Assay Detail
Binding
CHEMBL5243661
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Inhibition of small intimal microsomal fraction of cholesterol-fed rabbit ACAT using [1-14C]oleoyl CoA incubated for 5 mins
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Small intestine |
| Subcellular | Microsome |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Targeting Sterol <i>O</i>-Acyltransferase/Acyl-CoA:Cholesterol Acyltransferase (ACAT): A Perspective on Small-Molecule Inhibitors and Their Therapeutic Potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.20 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102026 | — | — | 1 | 8.22 |
| CHEMBL5275835 | — | — | 1 | 7.96 |
| CHEMBL278856 | — | — | 1 | 7.89 |
| CHEMBL296055 | — | — | 1 | 7.77 |
| CHEMBL23602 | — | — | 1 | 7.70 |
| CHEMBL405810 | — | — | 1 | 7.58 |
| CHEMBL46423 | NEVANIMIBE | 2.0 | 1 | 7.43 |
| CHEMBL295248 | — | — | 1 | 7.35 |
| CHEMBL417531 | — | — | 1 | 7.34 |
| CHEMBL542103 | NEVANIMIBE HYDROCHLORIDE | 2.0 | 1 | 7.28 |
| CHEMBL42673 | — | — | 1 | 7.25 |
| CHEMBL69844 | — | — | 1 | 7.24 |
| CHEMBL5282347 | — | — | 1 | 7.24 |
| CHEMBL5282801 | — | — | 1 | 7.20 |
| CHEMBL22373 | CL-976 | — | 1 | 6.85 |
| CHEMBL5285031 | — | — | 1 | 6.80 |
| CHEMBL113475 | — | — | 1 | 6.44 |
| CHEMBL5266932 | — | — | 1 | 6.43 |
| CHEMBL89873 | — | — | 1 | 6.04 |
| CHEMBL5275997 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102026 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5275835 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL278856 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL296055 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL23602 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL405810 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL46423 | NEVANIMIBE | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL295248 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL417531 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL542103 | NEVANIMIBE HYDROCHLORIDE | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL42673 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL69844 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5282347 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5282801 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL22373 | CL-976 | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5285031 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL113475 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5266932 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL89873 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5275997 | — | IC50 | = | 1000.0 | nM | 6.00 |