oral selective VPS34 kinase inhibitor
discontinued due to potential toxicity
SBDD and SAR optimization
Journal of Medicinal Chemistry
Genentech Inc.
“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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