Assay Detail
Functional
CHEMBL3882406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Bos taurus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel methods for identifying improved, non-sedating alpha-2 agonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.81 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 8.05 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.05 |
| CHEMBL1079 | TIZANIDINE | 4.0 | 1 | 6.58 |
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 6.42 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 5.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1215 | PHENYLEPHRINE | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL134 | CLONIDINE | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1079 | TIZANIDINE | EC50 | = | 264.0 | nM | 6.58 |
| CHEMBL778 | DEXMEDETOMIDINE | EC50 | = | 376.0 | nM | 6.42 |
| CHEMBL844 | BRIMONIDINE | EC50 | = | 1132.0 | nM | 5.95 |