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| ChEMBL ligand: CHEMBL1138 (Ezetimiba, Ezetimibe, Ezetimibe component of k-924, Ezetimibe component of liptruzet, Ezetimibe component of nexlizet, Ezetimibe component of roszet, Ezetimibe component of vytorin, Ezetrol, MK0653, NSC-758923, SCH-58235, SCH58235, Zetia) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Sodium/bile acid and sulphated solute cotransporter 1/Hepatic sodium/bile acid cotransporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5287] [GtoPdb: 959] [UniProtKB: Q14973] | ||||||||
| ChEMBL | Binding affinity to NTCP (unknown origin) | B | 4.6 | pKi | 25000 | nM | Ki | J Med Chem (2022) 65: 12546-12561 [PMID:36111355] |
| NPC1 like intracellular cholesterol transporter 1/NPC1-like intracellular cholesterol transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2027] [GtoPdb: 2629] [UniProtKB: Q9UHC9] | ||||||||
| GtoPdb | Measure of ezetimibe glucuronide binding to NPC1L1 | - | 6.66 | pKd | 220 | nM | Kd | Proc Natl Acad Sci USA (2005) 102: 8132-7 [PMID:15928087] |
| ChEMBL | Inhibition of NPC1L1 (unknown origin) assessed as inhibition of cholesterol cellular uptake by BCA colorimetric assay | B | 6.43 | pIC50 | 370 | nM | IC50 | Eur J Med Chem (2022) 230: 114111-114111 [PMID:35063734] |
| NPC1 like intracellular cholesterol transporter 1/NPC1-like intracellular cholesterol transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5161] [GtoPdb: 2629] [UniProtKB: Q6T3U3] | ||||||||
| ChEMBL | Displacement of [3H]ezetimibe-glucuronide from NPC1L1 in Sprague-Dawley rat brush border membrane | B | 6.7 | pKi | 200 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 546-553 [PMID:18063367] |
ChEMBL data shown on this page come from version 36:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]