Assay Detail
Binding
CHEMBL963253
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Displacement of [3H]cytisine from alpha4beta2 nAChR in rat brain membrane
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.42 | 10.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.33 |
| CHEMBL430497 | TEBANICLINE | 2.0 | 1 | 10.32 |
| CHEMBL389964 | — | — | 1 | 9.82 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.03 |
| CHEMBL494773 | — | — | 1 | 8.92 |
| CHEMBL449142 | — | — | 1 | 7.96 |
| CHEMBL492593 | — | — | 1 | 7.68 |
| CHEMBL504652 | TC-2216 | 1.0 | 1 | 7.48 |
| CHEMBL509239 | — | — | 1 | 7.32 |
| CHEMBL504595 | — | — | 1 | 7.13 |
| CHEMBL504126 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.047 | nM | 10.33 |
| CHEMBL430497 | TEBANICLINE | Ki | = | 0.048 | nM | 10.32 |
| CHEMBL389964 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL3 | NICOTINE | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL494773 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL449142 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL492593 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL504652 | TC-2216 | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL509239 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL504595 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL504126 | — | Ki | = | 240.0 | nM | 6.62 |