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ChEMBL ligand: CHEMBL1800807 (Anacetrapib, MK-0859, MK0859) |
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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 | Inhibition of full-length human recombinant CETP expressed in CHO cells by BODIPY-CE dye based fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2016) 24: 1811-1818 [PMID:26993745] |
ChEMBL | Inhibition of CETP in 95% human serum assessed as inhibition of transfer of [3H] cholesteryl oleate or [3H] triolein between LDL and HDL | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127668-127668 [PMID:33161125] |
ChEMBL | Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3056-3062 [PMID:22497761] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum by liquid scintillation analysis | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of BODIPY-labeled cholesteryl transfer to fluorescent substrate by fluorimetric assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2016) 123: 419-430 [PMID:27490022] |
ChEMBL | Inhibition of recombinant full length human CETP expressed in CHO cells assessed as reduction in BODIPY-CE transfer measured after 1 to 3 hrs by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2017) 126: 143-153 [PMID:27750148] |
ChEMBL | Inhibition of human CETP | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126824-126824 [PMID:31780304] |
ChEMBL | Inhibition of recombinant human CETP after 3 hrs using fluorescent cholesteryl containing HDL after 3 hrs by fluorescence assay | B | 7.47 | pIC50 | 33.8 | nM | IC50 | Eur J Med Chem (2017) 139: 201-213 [PMID:28802120] |
ChEMBL | Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2017) 60: 8466-8481 [PMID:29035537] |
GtoPdb | - | - | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2011) 54: 4880-95 [PMID:21682257] |
ChEMBL | Inhibition of human recombinant CETP-mediated cholesteryl ester transfer activity after 1 hr by fluorescent cholesteryl esters transfer assay | B | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2011) 54: 4880-4895 [PMID:21682257] |
ChEMBL | Inhibition of CETP-mediated neutral lipid transfer by fluorometric analysis | B | 7.76 | pIC50 | 17.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 199-203 [PMID:22142541] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein using exogenous LDL and HDL in 2% human serum by liquid scintillation analysis | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of [S35]-MK-0499 binding to human ERG expressed in HEK293 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
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]