Assay Detail
Binding
CHEMBL644125
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity against Acyl coenzyme A:cholesterol acyltransferase in intestinal microsomes isolated from cholesterol fed rabbits (IAI).
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 O-acyl transferase (ACAT) as hypocholesterolemic agents. The synthesis and biological activity of a series of malonester amides
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.10 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL164479 | — | — | 1 | 8.40 |
| CHEMBL160103 | — | — | 1 | 8.40 |
| CHEMBL422709 | — | — | 1 | 8.22 |
| CHEMBL164205 | — | — | 1 | 7.96 |
| CHEMBL162996 | — | — | 1 | 7.96 |
| CHEMBL163293 | — | — | 1 | 7.92 |
| CHEMBL159666 | — | — | 1 | 7.92 |
| CHEMBL163325 | — | — | 1 | 7.82 |
| CHEMBL163615 | — | — | 1 | 7.82 |
| CHEMBL349364 | — | — | 1 | 7.57 |
| CHEMBL163562 | — | — | 1 | 7.46 |
| CHEMBL163237 | — | — | 1 | 7.42 |
| CHEMBL350852 | — | — | 1 | 7.38 |
| CHEMBL164203 | — | — | 1 | 7.28 |
| CHEMBL161109 | — | — | 1 | 7.28 |
| CHEMBL163356 | — | — | 1 | 7.17 |
| CHEMBL159285 | — | — | 1 | 7.15 |
| CHEMBL351882 | — | — | 1 | 6.89 |
| CHEMBL163860 | — | — | 1 | 6.68 |
| CHEMBL162831 | — | — | 1 | 6.58 |
| CHEMBL163763 | — | — | 1 | 6.50 |
| CHEMBL159722 | — | — | 1 | 6.09 |
| CHEMBL163688 | — | — | 1 | 6.00 |
| CHEMBL433717 | — | — | 1 | 5.77 |
| CHEMBL348070 | — | — | 1 | 5.75 |
| CHEMBL164260 | — | — | 1 | 5.21 |
| CHEMBL349908 | — | — | 1 | 5.19 |
| CHEMBL351272 | — | — | 1 | - |
| CHEMBL162721 | — | — | 1 | - |
| CHEMBL163208 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL164479 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL160103 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL422709 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL164205 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL162996 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL163293 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL159666 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL163325 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL163615 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL349364 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL163562 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL163237 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL350852 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL164203 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL161109 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL163356 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL159285 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL351882 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL163860 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL162831 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL163763 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL159722 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL163688 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL433717 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL348070 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL164260 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL349908 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL351272 | — | IC50 | < | -73.0 | % | - |
| CHEMBL162721 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL163208 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL163214 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL163212 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL262010 | — | IC50 | > | 5000.0 | nM | - |