Assay Detail
Binding
CHEMBL618919
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]granisetron binding to 5-hydroxytryptamine 3 receptor of rat cortical membrane
14
Total Activities
14
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
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.45 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 9.46 |
| CHEMBL39364 | — | — | 1 | 9.40 |
| CHEMBL42911 | — | — | 1 | 9.10 |
| CHEMBL287987 | — | — | 1 | 9.08 |
| CHEMBL42912 | — | — | 1 | 9.01 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 8.74 |
| CHEMBL43193 | — | — | 1 | 8.72 |
| CHEMBL288591 | — | — | 1 | 8.52 |
| CHEMBL288069 | — | — | 1 | 8.24 |
| CHEMBL38919 | — | — | 1 | 7.72 |
| CHEMBL43187 | — | — | 1 | 7.54 |
| CHEMBL41462 | — | — | 1 | 7.34 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 6.92 |
| CHEMBL43467 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL289469 | GRANISETRON | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL39364 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL42911 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL287987 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL42912 | — | Ki | = | 0.98 | nM | 9.01 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL43193 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL288591 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL288069 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL38919 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL43187 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL41462 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL39 | SEROTONIN | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL43467 | — | Ki | > | 5300.0 | nM | - |