Assay Detail
Binding
CHEMBL619789
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide as a radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Synthesis and biochemical evaluation of tritium-labeled 1-methyl-N-(8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-1H-indazole-3-carboxa mide, a useful radioligand for 5HT3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.98 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18041 | ZACOPRIDE | 2.0 | 1 | 9.38 |
| CHEMBL56564 | TROPISETRON | 3.0 | 1 | 8.89 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 8.79 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 8.52 |
| CHEMBL38582 | — | — | 1 | 8.37 |
| CHEMBL2107804 | BEMESETRON | 2.0 | 1 | 7.58 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.30 |
| CHEMBL39109 | — | — | 1 | 5.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18041 | ZACOPRIDE | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL56564 | TROPISETRON | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL289469 | GRANISETRON | Ki | = | 1.62 | nM | 8.79 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 3.04 | nM | 8.52 |
| CHEMBL38582 | — | Ki | = | 4.26 | nM | 8.37 |
| CHEMBL2107804 | BEMESETRON | Ki | = | 26.05 | nM | 7.58 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL39109 | — | Ki | = | 1048.0 | nM | 5.98 |