Assay Detail
Binding
CHEMBL637685
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In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase in liver microsomes isolated from cholesterol-fed rabbits
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Liver |
| Subcellular | Microsome |
| 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. 1. Synthesis and hypocholesterolemic activity of dibenz[b,e]oxepin-11-carboxanilides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 47 | 6.81 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL353791 | — | — | 1 | 8.15 |
| CHEMBL166556 | — | — | 1 | 7.64 |
| CHEMBL348853 | — | — | 1 | 7.60 |
| CHEMBL167205 | — | — | 1 | 7.57 |
| CHEMBL166647 | — | — | 1 | 7.46 |
| CHEMBL165988 | — | — | 1 | 7.41 |
| CHEMBL353609 | — | — | 1 | 7.40 |
| CHEMBL167500 | — | — | 1 | 7.30 |
| CHEMBL352840 | — | — | 1 | 7.26 |
| CHEMBL168159 | — | — | 1 | 7.24 |
| CHEMBL355357 | — | — | 1 | 7.19 |
| CHEMBL168406 | — | — | 1 | 7.13 |
| CHEMBL351292 | — | — | 1 | 7.11 |
| CHEMBL433915 | — | — | 1 | 7.03 |
| CHEMBL167186 | — | — | 1 | 7.00 |
| CHEMBL353082 | — | — | 1 | 6.96 |
| CHEMBL355025 | — | — | 1 | 6.92 |
| CHEMBL353175 | — | — | 1 | 6.89 |
| CHEMBL165984 | — | — | 1 | 6.85 |
| CHEMBL167466 | — | — | 1 | 6.82 |
| CHEMBL354494 | — | — | 1 | 6.82 |
| CHEMBL354290 | — | — | 1 | 6.80 |
| CHEMBL354571 | — | — | 1 | 6.75 |
| CHEMBL167198 | — | — | 1 | 6.75 |
| CHEMBL353236 | — | — | 1 | 6.72 |
| CHEMBL352693 | — | — | 1 | 6.72 |
| CHEMBL353227 | — | — | 1 | 6.72 |
| CHEMBL353958 | — | — | 1 | 6.68 |
| CHEMBL167652 | — | — | 1 | 6.62 |
| CHEMBL423267 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL353791 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL166556 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL348853 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL167205 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL166647 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL165988 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL353609 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL167500 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL352840 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL168159 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL355357 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL168406 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL351292 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL433915 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL167186 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL353082 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL355025 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL353175 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL165984 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL167466 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL354494 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL354290 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL167198 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL354571 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL353236 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL352693 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL353227 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL353958 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL167652 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL423267 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL355255 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL353517 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL353660 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL277986 | CL-277082 | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL352772 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL166281 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL167532 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL354659 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL167785 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL166873 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL167674 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL167784 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL168617 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL353898 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL166042 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL352567 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL168160 | — | IC50 | = | 940.0 | nM | 6.03 |