| Literature DB >> 10853669 |
Z Zhao1, D O Arnaiz, B Griedel, S Sakata, J L Dallas, M Whitlow, L Trinh, J Post, A Liang, M M Morrissey, K J Shaw.
Abstract
Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500-1000-fold selectivity against thrombin and 50-100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong impact on the FXa inhibitory activity. Crystallography studies suggest that the 2-substituent may have a conformational effect favoring the extended binding conformation.Entities:
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Year: 2000 PMID： 10853669 DOI： 10.1016/s0960-894x(00)00139-6
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823