extraction of Daphne papyracea exhibits an inhibitory effect towards the HCV NS3/4A protease. Eight compounds are identified from the extract. Molecular docking study of the identified inhibitory compounds against HCV NS3/4A protease using boceprevir as a positive control, docking scores, overview
-
additional information
-
no inhibition by bestatin, EDTA, Mn2+, Mg2+, Ca2+, K+
-
additional information
hepatitis C virus genotype 1a
-
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
additional information
hepatitis C virus genotype 1a
design and synthesis of a series of potent NS3 protease inhibitors for the treatment of hepatitis C virus, structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides, overview
-
additional information
Hepatitis C virus genotype 1b
design and synthesis of a series of novel compounds by incorporating different amino acid residues in P1/P1' and P3/P3' position to develop antiviral agents. All designed compounds show moderate anti-HCV NS3 protease activity, detailed structure-activity relationship (SAR) analysis, overview
-
additional information
Hepatitis C virus genotype 1b
design and synthesis of a series of potent NS3 protease inhibitors for the treatment of hepatitis C virus, structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides, overview
-
additional information
Hepatitis C virus genotype 1b
structural analysis, differences in how inhibitors fit within the substrate envelope and interact with the binding site trend with differential drug resistance patterns, hydrogen bond interactions between ligands and side chain atoms in the HCV NS3/4A protease active site, and differential van der Waals interactions on the binding surface of HCV NS3/4A protease, detailed overview. There are many basic residues in the S6 pocket, such as R119, R123, R161, and K165, which make conserved interactions with the conserved acidic D or E residue at the P6 position of the substrate. A drug design strategies focusing on inhibitors with a P1-P3 macrocycle and flexible quinoxiline-related P2 moieties may be an optimal strategy, given high potency can be achieved without compromising the resistance profile. Another drug design strategy is extending inhibitors in the P1' and P4-P6 regions to make increased contacts with conserved residues in the S1' and S4-S6 pockets to increase inhibitor potency while decreasing susceptibility to drug resistance mutations. Q80K is a polymorphism that impacts the activity of most protease inhibitors. Boceprevir, telaprevir, simeprevir, danoprevir, asunaprevir, and faldaprevir are susceptible to mutations at Q80. Drug resistance mutations at residues R155, A156, and D168, are located close to the catalytic triad, impact the most inhibitors. Boceprevir and telaprevir are the oldest inhibitors and are susceptible to drug resistance, with main drug resistance mutations at residues V36, T54, R155, and A156
-
additional information
Hepatitis C virus genotype 2a
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
additional information
Hepatitis C virus genotype 4a
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
additional information
Hepatitis C virus genotype 4a
N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-phenoxyacetamide and N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-(naphthalen-2-yloxy)acetamide are not inhibitory. The inhibitory efficacy of four computer-designed and chemically-synthesized small-molecule compounds is evaluated against in vitro-expressed NS3/4A protease from HCV genotype 4a, the most prevalent genotype in Egypt, using a fluorescence-based enzymatic assay, overview. Molecular modeling. No inhibition by N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-phenoxyacetamide (BE115) and N-(3-cyano-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)-2-(naphthalen-2-yloxy)acetamide (BR116)
-
additional information
Hepatitis C virus genotype 5a
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
additional information
-
susceptibility/efficiency and resistance, respectively, of virus genotypes and variants with respect to antiviral agents, EC50 values, detailed overview
-
additional information
-
the P1 and P2 positions are most important for inhibitor binding, whilst the P3 and P4 positions have much less effect
-
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0.00000009
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000122
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000009
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000001
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0012
(10R,13R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10-cyclohexyl-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00039
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-oxo-2,7-dioxa-8-thia-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide 8,8-dioxide
-
-
0.00032
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00031
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00017
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00016
(11R,14R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-2-oxa-10,13-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-14-carboxamide
-
-
0.0011
(11S,14S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-1,10,13,17-tetraazabicyclo[14.2.1]nonadeca-16(19),17-diene-14-carboxamide
-
-
0.0000049
(1aR,5S,10R,22aR)-5-tert-butyl-9-cyclopropyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000165
(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000012
(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-9-propyl-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.0000001
(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000067
(1aR,5S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000063
(1aR,5S,10R,22aR)-9-(butan-2-yl)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000087
(1aR,5S,10S,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-14-methoxy-3,6-dioxo-9-phenoxy-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000053
(1aR,5S,8S,9S,10R,19E,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,21,22,22a-dodecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.0000017
(1aR,5S,8S,9S,10R,21aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-14-methoxy-3,6-dioxo-1a,3,4,5,6,9,10,17b,18,18a,19,20,21,21a-tetradecahydro-1H,8H-7,10-methanodicyclopropa[13,14:18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000043
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(difluoromethyl)cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000053
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethylcyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000563
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000838
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-1-[(cyclopropanesulfonyl)carbamoyl]-2-methylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000063
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000013
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2R)-2-(difluoromethyl)-1-[(1-methylcyclopropane-1-sulfonyl)carbamoyl]cyclopropyl]-9-ethyl-18-fluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.00000092
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(2,2-difluoroethyl)cyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.0000013
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-(2-fluoroethyl)cyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000094
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl]-18,18-difluoro-14-methoxy-9-methyl-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.000000081
(1aR,5S,8S,9S,10R,22aR)-5-tert-butyl-N-[(1R,2S)-1-[(cyclopropanesulfonyl)carbamoyl]-2-ethenylcyclopropyl]-9-ethyl-18,18-difluoro-14-methoxy-3,6-dioxo-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide
-
pH and temperature not specified in the publication
0.0000001
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000002
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000016
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000006
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000003
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000002
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
-
Ki below 0.00000002 mM, in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000045
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000003
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000009
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000018
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000008
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.000016
(1R,2S)-1-[([(1R,2R,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopentyl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0000013
(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0000011
(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000023
(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000108
(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0027
(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-cyclopentylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.0069
(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-tert-butylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.000016
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyldimethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethylpropylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.000022
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.01
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-methyl-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.005
(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl](methyl)carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000024
(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000004
(1R,5S)-3-(N-[[(1S)-1-cyclohexyl-2-cyclopropyl-2-oxoethyl]carbamoyl]-3-methyl-L-valyl)-N-[1-(cyclopropylamino)-1,2-dioxohept-6-yn-3-yl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
0.000007
(1R,5S)-3-[2(S)-[[[[1-[[[cyclobutyl(methyl)amino]sulfonyl]methyl]cyclohexyl]amino] carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000014
(1R,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[N-(tert-butylcarbamoyl)-3-methyl-L-valyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
0.000006
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyll]-butyl]-3-[2(S)-[[[[1-[[(dimethylamino)sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000002
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-2-[[[[1-[1(R)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000004
