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Copyright © 2019 American Chemical Society. Inhibitors based on a 3-acylaminoindazole scaffold were synthesized to yield potent dual AAK1/BMP2K inhibitors. Optimization furnished a small molecule chemical probe (SGC-AAK1-1, 25) that is potent and selective for AAK1/BMP2K over other NAK family members, demonstrates narrow activity in a kinome-wide screen, and is functionally active in cells. This inhibitor represents one of the best available small molecule tools to study the functions of AAK1 and BMP2K. ©

Original publication

DOI

10.1021/acsmedchemlett.9b00399

Type

Journal article

Journal

ACS Medicinal Chemistry Letters

Publication Date

01/01/2019