Assay Detail
Binding
CHEMBL4042376
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha3beta4 nAChR expressed in HEK293 cells pretreated for 5 mins followed by [3H]epibatidine addition after overnight incubation by beta counter
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 5.70 | 6.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3603941 | — | — | 1 | 6.59 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.58 |
| CHEMBL3603939 | — | — | 1 | 6.57 |
| CHEMBL1917232 | — | — | 1 | 6.51 |
| CHEMBL1186866 | — | — | 1 | 5.92 |
| CHEMBL4061221 | — | — | 1 | 5.24 |
| CHEMBL1186005 | — | — | 1 | 5.09 |
| CHEMBL4076895 | — | — | 1 | 5.05 |
| CHEMBL4095303 | — | — | 1 | 4.79 |
| CHEMBL4074865 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3603941 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL3 | NICOTINE | Ki | = | 261.0 | nM | 6.58 |
| CHEMBL3603939 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL1917232 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL1186866 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL4061221 | — | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL1186005 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL4076895 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL4095303 | — | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL4074865 | — | Ki | = | 22000.0 | nM | 4.66 |