Assay Detail
Binding
CHEMBL1285950
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Displacement of [3H]RX821002 from human alpha2A adrenoceptor expressed in CHO cells
19
Total Activities
19
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
Fruitful adrenergic α(2C)-agonism/α(2A)-antagonism combination to prevent and contrast morphine tolerance and dependence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.25 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1276220 | — | — | 1 | 7.68 |
| CHEMBL1276218 | — | — | 1 | 7.64 |
| CHEMBL273485 | — | — | 1 | 7.57 |
| CHEMBL374584 | — | — | 1 | 7.56 |
| CHEMBL1278084 | — | — | 1 | 7.40 |
| CHEMBL1276248 | — | — | 1 | 7.35 |
| CHEMBL1276219 | — | — | 1 | 7.35 |
| CHEMBL385310 | — | — | 1 | 7.34 |
| CHEMBL128168 | BIPHENYLINE | — | 1 | 7.32 |
| CHEMBL1276140 | — | — | 1 | 7.28 |
| CHEMBL495095 | ALLYPHENYLINE | — | 1 | 7.24 |
| CHEMBL222928 | — | — | 1 | 7.22 |
| CHEMBL397753 | — | — | 1 | 7.14 |
| CHEMBL242693 | — | — | 1 | 7.09 |
| CHEMBL396013 | — | — | 1 | 7.04 |
| CHEMBL1278085 | — | — | 1 | 7.01 |
| CHEMBL1276139 | — | — | 1 | 7.00 |
| CHEMBL1276247 | — | — | 1 | 6.78 |
| CHEMBL242265 | — | — | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1276220 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL1276218 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL273485 | — | Ki | = | 26.92 | nM | 7.57 |
| CHEMBL374584 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL1278084 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL1276248 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL1276219 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL385310 | — | Ki | = | 45.71 | nM | 7.34 |
| CHEMBL128168 | BIPHENYLINE | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL1276140 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL495095 | ALLYPHENYLINE | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL222928 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL397753 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL242693 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL396013 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL1278085 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL1276139 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1276247 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL242265 | — | Ki | = | 186.21 | nM | 6.73 |