Assay Detail
Binding
CHEMBL2020966
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [I125]angiotensin2 from AT1 receptor in Sprague-Dawley rat VSMC after 2.5 hrs by gamma spectrophotometry
30
Total Activities
10
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 novel potent angiotensin II receptor antagonists with anti-hypertension effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.24 | 9.31 |
| Ki | 10 | 8.40 | 9.48 |
| Inhibition | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017293 | — | — | 3 | 9.48 |
| CHEMBL1513 | IRBESARTAN | 4.0 | 3 | 9.39 |
| CHEMBL2017294 | — | — | 3 | 8.99 |
| CHEMBL1069 | VALSARTAN | 4.0 | 3 | 8.65 |
| CHEMBL2017292 | — | — | 3 | 8.18 |
| CHEMBL2017295 | — | — | 3 | 8.16 |
| CHEMBL2017297 | — | — | 3 | 7.92 |
| CHEMBL2017299 | — | — | 3 | 7.85 |
| CHEMBL2017298 | — | — | 3 | 7.75 |
| CHEMBL2017296 | — | — | 3 | 7.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017293 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL1513 | IRBESARTAN | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL2017293 | — | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL1513 | IRBESARTAN | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL2017294 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL2017294 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1069 | VALSARTAN | Ki | = | 2.22 | nM | 8.65 |
| CHEMBL1069 | VALSARTAN | IC50 | = | 2.64 | nM | 8.58 |
| CHEMBL2017292 | — | Ki | = | 6.65 | nM | 8.18 |
| CHEMBL2017295 | — | Ki | = | 6.88 | nM | 8.16 |
| CHEMBL2017292 | — | IC50 | = | 9.82 | nM | 8.01 |
| CHEMBL2017295 | — | IC50 | = | 10.18 | nM | 7.99 |
| CHEMBL2017297 | — | Ki | = | 12.16 | nM | 7.92 |
| CHEMBL2017299 | — | Ki | = | 14.06 | nM | 7.85 |
| CHEMBL2017297 | — | IC50 | = | 17.99 | nM | 7.75 |
| CHEMBL2017298 | — | Ki | = | 17.92 | nM | 7.75 |
| CHEMBL2017299 | — | IC50 | = | 20.81 | nM | 7.68 |
| CHEMBL2017296 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL2017298 | — | IC50 | = | 26.52 | nM | 7.58 |
| CHEMBL2017296 | — | IC50 | = | 35.97 | nM | 7.44 |
| CHEMBL1513 | IRBESARTAN | Inhibition | - | % | - | |
| CHEMBL1069 | VALSARTAN | Inhibition | - | % | - | |
| CHEMBL2017299 | — | Inhibition | - | % | - | |
| CHEMBL2017298 | — | Inhibition | - | % | - | |
| CHEMBL2017297 | — | Inhibition | - | % | - | |
| CHEMBL2017296 | — | Inhibition | - | % | - | |
| CHEMBL2017295 | — | Inhibition | - | % | - | |
| CHEMBL2017294 | — | Inhibition | - | % | - | |
| CHEMBL2017293 | — | Inhibition | - | % | - | |
| CHEMBL2017292 | — | Inhibition | - | % | - |