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Assay Detail

CHEMBL642848

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

Binding
Liver ACAT inhibitory activity was determined in vitro using [1-14C]oleolyl-CoA and microsomes isolated from the livers of cholesterol fed rats
3
Total Activities
3
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

Tetrazole-substituted ureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). A novel preparation of ureas from weakly nucleophilic amines
Purchase CF, White AD, Anderson MK, Bocan TM, Bousley RF, Hamelehle KL, Homan R, Krause BR, Lee P, Mueller SB, Speyer C, Stanfield RL, Reindel JF
Bioorg Med Chem Lett (1996) 6 : 1753 -1758
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.93 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49682 1 7.24
CHEMBL49524 1 7.21
CHEMBL297074 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49682 IC50 = 57.0 nM 7.24
CHEMBL49524 IC50 = 61.0 nM 7.21
CHEMBL297074 IC50 = 450.0 nM 6.35