dalcetrapib [Ligand Id: 12972] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 34:
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]
