Assay Detail
Binding
CHEMBL617704
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Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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 | 12 | 7.26 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 8.51 |
| CHEMBL159405 | — | — | 1 | 7.58 |
| CHEMBL350972 | — | — | 1 | 7.55 |
| CHEMBL355149 | — | — | 1 | 7.47 |
| CHEMBL159821 | — | — | 1 | 7.28 |
| CHEMBL348809 | — | — | 1 | 7.19 |
| CHEMBL349444 | — | — | 1 | 7.14 |
| CHEMBL162078 | — | — | 1 | 7.12 |
| CHEMBL351714 | — | — | 1 | 6.91 |
| CHEMBL159293 | — | — | 1 | 6.77 |
| CHEMBL160109 | — | — | 1 | 6.37 |
| CHEMBL161411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56564 | TROPISETRON | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL159405 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL350972 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL355149 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL159821 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL348809 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL349444 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL162078 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL351714 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL159293 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL160109 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL161411 | — | IC50 | > | 300.0 | nM | - |