Assay Detail
Binding
CHEMBL753469
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Inhibition of [3H]-nicotine binding at the nicotinic acetylcholine receptor alpha4-beta2
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 6 | 8.25 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL58231 | — | — | 1 | 9.35 |
| CHEMBL70050 | — | — | 1 | 9.20 |
| CHEMBL72470 | — | — | 1 | 8.99 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.90 |
| CHEMBL70774 | — | — | 1 | 7.09 |
| CHEMBL72010 | — | — | 1 | 5.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL58231 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL70050 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL72470 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL3 | NICOTINE | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL70774 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL72010 | — | Ki | = | 1072.0 | nM | 5.97 |