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Updated: Jun 5, 2026

Characterize Disease-related Mutants of RAF Family Kinases by Using a Set of Practical and Feasible Methods
Published on: July 17, 2019
Non-oxime inhibitors of B-Raf(V600E) kinase
Li Ren1, Steve Wenglowsky, Greg Miknis
1Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA.
Abstract:
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 and tricyclic pyrazole, while indazole could also be optimized for good cellular activity.
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