Assay Detail
Binding
CHEMBL652346
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In vitro binding affinity for angiotensin II AT1 receptor in rabbit aorta
8
Total Activities
8
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 highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.98 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293511 | — | — | 1 | 9.70 |
| CHEMBL335778 | — | — | 1 | 9.68 |
| CHEMBL131156 | — | — | 1 | 9.57 |
| CHEMBL7550 | L-158809 | — | 1 | 9.52 |
| CHEMBL336180 | — | — | 1 | 9.17 |
| CHEMBL334670 | — | — | 1 | 8.66 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | — | 1 | 8.22 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293511 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL335778 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL131156 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL7550 | L-158809 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL336180 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL334670 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL907 | CARBOXYLIC ACID METABOLITE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL191 | LOSARTAN | IC50 | = | 50.0 | nM | 7.30 |