Assay Detail
Binding
CHEMBL4402768
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Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of covalent antagonists for β1- and β2-adrenergic receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.37 | 10.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4456301 | — | — | 1 | 10.14 |
| CHEMBL4537221 | — | — | 1 | 9.80 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 9.49 |
| CHEMBL4463925 | — | — | 1 | 8.96 |
| CHEMBL4463246 | — | — | 1 | 8.47 |
| CHEMBL4566666 | — | — | 1 | 7.70 |
| CHEMBL4437569 | — | — | 1 | 7.29 |
| CHEMBL4553747 | — | — | 1 | 7.24 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 6.66 |
| CHEMBL645 | BISOPROLOL | 4.0 | 1 | 6.60 |
| CHEMBL4473272 | — | — | 1 | 6.50 |
| CHEMBL280822 | CGP-20712A | — | 1 | 6.00 |
| CHEMBL4456505 | — | — | 1 | 5.89 |
| CHEMBL4576034 | — | — | 1 | 5.85 |
| CHEMBL4443911 | — | — | 1 | 5.70 |
| CHEMBL4450085 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4456301 | — | Ki | = | 0.073 | nM | 10.14 |
| CHEMBL4537221 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL4463925 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4463246 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4566666 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4437569 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4553747 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL13 | METOPROLOL | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL645 | BISOPROLOL | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4473272 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL280822 | CGP-20712A | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4456505 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4576034 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4443911 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL4450085 | — | Ki | = | 2200.0 | nM | 5.66 |