Assay Detail
Binding
CHEMBL3385109
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat forebrain alpha2beta4 nAChR by competition binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL1907590) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 6.85 | 7.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1186374 | — | — | 1 | 7.34 |
| CHEMBL3356151 | — | — | 1 | 7.19 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.16 |
| CHEMBL3356150 | — | — | 1 | 6.58 |
| CHEMBL3356148 | — | — | 1 | 6.42 |
| CHEMBL3356152 | — | — | 1 | 6.41 |
| CHEMBL3356149 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1186374 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3356151 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL3 | NICOTINE | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3356150 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3356148 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL3356152 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL3356149 | — | Ki | > | 10000.0 | nM | - |