Assay Detail
Binding
CHEMBL1047077
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Displacement of [3H]RX821002 from human Alpha-2C adrenoceptor expressed in CHO cell membrane after 30 mins by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Might adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.63 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576623 | — | — | 1 | 7.10 |
| CHEMBL570973 | — | — | 1 | 7.07 |
| CHEMBL576078 | — | — | 1 | 6.83 |
| CHEMBL571314 | — | — | 1 | 6.58 |
| CHEMBL570863 | — | — | 1 | 6.57 |
| CHEMBL569933 | — | — | 1 | 6.31 |
| CHEMBL576819 | — | — | 1 | 6.30 |
| CHEMBL13852 | CIRAZOLINE | 2.0 | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576623 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL570973 | — | Ki | = | 85.11 | nM | 7.07 |
| CHEMBL576078 | — | Ki | = | 147.91 | nM | 6.83 |
| CHEMBL571314 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL570863 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL569933 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL576819 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL13852 | CIRAZOLINE | Ki | = | 549.54 | nM | 6.26 |