Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | highly potent and selective non-amidine inhibitor, reversibel inhibition, 5fold higher affinity for the free factor Xa than for the enzyme/substrate complex, inhibition mechanism, 19fold decreased inhibitory effect in presence of phospholipid | Homo sapiens | |
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide) | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.133 | - |
S2222 | factor Xa, pH 7.5, 22°C | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
extracellular | - |
Homo sapiens | - |
- |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Ca2+ | required, part of the prothrombinase complex | Homo sapiens |
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 |
---|---|---|---|
plasma | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg-4-nitroanilide + N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O | i.e. S2222, substrate is a 1:1 mixture of the 2 components | Homo sapiens | benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg + N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline | - |
? | |
N-benzoyl-Arg-4-nitroanilide + H2O | - |
Homo sapiens | N-benzoyl-Arg + 4-nitroaniline | - |
? | |
prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | the enzyme is part of the prothrombinase complex also including phospholipid and factor Va | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
factor Xa | - |
Homo sapiens |
More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
22 | - |
assay at, room temperature | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
Factor Va | part of the prothrombinase complex | Homo sapiens | |
Phospholipids | part of the prothrombinase complex, reduce the inhibitory effect of 3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | the Gla-domainless factor Xa shows a higher Ki in presence of phospholipids | Homo sapiens | |
0.000015 | - |
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | pH 7.5, 22°C, factor Xa | Homo sapiens | |
0.000016 | - |
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | pH 7.5, 22°C, Gla-domainless factor Xa | Homo sapiens | |
0.000318 | - |
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine | Homo sapiens | |
0.000454 | - |
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | pH 7.5, 22°C, prothrombinase complex | Homo sapiens | |
0.000464 | - |
3-chloro-N-[2-[[(4-fluorophenyl)amino]carbonyl]-4-methylphenyl]benzo[b]thiophene-2-carboxamide | pH 7.5, 22°C, Gla-domainless factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine | Homo sapiens | |
0.000592 | - |
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide) | pH 7.5, 22°C, factor Xa | Homo sapiens | |
0.000649 | - |
4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide) | pH 7.5, 22°C, factor Xa in presence of 0.02 mM phospholipid vesicles containing 80% phosphocholine and 20% phosphatidylserine | Homo sapiens |