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Assay Detail

CHEMBL3870595

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

Binding
Inhibition of recombinant CETP (unknown origin) assessed as inhibition of BODIPY-labeled cholesteryl transfer to fluorescent substrate by fluorimetric assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold.
Liu C, Luo C, Hao L, Wu Q, Xie H, Zhao S, Hao C, Zhao D, Cheng M.
Eur J Med Chem (2016) 123 : 419 -430
PubMed 27490022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.31 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800807 ANACETRAPIB 3.0 1 7.40
CHEMBL3955613 1 7.22
CHEMBL3946904 1 7.16
CHEMBL3913485 1 7.16
CHEMBL3976202 1 7.10
CHEMBL3931395 1 6.77
CHEMBL3909889 1 6.72
CHEMBL3964613 1 6.66
CHEMBL3958109 1 6.52
CHEMBL3922480 1 6.46
CHEMBL3918826 1 6.44
CHEMBL3904480 1 6.43
CHEMBL3963665 1 6.38
CHEMBL3907440 1 6.28
CHEMBL3941452 1 6.07
CHEMBL3890759 1 6.04
CHEMBL3903893 1 6.03
CHEMBL3984241 1 5.79
CHEMBL3958905 1 5.68
CHEMBL3960862 1 5.56
CHEMBL3927748 1 5.45
CHEMBL3975244 1 5.18
CHEMBL3966113 1 4.68
CHEMBL3962127 1 -
CHEMBL3901482 1 -
CHEMBL3963680 1 -
CHEMBL3984332 1 -
CHEMBL3972579 1 -
CHEMBL3965575 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800807 ANACETRAPIB IC50 = 40.0 nM 7.40
CHEMBL3955613 IC50 = 60.0 nM 7.22
CHEMBL3946904 IC50 = 70.0 nM 7.16
CHEMBL3913485 IC50 = 70.0 nM 7.16
CHEMBL3976202 IC50 = 80.0 nM 7.10
CHEMBL3931395 IC50 = 170.0 nM 6.77
CHEMBL3909889 IC50 = 190.0 nM 6.72
CHEMBL3964613 IC50 = 220.0 nM 6.66
CHEMBL3958109 IC50 = 300.0 nM 6.52
CHEMBL3922480 IC50 = 350.0 nM 6.46
CHEMBL3918826 IC50 = 360.0 nM 6.44
CHEMBL3904480 IC50 = 370.0 nM 6.43
CHEMBL3963665 IC50 = 420.0 nM 6.38
CHEMBL3907440 IC50 = 520.0 nM 6.28
CHEMBL3941452 IC50 = 860.0 nM 6.07
CHEMBL3890759 IC50 = 910.0 nM 6.04
CHEMBL3903893 IC50 = 930.0 nM 6.03
CHEMBL3984241 IC50 = 1620.0 nM 5.79
CHEMBL3958905 IC50 = 2070.0 nM 5.68
CHEMBL3960862 IC50 = 2760.0 nM 5.56
CHEMBL3927748 IC50 = 3520.0 nM 5.45
CHEMBL3975244 IC50 = 6630.0 nM 5.18
CHEMBL3966113 IC50 = 20970.0 nM 4.68
CHEMBL3962127 IC50 > 50000.0 nM -
CHEMBL3901482 IC50 > 50000.0 nM -
CHEMBL3963680 IC50 > 50000.0 nM -
CHEMBL3984332 IC50 > 50000.0 nM -
CHEMBL3972579 IC50 > 50000.0 nM -
CHEMBL3965575 IC50 > 50000.0 nM -