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-(2-cyclopropyl-1,1-dioxido-5(R)-isothiazolidinyl)cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.0000028
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(2-fluoro-1,1-dimethylethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000006
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(1-methylethyl)amino]-sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000008
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000009
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[ethyl(methyl)amino]sulfonyl]methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000008
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[(4-morpholinylsulfonyl)-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000007
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[[methyl(1-me5thylethyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000011
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-pemtyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000004
(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(2-cyclopropylethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cycloppropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000015
(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(cyclopropylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000014
(1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
-
-
0.00011
(1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide
-
-
0.0001
(1S,5R)-6,6-dichloro-3-[cyclohexyl[[[(1,1-dimethylethyl)amino]carbonyl]amino]acetyl]-N-[1-[1,2-dioxo-2-(2-propenylamino)ethyl]butyl]-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
-
-
0.000006
(1S,5R)-N-((S)-5-cyclopropyl-1-(cyclopropylamino)-1,2-dioxopentan-3-yl)-3-((S)-2-(3-(1-((N-cyclopropyl-N-methylsulfamoyl)methyl)cyclohexyl)ureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
0.00036
(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00023
(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000065
(1S,5R)-N-(1-amino-6,6,6-trifluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.0013
(1S,5R)-N-(1-amino-7,7,7-trifluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00016
(1S,5R)-N-(4-amino-1-((1s,3S)-3-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00021
(1S,5R)-N-(4-amino-1-(1-fluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.163
(1S,5R)-N-(4-amino-1-(1-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00005
(1S,5R)-N-(4-amino-1-(2,2-difluorocyclopropyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000098
(1S,5R)-N-(4-amino-1-(3,3-difluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000014 - 0.000035
(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
0.00012
(1S,5R)-N-(5-amino-1,1,1-trifluoro-4,5-dioxopentan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00001
(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
-
protease continous assay
0.000044
(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
protease continous assay
0.000016
(2-(3-((12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,-13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
protease continous assay
0.000015
(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
-
continous enzyme assay
0.00026
(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
continous enzyme assay
0.0023
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2,10-dioxa-13-azatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00011
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.0003
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[16.2.2.13,7]tricosa-1(20),3(23),4,6,18,21-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.21
(2R)-2-(acetylamino)-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
pH 6.5, 30°C
0.26
(2R)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
pH 6.5, 30°C
0.0000004
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000001 - 0.0000002
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
0.0000003
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000006
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-2-(4-methoxyphenyl)-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000009
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(6-methylpyridin-2-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000028
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-3-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-4-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000062
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(morpholin-4-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-[(2-phenylquinazolin-4-yl)oxy]-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.00000062 - 0.0000016
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine
0.0000064
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-([7-methoxy-2-[2-(methylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000024
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxyquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000047
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[2-(1H-imidazol-1-yl)-7-methoxyquinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000055
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000051
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrrol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000022
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(4-methyl-1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000012
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(5-methyl-1,3,4-oxadiazol-2-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.00042
(2S)-([N-[3-([[(10S,13S)-10-cyclohexyl-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-trien-13-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.000015
(2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00025
(2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00001
(2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00016
(2S)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[17.2.2.13,7]tetracosa-1(21),3(24),4,6,19,22-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.31
(2S)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
pH 6.5, 30°C
0.002
(2S)-2-[([(1R,4R)-2-[[(1R)-1-[[(1R)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]butanoic acid
-
-
0.002
(2S)-2-[[(2-[[(1S)-1-(methoxycarbonyl)-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.00028
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000503
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000523
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000038
(2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoic acid
-
-
0.0000012
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-([7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(3-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxyquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000012
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000008
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-([2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000003
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
pH and temperature not specified in the publication
0.0000002
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
pH and temperature not specified in the publication
0.0000014 - 0.0000028
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
0.0035
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,15-trioxo-1,4,10-triazacyclopentadecane-5-carboxamide
-
-
0.00066
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,16-trioxo-1,4,10-triazacyclohexadecane-5-carboxamide
-
-
0.00051
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,17-trioxo-1,4,10-triazacycloheptadecane-5-carboxamide
-
-
0.00044
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,18-trioxo-1,4,10-triazacyclooctadecane-5-carboxamide
-
-
0.000022 - 0.000055
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
0.000013
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.00001
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000021
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000019
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000006
(3S)-3-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.000021
(3S,18S)-18-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinoline-3-carboxamide
-
-
0.00011
(3S,6S)-6-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-3-carboxamide
-
-
0.00000015
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000083
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00021
(4S,7S,9R)-4-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2,5-dioxo-10,15-dioxa-3,6-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-7-carboxamide
-
-
0.000095
(5R,7S,10S)-10-cyclopentyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000071
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo(prop-2-en-1-ylamino)acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00014
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(1-phenylethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000176
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(pyridin-2-ylmethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00014
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclobutylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000078
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopentylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000085
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-1,6,7,9,10,11,12,14,15,16,17,18-dodecahydro-5H-2,22:5,8-dimethano-4,13,2,8,11-benzodioxatriazacycloicosine-7(3H)-carboxamide
-
-
0.000057
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000066
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[[(1-methylpropyl)amino](oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000242
(5R,7S,10S)-N-[(1S)-1-[(benzylamino)(oxo)acetyl]butyl]-10-tert-butyl-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00009
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-methyl-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.0016
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.0002
(5R,8S,10R)-5-tert-butyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-2,11,15-trioxa-4,7-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.00068
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.2.2]icosa-1(18),16,19-triene-8-carboxamide
-
-
0.00045
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.3.1]icosa-1(20),16,18-triene-8-carboxamide
-
-
0.000007
(5S,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-8-carboxamide
