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Assay Detail

CHEMBL649065

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% activity of the rabbit artery Acyl coenzyme A:cholesterol acyltransferase 1
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Acyl-CoA:cholesterol acyltransferase (CHEMBL6141)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

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 7 6.57 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30860 1 7.60
CHEMBL33780 1 7.40
CHEMBL33661 2 6.82
CHEMBL286812 1 5.43
CHEMBL289465 2 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30860 IC50 = 25.0 nM 7.60
CHEMBL33780 IC50 = 40.0 nM 7.40
CHEMBL33661 IC50 = 150.0 nM 6.82
CHEMBL33661 IC50 = 150.0 nM 6.82
CHEMBL286812 IC50 = 3700.0 nM 5.43
CHEMBL289465 IC50 = 4450.0 nM 5.35
CHEMBL289465 IC50 > 8500.0 nM -