Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | i.e. SN429 | Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
1-(3-[amino(imino)methyl]phenyl)-N-[[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
1-[3-(aminomethyl)phenyl]-N-3-fluoro-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | i.e. DPC423, highly potent, selective, and orally bioavailable inhibitor | Homo sapiens | |
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | i.e. DPC 423 | Homo sapiens | |
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide | - |
Homo sapiens | |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide | - |
Homo sapiens | |
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | i.e. SA862 | Homo sapiens | |
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
additional information | inhibitory effect, oral bioavailability and pharmakokinetic profile of DPC423 derivatives, overview | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cell surface | - |
Homo sapiens | 9986 | - |
extracellular | - |
Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
prothrombin + H2O | Homo sapiens | enzyme is responsible for the proteolysis of prothrombin to catalytically active thrombin | thrombin + ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Reaction | Comment | Organism | Reaction ID |
---|---|---|---|
selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin | scutelarin has similar specificity | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
blood | factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells | Homo sapiens | - |
endothelial cell | factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells | Homo sapiens | - |
platelet | factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? | |
prothrombin + H2O | enzyme is responsible for the proteolysis of prothrombin to catalytically active thrombin | Homo sapiens | thrombin + ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | factor Xa is part of the prothrombinase complex formed by factor Xa, nonenzymatic cofacor Va and Ca2+ on the phospholipid surface of platelets or endothelial cells | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
blood coagulation factor Xa | - |
Homo sapiens |
factor Xa | - |
Homo sapiens |
FXa | - |
Homo sapiens |
More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | - |
Homo sapiens | |
0.000000005 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.000000005 | - |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | below | Homo sapiens | |
0.000000005 | - |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | below | Homo sapiens | |
0.000000007 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide | - |
Homo sapiens | |
0.000000008 | - |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.000000008 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.000000009 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-chloro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.000000009 | - |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyridin-2-yl]-amide | - |
Homo sapiens | |
0.00000001 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-bromo-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000001 | - |
2-(3-carbamimidoyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide | - |
Homo sapiens | |
0.000000013 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.000000013 | - |
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-(2'-(methylsulfonyl))-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.000000015 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
0.00000002 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000004 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.000000041 | - |
2-(3-carbamimidoyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid [5-(2-sulfamoyl-phenyl)-pyrimidin-2-yl]-amide | - |
Homo sapiens | |
0.00000006 | - |
5-butyl-2-(3-carbamimidoyl-phenyl)-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000015 | - |
1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.00000015 | - |
3-(3-carbamimidoyl-phenyl)-isoxazole-4-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000016 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
0.00000029 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-4-bromo-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt | - |
Homo sapiens | |
0.00000036 | - |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000038 | - |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000046 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(fluoro)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.00000048 | - |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.0000008 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]4-yl]-N-methyl-1H-pyrrole-2-carboxamide trifluoroacetic acid salt | - |
Homo sapiens | |
0.00000089 | - |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (2'-methanesulfonyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.00000091 | - |
2-(3-aminomethyl-phenyl)-5-trifluoromethyl-2H-pyrazole-3-carboxylic acid (2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.0000013 | - |
1-(3-[amino(imino)methyl]phenyl)-N-[2'-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens | |
0.0000016 | - |
2-(3-aminomethyl-phenyl)-5-methyl-2H-pyrazole-3-carboxylic acid (3-fluoro-2'-sulfamoyl-biphenyl-4-yl)-amide | - |
Homo sapiens | |
0.0000027 | - |
1-[3-(aminomethyl)phenyl]-N-[2'-(aminosulfonyl)-[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide trifluoro acetic acid salt | - |
Homo sapiens | |
0.000011 | - |
1-[3-[amino(imino)methyl]phenyl]-N-[2'-(aminosulfonyl)[1,1'-biphenyl]-4-yl]-3-methyl-1H-pyrazole-5-carboxamide | - |
Homo sapiens |