Assay Detail
Binding
CHEMBL3887246
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioligand Binding Assay: The pharmacological profile of metopimazine, metopimazine acid (MPZA), domperidone, and metoclopramide were assessed by radioligand binding and by a functional antagonist assay. For the radioligand binding assay, cell membranes of dopamine D2 receptor expressing cells were incubated with [3H]spiperone and competing drugs in buffer. The assay was terminated by rapid filtration, and the bound radioactive signal was determined by liquid scintillation counting.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Methods for treating GI tract disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.52 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398615 | METOPIMAZINE | 2.0 | 1 | 10.15 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 8.89 |
| CHEMBL3954123 | — | — | 1 | 7.85 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398615 | METOPIMAZINE | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL219916 | DOMPERIDONE | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3954123 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL86 | METOCLOPRAMIDE | Ki | = | 64.0 | nM | 7.19 |