3.4.23.16 ((S)-1-(N'-(3',5'-difluoro-biphenyl-4-ylmethyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxyindan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester - 79145 3.4.23.16 ((S)-1-(N'-(4'-acetylamino-biphenyl-4-ylmethyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethylpropyl)-carbamic acid methyl ester - 78861 3.4.23.16 ((S)-1-(N'-(4-benzo[1,3]dioxol-5-yl-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxyindan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester - 78967 3.4.23.16 ((S)-1-(N'-benzyl-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester - 78823 3.4.23.16 ((S)-1-(N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-phenethyl-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester - 79146 3.4.23.16 ((S)-1-(N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-[4-(1-methyl-1H-pyrazol-4-yl)-benzyl]-hydrazinocarbonyl)-2,2-dimethyl-propyl)-carbamic acid methyl ester - 79144 3.4.23.16 ((S)-1-(N'-[4-(3,5-dimethyl-isoxazol-4-yl)-benzyl]-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl)-2,2-dimethylpropyl)-carbamic acid methyl ester - 79147 3.4.23.16 ((S)-1-[N'-(4-bromo-benzyl)-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester - 40259 3.4.23.16 ((S)-1-[N'-biphenyl-4-ylmethyl-N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester - 79139 3.4.23.16 ((S)-1-[N'-[(S)-3-Hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester - 40267 3.4.23.16 ((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-3-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester - 40258 3.4.23.16 ((S)-1-[N'-[(S)-3-hydroxy-3-((1S,2R)-2-hydroxy-indan-1-ylcarbamoyl)-4-phenyl-butyl]-N'-(4-pyridin-4-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl)-carbamic acid methyl ester - 78946 3.4.23.16 (1-Benzyl-3-benzylcarbamoyl-3,3-difluoro-2-oxo-propyl)-carbamic acid benzyl ester - 51058 3.4.23.16 (1S)-1-[1-[(1S)-1-[1-[(1S)-1-[1-[(1S)-1-(1-[(2S)-1-[(2-ammonioethyl)amino]-1-oxo-3-phenylpropan-2-yl]-1H-1,2,3-triazol-4-yl)-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethanamine - 81383 3.4.23.16 (1S)-1-[1-[(1S)-1-[1-[(1S)-1-[1-[(1S)-1-[1-[(2S)-1-(methylamino)-1-oxo-3-phenylpropan-2-yl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethanaminium - 79158 3.4.23.16 (1S)-2-methyl-1-[1-[(1S)-1-[1-[(1S)-1-[1-[(1S)-2-methyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]propyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]propan-1-amine - 79115 3.4.23.16 (1S)-2-methyl-1-[1-[(1S)-2-methyl-1-[1-[(1S)-1-[1-[(1S)-2-methyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]propyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]propyl]-1H-1,2,3-triazol-4-yl]propan-1-amine - 79151 3.4.23.16 (1S)-2-methyl-1-[1-[(1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]propan-1-aminium - 79153 3.4.23.16 (1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethanaminium - 79152 3.4.23.16 (1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1S)-2-phenyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethyl]-1H-1,2,3-triazol-4-yl]ethanamine - 79060 3.4.23.16 (2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-4,4,4-trifluoro-3-methylbut-2-enamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65067 3.4.23.16 (2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-4-oxopent-2-enamide - 65068 3.4.23.16 (2E)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(5-methylisoxazol-4-yl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-4,4,4-trifluoro-3-methylbut-2-enamide - 65069 3.4.23.16 (2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(1R,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide - 65077 3.4.23.16 (2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(2R,5S)-2-hydroxy-5-methylcyclopentyl]amino]-5-oxopentyl]-N-tert-butyl-4-(3-pyridin-3-ylpropanoyl)piperazine-2-carboxamide - 65078 3.4.23.16 (2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-2-hydroxy-3-methylbutanamide - 65100 3.4.23.16 (2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-2-hydroxy-3-methylbutanamide - 65101 3.4.23.16 (2S)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-2-hydroxy-3-methylbutanamide - 65102 3.4.23.16 (2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-2-hydroxy-3-methylbutanamide - 65103 3.4.23.16 (2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-2,3-dimethylbutanamide - 65104 3.4.23.16 (2S)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-2-hydroxy-3-methylbutanamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65105 3.4.23.16 (2S)-N-[(1S,2R,3S,4S)-1-benzyl-2,3-dihydroxy-4-[[(2S)-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanoyl]amino]-5-phenylpentyl]-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide - 65106 3.4.23.16 (2S)-N-[(1S,2S,4S)-1-benzyl-2-hydroxy-4-[[(2S)-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanoyl]amino]-5-phenylpentyl]-3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide - 65107 3.4.23.16 (2S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-2-hydroxy-3-methylbutanamide - 14971 3.4.23.16 (2S)-N-[(4S,7S,10S,11R,12R,13S)-10-benzyl-11,12-dihydroxy-4-(naphthalen-1-ylmethyl)-2,2-dioxido-5,8-dioxo-14-phenyl-7-(propan-2-yl)-2l6-thia-3,6,9-triazatetradecan-13-yl]-3-methyl-2-[[(2S)-2-[(methylsulfonyl)amino]-3-(naphthalen-1-yl)propanoyl]amino]butanamide) - 79181 3.4.23.16 (2S,2'S)-N,N'-[(2R,3R)-2,3-dihydroxybutane-1,4-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79253 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-1,6-bis(1,3-benzodioxol-5-yl)-3,4-dihydroxyhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79160 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-1,6-bis(2,4-dimethoxyphenyl)-3,4-dihydroxyhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79210 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-bis(4-hydroxyphenyl)hexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79164 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanamide) - 79315 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-2-benzyl-3-(tert-butylsulfonyl)propanoyl]amino]-3-methylbutanamide) - 79163 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-2-hydroxy-3-phenylpropanoyl]amino]-3-methylbutanamide) - 79174 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(4-methoxybenzyl)propanoyl]amino]-3-methylbutanamide) - 79177 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3,3-dimethylbutanamide) - 79157 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79175 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]pentanamide) - 79176 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[3-(tert-butylsulfonyl)propanoyl]amino]-3-methylbutanamide) - 78829 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[(naphthalen-1-yloxy)acetyl]amino]butanamide) - 79012 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[3-(pyridin-4-ylsulfonyl)propanoyl]amino]butanamide) - 79179 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide) - 24830 3.4.23.16 (2S,2'S)-N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis[2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-(1H-imidazol-4-yl)propanamide] - 79076 3.4.23.16 (2S,2'S)-N,N'-[(2S,3S,4S,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(3-methyl-2-[[methyl(pyridin-2-ylmethyl)carbamoyl]amino]butanamide) - 65111 3.4.23.16 (2S,2'S)-N,N'-[(3S,4R,5R,6S)-4,5-dihydroxy-1,8-di(pyridin-4-yl)octane-3,6-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 78924 3.4.23.16 (2S,2'S)-N,N'-[(3S,4R,5R,6S)-4,5-dihydroxy-1,8-diphenyloctane-3,6-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79169 3.4.23.16 (2S,2'S)-N,N'-[(6S,7R,8R,9S)-7,8-dihydroxytetradecane-6,9-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 78914 3.4.23.16 (2S,2'S)-N1,N1'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]butanediamide) - 79168 3.4.23.16 (2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-dicyclohexylhexane-3,4-diol compound has an improved response to V82A mutant enzyme 37037 3.4.23.16 (2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-1,6-diphenylhexane-3,4-diol - 37035 3.4.23.16 (2S,3S,4S,5S)-2,5-bis[N-[N-[[N-methyl-N-(2-pyridinylmethyl)amino]carbonyl]valinyl] amino]-6-cyclohexyl-1-phenylhexane-3,4-diol compound has an improved response to V82A mutant enzyme 37036 3.4.23.16 (2S,4S)-2-[(1R)-2-(benzylamino)-2-oxo-1-[(phenylacetyl)amino]ethyl]-N-[(1S)-1-hydroxy-2-phenylethyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 65113 3.4.23.16 (2S,4S)-N-[(1R,2R)-4-[(1H-benzimidazol-2-ylmethyl)amino]-1-benzyl-2-hydroxy-4-oxobutyl]-2-[(1R)-1-(benzylcarbamoyl)-3-oxo-4-phenylbutyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 65114 3.4.23.16 (2Z)-4,4,4-trifluoro-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-3-methylbut-2-enamide - 19214 3.4.23.16 (3aR,4R,7aS)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 41896 3.4.23.16 (3aR,5r,6aS)-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 79082 3.4.23.16 (3aR,7aR)-octahydro-1-benzofuran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 41897 3.4.23.16 (3aR,7aR)-octahydro-1H-inden-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 41898 3.4.23.16 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 41895 3.4.23.16 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-3-hydroxy-1-phenylbutan-2-yl]carbamate - 41900 3.4.23.16 (3aS,4S,7aR)-hexahydro-4H-furo[2,3-b]pyran-4-yl {(2S,3R)-3-hydroxy-4-[{[4-(hydroxymethyl)phenyl]sulfonyl}(2-methylpropyl)amino]-1-phenylbutan-2-yl}carbamate - 41901 3.4.23.16 (3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 79077 3.4.23.16 (3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate - 79079 3.4.23.16 (3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate - 79080 3.4.23.16 (3aS,5R,6aR)-hexahydro-2H-cyclopenta[b]furan-5-yl-(2S,3R)-4-(4-amino-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate - 47580 3.4.23.16 (3aS,5R,7aR)-hexahydro-4H-furo[2,3-b]pyran-5-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 86789 3.4.23.16 (3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-3-hydroxypentanamide - 65154 3.4.23.16 (3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-3-hydroxypentanamide - 65155 3.4.23.16 (3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-3-hydroxypentanamide - 65156 3.4.23.16 (3R)-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(5-methylisoxazol-4-yl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3-methylpent-4-enamide - 65157 3.4.23.16 (3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide - 65158 3.4.23.16 (3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide - 65159 3.4.23.16 (3R)-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-3-hydroxypentanamide - 65160 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-(13-methoxy-1,1-dioxido-3,4,5,6,7,8,9,10-octahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl)-1-phenylbutan-2-yl]carbamate GRL-246 158886 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(2-methylpropyl)([1-[2-(piperidin-1-yl)ethyl]-1H-benzimidazol-6-yl]sulfonyl)amino]-1-phenylbutan-2-yl]carbamate - 158894 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-12-methoxy-1,1-dioxido-4,5,6,9-tetrahydro-10,1,2-benzoxathiazacyclododecin-2(3H)-yl]-1-phenylbutan-2-yl]carbamate GRL-396 158787 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-13-methoxy-1,1-dioxido-3,4,5,6,9,10-hexahydro-2H-11,1,2-benzoxathiazacyclotridecin-2-yl]-1-phenylbutan-2-yl]carbamate GRL-216, blocks dimerization 158771 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-3-hydroxy-4-[(7Z)-14-methoxy-1,1-dioxido-4,5,6,9,10,11-hexahydro-12,1,2-benzoxathiazacyclotetradecin-2(3H)-yl]-1-phenylbutan-2-yl]carbamate GRL-286, blocks dimerization 158892 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate - 79090 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-3-hydroxy-4-[(4R)-4-[[4-(hydroxymethyl)-2-methylbenzyl]carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-4-oxo-1-phenylbutan-2-yl]carbamate - 79093 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-4-[(4-amino-2-methylbenzyl)carbamoyl]-5,5-dimethyl-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 79094 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 40209 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-yl-carbamate - 79085 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(2S,3R)-4-(4-amino-N-(((S)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate - 79087 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate - 78942 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate - 79086 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-3-hydroxy-4-(4-methoxy-N-(((S)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-1-phenylbutan-2-ylcarbamate - 79017 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((R)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate - 79249 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((R)-5-oxopyrrolidin-2-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate - 79043 3.4.23.16 (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl-(2S,3R)-4-(4-amino-N-(((S)-2-oxooxazolidin-4-yl)methyl)phenylsulfonamido)-3-hydroxy-1-phenylbutan-2-ylcarbamate - 79124 3.4.23.16 (3R,4aR,8aR)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-(phenylsulfanyl)butyl]decahydroisoquinoline-3-carboxamide - 65161 3.4.23.16 (3R,4aR,8aR)-N-tert-butyl-2-[(R)-2-hydroxy-3-(N-(2-phenylethyl)-4-aminophenylsulfonamido)propyl]decahydroisoquinoline-3-carboxamide - 72757 3.4.23.16 (3R,4aR,8aR)-N-tert-butyl-2-[(R)-2-hydroxy-3-(N-isobutyl-3-aminophenylsulfonamido)propyl]decahydroisoquinoline-3-carboxamide - 72758 3.4.23.16 (3R,4aR,8aR)-N-tert-butyl-2-[(R)-2-hydroxy-3-(N-isobutyl-4-aminophenylsulfonamido)propyl]decahydroisoquinoline-3-carboxamide - 72759 3.4.23.16 (3R,4aR,8aR)-N-tert-butyl-2-[(R)-2-hydroxy-3-(N-propyl-4-aminophenylsulfonamido)propyl]decahydroisoquinoline-3-carboxamide - 72760 3.4.23.16 (3R,4S,5S,6S)-2,7-dibenzyl-3,6-bis(phenoxymethyl)-1,2,7-thiadiazepane-4,5-diol 1,1-dioxide - 65176 3.4.23.16 (3R,6S,9S,10R,11R,12S,15S,18R)-3,9,12,18-tetrabenzyl-10,11-dihydroxy-4,7,14,17-tetraoxo-6,15-di(propan-2-yl)-5,8,13,16-tetraazaicosane-1,20-dioic acid - 79070 3.4.23.16 (3S)-tetrahydrofuran-3-yl [(2S,3R)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-1-phenylbutan-2-yl]carbamate - 79071 3.4.23.16 (3S)-tetrahydrofuran-3-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 79069 3.4.23.16 (3S,4aS,8aS)-2-((2R,3S)-4-(benzo[b]thiophen-2-yl)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)butyl)-N-tert-butyldecahydroisoquinoline-3-carboxamide - 78969 3.4.23.16 (3S,4aS,8aS)-N-tert-butyl-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-3-(4-phenylthiophen-2-yl)propyl)decahydroisoquinoline-3-carboxamide - 78899 3.4.23.16 (3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(4-phenylthiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide - 79073 3.4.23.16 (3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(thiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide - 79072 3.4.23.16 (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3S)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(thiophen-2-yl)butyl]decahydroisoquinoline-3-carboxamide - 78847 3.4.23.16 (3S,4S)-3-((benzyl[(2-bromo-4,5-dimethoxyphenyl)carbonyl]amino)methyl)-4-(([2-(2,4-dichlorophenyl)ethyl](4-phenylbutanoyl)amino)methyl)pyrrolidinium IC50 is 0.0198 mM, binding structure analysis, modelling 58317 3.4.23.16 (3S,4S)-3-((benzyl[(2-bromo-4,5-dimethoxyphenyl)carbonyl]amino)methyl)-4-(([2-(2,4-dichlorophenyl)ethyl][3-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)propanoyl]amino)methyl)pyrrolidinium IC50 is 0.0221 mM, binding structure analysis, modelling 58318 3.4.23.16 (4-[4-hydroxy-2-oxo-3-[(2-phenylethyl)sulfanyl]-2H-pyran-6-yl]phenoxy)acetic acid - 79066 3.4.23.16 (4aR,7aS)-octahydrocyclopenta[b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 86788 3.4.23.16 (4aS,7aR)-hexahydro-2H-furo[3,4-b]pyran-4-yl [(2S,3R)-3-hydroxy-4-{[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino}-1-phenylbutan-2-yl]carbamate - 41899 3.4.23.16 (4R)-3-[(2S,3S)-2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)carbonyl]amino]-4-phenylbutanoyl]-5,5-dimethyl-N-(2-methylbenzyl)-1,3-thiazolidine-4-carboxamide - 23887 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-L-prolinamide - 86769 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(2,5-dimethoxyphenyl)-L-prolinamide - 86776 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(2-methoxyphenyl)-L-prolinamide - 86774 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(3,4,5-trimethoxyphenyl)-L-prolinamide - 86777 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(3-methoxyphenyl)-L-prolinamide - 86775 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(4-methoxyphenyl)-L-prolinamide - 86772 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-(4-methylphenyl)-L-prolinamide - 86773 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-phenyl-L-prolinamide - 86771 3.4.23.16 (4R)-4-([[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl]oxy)-N-tert-butyl-L-prolinamide - 86770 3.4.23.16 (4R)-N-tert-butyl-3-[(2S,3S)-3-([(2,6-dimethylphenoxy)acetyl]amino)-2-hydroxy-4-phenylbutanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 65950 3.4.23.16 (4R,5S,6S,7S)-1,3-dibenzyl-5,6-dihydroxy-4,7-bis(phenoxymethyl)-1,3-diazepan-2-one - 65211 3.4.23.16 (5R)-1,3-dioxepan-5-yl [(2S,3S)-4-[(4R)-5,5-dimethyl-4-[(2-methylbenzyl)carbamoyl]-1,3-thiazolidin-3-yl]-3-hydroxy-4-oxo-1-phenylbutan-2-yl]carbamate - 79120 3.4.23.16 (5R)-4-hydroxy-5-(hydroxymethyl)-3-(13-methyltetradecanoyl)furan-2(5H)-one - 158900 3.4.23.16 (5R)-4-hydroxy-5-(hydroxymethyl)-3-(14-methylhexadecanoyl)furan-2(5H)-one - 158879 3.4.23.16 (5R)-4-hydroxy-5-(hydroxymethyl)-3-pentadecanoylfuran-2(5H)-one - 158898 3.4.23.16 (5R)-4-hydroxy-5-(hydroxymethyl)-3-tetradecanoylfuran-2(5H)-one - 158899 3.4.23.16 (5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41867 3.4.23.16 (5S)-3-(2,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 86782 3.4.23.16 (5S)-3-(3,4-difluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 86786 3.4.23.16 (5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 14963 3.4.23.16 (5S)-3-(3-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 86787 3.4.23.16 (5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 14964 3.4.23.16 (5S)-3-(3-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41883 3.4.23.16 (5S)-3-(3-aminophenyl)-N-[(1S,2R)-3-[(6-benzothiazolylsulfonyl)-(2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-2-oxooxazolidine-5-carboxamide - 41855 3.4.23.16 (5S)-3-(3-aminophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41889 3.4.23.16 (5S)-3-(3-aminophenyl)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41890 3.4.23.16 (5S)-3-(3-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 86785 3.4.23.16 (5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 14965 3.4.23.16 (5S)-3-(4-acetylphenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 86784 3.4.23.16 (5S)-3-(4-acetylphenyl)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41873 3.4.23.16 (5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41869 3.4.23.16 (5S)-3-(4-fluorophenyl)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41872 3.4.23.16 (5S)-3-[3-(acetylamino)phenyl]-N-[(1S,2R)-3-[(6-benzothiazolylsulfonyl)(2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-2-oxooxazolidine-5-carboxamide - 41856 3.4.23.16 (5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41891 3.4.23.16 (5S)-3-[3-(acetylamino)phenyl]-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41892 3.4.23.16 (5S)-N-[(1R,2S)-1-benzyl-3-[(4S)-7-fluoro-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]-2-hydroxypropyl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide - 167955 3.4.23.16 (5S)-N-[(1S,2R)-3-[(6-benzothiazolylsulfonyl)(2-methylpropyl)-amino]-2-hydroxy-1-((phenylmethyl)propyl)aminocarbonyl]-2-oxo-((3-oxazolidinyl)phenyl)carbamic acid methyl ester - 41857 3.4.23.16 (5S)-N-[(1S,2R)-3-[(6-benzothiazolylsulfonyl)(2-methylpropyl)-amino]-2-hydroxy-1-(phenylmethyl)propyl]-3-(3-nitrophenyl)-2-oxooxazolidine-5-carboxamide - 41854 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41863 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide - 41879 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 14966 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41861 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41887 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41884 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide - 86778 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41866 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide - 41882 3.4.23.16 (5S)-N-[(2S,3R)-3-hydroxy-4-[[[4-(hydroxymethyl)phenyl]sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41877 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide - 41858 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41864 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide - 41880 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 14962 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 86781 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 86779 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-nitrophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41888 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41870 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41885 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-phenyl-1,3-oxazolidine-5-carboxamide - 41859 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41865 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide - 41881 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41876 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41868 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41875 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(3-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41874 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41871 3.4.23.16 (5S)-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-[3-(methylsulfonyl)phenyl]-2-oxo-1,3-oxazolidine-5-carboxamide - 41886 3.4.23.16 (5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[2-(trifluoromethyl)phenyl]-1,3-oxazolidine-5-carboxamide - 41862 3.4.23.16 (5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-2-oxo-3-[3-(trifluoromethoxy)phenyl]-1,3-oxazolidine-5-carboxamide - 41878 3.4.23.16 (5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2,4-difluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 86780 3.4.23.16 (5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(2-hydroxyphenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 41860 3.4.23.16 (5S)-N-[(2S,3R)-4-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-(4-fluorophenyl)-2-oxo-1,3-oxazolidine-5-carboxamide - 86783 3.4.23.16 (5S,8S,11S,12R,13R,14S,17S)-11,14-dibenzyl-17-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-8-(2-carboxyethyl)-12,13-dihydroxy-2,2-dimethyl-5-(naphthalen-1-ylmethyl)-6,9,16-trioxo-3l6-thia-7,10,15-triazaicosan-20-oic acid 3,3-dioxide - 79134 3.4.23.16 (6R)-4-hydroxy-3-[[5-methyl-2-(propan-2-yl)phenyl]sulfanyl]-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 40256 3.4.23.16 (6S)-4-hydroxy-3-[[5-methyl-2-(propan-2-yl)phenyl]sulfanyl]-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 79135 3.4.23.16 (hydroxyethyl)amide isostere - 58735 3.4.23.16 (R)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea - 40253 3.4.23.16 (R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3,4-methylenedioxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66593 3.4.23.16 (R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66591 3.4.23.16 (R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66592 3.4.23.16 (R)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66590 3.4.23.16 (R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3,4-methylenedioxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66589 3.4.23.16 (R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66587 3.4.23.16 (R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66588 3.4.23.16 (R)-N-(2-methylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)butanoyl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide - 66586 3.4.23.16 (R)-N1-((1R,2R)-3-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2-(1H)-yl)-2-hydroxy-1-(4-phenylthiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide - 79183 3.4.23.16 (R)-N1-((2S,3R)-1-(benzo[b]thiophen-2-yl)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxybutan-2-yl)-2-(quinoline-2-carboxamido)succinamide - 79105 3.4.23.16 (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-2-hydroxy-1-(thiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide - 79103 3.4.23.16 (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(4-phenylthiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide - 79104 3.4.23.16 (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(thiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide - 79102 3.4.23.16 (S)-1-benzyl-3-(1-benzyl-2-oxo-ethyl)-1-piperidin-1-yl-urea - 40254 3.4.23.16 (S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(3-methoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide - 66595 3.4.23.16 (S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-ethoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide - 66596 3.4.23.16 (S)-N-(2,6-dimethylbenzyl)-3-[(2S,3S)-2-hydroxy-3-(3-amino-2-chlorobenzoyl)amino-4-(4-methoxyphenyl)-butanoyl]-3,3-dimethylpyrrolidine-2-carboxamide - 66594 3.4.23.16 (S,2S,2'S,3R,3'R)-N,N'-((2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl)bis(2-((S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanamido)-3-hydroxybutanamide) - 79291 3.4.23.16 (S,2S,2'S,3R,3'R)-N,N'-((2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl)bis(2-((S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanamido)-3-methylpentanamide) - 79106 3.4.23.16 (S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid tert-butylamide - 40279 3.4.23.16 (S,S,S,S)-1-[1-benzyl-3-(1-benzyl-2-oxo-ethyl)-ureido]-pyrrolidine-2-carboxylic acid [1-(1-tert-butylcarbamoyl-2-methyl-propylcarbamoyl)-2-methyl-butyl]-amide - 40252 3.4.23.16 1,3,4,7-tetrabenzyl-5,6-dihydroxy-1,3-diazepan-2-one - 79267 3.4.23.16 1-(4-Chloro-phenyl)-propane-1,2-dione 1-oxime slightly inhibitory 114576 3.4.23.16 1-(benzyl[[(2S)-1-oxo-3-phenylpropan-2-yl]carbamoyl]amino)-L-prolyl-N-tert-butyl-L-valinamide - 40263 3.4.23.16 1-Chloro-3-(4-chloro-phenyl)-propan-2-one slightly inhibitory 114575 3.4.23.16 1-[(1S)-2-methyl-1-[1-[(1S)-1-[1-[(1S)-1-[1-[(1S)-2-methyl-1-[1-[(1R)-1-phenylethyl]-1H-1,2,3-triazol-4-yl]propyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]-2-phenylethyl]-1H-1,2,3-triazol-4-yl]propyl]-4-(2-phenylethyl)-1H-1,2,3-triazole - 79268 3.4.23.16 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-L-prolyl-N-tert-butyl-L-valinamide - 40271 3.4.23.16 1-[(3R)-3-benzyl-3-([N-[(benzyloxy)carbonyl]-L-valyl]amino)-4-oxobutyl]-N-tert-butyl-L-prolinamide - 40241 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-4-(4-oxo-4H-chromene-2-carbonyl)-piperazine-2-carboxylic acid tert-butylamide IC50: 0.13 nM 51069 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-4-(naphthalen-2-yloxy)-pyrrolidine-2-carboxylic acid tert-butylamide IC50: 18 nM 51066 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-4-(quinoline-8-sulfonyl)-piperazine-2-carboxylic acid tert-butylamide IC50: 0.03 nM 51070 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-4-pyridin-3-ylmethyl-piperazine-2-carboxylic acid tert-butylamide IC50: 0.41 nM 51072 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-piperazine-2-carboxylic acid tert-butylamide IC50: 38 nM 51068 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-piperidine-2-carboxylic acid tert-butylamide IC50: 80 nM 51067 3.4.23.16 1-[2-Hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-pyrrolidine-2-carboxylic acid tert-butylamide IC50: 350 nM 51065 3.4.23.16 2'-([4-[3-(4-bromophenyl)propanoyl]phenyl]acetyl)biphenyl-2-carboxylic acid - 79218 3.4.23.16 2,3,4,5,5-pentahydroxy-N-[(2S,5S,8S,9R,10R,11S,14S,17S)-8,11,17-tribenzyl-9,10,20,21,22,23,23-heptahydroxy-3,6,13,16,19-pentaoxo-1-phenyl-5,14-di(propan-2-yl)-4,7,12,15,18-pentaazatricosan-2-yl]pentanamide - 79307 3.4.23.16 2,5-bis[[(2S)-2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-2-cyclohexylacetyl]amino]-1,2,5,6-tetradeoxy-1,6-diphenyl-L-iditol - 79204 3.4.23.16 2,5-bis[[(2S)-2-[[(2S)-3-(tert-butylsulfonyl)-2-(naphthalen-1-ylmethyl)propanoyl]amino]-2-cyclopentylacetyl]amino]-1,2,5,6-tetradeoxy-1,6-diphenyl-L-iditol - 78846 3.4.23.16 2,6-dimethylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 25 nM 52195 3.4.23.16 2,6-dimethylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 28 nM 52196 3.4.23.16 2-(2,5-dichlorobenzoyl)-4,5-dihydroxybenzoic acid - 79220 3.4.23.16 2-(2-{5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-2,6-diphenyl-hexanoylamino}-3-methyl-butyrylamino)-3-methyl-butyric acid methyl ester - 114807 3.4.23.16 2-(2-{5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-2-methyl-6-phenyl-hexanoylamino}-3-methyl-butyrylamino)-3-methyl-butyric acid methyl ester - 114808 3.4.23.16 