Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1

[Image: see text] We describe the identification and characterization of a series of covalent inhibitors of the C-terminal kinase domain (CTKD) of MSK1. The initial hit was identified via a high-throughput screening and represents a rare example of a covalent inhibitor which acts via an S(N)Ar react...

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Detalles Bibliográficos
Autores principales: Hall, Adrian, Abendroth, Jan, Bolejack, Madison J., Ceska, Tom, Dell’Aiera, Sylvie, Ellis, Victoria, Fox, David, François, Cyril, Muruthi, Muigai M., Prével, Camille, Poullennec, Karine, Romanov, Sergei, Valade, Anne, Vanbellinghen, Alain, Yano, Jason, Geraerts, Martine
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9290008/
https://www.ncbi.nlm.nih.gov/pubmed/35859861
http://dx.doi.org/10.1021/acsmedchemlett.2c00134

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