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Lookup NU author(s): Duncan Miller
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The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1.8 blockers. Subsequent optimization allowed the identification of compound 9, PF-06305591, as a potent, highly selective blocker with an excellent preclinical in vitro ADME and safety profile.
Author(s): Brown AD, Bagal SK, Blackwell P, Blakemore DC, Brown B, Bungay PJ, Corless M, Crawforth J, Fengas D, Fenwick DR, Gray V, Kenp M, Klute W, Malet-Sainz L, Miller D, Murata YC, Payne E, Skerratt S, Warmus JS
Publication type: Article
Publication status: Published
Journal: Bioorganic & Medicinal Chemistry
Print publication date: 01/01/2019
Online publication date: 04/12/2018
Acceptance date: 01/12/2018
ISSN (print): 0968-0896
ISSN (electronic): 1464-3391
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