Wells C., Couñago RM., Limas JC., Almeida TL., Cook JG., Drewry DH., Elkins JM., Gileadi O., Kapadia NR., Lorente-Macias A., Pickett JE., Riemen A., Ruela-de-Sousa RR., Willson TM., Zhang C., Zuercher WJ., Zutshi R., Axtman AD.

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.

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

Wells C., Couñago RM., Limas JC., Almeida TL., Cook JG., Drewry DH., Elkins JM., Gileadi O., Kapadia NR., Lorente-Macias A., Pickett JE., Riemen A., Ruela-de-Sousa RR., Willson TM., Zhang C., Zuercher WJ., Zutshi R., Axtman AD.

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