Assay Detail
Binding
CHEMBL644582
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Binding affinity for Angiotensin II receptor, type 1 measured by ability to displace [125I]- A II from its specific binding site in rat liver membrane
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Type-1 angiotensin II receptor B (CHEMBL263) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
A new series of imidazolones: highly specific and potent nonpeptide AT1 angiotensin II receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 6.74 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | 4.0 | 1 | 8.89 |
| CHEMBL938 | SARALASIN | 4.0 | 1 | 8.62 |
| CHEMBL116170 | — | — | 1 | 8.14 |
| CHEMBL325201 | — | — | 1 | 8.06 |
| CHEMBL439968 | — | — | 1 | 8.00 |
| CHEMBL191 | LOSARTAN | 4.0 | 1 | 7.85 |
| CHEMBL115984 | — | — | 1 | 7.75 |
| CHEMBL114687 | — | — | 1 | 7.70 |
| CHEMBL114267 | — | — | 1 | 7.62 |
| CHEMBL419583 | — | — | 1 | 7.57 |
| CHEMBL290988 | — | — | 1 | 7.46 |
| CHEMBL113674 | — | — | 1 | 7.42 |
| CHEMBL325445 | — | — | 1 | 7.33 |
| CHEMBL114720 | — | — | 1 | 7.31 |
| CHEMBL296883 | — | — | 1 | 7.25 |
| CHEMBL114710 | — | — | 1 | 7.23 |
| CHEMBL114983 | — | — | 1 | 7.22 |
| CHEMBL324452 | — | — | 1 | 7.21 |
| CHEMBL114656 | — | — | 1 | 7.18 |
| CHEMBL44268 | — | — | 1 | 7.10 |
| CHEMBL327018 | — | — | 1 | 7.10 |
| CHEMBL112343 | — | — | 1 | 6.96 |
| CHEMBL113330 | — | — | 1 | 6.85 |
| CHEMBL115193 | — | — | 1 | 6.82 |
| CHEMBL115492 | — | — | 1 | 6.82 |
| CHEMBL324785 | — | — | 1 | 6.72 |
| CHEMBL110974 | — | — | 1 | 6.66 |
| CHEMBL114368 | — | — | 1 | 6.60 |
| CHEMBL325684 | — | — | 1 | 6.58 |
| CHEMBL113039 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1513 | IRBESARTAN | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL938 | SARALASIN | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL116170 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL325201 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL439968 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL191 | LOSARTAN | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL115984 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL114687 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL114267 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL419583 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL290988 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL113674 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL325445 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL114720 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL296883 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL114710 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL114983 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL324452 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL114656 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL44268 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL327018 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL112343 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL113330 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL115193 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL115492 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL324785 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL110974 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL114368 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL325684 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL113039 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL324245 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL323244 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL332051 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL325905 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL410724 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL111968 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL115204 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL114771 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL114590 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL46782 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL325502 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL113701 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL45493 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL115771 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL324888 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL115835 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL444060 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL423325 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL325751 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL114625 | — | IC50 | = | 10000.0 | nM | 5.00 |