3.4.22.69 additional information - 2-(benzylsulfanyl)-4-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 2-(benzylsulfanyl)-4-(4-methoxyphenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 2-(benzylsulfanyl)-4-(4-methylphenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 2-(benzylsulfanyl)-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 4-(3-nitrophenyl)-6-oxo-2-[(2-phenylethyl)sulfanyl]-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 4-(4-methylphenyl)-2-[(4-nitrobenzyl)sulfanyl]-6-oxo-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 4-(4-methylphenyl)-6-oxo-2-[(2-phenylethyl)sulfanyl]-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - 6-oxo-4-phenyl-2-[(2-phenylethyl)sulfanyl]-1,6-dihydropyrimidine-5-carbonitrile IC50 above 0.05 mM 707708 3.4.22.69 additional information - additional information extracts of Rheum palmatum show IC50 values between 0.014 mg/ml and 0.059 mg/ml 707798 3.4.22.69 0.00003 - 5-chloropyridin-3-yl 1H-indole-4-carboxylate - 691304 3.4.22.69 0.00003 - 5-chloropyridin-3-yl 1H-indole-4-carboxylate pH and temperature not specified in the publication 731443 3.4.22.69 0.000051 - 2-(1H-benzotriazol-1-yl)-N-(biphenyl-4-yl)-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.00006 - 5-chloropyridin-3-yl 5-(4-nitrophenyl)-2-furoate - 678619 3.4.22.69 0.00006 - N-(2-chloro-4-nitrophenyl)-Nalpha-[[4-(dimethylamino)phenyl]carbonyl]phenylalaninamide - 679402 3.4.22.69 0.000063 - 5-chloropyridin-3-yl 5-(4-chlorophenyl)-2-furoate - 678619 3.4.22.69 0.000065 - (S)-N-((S)-1-(((S)-1-(1H-imidazol-4-yl)-3-oxopropan-2-yl)amino)-3-cyclohexyl-1-oxopropan-2-yl)-2-((S)-2-((S)-2-acetamido-3-hydroxypropanamido)propanamido)-3-methylbutanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.000065 - N-acetyl-Ser-Ala-Val-Cha-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.00008 - 5-chloropyridin-3-yl 1H-indole-7-carboxylate - 691304 3.4.22.69 0.000089 - 5-chloropyridin-3-yl 1-[(3-nitrophenyl)sulfonyl]-1H-indole-5-carboxylate - 691304 3.4.22.69 0.000108 - 5-chloropyridin-3-yl 2-oxo-2H-chromene-3-carboxylate - 678619 3.4.22.69 0.000122 - 5-chloropyridin-3-yl 5-(4-chloro-2-nitrophenyl)-2-furoate - 678619 3.4.22.69 0.000124 - 5-chloropyridin-3-yl 1-naphthoate - 678619 3.4.22.69 0.00014 - 5-chloropyridin-3-yl (3S)-2-acetyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylate - 691304 3.4.22.69 0.000164 - 5-chloropyridin-3-yl isonicotinate - 678619 3.4.22.69 0.00017 - 2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-N-(3-chlorophenethyl)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.0002 - 1-[(1H-indol-5-ylcarbonyl)oxy]-1H-benzotriazole - 691304 3.4.22.69 0.0002 - Nalpha-[(2E)-3-(4-chloro-2-fluorophenyl)prop-2-enoyl]-N-[(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]-D-phenylalaninamide pH and temperature not specified in the publication 753268 3.4.22.69 0.000208 - 5-chloropyridin-3-yl 5-(2-nitrophenyl)-2-furoate - 678619 3.4.22.69 0.00022 - N-(1-benzylpiperidin-4-yl)-2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00023 - 5-chloropyridin-3-yl 1H-indole-6-carboxylate - 691304 3.4.22.69 0.00024 - 2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-N-(3-methoxyphenethyl)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00027 - N-acetyl-Ala-Val-Cha-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.00028 - 2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-N-(4-methoxyphenethyl)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.0003 - 2,4-dichloro-5-methylphenyl 2,6-dinitro-4-(trifluoromethyl)phenyl sulfone - 681289 3.4.22.69 0.00031 - 5-chloropyridin-3-yl 1H-indole-5-carboxylate - 691304 3.4.22.69 0.000333 - 5-chloropyridin-3-yl 2-nitrobenzoate - 678619 3.4.22.69 0.00034 - N-acetyl-Ser-Val-Cha-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.00037 - 1-(2-naphthylmethyl)-2,3-dioxoindoline-5-carboxamide - 679402 3.4.22.69 0.00037 - 1-(2-naphthylmethyl)isatin-5-carboxamide - 709130 3.4.22.69 0.00037 - 5-chloropyridin-3-yl 1-[(4-methylphenyl)sulfonyl]-1H-indole-5-carboxylate - 691304 3.4.22.69 0.00038 - N-(4-(tert-butyl)phenyl)-2-chloro-N-(2-(cyclopentylamino)-2-oxo-1-(pyridin-3-yl)ethyl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00039 - N-acetyl-Ser-Ala-Val-Phe-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.0004 - 5-chloropyridin-3-yl 1-acetyl-1H-indole-5-carboxylate - 691304 3.4.22.69 0.00041 - N-(4-(tert-butyl)phenyl)-2-chloro-N-(2-(cyclohexylamino)-2-oxo-1-(pyridin-3-yl)ethyl) acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00042 - 2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-N-cyclohexyl-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.000434 - 5-chloropyridin-3-yl 4-chlorobenzoate - 678619 3.4.22.69 0.0005 - 5-bromopyridin-3-yl thiophene-2-carboxylate pH and temperature not specified in the publication 731443 3.4.22.69 0.0005 - 5-chloropyridin-3-yl 5-(3-nitrophenyl)-2-furoate - 678619 3.4.22.69 0.0005 - 5-chloropyridin-3-yl thiophene-2-carboxylate - 679402, 679408 3.4.22.69 0.000516 - 2-[(4-chlorophenyl)disulfanyl]-1,3,4-oxadiazole pH 7.3, 37°C 753488 3.4.22.69 0.00052 - 2-(N-(4-(tert-butyl)phenyl)vinylsulfonamido)-N-(3-phenylpropyl)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.0006 - (S)-2-((2S,3R)-2-((S)-2-acetamido-3-methylbutanamido)-3-(benzyloxy)butanamido)-4-methyl-N-((S)-4-(5-nitro-1,4-dioxo-3,4-dihydrophthalazin-2(1H)-yl)-3-oxo-1-((S)-2-oxopyrrolidin-3-yl)butan-2-yl)pentanamide - 679402 3.4.22.69 0.0006 - 4-((S)-2-((2S,3S)-2-((S)-2-acetamido-3-methylbutanamido)-3-(benzyloxy)butanamido)-4-methylpentanamido)-N,N-dimethyl-6-(5-nitro-1,4-dioxo-3,4-dihydrophthalazin-2(1H)-yl)-5-oxohexanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.000648 - 5-chloropyridin-3-yl 3-nitrobenzoate - 678619 3.4.22.69 0.00066 - (5S,8S,11S,E)-methyl 8-isobutyl-5-isopropyl-3,6,9-trioxo-11-(((S)-2-oxopyrrolidin-3-yl)methyl)-1-phenyl-2-oxa-4,7,10-triazatetradec-12-en-14-oate enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.000684 - 2-[(4-chlorophenyl)disulfanyl]pyrimidine pH 7.3, 37°C 753488 3.4.22.69 0.000697 - 5-chloropyridin-3-yl nicotinate - 678619 3.4.22.69 0.0007 - N-[4-(2-acetylpyridin-3-yl)phenyl]-2-(1H-benzotriazol-1-yl)-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.00084 - N-(4-(tert-butyl)phenyl)-2-chloro-N-(2-(cyclohexylamino)-2-oxo-1-(pyridin-4-yl)ethyl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00085 - N-(4-(tert-butyl)phenyl)-N-(2-(cyclohexylamino)-2-oxo-1-(pyridin-3-yl)ethyl)-4-hydroxybut-2-ynamide pH 7.3, 25°C 764634 3.4.22.69 0.0009 - sulfonyldi-4,1-phenylene bis(2,3,3-trichloroacrylate) - 681289 3.4.22.69 0.0009 - tert-butyl [1-[(2S)-1-([(2S)-4-(benzylamino)-3,4-dioxo-1-[(3S)-2-oxopyrrolidin-3-yl]butan-2-yl]amino)-3-cyclopropyl-1-oxopropan-2-yl]-2-oxo-1,2-dihydropyridin-3-yl]carbamate pH and temperature not specified in the publication 755546 3.4.22.69 0.00092 - N-benzyl-2-(N-(4-(tert-butyl)phenyl)-2-chloroacetamido)-2-(pyridin-3-yl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00095 - 1-(1-benzothiophen-2-ylmethyl)-5-iodo-1H-indole-2,3-dione - 679402, 679408 3.4.22.69 0.00097 - 2-(1H-benzotriazol-1-yl)-N-[4-(pyridin-3-yl)phenyl]-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.00098 - N-(4-(tert-butyl)phenyl)-2-chloro-N-(2-(cyclohexylamino)-1-(5-methylpyrazin-2-yl)-2-oxoethyl)acetamide pH 7.3, 25°C 764634 3.4.22.69 0.00098 - N-acetyl-Thr-Val-Cha-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.00104 - 5-(4-methylpiperidine-1-sulfonyl)-1-phenyl-1H-indole-2,3-dione pH and temperature not specified in the publication 753268 3.4.22.69 0.00106 - N-(2-cinnamoylthiophenyl)cinnamide - 691768 3.4.22.69 0.00108 - 5-chloropyridin-3-yl 1-acetyl-1H-indole-4-carboxylate - 691304 3.4.22.69 0.00118 - 5-(4-methylpiperidine-1-sulfonyl)-1H-indole-2,3-dione pH and temperature not specified in the publication 753268 3.4.22.69 0.0015 - 2-(1H-benzotriazol-1-yl)-N-[4-(benzylamino)phenyl]-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0015 - N-[(1R)-2-(tert-butylamino)-2-oxo-1-(pyridin-3-yl)ethyl]-N-(4-tert-butylphenyl)furan-2-carboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0017 - (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-4-methyl-2-((S)-3-methyl-2-(2-phenoxyacetamido)butanamido)pentanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0017 - N-[(benzyloxy)carbonyl]-L-valyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]-L-leucinamide pH and temperature not specified in the publication 731749 3.4.22.69 0.00193 - GC376 wild-type, pH 7.5, 25°C 765793 3.4.22.69 0.002 - 2-(1H-benzotriazol-1-yl)-N-[4-(pyridin-4-yl)phenyl]-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.002 - 3-[1-(4-benzyloxyphenyl)-1H-tetrazol-5-ylthio]-4-methoxyquinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0021 - 