Assay Detail
Binding
CHEMBL1647736
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Displacement of [3H]clonidine from imidazoline I1 receptor in Sprague-Dawley rat kidney 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 | Kidney |
| 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 |
|---|---|---|---|
| IC50 | 11 | 5.11 | 5.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1641681 | — | — | 1 | 5.74 |
| CHEMBL1641687 | — | — | 1 | 5.70 |
| CHEMBL1641679 | — | — | 1 | 5.49 |
| CHEMBL1641689 | — | — | 1 | 5.40 |
| CHEMBL1641680 | — | — | 1 | 5.12 |
| CHEMBL1641688 | — | — | 1 | 4.78 |
| CHEMBL1641685 | — | — | 1 | 4.67 |
| CHEMBL1641683 | — | — | 1 | 4.59 |
| CHEMBL1641682 | — | — | 1 | 4.49 |
| CHEMBL1641684 | — | — | 1 | - |
| CHEMBL1641686 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1641681 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL1641687 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL1641679 | — | IC50 | = | 3219.0 | nM | 5.49 |
| CHEMBL1641689 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL1641680 | — | IC50 | = | 7560.0 | nM | 5.12 |
| CHEMBL1641688 | — | IC50 | = | 16600.0 | nM | 4.78 |
| CHEMBL1641685 | — | IC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL1641683 | — | IC50 | = | 25600.0 | nM | 4.59 |
| CHEMBL1641682 | — | IC50 | = | 32500.0 | nM | 4.49 |
| CHEMBL1641684 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1641686 | — | IC50 | > | 100000.0 | nM | - |