SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)

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 collater...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Asquith, Christopher R. M., Berger, Benedict-Tilman, Wan, Jing, Bennett, James M., Capuzzi, Stephen J., Crona, Daniel J., Drewry, David H., East, Michael P., Elkins, Jonathan M., Fedrov, Oleg, Godoi, Paulo H., Hunter, Debra M., Knapp, Stefan, Müller, Susanne, Torrice, Chad D., Wells, Carrow I., Earp, H. Shelton, Willson, Timothy M., Zuercher, William J.
Formato: Artigo
Idioma:Inglês
Publicado em: 2019
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6567991/
https://ncbi.nlm.nih.gov/pubmed/30768268
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01213
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