2-(2-{5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-6-phenyl-2-propyl-hexanoylamino}-3-methyl-butyrylamino)-3-methyl-butyric acid methyl ester - 114809 3.4.23.16 2-(2-{5-[2-(2-amino-propionylamino)-propionylamino]-4-hydroxy-6-phenyl-hexanoylamino}-3-methyl-butyrylamino)-3-methyl-butyric acid methyl ester - 114810 3.4.23.16 2-(3,4-dihydroxy-5-oxo-2,5-dihydrofuran-2-yl)-2-hydroxyethyl 5-cyclohexylpentanoate - 79203 3.4.23.16 2-(4-chlorophenyl)-7-hydroxyquinoline-4-carboxylic acid - 79206 3.4.23.16 2-hydroxy-6-pentadecylbenzoic acid isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 18770 3.4.23.16 2-hydroxy-6-[(8Z)-pentadec-8-en-1-yl]benzoic acid isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 18769 3.4.23.16 2-hydroxyphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-2-hydroxyphenoxyacetyl IC50: 0.009 mM 52216 3.4.23.16 2-hydroxyphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-2-hydroxyphenoxyacetyl IC50: 0.007 mM 52217 3.4.23.16 2-O-acetyldryopteric acid A inhibitor isolated from Dryopteris crassirhizoma 73056 3.4.23.16 2-O-acetyldryopteric acid B inhibitor isolated from Dryopteris crassirhizoma 73057 3.4.23.16 2-[(10Z)-heptadec-10-en-1-yl]-6-hydroxybenzoic acid isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 18768 3.4.23.16 3,3,3-Tribromo-1-(2-methoxy-phenyl)-propane-1,2-dione 1-oxime highly inhibitory 114573 3.4.23.16 3,3-Dibromo-1-phenyl-propane-1,2-dione 1-oxime highly inhibitory 114574 3.4.23.16 3,4-dihydroxy-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]benzamide - 19218 3.4.23.16 3-(2,5-diethoxyphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one most potent inhibitor 86752 3.4.23.16 3-(2,5-diethoxyphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86759 3.4.23.16 3-(2,5-diethoxyphenylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86745 3.4.23.16 3-(2,5-dimethylphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one - 86751 3.4.23.16 3-(2,5-dimethylphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86758 3.4.23.16 3-(2,5-dimethylphenylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86744 3.4.23.16 3-(2-chlorophenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one - 86750 3.4.23.16 3-(2-chlorophenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86757 3.4.23.16 3-(2-chlorophenylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86743 3.4.23.16 3-(2-ethylphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one - 86749 3.4.23.16 3-(2-ethylphenylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86756 3.4.23.16 3-(2-ethylphenylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86742 3.4.23.16 3-(4,8-dimethyl-3,7-nonadienyl)-(5R)-(2,5-dihydroxyphenyl)-2(5H)-furanone ganomycin I 81385 3.4.23.16 3-(benzylsulfanyl)-4-hydroxy-6,6-diphenyl-5,6-dihydro-2H-pyran-2-one - 79239 3.4.23.16 3-(benzylsulfanyl)-4-hydroxy-6-phenyl-2H-pyran-2-one - 79240 3.4.23.16 3-(benzylsulfanyl)-4-hydroxy-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 79241 3.4.23.16 3-(benzylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one - 86753 3.4.23.16 3-(benzylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86760 3.4.23.16 3-(benzylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86746 3.4.23.16 3-(o-tolylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenylpyran-2-one - 86748 3.4.23.16 3-(o-tolylthio)-5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenylpyran-2-one - 86755 3.4.23.16 3-(o-tolylthio)-5,6-dihydro-4-hydroxy-6-phenyl-6-((phenylthio)methyl)pyran-2-one - 86741 3.4.23.16 3-benzyl-4-hydroxy-2H-chromen-2-one - 19213 3.4.23.16 3-Chloro-1-(4-chloro-phenyl)-propane-1,2-dione 1-oxime highly inhibitory 114572 3.4.23.16 3-fluoro-N-[(2S,3R)-3-hydroxy-4-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]-1-phenylbutan-2-yl]-2-methylbenzamide - 19209 3.4.23.16 3-pentadecylphenol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 38124 3.4.23.16 3-tert-Butylcarbamoyl-4-[2-hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-piperazine-1-carboxylic acid benzyl ester 0.35-0.37 nM 111923 3.4.23.16 3-tridecylphenol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 38125 3.4.23.16 3-[(10Z)-heptadec-10-en-1-yl]phenol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 38120 3.4.23.16 3-[(2-tert-butyl-5-methylphenyl)sulfanyl]-4-hydroxy-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 79236 3.4.23.16 3-[(2-tert-butylphenyl)sulfanyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 79237 3.4.23.16 3-[(2-tert-butylphenyl)sulfanyl]-4-hydroxy-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 79308 3.4.23.16 3-[(8Z)-pentadec-8-en-1-yl]phenol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 38121 3.4.23.16 3-[(benzylsulfanyl)(phenyl)methyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78849 3.4.23.16 3-[1-(benzylsulfanyl)-2-cyclopropylethyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78863 3.4.23.16 3-[1-(benzylsulfanyl)-3-methylbutyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78867 3.4.23.16 3-[1-(cyclohexylsulfanyl)-2-cyclopropylethyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 79009 3.4.23.16 3-[1-(cyclopentylsulfanyl)-2-cyclopropylethyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78864 3.4.23.16 3-[1-(cyclopentylsulfanyl)-3-methylbutyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78865 3.4.23.16 3-[cyclopentyl(cyclopentylsulfanyl)methyl]-4-hydroxy-6-phenyl-2H-pyran-2-one - 78873 3.4.23.16 4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis(benzylsulfamoyl)]dibenzamide - 26132 3.4.23.16 4,4'-[(3S,4S)-pyrrolidine-3,4-diylbis[[4-(trifluoromethyl)benzyl]sulfamoyl]]dibenzamide - 26133 3.4.23.16 4,5-anhydro-1,2,6-trideoxy-2-[[N-(phenoxyacetyl)-L-valyl]amino]-1,6-diphenyl-D-galactitol - 235175 3.4.23.16 4,7-dibenzyl-1,3-bis(2-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78915 3.4.23.16 4,7-dibenzyl-1,3-bis(2-ethoxyethyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78936 3.4.23.16 4,7-dibenzyl-1,3-bis(2-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 79162 3.4.23.16 4,7-dibenzyl-1,3-bis(3,3-dimethylbutyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78935 3.4.23.16 4,7-dibenzyl-1,3-bis(3-bromobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78937 3.4.23.16 4,7-dibenzyl-1,3-bis(3-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 79022 3.4.23.16 4,7-dibenzyl-1,3-bis(3-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78998 3.4.23.16 4,7-dibenzyl-1,3-bis(4-bromobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78939 3.4.23.16 4,7-dibenzyl-1,3-bis(4-chlorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78928 3.4.23.16 4,7-dibenzyl-1,3-bis(4-fluorobenzyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78927 3.4.23.16 4,7-dibenzyl-1,3-bis(cyclobutylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78955 3.4.23.16 4,7-dibenzyl-1,3-bis(cyclohexylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78931 3.4.23.16 4,7-dibenzyl-1,3-bis(cyclopentylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78933 3.4.23.16 4,7-dibenzyl-1,3-bis(cyclopropylmethyl)-5,6-dihydroxy-1,3-diazepan-2-one - 78884 3.4.23.16 4,7-dibenzyl-1,3-bis[2-(ethenyloxy)ethyl]-5,6-dihydroxy-1,3-diazepan-2-one - 78909 3.4.23.16 4,7-dibenzyl-1,3-dibutyl-5,6-dihydroxy-1,3-diazepan-2-one - 78890 3.4.23.16 4,7-dibenzyl-1,3-diethyl-5,6-dihydroxy-1,3-diazepan-2-one - 78886 3.4.23.16 4,7-dibenzyl-1,3-diheptyl-5,6-dihydroxy-1,3-diazepan-2-one - 78923 3.4.23.16 4,7-dibenzyl-1,3-dihexyl-5,6-dihydroxy-1,3-diazepan-2-one - 78880 3.4.23.16 4,7-dibenzyl-1-decyl-5,6-dihydroxy-3-nonyl-1,3-diazepan-2-one - 78877 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methoxybenzyl)-1,3-diazepan-2-one - 78878 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methoxyethyl)-1,3-diazepan-2-one - 78874 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methylprop-2-en-1-yl)-1,3-diazepan-2-one - 78959 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(2-methylpropyl)-1,3-diazepan-2-one - 78820 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-hydroxybenzyl)-1,3-diazepan-2-one - 78876 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-iodobenzyl)-1,3-diazepan-2-one - 78891 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methoxybenzyl)-1,3-diazepan-2-one - 78870 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbenzyl)-1,3-diazepan-2-one - 78911 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbut-2-en-1-yl)-1,3-diazepan-2-one - 78894 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-methylbutyl)-1,3-diazepan-2-one - 78898 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(3-nitrobenzyl)-1,3-diazepan-2-one - 79252 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-hydroxybenzyl)-1,3-diazepan-2-one - 78904 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methoxybenzyl)-1,3-diazepan-2-one - 78901 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methylbenzyl)-1,3-diazepan-2-one - 78900 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(4-methylpentyl)-1,3-diazepan-2-one - 79096 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(5-methylhexyl)-1,3-diazepan-2-one - 78843 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(naphthalen-1-ylmethyl)-1,3-diazepan-2-one - 78893 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(naphthalen-2-ylmethyl)-1,3-diazepan-2-one - 78892 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-2-ylmethyl)-1,3-diazepan-2-one - 42970 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-3-ylmethyl)-1,3-diazepan-2-one - 78896 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis(pyridin-4-ylmethyl)-1,3-diazepan-2-one - 78895 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[2-(2-methoxyethoxy)ethyl]-1,3-diazepan-2-one - 78910 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[2-(morpholin-4-yl)ethyl]-1,3-diazepan-2-one - 79196 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[3-(hydroxymethyl)benzyl]-1,3-diazepan-2-one - 78913 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[3-(trifluoromethyl)benzyl]-1,3-diazepan-2-one - 78912 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(hydroxymethyl)benzyl]-1,3-diazepan-2-one DMP323; enantiomer of DMP323 27268 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-bis[4-(trifluoromethyl)benzyl]-1,3-diazepan-2-one - 79141 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-di(prop-2-en-1-yl)-1,3-diazepan-2-one - 78907 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-di(prop-2-yn-1-yl)-1,3-diazepan-2-one - 78906 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-dimethyl-1,3-diazepan-2-one - 78905 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-dipentyl-1,3-diazepan-2-one - 79048 3.4.23.16 4,7-dibenzyl-5,6-dihydroxy-1,3-dipropyl-1,3-diazepan-2-one - 78908 3.4.23.16 4,7-dihydroxy-3-[4-(2-methoxyphenyl)butyl]-2H-chromen-2-one - 79059 3.4.23.16 4-acetylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.023 mM 52249 3.4.23.16 4-acetylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.019 mM 52250 3.4.23.16 4-amino-N-[(2R,3S)-3-{[(aminooxy)carbonyl]amino}-2-hydroxy-4-phenylbutyl]-N-{[(2S)-5-oxopyrrolidin-2-yl]methyl}benzenesulfonamide - 78960 3.4.23.16 4-Benzyl-1-[2-hydroxy-4-(2-hydroxy-indan-1-ylcarbamoyl)-5-phenyl-pentyl]-piperazine-2-carboxylic acid tert-butylamide IC50: 2.0 mM 51071 3.4.23.16 4-formylphenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.08 mM 52256 3.4.23.16 4-formylphenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-4-acetylphenoxyacetyl IC50: 0.068 mM 52257 3.4.23.16 4-hydroxy-3-(3-oxo-1-phenylbutyl)-2H-chromen-2-one - 78827 3.4.23.16 4-hydroxy-3-(3-phenoxypropyl)-2H-chromen-2-one - 79207 3.4.23.16 4-hydroxy-3-(4-phenylbutyl)-2H-chromen-2-one - 78837 3.4.23.16 4-hydroxy-3-[(2-methylphenyl)sulfanyl]-6-phenyl-2H-pyran-2-one - 79092 3.4.23.16 4-hydroxy-3-[(2-methylphenyl)sulfanyl]-6-phenyl-6-(2-phenylethyl)-5,6-dihydro-2H-pyran-2-one - 78836 3.4.23.16 4-hydroxy-3-[3-(phenylsulfanyl)propyl]-2H-chromen-2-one - 79260 3.4.23.16 4-hydroxy-3-[3-methyl-1-(phenylsulfanyl)butyl]-6-phenyl-2H-pyran-2-one - 78839 3.4.23.16 4-hydroxy-3-[4-(2-methoxyphenyl)butyl]-2H-chromen-2-one - 78838 3.4.23.16 4-hydroxy-6-(3-methylbutyl)-6-phenyl-3-[(2-phenylethyl)sulfanyl]-5,6-dihydro-2H-pyran-2-one - 79019 3.4.23.16 4-hydroxy-6-(3-methylphenyl)-3-[[2-(propan-2-yl)phenyl]sulfanyl]-2H-pyran-2-one - 79226 3.4.23.16 4-hydroxy-6-(4-hydroxyphenyl)-3-[(2-phenylethyl)sulfanyl]-2H-pyran-2-one - 79178 3.4.23.16 4-hydroxy-6-pentyl-6-phenyl-3-[(2-phenylethyl)sulfanyl]-5,6-dihydro-2H-pyran-2-one - 78835 3.4.23.16 4-hydroxy-6-phenyl-3-(phenylsulfanyl)-2H-pyran-2-one - 78834 3.4.23.16 4-hydroxy-6-phenyl-3-[(2-phenylethyl)sulfanyl]-2H-pyran-2-one - 79091 3.4.23.16 4-hydroxy-6-phenyl-3-[(2-phenylethyl)sulfanyl]-5,6-dihydro-2H-pyran-2-one - 78825 3.4.23.16 4-hydroxy-6-phenyl-3-[(2-phenylethyl)sulfanyl]-6-propyl-5,6-dihydro-2H-pyran-2-one - 42971 3.4.23.16 4-hydroxy-6-phenyl-3-[phenyl(phenylsulfanyl)methyl]-2H-pyran-2-one - 78879 3.4.23.16 4-hydroxy-6-phenyl-3-[[2-(propan-2-yl)phenyl]sulfanyl]-2H-pyran-2-one - 79130 3.4.23.16 4-hydroxy-6-phenyl-6-(2-phenylethyl)-3-(phenylsulfanyl)-5,6-dihydro-2H-pyran-2-one - 42972 3.4.23.16 4-hydroxy-6-phenyl-6-(2-phenylethyl)-3-[[2-(propan-2-yl)phenyl]sulfanyl]-5,6-dihydro-2H-pyran-2-one - 79078 3.4.23.16 4-hydroxy-7,8-dimethyl-3-(3-oxo-1-phenylbutyl)-2H-chromen-2-one - 42968 3.4.23.16 4-oxo-4H-chromene-2-carboxylic acid (1-{1-benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propylcarbamoyl}-2-methyl-propyl)-amide IC50: 0.1 nM 52274 3.4.23.16 4-[[(6-[[(4-aminothiophen-2-yl)carbonyl]amino]-1,3-benzoxazol-2-yl)carbonyl]amino]thiophene-2-carboxylic acid non-competitive 78917 3.4.23.16 5,5'-dithiobis(2-nitrobenzoic acid) enzyme activity is lost when a mixed disulfide is formed between 5,5'-dithiobis(2-nitrobenzoic acid) and Cys95, the same mixed disulfide at Cys67 reduces activity by 50%. Normal activity can be restored when the enzyme is treated with dithiothreitol 221 3.4.23.16 5,6-dihydro-4-hydroxy-6-((naphthalen-1-yloxy)methyl)-6-phenyl-3-(phenylthio)pyran-2-one - 86747 3.4.23.16 5,6-dihydro-4-hydroxy-6-((naphthalen-2-yloxy)methyl)-6-phenyl-3-(phenylthio)pyran-2-one - 86754 3.4.23.16 5,6-dihydro-4-hydroxy-6-phenyl-3-(phenylthio)-6-((phenylthio)methyl)pyran-2-one - 86740 3.4.23.16 5-(3-chlorobenzyl)-1,2-dihydro-3H-pyrazol-3-one - 78821 3.4.23.16 5-tridecylbenzene-1,3-diol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 25765 3.4.23.16 5-[(8Z)-pentadec-8-en-1-yl]benzene-1,3-diol isolated from the CH2Cl2 extracts of the sacrotestas of Ginkgo biloba 25764 3.4.23.16 5-[4-hydroxy-6-oxo-2-phenyl-5-[(2-phenylethyl)sulfanyl]-3,6-dihydro-2H-pyran-2-yl]pentanoic acid - 78991 3.4.23.16 A-790742 50% effective concentration ranges from 2 to 7 nM against wild-type HIV-1. The activity is lowered by approximately 7fold in the presence of 50% human serum. A-790742 maintains potent antiviral activity against lopinavir-resistant variants generated in vitro as well as against a panel of molecular clones containing proteases derived from HIV-1 patient isolates with multiple protease mutations. HIV-1 pNL4-3 clones with a single V82L or I84V mutation are phenotypically resistant to A-790742 and ritonavir 150616 3.4.23.16 A74704 - 115094 3.4.23.16 A79285 a pseudo-C2 symmetric inhibitor, which contains a central difluoroketone motif 115095 3.4.23.16 Ac-His-Gly-Trp-Ile-PSI[N-CH(CH2(CH3)2)-CH(OH)-CH2-CH2-C(O)]-Glu-His-Gly-Asp-NH2 - 51056 3.4.23.16 Ac-HMSFNL IC50: 0.19 mM 52308 3.4.23.16 Ac-HMTLNF - 115111 3.4.23.16 Ac-HTLNF - 115112 3.4.23.16 Ac-IGLTLNF - 115113 3.4.23.16 Ac-LTLNF - 115115 3.4.23.16 Ac-QIGMTLNF IC50: 0.44 mM 52314 3.4.23.16 Ac-RASQNY product inhibition with Ac-SQNYPVV as substrate 52315 3.4.23.16 Ac-RKIL product inhibition with Ac-RKILFLDG-NH2 as substrate 52317 3.4.23.16 Ac-SQNY product inhibition with Ac-RASQNYPVV or Ac-SQNYFLDG-NH2 as substrate 16995 3.4.23.16 Ac-TI-Nle-(CH2-NH)-Nle-QR-amide - 115122 3.4.23.16 Ac-TLNF IC50: 1.5 mM 52325 3.4.23.16 Ac-TLNF-NH2 IC50 is above 2 mM 52326 3.4.23.16 Ac-TVSFNF IC50: 0.08 mM 52327 3.4.23.16 Ace-T-I-Nle-r-Nle-Q-R substrate analogue, competitive inhibition of the HIV-1 protease, mimicks the p2-NC cleavage site 8630 3.4.23.16 Ace-T-I-Nle-r-Nle-Q-R substrate analogue peptide inhibitor 8630 3.4.23.16 Ace-TINlerNleQR - 239921 3.4.23.16 acetyl pepstatin 0.1 mg/ml, 98.5% inhibition 66597 3.4.23.16 acetyl pepstatin study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is most sensitive to mutantion D25N, with DeltaTm ratio for mutant/wild-type of 16.3. Binding is nearly abolished by the mutation D29N 66597 3.4.23.16 acetyl-pepstatin - 6778 3.4.23.16 AG1776 - 7656 3.4.23.16 allyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate - 86733 3.4.23.16 alpha2-Macroglobulin activity with Moloney murrine sarcoma virus-derived gag protein is inhibited at pH 5.5-7.4, activity with B chain of oxidized insulin is scarcely inhibited 1068 3.4.23.16 amprenavir - 1608 3.4.23.16 amprenavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is most sensitive to mutantion D25N, with DeltaTm ratio for mutant/wild-type of 35.8 1608 3.4.23.16 amprenavir less effective on HIV-2 protease than on HIV-1 protease 1608 3.4.23.16 Arg-Arg with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 5521 3.4.23.16 Arg-Arg-Leu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115277 3.4.23.16 Arg-Arg-Phe with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115278 3.4.23.16 Arg-Glu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 16842 3.4.23.16 Arg-Glu-Asp with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52405 3.4.23.16 Arg-Glu-Leu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115280 3.4.23.16 Arg-Leu-Ala-Phe with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115284 3.4.23.16 Arg-Leu-Asn-Phe IC50: 0.87 mM 52407 3.4.23.16 Asp-Asp - 30662 3.4.23.16 Asp-Asp-Leu - 52410 3.4.23.16 Asp-Asp-Phe - 52411 3.4.23.16 Asp-Glu-Leu - 52412 3.4.23.16 Asp-Leu-Ala-Phe - 52414 3.4.23.16 atazanavir - 2379 3.4.23.16 atazanavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 2379 3.4.23.16 atazanavir study on the use of suboptimal concentrations of inhibitors atazanavir and lopinavir. Even with high levels of inhibition of viral infectivity, IC90, most of the Gag and Gag-Pol polyproteins are processed, although slight but significant increases in processing intermediates of Gag Are detected. Drug treatments cause a significant increase in the proportion of viruses displaying either immature or aberrant mature morphologies. The aberrant mature particles are characterized by an electron-dense region at the viral periphery and an electron-lucent core structure in the viral center. Drug treatments cause only a slight decrease in overall thermodynamic stability of the viral RNA dimer 2379 3.4.23.16 ATBI aspartic protease inhibitor: Ala-Gly-Lys-Lys-Asp-Asp-Asp-Asp-Pro-Pro-Glu, from Bacillus sp. 19235 3.4.23.16 BEA369 molecular dynamics simulation study on the role of protonation in the protease complex with inhibitor BEA369. Protonation of aspartic acids Asp25/Asp25' has a strong influence on the dynamics behavior of the complex, the binding free energy of BEA369, and inhibitor-residue interactions. Relative binding free energies show that protonation of Asp25 results in the strongest binding of BEA369 to HIV-1 protease. Inhibitor-residue interactions indicate that protonation of Asp25 has the most favorable effect on binding of BEA369. Protonation of Asp25 strongly influences the water-mediated link of a conserved water molecule, Wat301 151752 