Assay Detail
Binding
CHEMBL637692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested for inhibition against acyl coenzyme A:cholesterol acyltransferase from rabbit aorta homogenate.
38
Total Activities
38
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 N-[2-(dimethylamino)-6-[3-(5-methyl-4-phenyl-1H-imidazol-1-yl)propoxy] phenyl]-N'-pentylurea and analogues. Novel potent inhibitors of acyl-CoA:cholesterol O-acyltransferase with antiatherosclerotic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.21 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42765 | — | — | 1 | 7.30 |
| CHEMBL42045 | — | — | 1 | 7.24 |
| CHEMBL46738 | — | — | 1 | 7.00 |
| CHEMBL296094 | — | — | 1 | 6.96 |
| CHEMBL43095 | — | — | 1 | 6.85 |
| CHEMBL440475 | — | — | 1 | 6.80 |
| CHEMBL42166 | — | — | 1 | 6.75 |
| CHEMBL44071 | — | — | 1 | 6.75 |
| CHEMBL43362 | — | — | 1 | 6.68 |
| CHEMBL47071 | — | — | 1 | 6.64 |
| CHEMBL291173 | — | — | 1 | 6.60 |
| CHEMBL43036 | — | — | 1 | 6.55 |
| CHEMBL44471 | — | — | 1 | 6.54 |
| CHEMBL42395 | — | — | 1 | 6.40 |
| CHEMBL41992 | — | — | 1 | 6.39 |
| CHEMBL43505 | — | — | 1 | 6.37 |
| CHEMBL42668 | — | — | 1 | 6.33 |
| CHEMBL296421 | — | — | 1 | 6.32 |
| CHEMBL40516 | — | — | 1 | 6.21 |
| CHEMBL298440 | — | — | 1 | 6.14 |
| CHEMBL44358 | — | — | 1 | 6.11 |
| CHEMBL43109 | — | — | 1 | 6.09 |
| CHEMBL277986 | CL-277082 | — | 1 | 6.05 |
| CHEMBL298486 | — | — | 1 | 6.00 |
| CHEMBL290627 | — | — | 1 | 5.97 |
| CHEMBL295979 | — | — | 1 | 5.89 |
| CHEMBL42942 | — | — | 1 | 5.88 |
| CHEMBL42813 | — | — | 1 | 5.85 |
| CHEMBL42488 | — | — | 1 | 5.82 |
| CHEMBL42082 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42765 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL42045 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL46738 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL296094 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL43095 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL440475 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL42166 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL44071 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL43362 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL47071 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL291173 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL43036 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL44471 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL42395 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL41992 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL43505 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL42668 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL296421 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL40516 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL298440 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL44358 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL43109 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL277986 | CL-277082 | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL298486 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL290627 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL295979 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL42942 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL42813 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL42488 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL42082 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL41127 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL297206 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL44495 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL288771 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL287842 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL41960 | — | IC50 | = | 7230.0 | nM | 5.14 |
| CHEMBL42111 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL42807 | — | IC50 | > | 10000.0 | nM | - |