Assay Detail
Binding
CHEMBL2211309
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Displacement of [125I]Angiotensin-2 from angiotensin AT1 receptor in Sprague-Dawley rat VSMC after 60 mins by gamma counting
27
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of new fluorine substituted derivatives as angiotensin II receptor antagonists with anti-hypertension and anti-tumor effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 9 | - | - |
| Ki | 9 | 8.43 | 9.38 |
| IC50 | 9 | 8.31 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206083 | — | — | 3 | 9.38 |
| CHEMBL191 | LOSARTAN | 4.0 | 3 | 8.85 |
| CHEMBL1069 | VALSARTAN | 4.0 | 3 | 8.68 |
| CHEMBL1513 | IRBESARTAN | 4.0 | 3 | 8.56 |
| CHEMBL2206084 | — | — | 3 | 8.42 |
| CHEMBL2206085 | — | — | 3 | 8.17 |
| CHEMBL2206086 | — | — | 3 | 8.04 |
| CHEMBL2206088 | — | — | 3 | 8.04 |
| CHEMBL2206087 | — | — | 3 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206083 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL2206083 | — | IC50 | = | 0.584 | nM | 9.23 |
| CHEMBL191 | LOSARTAN | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL191 | LOSARTAN | IC50 | = | 1.64 | nM | 8.79 |
| CHEMBL1069 | VALSARTAN | Ki | = | 2.08 | nM | 8.68 |
| CHEMBL1069 | VALSARTAN | IC50 | = | 2.64 | nM | 8.58 |
| CHEMBL1513 | IRBESARTAN | Ki | = | 2.75 | nM | 8.56 |
| CHEMBL1513 | IRBESARTAN | IC50 | = | 3.11 | nM | 8.51 |
| CHEMBL2206084 | — | Ki | = | 3.78 | nM | 8.42 |
| CHEMBL2206084 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL2206085 | — | Ki | = | 6.75 | nM | 8.17 |
| CHEMBL2206088 | — | Ki | = | 9.17 | nM | 8.04 |
| CHEMBL2206086 | — | Ki | = | 9.11 | nM | 8.04 |
| CHEMBL2206085 | — | IC50 | = | 9.98 | nM | 8.00 |
| CHEMBL2206088 | — | IC50 | = | 13.57 | nM | 7.87 |
| CHEMBL2206086 | — | IC50 | = | 13.48 | nM | 7.87 |
| CHEMBL2206087 | — | Ki | = | 17.65 | nM | 7.75 |
| CHEMBL2206087 | — | IC50 | = | 26.12 | nM | 7.58 |
| CHEMBL2206088 | — | Inhibition | - | % | - | |
| CHEMBL2206087 | — | Inhibition | - | % | - | |
| CHEMBL2206086 | — | Inhibition | - | % | - | |
| CHEMBL2206084 | — | Inhibition | - | % | - | |
| CHEMBL2206085 | — | Inhibition | - | % | - | |
| CHEMBL2206083 | — | Inhibition | - | % | - | |
| CHEMBL191 | LOSARTAN | Inhibition | - | % | - | |
| CHEMBL1513 | IRBESARTAN | Inhibition | - | % | - | |
| CHEMBL1069 | VALSARTAN | Inhibition | - | % | - |