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Synonyms: compound 2 [Li et al., 2018]
Compound class: Synthetic organic
Comment: BMS-823778 is an orally bioavailable clinical lead inhibitor of hydroxysteroid 11-beta dehydrogenase 1 (11β-HSD)  which is the enzyme that converts inactive cortisone to biologically active costisol . We show the chemical structure for BMS-823778 free base. Some bioactivity data may have been determined using the hydrochloride salt (PubChem CID 54669979). BMS-823778 was developed for potential treatment of type 2 diabetes and metabolic syndrome.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Cheng Y, Wang L, Iacono L, Zhang D, Chen W, Gong J, Humphreys WG, Gan J. (2018)
Clinical significance of CYP2C19 polymorphisms on the metabolism and pharmacokinetics of 11β-hydroxysteroid dehydrogenase type-1 inhibitor BMS-823778.
Br J Clin Pharmacol, 84 (1): 130-141. [PMID:28850715]
2. Gathercole LL, Lavery GG, Morgan SA, Cooper MS, Sinclair AJ, Tomlinson JW, Stewart PM. (2013)
11β-Hydroxysteroid dehydrogenase 1: translational and therapeutic aspects.
Endocr Rev, 34 (4): 525-55. [PMID:23612224]
3. Gong J, Hansen L, Iacono L. (2018)
Clinical Pharmacokinetics and the Impact of Genetic Polymorphism on a CYP2C19 Substrate, BMS-823778, in Healthy Subjects.
Drug Metab Dispos, 46 (3): 316-325. [PMID:29311135]
4. Gong J, Iacono L, Iyer RA, Humphreys WG, Zheng M. (2018)
Physiologically-based pharmacokinetic modelling of a CYP2C19 substrate, BMS-823778, utilizing pharmacogenetic data.
Br J Clin Pharmacol, 84 (6): 1335-1345. [PMID:29469197]
5. Li J, Kennedy LJ, Walker SJ, Wang H, Li JJ, Hong Z, O'Connor SP, Ye XY, Chen S, Wu S et al.. (2018)
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD-1).
ACS Med Chem Lett, 9 (12): 1170-1174. DOI: 10.1021/acsmedchemlett.8b00307 [PMID:30613321]