Assay Detail
Binding
CHEMBL751862
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Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.31 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | — | 1 | 10.30 |
| CHEMBL291498 | — | — | 1 | 9.59 |
| CHEMBL105374 | — | — | 1 | 9.00 |
| CHEMBL323325 | — | — | 1 | 8.96 |
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.40 |
| CHEMBL46486 | TETRAMETHYLAMMONIUM ION | — | 1 | 7.62 |
| CHEMBL6200 | NORNICOTINE | 1.0 | 1 | 7.54 |
| CHEMBL280963 | DL-ANABASINE | — | 1 | 7.04 |
| CHEMBL102246 | — | — | 1 | 6.35 |
| CHEMBL321099 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6623 | EPIBATIDINE | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL291498 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL105374 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL323325 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3 | NICOTINE | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL46486 | TETRAMETHYLAMMONIUM ION | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL6200 | NORNICOTINE | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL280963 | DL-ANABASINE | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL102246 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL321099 | — | Ki | - | nM | - |