Assay Detail
Binding
CHEMBL617812
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Concentration required to inhibit the binding of radioligand [3H]GR-65630 to serotonin 5-hydroxytryptamine-3 receptor (5-HT 3 receptor)in rat brain cortical membrane
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 28 | 8.49 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL164360 | — | — | 1 | 9.26 |
| CHEMBL349050 | — | — | 1 | 9.23 |
| CHEMBL164324 | — | — | 1 | 9.19 |
| CHEMBL164000 | — | — | 1 | 9.16 |
| CHEMBL351377 | — | — | 1 | 9.12 |
| CHEMBL40903 | — | — | 1 | 9.01 |
| CHEMBL416047 | — | — | 1 | 8.92 |
| CHEMBL39016 | — | — | 1 | 8.90 |
| CHEMBL349595 | — | — | 1 | 8.89 |
| CHEMBL40497 | — | — | 1 | 8.89 |
| CHEMBL349146 | — | — | 1 | 8.83 |
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 8.81 |
| CHEMBL38969 | — | — | 1 | 8.79 |
| CHEMBL38473 | — | — | 1 | 8.71 |
| CHEMBL432284 | — | — | 1 | 8.69 |
| CHEMBL40082 | — | — | 1 | 8.54 |
| CHEMBL1744066 | — | — | 1 | 8.43 |
| CHEMBL287760 | — | — | 1 | 8.42 |
| CHEMBL290959 | — | — | 1 | 8.29 |
| CHEMBL349048 | — | — | 1 | 8.18 |
| CHEMBL346973 | — | — | 1 | 8.07 |
| CHEMBL291296 | — | — | 1 | 8.00 |
| CHEMBL159835 | — | — | 1 | 7.52 |
| CHEMBL163859 | — | — | 1 | 7.41 |
| CHEMBL163800 | — | — | 1 | 6.83 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.64 |
| CHEMBL1744067 | — | — | 1 | - |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL164360 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL349050 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL164324 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL164000 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL351377 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL40903 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL416047 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL39016 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL349595 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL40497 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL349146 | — | IC50 | = | 1.48 | nM | 8.83 |
| CHEMBL46 | ONDANSETRON | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL38969 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL38473 | — | IC50 | = | 1.96 | nM | 8.71 |
| CHEMBL432284 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL40082 | — | IC50 | = | 2.86 | nM | 8.54 |
| CHEMBL1744066 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL287760 | — | IC50 | = | 3.81 | nM | 8.42 |
| CHEMBL290959 | — | IC50 | = | 5.14 | nM | 8.29 |
| CHEMBL349048 | — | IC50 | = | 6.56 | nM | 8.18 |
| CHEMBL346973 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL291296 | — | IC50 | = | 9.93 | nM | 8.00 |
| CHEMBL159835 | — | IC50 | = | 29.9 | nM | 7.52 |
| CHEMBL163859 | — | IC50 | = | 38.7 | nM | 7.41 |
| CHEMBL163800 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL1744067 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL219916 | DOMPERIDONE | IC50 | > | 1000.0 | nM | - |