1. Sgc-Aak1-1: A Chemical Probe Candidate For The Understudied Kinases Aak1 And Bike/Bmp2K
- Author
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Axtman, Alison D., Azeez, Kamal Abdul, Bennett, James M., Couñago, Rafael, Drewry, David H., Elkins, Jonathan M., Fedorov, Oleg, Gileadi, Opher, Godoi, Paulo, Knapp, Stefan, Leite, Tuanny, Müller, Susanne, Paradela, Luciana, Santiago, André da Silva, Ruela-de-la-Souza, Roberta, Strain-Damerall, Claire, Tillman-Berger, Benedict, Wells, Carrow I., Willson, Timothy M., and Zuercher, William J.
- Subjects
inorganic chemicals ,Kinase chemical probe ,cardiovascular system ,BIKE/BMP2K ,heterocyclic compounds ,AAK1 - Abstract
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.
- Published
- 2017
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