Assay Detail
Binding
CHEMBL4402767
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Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 | 7.77 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4537221 | — | — | 1 | 9.31 |
| CHEMBL4456301 | — | — | 1 | 8.96 |
| CHEMBL280822 | CGP-20712A | — | 1 | 8.85 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.62 |
| CHEMBL4437569 | — | — | 1 | 8.59 |
| CHEMBL645 | BISOPROLOL | 4.0 | 1 | 8.28 |
| CHEMBL4566666 | — | — | 1 | 7.66 |
| CHEMBL4553747 | — | — | 1 | 7.57 |
| CHEMBL4463246 | — | — | 1 | 7.54 |
| CHEMBL4463925 | — | — | 1 | 7.48 |
| CHEMBL4443911 | — | — | 1 | 7.31 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 7.31 |
| CHEMBL4576034 | — | — | 1 | 7.15 |
| CHEMBL4450085 | — | — | 1 | 6.82 |
| CHEMBL4473272 | — | — | 1 | 6.66 |
| CHEMBL4456505 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4537221 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL4456301 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL280822 | CGP-20712A | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL4437569 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL645 | BISOPROLOL | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL4566666 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4553747 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4463246 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL4463925 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4443911 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL13 | METOPROLOL | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4576034 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4450085 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4473272 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4456505 | — | Ki | = | 740.0 | nM | 6.13 |