Assay Detail
Functional
CHEMBL4375058
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Antagonist activity at beta2 adrenergic receptor (unknown origin) expressed in HEK293 cell assessed as inhibition of isoproterenol-induced cAMP production preincubated for 15 mins followed by isoproterenol addition and measured after 15 mins
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Probing the Existence of a Metastable Binding Site at the β<sub>2</sub>-Adrenergic Receptor with Homobivalent Bitopic Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.40 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1160734 | — | — | 1 | 9.14 |
| CHEMBL266195 | ALPRENOLOL | 2.0 | 1 | 8.94 |
| CHEMBL4514723 | — | — | 1 | 8.92 |
| CHEMBL4594173 | — | — | 1 | 8.81 |
| CHEMBL4446394 | — | — | 1 | 8.80 |
| CHEMBL4564189 | — | — | 1 | 8.75 |
| CHEMBL4462252 | — | — | 1 | 8.69 |
| CHEMBL4574652 | — | — | 1 | 8.66 |
| CHEMBL1395661 | — | — | 1 | 8.63 |
| CHEMBL4473518 | — | — | 1 | 8.49 |
| CHEMBL4450606 | — | — | 1 | 8.48 |
| CHEMBL4527821 | — | — | 1 | 8.28 |
| CHEMBL4442559 | — | — | 1 | 8.20 |
| CHEMBL4530266 | — | — | 1 | 7.92 |
| CHEMBL4434772 | — | — | 1 | 7.86 |
| CHEMBL4441975 | — | — | 1 | 7.59 |
| CHEMBL4474813 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1160734 | — | IC50 | = | 0.7244 | nM | 9.14 |
| CHEMBL266195 | ALPRENOLOL | IC50 | = | 1.148 | nM | 8.94 |
| CHEMBL4514723 | — | IC50 | = | 1.202 | nM | 8.92 |
| CHEMBL4594173 | — | IC50 | = | 1.549 | nM | 8.81 |
| CHEMBL4446394 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL4564189 | — | IC50 | = | 1.778 | nM | 8.75 |
| CHEMBL4462252 | — | IC50 | = | 2.042 | nM | 8.69 |
| CHEMBL4574652 | — | IC50 | = | 2.188 | nM | 8.66 |
| CHEMBL1395661 | — | IC50 | = | 2.344 | nM | 8.63 |
| CHEMBL4473518 | — | IC50 | = | 3.236 | nM | 8.49 |
| CHEMBL4450606 | — | IC50 | = | 3.311 | nM | 8.48 |
| CHEMBL4527821 | — | IC50 | = | 5.248 | nM | 8.28 |
| CHEMBL4442559 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4530266 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL4434772 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4441975 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL4474813 | — | IC50 | = | 213.8 | nM | 6.67 |