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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Bibliografske podrobnosti
izdano v:ACS Med Chem Lett
Main Authors: 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.
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2018
Online dostop: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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