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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 Med Chem Lett

Publication Date

12/03/2020

Volume

11

Pages

340 - 345