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Assay Detail

CHEMBL4603684

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Binding
Inhibition of human CETP
7
Total Activities
7
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

Synthesis, biological evaluation and SAR studies of ursolic acid 3β-ester derivatives as novel CETP inhibitors.
Chen C, Sun R, Sun Y, Chen X, Li F, Wen X, Yuan H, Chen D.
Bioorg Med Chem Lett (2020) 30 : 126824 -126824
PubMed 31780304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.71 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800807 ANACETRAPIB 3.0 1 7.44
CHEMBL4634660 1 5.62
CHEMBL509269 1 5.50
CHEMBL4647341 1 5.48
CHEMBL4646529 1 5.26
CHEMBL508934 1 4.96
CHEMBL169 URSOLIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800807 ANACETRAPIB IC50 = 36.0 nM 7.44
CHEMBL4634660 IC50 = 2400.0 nM 5.62
CHEMBL509269 IC50 = 3200.0 nM 5.50
CHEMBL4647341 IC50 = 3300.0 nM 5.48
CHEMBL4646529 IC50 = 5500.0 nM 5.26
CHEMBL508934 IC50 = 10900.0 nM 4.96
CHEMBL169 URSOLIC ACID IC50 > 50000.0 nM -