Assay Detail
Binding
CHEMBL4425965
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Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd 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 | 6.38 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378501 | CYANOPINDOLOL | — | 1 | 9.15 |
| CHEMBL420746 | CGP-12177 | — | 1 | 7.72 |
| CHEMBL521606 | NADOLOL | 4.0 | 1 | 7.16 |
| CHEMBL27 | PROPRANOLOL | 4.0 | 1 | 6.82 |
| CHEMBL1233766 | — | — | 1 | 6.20 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 6.13 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 5.96 |
| CHEMBL24 | ATENOLOL | 4.0 | 1 | 5.92 |
| CHEMBL714 | ALBUTEROL | 4.0 | 1 | 5.85 |
| CHEMBL13 | METOPROLOL | 4.0 | 1 | 4.81 |
| CHEMBL645 | BISOPROLOL | 4.0 | 1 | 4.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378501 | CYANOPINDOLOL | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL420746 | CGP-12177 | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL521606 | NADOLOL | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL27 | PROPRANOLOL | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL1233766 | — | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL434 | ISOPROTERENOL | Kd | = | 740.0 | nM | 6.13 |
| CHEMBL1263 | SALMETEROL | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL24 | ATENOLOL | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL714 | ALBUTEROL | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL13 | METOPROLOL | Kd | = | 15500.0 | nM | 4.81 |
| CHEMBL645 | BISOPROLOL | Kd | = | 33000.0 | nM | 4.48 |