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Thrombin Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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▼
ArgatrobanIC5038.0 [1]
ArgatrobanKi19.0 [1]
DabigatranIC502.61 [1]
DabigatranKi4.5 [1], 6.3 [2]
EfegatranIC5023.0 [1]
EfegatranKi5.5 [1], 7.0 [2], 10.0 [3], 18.0 [4]
MelagatranIC5069.2 [1]
MelagatranKi1.2 [1], 1.3 [2], 2.0 [3]
RazaxabanKi540.0 [1], 6300.0 [2]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[6-methyl-2-oxo-3-(2-phenylethylamino)pyrazin-1-yl]acetamideIC500.8 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[6-methyl-2-oxo-3-(2-phenylethylamino)pyrazin-1-yl]acetamideKi0.8 [1]
(2S)-3-(7-Carbamimidoylnaphthalen-2-yl)-2-[4-[(3S)-1-ethanimidoylpyrrolidin-3-yl]oxyphenyl]propanoic acidIC50100000.0 [1], 2000000.0 [2]
(2S)-3-(7-Carbamimidoylnaphthalen-2-yl)-2-[4-[(3S)-1-ethanimidoylpyrrolidin-3-yl]oxyphenyl]propanoic acidKi2000.0 [1], 5000.0 [2], 2000000.0 [3]
1-[n-(Naphthalen-2-Ylsulfonyl)glycyl-4-Carbamimidoyl-D-Phenylalanyl]piperidineIC50200.0 [1], 690.0 [2]
1-[n-(Naphthalen-2-Ylsulfonyl)glycyl-4-Carbamimidoyl-D-Phenylalanyl]piperidineKi4.0 [1], 6.0 [2], 6.5 [3]
(2S)-N-[(2S)-1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideIC5023.0 [1], 29.0 [2], 32.0 [3]
(2S)-N-[(2S)-1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi0.18 [1], 0.19 [2], 0.2 [3]
Sodium;[3-ethoxycarbonyl-2-[[3-ethoxycarbonyl-2-methyl-6-(2-phenylethoxy)-1-benzofuran-5-yl]oxymethyl]-6-methoxy-1-benzofuran-5-yl] sulfateIC501600.0 [1]
Sodium;[6-(cyclohexylmethoxy)-3-ethoxycarbonyl-2-[(3-ethoxycarbonyl-2-methyl-6-phenylmethoxy-1-benzofuran-5-yl)oxymethyl]-1-benzofuran-5-yl] sulfateIC502600.0 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-(benzylsulfonylamino)-6-methyl-2-oxopyridin-1-yl]acetamideKi0.5 [1]
Unii-IF979jqu3SKi0.38 [1], 0.4 [2]
Methyl-phe-pro-amino-cyclohexylglycineIC506.0 [1]
Methyl-phe-pro-amino-cyclohexylglycineKi4.9 [1], 5.0 [2]
BenzamidineKi300.0 [1], 1240.0 [2], 220000.0 [3], 258000.0 [4]
InogatranIC5017.0 [1], 1300.0 [2], 22400.0 [3]
InogatranKi15.0 [1]
Acetylphenylalanyl-prolyl-boroarginineKi0.04 [1]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-[(2R)-2-amino-3,3-diphenylpropanoyl]pyrrolidine-2-carboxamideIC500.1 [1]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-[(2R)-2-amino-3,3-diphenylpropanoyl]pyrrolidine-2-carboxamideKi0.1 [1]
Thrombin Inhibitor 2Ki5.2 [1]
(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-carboxamideIC505.0 [1]
(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-carboxamideKi0.6 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-(1-methylimidazol-2-yl)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideIC501500.0 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-(1-methylimidazol-2-yl)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi50.0 [1], 200.0 [2]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideIC5019.0 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi2.1 [1], 3.6 [2]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-pyridin-2-ylpentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideIC50930.0 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-pyridin-2-ylpentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi85.0 [1]
2-[(3S)-3-(Benzylsulfonylamino)-2-oxopiperidin-1-yl]-N-[(3S)-1-carbamimidoyl-2-hydroxypiperidin-3-yl]acetamideIC506.2 [1]
2-[(3S)-3-(Benzylsulfonylamino)-2-oxopiperidin-1-yl]-N-[(3S)-1-carbamimidoyl-2-hydroxypiperidin-3-yl]acetamideKi1.0 [1]
2-[(7-Carbamimidoylnaphthalen-2-yl)methyl-[4-(1-ethanimidoylpiperidin-4-yl)oxyphenyl]sulfamoyl]acetic acidIC507.7 [1]
