SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K

Carrow Wells,Rafael M. Couñago,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（2020）

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摘要

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, ) 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.

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关键词

AAK1,BMP2K,acylaminoindazole,NAK family,endocytosis,protein kinase

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