Assay Detail
Binding
CHEMBL3239467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-angiotensin 2 from angiotensin AT1 receptor in VSMC of Sprague-Dawley rat thoracic aorta after 60 mins by gamma-counting
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of new 5-nitro benzimidazole derivatives as AT1 antagonists with anti-hypertension activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.38 | 8.99 |
| Ki | 7 | 8.48 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3233516 | — | — | 2 | 9.01 |
| CHEMBL3233518 | — | — | 2 | 8.65 |
| CHEMBL191 | LOSARTAN | 4.0 | 2 | 8.60 |
| CHEMBL3233514 | — | — | 2 | 8.52 |
| CHEMBL3233515 | — | — | 2 | 8.37 |
| CHEMBL3233519 | — | — | 2 | 8.31 |
| CHEMBL3233517 | — | — | 2 | 7.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3233516 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL3233516 | — | IC50 | = | 1.03 | nM | 8.99 |
| CHEMBL3233518 | — | Ki | = | 2.22 | nM | 8.65 |
| CHEMBL191 | LOSARTAN | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL3233514 | — | Ki | = | 3.04 | nM | 8.52 |
| CHEMBL3233518 | — | IC50 | = | 3.32 | nM | 8.48 |
| CHEMBL191 | LOSARTAN | IC50 | = | 3.54 | nM | 8.45 |
| CHEMBL3233514 | — | IC50 | = | 4.12 | nM | 8.38 |
| CHEMBL3233515 | — | Ki | = | 4.23 | nM | 8.37 |
| CHEMBL3233519 | — | Ki | = | 4.89 | nM | 8.31 |
| CHEMBL3233519 | — | IC50 | = | 5.11 | nM | 8.29 |
| CHEMBL3233515 | — | IC50 | = | 5.43 | nM | 8.27 |
| CHEMBL3233517 | — | Ki | = | 13.42 | nM | 7.87 |
| CHEMBL3233517 | — | IC50 | = | 15.74 | nM | 7.80 |