Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors

[Image: see text] Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded chemical library (DECL) screen. After hit analysis a...

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Udgivet i:ACS Med Chem Lett
Main Authors: Veerman, Johan J. N., Bruseker, Yorik B., Damen, Eddy, Heijne, Erik H., van Bruggen, Wendy, Hekking, Koen F. W., Winkel, Rob, Hupp, Christopher D., Keefe, Anthony D., Liu, Julie, Thomson, Heather A., Zhang, Ying, Cuozzo, John W., McRiner, Andrew J., Mulvihill, Mark J., van Rijnsbergen, Peter, Zech, Birgit, Renzetti, Louis M., Babiss, Lee, Müller, Gerhard
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2021
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC8040042/
https://ncbi.nlm.nih.gov/pubmed/33859795
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00547
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