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Literature summary extracted from

  • Adler, M.; Kochanny, M.J.; Ye, B.; Rumennik, G.; Light, D.R.; Biancalana, S.; Whitlow, M.
    Crystal structures of two potent nonamidine inhibitors bound to factor Xa (2002), Biochemistry, 41, 15514-15523.
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.21.6 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

EC Number Inhibitors Comment Organism Structure
3.4.21.6 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
3.4.21.6 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

EC Number Organism UniProt Comment Textmining
3.4.21.6 Homo sapiens P00742
-
-

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.6 prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?

Synonyms

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 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