Assay Detail
Binding
CHEMBL753468
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Inhibition of [3H]epibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| 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 | 10 | 9.68 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | 10.74 |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | — | 1 | 10.70 |
| CHEMBL301901 | — | — | 1 | 10.64 |
| CHEMBL298517 | (+)-EPIBATIDINE | — | 1 | 10.59 |
| CHEMBL56682 | — | — | 1 | 10.57 |
| CHEMBL54586 | — | — | 1 | 10.15 |
| CHEMBL56358 | — | — | 1 | 8.89 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.82 |
| CHEMBL300837 | — | — | 1 | 8.07 |
| CHEMBL56677 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL56817 | DESCHLOROEPIBATIDINE | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL301901 | — | Ki | = | 0.023 | nM | 10.64 |
| CHEMBL298517 | (+)-EPIBATIDINE | Ki | = | 0.026 | nM | 10.59 |
| CHEMBL56682 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL54586 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL56358 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3 | NICOTINE | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL300837 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL56677 | — | Ki | = | 26.4 | nM | 7.58 |