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Assay Detail

CHEMBL2033274

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

Binding
Inhibition of CETP in human plasma assessed as transfer of fluorescently labelled cholesteryl ester to VLDL by fluorimetry
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
Escribano A, Mateo AI, Martin de la Nava EM, Mayhugh DR, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel AG, Sweetana SA, Cannady EA, Mantlo NB.
Bioorg Med Chem Lett (2012) 22 : 3671 -3675
PubMed 22543028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.03 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2032415 1 7.89
CHEMBL2029489 1 7.82
CHEMBL2029482 1 7.82
CHEMBL2029483 1 7.80
CHEMBL2029481 1 7.64
CHEMBL2032417 1 7.62
CHEMBL2032416 1 7.58
CHEMBL2029484 1 7.54
CHEMBL2032422 1 7.44
CHEMBL2032424 1 7.43
CHEMBL479527 TORCETRAPIB 3.0 1 7.41
CHEMBL2029379 1 7.40
CHEMBL2032421 1 7.38
CHEMBL2029486 1 7.36
CHEMBL2032425 1 7.33
CHEMBL2032420 1 7.33
CHEMBL2032418 1 7.32
CHEMBL2029487 1 7.31
CHEMBL2032426 1 7.27
CHEMBL2032419 1 7.26
CHEMBL2029490 1 7.25
CHEMBL2029477 1 7.25
CHEMBL2032413 1 7.24
CHEMBL2032423 1 7.24
CHEMBL2029480 1 7.21
CHEMBL2032427 1 7.13
CHEMBL2029494 1 7.11
CHEMBL2029492 1 6.82
CHEMBL2029491 1 6.79
CHEMBL2029476 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2032415 IC50 = 13.0 nM 7.89
CHEMBL2029489 IC50 = 15.0 nM 7.82
CHEMBL2029482 IC50 = 15.0 nM 7.82
CHEMBL2029483 IC50 = 16.0 nM 7.80
CHEMBL2029481 IC50 = 23.0 nM 7.64
CHEMBL2032417 IC50 = 24.0 nM 7.62
CHEMBL2032416 IC50 = 26.0 nM 7.58
CHEMBL2029484 IC50 = 29.0 nM 7.54
CHEMBL2032422 IC50 = 36.0 nM 7.44
CHEMBL2032424 IC50 = 37.0 nM 7.43
CHEMBL479527 TORCETRAPIB IC50 = 39.0 nM 7.41
CHEMBL2029379 IC50 = 40.0 nM 7.40
CHEMBL2032421 IC50 = 42.0 nM 7.38
CHEMBL2029486 IC50 = 44.0 nM 7.36
CHEMBL2032420 IC50 = 47.0 nM 7.33
CHEMBL2032425 IC50 = 47.0 nM 7.33
CHEMBL2032418 IC50 = 48.0 nM 7.32
CHEMBL2029487 IC50 = 49.0 nM 7.31
CHEMBL2032426 IC50 = 54.0 nM 7.27
CHEMBL2032419 IC50 = 55.0 nM 7.26
CHEMBL2029477 IC50 = 56.0 nM 7.25
CHEMBL2029490 IC50 = 56.0 nM 7.25
CHEMBL2032413 IC50 = 57.0 nM 7.24
CHEMBL2032423 IC50 = 58.0 nM 7.24
CHEMBL2029480 IC50 = 61.0 nM 7.21
CHEMBL2032427 IC50 = 74.0 nM 7.13
CHEMBL2029494 IC50 = 78.0 nM 7.11
CHEMBL2029492 IC50 = 151.0 nM 6.82
CHEMBL2029491 IC50 = 162.0 nM 6.79
CHEMBL2029476 IC50 = 187.0 nM 6.73
CHEMBL2032412 IC50 = 195.0 nM 6.71
CHEMBL2029493 IC50 = 218.0 nM 6.66
CHEMBL2029496 IC50 = 327.0 nM 6.49
CHEMBL2032414 IC50 = 2310.0 nM 5.64
CHEMBL2029488 IC50 = 2350.0 nM 5.63
CHEMBL2029485 IC50 = 3790.0 nM 5.42
CHEMBL2029495 IC50 = 10100.0 nM 5.00
CHEMBL2029479 IC50 = 20000.0 nM 4.70
CHEMBL2029478 IC50 > 50000.0 nM -