Assay Detail
Binding
CHEMBL752537
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Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta2 using [3H]epibatidine
6
Total Activities
6
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; alpha3/beta2 (CHEMBL1907587) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.37 | 10.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.46 |
| CHEMBL417586 | — | — | 1 | 8.26 |
| CHEMBL53620 | — | — | 1 | 8.21 |
| CHEMBL55732 | — | — | 1 | 8.05 |
| CHEMBL56045 | — | — | 1 | 7.90 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL417586 | — | Ki | = | 5.44 | nM | 8.26 |
| CHEMBL53620 | — | Ki | = | 6.19 | nM | 8.21 |
| CHEMBL55732 | — | Ki | = | 8.99 | nM | 8.05 |
| CHEMBL56045 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL3 | NICOTINE | Ki | = | 47.0 | nM | 7.33 |