-
-
0.000025
(6R,8S,11R)-11-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.00003
(6R,8S,11S)-11-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-8-carboxamide
-
-
0.00000014
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.000037
(6S,11S,20S)-11-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-20-carboxamide
-
-
0.000044
(6S,8S,9R,10S,13S)-13-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-triene-10-carboxamide
-
-
0.00007
(7R,9S)-12-(2,3-dihydro-1H-inden-1-yl)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000008
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000026
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-15-methyl-11,14-dioxo-2,6-dioxa-10,13,15-triazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-9-carboxamide
-
-
0.000032
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methoxy-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00003
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000012
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-19-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000008
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00001
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
0.000036
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-6-(phenylsulfonyl)-2-oxa-6,10,13-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000006
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00006
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00006
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.000008
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[[4-(dimethylamino)-2,4-dioxo-3-phenylbutyl]amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.000017
(7R,9S,12S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000019
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(1-methylethyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00004
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(2-methylpropyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00031
(7R,9S,12S)-N-(1-[[(2-[[(S)-cyano(phenyl)methyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000015
(7S,12S,21S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-21-carboxamide
-
-
0.0012
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0023
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0017
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0066
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.00056
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-4,4-difluoro-butyric acid
-
-
0.00003
(S)-2-[[(1R,4R)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
0.002
(S)-2-[[(1S,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonylmethyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
0.00013
(Z)-(1R,4R,6S,14R,16R)-12-tert-butoxycarbonylamino-16-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,13-dioxo-3,12-diaza-tricyclo[12.3.0. 04, 6]heptadec-7-ene-4-carboxylic acid
-
-
0.000006
(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.000031
(Z)-(1R,4R,6S,15R,17R)-13-tert-butoxycarbonylamino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.000044
(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.00026
(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo-[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.00012
(Z)-(1R,4R,6S,16R,18R)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
0.00071
(Z)-(1R,4R,6S,16R,18R)-14-tert-butoxycarbonylamino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
0.000015
(Z)-(1R,4R,6S,17R) and (1S,4R,6S,17S)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadeca-7,15-diene-4-carboxylic acid
-
-
0.01
(Z)-(1R,4R,6S,17R,19R)-15-amino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
0.01
(Z)-(1R,4R,6S,17R,19R)-15-tert-butoxycarbonylamino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
0.00011
(Z)-(1R,4R,6S,18R) and (1S,4R,6S,18S)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadeca-7,16-diene-4-carboxylic acid
-
-
0.00009
1,1-dimethylethyl [1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[1,2-dioxo-2-(2-propenylamino) ethyl]butyl]-amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
0.00002
1,1-dimethylethyl [2-[(1S,5R)-2(S)-[[[1-(2-amino-1,2-dioxoethyl)butyl]amino]carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]-carbamate
-
-
0.000015
1,1-dimethylethyl[1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[2-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxoethyl]amino]-1,2-dioxoethyl]-butyl]amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
0.000007
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[ [1-(cyclopropyl-methyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl]amino]-2,3-dioxopropyl]-amino]carbonyl]-3-azabicyclo[3.1.0]-hexan-3-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
0.000009
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[1-(cyclobutylmethyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxomethyl]amino]-2,3-dioxopropylamino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxomethyl]carbamate
-
-
0.26
1,10-phenanthroline
-
-
0.00045
1-(2-(6-Benzyl-3-(3-(tert-butyl)ureido)-2-oxopyrazin-1(2H)-yl)acetamido)-3-hydroxy-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00015
1-(2-(6-benzyl-3-(3-(tert-butyl)ureido)-5-chloro-2-oxopyrazin-1(2H)-yl)acetamido)-3-(benzyloxy)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.0002 - 0.0003
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
0.000052 - 0.00377
1-aminocyclopropane-1-carboxylic acid ketoacid
0.00037 - 0.00562
1-aminocyclopropane-1-carboxylic acid ketotetrazole
0.00149 - 0.0041
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
0.0000062 - 0.00032
1-aminocyclopropanecarboxylic acid
0.000006
12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)-methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000015
12-tert-butyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000017
12-tert-butyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)-aminooxalyl)butyl)amide
-
protease continous assay
0.000065
2,2,2-trifluoro-1,1-dimethylethyl[2-[(1S,5R)-2(S)-[[[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]amino]-carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]carbamate
-
-
0.00003 - 0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-(pyrimidin-5-yl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
0.00002 - 0.00011
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-fluoro-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
0.00013
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((2-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00023
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((3-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)-4-vinylbenzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00026
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-Nmethyl-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-Ntosylbenzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000017 - 0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoic acid
0.00022
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00003 - 0.00014
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
0.00009 - 0.00031
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-[(naphthalen-1-yl)methyl]-2-oxopyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
0.00007 - 0.00027
2-(2-[6-benzyl-3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
0.000024 - 0.00014
2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)-N-(4-(2-oxo-2-(4-(trifluoromethyl)phenylsulfonamido)ethyl)phenyl)acetamide
0.0008
2-(4-[3-[1-Carboxy-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid
pH 6.5, 30°C
0.001
2-(4-[3-[1-tert-Butoxycarbonyl-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid tert-butyl ester
pH 6.5, 30°C
0.01
2-(6-benzyl-3-(3-(tert-butyl)ureido)-5-chloro-2-oxopyrazin-1(2H)-yl)acetate
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.03
3,4-dichloroisocoumarin
-
-
0.0001
3-(2-(3-(3-(tert-b-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-5-(trifluoromethyl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00017
3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.14
3-(4-hydroxy-3,5-diiodophenyl)-2-phenylpropanoic acid
pH 6.5, 30°C
0.1
3-(4-hydroxy-3,5-diiodophenyl)-3-phenylpropanoic acid
pH 6.5, 30°C
0.08
3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
pH 6.5, 30°C
0.00002 - 0.00007
3-(benzyloxy)-1-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
0.000021
3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)-henicosa-13(21),14,16(20)-triene-18-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
continous enzyme assay
0.0034
3-[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]propanoic acid
-
-
0.0043
3-[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]propanoic acid
-
-
0.0185
3-[2-(2-Benzyloxycarbonylamino-3-methyl-pentanoylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.017
3-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.000004
3-[2-(2-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-carboxy-butyrylamino)-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.00003
3-[2-(3-tert-butyl-ureido)-2-indan-2-yl-acetyl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.000007
3-[2-(3-tert-butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.0046
3-[2-[2-(2-Acetylamino-3,3-diphenyl-propionylamino)-4-tert-butoxycarbonyl-butyrylamino]-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.00006 - 0.00026
4-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
0.45
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
-
0.0021 - 0.004
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
0.0006 - 0.0013
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
0.18
4-(4-hydroxy-3,5-diiodophenyl)butanoic acid
pH 6.5, 30°C
1.89
4-(amidinophenyl)-methanesulfonyl fluoride
-
-
0.00015
4-bromo-2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.6
4-hydroxy-3,5-diiodobenzoic acid
pH 6.5, 30°C
0.0073 - 0.0135
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
0.000019 - 0.00003
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
0.06
4MeBu-P-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30°C
0.000007
5-cyclohexyl-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo(15.3.1.17,10)-docosa-1(21),17,19-triene-8-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000015
6,6-dichloro-3-[2-cyclohexyl-2-(3-cyclohexyl-ureido)-acetyl]-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.0038 - 0.004
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
0.3
acetyl-3,3-diphenylalanine-beta-cyclohexylalanine-Cys-OH