2-(1H-benzotriazol-1-yl)-N-[4-(methylamino)phenyl]-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0022 - benzyl ((S)-1-(((S)-1-(((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)carbamate enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0025 - 2-phenylethyl 2-methyl-4-(2-nitrophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate - 679402 3.4.22.69 0.0025 - 3,4-dichloro-5-[2-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-oxoethyl]furan-2(5H)-one - 679408 3.4.22.69 0.0025 - 3-(4-bromophenyl)-5-(4-chlorophenyl)-1-(3,4-dichlorophenyl)-4-(1H-imidazol-1-yl)-4,5-dihydro-1H-pyrazole - 692371 3.4.22.69 0.0026 - bis[1,3]thiazolo[4,5-b:5',4'-e]pyridine-2,6-diamine - 679402, 679408 3.4.22.69 0.0026 - iguesterin - 707696 3.4.22.69 0.0029 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]propanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.003 - S-[5-(trichloromethyl)-4H-1,2,4-triazol-3-yl] 5-(phenylethynyl)furan-2-carbothioate - 681289 3.4.22.69 0.0033 - 4-[(E)-[(2-methoxyphenyl)imino]methyl]-2-phenyl-1,3-oxazol-5-yl acetate - 692371 3.4.22.69 0.0034 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]-3-methoxypropanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0036 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]-2-methylpropanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0037 - 1,2,3,4,6-pentagalloylglucose pH not specified in the publication, temperature not specified in the publication 764084 3.4.22.69 0.00374 - GC376 mutant P108S, pH 7.5, 25°C 765793 3.4.22.69 0.0038 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)cyclobutanecarboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0041 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)-2-methylpropanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0041 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]cyclopropanecarboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0042 - (-)-epigallocatechin-3-gallate pH not specified in the publication, temperature not specified in the publication 764084 3.4.22.69 0.0043 - 2-(4-aminophenyl)-6-methyl-1H-benzimidazole-7-sulfonic acid - 679402, 679408 3.4.22.69 0.005 - (2E)-N-[2-[4-(dimethylamino)butyl]phenyl]-3-phenylprop-2-enamide pH and temperature not specified in the publication 731443 3.4.22.69 0.005 - 5-(1,3-dimethyl-1H-pyrazol-5-yl)-N-(3-methyl-4-nitroisoxazol-5-yl)thiophene-2-carboxamide - 681289 3.4.22.69 0.0055 - pristimerin - 707696 3.4.22.69 0.0057 - N-acetyl-Ser-Ala-Val-Leu-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.006 - 5-[(4-chlorophenyl)sulfonyl]pyrimidine-2,4-diamine - 681289 3.4.22.69 0.0061 - 4-(4-chlorophenyl)-2-[(4-nitrobenzyl)sulfanyl]-6-oxo-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.0061 - 4-(4-chlorophenyl)-2-[(4-nitrobenzyl)sulfanyl]-6-oxo-1,6-dihydropyrimidine-5-carbonitrile enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0062 - N-[4-(acetylamino)phenyl]-2-(1H-benzotriazol-1-yl)-N-[(1R)-2-[(2-methylbutan-2-yl)amino]-1-(1-methyl-1H-pyrrol-3-yl)-2-oxoethyl]acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0067 - tert-butyl [1-[(2S)-1-([(2S)-4-(benzylamino)-3,4-dioxo-1-[(3S)-2-oxopyrrolidin-3-yl]butan-2-yl]amino)-3-cyclopropyl-1-oxopropan-2-yl]-2-oxo-1,2-dihydropyridin-3-yl]carbamate pH and temperature not specified in the publication 755546 3.4.22.69 0.0068 - 4-[(Z)-[1-(4-fluorophenyl)-5-oxo-3-phenyl-1,5-dihydro-4H-pyrazol-4-ylidene]methyl]benzoic acid enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0069 - 1,2,3,4,6-pentagalloylglucose pH not specified in the publication, temperature not specified in the publication 764084 3.4.22.69 0.0069 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)propanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.007 - 2-benzyl-2H-isoindole-4,7-dione - 692371 3.4.22.69 0.007 - 3,4-dichloro-5-[2-(5-chloro-3-methyl-1-benzothien-2-yl)-2-oxoethyl]furan-2(5H)-one - 679402, 679408 3.4.22.69 0.007 - methyl 4-hydroxy-6-(trifluoromethyl)furo[2,3-b]pyridine-2-carboxylate - 679402, 679408 3.4.22.69 0.0071 - (2E)-1-[3-(2-hydroperoxy-3-methylbut-3-en-1-yl)-2-hydroxy-4-methoxyphenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one pH and temperature not specified in the publication 753268 3.4.22.69 0.0072 - 4-methoxy-6-[([1,3]thiazolo[5,4-b]pyridin-2-ylsulfinyl)methyl]-2H-pyran-2-one - 692371 3.4.22.69 0.0077 - N-[4-(acetylamino)phenyl]-2-(1H-benzotriazol-1-yl)-N-[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.008 - N-[4-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)benzyl]-1-propyl-1H-benzimidazol-2-amine - 692371 3.4.22.69 0.0081 - 1-butyl-N-[4-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)benzyl]-1H-benzimidazol-2-amine - 692371 3.4.22.69 0.0081 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]cyclobutanecarboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0084 - N-[4-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)benzyl]-1-ethyl-1H-benzimidazol-2-amine - 692371 3.4.22.69 0.0085 - 2-[4-(chloroacetyl)-2-oxo-1,2,5,6-tetrahydropyridin-3-yl]-N-(3-chlorophenyl)acetamide pH 7.3, temperature not specified in the publication 764635 3.4.22.69 0.0091 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)cyclopropanecarboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0095 - N-[(benzyloxy)carbonyl]-L-valyl-N-[(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]-1-(1,3-thiazol-2-yl)propan-2-yl]-L-leucinamide pH and temperature not specified in the publication 731749 3.4.22.69 0.0098 - 2-acetyl-3-(3-iodophenyl)-7-methoxy-3,3a,4,5-tetrahydro-2H-benzo[g]indazole - 692371 3.4.22.69 0.0099 - tingenone - 707696 3.4.22.69 0.01 - (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-2-(2-((3-methoxyphenyl)amino)acetamido)-4-methylpentanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.01 - 3-[1-(4-benzyloxyphenyl)-1H-tetrazol-5-ylthio]-4-hydroxyquinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.01 - 3-[N-[N-benzyloxycarbonyl-L-Ala-L-Val-L-Leu]]-4-phenyl-1,1,1-trifluorobutan-2-one - 691222 3.4.22.69 0.01 - 5,7-dichloro-4-hydroxy-3-[[1-(4-hydroxyphenyl)-1H-tetrazol-5-yl]sulfanyl]quinolin-2(1H)-one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.01 - betulinic acid - 681313 3.4.22.69 0.01 - Bz-Ala-Val-Leu-Phe-trifluromethyl ketone enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.01 - N-(3-methoxyphenyl)glycyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]-L-leucinamide pH and temperature not specified in the publication 731749 3.4.22.69 0.01 - N-acetyl-Asn-Val-Cha-His in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.01 - N-tert-butyl-L-seryl-L-valyl-N-[(1S,2E)-4-ethoxy-4-oxo-1-[2-(2-oxopyrrolidin-3-yl)ethyl]but-2-en-1-yl]-L-leucinamide - 678690 3.4.22.69 0.01 - N-[3-(5-tert-butyl-2-methyl-3-furyl)-1H-pyrazol-5-yl]thiophene-2-sulfonamide - 681289 3.4.22.69 0.0103 - 2-methylpropyl [4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]carbamate pH and temperature not specified in the publication 731443 3.4.22.69 0.0103 - celastrol - 707696 3.4.22.69 0.0106 - 2-[(4-nitrobenzyl)sulfanyl]-4-(3-nitrophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.0106 - 5,7-dichloro-4-hydroxy-3-[[1-(4-hydroxyphenyl)-1H-tetrazol-5-yl]sulfanyl]quinolin-2(1H)-one - 692371 3.4.22.69 0.011 - N-[4-(acetylamino)phenyl]-N-[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]-2-(4-phenyl-1H-1,2,3-triazol-1-yl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0118 - ellagic acid pH 7.3, 25°C 764693 3.4.22.69 0.0119 - curcumin pH 7.3, 25°C 764693 3.4.22.69 0.012 - 1-[(4-chlorophenyl)sulfonyl]-2-nitro-4-(trifluoromethyl)benzene - 681289 3.4.22.69 0.0125 - 3-[1-(4-ethoxyphenyl)-1H-tetrazol-5-ylthio]-4-hydroxyquinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 4-benzyloxy-3-[1-(4-benzyloxyphenyl)-1H-tetrazol-5-ylthio]quinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 4-benzyloxy-3-[1-(4-ethoxyphenyl)-1H-tetrazol-5-ylthio]quinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 4-benzyloxy-3-[1-(4-methoxyphenyl)-1H-tetrazol-5-ylthio]quinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 4-hydroxy-3-[1-(4-hydroxyphenyl)-1H-tetrazol-5-ylthio]quinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 4-hydroxy-3-[1-(4-methoxyphenyl)-1H-tetrazol-5-ylthio]quinolin-2-(1H)one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - 5,7-dichloro-4-hydroxy-3-[1-(4-methoxy-phenyl)-1H-tetrazol-5-ylsulfanyl]-1H-quinolin-2-one in 10 mM HEPES at pH 7.5, temperature not specified in the publication 717450 3.4.22.69 0.0125 - N-[4-(2-acetylpyrimidin-5-yl)phenyl]-2-(1H-benzotriazol-1-yl)-N-(thiophen-3-ylmethyl)acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.013 - 2-(5-bromopyridin-3-yl)-1-(5-(4-chlorophenyl)furan-2-yl)ethanone - 691200 3.4.22.69 0.013 - 