Assay Detail
Functional
CHEMBL5504550
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Agonist activity at alpha2B-adrenoceptor (unknown origin) expressed in U2OS-EGFP-NFAT2-alpha2B-AR cells assessed as increase in intracellular calcium level measured after 15 mins incubation by Micro automated microscopy
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Designing Chromane Derivatives as α<sub>2A</sub>-Adrenoceptor Selective Agonists via Conformation Constraint.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 7.33 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 8.72 |
| CHEMBL5557226 | — | — | 1 | 7.62 |
| CHEMBL5558506 | — | — | 1 | 7.34 |
| CHEMBL5512438 | — | — | 1 | 7.08 |
| CHEMBL5558705 | — | — | 1 | 7.00 |
| CHEMBL5532450 | — | — | 1 | 6.79 |
| CHEMBL5558235 | — | — | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | EC50 | = | 1.91 | nM | 8.72 |
| CHEMBL5557226 | — | EC50 | = | 24.1 | nM | 7.62 |
| CHEMBL5558506 | — | EC50 | = | 45.8 | nM | 7.34 |
| CHEMBL5512438 | — | EC50 | = | 83.4 | nM | 7.08 |
| CHEMBL5558705 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5532450 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5558235 | — | EC50 | = | 186.0 | nM | 6.73 |