Assay Detail
Functional
CHEMBL617803
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 5-HT (1 ug/mL) induced depolarization in rat vagus nerve (5-hydroxytryptamine 3 receptor antagonism)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Vagus nerve |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Pyrazolo[1,5-a]pyridines and pyrazolo[1,5-b]pyridazines as 5ht3-antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.14 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 8.85 |
| CHEMBL159405 | — | — | 1 | 7.38 |
| CHEMBL162078 | — | — | 1 | 7.08 |
| CHEMBL348809 | — | — | 1 | 7.00 |
| CHEMBL355149 | — | — | 1 | 6.98 |
| CHEMBL159821 | — | — | 1 | 6.91 |
| CHEMBL159293 | — | — | 1 | 6.52 |
| CHEMBL349444 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56564 | TROPISETRON | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL159405 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL162078 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL348809 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL355149 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL159821 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL159293 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL349444 | — | IC50 | = | 419.0 | nM | 6.38 |