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Literature summary for 1.17.4.4 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

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

Localization

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

Organism

Organism UniProt Comment Textmining
Canis lupus familiaris
-
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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