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Literature summary for 3.4.21.6 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
Search for more literature for 3.4.21.6

Inhibitors

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

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Reaction

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
a

Source Tissue

Source Tissue Comment Organism Textmining
plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

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

Synonyms

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

pH Optimum

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

Cofactor

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 [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