Assay Detail
Functional
CHEMBL872983
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ACAT activity was determined in rat hepatic microsomes by measuring the formation of labeled cholesteryl oleate (pmol/midmg) from [14C]oleoyl-CoA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.55 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274185 | LECIMIBIDE | 2.0 | 1 | 8.00 |
| CHEMBL273826 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274185 | LECIMIBIDE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL273826 | — | IC50 | = | 80.0 | nM | 7.10 |