Assay Detail
Binding
CHEMBL618920
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor
12
Total Activities
11
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
Synthesis and structure-affinity relationships of novel N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)pyridine-3-carboxamides with potent serotonin 5-HT3 and dopamine D2 receptor antagonistic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.50 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL28992 | — | — | 1 | 9.70 |
| CHEMBL301039 | — | — | 2 | 9.10 |
| CHEMBL296522 | RENZAPRIDE | 3.0 | 1 | 8.28 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 7.02 |
| CHEMBL34291 | — | — | 1 | 6.82 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.68 |
| CHEMBL164425 | — | — | 1 | 6.57 |
| CHEMBL60889 | MOSAPRIDE | 3.0 | 1 | 5.92 |
| CHEMBL20748 | — | — | 1 | - |
| CHEMBL164169 | — | — | 1 | - |
| CHEMBL325109 | CLEBOPRIDE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL28992 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL301039 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL296522 | RENZAPRIDE | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL301039 | — | Ki | = | 41.8 | nM | 7.38 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 94.7 | nM | 7.02 |
| CHEMBL34291 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL164425 | — | Ki | = | 267.0 | nM | 6.57 |
| CHEMBL60889 | MOSAPRIDE | Ki | = | 1189.0 | nM | 5.92 |
| CHEMBL20748 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL164169 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL325109 | CLEBOPRIDE | Ki | > | 1000.0 | nM | - |