Crystallization (Comment) | Organism |
---|---|
purified factor Xa, cleaved to des-Gla-factor Xa via limited proteolysis with chymotrypsin, is crystallized in complex with inhibitors 3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide and 3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide, within 2-4 weeks in 15-21% PEG 1500 and 10 mM CaCl2, or from 0.1 M imidazole/malate, pH 5.5, 0.5 M sodium acetate, pH 5.0, 24% PEG 3350, and 5 mM CaCl2, X-ray diffraction structure determination and analysis at 2.1-25 A | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-chloro-N-(4-chloro-2-([(4-chlorophenyl)-amino]carbonyl)phenyl)-4-[(4-methyl-1-piperazinyl)methyl]-2-thiophenecarboxamide | binding structure and mechanism | Homo sapiens | |
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide | binding structure and mechanism, good bioavailability | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P00742 | - |
- |
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 |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
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 |
---|---|---|---|---|---|
0.000000007 | - |
3-chloro-N-(4-chloro-2-([(5-chloro-2-pyridinyl)amino]carbonyl)-6-methoxyphenyl)-4-([(4,5-dihydro-2-oxazolyl)methylamino]methyl)-2-thiophenecarboxamide | - |
Homo sapiens |