Assay Detail
Binding
CHEMBL4361683
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Displacement of [3H]epibatidine from alpha4beta2 nAChR in rat cerebral cortex membrane
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| 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
Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.66 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4460815 | — | — | 1 | 11.00 |
| CHEMBL4543232 | — | — | 1 | 10.51 |
| CHEMBL4441630 | — | — | 1 | 10.38 |
| CHEMBL4565381 | — | — | 1 | 10.36 |
| CHEMBL4556523 | — | — | 1 | 10.29 |
| CHEMBL4444866 | — | — | 1 | 9.97 |
| CHEMBL4581470 | — | — | 1 | 9.71 |
| CHEMBL4453342 | — | — | 1 | 9.50 |
| CHEMBL4435435 | — | — | 1 | 9.44 |
| CHEMBL4447564 | — | — | 1 | 9.39 |
| CHEMBL4532589 | — | — | 1 | 9.25 |
| CHEMBL4462607 | — | — | 1 | 9.08 |
| CHEMBL4530364 | — | — | 1 | 9.01 |
| CHEMBL4571320 | — | — | 1 | 8.96 |
| CHEMBL4476500 | — | — | 1 | 8.89 |
| CHEMBL4472986 | — | — | 1 | 8.74 |
| CHEMBL298826 | (-)-EPIBATIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4460815 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL4543232 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL4441630 | — | Ki | = | 0.042 | nM | 10.38 |
| CHEMBL4565381 | — | Ki | = | 0.044 | nM | 10.36 |
| CHEMBL4556523 | — | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL4444866 | — | Ki | = | 0.106 | nM | 9.97 |
| CHEMBL4581470 | — | Ki | = | 0.196 | nM | 9.71 |
| CHEMBL4453342 | — | Ki | = | 0.315 | nM | 9.50 |
| CHEMBL4435435 | — | Ki | = | 0.366 | nM | 9.44 |
| CHEMBL4447564 | — | Ki | = | 0.404 | nM | 9.39 |
| CHEMBL4532589 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL4462607 | — | Ki | = | 0.828 | nM | 9.08 |
| CHEMBL4530364 | — | Ki | = | 0.985 | nM | 9.01 |
| CHEMBL4571320 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4476500 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4472986 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL298826 | (-)-EPIBATIDINE | Ki | = | 5e-05 | nM | - |