-
-
0.009 - 0.055
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
0.0028 - 0.025
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
0.0018 - 0.018
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
0.016 - 0.025
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
0.0012
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys
-
pH 6.5, 30°C, strain 1a
0.0011 - 0.03
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
0.018 - 0.024
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
0.000012
acetyl-Asp-D-(gamma-carboxyglutamic acid)-Leu-Ile-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30°C
0.000041
acetyl-Asp-Glu-(3,3-diphenylalanine)-Glu-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30°C
0.00022
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30°C
0.000055 - 0.04
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
0.00005
acetyl-Asp-Glu-3,3-diphenylalanine-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.046
acetyl-Asp-Glu-3,3-diphenylalanine-Ile-beta-cyclohexylalanine-OH
-
-
0.00049
acetyl-Asp-Glu-Leu-Glu-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30°C
0.0026
acetyl-Asp-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.00006
acetyl-Asp-Glu-Leu-Ile-beta-cyclohexylalanine-Cys-OH
-
-
0.00035
acetyl-Asp-Glu-Met-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.00036
acetyl-Asp-Glu-Met-Glu-Glu-Cys
-
pH 7.5, 30°C
0.001
acetyl-Asp-Glu-Met-Glu-Glu-Cys-OH
-
-
0.000013
acetyl-Asp-Glu-Val-Val-Pro-boroAlg-OH
-
-
0.17 - 0.21
acetyl-DEMEEC-OH
0.4 - 0.45
acetyl-DYPSPC-OH
0.46 - 0.51
acetyl-ECTTPC-OH
0.1 - 0.15
acetyl-EDVVCC-OH
0.000096
acetyl-EEVVP-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30°C
0.0016
acetyl-EEVVP-norvaline-(CO)-phenethylamide
-
pH 6.5, 30°C
0.0014
acetyl-Glu-3,3-diphenylalanine-Glu-beta-cyclohexyalanine-Cys-OH
-
-
0.46
acetyl-Glu-beta-cyclohexylalanine-Cys-OH
-
-
5
acetyl-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.08
acetyl-P-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30°C
0.04 - 0.05
acetyl-QSVVCC-OH
0.00059
alpha1-antitrypsin
-
pH 8.0, 18°C
-
0.00001761 - 0.000026
Aprotinin
0.0000004
asunaprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000049
benzyl 1-([[(2S)-1-[(1R,5S)-2-[(4-amino-1-cyclopropyl-3,4-dioxobutan-2-yl)carbamoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hex-3-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]amino)cyclohexanecarboxylate
-
pH and temperature not specified in the publication
0.000001 - 0.0012
BILN 2061
0.00000038 - 0.00061
BILN-2061
0.00075
Bz-Ala-Lys-Arg-Arg-H
-
-
0.0004
Bz-Lys-Arg-Arg-H
-
-
0.0009
Bz-Nle-Ala-Arg-Arg-H
-
-
0.125
Bz-Nle-Lys-Ala-Arg-H
-
-
0.03315
Bz-Nle-Lys-Arg-Ala-H
-
-
0.0004
Bz-Nle-Lys-Arg-Arg-H
-
-
0.0112
Bz-Nle-Lys-Arg-Lys-H
-
-
0.062
Bz-Nle-Lys-Arg-Phe-H
-
-
0.00005
Bz-Nle-Lys-Lys-Arg-B(OH)2
-
-
0.0012
Bz-Nle-Lys-Lys-Arg-H
-
-
0.0156
Bz-Nle-Lys-Phe-Arg-H
-
-
0.0015
Bz-Nle-Phe-Arg-Arg-H
-
-
0.00025
Bz-Phe-Lys-Arg-Arg-H
-
-
0.00000019
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.0000000091
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.0000044
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0. 04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.000001
danoprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000002
deca-D-Arg-NH2
-
pH 8.0, 18°C
0.000001
dodeka-D-Arg-NH2
-
pH 8.0, 18°C
0.00000097
faldaprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000124
fluorescein-L-Asp-D-Glu-L-Leu-L-Ile-L-beta-cyclohexylalanine-L-Cys-L-Pro-L-beta-cyclohexylalanine-L-Asp-L-Leu-NH2
-
pH 7.3, 30°C
0.00000014
grazoprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000041
hepta-D-Arg-NH2
-
pH 8.0, 18°C
0.000478
hexa-D-Arg-NH2
-
pH 8.0, 18°C
0.000098 - 0.00275
L-aminobutyric acid carboxylic acid
0.000051 - 0.00082
L-aminobutyric acid pentafluoroethyl ketone
0.000016 - 0.00045
L-norvaline carboxylic acid
0.000134 - 0.00188
L-norvaline ketotetrazole
0.000117 - 0.00035
L-norvaline pentafluoroethyl ketone
0.000015 - 0.00012
methyl 2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoate
0.00000006 - 0.0000014
MK-7009
0.00003 - 0.00018
N-((2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
0.00006 - 0.00019
N-((3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
0.00017
N-((4-(2-(3-(3-(tert-butyl)ureido)-5-chloro- 6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000041 - 0.000078
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
0.0000095 - 0.000015
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
0.000102
N-([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
0.00256
N-([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
1.17
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-beta-phenyl-L-phenylalanyl-L-alpha-glutamyl-3-cyclohexyl-L-alanine
-
-
0.00000074
N-acetyl-L-alpha-aspartyl-N-[(1S)-2-[[(1S)-1-([(2S,4R)-2-[[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]carbamoyl]-4-[(2-phenylquinolin-4-yl)oxy]pyrrolidin-1-yl]carbonyl)-2,2-dimethylpropyl]amino]-1-cyclohexyl-2-oxoethyl]-D-alpha-glutamine
-
-
0.000071 - 0.00011
N-acetyl-L-aspartyl-L-glutamyl-L-isoleucyl-L-valyl-(3R)-3-(benzyloxy)-L-prolyl-N-[(1S)-1-phenylethyl]-L-norleucinamide
0.03
N-tosyl-Phe chloromethyl ketone
-
-
0.000067
N-[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]-L-norvaline
-
-
0.000003
N-[(2S)-2-[(N-acetyl-L-alpha-aspartyl-D-alpha-glutamyl)amino]-2-cyclohexylacetyl]-L-valyl-(4S)-4-(naphthalen-2-ylmethoxy)-D-prolyl-D-norvaline
-
-
0.00025 - 0.00041
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
0.002 - 0.0036
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
0.0000004 - 0.0000005
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
0.0000002
N-[17-[8-chloro-2-(4-isopropylthiazol-2-yl)-7-methoxy-quinolin-4-yloxy]-2,14-dioxo-3,15-diazatricyclo [13.3.0.0]octadec-7-ene-4-carbonyl]-(1-methylcyclo propyl)-(1-methylcyclopropyl)sulfonamide
-
-
0.00004 - 0.00017
N-[2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chlorobenzene-1-sulfonyl]-4-(trifluoromethyl)benzamide
0.15
Nalpha-p-tosyl-Lys chloromethyl ketone
-
-
0.000007
narlaprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000006
nona-D-Arg-NH2
-
pH 8.0, 18°C
0.000017
octa-D-Arg-NH2
-
pH 8.0, 18°C
0.6
phenylmethanesulfonyl fluoride
-
-
0.000021 - 0.000028
SCH-503034
0.02
SCH217135
-
pH 6.5, 30°C
0.048
SCH217142
-
pH 6.5, 30°C
0.06
SCH217942
-
pH 6.5, 30°C
0.00000036
simeprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000091
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
pH 7.5, 30°C
0.000098
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
pH 7.5, 30°C
0.0000038
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
pH 7.5, 30°C
0.0000136
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
pH 7.5, 30°C
0.000081
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
pH 7.5, 30°C
0.000028
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
pH 7.5, 30°C
0.000015 - 0.00004
telaprevir
0.000041
tert-butyl (1-cyclohexyl-2-[(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl)carbamate
-
continuous protease assay
0.000027
tert-butyl (1-[[(3R)-3-([1-(2-cyclobutylethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
continuous protease assay
0.000019
tert-butyl (1-[[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
continuous protease assay
0.002
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
0.002
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
0.00026
tert-butyl (2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.0023
tert-butyl (2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.000044
tert-butyl (2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.000038
tert-butyl (2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoate
-
-
0.00004
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]-4-methylpentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
continuous protease assay
0.000081
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
continuous protease assay
0.00002
tert-butyl [1-cyclohexyl-2-[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl]carbamate
-
continuous protease assay
0.000051
tert-butyl [2-[(3R)-3-([1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
continuous protease assay
0.007
trans-1,2-cyclohexanediamine-N,N,N',N'-tetraacetic acid
-
-
0.000001
undeca-D-Arg-NH2
-
pH 8.0, 18°C
0.00000005 - 0.00000074
vaniprevir
0.0039
[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]acetic acid
-
-
0.005
[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]acetic acid
-
-
0.00000007
[(Z)-(1R,4R,6S,15R,17R)-4-cyclopropanesulfonylaminocarbonyl-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-en-13-yl]-carbamic acid tert-butyl ester
-
-
0.000009
[1-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-3-carbonyl]-2,2-dimethyl-propyl]-carbamic acid tert-butyl ester
-
-
0.00006
[2-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hex-3-yl]-1-indan-2-yl-2-oxo-ethyl]-carbamic acid tert-butyl ester
-
-
additional information
additional information
-
peptidyl-alphe ketoamides with Ki-values ranging from 0.17 nM to 5.6 mM
-
0.000014
(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000035
(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.0000001
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.00000062
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine
-
wild type enzyme, at 23°C
0.0000016
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.0000014
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
-
wild type enzyme, at 23°C
0.0000028
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.000022
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
wild type enzyme, at 23°C
0.000055
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.00001
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00001
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.0002
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
with Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide as substrate
0.0003
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
with Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide as substrate
0.000052
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 6.0
0.00019
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 6.0 and 100 mM NaCl
0.00182
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 8.0 and 100 mM NaCl
0.00377
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 8.0
0.00037
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 6.0
0.00107
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 6.0 and 100 mM NaCl
0.00227
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 8.0 and 100 mM NaCl
