Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.

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Young WB, Sprengeler P, Shrader WD, Li Y, Rai R, Verner E, Jenkins T, Fatheree P, Kolesnikov A, Janc JW, Cregar L, Elrod K, Katz B

Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.

Bioorg Med Chem Lett. 2006 Feb;16(3):710-3. Epub 2005 Oct 27.

PubMed ID

16257204 [ View in PubMed

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Abstract

Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery of potent inhibitors of fIIa, fXa, and fVIIa. SAR studies that led to the development of selective inhibitors of fXa will also be detailed.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Hemi-Babim	Prothrombin	Ki (nM)	1	N/A	N/A	Details
Hemi-Babim	Prothrombin	Ki (nM)	70000	N/A	N/A	Details