2-[(7-Carbamimidoylnaphthalen-2-yl)methyl-[4-(1-ethanimidoylpiperidin-4-yl)oxyphenyl]sulfamoyl]acetic acidKi10000.0 [1], 100000.0 [2]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamideKi6000.0 [1]
4-[(Z)-[(3Z)-3-[(4-Carbamimidoylphenyl)methylidene]-2-oxocycloheptylidene]methyl]benzenecarboximidamideKi430.0 [1], 530.0 [2]
Cyclotheonamide AIC5023.0 [1], 1500.0 [2]
Cyclotheonamide AKi1.0 [1], 180.0 [2]
2-(3-Carbamimidoylphenyl)-5-methyl-N-[4-(2-sulfamoylphenyl)phenyl]pyrazole-3-carboxamideKi300.0 [1]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-(9-hydroxyfluorene-9-carbonyl)pyrrolidine-2-carboxamideIC504.0 [1]
(2S)-N-[(4-Aminocyclohexyl)methyl]-1-(9-hydroxyfluorene-9-carbonyl)pyrrolidine-2-carboxamideKi1.5 [1]
1-[[5-(5-Chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-(1-propan-2-ylpiperidin-4-yl)indole-2-carboxamideIC50420.0 [1]
1-[[5-(5-Chlorothiophen-2-yl)-1,2-oxazol-3-yl]methyl]-N-(1-propan-2-ylpiperidin-4-yl)indole-2-carboxamideKi2760.0 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-[(2,2-difluoro-2-pyridin-2-ylethyl)amino]-6-methyl-2-oxopyrazin-1-yl]acetamideIC500.04 [1]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-[(2,2-difluoro-2-pyridin-2-ylethyl)amino]-6-methyl-2-oxopyrazin-1-yl]acetamideKi0.04 [1]
4-[2-(3-Benzenesulfonylamino-phenoxy)-ethylamino]-pyridiniumKi23.0 [1], 300.0 [2], 316.0 [3]
2-[6-Chloro-3-[[2,2-difluoro-2-(1-oxidopyridin-1-ium-2-yl)ethyl]amino]-2-oxopyrazin-1-yl]-N-[[5-chloro-2-(tetrazol-1-yl)phenyl]methyl]acetamideKi0.0 [1]
(2S)-N-[(2S)-1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2S)-3-hydroxy-2-(naphthalen-1-ylsulfonylamino)propanoyl]pyrrolidine-2-carboxamideIC50110.0 [1]
(2S)-N-[(2S)-1-(1,3-Benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2S)-3-hydroxy-2-(naphthalen-1-ylsulfonylamino)propanoyl]pyrrolidine-2-carboxamideKi0.78 [1], 0.8 [2], 10.0 [3]
2-[[(2S)-1-[(2S)-2-[(5-Carbamimidoylthiophen-2-yl)methylcarbamoyl]pyrrolidin-1-yl]-1-oxo-3,3-diphenylpropan-2-yl]amino]acetic acidIC502.1 [1], 5.0 [2], 16.0 [3]
2-[[(2S)-1-[(2S)-2-[(5-Carbamimidoylthiophen-2-yl)methylcarbamoyl]pyrrolidin-1-yl]-1-oxo-3,3-diphenylpropan-2-yl]amino]acetic acidKi0.02 [1]
beta-SitosterolIC501500000.0 [1]
beta-SitosterolKi267.2 [1]
BetrixabanIC5010000.0 [1], 18000.0 [2]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide;hydrochlorideIC50100000.0 [1]
2-[3-(Aminomethyl)phenyl]-N-[2-fluoro-4-(2-methylsulfonylphenyl)phenyl]-5-(trifluoromethyl)pyrazole-3-carboxamide;hydrochlorideKi6000.0 [1]
Wx-uk1 free baseKi490.0 [1]
(3S)-1-Carbamimidoyl-N-[[(2S)-1-[(2S)-3-hydroxy-2-(naphthalen-2-ylsulfonylamino)propanoyl]pyrrolidin-2-yl]methyl]piperidine-3-carboxamideIC5018.0 [1]
(3S)-1-Carbamimidoyl-N-[[(2S)-1-[(2S)-3-hydroxy-2-(naphthalen-2-ylsulfonylamino)propanoyl]pyrrolidin-2-yl]methyl]piperidine-3-carboxamideKi3.44 [1], 3.6 [2]
4-[2-(3-Benzenesulfonylamino-5-methyl-phenoxy)-ethylamino]-pyridiniumKi23.0 [1], 25.0 [2]
2-(2-Hydroxyphenyl)-1H-indole-5-carboxamidineIC5038000.0 [1]
2-(2-Hydroxyphenyl)-1H-indole-5-carboxamidineKi13000.0 [1]
N-[2-(Diaminomethylideneamino)oxyethyl]-2-[6-methyl-3-[(3-methylphenyl)sulfonylamino]-2-oxopyridin-1-yl]acetamideIC504.0 [1]
N-[2-(Diaminomethylideneamino)oxyethyl]-2-[6-methyl-3-[(3-methylphenyl)sulfonylamino]-2-oxopyridin-1-yl]acetamideKi4.0 [1]
6-(N-Phenylcarbamyl)-2-naphthalenecarboxamidineIC5056000.0 [1]
6-(N-Phenylcarbamyl)-2-naphthalenecarboxamidineKi5600.0 [1], 5640.0 [2]
3-[6-(3-Carbamimidoylphenoxy)-3,5-difluoro-4-methylpyridin-2-yl]oxybenzenecarboximidamideKi22000.0 [1]
