Published August 28, 2017 | Version v1
Presentation Open

SGC-AAK1-1: A chemical probe candidate for the understudied kinases AAK1 and BIKE/BMP2K

Authors/Creators

  • 1. Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, USA
  • 2. Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, UK
  • 3. Structural Genomics Consortium, Universidade Estadual de Campinas - UNICAMP, Campinas, São Paulo, Brazil
  • 4. Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building, Oxford, UK and Structural Genomics Consortium, Universidade Estadual de Campinas - UNICAMP, Campinas, São Paulo, Brazil
  • 5. Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences and Institute of Pharmaceutical Chemistry, Göthe University Frankfurt, Frankfurt am Main, Germany

Description

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. 

Notes

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.

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