Assay Detail
Binding
CHEMBL873046
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]epibatidine binding at the alpha beta nicotinic AChR in male rat cerebral cortex
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2-exo-2-(2'-substituted-3'-phenyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptanes. Novel nicotinic antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 9.62 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 10.74 |
| CHEMBL291961 | — | — | 1 | 10.68 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.59 |
| CHEMBL56682 | — | — | 1 | 10.57 |
| CHEMBL58935 | — | — | 3 | 9.62 |
| CHEMBL131785 | — | — | 1 | 9.48 |
| CHEMBL56358 | — | — | 1 | 8.89 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.82 |
| CHEMBL130621 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL291961 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL56682 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL58935 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL131785 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL56358 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3 | NICOTINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL130621 | — | Ki | = | 57.5 | nM | 7.24 |