2,7-Bis(4-amidinobenzylidene)cycloheptanoneKi530.0 [1], 6200.0 [2]
3-[[(3S)-3-[(7-Methoxynaphthalen-2-yl)sulfonylamino]-2-oxopyrrolidin-1-yl]methyl]benzenecarboximidamideKi1400.0 [1], 1430.0 [2]
3-Amino-5-[1-[2-[(4-carbamimidoylphenyl)methylamino]-2-oxoethyl]-3-chloro-6-oxo-5-(propan-2-ylamino)pyrazin-2-yl]benzoic acidIC50100000.0 [1]
2,6-Bis(3-amidinophenoxy)pyridine-4-carboxylic acidKi27000.0 [1]
3-[6-(3-Carbamimidoyl-phenoxy)-3,5-difluoro-4-methyl-pyridin-2-yloxy]-N,N-dimethyl-benzamideKi5000.0 [1], 15000.0 [2]
2-[6-Cyano-3-[(2,2-difluoro-2-pyridin-2-ylethyl)amino]-2-oxopyrazin-1-yl]-N-[(3-fluoropyridin-2-yl)methyl]acetamideIC502.3 [1]
2-[6-Cyano-3-[(2,2-difluoro-2-pyridin-2-ylethyl)amino]-2-oxopyrazin-1-yl]-N-[(3-fluoropyridin-2-yl)methyl]acetamideKi2.3 [1]
2-Chlorobenzenesulfonic acid 3-methyl-5-(1-amidinopiperidine-4-ylmethoxy)phenyl esterKi4.6 [1]
(2S)-2-[[(2R)-2-(Benzylsulfonylamino)-3-phenylpropanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]-3-phenylpropanamideIC504000.0 [1]
(2R)-2-(Benzylsulfonylamino)-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-1-oxo-3-pyridin-3-ylpropan-2-yl]-3-phenylpropanamideIC50100000.0 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-oxo-1-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)pentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi3.4 [1]
(2S)-N-[(2S)-1-(1-Benzothiophen-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi2400.0 [1]
(2S)-N-[(2S)-5-(Diaminomethylideneamino)-1-(1-methylbenzimidazol-2-yl)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi8.1 [1]
2-[3-(Aminomethyl)phenyl]-5-methyl-N-[4-(2-sulfamoylphenyl)phenyl]pyrazole-3-carboxamideKi6000.0 [1], 21000.0 [2]
N-[(4-Carbamimidoylphenyl)methyl]-2-[5-chloro-2-oxo-6-phenyl-3-(2-phenylethylamino)pyrazin-1-yl]acetamideIC50150.0 [1], 160.0 [2]
(S)-3-(4-Aminomethyl-phenyl)-N-cyclopentyl-N-methyl-2-(naphthalene-2-sulfonylamino)-propionamideKi18.3 [1], 50.0 [2]
N-[(6-Amino-2-methylpyridin-3-yl)methyl]-2-[3-[(2,2-difluoro-2-phenylethyl)amino]-6-methyl-2-oxopyrazin-1-yl]acetamideKi0.1 [1]
(2S)-N-[(2S)-1-(1,3-Benzoxazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-1-[(2R)-2-(methylamino)-3-phenylpropanoyl]pyrrolidine-2-carboxamideKi3.8 [1], 6.2 [2]
(2S)-2-[[(2R)-2-(Benzylsulfonylamino)-3-phenylpropanoyl]amino]-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]butanediamideIC5060000.0 [1]
(2R)-2-(Benzylsulfonylamino)-N-[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxo-1-(1,3-thiazol-2-yl)pentan-2-yl]amino]-3-(2-fluorophenyl)-1-oxopropan-2-yl]-3-phenylpropanamideIC5030000.0 [1]
(S)-3-(4-Carbamimidoyl-phenyl)-N-cyclopentyl-N-methyl-2-(naphthalene-2-sulfonylamino)-propionamideKi6.8 [1]
2-Chlorobenzenesulfonic acid 3-methyl-5-(4-guanidinobutoxy)phenyl esterKi1.3 [1], 13.0 [2]
N-(3-Chloro-benzyl)-2-(6-methyl-2-oxo-3-phenylmethanesulfonylamino-2H-pyridin-1-yl)-acetamideKi7.0 [1], 7.1 [2]
2-[6-Chloro-3-[[2,2-difluoro-2-(1-oxidopyridin-1-ium-2-yl)ethyl]amino]-2-oxopyrazin-1-yl]-N-[(2-fluorophenyl)methyl]acetamideKi2.3 [1]
(2S)-3-(7-Carbamimidoylnaphthalen-2-yl)-2-[4-[(3S)-1-ethanimidoylpyrrolidin-3-yl]oxyphenyl]propanoic acid;hydrochlorideIC5010000.0 [1]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Thrombin Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 21 Nov. 2024, https://www.aatbio.com/data-sets/thrombin-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, November 21). Quest Database™ Thrombin Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/thrombin-inhibitors-ic50-ki.
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