Assay Detail
Binding
CHEMBL4397555
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Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
23
Total Activities
23
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
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.21 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324665 | CARAZOLOL | 2.0 | 1 | 10.05 |
| CHEMBL3799125 | — | — | 1 | 9.68 |
| CHEMBL3798017 | (R)-Carvedilol | — | 1 | 8.47 |
| CHEMBL4593181 | — | — | 1 | 8.19 |
| CHEMBL4451135 | — | — | 1 | 8.18 |
| CHEMBL4435895 | — | — | 1 | 7.92 |
| CHEMBL1160694 | — | — | 1 | 7.85 |
| CHEMBL4513932 | — | — | 1 | 7.62 |
| CHEMBL3800303 | — | — | 1 | 7.07 |
| CHEMBL3797876 | — | — | 1 | 6.80 |
| CHEMBL1160723 | LEVISOPRENALINE | 2.0 | 1 | 6.66 |
| CHEMBL4470694 | — | — | 1 | 6.51 |
| CHEMBL4436343 | — | — | 1 | 6.48 |
| CHEMBL4450756 | — | — | 1 | 6.47 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.26 |
| CHEMBL4439238 | — | — | 1 | 6.07 |
| CHEMBL4437939 | — | — | 1 | 5.92 |
| CHEMBL4459109 | — | — | 1 | 5.62 |
| CHEMBL4515498 | — | — | 1 | 5.13 |
| CHEMBL4525632 | — | — | 1 | - |
| CHEMBL4561683 | — | — | 1 | - |
| CHEMBL4518727 | — | — | 1 | - |
| CHEMBL4459541 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324665 | CARAZOLOL | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL3799125 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL4593181 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL4451135 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4435895 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1160694 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4513932 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3800303 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL3797876 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL1160723 | LEVISOPRENALINE | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL4470694 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4436343 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL4450756 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL1263 | SALMETEROL | Ki | = | 550.0 | nM | 6.26 |
| CHEMBL4439238 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL4437939 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL4459109 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL4515498 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL4525632 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4561683 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4518727 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4459541 | — | Ki | > | 10000.0 | nM | - |