3.4.23.16 benzyl [(5S,8S,9R,10R,11S,14S)-8,11-dibenzyl-9,10-dihydroxy-15-methyl-3,6,13-trioxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,12-triazahexadecan-14-yl]carbamate - 79125 3.4.23.16 bis-[(L-valine-N-methylamide)-2-phenyl-3-yl-propionamide] sulfide - 81395 3.4.23.16 bis-[(L-valine-N-methylamide)-2-phenyl-3-yl-propionamide] sulfoxide - 81396 3.4.23.16 bis-[(L-valine-N-methylamide)-2-phenyl-3-yl-propionamide] sulfoximine - 81397 3.4.23.16 bis-[[N-(1S,2R)-2,3-dihydro-2-hydroxy-1H-inden-1-yl]-2S-phenyl-3-yl-propionamide] sulfoximine - 81398 3.4.23.16 bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfide - 81389 3.4.23.16 bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoxide - 81391 3.4.23.16 bis-[[N-(2R)-phenylglycinol]-2-phenyl-3-yl-propionamide]sulfoximine - 81393 3.4.23.16 bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfide - 81390 3.4.23.16 bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoxide - 81392 3.4.23.16 bis-[[N-(2S)-phenylglycinol]-2-phenyl-3-yl-propionamide] sulfoximine - 81394 3.4.23.16 compound J - 66585 3.4.23.16 darunavir - 1901 3.4.23.16 darunavir mutations in the gag region NC-p1/TFP-p6/p6pol may influence the selection of darunavir resistance mutations. The I437T/V gag mutation that confers resistance to protease inhibitors reduces the selection of such mutations. Virus with L76V in protease or I437T/V in gag may be already resistant to darunavir 1901 3.4.23.16 darunavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 1901 3.4.23.16 darunavir TMC-114 1901 3.4.23.16 DMP128 - 160171 3.4.23.16 DMP323 - 13449 3.4.23.16 dryopteric acid A inhibitor isolated from Dryopteris crassirhizoma 73481 3.4.23.16 dryopteric acid B inhibitor isolated from Dryopteris crassirhizoma 73482 3.4.23.16 E-R-Q-A-N-r-F-L-G-K-I substrate analogue, competitive inhibition of the HIV-1 protease, mimicks the NC/p1 cleavage site 58736 3.4.23.16 ethyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate - 86734 3.4.23.16 FLREDLAF with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52544 3.4.23.16 fosamprenavir - 167956 3.4.23.16 fullerene C60 „Bucky Ball" 115686 3.4.23.16 GADIFYLDGA - 139125 3.4.23.16 GAEVFYVDGA - 139126 3.4.23.16 ganomycin B competitive inhibition 34514 3.4.23.16 GAQTFYVDGA - 139127 3.4.23.16 GEDLAF with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52553 3.4.23.16 Glu-Arg-Leu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115730 3.4.23.16 Glu-Arg-Leu-Ala with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115731 3.4.23.16 Glu-Arg-Phe with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 115732 3.4.23.16 Glu-Asn-Leu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52558 3.4.23.16 Glu-Asp-Leu - 52559 3.4.23.16 Glu-Asp-Leu-Ala - 52560 3.4.23.16 Glu-Asp-Phe - 52561 3.4.23.16 Glu-Glu-Leu with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52562 3.4.23.16 Glu-Lys-Phe with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52563 3.4.23.16 GRL-06579A - 137309 3.4.23.16 GRL-98065 I50V, V82A and I84V mutant proteins show high levels of resistence 101734 3.4.23.16 IGRNLLTQIGCTLNF IC50: 0.41 mM 52596 3.4.23.16 indinavir IC50: 1.3 nM 1036 3.4.23.16 indinavir - 1036 3.4.23.16 indinavir drug used in AIDS therapy, mechanism of drug resistance, overview 1036 3.4.23.16 indinavir structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases 1036 3.4.23.16 indinavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 1036 3.4.23.16 indinavir 98.8% inhibition at 10 nM 1036 3.4.23.16 JG-365 - 52609 3.4.23.16 JG365 - 32984 3.4.23.16 JG365 9 nM 32984 3.4.23.16 KNI-272 - 35418 3.4.23.16 KNI-272 transition-state analog 35418 3.4.23.16 KNI-279 - 129556 3.4.23.16 KNI-727 potent, small, water-soluble dipeptide-type HIV-1 protease inhibitor 33449 3.4.23.16 KVS-1 - 81384 3.4.23.16 Kyn-(D-alpha-(2-thienyl)glycine)-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM 52629 3.4.23.16 Kyn-Thr-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 4 nM 52630 3.4.23.16 Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM 52631 3.4.23.16 Kyn-Val-Phe-PSI(S,R,S)[OH]-Phe-Val-Kyn IC50: 4 nM 52632 3.4.23.16 Kyn-Val-Phe-PSI(S,S,S)[OH]-Phe-2,6-dimethylphenoxyacetyl IC50: 3 nM 52633 3.4.23.16 L-700,417 IC50: 0.67 mM 51054 3.4.23.16 L-704,486 IC50: 7.8 nM 51064 3.4.23.16 Leu-Leu-Glu-Tyr-Val-Met-OH 0.1 mg/ml, 47.2% inhibition 139129 3.4.23.16 Leu-Leu-Glu-Tyr-Val-Phe-OH 0.1 mg/ml, 52.3% inhibition 139128 3.4.23.16 Leu-Leu-Glu-Tyr-Val-Trp-OH 0.1 mg/ml, 64.9% inhibition 139131 3.4.23.16 Leu-Leu-Glu-Tyr-Val-Tyr-OH 0.1 mg/ml, 58.6% inhibition 139130 3.4.23.16 lopinavir - 1430 3.4.23.16 lopinavir computer simulation of comlex with HIV-1 protease 1430 3.4.23.16 lopinavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 1430 3.4.23.16 lopinavir study on the use of suboptimal concentrations of inhibitors atazanavir and lopinavir. Even with high levels of inhibition of viral infectivity, IC90, most of the Gag and Gag-Pol polyproteins are processed, although slight but significant increases in processing intermediates of Gag Are detected. Drug treatments cause a significant increase in the proportion of viruses displaying either immature or aberrant mature morphologies. The aberrant mature particles are characterized by an electron-dense region at the viral periphery and an electron-lucent core structure in the viral center. Drug treatments cause only a slight decrease in overall thermodynamic stability of the viral RNA dimer 1430 3.4.23.16 LTLNF - 115982 3.4.23.16 lysyl-tRNA synthetase - 129554 3.4.23.16 manassantin A - 81387 3.4.23.16 methyl (7S,10R,16S)-10-benzyl-13-(4-bromobenzyl)-10-hydroxy-7-isopropyl-17,17-dimethyl-6,9,15-trioxo-2-oxa-5,8,13,14-tetraazaoctadecan-16-ylcarbamate - 79110 3.4.23.16 methyl (7S,10S,16S)-10-benzyl-13-(4-bromobenzyl)-10-hydroxy-7-isopropyl-17,17-dimethyl-6,9,15-trioxo-2-oxa-5,8,13,14-tetraazaoctadecan-16-ylcarbamate - 78961 3.4.23.16 methyl (S)-1-(2-((R)-3-benzyl-3-hydroxy-4-((S)-3-methyl-1-(methylamino)-1-oxobutan-2-ylamino)-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79033 3.4.23.16 methyl (S)-1-(2-((R)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79275 3.4.23.16 methyl (S)-1-(2-((S)-3-benzyl-3-hydroxy-4-((S)-3-methyl-1-(methylamino)-1-oxobutan-2-ylamino)-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79031 3.4.23.16 methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79032 3.4.23.16 methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-3-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79037 3.4.23.16 methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-(pyridin-4-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79298 3.4.23.16 methyl (S)-1-(2-((S)-3-benzyl-4-((S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-ylamino)-3-hydroxy-4-oxobutyl)-2-(4-bromobenzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate - 79286 3.4.23.16 methyl 4-[([6-[([4-[(tert-butoxycarbonyl)amino]thiophen-2-yl]carbonyl)amino]-1,3-benzoxazol-2-yl]carbonyl)amino]thiophene-2-carboxylate non-competitive 19219 3.4.23.16 methyl [(2S)-1-[2-[(2S)-2-benzyl-2-hydroxy-3-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-3-oxopropyl]-2-[4-(pyridin-3-yl)benzyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate - 79036 3.4.23.16 methyl [(2S)-1-[2-[(4R)-4-benzyl-4-hydroxy-5-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-2-[4-(pyridin-4-yl)benzyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate - 78956 3.4.23.16 methyl [3-[(5S)-5-([(2S,3R)-4-[(1,3-benzodioxol-5-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamoyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate - 41894 3.4.23.16 methyl [3-[(5S)-5-[[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]-1-phenylbutan-2-yl]carbamoyl]-2-oxo-1,3-oxazolidin-3-yl]phenyl]carbamate - 41893 3.4.23.16 additional information design of tight-binding human immunodeficiency virus type 1 protease inhibitors 2 3.4.23.16 additional information oxim derivatives containing halogenomethylketone and phenyl moieties are specific HIV-1 protease inhibitors 2 3.4.23.16 additional information RVL-(reduced peptide bond)-FEA-Nle-NH2 and Ac-TI-Nle-(reduced peptide bond)-Nle-QR-NH2 2 3.4.23.16 additional information design of hydrolytically-stable cyclic peptidomimetic inhibitors of HIV-1 protease 2 3.4.23.16 additional information substrate-based cyclic peptidomimetics of Phe-Ile-Val that inhibit HIV-1 protease using a novel enzyme-binding mode 2 3.4.23.16 additional information active site inhibitor binding structure analysis, overview 2 3.4.23.16 additional information synthesis of diverse prodrugs of the water-soluble dipeptide-type HIV-1 protease inhibitors KNI-727, KNI-272, and KNI-279 by O to N acyl migration, and analysis of the water-solubility and stability of the prodrugs, overview 2 3.4.23.16 additional information molecular basis for substrate recognition and drug resistance, structure analysis of substrate analogue inhibitors bound to wild-type enzyme, mutant V82A enzyme, and mutant I84V enzyme, overview 2 3.4.23.16 additional information design of enzyme inhibitors active on multidrug-resistant virus, overview 2 3.4.23.16 additional information inhibition analysis with eight clinically used protease inhibitors reveales that the natural polymorphisms found in subtype C protease, in combination with drug resistance mutations, can influence enzymatic catalytic efficiency and inhibitor resistance 2 3.4.23.16 additional information the conformational flexibility of HIV-1 protease inhibitors directly contributes to the enzyme inhibition 2 3.4.23.16 additional information two possible mechanisms of the irreversible inhibition of HIV-1 protease by epoxide inhibitors are investigated on an enzymatic model using ab initio (MP2) and density functional theory methods (B3LYP, MPW1K and M05-2X). The calculations predict the inhibition as a general acid-catalyzed nucleophilic substitution reaction proceeding by a concerted SN2 mechanism with a reaction barrier of ca. 15–21 kcal/mol. The irreversible nature of the inhibition is characterized by a large negative reaction energy of ca. -17-(-24) kcal/mol. A mechanism with a direct proton transfer from an aspartic acid residue of the active site onto the epoxide ring has been shown to be preferred compared to one with the proton transfer from the acid catalyst facilitated by a bridging catalytic water molecule 2 3.4.23.16 additional information the failure of an HIV protease inhibitor to fit within the substrate envelope appears to correlate with its susceptibility to mutational resistance 2 3.4.23.16 additional information computational techniques to improve binding affinity are successfully applied to design peptide sequences that bind tighter to inactivated (D25N) HIV-1 protease 2 3.4.23.16 additional information identification of the native pose of HIV-1 protease inhibitors by quantum mechanical/molecular mechanical models and comparison with the AMBER force field and ChemScore and GoldScore scoring functions. For the discrimination of native from non-native poses, solvent-corrected HF/6-31G:AMBER and AMBER functions exhibit the best overall performance. The electrostatic component of the MM and QM/MM functions appears important for discriminating the native pose of the ligand. There is no advantage to binding mode prediction by incorporating active site polarization at the PM3-D level. Choice of the protonation state of the aspartyl dyad in the HIV-1 protease active site influences the ability of scoring methods to determine the native binding pose 2 3.4.23.16 additional information analysis of the differences of binding patterns between the two type HIV proteases, HIV-1 protease and HIV-2 protease, using the interaction entropy (IE) method for the entropy change calculation combined with the polarized force field, and the two inhibitors darunavir and amprenavir. The bridging water W301 is favorable to the binding of HIV-1 complexes, in contrast to HIV-2 protease complexes. The volume of pocket, B-factor of Calpha atoms and the distance of flap tip in HIV-2 complexes are smaller than that of HIV-1 consistently. Predicated hot-spot residues (Ala28/Ala28', Ile50/Ile50', and Ile84/Ile84') are nearly same in the four systems. The contribution to the free energy of Asp30 residue is more favorable in HIV-1 system than in HIV-2 system. Molecular dynamics simulation and binding free energy calculations, and protonation states of the enzymes, overview 2 3.4.23.16 additional information comparison of the HIV-1 protease (PR1) and HIV-2 protease (PR2) binding pockets extracted from structures complexed with 12 ligands, overview. Structural comparison of PR1 and PR2 pockets highlight structural changes induced by their sequence variations. PR2 pockets are more hydrophobic with more oxygen atoms and fewer nitrogen atoms than PR1 pockets. Modelling of PR1 mutant structures containing V32I and L76M substitutions reveals a cooperative mechanism leading to structural deformation of flap-residue 45 that can modify PR2 flexibility. Substitutions in the PR1 and PR2 pockets can modify PI binding and flap flexibility, which might underlie PR2 resistance against PIs 2 3.4.23.16 morpholine-4-carboxylic acid (1-{1-benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propylcarbamoyl}-2-methyl-propyl)-amide IC50: 2.4 nM 52669 3.4.23.16 MTLNF - 116093 3.4.23.16 MTV-101 - 160168 3.4.23.16 MVT-101 - 32985 3.4.23.16 N,N'-(3S,4S)-pyrrolidine-3,4-diylbis(4-amino-N-benzylbenzenesulfonamide) - 26150 3.4.23.16 N,N'-(3S,4S)-pyrrolidine-3,4-diylbis[N-(4-iodobenzyl)benzenesulfonamide] - 26151 3.4.23.16 N,N'-[(2S,3R,4R,5S)-3,4-dihydroxy-1,6-diphenylhexane-2,5-diyl]bis(2-[[(2S)-3-(tert-butylsulfonyl)-2-(pyridin-4-ylmethyl)propanoyl]amino]-3-methylbutanamide) - 79067 3.4.23.16 N-(1-{1-benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propylcarbamoyl}-2-methyl-propyl)-isonicotinamide IC50: 1.3 nM 52699 3.4.23.16 N-(1-{1-benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propylcarbamoyl}-2-methyl-propyl)-nicotinamide IC50: 0.8 nM 52700 3.4.23.16 N-methyl bis-[N-(2,2-dimethyl-8,8a-dihydro-3aH-indeno[(1S,2R)-1,2]-oxazol-3-yl) 2R-benzyl-3-yl propianamide] sulfoximine - 81399 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-2-thiophen-3-ylacetamide - 65840 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]pyridazine-4-carboxamide - 65841 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-2,4,5-trifluoro-3-hydroxybenzamide - 65842 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-2-methylbenzamide - 65843 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3,4,5-trihydroxybenzamide - 65844 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3,4-dihydroxybenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65845 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(3-methoxyphenyl)sulfonyl](thiophen-2-ylmethyl)amino]propyl]-3-fluoro-2-methylbenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65846 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-3-hydroxybenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65847 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-4-oxohexanamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65848 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]cyclopropane-1,1-dicarboxamide - 65849 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-3-hydroxybenzamide - 65850 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-4-oxohexanamide - 65851 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]cyclopropane-1,1-dicarboxamide - 65852 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-3-hydroxybenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65853 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-4-oxohexanamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65854 3.4.23.16 N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]cyclopropane-1,1-dicarboxamide - 65855 3.4.23.16 N-[(1S,2R)-1-benzyl-3-[(butylsulfonyl)(3-chlorobenzyl)amino]-2-hydroxypropyl]-2,3-dichlorobenzamide - 65856 3.4.23.16 N-[(1S,2R)-1-benzyl-3-[(butylsulfonyl)(3-chlorobenzyl)amino]-2-hydroxypropyl]-2-bromo-3-methylbenzamide - 65857 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65859 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65860 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide - 65861 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide - 65862 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide - 65863 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide - 65864 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-3-hydroxybenzamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65865 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-4-oxohexanamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65866 3.4.23.16 N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]cyclopropane-1,1-dicarboxamide - 65867 3.4.23.16 N-[(2R,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86764 3.4.23.16 N-[(2S)-2-[(N-acetylthreonylisoleucyl)amino]hexyl]norleucyl-N-(3-carbamimidamido-1-carbamoylpropyl)-6-oxolysinamide i.e. RPB, nonhydrolyzable substrate analogue. Study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry. Binding is nearly abolished by the mutation D29N, but hyrdly affected by mutation D25N 150722 3.4.23.16 N-[(2S,3R)-3-hydroxy-4-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]-1-phenylbutan-2-yl]-4-oxohexanamide - 14957 3.4.23.16 N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide - 14958 3.4.23.16 N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-3-hydroxybenzamide - 14956 3.4.23.16 N-[(2S,3R)-4-[(cyclopropylmethyl)(furan-2-ylsulfonyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide - 19217 3.4.23.16 N-[(2S,3R)-4-[(cyclopropylmethyl)[(3-methoxyphenyl)sulfonyl]amino]-3-hydroxy-1-phenylbutan-2-yl]-N'-methylbutanediamide - 19212 3.4.23.16 N-[(2S,6S)-6-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-7-hydroxyheptan-2-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86763 3.4.23.16 N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-1,8-dihydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86768 3.4.23.16 N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxy-2-methyloctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86767 3.4.23.16 N-[(3S,7S)-7-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-8-hydroxyoctan-3-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86765 3.4.23.16 N-[(4S,8S)-8-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-9-hydroxynonan-4-yl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86766 3.4.23.16 N-[(5S)-5-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86761 3.4.23.16 N-[(5S)-5-[[(4-aminophenyl)sulfonyl](3-methylbutyl)amino]-6-hydroxyhexyl]-Nalpha-(methoxycarbonyl)-beta-phenyl-L-phenylalaninamide - 86762 3.4.23.16 N1-[1-Benzyl-3-(2-tert-butylcarbamoyl-pyrrolidin-1-yl)-2-methoxy-3-oxo-propyl]-2-[2-(naphthalen-1-yloxy)-acetylamino]-succinamide - 51057 3.4.23.16 N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]propyl]-L-alaninamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65957 3.4.23.16 N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](2-methylpropyl)amino]propyl]-L-valinamide - 65958 3.4.23.16 N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl](pentyl)amino]propyl]-L-valinamide - 65959 3.4.23.16 N2-acetyl-N-[(1S,2R)-1-benzyl-2-hydroxy-3-[[(4-methoxyphenyl)sulfonyl][(2S)-2-methylbutyl]amino]propyl]-L-valinamide - 65960 3.4.23.16 