Assay Detail
Binding
CHEMBL672457
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Striatum |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
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 | 10 | 7.65 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL164169 | — | — | 1 | 9.55 |
| CHEMBL325109 | CLEBOPRIDE | 2.0 | 1 | 7.92 |
| CHEMBL20748 | — | — | 1 | 7.61 |
| CHEMBL1729 | CISAPRIDE | 4.0 | 1 | 6.64 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.52 |
| CHEMBL301039 | — | — | 2 | - |
| CHEMBL296522 | RENZAPRIDE | 3.0 | 1 | - |
| CHEMBL60889 | MOSAPRIDE | 3.0 | 1 | - |
| CHEMBL164425 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL164169 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL325109 | CLEBOPRIDE | Ki | = | 11.9 | nM | 7.92 |
| CHEMBL20748 | — | Ki | = | 24.3 | nM | 7.61 |
| CHEMBL1729 | CISAPRIDE | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL301039 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL296522 | RENZAPRIDE | Ki | > | 10000.0 | nM | - |
| CHEMBL60889 | MOSAPRIDE | Ki | > | 10000.0 | nM | - |
| CHEMBL301039 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL164425 | — | Ki | > | 1000.0 | nM | - |