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Literature summary extracted from

  • Liang, A.M.; Light, D.R.; Kochanny, M.; Rumennik, G.; Trinh, L.; Lentz, D.; Post, J.; Morser, J.; Snider, M.
    Discovery and characterization of a potent and selective non-amidine inhibitor of human factor Xa (2003), Biochem. Pharmacol., 65, 1407-1418.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.6 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
3.4.21.6 4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide)
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.6 0.133
-
 S2222 factor Xa, pH 7.5, 22°C Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.6 extracellular
-
 Homo sapiens
-
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.21.6 Ca2+ required, part of the prothrombinase complex Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Homo sapiens
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.6 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
-
 ?
3.4.21.6 N-benzoyl-Arg-4-nitroanilide + H2O
-
 Homo sapiens N-benzoyl-Arg + 4-nitroaniline
-
 ?
3.4.21.6 prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.4.21.6 More the enzyme is part of the prothrombinase complex also including phospholipid and factor Va Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 factor Xa
-
 Homo sapiens
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.6 22
-
 assay at, room temperature Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.21.6 7.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
3.4.21.6 Factor Va part of the prothrombinase complex Homo sapiens
3.4.21.6 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]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 additional information
-
 additional information the Gla-domainless factor Xa shows a higher Ki in presence of phospholipids Homo sapiens
3.4.21.6 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
3.4.21.6 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
3.4.21.6 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
3.4.21.6 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
3.4.21.6 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
3.4.21.6 0.000592
-
 4,4'-[2,6-pyridinediylbis(oxy)]bis(benzenecarboximidamide) pH 7.5, 22°C, factor Xa Homo sapiens
3.4.21.6 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