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Dec. 20, 2021

Critical On-Target Toxicity with a 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.

Drug Hunter Team

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 [...]



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