0.00562
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 8.0
0.00149
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 6.0
0.00168
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.0032
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.0041
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 8.0
0.0000062
1-aminocyclopropanecarboxylic acid
-
at pH 6.0
0.000025
1-aminocyclopropanecarboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.0002
1-aminocyclopropanecarboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00032
1-aminocyclopropanecarboxylic acid
-
at pH 8.0
0.00003
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-(pyrimidin-5-yl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-(pyrimidin-5-yl)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00002
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-fluoro-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00011
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-4-fluoro-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000017
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoic acid
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00012
2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoic acid
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00003
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00014
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00009
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-[(naphthalen-1-yl)methyl]-2-oxopyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00031
2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-6-[(naphthalen-1-yl)methyl]-2-oxopyrazin-1(2H)-yl]acetamido)-4-chloro-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00007
2-(2-[6-benzyl-3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00027
2-(2-[6-benzyl-3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxopyrazin-1(2H)-yl]acetamido)-N-[4-(trifluoromethyl)benzene-1-sulfonyl]benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000024
2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)-N-(4-(2-oxo-2-(4-(trifluoromethyl)phenylsulfonamido)ethyl)phenyl)acetamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00014
2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)-N-(4-(2-oxo-2-(4-(trifluoromethyl)phenylsulfonamido)ethyl)phenyl)acetamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00002
3-(benzyloxy)-1-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00007
3-(benzyloxy)-1-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)cyclobutane-1-carboxamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00006
4-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00026
4-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)-N-((4-(trifluoromethyl)phenyl)sulfonyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.0021
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
wild-type enzyme
0.0023
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136R
0.004
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136M
0.0006
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
wild-type enzyme
0.0009
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136R
0.0013
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136M
0.0073
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
wild-type enzyme
0.0083
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
mutant enzyme K136R
0.0135
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
mutant enzyme K136M
0.000019
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.00003
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.0038
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
for Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide
0.004
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
for AAc-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
0.009
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a
0.01
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.01
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.01
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.013
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R
0.04
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.045
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.05
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.055
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.0028
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.0032
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R
0.0045
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a
0.005
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.0052
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.02
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.02
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.025
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.025
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.0018
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a
0.0027
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.0029
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R
0.0033
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.004
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.01
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.013
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.015
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.018
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.016
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a
0.02
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.02
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.021
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.021
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.023
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.023
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.024
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T12 3R
0.025
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.0011
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.0022
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.0026
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.0032
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R
0.024
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.025
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.03
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.03
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.018
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T
0.018
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme Q168D
0.019
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a
0.019
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R
0.02
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme R123T/D168Q
0.021
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a
0.022
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 3a, mutant enzyme T123R/Q168D
0.023
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1b
0.024
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30°C, strain 1a, mutant enzyme D168Q
0.000055
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R161S
0.00006
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R123T
0.0000615
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K165S
0.000079
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R109Q
0.000129
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R155S
0.000179
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K165S/R1161S
0.00031
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K136M/R109Q
0.000313
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K136M
0.04
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, wild-type enzyme
0.17
acetyl-DEMEEC-OH
-
pH 6.5, 30°C, strain 1b
0.2
acetyl-DEMEEC-OH
-
pH 6.5, 30°C, strain 1a
0.21
acetyl-DEMEEC-OH
-
pH 6.5, 30°C, strain 3a
0.4
acetyl-DYPSPC-OH
-
pH 6.5, 30°C, strain 1b
0.43
acetyl-DYPSPC-OH
-
pH 6.5, 30°C, strain 3a
0.45
acetyl-DYPSPC-OH
-
pH 6.5, 30°C, strain 1a
0.46
acetyl-ECTTPC-OH
-
pH 6.5, 30°C, strain 1b
0.5
acetyl-ECTTPC-OH
-
pH 6.5, 30°C, strain 1a
0.51
acetyl-ECTTPC-OH
-
pH 6.5, 30°C, strain 3a
0.1
acetyl-EDVVCC-OH
-
pH 6.5, 30°C, strain 3a
0.13
acetyl-EDVVCC-OH
-
pH 6.5, 30°C, strain 1a
0.15
acetyl-EDVVCC-OH
-
pH 6.5, 30°C, strain 1b
0.04
acetyl-QSVVCC-OH
-
pH 6.5, 30°C, strain 1a
0.04
acetyl-QSVVCC-OH
-
pH 6.5, 30°C, strain 3a
0.05
acetyl-QSVVCC-OH
-
pH 6.5, 30°C, strain 1b
0.00001761
Aprotinin
-
-
0.000026
Aprotinin
-
pH 8.0, 18°C
0.000001
BILN 2061
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C
0.0000014
BILN 2061
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C
0.000003
BILN 2061
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C
0.0000037
BILN 2061
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C
0.000015
BILN 2061
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C
0.000019
BILN 2061
wild-type, pH 7.8, 30°C
0.0012
BILN 2061
or above, mutant A156T, pH 7.8, 30°C
0.0012
BILN 2061
or above, mutant A156V, pH 7.8, 30°C
0.00000038
BILN-2061
-
-
0.000003
BILN-2061
-
NS3/4A genotype 1b
0.0000081
BILN-2061
-
NS3/4A genotype 1a
0.00007
BILN-2061
-
NS3/4A genotype 2a
0.00061
BILN-2061
-
NS3/4A genotype 2b
0.000014
boceprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000014
boceprevir
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.000098
L-aminobutyric acid carboxylic acid
-
at pH 6.0
0.00025
L-aminobutyric acid carboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.00125
L-aminobutyric acid carboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00275
L-aminobutyric acid carboxylic acid
-
at pH 8.0
0.000051
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.000084
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 6.0
0.00015
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.00082
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 8.0
0.000016
L-norvaline carboxylic acid
-
at pH 6.0
0.000031
L-norvaline carboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.000245
L-norvaline carboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00045
L-norvaline carboxylic acid
-
at pH 8.0
0.000134
L-norvaline ketotetrazole
-
at pH 6.0
0.00046
L-norvaline ketotetrazole
-
at pH 6.0 and 100 mM NaCl
0.00174
L-norvaline ketotetrazole
-
at pH 8.0
0.00188
L-norvaline ketotetrazole
-
at pH 8.0 and 100 mM NaCl
0.000117
L-norvaline pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.000145
L-norvaline pentafluoroethyl ketone
-
at pH 8.0
0.00015
L-norvaline pentafluoroethyl ketone
-
at pH 6.0
0.00035
L-norvaline pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.000015
