Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(3-allylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 700 nM | Homo sapiens | |
2-(3-benzylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 770 nM | Homo sapiens | |
2-(3-benzylsulfanyl-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.0064 mM | Homo sapiens | |
2-(3-butylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.0032 mM | Homo sapiens | |
2-[3-(2-amino-ethylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.0021 mM | Homo sapiens | |
2-[3-(3-amino-propylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 890 nM | Homo sapiens | |
2-[3-(4-amino-butylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 980 nM | Homo sapiens | |
2-[3-(4-tert-butyl-cyclohexylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.003 mM | Homo sapiens | |
2-[3-(adamantan-1-ylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.013 mM | Homo sapiens | |
2-[6-(3-acetylamino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.00161 mM | Homo sapiens | |
2-[6-(3-amino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 70 nM | Homo sapiens | |
2-[6-(3-amino-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 20 nM | Homo sapiens | |
2-[6-(3-amino-phenyl)-5-chloro-3-isopropylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 20 nM | Homo sapiens | |
2-[6-(3-bromo-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | pH 8.0, IC50: 0.0042 mM | Homo sapiens | |
3-amino-5-[1-[2-([4-[amino(imino)methyl]benzyl]amino)-2-oxoethyl]-3-chloro-5-(isopropylamino)-6-oxo-1,6-dihydropyrazin-2-yl]benzoic acid | pH 8.0, IC50: 16 nM, potent and highly selective inhibitor, selectivity versus factor Xa and thrombin | Homo sapiens | |
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid | pH 8.0, IC50: 360 nM | Homo sapiens | |
3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid methyl ester | pH 8.0, IC50: 780 nM | Homo sapiens | |
N-(3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-6-oxo-5-phenethylamino-1,6-dihydro-pyrazin-2-yl]-phenyl)-2,2,2-trifluoro-acetamide | pH 8.0, IC50: 450 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 340 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-m-tolyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.001 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-o-tolyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 430 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-p-tolyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.00414 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 630 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-phenylamino-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.0112 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-prop-2-ynylamino-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 720 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-propylamino-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 400 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-pyrrolidin-1-yl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.0063 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclobutylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 400 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclohexylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.0014 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-ethylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 400 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-isopropylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 200 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-methylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 700 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-ethyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.00345 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-methyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.00428 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(2-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0027 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(3-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0029 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(1-propyl-butylamino)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0018 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-phenyl-propylamino)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0126 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-trifluoromethyl-benzylamino)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0063 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(4-phenyl-butylamino)-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0041 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1,1-dioxo-tetrahydro-16-thiophen-3-ylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.001 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0098 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 430 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 840 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-pentylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 900 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0038 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-dimethylamino-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0209 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-hydroxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 500 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-methoxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 880 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-morpholin-4-yl-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.008 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.006 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-dimethylamino-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0176 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-hydroxy-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 500 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-chloro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0043 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-hydroxy-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 600 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(6-hydroxy-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 470 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(isopropyl-methyl-amino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0091 