Assay Detail
Binding
CHEMBL617841
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]mesulergine bound to 5-hydroxytryptamine 2C receptor in rat cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cortex |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 6.31 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 9.14 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 6.72 |
| CHEMBL287987 | — | — | 1 | 5.55 |
| CHEMBL43355 | — | — | 1 | 5.36 |
| CHEMBL352107 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL287987 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL43355 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL352107 | — | Ki | = | 16000.0 | nM | 4.80 |