Assay Detail
Functional
CHEMBL1960289
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human adrenoceptor aplha 2A expressed in CHO cells assessed as rate of extracellular acidification by cytosensor microphysiometric analysis
6
Total Activities
6
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 | 6 | 7.47 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | 4.0 | 1 | 8.20 |
| CHEMBL157955 | — | — | 1 | 7.93 |
| CHEMBL155866 | — | — | 1 | 7.73 |
| CHEMBL1956201 | — | — | 1 | 7.50 |
| CHEMBL1956202 | — | — | 1 | 7.20 |
| CHEMBL1956200 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17860 | LOFEXIDINE | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL157955 | — | EC50 | = | 11.75 | nM | 7.93 |
| CHEMBL155866 | — | EC50 | = | 18.62 | nM | 7.73 |
| CHEMBL1956201 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL1956202 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL1956200 | — | EC50 | = | 562.34 | nM | 6.25 |