Assay Detail
Binding
CHEMBL652724
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Binding affinity against AT-1 receptor from rabbit aorta using [125I]-Sar1-Ile8-Ang II without BSA
9
Total Activities
9
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
A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.71 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24322 | — | — | 1 | 10.00 |
| CHEMBL302102 | — | — | 1 | 8.77 |
| CHEMBL326217 | — | — | 1 | 8.68 |
| CHEMBL324629 | — | — | 1 | 8.62 |
| CHEMBL24861 | — | — | 1 | 8.60 |
| CHEMBL322471 | — | — | 1 | 8.60 |
| CHEMBL110265 | — | — | 1 | 8.41 |
| CHEMBL280526 | — | — | 1 | 8.40 |
| CHEMBL108981 | — | — | 1 | 8.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24322 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL302102 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL326217 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL324629 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL24861 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL322471 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL110265 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL280526 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL108981 | — | IC50 | = | 4.9 | nM | 8.31 |