Assay Detail
Functional
CHEMBL1647738
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Agonist activity at human recombinant alpha2A adrenergic receptor expressed in CHO cells assessed as induction of [35S]GTPgammaS binding after 60 mins by scintillation counting
11
Total Activities
11
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
3-[(Imidazolidin-2-yl)imino]indazole ligands with selectivity for the α(2)-adrenoceptor compared to the imidazoline I(1) receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 7.35 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | 4.0 | 1 | 8.82 |
| CHEMBL1641682 | — | — | 1 | 7.85 |
| CHEMBL1641690 | — | — | 1 | 7.82 |
| CHEMBL134 | CLONIDINE | 4.0 | 1 | 7.55 |
| CHEMBL1186788 | — | — | 1 | 7.43 |
| CHEMBL1641689 | — | — | 1 | 7.14 |
| CHEMBL1641679 | — | — | 1 | 7.09 |
| CHEMBL1437 | NOREPINEPHRINE | 4.0 | 1 | 6.96 |
| CHEMBL1186220 | MARSANIDINE | — | 1 | 6.80 |
| CHEMBL1186774 | — | — | 1 | 6.75 |
| CHEMBL1641681 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL778 | DEXMEDETOMIDINE | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1641682 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1641690 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL134 | CLONIDINE | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1186788 | — | EC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1641689 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1641679 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1437 | NOREPINEPHRINE | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1186220 | MARSANIDINE | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1186774 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1641681 | — | EC50 | = | 240.0 | nM | 6.62 |