Assay Detail
Binding
CHEMBL4679296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]alpha-bungarotoxin from alpha7nAChR in rat hippocampus membranes preincubated for 5 mins followed by [125I]alpha-bungarotoxin addition and measured after overnight incubation by liquid scintillation beta counter analysis
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Hippocampus |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent α4β2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the α3β4 Subtype.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 4.88 | 6.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.63 |
| CHEMBL1917231 | — | — | 1 | 6.37 |
| CHEMBL4755768 | — | — | 1 | 5.68 |
| CHEMBL4785648 | — | — | 1 | 5.58 |
| CHEMBL4762584 | — | — | 1 | 5.09 |
| CHEMBL4792797 | — | — | 1 | 4.98 |
| CHEMBL4798883 | — | — | 1 | 4.98 |
| CHEMBL4744398 | — | — | 1 | 4.87 |
| CHEMBL4758050 | — | — | 1 | 4.72 |
| CHEMBL1917232 | — | — | 1 | 4.70 |
| CHEMBL1186866 | — | — | 1 | 4.68 |
| CHEMBL4778976 | — | — | 1 | 4.57 |
| CHEMBL4783660 | — | — | 1 | 4.50 |
| CHEMBL1917229 | — | — | 1 | 4.44 |
| CHEMBL4792229 | — | — | 1 | 4.38 |
| CHEMBL4741357 | — | — | 1 | 4.35 |
| CHEMBL4747289 | — | — | 1 | 4.34 |
| CHEMBL4784011 | — | — | 1 | 4.30 |
| CHEMBL1917230 | — | — | 1 | 4.29 |
| CHEMBL4095303 | — | — | 1 | 4.05 |
| CHEMBL4740421 | — | — | 1 | - |
| CHEMBL4788079 | — | — | 1 | - |
| CHEMBL4799765 | — | — | 1 | - |
| CHEMBL4760797 | — | — | 1 | - |
| CHEMBL4776494 | — | — | 1 | - |
| CHEMBL4762415 | — | — | 1 | - |
| CHEMBL4783337 | — | — | 1 | - |
| CHEMBL4790023 | — | — | 1 | - |
| CHEMBL4782049 | — | — | 1 | - |
| CHEMBL4743341 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 234.0 | nM | 6.63 |
| CHEMBL1917231 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL4755768 | — | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL4785648 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL4762584 | — | Ki | = | 8100.0 | nM | 5.09 |
| CHEMBL4792797 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL4798883 | — | Ki | = | 10500.0 | nM | 4.98 |
| CHEMBL4744398 | — | Ki | = | 13500.0 | nM | 4.87 |
| CHEMBL4758050 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL1917232 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL1186866 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL4778976 | — | Ki | = | 26800.0 | nM | 4.57 |
| CHEMBL4783660 | — | Ki | = | 31500.0 | nM | 4.50 |
| CHEMBL1917229 | — | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL4792229 | — | Ki | = | 42200.0 | nM | 4.38 |
| CHEMBL4741357 | — | Ki | = | 44500.0 | nM | 4.35 |
| CHEMBL4747289 | — | Ki | = | 45500.0 | nM | 4.34 |
| CHEMBL4784011 | — | Ki | = | 50000.0 | nM | 4.30 |
| CHEMBL1917230 | — | Ki | = | 51000.0 | nM | 4.29 |
| CHEMBL4095303 | — | Ki | = | 89000.0 | nM | 4.05 |
| CHEMBL4740421 | — | Ki | - | — | - | |
| CHEMBL4788079 | — | Ki | - | — | - | |
| CHEMBL4799765 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4760797 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4776494 | — | Ki | - | — | - | |
| CHEMBL4762415 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4783337 | — | Ki | = | 109000.0 | nM | - |
| CHEMBL4790023 | — | Ki | - | — | - | |
| CHEMBL4782049 | — | Ki | - | — | - | |
| CHEMBL4743341 | — | Ki | - | — | - | |
| CHEMBL4759608 | — | Ki | - | — | - |