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Assay Detail

CHEMBL885300

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

Binding
Inhibitory concentration was evaluated as concentration required to inhibit 50% of the Acyl coenzyme A:cholesterol acyltransferase 1 activity obtained from human hepatic microsomal enzyme
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Sterol O-acyltransferase 1 (CHEMBL2782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acyl-CoA:Cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3-Dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT.
Astles PC, Ashton MJ, Bridge AW, Harris NV, Hart TW, Parrott DP, Porter B, Riddell D, Smith C, Williams RJ.
J Med Chem (1996) 39 : 1423 -1432
PubMed 8691472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.55 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33780 1 7.40
CHEMBL286812 1 6.37
CHEMBL33842 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33780 IC50 = 40.0 nM 7.40
CHEMBL286812 IC50 = 430.0 nM 6.37
CHEMBL33842 IC50 = 1300.0 nM 5.89