Assay Detail
Binding
CHEMBL648856
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In vitro inhibitory activity against Angiotensin II receptor, type 1 to displace 125I-Sar,Ile8-AII in rabbit aorta
25
Total Activities
25
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
Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.23 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL350121 | — | — | 1 | 9.70 |
| CHEMBL162148 | — | — | 1 | 9.30 |
| CHEMBL165349 | — | — | 1 | 8.77 |
| CHEMBL348758 | — | — | 1 | 8.72 |
| CHEMBL165354 | — | — | 1 | 8.70 |
| CHEMBL59957 | — | — | 1 | 8.62 |
| CHEMBL163486 | — | — | 1 | 8.59 |
| CHEMBL349389 | — | — | 1 | 8.54 |
| CHEMBL164059 | — | — | 1 | 8.37 |
| CHEMBL349856 | — | — | 1 | 8.24 |
| CHEMBL423801 | — | — | 1 | 8.22 |
| CHEMBL115021 | — | — | 1 | 8.22 |
| CHEMBL162859 | — | — | 1 | 8.21 |
| CHEMBL352675 | — | — | 1 | 8.15 |
| CHEMBL163485 | — | — | 1 | 8.13 |
| CHEMBL291582 | — | — | 1 | 8.10 |
| CHEMBL350493 | — | — | 1 | 8.06 |
| CHEMBL349869 | — | — | 1 | 7.92 |
| CHEMBL164617 | — | — | 1 | 7.89 |
| CHEMBL422200 | — | — | 1 | 7.82 |
| CHEMBL349652 | — | — | 1 | 7.70 |
| CHEMBL163628 | — | — | 1 | 7.68 |
| CHEMBL350851 | — | — | 1 | 7.50 |
| CHEMBL349020 | — | — | 1 | 7.41 |
| CHEMBL164552 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL350121 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL162148 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL165349 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL348758 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL165354 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL59957 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL163486 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL349389 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL164059 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL349856 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL423801 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL115021 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL162859 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL352675 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL163485 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL291582 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL350493 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL349869 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL164617 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL422200 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL349652 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL163628 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL350851 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL349020 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL164552 | — | IC50 | = | 50.0 | nM | 7.30 |