molecules of the month

“compound 5”

oral selective VPS34 kinase inhibitor

discontinued due to potential toxicity

SBDD and SAR optimization

Journal of Medicinal Chemistry

Genentech Inc.

Chemical structure of Genentech VPS34 kinase inhibitor, compound 5
1 min read

11.   The Genentech VPS34 kinase inhibitor, compound 5, is a selective kinase inhibitor that is unusually polar for a kinase inhibitor (logD = 1.0, PPB = 23%) but maintains low clearance. The article was nominated by reviewers Joachim Rudolph, Callie Bryan, Christian Kuttruff, and Julien Lefranc for its interesting tricyclic structure and disclosure of tolerability findings related to VPS34 inhibiton.

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