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Trypsin I Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
2-[(3S)-3-(Benzylsulfonylamino)-2-oxopiperidin-1-yl]-N-[(3S)-1-carbamimidoyl-2-hydroxypiperidin-3-yl]acetamideIC50791.0 [1], 1271.0 [2]
Acetylphenylalanyl-prolyl-boroarginineKi0.04 [1], 9.0 [2]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[6-methyl-2-oxo-3-(2-phenylethylamino)pyrazin-1-yl]acetamideKi1800.0 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-(benzylsulfonylamino)-6-methyl-2-oxopyridin-1-yl]acetamideKi3200.0 [1]
4-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]cyclohexane-1-carboxylic acidKi1.7 [1], 2.57 [2]
(6S,8As)-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-4-oxo-2-(3-phenylpropanoyl)-1,3,6,7,8,8a-hexahydropyrrolo[1,2-a]pyrazine-6-carboxamideIC501.0 [1]
(6S,8As)-N-[(2S)-3-(1-carbamimidoylpiperidin-3-yl)-1-oxo-1-(1,3-thiazol-2-yl)propan-2-yl]-4-oxo-2-(3-phenylpropanoyl)-1,3,6,7,8,8a-hexahydropyrrolo[1,2-a]pyrazine-6-carboxamideIC504350.0 [1], 4360.0 [2]
(6S,8As)-N-[(2S)-3-(1-carbamimidoylpiperidin-3-yl)-1-oxo-1-(1,3-thiazol-2-yl)propan-2-yl]-4-oxo-2-(3-phenylpropanoyl)-1,3,6,7,8,8a-hexahydropyrrolo[1,2-a]pyrazine-6-carboxamideKi4000.0 [1]
NafamostatIC5017.0 [1], 20.0 [2]
Naphthalene-2-carboximidamideKi7780.0 [1], 7800.0 [2]
1-[n-(Naphthalen-2-Ylsulfonyl)glycyl-4-Carbamimidoyl-D-Phenylalanyl]piperidineIC50169.0 [1], 170.0 [2]
2-(3-Carbamimidoylphenyl)-5-methyl-N-[4-(2-sulfamoylphenyl)phenyl]pyrazole-3-carboxamideKi16.0 [1]
2-{5-[Amino(iminio)methyl]-1H-indol-2-YL}-6-bromo-4-methylbenzenolateKi320.0 [1], 640.0 [2]
6-(N-Phenylcarbamyl)-2-naphthalenecarboxamidineKi325.0 [1], 330.0 [2]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-(9-hydroxyfluorene-9-carbonyl)pyrrolidine-2-carboxamideKi860.0 [1]
(2R,3R)-3-[(Biphenyl-4-carbonyl)-amino]-2-(3-carbamimidoyl-benzyl)-butyric acid methyl esterKi69.0 [1]
[5-[4-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carbonyl]oxycyclooctyl] 4-[[4-(diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carboxylateKi39000.0 [1]
Methyl 2-[3-(3-carbamimidoylphenyl)-5-[[4-(2-sulfamoylphenyl)phenyl]carbamoyl]-4H-1,2-oxazol-5-yl]acetate;2,2,2-trifluoroacetic acidKi110.0 [1]
2-[(2S)-4-Benzyl-2-(naphthalen-2-ylmethyl)-3,6-dioxopiperazin-1-yl]-N-[(2S)-3-(1-carbamimidoylpiperidin-3-yl)-1-oxo-1-(1,3-thiazol-2-yl)propan-2-yl]acetamideIC5011000.0 [1], 11100.0 [2]
3-(3-Carbamimidoylphenyl)-N-[5-(2-sulfamoylphenyl)pyridin-2-yl]-5-(tetrazol-1-ylmethyl)-4H-1,2-oxazole-5-carboxamideKi18.0 [1], 31.0 [2]
Methyl 2-[3-(3-carbamimidoylphenyl)-5-[(4-carbamimidoylphenyl)carbamoyl]-4H-1,2-oxazol-5-yl]acetateKi480.0 [1]
N-[(4-Aminocyclohexyl)methyl]-2-[3-(benzylsulfonylamino)-6-methyl-2-oxopyridin-1-yl]acetamideKi3000.0 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-(benzylsulfonylamino)-2-oxopyridin-1-yl]acetamideKi20000.0 [1]
[5-[4-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carbonyl]oxycyclooctyl] 4-(benzylcarbamoyl)piperazine-1-carboxylateKi182000.0 [1]
[5-[4-(Benzylcarbamoyl)piperazine-1-carbonyl]oxycyclooctyl] 4-(benzylcarbamoyl)piperazine-1-carboxylateKi44000.0 [1]
Methyl 2-[3-(3-carbamimidoylphenyl)-5-[[5-(2-sulfamoylphenyl)pyridin-2-yl]carbamoyl]-4H-1,2-oxazol-5-yl]acetate;2,2,2-trifluoroacetic acidKi25.0 [1], 52.0 [2]
Methyl 2-[3-(3-carbamimidoylphenyl)-5-[[5-(2-sulfamoylphenyl)pyrimidin-2-yl]carbamoyl]-4H-1,2-oxazol-5-yl]acetate;2,2,2-trifluoroacetic acidKi170.0 [1], 330.0 [2]
Tert-butyl (3S)-4-[[3-(1-aminoisoquinolin-6-yl)-1-oxo-1-piperidin-1-ylpropan-2-yl]amino]-3-[(4-methoxy-2,3,6-trimethylphenyl)sulfonylamino]-4-oxobutanoateIC50378000.0 [1]
1,4-Bis[[2-oxo-2-[4-(aminomethyl)benzylamino]ethyl]carbamoyloxymethyl]benzeneKi84000.0 [1]
3-(3-Carbamimidoylphenyl)-N-[4-(2-sulfamoylphenyl)phenyl]-5-(tetrazol-1-ylmethyl)-4H-1,2-oxazole-5-carboxamideKi45.0 [1], 91.0 [2]
2-(2-Hydroxy-3-phenyl-5-methylphenyl)-1H-indole-5-carboxamidineKi130.0 [1], 1800.0 [2]
