Assay Detail
Binding
CHEMBL1047080
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Displacement of [3H]RX821002 from human alpha2A 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 | 7.42 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL576623 | — | — | 1 | 7.64 |
| CHEMBL570863 | — | — | 1 | 7.61 |
| CHEMBL571314 | — | — | 1 | 7.57 |
| CHEMBL576819 | — | — | 1 | 7.46 |
| CHEMBL569933 | — | — | 1 | 7.31 |
| CHEMBL576078 | — | — | 1 | 7.30 |
| CHEMBL570973 | — | — | 1 | 7.24 |
| CHEMBL13852 | CIRAZOLINE | 2.0 | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL576623 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL570863 | — | Ki | = | 24.55 | nM | 7.61 |
| CHEMBL571314 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL576819 | — | Ki | = | 34.67 | nM | 7.46 |
| CHEMBL569933 | — | Ki | = | 48.98 | nM | 7.31 |
| CHEMBL576078 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL570973 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL13852 | CIRAZOLINE | Ki | = | 58.88 | nM | 7.23 |