Assay Detail
Binding
CHEMBL752378
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In vitro Binding affinity towards alpha-3 (PC12) nAChR was determined
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | PC-12 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Neuronal acetylcholine receptor subunit alpha-3 (CHEMBL3068) ↗| Type | SINGLE PROTEIN |
| 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 | 4 | 5.32 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3 | NICOTINE | 4.0 | 1 | 6.66 |
| CHEMBL111583 | — | — | 1 | 5.64 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 4.80 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3 | NICOTINE | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL111583 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL56564 | TROPISETRON | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL289469 | GRANISETRON | Ki | = | 67000.0 | nM | 4.17 |