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ChEMBL ligand: CHEMBL313006 (Dalcetrapib, JTT-705, RO-4607381, RO4607381) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cholesteryl ester transfer protein/Cholesteryl ester transfer protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3572] [GtoPdb: 3248] [UniProtKB: P11597] | ||||||||
ChEMBL | In vitro concentration required to inhibit 50% of cholesteryl ester transfer protein mediated cholesteryl ester transfer from HDL to VLDL and LDL in human plasma | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2000) 43: 3566-3572 [PMID:11000011] |
ChEMBL | In vitro inhibition of CETP activity was assessed by measuring the rate of [3H]- cholesteryl ester transfer from HDL to apoprotein B-containing lipoproteins in human plasma | B | 5.22 | pIC50 | 6000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2589-2591 [PMID:15109658] |
ChEMBL | Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2017) 60: 8466-8481 [PMID:29035537] |
GtoPdb | - | - | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2017) 60: 8466-8481 [PMID:29035537] |
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]