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Assay Detail

CHEMBL641221

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

Functional
Acyl coenzyme A:cholesterol acyltransferase activity was determined in J774 macrophages 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
Confidence 0 — Uncurated / Unknown
Curated By Intermediate

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 8.41 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273826 1 9.22
CHEMBL274185 LECIMIBIDE 2.0 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273826 IC50 = 0.6 nM 9.22
CHEMBL274185 LECIMIBIDE IC50 = 25.0 nM 7.60