Assay Detail
Binding
CHEMBL5147131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from human alpha4beta2 nAChR expressed in HEK293 cell membrane incubated for 3 hrs by scinitillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Pyrrolidinyl benzofurans and benzodioxanes: Selective α4β2 nicotinic acetylcholine receptor ligands with different activity profiles at the two receptor stoichiometries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.33 | 6.76 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5183330 | — | — | 1 | 6.76 |
| CHEMBL433777 | — | — | 1 | 6.14 |
| CHEMBL5186760 | — | — | 1 | 6.08 |
| CHEMBL5200048 | — | — | 1 | - |
| CHEMBL5178221 | — | — | 1 | - |
| CHEMBL5200745 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5183330 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL433777 | — | Ki | = | 718.0 | nM | 6.14 |
| CHEMBL5186760 | — | Ki | = | 828.0 | nM | 6.08 |
| CHEMBL5200048 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5178221 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5200745 | — | Ki | = | 181000.0 | nM | - |