Assay Detail
Binding
CHEMBL3117635
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Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.11 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1017 | TELMISARTAN | 4.0 | 1 | 8.70 |
| CHEMBL3115247 | — | — | 1 | 8.22 |
| CHEMBL3115243 | — | — | 1 | 7.64 |
| CHEMBL3115246 | — | — | 1 | 7.22 |
| CHEMBL3115242 | — | — | 1 | 7.07 |
| CHEMBL3115245 | — | — | 1 | 7.01 |
| CHEMBL3115236 | — | — | 1 | 6.89 |
| CHEMBL601678 | — | — | 1 | 6.54 |
| CHEMBL3115244 | — | — | 1 | 6.00 |
| CHEMBL3115241 | — | — | 1 | 5.77 |
| CHEMBL3115240 | — | — | 1 | - |
| CHEMBL3115239 | — | — | 1 | - |
| CHEMBL3115238 | — | — | 1 | - |
| CHEMBL3115237 | — | — | 1 | - |
| CHEMBL602468 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1017 | TELMISARTAN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3115247 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3115243 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3115246 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3115242 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3115245 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL3115236 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL601678 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL3115244 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3115241 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL3115240 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3115239 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3115238 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3115237 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL602468 | — | IC50 | > | 10000.0 | nM | - |