Assay Detail
Binding
CHEMBL4425964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting
11
Total Activities
11
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
Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 8.15 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 10.00 |
| CHEMBL420746 | CGP-12177 | — | 1 | 9.70 |
| CHEMBL1233766 | — | — | 1 | 9.52 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 9.52 |
| CHEMBL521606 | NADOLOL | 4.0 | 1 | 8.89 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 6.89 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 6.89 |
| CHEMBL645 | BISOPROLOL | 4.0 | 1 | 6.82 |
| CHEMBL714 | ALBUTEROL | 4.0 | 1 | 6.66 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | 6.58 |
| CHEMBL378501 | CYANOPINDOLOL | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL27 | PROPRANOLOL | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL420746 | CGP-12177 | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL1233766 | — | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL1263 | SALMETEROL | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL521606 | NADOLOL | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL13 | METOPROLOL | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL434 | ISOPROTERENOL | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL645 | BISOPROLOL | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL714 | ALBUTEROL | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL24 | ATENOLOL | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL378501 | CYANOPINDOLOL | Kd | = | 0.001 | nM | - |