Sgc-Aak1-1: A Chemical Probe Candidate For The Understudied Kinases Aak1 And Bike/Bmp2K

SGC-AAK1-1 is presented as a chemical probe for the understudied kinases (adaptor protein 2)-associated kinase (AAK1) and (bone morphogenetic protein 2)-inducible kinase (BIKE/BMP2K). SGC-AAK1-1 is potent with submicromolar cellular target engagement with AAK1. The compound shows > 30-fold selectivity in binding relative to all other kinases profiled with the exception of RIOK1, RIOK3, and PIP5K1C. A closely related molecule that is significantly less potent with AAK1 and BIKE/BMP2K, SGC-AAK1-1N, is included as a negative control.
The SGC is a registered charity (number 1097737) that receives funds from AbbVie, Bayer Pharma AG, Boehringer Ingelheim, Canada Foundation for Innovation, Eshelman Institute for Innovation, Genome Canada, Innovative Medicines Initiative (EU/EFPIA), Janssen, Merck & Co., Novartis Pharma AG, Ontario Ministry of Economic Development and Innovation, Pfizer, São Paulo Research Foundation-FAPESP, Takeda, and Wellcome Trust.