Assay Detail
Functional
CHEMBL3603442
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
14
Total Activities
14
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
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 6.72 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 8.04 |
| CHEMBL3601310 | — | — | 1 | 7.48 |
| CHEMBL3601203 | — | — | 1 | 7.21 |
| CHEMBL3601200 | — | — | 1 | 6.66 |
| CHEMBL3601201 | — | — | 1 | 6.60 |
| CHEMBL3601202 | — | — | 1 | 6.56 |
| CHEMBL3601308 | — | — | 1 | 6.09 |
| CHEMBL3601204 | — | — | 1 | 6.07 |
| CHEMBL3600395 | — | — | 1 | 5.81 |
| CHEMBL3601305 | — | — | 1 | - |
| CHEMBL3601306 | — | — | 1 | - |
| CHEMBL3601307 | — | — | 1 | - |
| CHEMBL3601309 | — | — | 1 | - |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1437 | NOREPINEPHRINE | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL3601310 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3601203 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3601200 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3601201 | — | EC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3601202 | — | EC50 | = | 277.0 | nM | 6.56 |
| CHEMBL3601308 | — | EC50 | = | 812.0 | nM | 6.09 |
| CHEMBL3601204 | — | EC50 | = | 857.0 | nM | 6.07 |
| CHEMBL3600395 | — | EC50 | = | 1548.0 | nM | 5.81 |
| CHEMBL3601305 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3601306 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3601307 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3601309 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL434 | ISOPROTERENOL | EC50 | - | — | - |