Synonyms: compound 87 ]PMID: 34375108] | MK8262
Compound class:
Synthetic organic
Comment: MK-8262 is a small molecule that inhibits cholesterylester transfer protein (CETP; P11597) [2]. It was developed as a best-in-class back-up clinical candidate to anacetrapib, but like anacetrapib its development was discontinued. CETP was considered as a target for prevention of dyslipidemia and reducing cardiovascular mortality, with CETP inhibitors proposed as a direct route to raise HDL.
Clinical trial results for a number of CETP inhibitors have failed to show clinical benefit. Failed candidates in addition to this one, include evacetrapib, anacetrapib, torcetrapib, and dalcetrapib [1]. 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. ✖ |
|
References |
1. Ready JM. (2021)
Toward a Best-in-Class Inhibitor of Cholesteryl Ester Transfer Protein (CETP). J Med Chem, 64 (18): 13212-13214. [PMID:34498872] |
2. Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R et al.. (2021)
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties. J Med Chem, 64 (18): 13215-13258. [PMID:34375108] |