Assay Detail
Binding
CHEMBL643358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against Acyl coenzyme A:cholesterol acyltransferase (ACAT) in rabbit intestinal microsomes
60
Total Activities
60
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 O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 60 | 7.25 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL79602 | — | — | 1 | 7.92 |
| CHEMBL78870 | — | — | 1 | 7.85 |
| CHEMBL311524 | — | — | 1 | 7.75 |
| CHEMBL557744 | — | — | 1 | 7.72 |
| CHEMBL311285 | — | — | 1 | 7.70 |
| CHEMBL81651 | — | — | 1 | 7.68 |
| CHEMBL310162 | — | — | 1 | 7.66 |
| CHEMBL80396 | — | — | 1 | 7.66 |
| CHEMBL309728 | — | — | 1 | 7.66 |
| CHEMBL420021 | — | — | 1 | 7.64 |
| CHEMBL78643 | — | — | 1 | 7.62 |
| CHEMBL80742 | — | — | 1 | 7.62 |
| CHEMBL312804 | — | — | 1 | 7.60 |
| CHEMBL78425 | — | — | 1 | 7.58 |
| CHEMBL78773 | — | — | 1 | 7.57 |
| CHEMBL80973 | — | — | 1 | 7.57 |
| CHEMBL78737 | — | — | 1 | 7.57 |
| CHEMBL80585 | — | — | 1 | 7.55 |
| CHEMBL310159 | — | — | 1 | 7.55 |
| CHEMBL78387 | — | — | 1 | 7.54 |
| CHEMBL77842 | — | — | 1 | 7.52 |
| CHEMBL277986 | CL-277082 | — | 1 | 7.48 |
| CHEMBL78558 | — | — | 1 | 7.48 |
| CHEMBL78144 | — | — | 1 | 7.46 |
| CHEMBL419093 | — | — | 1 | 7.44 |
| CHEMBL80288 | — | — | 1 | 7.42 |
| CHEMBL309877 | — | — | 1 | 7.41 |
| CHEMBL80634 | — | — | 1 | 7.38 |
| CHEMBL310523 | — | — | 1 | 7.38 |
| CHEMBL80229 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL79602 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL78870 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL311524 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL557744 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL311285 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL81651 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL310162 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL80396 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL309728 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL420021 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL78643 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL80742 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL312804 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL78425 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL78737 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL80973 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL78773 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL80585 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL310159 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL78387 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL77842 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL277986 | CL-277082 | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL78558 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL78144 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL419093 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL80288 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL309877 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL80634 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL310523 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL80229 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL80762 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL311193 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL81411 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL78597 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL79237 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL78075 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL78861 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL307935 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL81477 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL420577 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL80780 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL312422 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL312798 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL311725 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL309757 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL81392 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL80751 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL78869 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL79001 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL312095 | — | IC50 | = | 180.0 | nM | 6.75 |