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(2-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 340 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(3-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 200 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.003 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0018 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0016 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.00198 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-dimethylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0012 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0023 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methanesulfonylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 600 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0052 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 600 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-nitro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.00252 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.00888 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.0081 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | pH 8.0, IC50: 0.02345 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-2-oxo-6-phenyl-3-[2-(3-trifluoromethyl-phenyl)-ethylamino]-2H-pyrazin-1-yl}-acetamide | pH 8.0, IC50: 0.03 mM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(3-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide | pH 8.0, IC50: 180 nM | Homo sapiens | |
N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(4-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide | pH 8.0, IC50: 600 nM | Homo sapiens | |
N-(5-carbamimidoyl-pyridin-2-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.0167 mM | Homo sapiens | |
N-(6-carbamimidoyl-pyridin-3-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | pH 8.0, IC50: 0.0014 mM | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-methylsulfonyl-D-Phe-Gly-Arg-p-nitroanilide + H2O | - |
Homo sapiens | N-methylsulfonyl-D-Phe-Gly-Arg + p-nitroaniline | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000016 | - |
pH 8.0, IC50: 16 nM, potent and highly selective inhibitor, selectivity versus factor Xa and thrombin | Homo sapiens | 3-amino-5-[1-[2-([4-[amino(imino)methyl]benzyl]amino)-2-oxoethyl]-3-chloro-5-(isopropylamino)-6-oxo-1,6-dihydropyrazin-2-yl]benzoic acid | |
0.00002 | - |
pH 8.0, IC50: 20 nM | Homo sapiens | 2-[6-(3-amino-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00002 | - |
pH 8.0, IC50: 20 nM | Homo sapiens | 2-[6-(3-amino-phenyl)-5-chloro-3-isopropylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00007 | - |
pH 8.0, IC50: 70 nM | Homo sapiens | 2-[6-(3-amino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00018 | - |
pH 8.0, IC50: 180 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(3-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide | |
0.0002 | - |
pH 8.0, IC50: 200 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(3-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide | |
0.0002 | - |
pH 8.0, IC50: 200 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-isopropylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.00034 | - |
pH 8.0, IC50: 340 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-cyclobutylamino-6-(2-hydroxy-phenyl)-2-oxo-2H-pyrazin-1-yl]-acetamide | |
0.00034 | - |
pH 8.0, IC50: 340 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.00036 | - |
pH 8.0, IC50: 360 nM | Homo sapiens | 3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid | |
0.0004 | - |
pH 8.0, IC50: 400 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-ethylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0004 | - |
pH 8.0, IC50: 400 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-propylamino-2H-pyrazin-1-yl)-acetamide | |
0.0004 | - |
pH 8.0, IC50: 400 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclobutylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.00043 | - |
pH 8.0, IC50: 430 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-o-tolyl-2H-pyrazin-1-yl)-acetamide | |
0.00043 | - |
pH 8.0, IC50: 430 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.00045 | - |
pH 8.0, IC50: 450 nM | Homo sapiens | N-(3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-6-oxo-5-phenethylamino-1,6-dihydro-pyrazin-2-yl]-phenyl)-2,2,2-trifluoro-acetamide | |
0.00047 | - |
pH 8.0, IC50: 470 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(6-hydroxy-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0005 | - |
pH 8.0, IC50: 500 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-hydroxy-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0006 | - |
pH 8.0, IC50: 600 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0006 | - |
pH 8.0, IC50: 600 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methanesulfonylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0006 | - |
pH 8.0, IC50: 600 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-{5-chloro-3-[2-(4-chloro-phenyl)-ethylamino]-2-oxo-6-phenyl-2H-pyrazin-1-yl}-acetamide | |
0.0006 | - |
pH 8.0, IC50: 600 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-hydroxy-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.00063 | - |
pH 8.0, IC50: 630 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0007 | - |
pH 8.0, IC50: 700 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-methylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0007 | - |
pH 8.0, IC50: 700 nM | Homo sapiens | 2-(3-allylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00072 | - |
pH 8.0, IC50: 720 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-prop-2-ynylamino-2H-pyrazin-1-yl)-acetamide | |
0.00077 | - |
pH 8.0, IC50: 770 nM | Homo sapiens | 2-(3-benzylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00078 | - |
pH 8.0, IC50: 780 nM | Homo sapiens | 3-[1-[(4-carbamimidoyl-benzylcarbamoyl)-methyl]-3-chloro-5-isopropylamino-6-oxo-1,6-dihydro-pyrazin-2-yl]-benzoic acid methyl ester | |
0.00084 | - |
pH 8.0, IC50: 840 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-butylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.00089 | - |
pH 8.0, IC50: 890 nM | Homo sapiens | 2-[3-(3-amino-propylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.0009 | - |
pH 8.0, IC50: 900 nM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-methyl-pentylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.00098 | - |
pH 8.0, IC50: 980 nM | Homo sapiens | 2-[3-(4-amino-butylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.001 | - |
