Assay Detail
Functional
CHEMBL5504552
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Agonist activity at alpha1A-adrenoceptor (unknown origin) expressed in HEK293T cells assessed as fluorescence intensity measured after 30 mins by IP-one homogeneous time-resolved fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| 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 | 7.97 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5558506 | — | — | 1 | 8.62 |
| CHEMBL5532450 | — | — | 1 | 8.59 |
| CHEMBL5557226 | — | — | 1 | 8.39 |
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 7.88 |
| CHEMBL5558705 | — | — | 1 | 7.53 |
| CHEMBL5558235 | — | — | 1 | 7.49 |
| CHEMBL5512438 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5558506 | — | EC50 | = | 2.42 | nM | 8.62 |
| CHEMBL5532450 | — | EC50 | = | 2.55 | nM | 8.59 |
| CHEMBL5557226 | — | EC50 | = | 4.05 | nM | 8.39 |
| CHEMBL778 | DEXMEDETOMIDINE | EC50 | = | 13.03 | nM | 7.88 |
| CHEMBL5558705 | — | EC50 | = | 29.84 | nM | 7.53 |
| CHEMBL5558235 | — | EC50 | = | 32.04 | nM | 7.49 |
| CHEMBL5512438 | — | EC50 | = | 48.38 | nM | 7.32 |