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Assay Detail

CHEMBL872983

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

Functional
ACAT activity was determined in rat hepatic microsomes by measuring the formation of labeled cholesteryl oleate (pmol/midmg) from [14C]oleoyl-CoA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Liver
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL285)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
Maduskuie TP, Wilde RG, Billheimer JT, Cromley DA, Germain S, Gillies PJ, Higley CA, Johnson AL, Pennev P, Shimshick EJ.
J Med Chem (1995) 38 : 1067 -1083
PubMed 7707310 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.55 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 8.00
CHEMBL273826 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 10.0 nM 8.00
CHEMBL273826 IC50 = 80.0 nM 7.10