Assay Detail
Binding
CHEMBL4042375
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Displacement of [125I]alpha-bungarotoxin from rat hippocampus membrane alpha7* nAChR pretreated for 5 mins followed by [125I]alpha-bungarotoxin addition after overnight incubation by gamma counter
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at α4β2 nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.48 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3603941 | — | — | 1 | 7.24 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.63 |
| CHEMBL1917232 | — | — | 1 | 6.37 |
| CHEMBL3603939 | — | — | 1 | 5.94 |
| CHEMBL4072628 | — | — | 1 | 4.92 |
| CHEMBL1186005 | — | — | 1 | 4.84 |
| CHEMBL1186866 | — | — | 1 | 4.68 |
| CHEMBL4099531 | — | — | 1 | 4.62 |
| CHEMBL4095303 | — | — | 1 | 4.05 |
| CHEMBL4074865 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3603941 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL3 | NICOTINE | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL1917232 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL3603939 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL4072628 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1186005 | — | Ki | = | 14600.0 | nM | 4.84 |
| CHEMBL1186866 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL4099531 | — | Ki | = | 24000.0 | nM | 4.62 |
| CHEMBL4095303 | — | Ki | = | 89000.0 | nM | 4.05 |
| CHEMBL4074865 | — | Ki | > | 10000.0 | nM | - |