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Instruments / Technical Area	Publication Details	Published	Actions
I03-Macromolecular Crystallography	A chemical probe targeting AAK1 and BMP2K Carrow Wells , Rafael M. Counago , Juanita C. Limas , Tuanny L. Almeida , Jeanette Gowen Cook , David H Drewry , Jonathan M. Elkins , Opher Gileadi , Nirav R. Kapadia , Alvaro Lorente-Macias , Julie E. Pickett , Alexander Riemen , Roberta R. Ruela-De-Sousa , Timothy M. Willson , Cunyu Zhang , William J Zuercher , Reena Zutshi , Alison D. Axtman Acs Medicinal Chemistry Letters DOI: 10.1021/acsmedchemlett.9b00399 Diamond Proposal Number(s): [14664] Show Abstract ▼ Abstract: 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.	Oct 2019

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