Assay Detail
Binding
CHEMBL753471
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Non-specific binding in presence of 300 uM nicotine at nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted 5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Epibatidine analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 9.88 | 10.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | — | 1 | 10.51 |
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 10.35 |
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 10.24 |
| CHEMBL54586 | — | — | 1 | 9.32 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.045 | nM | 10.35 |
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.058 | nM | 10.24 |
| CHEMBL54586 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3 | NICOTINE | Ki | = | 1.01 | nM | 9.00 |