Assay Detail
Binding
CHEMBL646055
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Concentration required for the in vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase (ACAT) in liver microsomes isolated from cholesterol-fed rats was determined
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 13. Design, synthesis and biological evaluation of tetrazole anilides as potent inhibitors of ACAT in vitro and hypocholesterolemic agents in vivo
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.31 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306344 | — | — | 1 | 8.00 |
| CHEMBL77370 | — | — | 3 | 7.85 |
| CHEMBL102912 | — | — | 1 | 7.66 |
| CHEMBL100448 | — | — | 1 | 7.28 |
| CHEMBL103748 | — | — | 1 | 7.10 |
| CHEMBL22373 | CL-976 | — | 1 | 6.96 |
| CHEMBL318600 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306344 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL77370 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL102912 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL77370 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL100448 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL103748 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL22373 | CL-976 | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL318600 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL77370 | — | IC50 | = | 330.0 | nM | 6.48 |