methyl 2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoate
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00012
methyl 2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(2-cyclohexylethyl)-2-oxopyrazin-1(2H)-yl)acetamido)benzoate
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00000006
MK-7009
-
NS3/4A genotype 1b
0.00000007
MK-7009
-
NS3/4A genotype 1a
0.000001
MK-7009
-
NS3/4A genotype 2a
0.0000014
MK-7009
-
NS3/4A genotype 2b
0.00003
N-((2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00018
N-((2-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.00006
N-((3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00019
N-((3-(2-(3-(3-(tert-butyl)ureido)-5-chloro-6-(naphthalen-1-ylmethyl)-2-oxopyrazin-1(2H)-yl)acetamido)phenyl)sulfonyl)-4-(trifluoromethyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000041
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
wild type enzyme, at 23°C
0.000078
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.0000095
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
wild type enzyme, at 23°C
0.000015
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.000071
N-acetyl-L-aspartyl-L-glutamyl-L-isoleucyl-L-valyl-(3R)-3-(benzyloxy)-L-prolyl-N-[(1S)-1-phenylethyl]-L-norleucinamide
-
wild type enzyme, at 23°C
0.00011
N-acetyl-L-aspartyl-L-glutamyl-L-isoleucyl-L-valyl-(3R)-3-(benzyloxy)-L-prolyl-N-[(1S)-1-phenylethyl]-L-norleucinamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.00025
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
wild type enzyme, at 23°C
0.00041
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.002
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
wild type enzyme, at 23°C
0.0036
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23°C
0.0000004
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
-
-
0.0000005
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
hepatitis C virus genotype 1a
-
-
0.00004
N-[2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chlorobenzene-1-sulfonyl]-4-(trifluoromethyl)benzamide
-
inhibition of enzyme mutant R155K, pH and temperature not specified in the publication
0.00017
N-[2-(2-[3-[(tert-butylcarbamoyl)amino]-5-chloro-2-oxo-6-(2-phenylethyl)pyrazin-1(2H)-yl]acetamido)-4-chlorobenzene-1-sulfonyl]-4-(trifluoromethyl)benzamide
-
inhibition of full-length wild-type enzyme, pH and temperature not specified in the publication
0.000021
SCH-503034
-
NS3/4A genotype 1a
0.000021
SCH-503034
-
NS3/4A genotype 2b
0.000025
SCH-503034
-
NS3/4A genotype 2a
0.000028
SCH-503034
-
NS3/4A genotype 1b
0.000015
telaprevir
-
pH and temperature not specified in the publication
0.0000344
telaprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00004
telaprevir
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.00000005
vaniprevir
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000074
vaniprevir
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000042
VX-950
-
NS3/4A genotype 2b
0.000054
VX-950
-
NS3/4A genotype 2a
0.000093
VX-950
-
NS3/4A genotype 1b
0.0001
VX-950
wild-type, pH 7.8, 30°C
0.00013
VX-950
-
NS3/4A genotype 1a
0.0099
VX-950
mutant A156T, pH 7.8, 30°C
0.033
VX-950
mutant A156V, pH 7.8, 30°C
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000008
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000006
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.01855 - 0.07006
(-)-epicatechin-3-O-gallate
0.00851 - 0.05647
(-)-epigallocatechin-3-O-gallate
0.0000029
(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-15-oxo-1,2,3,7,8,9,10,12a,13,14,15,15a-dodecahydrocyclopropa[f]pyrrolo[1,2-b][1,2,5]thiadiazacyclotetradecine-13a(6H)-carboxamide 5,5-dioxide
Hepacivirus C
-
pH not specified in the publication, temperature not specified in the publication
0.0000004
(11Z,13aR,15aS)-N-(cyclopropylsulfonyl)-2-([7-methoxy-8-methyl-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl]oxy)-5,15-dioxo-1,2,3,5,6,7,8,9,10,12a,13,14,15,15a-tetradecahydro-13aH-cyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclotetradecine-13a-carboxamide
Hepacivirus C
-
pH not specified in the publication, temperature not specified in the publication
0.0004
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
Hepacivirus C
-
-
0.13
(1R)-2-but-3-en-1-yl-1-[[(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]hept-6-enoyl]-4-(quinolin-4-yloxy)-L-prolyl]amino]cyclopropanecarboxylic acid
Hepacivirus C
-
-
0.000001
(2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14-carboxylic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000077
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.004
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-5,16-dioxo-2-(quinolin-4-yloxy)-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.00024
(2R,6S,10Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.0001
(2R,6S,12Z,14aR,16aS)-2-[(8-chloro-2-ethoxyquinolin-4-yl)oxy]-6-[[(cyclopentyloxy)carbonyl]amino]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.000011
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.0001
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[(4-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.0001
(2R,6S,12Z,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[(5-ethoxythieno[3,2-b]pyridin-7-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.000028
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
Hepacivirus C
-
-
0.034
(2S,4S)-1-((S)-2-(furan-2-carboxamido)-3,3-dimethylbutanoyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0074
(2S,4S)-1-((S)-2-benzamido-2-cyclohexylacetyl)-N-((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0025
(2S,4S)-1-((S)-2-benzamido-2-cyclohexylacetyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0019
(2S,4S)-1-((S)-2-cyclohexyl-2-(thiophene-2-carboxamido)acetyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.1
(2S,4S)-1-((S)-2-cyclohexyl-2-isobutyramidoacetyl)-N-((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.1
(2S,4S)-1-((S)-2-isobutyramido-3-phenylpropanoyl)-N-((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidine-2-carboxamide
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.053
(3R,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
Hepacivirus C
-
-
0.0075
(3S,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
Hepacivirus C
-
-
0.0000021
(4R,6S,7Z,15S,17S)-17-[((7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl)oxy)methyl]-13-methyl-N-[(1-methylcyclopropyl)sulfonyl]-2,14-dioxo-1,3,13-triazatricyclo[13.2.0.0-4,6-]heptadec-7-ene-4-carboxamide
Hepacivirus C
pH not specified in the publication, temperature not specified in the publication
0.0000013
(4R,6S,7Z,15S,17S)-17-[((8-chloro-7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinolin-4-yl)oxy)methyl]-13-methyl-N-[(1-methylcyclopropyl)sulfonyl]-2,14-dioxo-1,3,13-triazatricyclo[13.2.0.0-4,6-]heptadec-7-ene-4-carboxamide
Hepacivirus C
pH not specified in the publication, temperature not specified in the publication
0.000006
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000086
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000044
(R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000006
(R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000009
(R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000008
(R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000003
(S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000003
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000001
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000006
(S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.000003
(S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.78 - 5.9
1,10-phenanthroline
0.00064
1,3,4-tri-O-galloyl-beta-D-glucose
Hepacivirus C
-
-
0.00642
1,3,6-tri-O-galloyl-beta-D-glucose
Hepacivirus C
-
-
0.0097
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-2-vinyl-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.0097 mM
0.33
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.33 mM
1
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-hydroxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: above 1 mM
0.08
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-phenoxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: above 0.08 mM
0.006
1-([4-(3'-Acetylamino-biphenyl-3-yloxy)-1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.006 mM
0.00064
1-O-(3-O-galloylgalloyl)-2,3,4-tri-O-galloyl-beta-D-glucose
Hepacivirus C
-
-
0.025
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.025 mM
0.2
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-thiophen-3-yl-pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: above 0.2 mM
0.006
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3'-nitro-biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.006 mM
0.05
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.05 mM
0.032
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-morpholin-4-yl-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.032 mM
0.2
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: above 0.2 mM
0.035
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.035 mM
0.025
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.025 mM
0.04
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.04 mM
0.05
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-chloro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.05 mM
0.1
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-fluoro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.1 mM
0.01
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-iodo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.01 mM
0.1
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(5-chloro-quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.1 mM
0.016
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(6-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.016 mM
0.002
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-chloro-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.002 mM
0.0008
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.0008 mM
0.006
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.006 mM
0.009
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.009 mM
0.02
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.02 mM
0.02
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.02 mM
0.2
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: above 0.2 mM
0.006
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.006 mM
0.035
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.035 mM
0.008
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-1-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.008 mM
