Assay Detail
Functional
CHEMBL3882402
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Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PC-12 |
| 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 | 7.95 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 9.10 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 9.07 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 8.00 |
| CHEMBL1079 | TIZANIDINE | 4.0 | 1 | 7.07 |
| CHEMBL1215 | PHENYLEPHRINE | 4.0 | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL844 | BRIMONIDINE | EC50 | = | 0.86 | nM | 9.07 |
| CHEMBL134 | CLONIDINE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1079 | TIZANIDINE | EC50 | = | 86.0 | nM | 7.07 |
| CHEMBL1215 | PHENYLEPHRINE | EC50 | = | 306.0 | nM | 6.51 |