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Synonyms: SCH 58235 | SCH-58235 | Zetia®
ezetimibe is an approved drug (FDA (2002))
Compound class: Synthetic organic
Comment: Inhibits the intestinal cholesterol uptake protein Niemann-Pick C1-like protein 1 (NPC1L1). Analysis of cryo-EM structures reveals how NPC1L1 transports cholesterol and the mechanism of ezetimibe inhibition .
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.✖
View more information in the IUPHAR Pharmacology Education Project: ezetimibe
1. Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, Crona JH, Davis Jr HR, Dean DC, Detmers PA et al.. (2005)
The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).
Proc Natl Acad Sci USA, 102 (23): 8132-7. [PMID:15928087]
2. Huang CS, Yu X, Fordstrom P, Choi K, Chung BC, Roh SH, Chiu W, Zhou M, Min X, Wang Z. (2020)
Cryo-EM structures of NPC1L1 reveal mechanisms of cholesterol transport and ezetimibe inhibition.
Sci Adv, 6 (25): eabb1989. DOI: 10.1126/sciadv.abb1989 [PMID:32596471]
3. Oswald S, König J, Lütjohann D, Giessmann T, Kroemer HK, Rimmbach C, Rosskopf D, Fromm MF, Siegmund W. (2008)
Disposition of ezetimibe is influenced by polymorphisms of the hepatic uptake carrier OATP1B1.
Pharmacogenet Genomics, 18 (7): 559-68. [PMID:18551036]