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Assay Detail

CHEMBL1104194

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of CETP assessed as cholesterol ester transfer after 4 hrs by microemulsion based fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cholesteryl ester transfer protein (CHEMBL3572)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tetrahydrochinoline derived CETP inhibitors.
Schmeck C, Gielen-Haertwig H, Vakalopoulos A, Bischoff H, Li V, Wirtz G, Weber O.
Bioorg Med Chem Lett (2010) 20 : 1740 -1743
PubMed 20137927 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.68 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1081450 1 7.77
CHEMBL479527 TORCETRAPIB 3.0 1 7.75
CHEMBL1081802 1 7.66
CHEMBL1086624 1 7.62
CHEMBL1081288 1 7.60
CHEMBL1081287 1 7.52
CHEMBL1086623 1 7.51
CHEMBL1086637 1 7.48
CHEMBL1081307 1 7.41
CHEMBL1080543 1 7.26
CHEMBL1080866 1 7.22
CHEMBL1087412 1 7.16
CHEMBL1087413 1 7.16
CHEMBL1080751 1 7.16
CHEMBL1080749 1 7.10
CHEMBL1087411 1 7.05
CHEMBL1081607 1 7.00
CHEMBL1080750 1 7.00
CHEMBL1087784 1 6.52
CHEMBL1076557 1 6.30
CHEMBL1087783 1 6.22
CHEMBL1088039 1 6.22
CHEMBL1087782 1 5.70
CHEMBL1080709 1 5.70
CHEMBL1080710 1 5.52
CHEMBL1087154 1 5.52
CHEMBL1081083 1 5.40
CHEMBL1086625 1 5.35
CHEMBL1076558 1 4.82
CHEMBL1080385 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1081450 IC50 = 17.0 nM 7.77
CHEMBL479527 TORCETRAPIB IC50 = 18.0 nM 7.75
CHEMBL1081802 IC50 = 22.0 nM 7.66
CHEMBL1086624 IC50 = 24.0 nM 7.62
CHEMBL1081288 IC50 = 25.0 nM 7.60
CHEMBL1081287 IC50 = 30.0 nM 7.52
CHEMBL1086623 IC50 = 31.0 nM 7.51
CHEMBL1086637 IC50 = 33.0 nM 7.48
CHEMBL1081307 IC50 = 39.0 nM 7.41
CHEMBL1080543 IC50 = 55.0 nM 7.26
CHEMBL1080866 IC50 = 60.0 nM 7.22
CHEMBL1087412 IC50 = 70.0 nM 7.16
CHEMBL1087413 IC50 = 70.0 nM 7.16
CHEMBL1080751 IC50 = 70.0 nM 7.16
CHEMBL1080749 IC50 = 80.0 nM 7.10
CHEMBL1087411 IC50 = 90.0 nM 7.05
CHEMBL1081607 IC50 = 100.0 nM 7.00
CHEMBL1080750 IC50 = 100.0 nM 7.00
CHEMBL1087784 IC50 = 300.0 nM 6.52
CHEMBL1076557 IC50 = 500.0 nM 6.30
CHEMBL1087783 IC50 = 600.0 nM 6.22
CHEMBL1088039 IC50 = 600.0 nM 6.22
CHEMBL1087782 IC50 = 2000.0 nM 5.70
CHEMBL1080709 IC50 = 2000.0 nM 5.70
CHEMBL1080710 IC50 = 3000.0 nM 5.52
CHEMBL1087154 IC50 = 3000.0 nM 5.52
CHEMBL1081083 IC50 = 4000.0 nM 5.40
CHEMBL1086625 IC50 = 4500.0 nM 5.35
CHEMBL1076558 IC50 = 15000.0 nM 4.82
CHEMBL1080385 IC50 = 15000.0 nM 4.82
CHEMBL1080732 IC50 > 20000.0 nM -
CHEMBL1080731 IC50 > 20000.0 nM -