Assay Detail
Binding
CHEMBL1647735
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Displacement of [3H]2BFI from imidazoline I1 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 | 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 |
|---|---|---|---|
| Ki | 11 | 6.14 | 7.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1641689 | — | — | 1 | 7.51 |
| CHEMBL1641681 | — | — | 1 | 7.34 |
| CHEMBL1641682 | — | — | 1 | 6.88 |
| CHEMBL1641679 | — | — | 1 | 6.87 |
| CHEMBL1641683 | — | — | 1 | 6.78 |
| CHEMBL1641688 | — | — | 1 | 6.49 |
| CHEMBL1641687 | — | — | 1 | 6.39 |
| CHEMBL1641680 | — | — | 1 | 5.27 |
| CHEMBL1641686 | — | — | 1 | 5.00 |
| CHEMBL1641685 | — | — | 1 | 4.99 |
| CHEMBL1641684 | — | — | 1 | 4.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1641689 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL1641681 | — | Ki | = | 45.2 | nM | 7.34 |
| CHEMBL1641682 | — | Ki | = | 132.7 | nM | 6.88 |
| CHEMBL1641679 | — | Ki | = | 133.6 | nM | 6.87 |
| CHEMBL1641683 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL1641688 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL1641687 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL1641680 | — | Ki | = | 5380.0 | nM | 5.27 |
| CHEMBL1641686 | — | Ki | = | 9910.0 | nM | 5.00 |
| CHEMBL1641685 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL1641684 | — | Ki | = | 93000.0 | nM | 4.03 |