Assay Detail
Functional
CHEMBL4340581
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
28
Total Activities
26
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
Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent β<sub>2</sub>-adrenoceptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 9.90 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445289 | — | — | 2 | 10.68 |
| CHEMBL4473515 | — | — | 2 | 10.44 |
| CHEMBL4469364 | — | — | 1 | 10.39 |
| CHEMBL4577508 | — | — | 1 | 10.39 |
| CHEMBL4473790 | — | — | 1 | 10.37 |
| CHEMBL4561253 | — | — | 1 | 10.31 |
| CHEMBL4556022 | — | — | 1 | 10.30 |
| CHEMBL4576089 | — | — | 1 | 10.29 |
| CHEMBL4575759 | — | — | 1 | 10.19 |
| CHEMBL4588479 | — | — | 1 | 10.13 |
| CHEMBL4536813 | — | — | 1 | 10.13 |
| CHEMBL4537644 | — | — | 1 | 10.12 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 10.11 |
| CHEMBL4438531 | — | — | 1 | 10.09 |
| CHEMBL4454489 | — | — | 1 | 9.88 |
| CHEMBL4541263 | — | — | 1 | 9.82 |
| CHEMBL4542430 | — | — | 1 | 9.79 |
| CHEMBL4473349 | — | — | 1 | 9.66 |
| CHEMBL4460095 | — | — | 1 | 9.65 |
| CHEMBL4566727 | — | — | 1 | 9.52 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | 9.50 |
| CHEMBL4541169 | — | — | 1 | 9.30 |
| CHEMBL4441752 | — | — | 1 | 9.30 |
| CHEMBL4518961 | — | — | 1 | 9.03 |
| CHEMBL4516838 | — | — | 1 | 8.60 |
| CHEMBL4550290 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445289 | — | EC50 | = | 0.021 | nM | 10.68 |
| CHEMBL4445289 | — | EC50 | = | 0.02089 | nM | 10.68 |
| CHEMBL4473515 | — | EC50 | = | 0.03631 | nM | 10.44 |
| CHEMBL4473515 | — | EC50 | = | 0.036 | nM | 10.44 |
| CHEMBL4469364 | — | EC50 | = | 0.04074 | nM | 10.39 |
| CHEMBL4577508 | — | EC50 | = | 0.04074 | nM | 10.39 |
| CHEMBL4473790 | — | EC50 | = | 0.04266 | nM | 10.37 |
| CHEMBL4561253 | — | EC50 | = | 0.04898 | nM | 10.31 |
| CHEMBL4556022 | — | EC50 | = | 0.05012 | nM | 10.30 |
| CHEMBL4576089 | — | EC50 | = | 0.05129 | nM | 10.29 |
| CHEMBL4575759 | — | EC50 | = | 0.06457 | nM | 10.19 |
| CHEMBL4536813 | — | EC50 | = | 0.07413 | nM | 10.13 |
| CHEMBL4588479 | — | EC50 | = | 0.07413 | nM | 10.13 |
| CHEMBL4537644 | — | EC50 | = | 0.07586 | nM | 10.12 |
| CHEMBL1263 | SALMETEROL | EC50 | = | 0.07762 | nM | 10.11 |
| CHEMBL4438531 | — | EC50 | = | 0.08128 | nM | 10.09 |
| CHEMBL4454489 | — | EC50 | = | 0.1318 | nM | 9.88 |
| CHEMBL4541263 | — | EC50 | = | 0.1514 | nM | 9.82 |
| CHEMBL4542430 | — | EC50 | = | 0.1622 | nM | 9.79 |
| CHEMBL4473349 | — | EC50 | = | 0.2188 | nM | 9.66 |
| CHEMBL4460095 | — | EC50 | = | 0.2239 | nM | 9.65 |
| CHEMBL4566727 | — | EC50 | = | 0.302 | nM | 9.52 |
| CHEMBL434 | ISOPROTERENOL | EC50 | = | 0.3162 | nM | 9.50 |
| CHEMBL4541169 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4441752 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4518961 | — | EC50 | = | 0.9333 | nM | 9.03 |
| CHEMBL4516838 | — | EC50 | = | 2.512 | nM | 8.60 |
| CHEMBL4550290 | — | EC50 | = | 9.12 | nM | 8.04 |