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

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.

SUBMITTER: Wells C

PROVIDER: S-EPMC7073879 | biostudies-literature | 2020 Mar

REPOSITORIES: biostudies-literature

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

Wells Carrow C Couñago Rafael M RM Limas Juanita C JC Almeida Tuanny L TL Cook Jeanette Gowen JG Drewry David H DH Elkins Jonathan M JM Gileadi Opher O Kapadia Nirav R NR Lorente-Macias Alvaro A Pickett Julie E JE Riemen Alexander A Ruela-de-Sousa Roberta R RR Willson Timothy M TM Zhang Cunyu C Zuercher William J WJ Zutshi Reena R Axtman Alison D AD

ACS medicinal chemistry letters 20191023 3

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, <b>25</b>) 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. ...[more]

PMID: 32184967

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