Assay Detail
Functional
CHEMBL894699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human brain adrenergic alpha2 receptor by [35S]GTPgammaS binding assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Guanidine and 2-aminoimidazoline aromatic derivatives as alpha(2)-adrenoceptor antagonists, 1: toward new antidepressants with heteroatomic linkers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 4.97 | 6.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL75389 | — | — | 1 | 6.78 |
| CHEMBL230861 | — | — | 1 | 5.56 |
| CHEMBL844 | BRIMONIDINE | 4.0 | 1 | 4.94 |
| CHEMBL230644 | — | — | 1 | 4.52 |
| CHEMBL242839 | — | — | 1 | 4.38 |
| CHEMBL9441 | — | — | 1 | 4.34 |
| CHEMBL42139 | — | — | 1 | 4.25 |
| CHEMBL244987 | — | — | 1 | - |
| CHEMBL244986 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL75389 | — | EC50 | = | 166.0 | nM | 6.78 |
| CHEMBL230861 | — | EC50 | = | 2760.0 | nM | 5.56 |
| CHEMBL844 | BRIMONIDINE | EC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL230644 | — | EC50 | = | 30400.0 | nM | 4.52 |
| CHEMBL242839 | — | EC50 | = | 42200.0 | nM | 4.38 |
| CHEMBL9441 | — | EC50 | = | 45300.0 | nM | 4.34 |
| CHEMBL42139 | — | EC50 | = | 56400.0 | nM | 4.25 |
| CHEMBL244987 | — | EC50 | = | 332000.0 | nM | - |
| CHEMBL244986 | — | EC50 | = | 120000.0 | nM | - |