2-(5-bromopyridin-3-yl)-1-[5-(4-chlorophenyl)furan-2-yl]ethanone pH and temperature not specified in the publication 731443 3.4.22.69 0.013 - 4,6-dimethyl-2-[(4-methylphenyl)sulfonyl]-5-nitronicotinonitrile - 681289 3.4.22.69 0.013 - 4,6-dimethyl-5-nitro-2-(phenylsulfonyl)nicotinonitrile - 681289 3.4.22.69 0.0133 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]-2,2-dimethylpropanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0135 - N-(2-carbomethoxyethylthiophenyl)cinnamide - 691768 3.4.22.69 0.0139 - epigallocatechin gallate pH 7.3, 25°C 764693 3.4.22.69 0.014 - (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-2-(2-((2-methoxyphenyl)amino)acetamido)-4-methylpentanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.015 - 2-[(4-chlorophenyl)sulfonyl]-5-nitropyridine 1-oxide - 681289 3.4.22.69 0.015 - 3-[N-(N-benzyloxycarbonyl-L-Leu)]-4-phenyl-1,1,1-trifluorobutan-2-one - 691222 3.4.22.69 0.015 - N-tert-butyl-L-seryl-L-valyl-N-[(1S,2E)-4-ethoxy-1-[[(3S)-3-methyl-2-oxopyrrolidin-3-yl]methyl]-4-oxobut-2-en-1-yl]-L-phenylalaninamide - 678690 3.4.22.69 0.015 - N-[4-[(4-chlorophenyl)sulfonyl]-3-(methylthio)-1H-pyrazol-5-yl]thiophene-2-carboxamide - 681289 3.4.22.69 0.016 - 2-[(2-acetylphenyl)sulfonyl]benzoic acid - 681289 3.4.22.69 0.016 - 3-[(2-furylmethyl)amino]-6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-2-benzothiophene-1-carbonitrile - 681289 3.4.22.69 0.016 - 4-[(3,5-dibromo-4-hydroxyphenyl)sulfonyl]benzoic acid - 681289 3.4.22.69 0.016 - diethyl (2E,2'E)-3,3'-[sulfonylbis(benzene-4,1-diylimino)]bis(2-cyanoprop-2-enoate) - 681289 3.4.22.69 0.0169 - 4-(4-chlorophenyl)-6-oxo-2-[(2-phenylethyl)sulfanyl]-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.0169 - resveratrol pH 7.3, 25°C 764693 3.4.22.69 0.0172 - 3-benzyl-1-[(6,7-dimethyl-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)methyl]-1-[2-(2-methylphenyl)ethyl]urea enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0172 - 3-benzyl-1-[(6,7-dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl]-1-[2-(2-methylphenyl)ethyl]urea - 691218 3.4.22.69 0.018 - 2',5'-dimethyl-3-(methylthio)-4'-nitro-5-(2-thienyl)-2'H-1,3'-bipyrazole-4-carbonitrile - 681289 3.4.22.69 0.018 - 4-(5-chloro-2-thienyl)-2-[(2-thienylsulfonyl)methyl]-1,3-thiazole - 681289 3.4.22.69 0.0182 - 2-[(2-cyclohexylquinazolin-4-yl)sulfanyl]-N-(furan-2-ylmethyl)acetamide - 691218 3.4.22.69 0.019 - N-[4-(1H-imidazol-4-yl)phenyl]-2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)acetamide pH 7.5, 25°C 765227 3.4.22.69 0.0191 - 5-bromo-2-[(2Z)-2-[5-cyano-1-(3-hydroxypropyl)-4-methyl-2,6-dioxo-1,6-dihydropyridin-3(2H)-ylidene]hydrazinyl]benzoic acid pH 7.3, temperature not specified in the publication 764635 3.4.22.69 0.0197 - N-(2-allylthiophenyl)cinnamide - 691768 3.4.22.69 0.02 - 3-[N-(N-benzyloxycarbonyl-L-Phe)]-4-phenyl-1,1,1-trifluorobutan-2-one - 691222 3.4.22.69 0.02 - ML300 pH 7.5, 25°C 765227 3.4.22.69 0.02 - N-(2,2'-bithien-5-ylmethyl)-1,3-dimethyl-4-nitro-1H-pyrazol-5-amine - 681289 3.4.22.69 0.02 - N-(4-aminophenyl)-2-(1H-benzotriazol-1-yl)-N-[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0203 - 4-(4-methoxyphenyl)-6-oxo-2-[(2-phenylethyl)sulfanyl]-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.021 - benzyl ((S)-1-(((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)carbamate enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.0217 - dihydrocelastrol - 707696 3.4.22.69 0.0221 - N-[4-[(1H-benzotriazol-1-ylacetyl)(thiophen-3-ylmethyl)amino]phenyl]cyclohexanecarboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0225 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)-2,2-dimethylpropanamide pH and temperature not specified in the publication 731443 3.4.22.69 0.0234 - quercetin pH 7.3, 25°C 764693 3.4.22.69 0.0235 - curcumin - 707696 3.4.22.69 0.024 - (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-4-methyl-2-(2-phenoxyacetamido)pentanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.024 - 2-(3',4'-dihydroxyphenyl)-5,7-dihydroxy-3-beta-L-fucosyl-4H-chromen-4-one - 678590 3.4.22.69 0.025 - (-)-epigallocatechin-3-gallate pH not specified in the publication, temperature not specified in the publication 764084 3.4.22.69 0.025 - 1,1'-sulfonylbis(4-nitrobenzene) - 681289 3.4.22.69 0.025 - savinin - 681313 3.4.22.69 0.0253 - 2-(1H-benzotriazol-1-yl)-N-[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]-N-[4-[(methylsulfonyl)amino]phenyl]acetamide