SGC-GAK-1 is presented as a chemical probe for the understudied cyclin G associated kinase (GAK). SGC-GAK-1 is potent and shows submicromolar cellular target engagement with GAK. The compound shows > 30-fold selectivity relative to all other kinases profiled with the exception of RIPK2. A closely related molecule that is significantly less potent with GAK, SGC-GAK-1N, is included as a negative control. In addition, a compound having potent activity at RIPK2 but not GAK, HY-19764, is offered to control for the activity of RIPK2.

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.