N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(2-methylpropyl)amino]-1-benzyl-2-hydroxypropyl]-L-valinamide - 65961 3.4.23.16 N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-1-benzyl-2-hydroxypropyl]-L-valinamide broad specificity against a clinically relevant panel of drug-resistant HIV-1 protease variants 65962 3.4.23.16 N2-acetyl-N-[(1S,2R)-3-[(1,3-benzothiazol-6-ylsulfonyl)[(2S)-2-methylbutyl]amino]-1-benzyl-2-hydroxypropyl]-L-valinamide - 65963 3.4.23.16 N2-acetyl-N-[(2S,3R)-3-hydroxy-1-phenyl-4-[(thiophen-2-ylmethyl)[(2,4,5-trifluorophenyl)sulfonyl]amino]butan-2-yl]-L-alaninamide - 19210 3.4.23.16 N2-acetyl-N-[(2S,3R)-4-[(1,3-benzothiazol-6-ylsulfonyl)(pentyl)amino]-3-hydroxy-1-phenylbutan-2-yl]-L-valinamide - 14959 3.4.23.16 N2-[(2S)-2-[(3R)-5-[(1S)-1-(L-alanylamino)ethyl]-3-benzyl-2,3,6,7-tetrahydro-1H-azepin-1-yl]propanoyl]-N-[(1S,2S,4R)-1-benzyl-2-hydroxy-4-[5-(2-methylpropanoyl)-1H-imidazol-2-yl]-5-phenylpentyl]-L-valinamide - 36905 3.4.23.16 N2-[(2S,4S,5S)-5-(acetylamino)-6-cyclohexyl-4-hydroxy-2-(1-methylethyl)hexanoyl]-L-glutaminyl-L-argininamide - 65955 3.4.23.16 nelfinavir IC50: 1.9 nM 1193 3.4.23.16 nelfinavir - 1193 3.4.23.16 nelfinavir structural analyses of the subtype C protease bound to nelfinavir and indinavir showed that these inhibitors form similar interactions with the residues in the active site of subtype B and C proteases 1193 3.4.23.16 nelfinavir in the HIV-1 protease sequence of viral variants resistant to the inhibitor nelfinavir, the mutations D30N and L90M appear frequently 1193 3.4.23.16 nelfinavir computer simulation of comlex with HIV-1 protease 1193 3.4.23.16 nelfinavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 1193 3.4.23.16 P27 peptide i.e. PQITLRKKRRQRRRPPQVSFNFCTLNF. Incubation of mutant L10I/K45R/I54V/L63P/A71V/V82T/L90M/I93L with peptide leads to dose- and time-dependent formation of protease monomers, while incubation with a active-site inhibitor does not change the elution profile of the protease. The monomeric protease induced by P27 has fluorescent characteristics consistent with unfolded protein 151753 3.4.23.16 pepstatin - 396 3.4.23.16 pepstatin A - 309 3.4.23.16 Phe-Asp-Asp-Phe with KARV-Nle-Phe(NO2)-EA-Nle-NH2 as substrate 52818 3.4.23.16 Phe-Leu-Asp-Gly product inhibition with Ac-RKILFLDG-NH2 as substrate 52819 3.4.23.16 Phe-Leu-Asp-Gly-NH2 product inhibition with Ac-SQNYFLDG-NH2 as substrate 44673 3.4.23.16 phenoxyacetyl-Phe-PSI(S,R,S)[OH]-Phe-phenoxyacetyl IC50: 0.017 mM 52823 3.4.23.16 phenoxyacetyl-Phe-PSI(S,S,S)[OH]-Phe-phenoxyacetyl IC50: 0.005 mM 52824 3.4.23.16 phenyl N-[(1R,2S)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate - 86735 3.4.23.16 pyridin-3-ylmethyl [(5S,8S,9R,10R,11S,14S)-8,11-dibenzyl-9,10-dihydroxy-15-methyl-3,6,13-trioxo-5-(propan-2-yl)-1-(pyridin-3-yl)-2-oxa-4,7,12-triazahexadecan-14-yl]carbamate - 78971 3.4.23.16 pyridine-2-carboxylic acid (1-{1-benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propylcarbamoyl}-2-methyl-propyl)-amide IC50: 4.6 nM 52865 3.4.23.16 pyrrolidinemehylene diamine derivatives binding mode of pyrrolidine-based aspartyl protease inhibitors: design, synthesis and crystal structure in complex with HIV protease, overview 129555 3.4.23.16 QF34 - 160170 3.4.23.16 R-P-G-N-F-r-L-Q-S-R-P substrate analogue, competitive inhibition of the HIV-1 protease, mimicks the pI-p6 cleavage site 23705 3.4.23.16 R-V-L-r-F-E-A-Nle substrate analogue, competitive inhibition of the HIV-1 protease, mimicks the CA/p2 cleavage site 8629 3.4.23.16 R-V-L-r-F-E-A-Nle substrate analogue peptide inhibitor 8629 3.4.23.16 rac-(3S,4S)-N-benzyl-2-(2,6-dimethyl-phenoxy)-N-4-[[(isobutyl-(toluene-4-sulfonyl)-amino)-methyl]-pyrrolidin-3-ylmethyl]-acetamide IC50 is 0.0121 mM, binding structure analysis, modelling 58739 3.4.23.16 rac-(3S,4S)-N-[4-([4-amino-benzenesulfonyl-isobutyl-amino]-methyl)-pyrrolidin-3-ylmethyl]-N-benzyl-2-(2,6-dimethyl-phenoxy)-acetamide IC50 is 0.0033 mM, binding structure analysis, modelling 58738 3.4.23.16 rac-(3S,4S)-N-[4-([benzenesulfonyl-isobutyl-amino]-methyl)-pyrrolidin-3-ylmethyl]-N-benzyl-2-(2,6-dimethyl-phenoxy)-acetamide IC50 is 0.0022 mM, binding structure analysis, modelling 58737 3.4.23.16 renin inhibitors - 116650 3.4.23.16 ritonavir IC50: 3 nM 996 3.4.23.16 ritonavir - 996 3.4.23.16 ritonavir HIV-1 pNL4-3 clones with a single V82L or I84V mutation are phenotypically resistant to A-790742 and ritonavir 996 3.4.23.16 ritonavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 996 3.4.23.16 ritronavir - 160172 3.4.23.16 RTLNLGL IC50 is above 0.8 mM 52897 3.4.23.16 RVLrFEANle - 239920 3.4.23.16 saquinavir - 997 3.4.23.16 saquinavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 997 3.4.23.16 saururin B - 81388 3.4.23.16 SB203386 - 52904 3.4.23.16 SB204,144 - 116701 3.4.23.16 schisanlactone A dimerization inhibitor 81386 3.4.23.16 Ser-Leu-Asn-Phe IC50: 0.47 mM 52908 3.4.23.16 SFNL IC50: 0.28 mM 52914 3.4.23.16 SFNLE IC50: 0.31 mM 52915 3.4.23.16 SKF 107457 - 52916 3.4.23.16 SKF 108361 - 116744 3.4.23.16 t-butyl 3-isopropyl-3-(2S,3S)-2-hydroxy-3-(-quinaldoyl-L-asparaginyl)amino-4-phenylbutylcarbazate i.e. DG-35-VIII, inhibits processing of the Pr55gag and Pr160gag-pol precursor proteins 116838 3.4.23.16 tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[CH2CH2NH]-Phe-Glu-Phe-NH2, an ethyleneamine inhibitor, interactions with the enzyme, overview 35416 3.4.23.16 tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Gln-Phe-NH2, a pseudotetrapeptide inhibitor with an acyclic S-hydroxyethylamine isostere, interactions with the enzyme and binding structure, overview 35415 3.4.23.16 tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2NH]-Phe-Glu-Phe-NH2, a pseudotetrapeptide inhibitor with an acyclic S-hydroxyethylamine isostere, interactions with the enzyme and binding structure, overview 35414 3.4.23.16 tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2 i.e. tert-butoxycarbonyl-Phe-psi[S-CH(OH)CH2]-Phe-Gln-Phe-NH2, a hydroxyethylene inhibitor, interactions with the enzyme, overview 35417 3.4.23.16 tert-butyl N-[(1R,2S)-1-benzyl-3-[(4S)-7-fluoro-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]-2-hydroxypropyl]carbamate - 86736 3.4.23.16 tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-7-(trifluoromethyl)-1,3,4,5-tetrahydro-2H-1lambda6,-2-benzothiazepin-2-yl]propyl]carbamate - 86737 3.4.23.16 tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-4-methyl-1,1-dioxo-8-(trifluoromethyl)-1,3,4,5-tetrahydro-2H-1lambda6,-2-benzothiazepin-2-yl]propyl]carbamate - 86738 3.4.23.16 tert-butyl N-[(1S,2R)-1-benzyl-2-hydroxy-3-[(4S)-7-methoxy-4-methyl-1,1-dioxo-1,3,4,5-tetrahydro-2H-1lambda6,2-benzothiazepin-2-yl]propyl]carbamate - 86739 3.4.23.16 Thr-Leu-Asn-Leu IC50: 0.38 mM 52938 3.4.23.16 Thr-Leu-Asn-Phe-NH2 IC50 is above 2 mM 52939 3.4.23.16 Thr-Leu-Asn-Tyr IC50 is about 1 mM 52940 3.4.23.16 Thr-Phe-Asn-Phe IC50: 0.45 mM 52941 3.4.23.16 tipranavir IC50 is 30 nM, interacts with residues Asp25 and Asp25', and Ile50 and Ile50' 2316 3.4.23.16 tipranavir - 2316 3.4.23.16 tipranavir study on impact of active site region aspartyl residues 25 and 29 on the binding by differential scanning calorimetry 2316 3.4.23.16 TL-3 - 40443 3.4.23.16 TLNLGF IC50 is above 0.8 mM 52947 3.4.23.16 U-71017 i.e. Poa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp 52955 3.4.23.16 U-71038 i.e. Boc-Pro-Phe-Nalpha-MeHis-Leu-PSI[CH(OH)CH2]Val-Ile-Amp 52956 3.4.23.16 U-75875 - 52957 3.4.23.16 U-75875 i.e. Noa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp 52957 3.4.23.16 U-79213 i.e. Poa-His-Cha-PSI[CH(OH)CH2]Val-Ile-Amp 52958 3.4.23.16 U-81749E i.e. Tba-Cha-PSI[CH(OH)CH2]Val-Ile-Amp 52959 3.4.23.16 U-85548E - 116957 3.4.23.16 U-89360E - 52960 3.4.23.16 UCSF8 - 52961 3.4.23.16 UIC-94017 TMC-114, a broad-spectrum, potent non-peptide inhibitor of HIV-1 protease, the inhibitor shows low cytotoxicity, enzyme binding structure analysis 23670 3.4.23.16 ursolic acid - 2291 3.4.23.16 ursolic acid dimerization inhibitor 2291 3.4.23.16 V-S-F-N-F-r-P-Q-I-T-K-K substrate analogue, competitive inhibition of the HIV-1 protease, mimicks the p6pol-PR cleavage site 23704 3.4.23.16 XK263 - 160169 3.4.23.16 [1-(1-Benzyl-3-benzylcarbamoyl-3,3-difluoro-2-oxo-propylcarbamoyl)-2-methyl-propyl]-carbamic acid benzyl ester - 51059 3.4.23.16 [1-(1-{1-benzyl-3-[2-(1-tert-butylcarbamoyl-2-methyl-butylcarbamoyl)-pyrrolidin-1-yl]-2-methoxy-propylcarbamoyl}-2-carbamoyl-ethylcarbamoyl)-3-methyl-butyl]-carbamic acid benzyl ester IC50: 750 nM 52127 3.4.23.16 [1-Benzyl-2-hydroxy-4-(3-hydroxy-indan-1-ylcarbamoyl)-7-phenyl-hept-6-enyl]-carbamic acid tert-butyl ester IC50: 0.55 nM 51060 3.4.23.16 [1-Benzyl-3-(3-benzyl-1-isothiochroman-4-yl-2-oxo-pyrrolidin-3-yl)-2-hydroxy-propyl]-carbamic acid tert-butyl ester IC50: 111 nM 51062 3.4.23.16 [1-Benzyl-3-[3-benzyl-1-(2-hydroxy-5-methyl-cyclopentyl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propyl]-carbamic acid tert-butyl ester IC50: 17 nM 51063 3.4.23.16 [1-Benzyl-4-(2,2-dioxo-2lambda6-isothiochroman-4-ylcarbamoyl)-2-hydroxy-7-phenyl-hept-6-enyl]-carbamic acid tert-butyl ester IC50: 2.3 nM 51061 3.4.23.16 {1-benzyl-3-[3-benzyl-1-(2,2-dioxo-2l6-isothiochroman-4-yl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propyl}-carbamic acid tert-butyl ester IC50: 14 nM 52132 3.4.23.16 {1-benzyl-3-[3-benzyl-1-(2-hydroxy-indan-1-yl)-2-oxo-pyrrolidin-3-yl]-2-hydroxy-propyl}-carbamic acid tert-butyl ester 37 nM 114717 3.4.23.16 {1-[1-benzyl-3-(2-tert-butylcarbamoyl-piperidin-1-yl)-2-methoxy-propylcarbamoyl]-2-carbamoyl-ethyl}-carbamic acid benzyl ester IC50: 18 nM 52130 3.4.23.16 {1-[1-benzyl-3-(2-tert-butylcarbamoyl-pyrrolidin-1-yl)-2-methoxy-propylcarbamoyl]-2-carbamoyl-ethyl}-carbamic acid benzyl ester IC50: 210 nM 52131