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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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.
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