Assay Detail
Binding
CHEMBL751222
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Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.51 | 7.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56296 | — | — | 1 | 7.05 |
| CHEMBL55606 | — | — | 1 | 6.85 |
| CHEMBL54826 | — | — | 1 | 5.71 |
| CHEMBL54580 | — | — | 1 | 5.04 |
| CHEMBL55297 | — | — | 1 | 4.77 |
| CHEMBL293527 | — | — | 1 | 4.70 |
| CHEMBL55479 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56296 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL55606 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL54826 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL54580 | — | Ki | = | 9150.0 | nM | 5.04 |
| CHEMBL55297 | — | Ki | = | 17000.0 | nM | 4.77 |
| CHEMBL293527 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL55479 | — | Ki | = | 38000.0 | nM | 4.42 |