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) [5] which is the enzyme that converts inactive cortisone to biologically active costisol [2]. 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 ChartsThese 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. ✖ |
|
No information available. |
Summary of Clinical Use |
BMS-823778 progressed to Phase 2 clinical evaluation in patients with atherosclerosis or hypertension but the trials were terminated/withdrawn. Click here to link to ClinicalTrials.gov's full list of BMS-823778 trials. |
Pharmacokinetics |
Elimination |
Systemic clearance of BMS-823778 was found to be directly correlated with the genetic polymorphism of CYP2C19 [1,3-4]. |