Assay Detail
Binding
CHEMBL675892
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Inhibition of the binding of radioligand [3H]spiperone to dopamine receptor D2 in rat brain synaptic membrane
25
Total Activities
25
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
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 |
|---|---|---|---|
| IC50 | 25 | 7.29 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL416047 | — | — | 1 | 8.16 |
| CHEMBL164000 | — | — | 1 | 7.89 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | 7.87 |
| CHEMBL349050 | — | — | 1 | 7.68 |
| CHEMBL40903 | — | — | 1 | 7.63 |
| CHEMBL164324 | — | — | 1 | 7.56 |
| CHEMBL40082 | — | — | 1 | 7.46 |
| CHEMBL164360 | — | — | 1 | 7.37 |
| CHEMBL351377 | — | — | 1 | 7.33 |
| CHEMBL287760 | — | — | 1 | 7.32 |
| CHEMBL291296 | — | — | 1 | 7.12 |
| CHEMBL38473 | — | — | 1 | 7.12 |
| CHEMBL349146 | — | — | 1 | 7.06 |
| CHEMBL40497 | — | — | 1 | 6.91 |
| CHEMBL346973 | — | — | 1 | 6.90 |
| CHEMBL349595 | — | — | 1 | 6.86 |
| CHEMBL432284 | — | — | 1 | 6.70 |
| CHEMBL1744066 | — | — | 1 | 6.20 |
| CHEMBL159835 | — | — | 1 | - |
| CHEMBL1744067 | — | — | 1 | - |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | - |
| CHEMBL163859 | — | — | 1 | - |
| CHEMBL159972 | — | — | 1 | - |
| CHEMBL349048 | — | — | 1 | - |
| CHEMBL163800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL416047 | — | IC50 | = | 6.88 | nM | 8.16 |
| CHEMBL164000 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL219916 | DOMPERIDONE | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL349050 | — | IC50 | = | 20.9 | nM | 7.68 |
| CHEMBL40903 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL164324 | — | IC50 | = | 27.8 | nM | 7.56 |
| CHEMBL40082 | — | IC50 | = | 34.6 | nM | 7.46 |
| CHEMBL164360 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL351377 | — | IC50 | = | 47.1 | nM | 7.33 |
| CHEMBL287760 | — | IC50 | = | 48.1 | nM | 7.32 |
| CHEMBL291296 | — | IC50 | = | 75.2 | nM | 7.12 |
| CHEMBL38473 | — | IC50 | = | 76.4 | nM | 7.12 |
| CHEMBL349146 | — | IC50 | = | 86.4 | nM | 7.06 |
| CHEMBL40497 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL346973 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL349595 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL432284 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1744066 | — | IC50 | = | 637.0 | nM | 6.20 |
| CHEMBL159835 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1744067 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL46 | ONDANSETRON | IC50 | > | 1000.0 | nM | - |
| CHEMBL163859 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL159972 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL349048 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL163800 | — | IC50 | > | 1000.0 | nM | - |