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Article

Non-oxime inhibitors of B-Raf(V600E) kinase.

Bioorganic & medicinal chemistry letters - 15 Feb 2011

Ren Li, Wenglowsky Steve, Miknis Greg, Rast Bryson, Buckmelter Alex J, Ely Robert J, Schlachter Stephen, Laird Ellen R, Randolph Nikole, Callejo Michele, Martinson Matthew, Galbraith Sarah, Brandhuber Barbara J, Vigers Guy, Morales Tony, Voegtli Walter C, Lyssikatos Joseph

Abstract excerpt

The development of inhibitors of B-Raf(V600E) serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME properties. Several of the head-groups explored, including naphthol, phenol and hydroxyamidine, possessed good activity but had poor pharmacokinetic exposure in mice. Exposure was improved by incorporating more metabolically stable groups such as indazole...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Source

Identifiers

PMID: 21251822
DOI: 10.1016/j.bmcl.2010.12.061

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 5 Sept 2026. Manifest publication-graph-cohort-2026-09-05.1.

Source receipt: pubmed, retrieved 5 Sept 2026.

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