Assay Detail
Binding
CHEMBL750860
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Binding affinity to Nicotinic acetylcholine receptor alpha3-beta4 using +/-[3H]epibatidine as radioligand in pig adrenal gland
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Tissue | Adrenal gland |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit beta-4 (CHEMBL2658) ↗| Type | SINGLE PROTEIN |
| 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 | 8.19 | 10.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.66 |
| CHEMBL275466 | — | — | 1 | 8.89 |
| CHEMBL10585 | — | — | 1 | 8.60 |
| CHEMBL274538 | — | — | 1 | 8.21 |
| CHEMBL25619 | — | — | 1 | 7.72 |
| CHEMBL10886 | — | — | 1 | 7.70 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.14 |
| CHEMBL10863 | — | — | 1 | 6.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL275466 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL10585 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL274538 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL25619 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL10886 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3 | NICOTINE | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL10863 | — | Ki | = | 259.0 | nM | 6.59 |