Assay Detail
Binding
CHEMBL639305
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In vitro inhibitory activity against ACAT was determined in rabbit intestinal microsome from cholesterol-fed animals
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Intestine |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
A series of conformationally and sterically constrained analogs of N-phenyl-N-aralkylurea ACAT inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.20 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL72792 | — | — | 1 | 7.77 |
| CHEMBL296055 | — | — | 1 | 7.77 |
| CHEMBL431981 | — | — | 1 | 7.62 |
| CHEMBL304612 | — | — | 1 | 7.57 |
| CHEMBL74463 | — | — | 1 | 7.57 |
| CHEMBL306266 | — | — | 1 | 7.57 |
| CHEMBL74684 | — | — | 1 | 7.54 |
| CHEMBL71051 | — | — | 1 | 7.52 |
| CHEMBL303612 | — | — | 1 | 7.51 |
| CHEMBL302284 | — | — | 1 | 7.47 |
| CHEMBL308926 | — | — | 1 | 7.44 |
| CHEMBL303881 | — | — | 1 | 7.41 |
| CHEMBL71075 | — | — | 1 | 7.39 |
| CHEMBL72261 | — | — | 1 | 7.38 |
| CHEMBL72531 | — | — | 1 | 7.28 |
| CHEMBL46423 | NEVANIMIBE | 2.0 | 1 | 7.28 |
| CHEMBL73336 | — | — | 1 | 7.20 |
| CHEMBL69844 | — | — | 1 | 7.06 |
| CHEMBL307540 | — | — | 1 | 7.04 |
| CHEMBL309182 | — | — | 1 | 7.04 |
| CHEMBL71041 | — | — | 1 | 7.02 |
| CHEMBL310031 | — | — | 1 | 6.96 |
| CHEMBL305235 | — | — | 1 | 6.46 |
| CHEMBL70491 | — | — | 1 | 6.09 |
| CHEMBL306349 | — | — | 1 | 6.07 |
| CHEMBL305819 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL72792 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL296055 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL431981 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL304612 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL74463 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL306266 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL74684 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL71051 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL303612 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL302284 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL308926 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL303881 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL71075 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL72261 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL72531 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL46423 | NEVANIMIBE | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL73336 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL69844 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL307540 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL309182 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL71041 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL310031 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL305235 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL70491 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL306349 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL305819 | — | IC50 | = | 910.0 | nM | 6.04 |