Assay Detail
ADMET
CHEMBL4051037
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Agonist activity at recombinant human alpha1A adrenergic receptor expressed in HEK293 cells assessed as intercellular Ca mobilization by Fura-2AM dye-based fluorescence assay
12
Total Activities
12
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
Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 6.54 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 8.04 |
| CHEMBL4104183 | — | — | 1 | 6.79 |
| CHEMBL3601200 | — | — | 1 | 6.66 |
| CHEMBL3601204 | — | — | 1 | 6.07 |
| CHEMBL4080868 | — | — | 1 | 5.90 |
| CHEMBL4105097 | — | — | 1 | 5.75 |
| CHEMBL434 | ISOPROTERENOL | 4.0 | 1 | - |
| CHEMBL4089669 | — | — | 1 | - |
| CHEMBL4088750 | — | — | 1 | - |
| CHEMBL4067502 | — | — | 1 | - |
| CHEMBL3601305 | — | — | 1 | - |
| CHEMBL3601307 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1437 | NOREPINEPHRINE | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4104183 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL3601200 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3601204 | — | EC50 | = | 857.0 | nM | 6.07 |
| CHEMBL4080868 | — | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4105097 | — | EC50 | = | 1757.0 | nM | 5.75 |
| CHEMBL434 | ISOPROTERENOL | EC50 | - | — | - | |
| CHEMBL4089669 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4088750 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4067502 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3601305 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3601307 | — | EC50 | > | 10000.0 | nM | - |