Assay Detail
Binding
CHEMBL4679290
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-epibatidine from human alpha4beta2 nAChR S108A mutant transfected in human Hela cell membranes preincubated for 5 mins followed by [3H]-Epibatidine addition and measured after overnight incubation by liquid scintillation beta counter analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 5 | 7.31 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917231 | — | — | 1 | 8.92 |
| CHEMBL4785648 | — | — | 1 | 8.22 |
| CHEMBL4741357 | — | — | 1 | 6.81 |
| CHEMBL4095303 | — | — | 1 | 6.58 |
| CHEMBL1186866 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917231 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL4785648 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4741357 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL4095303 | — | Ki | = | 265.0 | nM | 6.58 |
| CHEMBL1186866 | — | Ki | = | 912.0 | nM | 6.04 |