Assay Detail
Binding
CHEMBL670403
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against dopamine D2 receptor in rat brain synaptic membrane using [3H]-spiperone as radioligand
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
A novel series of N-(hexahydro-1,4-diazepin-6-yl) and N-(hexahydroazepin- 3-yl)benzamides with high affinity for 5-HT3 and dopamine D2 receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.17 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 8.60 |
| CHEMBL1788262 | — | — | 1 | 8.35 |
| CHEMBL348517 | — | — | 1 | 7.96 |
| CHEMBL1788263 | — | — | 1 | 7.72 |
| CHEMBL345220 | — | — | 1 | 7.60 |
| CHEMBL40082 | — | — | 1 | 7.46 |
| CHEMBL347587 | — | — | 1 | 7.41 |
| CHEMBL436021 | — | — | 1 | 7.24 |
| CHEMBL156188 | — | — | 1 | 7.21 |
| CHEMBL1788260 | — | — | 1 | 7.06 |
| CHEMBL351119 | — | — | 1 | 7.06 |
| CHEMBL346973 | — | — | 1 | 6.90 |
| CHEMBL157784 | — | — | 1 | 6.74 |
| CHEMBL345592 | — | — | 1 | 6.66 |
| CHEMBL347902 | — | — | 1 | 6.64 |
| CHEMBL1788261 | — | — | 1 | 6.50 |
| CHEMBL2093035 | — | — | 1 | 6.43 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.32 |
| CHEMBL2093034 | — | — | 1 | 6.29 |
| CHEMBL2093036 | — | — | 1 | - |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL1788262 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL348517 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1788263 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL345220 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL40082 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL347587 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL436021 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL156188 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1788260 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL351119 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL346973 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL157784 | — | IC50 | = | 181.0 | nM | 6.74 |
| CHEMBL345592 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL347902 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1788261 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2093035 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2093034 | — | IC50 | = | 517.0 | nM | 6.29 |
| CHEMBL2093036 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL46 | ONDANSETRON | IC50 | > | 1000.0 | nM | - |