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Assay Detail

CHEMBL645923

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

Binding
Compound was evaluated for the Acyl coenzyme A:cholesterol acyltransferase inhibition using microsomes isolated from the livers of cholesterol fed rats.
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
Sliskovic DR, Krause BR, Picard JA, Anderson M, Bousley RF, Hamelehle KL, Homan R, Julian TN, Rashidbaigi ZA, Stanfield RL.
J Med Chem (1994) 37 : 560 -562
PubMed 8126693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.75 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274185 LECIMIBIDE 2.0 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274185 LECIMIBIDE IC50 = 18.0 nM 7.75