0.004
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.004 mM
0.31
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2,2-diethyl-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.31 mM
0.0048
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-ethyl-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.0048 mM
0.00063
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.00063 mM
0.014
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
IC50: 0.014 mM
0.19
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.19 mM
0.17
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.17 mM
0.005
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.005 mM
0.25
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
Hepacivirus C
-
IC50: 0.25 mM
0.2
2'-[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-5-(1-carboxy-cyclopropylcarbamoyl)-pyrrolidin-3-yloxy]-biphenyl-4-carboxylic acid
Hepacivirus C
-
IC50: above 0.2 mM
0.1
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
Hepacivirus C
-
IC50: above 0.1 mM
0.054
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
Hepacivirus C
-
IC50: 0.054 mM
0.0017
2-(4-Butyl-phenyl)-2-phenylsulfanyl-indan-1,3-dione
Hepacivirus C
-
IC50: 0.0017 mM
0.53
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-pentanoic acid
Hepacivirus C
IC50: 0.53 mM
0.14
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbony]}-amino)-3-mercapto-propionic acid
Hepacivirus C
IC50: 0.14 mM
0.0036
2-Methyl-2-phenylsulfanyl-indan-1,3-dione
Hepacivirus C
-
IC50: 0.0036 mM
0.00062
2-O-(4-O-galloylgalloyl)-1,3,4-tri-O-galloyl-beta-D-glucose
Hepacivirus C
-
-
0.012
2-Phenyl-2-phenylsulfanyl-indan-1,3-dione
Hepacivirus C
-
IC50: 0.012 mM
0.0031
2-Phenylsulfanyl-2-p-tolyl-indan-1,3-dione
Hepacivirus C
-
IC50: 0.0031 mM
0.3
2-[1-[1-(1-Carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
Hepacivirus C
-
IC50: 0.015 mM, wild-type enzyme, IC50: 0.017 mM, mutant enzyme K136R, IC50: 0.027 mM, mutant enzyme K136M, IC50: 0.05 mM, mutant enzyme K136S, IC50: above 0.3 mM, mutant enzyme R109Q
0.032
2-[1-[2-Carboxy-1-(1-ethylcarbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
Hepacivirus C
-
IC50: 0.032 mM
0.00091
3,3'-digalloylprocyanidin B2
Hepacivirus C
-
-
0.00077 - 0.02596
3,3'-digalloylproprodelphinidin B2
0.46
3,6-di-O-galloyl-beta-D-glucose
Hepacivirus C
-
-
0.0092
3-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
Hepacivirus C
-
IC50: 0.0092 mM
0.025
3-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
Hepacivirus C
-
IC50: 0.025 mM
0.0007
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid
Hepacivirus C
-
IC50: 0.0007 mM
0.0032
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid methyl ester
Hepacivirus C
-
IC50: 0.0032 mM
0.002
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
Hepacivirus C
-
IC50: 0.002 mM
0.017
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
Hepacivirus C
-
IC50: 0.017 mM
0.04
4-Benzyloxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 0.04 mM
0.019
4-Isobutoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 0.019 mM
0.0065
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
Hepacivirus C
-
IC50: 0.0065 mM
0.2
4-tert-Butoxycarbonylamino-4-[1-(1-carboxy-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: above 0.2 mM
0.027
4-tert-Butoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 0.027 mM
0.2
4-[1-(1-Benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-4-tert-butoxycarbonylamino-butyric acid
Hepacivirus C
-
IC50: above 0.2 mM
0.000002
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl)-butyric acid
Hepacivirus C
-
IC50: 2 nM
0.00025
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[1-(1-benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-2-cyclohexyl-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 250 nM
0.000007
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 7 nM
0.00154
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(2-cyclohexyl-ethylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 1540 nM
0.0017
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(indan-2-ylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 1700 nM
0.0015
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(2-phenyl-cyclopropylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 1500 nM
0.00021
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(3-phenyl-propylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 210 nM
0.07
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(methyl-phenethyl-carbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
Hepacivirus C
-
IC50: 0.07 mM
0.0006
acetyl-Asp-D-Glu-Leu-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
Hepacivirus C
-
IC50: 0.0006 mM, inhibitor is cleaved by NS3/4A protease
0.0034
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
Hepacivirus C
-
IC50: 0.0034 mM, inhibitor is cleaved by NS3/4A protease
0.0019
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
Hepacivirus C
-
IC50: 0.0019 mM, inhibitor is cleaved by NS3/4A protease
0.0035
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(Me)Ala-Nle-Ser-Tyr-NH2
Hepacivirus C
-
IC50: 0.0035 mM, inhibitor is cleaved by NS3/4A protease
0.001
acetyl-Glu-Asp-Val-Val-Leu-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
Hepacivirus C
-
IC50: 0.001 mM, inhibitor is cleaved by NS3/4A protease
0.0000713
antibody Fv fragment
Hepacivirus C
-
specific for the HCV NS3 protease domain, IC50: 71.3 nM
-
5
Asp-Glu-Leu-Ile-L-cyclohexylalanine-aminobutyryl-(Me)Ala-Ser-His-Leu
Hepacivirus C
-
IC50: 5 mM
0.000015
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-OH
Hepacivirus C
-
IC50: 15 nM
0.0000002
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-L-cyclohexylalanine-Asp-Leu
Hepacivirus C
-
IC50 below 0.2 nM
0.00001
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-Nle-Ser-Leu
Hepacivirus C
-
IC50: 10 nM
0.0045
benzyl((S)-1-cyclohexyl-2-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-2-oxoethyl)carbamate
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0000003 - 0.000037
BILN 2061
0.000003
BILN-2061
Hepacivirus C
-
-
0.000001 - 0.000012
BMS-605339
0.7
Bz-Ala-Lys-Arg-Arg-H
West Nile virus
-
-
2.6
Bz-D-Nle-Lys-Arg-Arg-H
West Nile virus
-
-
9.3
Bz-N-Me-Nle-Lys-Arg-Arg-H
West Nile virus
-
-
3.8
Bz-Nle-Ala-Arg-Arg-H
West Nile virus
-
-
23.8
Bz-Nle-D-Lys-Arg-Arg-H
West Nile virus
-
-
262
Bz-Nle-Lys-Ala-Arg-H
West Nile virus
-
-
202.8
Bz-Nle-Lys-Arg-(p-Cl)-Phe-H
West Nile virus
-
-
62
Bz-Nle-Lys-Arg-(p-CN)-Phe-H
West Nile virus
-
-
11.8
Bz-Nle-Lys-Arg-(p-guanidinyl)-Phe-H
West Nile virus
-
-
22.7
Bz-Nle-Lys-Arg-(p-Ph)-Phe-H
West Nile virus
-
-
4.6
Bz-Nle-Lys-Arg-Ala-H
West Nile virus
-
-
4.1
Bz-Nle-Lys-Arg-Arg-H
West Nile virus
-
-
14
Bz-Nle-Lys-Arg-D-Arg-H
West Nile virus
-
-
43.1
Bz-Nle-Lys-Arg-His-H
West Nile virus
-
-
57.7
Bz-Nle-Lys-Arg-Lys-H
West Nile virus
-
-
109.8
Bz-Nle-Lys-Arg-Phe-H
West Nile virus
-
-
90.9
Bz-Nle-Lys-Arg-Phg-H
West Nile virus
-
-
10
Bz-Nle-Lys-Arg-Trp-H
West Nile virus
-
-
41.5
Bz-Nle-Lys-Arg-Tyr-H
West Nile virus
-
-
128.6
Bz-Nle-Lys-D-Arg-Arg-H
West Nile virus
-
-
99.5
Bz-Nle-Lys-Lys(Z)-Arg-H
West Nile virus
-
-
1.9
Bz-Nle-Lys-Lys-Arg-H
West Nile virus
-
-
57.8
Bz-Nle-Lys-N-Me-Arg-Arg-H
West Nile virus
-
-
108
Bz-Nle-Lys-Phe-Arg-H
West Nile virus
-
-
73.6
Bz-Nle-N-Me-Lys-Arg-Arg-H
West Nile virus
-
-
4.2
Bz-Nle-Phe-Arg-Arg-H
West Nile virus
-
-
14.3
Bz-Nle-Pro-Arg-Arg-H
West Nile virus
-
-
1.2
Bz-Phe-Lys-Arg-Arg-H
West Nile virus
-
-
0.0000025
ITMN-191
Hepacivirus C
-
-
0.00008 - 0.00366
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
0.000004 - 0.000026
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
0.000002 - 0.000009
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
0.000057 - 0.00406
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
0.00019 - 0.00247
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
0.000052 - 0.0037
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
0.000076 - 0.00327
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
0.000105 - 0.00147
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
0.00014 - 0.00236
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
0.000136 - 0.00231
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
0.00008 - 0.00645
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
0.000568 - 0.00424
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
0.000134 - 0.0077
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
0.000728 - 0.00394
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
0.000005 - 0.000024
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
0.00062 - 0.00321
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
0.00005 - 0.000265
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
0.000026 - 0.000412
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
0.000291 - 0.00495
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
0.000162 - 0.00346
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
0.000703 - 0.00837
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
0.000101 - 0.00625
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
0.000002 - 0.000041
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
0.000007 - 0.000097
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
0.000002 - 0.000039
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
0.00096 - 0.0034
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
0.000127 - 0.00112
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
0.1
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(4-methoxybenzamido)-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.1
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-[(naphthalene-2-carbonyl)amino]-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.0021
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-[2-(2,3-dimethylanilino)benzamido]-L-prolyl-N-(cyclopropanesulfonyl)-L-leucinamide
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0015 - 0.0305
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
0.0039 - 0.0707
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
0.00002
N-(tert-butylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
Hepacivirus C
pH not specified in the publication, temperature not specified in the publication
0.000003
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3R)-2-carboxy-3-ethenylcyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
Hepacivirus C
-
pH and temperature not specified in the publication
0.0000009
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3S)-2-ethenyl-3-phosphonocyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
