Assay Detail
Functional
CHEMBL648491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vivo percent inhibition of Angiotensin II receptor, type 1 induced increase in diastolic blood pressure in pithed rat at 3 mg/kg i.d.
6
Total Activities
6
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Functional |
| Tissue | Artery |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
(6-oxo-3-pyridazinyl)-benzimidazoles as potent angiotensin II receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.20 | 7.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| DOSE | DOSE | 3.0 | mg.kg-1 | — |
| ROUTE | ROUTE | - | — | Intraduodenal |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL24266 | — | — | 1 | 7.40 |
| CHEMBL2079790 | — | — | 1 | 7.25 |
| CHEMBL284704 | — | — | 1 | 7.24 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.13 |
| CHEMBL2079785 | — | — | 1 | 7.10 |
| CHEMBL24224 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL24266 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2079790 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL284704 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL191 | LOSARTAN | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2079785 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL24224 | — | IC50 | = | 80.0 | nM | 7.10 |