Assay Detail
Binding
CHEMBL754303
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Displacement of [3H]cytisine from Nicotinic acetylcholine receptor alpha4-beta2 in rat forebrain
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.22 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.03 |
| CHEMBL130814 | — | — | 2 | 8.72 |
| CHEMBL2112670 | — | — | 1 | 8.32 |
| CHEMBL2112671 | — | — | 1 | 7.28 |
| CHEMBL2111861 | — | — | 1 | 6.83 |
| CHEMBL335828 | — | — | 2 | 6.50 |
| CHEMBL2111860 | — | — | 1 | 6.27 |
| CHEMBL2112676 | — | — | 1 | 6.02 |
| CHEMBL2111859 | — | — | 1 | 5.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL130814 | — | Ki | = | 1.89 | nM | 8.72 |
| CHEMBL130814 | — | Ki | = | 2.32 | nM | 8.63 |
| CHEMBL2112670 | — | Ki | = | 4.79 | nM | 8.32 |
| CHEMBL2112671 | — | Ki | = | 53.1 | nM | 7.28 |
| CHEMBL2111861 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL335828 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL2111860 | — | Ki | = | 533.0 | nM | 6.27 |
| CHEMBL2112676 | — | Ki | = | 962.0 | nM | 6.02 |
| CHEMBL335828 | — | Ki | = | 1040.0 | nM | 5.98 |
| CHEMBL2111859 | — | Ki | = | 1360.0 | nM | 5.87 |