Assay Detail
Binding
CHEMBL646538
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested in vitro to inhibit Acyl coenzyme A:cholesterol acyltransferase in intestinal microsomes isolated from cholesterol-fed rabbits.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Intestine |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Inhibitors of acyl-CoA:cholesterol acyltransferase. 1. Identification and structure-activity relationships of a novel series of fatty acid anilide hypocholesterolemic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.66 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL46510 | — | — | 1 | 7.37 |
| CHEMBL40519 | — | — | 1 | 7.29 |
| CHEMBL40518 | — | — | 1 | 7.23 |
| CHEMBL41845 | — | — | 1 | 7.14 |
| CHEMBL40644 | — | — | 1 | 7.05 |
| CHEMBL43812 | — | — | 1 | 5.35 |
| CHEMBL44154 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL46510 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL40519 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL40518 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL41845 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL40644 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL43812 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL44154 | — | IC50 | = | 6300.0 | nM | 5.20 |