Chemical structure of Genentech VPS34 kinase inhibitor, compound 5

oral selective VPS34 kinase inhibitor

discontinued due to potential toxicity

SBDD and SAR optimization

Journal of Medicinal Chemistry

Genentech Inc.

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.…

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