Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1)

[Image: see text] BMS-823778 (2), a 1,2,4-triazolopyridinyl-methanol derived analog, was identified as a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) enzyme (IC(50) = 2.3 nM) with >10,000-fold selectivity over 11β-HSD-2. Compound 2 exhibits robust ac...

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Опубликовано в: :ACS Med Chem Lett
Главные авторы: Li, Jun, Kennedy, Lawrence J., Walker, Steven J., Wang, Haixia, Li, James J., Hong, Zhenqiu, O’Connor, Stephen P., Ye, Xiang-yang, Chen, Stephanie, Wu, Shung, Yoon, David S., Nayeem, Akbar, Camac, Daniel M., Ramamurthy, Vidhyashankar, Morin, Paul E., Sheriff, Steven, Wang, Mengmeng, Harper, Timothy W., Golla, Rajasree, Seethala, Ramakrishna, Harrity, Thomas, Ponticiello, Randolph P., Morgan, Nathan N., Taylor, Joseph R., Zebo, Rachel, Maxwell, Brad, Moulin, Frederick, Gordon, David A., Robl, Jeffrey A.
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2018
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC6295842/
https://ncbi.nlm.nih.gov/pubmed/30613321
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00307
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