Assay Detail
Binding
CHEMBL4397556
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Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO 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 | Homo sapiens |
| Cell Type | CHO |
| 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 | 7.36 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL324665 | CARAZOLOL | 2.0 | 1 | 10.52 |
| CHEMBL3799125 | — | — | 1 | 10.52 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 9.60 |
| CHEMBL3798017 | (R)-Carvedilol | — | 1 | 9.06 |
| CHEMBL4451135 | — | — | 1 | 8.48 |
| CHEMBL4513932 | — | — | 1 | 8.27 |
| CHEMBL4593181 | — | — | 1 | 8.14 |
| CHEMBL1160694 | — | — | 1 | 7.92 |
| CHEMBL3800303 | — | — | 1 | 7.75 |
| CHEMBL4435895 | — | — | 1 | 7.68 |
| CHEMBL4436343 | — | — | 1 | 7.58 |
| CHEMBL1160723 | LEVISOPRENALINE | 2.0 | 1 | 7.34 |
| CHEMBL3797876 | — | — | 1 | 7.01 |
| CHEMBL4470694 | — | — | 1 | 6.92 |
| CHEMBL4450756 | — | — | 1 | 6.77 |
| CHEMBL4439238 | — | — | 1 | 6.38 |
| CHEMBL4437939 | — | — | 1 | 6.16 |
| CHEMBL4459109 | — | — | 1 | 6.13 |
| CHEMBL4525632 | — | — | 1 | 6.04 |
| CHEMBL4459541 | — | — | 1 | 5.42 |
| CHEMBL4518727 | — | — | 1 | 5.28 |
| CHEMBL4561683 | — | — | 1 | 5.16 |
| CHEMBL4515498 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL324665 | CARAZOLOL | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3799125 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL1263 | SALMETEROL | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3798017 | (R)-Carvedilol | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL4451135 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4513932 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL4593181 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL1160694 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3800303 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4435895 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4436343 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1160723 | LEVISOPRENALINE | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3797876 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL4470694 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4450756 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL4439238 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL4437939 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL4459109 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL4525632 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL4459541 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL4518727 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL4561683 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL4515498 | — | Ki | = | 7900.0 | nM | 5.10 |