Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1.
Autor: | Hall A; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Abendroth J; UCB Seattle, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., Bolejack MJ; UCB Seattle, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., Ceska T; UCB, 216 Bath Road, Slough SL1 3WE, U.K., Dell'Aiera S; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Ellis V; UCB, 216 Bath Road, Slough SL1 3WE, U.K., Fox D 3rd; UCB Seattle, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., François C; NovAliX, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Muruthi MM; UCB Seattle, 7869 NE Day Road West, Bainbridge Island, Washington 98110, United States., Prével C; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Poullennec K; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Romanov S; NANOSYN, 3100 Central Expressway, Santa Clara, California 95051, United States., Valade A; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Vanbellinghen A; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium., Yano J; UCB Boston, 87 Cambridge Park Drive, Cambridge, Massachusetts 02140, United States., Geraerts M; UCB, Avenue de l'Industrie, Braine-L'Alleud 1420, Belgium. |
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Jazyk: | angličtina |
Zdroj: | ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 Jun 25; Vol. 13 (7), pp. 1099-1108. Date of Electronic Publication: 2022 Jun 25 (Print Publication: 2022). |
DOI: | 10.1021/acsmedchemlett.2c00134 |
Abstrakt: | 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 Competing Interests: The authors declare the following competing financial interest(s): Some of the authors may hold stock, stock awards, or stock options in the companies which employ them. (© 2022 American Chemical Society.) |
Databáze: | MEDLINE |
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