Assay Detail
Binding
CHEMBL3385111
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]epibatidine from rat forebrain alpha3beta4 nAChR by competition binding assay
9
Total Activities
9
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; alpha3/beta4 (CHEMBL1907593) ↗| 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 | 9 | 5.95 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | 4.0 | 1 | 7.07 |
| CHEMBL1186374 | — | — | 1 | 6.70 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.58 |
| CHEMBL3356149 | — | — | 1 | 5.60 |
| CHEMBL3356151 | — | — | 1 | 5.60 |
| CHEMBL3356150 | — | — | 1 | 5.10 |
| CHEMBL2024096 | — | — | 1 | 5.00 |
| CHEMBL3356148 | — | — | 1 | - |
| CHEMBL3356152 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1076903 | VARENICLINE | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL1186374 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3 | NICOTINE | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3356149 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL3356151 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL3356150 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL2024096 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3356148 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3356152 | — | Ki | > | 10000.0 | nM | - |