Assay Detail
ADMET
CHEMBL4610313
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Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β<sub>2</sub>-adrenoceptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 8.05 | 8.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4645927 | — | — | 1 | 8.91 |
| CHEMBL4635163 | — | — | 1 | 8.85 |
| CHEMBL1711 | ISOPROTERENOL HYDROCHLORIDE | 4.0 | 1 | 8.81 |
| CHEMBL4642770 | — | — | 1 | 8.41 |
| CHEMBL4636255 | — | — | 1 | 8.38 |
| CHEMBL4646881 | — | — | 1 | 8.27 |
| CHEMBL4641262 | — | — | 1 | 8.25 |
| CHEMBL4645203 | — | — | 1 | 8.09 |
| CHEMBL4645694 | — | — | 1 | 7.91 |
| CHEMBL4638864 | — | — | 1 | 7.83 |
| CHEMBL2105743 | OLODATEROL HYDROCHLORIDE | 4.0 | 1 | 7.56 |
| CHEMBL4644638 | — | — | 1 | 7.54 |
| CHEMBL4634131 | — | — | 1 | 7.44 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 6.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4645927 | — | EC50 | = | 1.23 | nM | 8.91 |
| CHEMBL4635163 | — | EC50 | = | 1.413 | nM | 8.85 |
| CHEMBL1711 | ISOPROTERENOL HYDROCHLORIDE | EC50 | = | 1.549 | nM | 8.81 |
| CHEMBL4642770 | — | EC50 | = | 3.89 | nM | 8.41 |
| CHEMBL4636255 | — | EC50 | = | 4.169 | nM | 8.38 |
| CHEMBL4646881 | — | EC50 | = | 5.37 | nM | 8.27 |
| CHEMBL4641262 | — | EC50 | = | 5.623 | nM | 8.25 |
| CHEMBL4645203 | — | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4645694 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4638864 | — | EC50 | = | 14.79 | nM | 7.83 |
| CHEMBL2105743 | OLODATEROL HYDROCHLORIDE | EC50 | = | 27.54 | nM | 7.56 |
| CHEMBL4644638 | — | EC50 | = | 28.84 | nM | 7.54 |
| CHEMBL4634131 | — | EC50 | = | 36.31 | nM | 7.44 |
| CHEMBL1263 | SALMETEROL | EC50 | = | 316.23 | nM | 6.50 |