ezetimibe [Ligand Id: 6816] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1138 (Ezetimibe, 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 |
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| NPC1 like intracellular cholesterol transporter 1 in Human [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] |
| NPC1 like intracellular cholesterol transporter 1/Niemann-Pick C1-like protein 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
