Assay Detail
Binding
CHEMBL1960288
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Displacement of [3H]RS-79948-197 from human adrenoceptor aplha 2C 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 | 6.23 | 7.16 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 7.16 |
| CHEMBL157206 | — | — | 1 | 6.89 |
| CHEMBL155866 | — | — | 1 | 6.60 |
| CHEMBL1956195 | CYCLOMETHYLINE | — | 1 | 6.56 |
| CHEMBL157955 | — | — | 1 | 6.56 |
| CHEMBL1956192 | — | — | 1 | 6.55 |
| CHEMBL156336 | — | — | 1 | 6.54 |
| CHEMBL14208 | — | — | 1 | 6.40 |
| CHEMBL266613 | — | — | 1 | 6.34 |
| CHEMBL1956191 | — | — | 1 | 6.31 |
| CHEMBL1956194 | — | — | 1 | 6.22 |
| CHEMBL1956203 | — | — | 1 | 6.20 |
| CHEMBL1956197 | — | — | 1 | 6.17 |
| CHEMBL1956196 | — | — | 1 | 6.12 |
| CHEMBL1956199 | — | — | 1 | 6.08 |
| CHEMBL1956193 | — | — | 1 | 6.01 |
| CHEMBL1956200 | — | — | 1 | 5.42 |
| CHEMBL1956202 | — | — | 1 | 5.13 |
| CHEMBL1956201 | — | — | 1 | 5.06 |
| CHEMBL1956198 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | Ki | = | 69.18 | nM | 7.16 |
| CHEMBL157206 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL155866 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL1956195 | CYCLOMETHYLINE | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL157955 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL1956192 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL156336 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL14208 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL266613 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL1956191 | — | Ki | = | 489.78 | nM | 6.31 |
| CHEMBL1956194 | — | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL1956203 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL1956197 | — | Ki | = | 676.08 | nM | 6.17 |
| CHEMBL1956196 | — | Ki | = | 758.58 | nM | 6.12 |
| CHEMBL1956199 | — | Ki | = | 831.76 | nM | 6.08 |
| CHEMBL1956193 | — | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL1956200 | — | Ki | = | 3801.89 | nM | 5.42 |
| CHEMBL1956202 | — | Ki | = | 7413.1 | nM | 5.13 |
| CHEMBL1956201 | — | Ki | = | 8709.64 | nM | 5.06 |
| CHEMBL1956198 | — | pKi | - | — | - |