Assay Detail
Binding
CHEMBL1647734
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Displacement of [3H]RX821002 from alpha2 adrenergic receptor in Sprague-Dawley rat brain membrane after 45 mins by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 |
|---|---|---|---|
| Ki | 11 | 6.35 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1641681 | — | — | 1 | 7.80 |
| CHEMBL1641682 | — | — | 1 | 7.65 |
| CHEMBL1641679 | — | — | 1 | 7.41 |
| CHEMBL1641689 | — | — | 1 | 6.88 |
| CHEMBL1641688 | — | — | 1 | 6.75 |
| CHEMBL1641687 | — | — | 1 | 6.30 |
| CHEMBL1641683 | — | — | 1 | 6.13 |
| CHEMBL1641686 | — | — | 1 | 5.84 |
| CHEMBL1641680 | — | — | 1 | 5.19 |
| CHEMBL1641684 | — | — | 1 | 4.97 |
| CHEMBL1641685 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1641681 | — | Ki | = | 15.9 | nM | 7.80 |
| CHEMBL1641682 | — | Ki | = | 22.6 | nM | 7.65 |
| CHEMBL1641679 | — | Ki | = | 39.4 | nM | 7.41 |
| CHEMBL1641689 | — | Ki | = | 133.0 | nM | 6.88 |
| CHEMBL1641688 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL1641687 | — | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL1641683 | — | Ki | = | 748.0 | nM | 6.13 |
| CHEMBL1641686 | — | Ki | = | 1460.0 | nM | 5.84 |
| CHEMBL1641680 | — | Ki | = | 6420.0 | nM | 5.19 |
| CHEMBL1641684 | — | Ki | = | 10600.0 | nM | 4.97 |
| CHEMBL1641685 | — | Ki | = | 11400.0 | nM | 4.94 |