pH 8.0, IC50: 0.001 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-m-tolyl-2H-pyrazin-1-yl)-acetamide | |
0.001 | - |
pH 8.0, IC50: 0.001 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1,1-dioxo-tetrahydro-16-thiophen-3-ylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0012 | - |
pH 8.0, IC50: 0.0012 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-dimethylamino-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0014 | - |
pH 8.0, IC50: 0.0014 mM | Homo sapiens | N-(6-carbamimidoyl-pyridin-3-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0014 | - |
pH 8.0, IC50: 0.0014 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-3-cyclohexylamino-2-oxo-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0016 | - |
pH 8.0, IC50: 0.0016 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.00161 | - |
pH 8.0, IC50: 0.00161 mM | Homo sapiens | 2-[6-(3-acetylamino-phenyl)-5-chloro-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.0018 | - |
pH 8.0, IC50: 0.0018 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0018 | - |
pH 8.0, IC50: 0.0018 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(1-propyl-butylamino)-2H-pyrazin-1-yl]-acetamide | |
0.00198 | - |
pH 8.0, IC50: 0.00198 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0021 | - |
pH 8.0, IC50: 0.0021 mM | Homo sapiens | 2-[3-(2-amino-ethylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.0023 | - |
pH 8.0, IC50: 0.0023 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.00252 | - |
pH 8.0, IC50: 0.00252 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-nitro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0027 | - |
pH 8.0, IC50: 0.0027 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(2-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide | |
0.0029 | - |
pH 8.0, IC50: 0.0029 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-3-phenethylamino-6-(3-trifluoromethyl-phenyl)-2H-pyrazin-1-yl]-acetamide | |
0.003 | - |
pH 8.0, IC50: 0.003 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(2-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.003 | - |
pH 8.0, IC50: 0.003 mM | Homo sapiens | 2-[3-(4-tert-butyl-cyclohexylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.0032 | - |
pH 8.0, IC50: 0.0032 mM | Homo sapiens | 2-(3-butylamino-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00345 | - |
pH 8.0, IC50: 0.00345 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-ethyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide | |
0.0038 | - |
pH 8.0, IC50: 0.0038 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0041 | - |
pH 8.0, IC50: 0.0041 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(4-phenyl-butylamino)-2H-pyrazin-1-yl]-acetamide | |
0.00414 | - |
pH 8.0, IC50: 0.00414 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-3-phenethylamino-6-p-tolyl-2H-pyrazin-1-yl)-acetamide | |
0.0042 | - |
pH 8.0, IC50: 0.0042 mM | Homo sapiens | 2-[6-(3-bromo-phenyl)-5-chloro-3-cyclobutylamino-2-oxo-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.00428 | - |
pH 8.0, IC50: 0.00428 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-6-methyl-2-oxo-3-phenethylamino-2H-pyrazin-1-yl)-acetamide | |
0.0043 | - |
pH 8.0, IC50: 0.0043 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(4-chloro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0052 | - |
pH 8.0, IC50: 0.0052 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(3-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.006 | - |
pH 8.0, IC50: 0.006 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3,5-difluoro-benzylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0063 | - |
pH 8.0, IC50: 0.0063 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-trifluoromethyl-benzylamino)-2H-pyrazin-1-yl]-acetamide | |
0.0063 | - |
pH 8.0, IC50: 0.0063 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-pyrrolidin-1-yl-2H-pyrazin-1-yl)-acetamide | |
0.0064 | - |
pH 8.0, IC50: 0.0064 mM | Homo sapiens | 2-(3-benzylsulfanyl-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl)-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.008 | - |
pH 8.0, IC50: 0.008 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-morpholin-4-yl-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0081 | - |
pH 8.0, IC50: 0.0081 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-fluoro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.00888 | - |
pH 8.0, IC50: 0.00888 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-chloro-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.0091 | - |
pH 8.0, IC50: 0.0091 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(isopropyl-methyl-amino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0098 | - |
pH 8.0, IC50: 0.0098 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(1-ethyl-hexylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0112 | - |
pH 8.0, IC50: 0.0112 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-(5-chloro-2-oxo-6-phenyl-3-phenylamino-2H-pyrazin-1-yl)-acetamide | |
0.0126 | - |
pH 8.0, IC50: 0.0126 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-2-oxo-6-phenyl-3-(3-phenyl-propylamino)-2H-pyrazin-1-yl]-acetamide | |
0.013 | - |
pH 8.0, IC50: 0.013 mM | Homo sapiens | 2-[3-(adamantan-1-ylamino)-5-chloro-2-oxo-6-phenyl-2H-pyrazin-1-yl]-N-(4-carbamimidoyl-benzyl)-acetamide | |
0.0167 | - |
pH 8.0, IC50: 0.0167 mM | Homo sapiens | N-(5-carbamimidoyl-pyridin-2-ylmethyl)-2-(2-oxo-3-phenethylamino-6-phenyl-2H-pyrazin-1-yl)-acetamide | |
0.0176 | - |
pH 8.0, IC50: 0.0176 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(3-dimethylamino-propylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.0209 | - |
pH 8.0, IC50: 0.0209 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-dimethylamino-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
0.02345 | - |
pH 8.0, IC50: 0.02345 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-6-(4-methoxy-phenyl)-2-oxo-3-phenethylamino-2H-pyrazin-1-yl]-acetamide | |
0.03 | - |
pH 8.0, IC50: 0.03 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-{5-chloro-2-oxo-6-phenyl-3-[2-(3-trifluoromethyl-phenyl)-ethylamino]-2H-pyrazin-1-yl}-acetamide | |
500 | - |
pH 8.0, IC50: 500 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-hydroxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide | |
880 | - |
pH 8.0, IC50: 880 mM | Homo sapiens | N-(4-carbamimidoyl-benzyl)-2-[5-chloro-3-(2-methoxy-ethylamino)-2-oxo-6-phenyl-2H-pyrazin-1-yl]-acetamide |