Published August 28, 2017
| Version v1
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SGC-GAK-1: A chemical probe candidate for the understudied kinase GAK
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, 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
- 4. 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
- 6. School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, Kuopio, Finland
Description
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.
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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