Assay Detail
Binding
CHEMBL4397558
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Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
8
Total Activities
7
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
Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 6.30 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1160723 | LEVISOPRENALINE | 2.0 | 1 | 7.60 |
| CHEMBL3797876 | — | — | 1 | 7.40 |
| CHEMBL4435895 | — | — | 2 | 6.52 |
| CHEMBL1160694 | — | — | 1 | 6.20 |
| CHEMBL3800303 | — | — | 1 | 5.70 |
| CHEMBL4593181 | — | — | 1 | 5.60 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1160723 | LEVISOPRENALINE | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3797876 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4435895 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1160694 | — | EC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4435895 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3800303 | — | EC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4593181 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL1263 | SALMETEROL | EC50 | = | 5011.87 | nM | 5.30 |