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Assay Detail

CHEMBL1015030

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

Binding
Inhibition of CETP-mediated transfer of [3H]cholesteryl ester from HDL donar particles to LDL acceptor particles in presence of buffer
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein inhibitor.
Kuo GH, Rano T, Pelton P, Demarest KT, Gibbs AC, Murray WV, Damiano BP, Connelly MA.
J Med Chem (2009) 52 : 1768 -1772
PubMed 19236017 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69563 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69563 IC50 = 3.0 nM 8.52