Assay Detail
Binding
CHEMBL756123
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Binding affinity to Nicotinic acetylcholine receptor alpha4-beta2 using +/-[3H]epibatidine as radioligand in rat brain
8
Total Activities
8
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
Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 9.17 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275466 | — | — | 1 | 10.40 |
| CHEMBL274538 | — | — | 1 | 10.29 |
| CHEMBL10886 | — | — | 1 | 9.85 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 9.08 |
| CHEMBL25619 | — | — | 1 | 8.96 |
| CHEMBL10863 | — | — | 1 | 7.92 |
| CHEMBL10585 | — | — | 1 | 7.72 |
| CHEMBL6623 | EPIBATIDINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275466 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL274538 | — | Ki | = | 0.051 | nM | 10.29 |
| CHEMBL10886 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL3 | NICOTINE | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL25619 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL10863 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL10585 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.008 | nM | - |