Hepacivirus C
-
pH and temperature not specified in the publication
0.00066
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[[[3-(dimethylamino)propyl]methylamino]carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
Hepacivirus C
-
IC50: 0.00066 mM
0.00005 - 0.0034
telaprevir
0.00005
tert-butyl [(2R,6S,12Z,14aR,16aS)-14a-[(cyclopropylsulfonyl)carbamoyl]-2-[(6-methoxyisoquinolin-1-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,11,13a,14,14a,15,16,16a-tetradecahydro-5H-cyclopropa[e]pyrrolo[2,1-i][1,7,10]oxadiazacyclopentadecin-6-yl]carbamate
Hepacivirus C
-
-
0.0071
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxo-3-phenylpropan-2-yl)carbamate
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.1
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamate
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.1
tert-butyl((S)-1-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)carbamate
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.0059
tert-butyl((S)-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxo-3-phenylpropan-2-yl)carbamate
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.072
tert-butyl((S)-1-cyclohexyl-2-((2S,4S)-2-(((R)-1-(cyclopropanesulfonamido)-1-oxo-3-phenylpropan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-2-oxoethyl)-carbamate
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.1
tert-butyl((S)-3,3-dimethyl-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxobutan-2-yl)carbamate
Hepatitis C virus genotype 1b
above, pH 7.5, temperature not specified in the publication
0.0056
tert-butyl((S)-3-(1H-indol-3-yl)-1-((2S,4S)-2-(((S)-4-methyl-1-(4-methylphenylsulfonamido)-1-oxopentan-2-yl)carbamoyl)-4-(4-phenyl-1H-1,2,3-triazol-1-yl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamate
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.000001
[(2R,6R,12Z,13aS,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl]phosphonic acid
Hepacivirus C
-
pH and temperature not specified in the publication
0.0005
[1-(6-Ethyl-4-methanesulfonyl-5-oxo-hexahydro-pyrrolo[3,2-b]pyrrole-1-carbonyl)-2-methyl-propyl]-carbamic acid tert-butyl ester
Hepacivirus C
-
IC50: 0.0005 mM
0.4
[1-[1-(2-Mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-2-methyl-propyl]-carbamic acid benzyl ester
Hepacivirus C
-
IC50: 0.4 mM
0.01855
(-)-epicatechin-3-O-gallate
Hepacivirus C
-
-
0.07006
(-)-epicatechin-3-O-gallate
Hepacivirus C
-
methylation of the inhibitor
0.00851
(-)-epigallocatechin-3-O-gallate
Hepacivirus C
-
-
0.04455
(-)-epigallocatechin-3-O-gallate
Hepacivirus C
-
acetylation of the inhibitor
0.05647
(-)-epigallocatechin-3-O-gallate
Hepacivirus C
-
methylation of the inhibitor
0.78
1,10-phenanthroline
Hepacivirus C
inhibition of NS2/3 auto-cleavage of mutant H1175A in the absence of NS4A peptide
0.79
1,10-phenanthroline
Hepacivirus C
inhibition of NS2/3 auto-cleavage of the wild-type in the absence of NS4A peptide
0.89
1,10-phenanthroline
Hepacivirus C
inhibition of NS2/3 auto-cleavage of the wild-type in the presence of NS4A peptide
1.56
1,10-phenanthroline
Hepacivirus C
inhibition of mutant H1175A NS3 protease activity in the absence of NS4A peptide
1.9
1,10-phenanthroline
Hepacivirus C
inhibition of wild-type NS3 protease activity in the absence of NS4A peptide
2.1
1,10-phenanthroline
Hepacivirus C
inhibition of mutant H1175A NS3 protease activity in the presence of NS4A peptide
5.9
1,10-phenanthroline
Hepacivirus C
inhibition of wild-type NS3 protease activity in the presence of NS4A peptide
0.00077
3,3'-digalloylproprodelphinidin B2
Hepacivirus C
-
-
0.02596
3,3'-digalloylproprodelphinidin B2
Hepacivirus C
-
acetylation of the inhibitor
0.0000003
BILN 2061
Hepacivirus C
-
-
0.0000047
BILN 2061
Hepacivirus C
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23°C
0.0000048
BILN 2061
Hepacivirus C
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23°C
0.0000053
BILN 2061
Hepacivirus C
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23°C
0.0000102
BILN 2061
Hepacivirus C
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23°C
0.000037
BILN 2061
Hepacivirus C
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23°C
0.000001
BMS-605339
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000012
BMS-605339
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00008
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00366
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-(3-chlorophenyl)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000004
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000026
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000009
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-biphenyl-4-yl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-methoxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000057
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00406
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluorophenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00019
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00247
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluorophenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000052
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0037
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000076
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00327
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(3-methylphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000105
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00147
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-methoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00014
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00236
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropanesulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-phenyl-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000136
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00231
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(2,5-dimethylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00008
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00645
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3,5-dimethylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000568
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00424
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(3-fluoro-4-methylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000134
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0077
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(4-fluoro-3-methylphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000728
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00394
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-(5-fluoro-2-methoxyphenyl)-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000005
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000024
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(2'-methoxybiphenyl-4-yl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00062
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00321
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4'-methoxybiphenyl-3-yl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00005
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000265
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-(4-phenoxyphenyl)-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000026
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000412
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-naphthalen-2-yl-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000291
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00495
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[2-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000162
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00346
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(morpholin-4-ylmethyl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000703
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00837
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000101
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00625
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[3-(propan-2-yloxy)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000041
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1,3-thiazol-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000007
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000097
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(1H-pyrrol-1-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000002
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.000039
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-[4-(pyridin-2-yl)phenyl]-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.00096
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0034
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-[3-(dimethylamino)phenyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.000127
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.00112
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-4-(1,3-benzothiazol-2-yl)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.0015
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0305
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-hydroxy-4-prop-2-en-1-yl-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.0039
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
hepatitis C virus genotype 1a
pH and temperature not specified in the publication
0.0707
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)acetyl]-2-ethenylcyclopropyl]-4-oxo-L-prolinamide
Hepatitis C virus genotype 1b
pH and temperature not specified in the publication
0.032
ribavirin
Hepacivirus C
-
mutant R155T
0.037
ribavirin
Hepacivirus C
-
mutant R155K
0.039
ribavirin
Hepacivirus C
-
mutant R155M
0.058
ribavirin
Hepacivirus C
-
wild-type
0.00005
telaprevir
Hepacivirus C
-
wild-type, genotype 1a
0.000063
telaprevir
Hepacivirus C
-
wild-type, genotype 1b
0.00013
telaprevir
Hepacivirus C
-
mutant V36L
0.00023
telaprevir
Hepacivirus C
-
mutant V36A
0.00027
telaprevir
Hepacivirus C
-
mutant V36M
0.00045
telaprevir
Hepatitis C virus genotype 1b
pH 7.5, temperature not specified in the publication
0.0034
telaprevir
Hepacivirus C
-
mutant V36M/R155K
0.00005
VX-950
Hepacivirus C
-
wild-type
0.00049
VX-950
Hepacivirus C
-
mutant R155T
0.00051
VX-950
Hepacivirus C
-
mutant R155K
0.00088
VX-950
Hepacivirus C
-
mutant R155I
0.00115
VX-950
Hepacivirus C
-
mutant R155S
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