Assay Detail
Binding
CHEMBL4402769
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Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 3 | 8.34 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL280822 | CGP-20712A | — | 1 | 8.92 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 8.85 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 7.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL280822 | CGP-20712A | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL27 | PROPRANOLOL | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL13 | METOPROLOL | Ki | = | 55.0 | nM | 7.26 |