Assay Detail
Binding
CHEMBL645895
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Inhibition against acyl coenzyme A:cholesterol acyltransferase derived from rabbit aorta homogenate
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Acyl-CoA:cholesterol acyltransferase (CHEMBL6141) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Structure-activity relationship of a series of phenylureas linked to 4-phenylimidazole. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity. 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 74 | 6.77 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL46450 | — | — | 1 | 7.92 |
| CHEMBL297553 | — | — | 1 | 7.72 |
| CHEMBL42296 | — | — | 1 | 7.72 |
| CHEMBL42477 | — | — | 1 | 7.51 |
| CHEMBL295867 | — | — | 1 | 7.36 |
| CHEMBL441429 | — | — | 1 | 7.35 |
| CHEMBL44848 | — | — | 1 | 7.32 |
| CHEMBL417896 | — | — | 1 | 7.30 |
| CHEMBL42760 | — | — | 1 | 7.26 |
| CHEMBL46430 | — | — | 1 | 7.22 |
| CHEMBL295878 | — | — | 1 | 7.20 |
| CHEMBL296852 | — | — | 1 | 7.17 |
| CHEMBL44863 | — | — | 1 | 7.17 |
| CHEMBL297351 | — | — | 1 | 7.16 |
| CHEMBL43989 | — | — | 1 | 7.15 |
| CHEMBL44336 | — | — | 1 | 7.14 |
| CHEMBL43603 | — | — | 1 | 7.14 |
| CHEMBL44318 | — | — | 1 | 7.10 |
| CHEMBL295033 | — | — | 1 | 7.08 |
| CHEMBL47030 | — | — | 1 | 7.07 |
| CHEMBL295171 | — | — | 1 | 7.06 |
| CHEMBL297580 | — | — | 1 | 7.05 |
| CHEMBL42165 | — | — | 1 | 7.01 |
| CHEMBL42821 | — | — | 1 | 7.00 |
| CHEMBL296412 | — | — | 1 | 7.00 |
| CHEMBL297454 | — | — | 1 | 7.00 |
| CHEMBL46418 | — | — | 1 | 7.00 |
| CHEMBL296094 | — | — | 1 | 6.96 |
| CHEMBL46641 | — | — | 1 | 6.92 |
| CHEMBL44956 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL46450 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL297553 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL42296 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL42477 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL295867 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL441429 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL44848 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL417896 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL42760 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL46430 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL295878 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL296852 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL44863 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL297351 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL43989 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL44336 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL43603 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL44318 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL295033 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL47030 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL295171 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL297580 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL42165 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL46418 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL297454 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL42821 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL296412 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL296094 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL46641 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL44956 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL296463 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL44755 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL47095 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL43675 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL45033 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL290000 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL43107 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL288332 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL298236 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL47093 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL290630 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL297054 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL296714 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL43908 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL45319 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL43592 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL42873 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL43422 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL47084 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL294932 | — | IC50 | = | 370.0 | nM | 6.43 |