The BMS AAK1 kinase inhibitor, compound 59 , is brain-penetrant and acts on the CNS. The target was identified from a phenotypic screen of mouse knockouts, and a non-brain penetrant inhibitor doesn’t show in vivo activity, confirming the central activity needed on the target. Targeting a kinase in the CNS for pain is bold due to the high bar [...]
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Dec. 16, 2021
compound 59: a Brain-Penetrant AAK1 Kinase Inhibitor
compound 59
brain penetrant AAK1 kinase inhibitor efficacious in neuropathic pain model from biochemical screen of in-house library Journal of Medicinal Chemistry Bristol Myers Squibb, Wallingford, US