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J Med Chem. 2019 Mar 14;62(5):2830-2836. doi: 10.1021/acs.jmedchem.8b01213. Epub 2019 Feb 26.

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

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Structural Genomics Consortium, Johann Wolfgang Goethe University, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15 , D-60438 Frankfurt am Main , Germany.
Institute for Pharmaceutical Chemistry , Johann Wolfgang Goethe University , Max-von-Laue-Straße 9 , D-60438 Frankfurt am Main , Germany.
Structural Genomics Consortium and Target Discovery Institute, Nuffield Department of Clinical Medicine, University of Oxford, Old Road Campus Research Building , Oxford OX3 7DQ , U.K.
Structural Genomics Consortium , Universidade Estadual de Campinas , Campinas , São Paulo 13083-886 , Brazil.


We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK), together with a structurally related negative control SGC-GAK-1N (14). 11 was highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent RIPK2 inhibitor lacking GAK activity. Together, this chemical probe set can be used to interrogate GAK cellular biology.

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