Discovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors

[Image: see text] To identify BCATm inhibitors suitable for in vivo study, Encoded Library Technology (ELT) was used to affinity screen a 117 million member benzimidazole based DNA encoded library, which identified an inhibitor series with both biochemical and cellular activities. Subsequent SAR stu...

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Pubblicato in:ACS Med Chem Lett
Autori principali: Deng, Hongfeng, Zhou, Jingye, Sundersingh, Flora, Messer, Jeffrey A., Somers, Donald O., Ajakane, Myriam, Arico-Muendel, Christopher C., Beljean, Arthur, Belyanskaya, Svetlana L., Bingham, Ryan, Blazensky, Emily, Boullay, Anne-Benedicte, Boursier, Eric, Chai, Jing, Carter, Paul, Chung, Chun-Wa, Daugan, Alain, Ding, Yun, Herry, Kenny, Hobbs, Clare, Humphries, Eric, Kollmann, Christopher, Nguyen, Van Loc, Nicodeme, Edwige, Smith, Sarah E., Dodic, Nerina, Ancellin, Nicolas
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2016
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC4834658/
https://ncbi.nlm.nih.gov/pubmed/27096045
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00389
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