Toggle Main Menu Toggle Search

Open Access padlockePrints

The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain

Lookup NU author(s): Duncan MillerORCiD


Full text for this publication is not currently held within this repository. Alternative links are provided below where available.


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.

Publication metadata

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

Year: 2019

Volume: 27

Issue: 1

Pages: 230-239

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

Publisher: Elsevier


DOI: 10.1016/j.bmc.2018.12.002


Altmetrics provided by Altmetric