Assay Detail
Binding
CHEMBL617809
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Binding affinity against 5-hydroxytryptamine 3 receptor in rat cortical membrane using [3H]GR-65630 as radioligand
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Serotonin 3 (5-HT3) receptor (CHEMBL2094116) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
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 | 22 | 7.78 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL46 | ONDANSETRON | 4.0 | 1 | 8.85 |
| CHEMBL1788261 | — | — | 1 | 8.82 |
| CHEMBL157784 | — | — | 1 | 8.72 |
| CHEMBL40082 | — | — | 1 | 8.54 |
| CHEMBL2093035 | — | — | 1 | 8.35 |
| CHEMBL156188 | — | — | 1 | 8.32 |
| CHEMBL348517 | — | — | 1 | 8.18 |
| CHEMBL2093034 | — | — | 1 | 8.15 |
| CHEMBL346973 | — | — | 1 | 8.07 |
| CHEMBL156346 | — | — | 1 | 8.02 |
| CHEMBL2093036 | — | — | 1 | 8.00 |
| CHEMBL1788260 | — | — | 1 | 7.92 |
| CHEMBL345592 | — | — | 1 | 7.62 |
| CHEMBL347587 | — | — | 1 | 7.48 |
| CHEMBL347902 | — | — | 1 | 7.44 |
| CHEMBL436021 | — | — | 1 | 7.43 |
| CHEMBL345220 | — | — | 1 | 7.30 |
| CHEMBL1788262 | — | — | 1 | 7.01 |
| CHEMBL1788263 | — | — | 1 | 6.87 |
| CHEMBL351119 | — | — | 1 | 6.19 |
| CHEMBL86 | METOCLOPRAMIDE | 4.0 | 1 | 6.06 |
| CHEMBL219916 | DOMPERIDONE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL46 | ONDANSETRON | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1788261 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL157784 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL40082 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2093035 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL156188 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL348517 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2093034 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL346973 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL156346 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL2093036 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1788260 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL345592 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL347587 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL347902 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL436021 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL345220 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1788262 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL1788263 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL351119 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL86 | METOCLOPRAMIDE | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL219916 | DOMPERIDONE | IC50 | > | 100.0 | nM | - |