Assay Detail
Binding
CHEMBL619076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 6.89 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 7.84 |
| CHEMBL34291 | — | — | 1 | 7.68 |
| CHEMBL296522 | RENZAPRIDE | 3.0 | 1 | 7.39 |
| CHEMBL301039 | — | — | 2 | 7.32 |
| CHEMBL60889 | MOSAPRIDE | 3.0 | 1 | 7.16 |
| CHEMBL325109 | CLEBOPRIDE | 2.0 | 1 | 6.98 |
| CHEMBL164169 | — | — | 1 | 6.63 |
| CHEMBL28992 | — | — | 1 | 6.42 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.26 |
| CHEMBL164425 | — | — | 1 | 6.08 |
| CHEMBL20748 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1729 | CISAPRIDE | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL34291 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL296522 | RENZAPRIDE | Ki | = | 40.4 | nM | 7.39 |
| CHEMBL301039 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL60889 | MOSAPRIDE | Ki | = | 69.9 | nM | 7.16 |
| CHEMBL325109 | CLEBOPRIDE | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL164169 | — | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL28992 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 546.0 | nM | 6.26 |
| CHEMBL164425 | — | Ki | = | 832.0 | nM | 6.08 |
| CHEMBL20748 | — | Ki | = | 867.0 | nM | 6.06 |
| CHEMBL301039 | — | Ki | > | 1000.0 | nM | - |