Assay Detail
Binding
CHEMBL1647733
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Displacement of [3H]prazosin from alpha1 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 | 6.42 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1641682 | — | — | 1 | 7.33 |
| CHEMBL1641681 | — | — | 1 | 7.16 |
| CHEMBL1641684 | — | — | 1 | 6.92 |
| CHEMBL1641683 | — | — | 1 | 6.71 |
| CHEMBL1641686 | — | — | 1 | 6.61 |
| CHEMBL1641687 | — | — | 1 | 6.41 |
| CHEMBL1641688 | — | — | 1 | 6.29 |
| CHEMBL1641689 | — | — | 1 | 6.17 |
| CHEMBL1641680 | — | — | 1 | 6.01 |
| CHEMBL1641685 | — | — | 1 | 4.54 |
| CHEMBL1641679 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1641682 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL1641681 | — | Ki | = | 69.3 | nM | 7.16 |
| CHEMBL1641684 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL1641683 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL1641686 | — | Ki | = | 244.0 | nM | 6.61 |
| CHEMBL1641687 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL1641688 | — | Ki | = | 508.0 | nM | 6.29 |
| CHEMBL1641689 | — | Ki | = | 684.0 | nM | 6.17 |
| CHEMBL1641680 | — | Ki | = | 984.0 | nM | 6.01 |
| CHEMBL1641685 | — | Ki | = | 29000.0 | nM | 4.54 |
| CHEMBL1641679 | — | Ki | - | — | - |