Assay Detail
Binding
CHEMBL649710
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Inhibition of Angiotensin II receptor type 1 in rabbit aorta binding assay
12
Total Activities
12
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 | Intermediate |
Target
Type-1 angiotensin II receptor (CHEMBL3948) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.34 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293511 | — | — | 1 | 9.52 |
| CHEMBL58291 | — | — | 1 | 9.52 |
| CHEMBL7550 | L-158809 | — | 1 | 9.10 |
| CHEMBL57976 | — | — | 1 | 8.82 |
| CHEMBL58156 | — | — | 1 | 8.64 |
| CHEMBL56549 | — | — | 1 | 8.28 |
| CHEMBL293949 | — | — | 1 | 8.12 |
| CHEMBL58499 | — | — | 1 | 8.00 |
| CHEMBL57853 | — | — | 1 | 8.00 |
| CHEMBL300154 | — | — | 1 | 7.62 |
| CHEMBL299897 | — | — | 1 | 7.36 |
| CHEMBL292829 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293511 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL58291 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL7550 | L-158809 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL57976 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL58156 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL56549 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL293949 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL58499 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL57853 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL300154 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL299897 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL292829 | — | IC50 | = | 87.0 | nM | 7.06 |