2-[3-(Benzylsulfonylamino)-6-methyl-2-oxopyridin-1-yl]-N-[(1-carbamimidoylpiperidin-4-yl)methyl]acetamideKi570.0 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[(3R)-3,6-dimethyl-3-(2-methylpropyl)-2,8-dioxo-1,4-dihydro-1,7-naphthyridin-7-yl]acetamideKi0.24 [1], 860.0 [2]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[6-methyl-3,3-bis(2-methylpropyl)-2,8-dioxo-1,4-dihydro-1,7-naphthyridin-7-yl]acetamideKi0.27 [1], 1500.0 [2]
4-[2-(Tert-butylsulfamoyl)phenyl]-N-[(1R)-4-(diaminomethylideneamino)-1-[(2S,6R)-2,9,9-trimethyl-3,5-dioxa-4-boratricyclo[6.1.1.02,6]decan-4-yl]butyl]-2-methylbenzamideKi0.7 [1]
[5-[4-[[4-(Diaminomethylideneamino)phenyl]methylcarbamoyl]piperazine-1-carbonyl]oxycyclooctyl] 4-[(4-aminocyclohexyl)methylcarbamoyl]piperazine-1-carboxylateKi141000.0 [1], 171000.0 [2]
N-[(2S)-3-(1-Carbamimidoylpiperidin-3-yl)-1-oxo-1-(1,3-thiazol-2-yl)propan-2-yl]-2-[(2S)-2-(naphthalen-2-ylmethyl)-3,6-dioxo-4-(3-phenylpropyl)piperazin-1-yl]acetamideIC5027000.0 [1]
N-[(2S)-3-(1-Carbamimidoylpiperidin-3-yl)-1-oxo-1-(1,3-thiazol-2-yl)propan-2-yl]-2-[(2S)-2-(naphthalen-2-ylmethyl)-3,6-dioxo-4-(3-phenylpropyl)piperazin-1-yl]acetamideKi13.5 [1]
2-[3-(Benzylsulfonylamino)-2-oxopyridin-1-yl]-N-[(3S)-1-carbamimidoyl-2-hydroxypiperidin-3-yl]acetamideIC5026.2 [1]
2-[(3S)-3-(Benzylsulfonylamino)-2-oxoazepan-1-yl]-N-[(3S)-1-carbamimidoyl-2-hydroxypiperidin-3-yl]acetamideIC50101.0 [1], 151.8 [2]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2,2-dimethyl-3-oxo-3-[(2-oxo-1H-pyridin-3-yl)amino]propyl]thiophene-2-carboxylateKi4.54 [1]
(3S)-1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]pyrrolidine-3-carboxylic acidKi1.33 [1], 2.0 [2]
(2S)-2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-2-(4-hydroxyphenyl)acetic acidKi0.96 [1], 1.14 [2]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]butanedioic acidKi1.04 [1]
(2S)-2-[[1-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]cyclobutanecarbonyl]amino]butanedioic acidKi0.61 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]acetic acidKi0.42 [1]
(2S)-2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-3-hydroxypropanoic acidKi0.75 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]-prop-2-enylamino]acetic acidKi0.5 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-2-methylpropanoic acidKi0.95 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]-propylamino]acetic acidKi1.5 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-3-hydroxypropanoic acidKi1.78 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-3-methylbutanoic acidKi5.18 [1]
3-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]propanoic acidKi2.5 [1]
2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoic acidKi2.49 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]butanoic acidKi1.93 [1]
2-[(2S)-1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]pyrrolidin-2-yl]acetic acidKi3.88 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]pentanedioic acidKi1.96 [1]
(2S)-4-Amino-2-[[2-[[5-(4-carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-4-oxobutanoic acidKi1.69 [1]
5-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-2-hydroxybenzoic acidKi0.92 [1]
1-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]cyclobutane-1-carboxylic acidKi1.49 [1]
4-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-4-(2-carboxyethyl)heptanedioic acidKi1.59 [1]
5-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]benzene-1,3-dicarboxylic acidKi0.49 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2,2-dimethyl-3-oxo-3-[2-(2H-tetrazol-5-yl)ethylamino]propyl]thiophene-2-carboxylateKi1.6 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2,2-dimethyl-3-oxo-3-(2H-tetrazol-5-ylmethylamino)propyl]thiophene-2-carboxylateKi0.75 [1]
5-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]benzene-1,3-dicarboxylic acidKi1.58 [1]
4-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]phthalic acidKi0.21 [1]
