Assay Detail
Binding
CHEMBL1061441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat alpha2beta2 nicotinic receptor expressed in human HEK293 cells by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-2 (CHEMBL2584) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of novel carbon-11 labeled pyridyl ethers: candidate ligands for in vivo imaging of alpha4beta2 nicotinic acetylcholine receptors (alpha4beta2-nAChRs) in the brain with positron emission tomography.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.77 | 10.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL563479 | — | — | 1 | 10.66 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.60 |
| CHEMBL563831 | — | — | 1 | 10.51 |
| CHEMBL560788 | — | — | 1 | 10.46 |
| CHEMBL552408 | — | — | 1 | 10.30 |
| CHEMBL308538 | — | — | 1 | 8.85 |
| CHEMBL551062 | — | — | 1 | 8.82 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.92 |
| CHEMBL558513 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL563479 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.025 | nM | 10.60 |
| CHEMBL563831 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL560788 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL552408 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL308538 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL551062 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3 | NICOTINE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL558513 | — | Ki | = | 0.0056 | nM | - |