Assay Detail
Binding
CHEMBL4042374
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat cerebral cortex membrane alpha4beta2* nAChR pretreated for 5 mins followed by [3H]epibatidine addition after overnight incubation by beta counter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| 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 | 12 | 6.33 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.40 |
| CHEMBL3603941 | — | — | 1 | 7.96 |
| CHEMBL1917232 | — | — | 1 | 7.92 |
| CHEMBL3603939 | — | — | 1 | 7.72 |
| CHEMBL1186866 | — | — | 1 | 6.58 |
| CHEMBL4095303 | — | — | 1 | 6.39 |
| CHEMBL1186005 | — | — | 1 | 6.33 |
| CHEMBL4061221 | — | — | 1 | 5.79 |
| CHEMBL4076895 | — | — | 1 | 5.44 |
| CHEMBL4074865 | — | — | 1 | 4.52 |
| CHEMBL4072628 | — | — | 1 | 4.52 |
| CHEMBL4099531 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3603941 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1917232 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3603939 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1186866 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL4095303 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL1186005 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL4061221 | — | Ki | = | 1640.0 | nM | 5.79 |
| CHEMBL4076895 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL4074865 | — | Ki | = | 30400.0 | nM | 4.52 |
| CHEMBL4072628 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL4099531 | — | Ki | = | 43000.0 | nM | 4.37 |