1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]azetidine-3-carboxylic acidKi1.85 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]-prop-2-enylamino]ethanesulfonic acidKi3.17 [1]
(2S)-2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-3-methylbutanoic acidKi2.02 [1]
2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]-methylamino]acetic acidKi1.76 [1]
(2S)-2-[[1-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]cyclopentanecarbonyl]amino]butanedioic acidKi4.1 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2-ethyl-2-(2H-tetrazol-5-ylmethylcarbamoyl)butyl]thiophene-2-carboxylateKi3.54 [1]
2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]-methylamino]acetic acidKi1.33 [1]
(2S)-1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]pyrrolidine-2-carboxylic acidKi1.69 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-3-hydroxybutanoic acidKi1.74 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-3-phenylpropanoic acidKi8.3 [1]
(2S)-1-[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]pyrrolidine-2-carboxylic acidKi3.57 [1]
2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]-propylamino]acetic acidKi7.91 [1]
1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]piperidine-4-carboxylic acidKi3.1 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]propanoic acidKi1.67 [1]
(2S)-2-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]pentanoic acidKi3.84 [1]
4-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]butanoic acidKi2.73 [1]
4-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]benzoic acidKi2.89 [1]
3-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]benzoic acidKi0.7 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2-ethyl-2-[[(3S)-5-oxooxolan-3-yl]carbamoyl]butyl]thiophene-2-carboxylateKi2.73 [1]
(2S)-2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-2-cyclohexylacetic acidKi3.07 [1]
(2S)-2-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]-2-phenylacetic acidKi1.45 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[2,2-dimethyl-3-oxo-3-(pyridin-3-ylamino)propyl]thiophene-2-carboxylateKi3.6 [1]
(2S)-5-Amino-2-[[2-[[5-(4-carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]-5-oxopentanoic acidKi3.88 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[3-[(6-methoxypyridin-3-yl)amino]-2,2-dimethyl-3-oxopropyl]thiophene-2-carboxylateKi3.36 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[3-(3,3-difluoroazetidin-1-yl)-2,2-dimethyl-3-oxopropyl]thiophene-2-carboxylateKi3.89 [1]
2-[4-[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]phenyl]acetic acidKi3.35 [1]
2-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]-3,4-dihydro-1H-isoquinoline-7-carboxylic acidKi3.49 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[3-[(2-methoxypyridin-3-yl)amino]-2,2-dimethyl-3-oxopropyl]thiophene-2-carboxylateKi1.87 [1]
(2S)-2-Amino-5-[[2-[[5-(4-carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]pentanoic acidKi5.78 [1]
4-[[[2-[[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]methyl]-2-ethylbutanoyl]amino]methyl]benzoic acidKi9.27 [1]
(4-Carbamimidoyl-2-fluorophenyl) 5-[3-[(6-fluoropyridin-3-yl)amino]-2,2-dimethyl-3-oxopropyl]thiophene-2-carboxylateKi3.3 [1]
1-[[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]cyclopropane-1-carboxylic acidKi1.01 [1]
Dimethyl 5-[[3-[5-(4-carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]amino]benzene-1,3-dicarboxylateKi1.02 [1]
(2S)-1-[3-[5-(4-Carbamimidoyl-2-fluorophenoxy)carbonylthiophen-2-yl]-2,2-dimethylpropanoyl]aziridine-2-carboxylic acidKi0.96 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Trypsin I Inhibitors (IC50, Ki)." AAT Bioquest, Inc.22 Dec2024https://www.aatbio.com/data-sets/trypsin-i-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024December 22). Quest Database™ Trypsin I Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/trypsin-i-inhibitors-ic50-ki.
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