Assay Detail
Functional
CHEMBL643360
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase in intestinal microsomes isolated from cholesterol-fed rabbits
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Intestine |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Inhibitors of acyl-CoA:cholesterol acyltransferase. 5. Identification and structure-activity relationships of novel beta-ketoamides as hypocholesterolemic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.00 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL102026 | — | — | 1 | 8.22 |
| CHEMBL316724 | — | — | 1 | 7.96 |
| CHEMBL102041 | — | — | 1 | 7.96 |
| CHEMBL98602 | — | — | 1 | 7.66 |
| CHEMBL98640 | — | — | 1 | 7.62 |
| CHEMBL101922 | — | — | 1 | 7.46 |
| CHEMBL431235 | — | — | 1 | 7.36 |
| CHEMBL99164 | — | — | 1 | 7.28 |
| CHEMBL98953 | — | — | 1 | 7.24 |
| CHEMBL318825 | — | — | 1 | 6.68 |
| CHEMBL101517 | — | — | 1 | 6.64 |
| CHEMBL98482 | — | — | 1 | 6.58 |
| CHEMBL101489 | — | — | 1 | 6.43 |
| CHEMBL99162 | — | — | 1 | 6.40 |
| CHEMBL317863 | — | — | 1 | 6.09 |
| CHEMBL420829 | — | — | 1 | 6.00 |
| CHEMBL98600 | — | — | 1 | 5.46 |
| CHEMBL98377 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL102026 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL316724 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL102041 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL98602 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL98640 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL101922 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL431235 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL99164 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL98953 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL318825 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL101517 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL98482 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL101489 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL99162 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL317863 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL420829 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL98600 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL98377 | — | IC50 | > | 1000.0 | nM | - |