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Literature summary extracted from

  • Choppin, A.; Irwin, I.; Lach, L.; McDonald, M.G.; Rettie, A.E.; Shao, L.; Becker, C.; Palme, M.P.; Paliard, X.; Bowersox, S.; Dennis, D.M.; Druzgala, P.
    Effect of tecarfarin, a novel vitamin K epoxide reductase inhibitor, on coagulation in beagle dogs (2009), Br. J. Pharmacol., 158, 1536-1547.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.17.4.4 ATI-5900 very poor VKORC1 inhibitor Canis lupus familiaris
1.17.4.4 ATI-5900 very poor VKORC1 inhibitor Homo sapiens
1.17.4.4 tecarfarin ATI-5923, non-competitive inhibitor of VKORC1 Canis lupus familiaris
1.17.4.4 tecarfarin ATI-5923, non-competitive inhibitor of VKORC1 Homo sapiens
1.17.4.4 warfarin non-competitive inhibitor of VKORC1 Canis lupus familiaris
1.17.4.4 warfarin non-competitive inhibitor of VKORC1 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.17.4.4 microsome
-
 Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
1.17.4.4 Canis lupus familiaris
-
-
-
1.17.4.4 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.17.4.4 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.17.4.4 vitamin K 2,3-epoxide + dithiothreitol
-
 Homo sapiens vitamin K + oxidized dithiothreitol
-
 ?
1.17.4.4 vitamin K 2,3-epoxide + dithiothreitol
-
 Canis lupus familiaris vitamin K + oxidized dithiothreitol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.17.4.4 vitamin K epoxide reductase
-
 Homo sapiens
1.17.4.4 vitamin K epoxide reductase
-
 Canis lupus familiaris
1.17.4.4 VKOR
-
 Homo sapiens
1.17.4.4 VKOR
-
 Canis lupus familiaris
1.17.4.4 VKORC1
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.17.4.4 0.00067
-
 in 250 mM potassium phosphate, 500 mM potassium chloride, 20% (v/v) glycerol and 0.75% (w/v) CHAPS at pH 7.85 and 25°C Homo sapiens tecarfarin
1.17.4.4 0.00084
-
 in 250 mM potassium phosphate, 500 mM potassium chloride, 20% (v/v) glycerol and 0.75% (w/v) CHAPS at pH 7.85 and 25°C Homo sapiens warfarin
1.17.4.4 0.27
-
 in 250 mM potassium phosphate, 500 mM potassium chloride, 20% (v/v) glycerol and 0.75% (w/v) CHAPS at pH 7.85 and 25°C Homo sapiens ATI-5900