Assay Detail
Binding
CHEMBL3362767
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Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| 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 Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.02 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293950 | — | — | 1 | 6.09 |
| CHEMBL3318890 | — | — | 1 | 5.47 |
| CHEMBL3318891 | — | — | 1 | 4.52 |
| CHEMBL3318894 | — | — | 1 | 4.00 |
| CHEMBL3318901 | — | — | 1 | - |
| CHEMBL3318897 | — | — | 1 | - |
| CHEMBL3318902 | — | — | 1 | - |
| CHEMBL3318896 | — | — | 1 | - |
| CHEMBL3318892 | — | — | 1 | - |
| CHEMBL3318889 | — | — | 1 | - |
| CHEMBL3318893 | — | — | 1 | - |
| CHEMBL3318895 | — | — | 1 | - |
| CHEMBL3318898 | — | — | 1 | - |
| CHEMBL3318899 | — | — | 1 | - |
| CHEMBL3318900 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293950 | — | Ki | = | 820.0 | nM | 6.09 |
| CHEMBL3318890 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL3318891 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL3318894 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL3318901 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL3318897 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318902 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318896 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL3318892 | — | Ki | > | 300000.0 | nM | - |
| CHEMBL3318889 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318893 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318895 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318898 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318899 | — | Ki | = | 300000.0 | nM | - |
| CHEMBL3318900 | — | Ki | > | 300000.0 | nM | - |