Assay Detail
Binding
CHEMBL1960287
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Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2B expressed in CHO cells
20
Total Activities
20
Compounds Tested
2
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
Might the observed α(2A)-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.05 | 7.17 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 7.17 |
| CHEMBL155866 | — | — | 1 | 6.74 |
| CHEMBL157955 | — | — | 1 | 6.57 |
| CHEMBL157206 | — | — | 1 | 6.56 |
| CHEMBL156336 | — | — | 1 | 6.55 |
| CHEMBL1956191 | — | — | 1 | 6.48 |
| CHEMBL1956192 | — | — | 1 | 6.45 |
| CHEMBL1956195 | CYCLOMETHYLINE | — | 1 | 6.39 |
| CHEMBL1956199 | — | — | 1 | 6.06 |
| CHEMBL1956194 | — | — | 1 | 6.06 |
| CHEMBL266613 | — | — | 1 | 6.03 |
| CHEMBL1956197 | — | — | 1 | 5.98 |
| CHEMBL1956196 | — | — | 1 | 5.88 |
| CHEMBL14208 | — | — | 1 | 5.80 |
| CHEMBL1956193 | — | — | 1 | 5.79 |
| CHEMBL1956201 | — | — | 1 | 5.68 |
| CHEMBL1956203 | — | — | 1 | 5.34 |
| CHEMBL1956202 | — | — | 1 | 5.21 |
| CHEMBL1956200 | — | — | 1 | 4.29 |
| CHEMBL1956198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL155866 | — | Ki | = | 181.97 | nM | 6.74 |
| CHEMBL157955 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL157206 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL156336 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL1956191 | — | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL1956192 | — | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL1956195 | CYCLOMETHYLINE | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL1956199 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL1956194 | — | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL266613 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL1956197 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL1956196 | — | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL14208 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1956193 | — | Ki | = | 1621.81 | nM | 5.79 |
| CHEMBL1956201 | — | Ki | = | 2089.3 | nM | 5.68 |
| CHEMBL1956203 | — | Ki | = | 4570.88 | nM | 5.34 |
| CHEMBL1956202 | — | Ki | = | 6165.95 | nM | 5.21 |
| CHEMBL1956200 | — | Ki | = | 51286.14 | nM | 4.29 |
| CHEMBL1956198 | — | pKi | - | — | - |