Phenyltriazolinones as potent factor Xa inhibitors.

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Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR

Phenyltriazolinones as potent factor Xa inhibitors.

Bioorg Med Chem Lett. 2010 Feb 15;20(4):1373-7. doi: 10.1016/j.bmcl.2010.01.011. Epub 2010 Jan 11.

PubMed ID

20100660 [ View in PubMed

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Abstract

We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Apixaban	Coagulation factor X	Ki (nM)	0.08	N/A	N/A	Details