Assay Detail
Binding
CHEMBL1960286
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Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2A 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 | 7.11 | 8.36 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 8.36 |
| CHEMBL155866 | — | — | 1 | 7.93 |
| CHEMBL157206 | — | — | 1 | 7.78 |
| CHEMBL1956192 | — | — | 1 | 7.64 |
| CHEMBL156336 | — | — | 1 | 7.62 |
| CHEMBL1956191 | — | — | 1 | 7.54 |
| CHEMBL157955 | — | — | 1 | 7.50 |
| CHEMBL1956195 | CYCLOMETHYLINE | — | 1 | 7.44 |
| CHEMBL1956199 | — | — | 1 | 7.24 |
| CHEMBL1956194 | — | — | 1 | 7.14 |
| CHEMBL266613 | — | — | 1 | 7.14 |
| CHEMBL14208 | — | — | 1 | 7.08 |
| CHEMBL1956197 | — | — | 1 | 7.08 |
| CHEMBL1956196 | — | — | 1 | 7.01 |
| CHEMBL1956193 | — | — | 1 | 6.74 |
| CHEMBL1956203 | — | — | 1 | 6.31 |
| CHEMBL1956202 | — | — | 1 | 5.99 |
| CHEMBL1956201 | — | — | 1 | 5.98 |
| CHEMBL1956200 | — | — | 1 | 5.50 |
| CHEMBL1956198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | Ki | = | 4.365 | nM | 8.36 |
| CHEMBL155866 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL157206 | — | Ki | = | 16.6 | nM | 7.78 |
| CHEMBL1956192 | — | Ki | = | 22.91 | nM | 7.64 |
| CHEMBL156336 | — | Ki | = | 23.99 | nM | 7.62 |
| CHEMBL1956191 | — | Ki | = | 28.84 | nM | 7.54 |
| CHEMBL157955 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL1956195 | CYCLOMETHYLINE | Ki | = | 36.31 | nM | 7.44 |
| CHEMBL1956199 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL1956194 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL266613 | — | Ki | = | 72.44 | nM | 7.14 |
| CHEMBL14208 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL1956197 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL1956196 | — | Ki | = | 97.72 | nM | 7.01 |
| CHEMBL1956193 | — | Ki | = | 181.97 | nM | 6.74 |
| CHEMBL1956203 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL1956202 | — | Ki | = | 1023.29 | nM | 5.99 |
| CHEMBL1956201 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL1956200 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL1956198 | — | pKi | - | — | - |