Assay Detail
Functional
CHEMBL1960290
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Agonist activity at human adrenoceptor aplha 2B expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 20 | 5.91 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 6.90 |
| CHEMBL1956191 | — | — | 1 | 6.79 |
| CHEMBL1956203 | — | — | 1 | 6.70 |
| CHEMBL1956193 | — | — | 1 | 6.62 |
| CHEMBL266613 | — | — | 1 | 6.60 |
| CHEMBL1956202 | — | — | 1 | 6.53 |
| CHEMBL1956192 | — | — | 1 | 6.50 |
| CHEMBL1956201 | — | — | 1 | 6.50 |
| CHEMBL157206 | — | — | 1 | 6.30 |
| CHEMBL157955 | — | — | 1 | 6.00 |
| CHEMBL155866 | — | — | 1 | 5.83 |
| CHEMBL1956194 | — | — | 1 | 5.80 |
| CHEMBL14208 | — | — | 1 | 5.76 |
| CHEMBL1956198 | — | — | 1 | 5.50 |
| CHEMBL1956196 | — | — | 1 | 5.50 |
| CHEMBL1956195 | CYCLOMETHYLINE | — | 1 | 5.48 |
| CHEMBL1956200 | — | — | 1 | 5.00 |
| CHEMBL156336 | — | — | 1 | 5.00 |
| CHEMBL1956197 | — | — | 1 | 4.89 |
| CHEMBL1956199 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1956191 | — | EC50 | = | 162.18 | nM | 6.79 |
| CHEMBL1956203 | — | EC50 | = | 199.53 | nM | 6.70 |
| CHEMBL1956193 | — | EC50 | = | 239.88 | nM | 6.62 |
| CHEMBL266613 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL1956202 | — | EC50 | = | 295.12 | nM | 6.53 |
| CHEMBL1956192 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL1956201 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL157206 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL157955 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL155866 | — | EC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL1956194 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL14208 | — | EC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL1956198 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1956196 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL1956195 | CYCLOMETHYLINE | EC50 | = | 3311.31 | nM | 5.48 |
| CHEMBL1956200 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL156336 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1956197 | — | EC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL1956199 | — | EC50 | = | 100000.0 | nM | 4.00 |