pH and temperature not specified in the publication 731443 3.4.22.69 0.026 - acetyl-Thr-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO - 691242 3.4.22.69 0.026 - N-(4-[(1H-benzotriazol-1-ylacetyl)[2-(tert-butylamino)-2-oxo-1-(thiophen-3-yl)ethyl]amino]phenyl)-1,2-oxazole-5-carboxamide pH and temperature not specified in the publication 731443 3.4.22.69 0.026 - N-acetyl-L-threonyl-N-[(3R,4S,4aR,8aS)-2-(4-bromobenzoyl)-3-([[(2S)-1-(1H-imidazol-4-yl)-3-oxopropan-2-yl]amino]methyl)decahydroisoquinolin-4-yl]glycinamide pH 7.5, 37°C 752974 3.4.22.69 0.0263 - 4-(4-methoxyphenyl)-2-[(4-nitrobenzyl)sulfanyl]-6-oxo-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.028 - 2-(5-bromopyridin-3-yl)-1-(5-(4-chlorophenyl)furan-2-yl)-2-fluoroethanone - 691200 3.4.22.69 0.03 - (R)-N-cinnamoyl serine(benzoyl)cyclohexylamide pH 4.0, temperature not specified in the publication 752992 3.4.22.69 0.0318 - tafenoquine pH 7.8, 25°C 765085 3.4.22.69 0.032 - 2-(3',4'-dihydroxyphenyl)-5,7-dihydroxy-3-beta-D-arabinosyl-4H-chromen-4-one - 678590 3.4.22.69 0.032 - tetraethyl 2,2'-[sulfonylbis(benzene-4,1-diyliminomethylylidene)]dipropanedioate - 681289 3.4.22.69 0.03317 - 3,4',5,7,8-pentahydroxyflavone pH 6.5, 37°C 754293 3.4.22.69 0.0353 - 2-[(4-nitrobenzyl)sulfanyl]-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile - 707708 3.4.22.69 0.0361 - 2-[3-[(2Z)-3-(2H-1,3-benzodioxol-5-yl)prop-2-enoyl]-3-hydroxy-2-oxo-2,3-dihydro-1H-indol-1-yl]acetamide pH 7.3, temperature not specified in the publication 764635 3.4.22.69 0.0362 - (4E)-1,7-bis(3,4-dihydroxyphenyl)hept-4-en-3-one pH and temperature not specified in the publication 753268 3.4.22.69 0.037 - acetyl-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO - 691242 3.4.22.69 0.037 - N-acetyl-Ser-Ala-Val-Leu-NHCH-(CH2CH2CON(CH3)2)-CHO in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.03745 - apigenin-7-O-rhamnoglucoside pH 6.5, 37°C 754293 3.4.22.69 0.03778 - 5,7-dihydroxy 4',6-dimethoxyflavone 7-rutinoside pH 6.5, 37°C 754293 3.4.22.69 0.03857 - N-[(1Z)-3-[[3-(dimethylamino)propyl]amino]-1-[5-(3-nitrophenyl)furan-2-yl]-3-oxoprop-1-en-2-yl]-4-methylbenzamide pH and temperature not specified in the publication 717343 3.4.22.69 0.04 - 2-(4,5-dihydro-1,3-thiazol-2-yl)-1-(1,3-thiazol-2-yl)ethanone - 681289 3.4.22.69 0.04 - 3-[N-(N-tert-butoxycarbonyl)-L-Leu]-1,1,1-trifluorobutan-2-one - 691222 3.4.22.69 0.04 - 3-[N-[N-tert-butoxycarbonyl-L-gamma-Glu(OtBu)-L-Ala]]-1,1,1-trifluoropropan-2-one - 691222 3.4.22.69 0.04 - curcumin - 681313 3.4.22.69 0.04 - niclosamide - 681313 3.4.22.69 0.041 - (2S)-2-([[(3S,4aR,8aS)-2-(4-bromobenzoyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.04139 - N-[(1Z)-3-[[3-(dimethylamino)propyl]amino]-1-[5-(2-nitrophenyl)furan-2-yl]-3-oxoprop-1-en-2-yl]-4-methylbenzamide pH and temperature not specified in the publication 717343 3.4.22.69 0.043 - (S)-N-((S)-1-(benzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-2-(2-(4-methoxyphenyl)acetamido)-4-methylpentanamide enzyme mutant R188I, pH and temperature not specified in the publication 731748 3.4.22.69 0.043 - 1,6-di(propan-2-yl)-N-(4-[[4-(prop-2-en-1-yl)-5-sulfanylidene-4,5-dihydro-1H-1,2,4-triazol-3-yl]methyl]-1,3-thiazol-2-yl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide mutant R188I, pH not specified in the publication, temperature not specified in the publication 752992 3.4.22.69 0.043 - 2-(3',4'-dihydroxyphenyl)-5,7-dihydroxy-3-beta-D-galactosyl-4H-chromen-4-one - 678590 3.4.22.69 0.0437 - N-[2-(2-cyanocinnamoylthio)phenyl]-2-cyanocinnamide - 691768 3.4.22.69 0.046 - esculetin-4-carboxylic acid ethyl ester - 678512 3.4.22.69 0.048 - N-(4-methyl-2-[2-[(2S)-1-oxo-3-(thiophen-2-yl)propan-2-yl]hydrazinyl]pentanoyl)valyl-N-(1-hydroxy-3,4-dioxopentan-2-yl)alaninamide in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.049 - 2-(3',4'-dihydroxyphenyl)-5,7-dihydroxy-3-beta-D-glucosyl-4H-chromen-4-one - 678590 3.4.22.69 0.05 - 3-(N-L-gamma-Glu-L-Ala)-1,1,1-trifluoropropan-2-one - 691222 3.4.22.69 0.05 - 3-[N-[N-decanoyl-L-Leu]]-4-phenyl-1,1,1-trifluorobutan-2-one - 691222 3.4.22.69 0.057 - (2S)-2-([[(3R,4aS,8aR)-2-(4-fluorophenyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-5-yl)propanal pH 7.7, 37°C 752951 3.4.22.69 0.057 - (2S)-2-([[(3S,4aR,8aS)-2-(4-fluorobenzoyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.057 - 2-(5-bromopyridin-3-yl)-1-(5-(4-chlorophenyl)furan-2-yl)-2,2-difluoroethanone - 691200 3.4.22.69 0.05835 - 4-([[4-cyclohexyl-5-(naphthalen-1-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)-1,3-thiazol-2-amine pH and temperature not specified in the publication 717343 3.4.22.69 0.061 - 2-(3',4'-dihydroxyphenyl)-5-hydroxy-3,7-di(beta-D-galactosyl)-4H-chromen-4-one - 678590 3.4.22.69 0.062 - N-(2-[2-[(2S)-1-cyclohexyl-3-oxopropan-2-yl]hydrazinyl]-4-methylpentanoyl)valyl-N-(1-hydroxy-3,4-dioxopentan-2-yl)alaninamide in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.06279 - 1-[2-(dimethylamino)ethyl]-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-4-[2-methyl-4-(2-methylpropoxy)benzoyl]-1,5-dihydro-2H-pyrrol-2-one pH and temperature not specified in the publication 717343 3.4.22.69 0.063 - (2S)-2-([[(3S,4aR,8aS)-2-(4-bromobenzoyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-5-yl)propanal pH 7.7, 37°C 752951 3.4.22.69 0.063 - 2-(1H-benzotriazol-1-yl)-N-[4-(1H-imidazol-4-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.065 - (R)-N-(E)-3',4',5'-trimethoxy-3-phenylprop-2-enoicserine(benzoyl)cyclohexylamide pH 4.0, temperature not specified in the publication 752992 3.4.22.69 0.068 - (2S)-2-([[(3S,4aR,8aS)-2-benzoyldecahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.068 - N-[4-(1H-imidazol-4-yl)phenyl]-2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)acetamide pH 7.5, 25°C 765227 3.4.22.69 0.075 - 2-(5-bromopyridin-3-yl)-1-(2-(4-chlorophenyl)oxazol-5-yl)ethanone - 691200 3.4.22.69 0.07709 - N-[(1E)-3-[(2E)-2-(4-hydroxy-3,5-dimethoxybenzylidene)hydrazinyl]-3-oxo-1-phenylprop-1-en-2-yl]benzamide pH and temperature not specified in the publication 717343 3.4.22.69 0.08 - ethyl (2E,4S)-4-[[(2R,5S)-5-[(N-tert-butyl-L-seryl)amino]-6-methyl-2-(3-methylbut-2-en-1-yl)-4-oxoheptanoyl]amino]-5-[(3S)-3-methyl-2-oxopyrrolidin-3-yl]pent-2-enoate - 678690 3.4.22.69 0.09072 - N-(furan-2-ylmethyl)-2-[[5-(morpholin-4-yl)-1,2,3,4-tetrahydropyrimido[4',5':4,5]thieno[2,3-c]isoquinolin-8-yl]sulfanyl]acetamide pH and temperature not specified in the publication 717343 3.4.22.69 0.095 - (2S)-2-([[(1S,3S,4aR,8aS)-1[butyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methylamino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.1 - (2S)-2-([[(1S,4aR,8aS)-1-[[butyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.1014 - 4-[(2,4-dimethyl-1,3-thiazol-5-yl)carbonyl]-3-hydroxy-1-[3-(morpholin-4-yl)propyl]-5-(3-nitrophenyl)-1,5-dihydro-2H-pyrrol-2-one pH and temperature not specified in the publication 717343 3.4.22.69 0.106 - 2-(1H-benzotriazol-1-yl)-N-[4-(1H-pyrazol-4-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.108 - (2S)-2-([[(3S,4aR,8aS)-2-(biphenyl-4-ylcarbonyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-5-yl)propanal pH 7.7, 37°C 752951 3.4.22.69 0.108 - (2S)-2-([[(3S,4aR,8aS)-2-([1,1'-biphenyl]-4-carbonyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.109 - 2-(1H-benzotriazol-1-yl)-N-[4-(1H-pyrazol-4-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.125 - N-[2-(3-dimethylaminopropylthio)phenyl]-2-cyanocinnamide - 691768 3.4.22.69 0.135 - (2S)-2-([[(3S,4aR,8aS)-2-([1,1'-biphenyl]-2-carbonyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.135 - (2S)-2-([[(3S,4aR,8aS)-2-([1,1'-biphenyl]-3-carbonyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.148 - 2-(1H-benzotriazol-1-yl)-N-[4-(1H-imidazol-4-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.155 - acetyl-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO - 691242 3.4.22.69 0.171 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[5-(1H-pyrazol-4-yl)-2-pyridyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.175 - (2S)-2-([[(3R,4aS,8aR)-2-(4-bromobenzoyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.175 - N-acetyl-L-threonyl-N-[(3R,4S,4aR,8aS)-3-([[(2S)-1,1-bis(ethylsulfanyl)-3-(1H-imidazol-4-yl)propan-2-yl]amino]methyl)-2-(4-bromobenzoyl)decahydroisoquinolin-4-yl]glycinamide pH 7.5, 37°C 752974 3.4.22.69 0.197 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[2-methoxy-4-(1H-pyrazol-4-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.2 - N-[(5-methyl-4,5-dihydro-1H-pyrazol-3-yl)carbonyl]-L-valyl-N-[(1S,2E)-4-ethoxy-1-[[(3S)-3-methyl-2-oxopyrrolidin-3-yl]methyl]-4-oxobut-2-en-1-yl]-L-leucinamide - 678690 3.4.22.69 0.206 