Assay Detail
Binding
CHEMBL1959312
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Displacement of [3H]RX821002 from human alpha2A adrenergic receptor expressed in CHO cells after 30 mins by scintillation counting
9
Total Activities
9
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 | Autocuration |
Publication
Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 5.98 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10316 | IDAZOXAN | 3.0 | 1 | 8.15 |
| CHEMBL1956902 | — | — | 1 | 6.40 |
| CHEMBL1956900 | — | — | 1 | 6.30 |
| CHEMBL1956906 | — | — | 1 | 5.42 |
| CHEMBL1956903 | — | — | 1 | 5.27 |
| CHEMBL1956904 | — | — | 1 | 5.20 |
| CHEMBL1956901 | — | — | 1 | 5.10 |
| CHEMBL1956899 | — | — | 1 | - |
| CHEMBL1956905 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10316 | IDAZOXAN | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL1956902 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL1956900 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL1956906 | — | Ki | = | 3801.89 | nM | 5.42 |
| CHEMBL1956903 | — | Ki | = | 5370.32 | nM | 5.27 |
| CHEMBL1956904 | — | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL1956901 | — | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL1956899 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1956905 | — | Ki | > | 10000.0 | nM | - |