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Assay Detail

CHEMBL642846

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

Binding
Inhibitory activity was evaluated in rat liver microsomes using Acyl coenzyme A:cholesterol acyltransferase microsomal assay.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-oleoyl-1,2,3,4-tetrahydroisoquinolines as conformationally restricted inhibitors of acyl-CoA:cholesterol acyl transferase (ACAT)
Dugar S, Clader JW, Burrier RE, Kogan TP
Bioorg Med Chem Lett (1993) 3 : 571 -576
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.78 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41240 1 6.82
CHEMBL154341 1 5.57
CHEMBL154377 1 5.42
CHEMBL152502 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41240 IC50 = 150.0 nM 6.82
CHEMBL154341 IC50 = 2700.0 nM 5.57
CHEMBL154377 IC50 = 3800.0 nM 5.42
CHEMBL152502 IC50 = 4800.0 nM 5.32