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[3-methoxy-4-(1H-pyrazol-4-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.206 - N-(2-benzylthiophenyl)cinnamide - 691768 3.4.22.69 0.208 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[2-methoxy-4-(1H-pyrazol-4-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.214 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[5-(1H-pyrazol-4-yl)-2-pyridyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.215 - (S)-2-[([(3R,4aS,8aR)-2-[3-(phenylamino)-propan-1-carbonyl]decahydroisoquinolin-3-yl]methyl)amino]-3-(1H-imidazol-4-yl)-propanal pH 7.5, 37°C 753022 3.4.22.69 0.24 - (2S)-2-([[(3R,4aS,8aR)-2-([1,1'-biphenyl]-4-carbonyl)decahydroisoquinolin-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C 752951 3.4.22.69 0.25 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[4-(3-pyridyl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.26 - (2S)-2-([[(1S,3R,4aR,8aS)-1-[[butyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.27 - N-[4-(1H-pyrazol-4-yl)phenyl]-2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)acetamide pH 7.5, 25°C 765227 3.4.22.69 0.276 - (S)-2-[([(3S,4aR,8aS)-2-[3-(phenylamino)-propan-1-carbonyl]decahydroisoquinolin-3-yl]methyl)amino]-3-(1H-imidazol-4-yl)-propanal pH 7.5, 37°C 753022 3.4.22.69 0.293 - N-[2-(2-pyridylmethylthio)phenyl]cinnamide - 691768 3.4.22.69 0.3 - N-[(5-methyl-4,5-dihydro-1H-pyrazol-3-yl)carbonyl]-L-valyl-N-[(1S,2E)-4-ethoxy-1-[[(3S)-3-methyl-2-oxopyrrolidin-3-yl]methyl]-4-oxobut-2-en-1-yl]-L-phenylalaninamide - 678690 3.4.22.69 0.323 - cinanserin - 691768 3.4.22.69 0.328 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[3-methoxy-4-(1H-pyrazol-4-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.33 - N-acetyl-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CH=CHCOOEt in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 0.333 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[6-(1H-pyrazol-4-yl)-3-pyridyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.334 - N-[4-(1H-pyrazol-4-yl)phenyl]-2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)acetamide pH 7.5, 25°C 765227 3.4.22.69 0.336 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[6-(1H-pyrazol-4-yl)-3-pyridyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.347 - N-[2-(3-pyridylmethylthio)phenyl]cinnamide - 691768 3.4.22.69 0.39 - 2-(benzotriazol-1-yl)-N-[(3-chlorophenyl)methyl]-N-[4-(3-pyridyl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.42 - (2S)-2-([[(1S,4aR,8aS)-1-[[benzyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.42 - (2S)-3-(1H-imidazol-4-yl)-2-([[(1S,4aR,8aS)-1-[[methyl(prop-2-en-1-yl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.44 - (2S)-2-(8[(1R,3S,4aR,8aS)-1-[[butyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.657 - 2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)-N-[4-(2-oxo-1,2-dihydropyridin-3-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.746 - 2-(1H-benzo[d][1,2,3]triazol-1-yl)-N-(3-chlorobenzyl)-N-[4-(2-oxo-1,2-dihydropyridin-3-yl)phenyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.78 - (2S)-2-([(1R,3R,4aR,8aS)-1-8[butyl(methyl)amino]methyl]octahydro-1H-2-benzopyran-3-yl]methyl]amino)-3-(1H-imidazol-4-yl)propanal pH 7.5, 37°C, mutant enzyme R188I 752975 3.4.22.69 0.8 - ethyl (2E,4S)-4-[[(2R,5S)-6-methyl-2-(3-methylbut-2-en-1-yl)-5-[[(5-methylisoxazol-3-yl)carbonyl]amino]-4-oxoheptanoyl]amino]-5-[(3S)-3-methyl-2-oxopyrrolidin-3-yl]pent-2-enoate - 678690 3.4.22.69 0.87 - ethyl (2E,4S)-4-[[(2R,5S)-2-benzyl-6-methyl-5-[[(5-methylisoxazol-3-yl)carbonyl]amino]-4-oxoheptanoyl]amino]-5-[(3S)-3-methyl-2-oxopyrrolidin-3-yl]pent-2-enoate - 678690 3.4.22.69 0.93 - 2-(1H-benzotriazol-1-yl)-N-[4-(pyridin-3-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 0.95 - 2-(1H-benzotriazol-1-yl)-N-[4-(pyridin-3-yl)phenyl]-N-[(thiophen-3-yl)methyl]acetamide pH 7.5, 25°C 765227 3.4.22.69 2 - N-(4-methyl-2-[2-[(2S)-1-oxo-3-phenylpropan-2-yl]hydrazinyl]pentanoyl)valyl-N-(1-hydroxy-3,4-dioxopentan-2-yl)alaninamide IC50 about 2 mM, in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 3 - N-(2-[2-[(2S)-3,3-dimethyl-1-oxobutan-2-yl]hydrazinyl]-4-methylpentanoyl)valyl-N-(1-hydroxy-3,4-dioxopentan-2-yl)alaninamide IC50 about 3 mM, in 10 mM Tris-HCl buffer, pH 7.5, containing 7 mM dithiothreitol, at 37°C 717978 3.4.22.69 6 - acetyl-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO - 691242