Assay Detail
Binding
CHEMBL751867
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In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined
7
Total Activities
7
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
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.31 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 8.64 |
| CHEMBL108799 | — | — | 1 | 5.58 |
| CHEMBL111583 | — | — | 1 | 5.11 |
| CHEMBL320963 | — | — | 1 | 4.85 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 4.42 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 4.34 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL108799 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL111583 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL320963 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL289469 | GRANISETRON | Ki | = | 38000.0 | nM | 4.42 |
| CHEMBL46 | ONDANSETRON | Ki | = | 46000.0 | nM | 4.34 |
| CHEMBL56564 | TROPISETRON | Ki | = | 55000.0 | nM | 4.26 |