Assay Detail
Binding
CHEMBL619785
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [3H]granisetron specifically bound to 5-hydroxytryptamine 3 receptor in rat cortical membrane
27
Total Activities
27
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
Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.77 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL43355 | — | — | 1 | 9.64 |
| CHEMBL289469 | GRANISETRON | 4.0 | 1 | 9.46 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.92 |
| CHEMBL64279 | — | — | 1 | 8.77 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 8.74 |
| CHEMBL43193 | — | — | 1 | 8.72 |
| CHEMBL164031 | — | — | 1 | 8.72 |
| CHEMBL288591 | — | — | 1 | 8.52 |
| CHEMBL352148 | — | — | 1 | 8.32 |
| CHEMBL162390 | — | — | 1 | 7.96 |
| CHEMBL163595 | — | — | 1 | 7.89 |
| CHEMBL352107 | — | — | 1 | 7.85 |
| CHEMBL337213 | — | — | 1 | 7.42 |
| CHEMBL336522 | — | — | 1 | 7.32 |
| CHEMBL41140 | 6-NITROQUIPAZINE | — | 1 | 7.24 |
| CHEMBL163440 | — | — | 1 | 7.23 |
| CHEMBL126350 | — | — | 1 | 7.09 |
| CHEMBL287987 | — | — | 1 | 7.08 |
| CHEMBL163279 | — | — | 1 | 6.96 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 6.92 |
| CHEMBL351752 | — | — | 1 | 6.70 |
| CHEMBL349542 | — | — | 1 | 6.70 |
| CHEMBL162437 | — | — | 1 | 6.18 |
| CHEMBL165721 | — | — | 1 | 6.08 |
| CHEMBL166214 | — | — | 1 | - |
| CHEMBL165861 | — | — | 1 | - |
| CHEMBL162219 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL43355 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL289469 | GRANISETRON | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL56 | 8-OH-DPAT | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL64279 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL43193 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL164031 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL288591 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL352148 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL162390 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL163595 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL352107 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL337213 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL336522 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL41140 | 6-NITROQUIPAZINE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL163440 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL126350 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL287987 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL163279 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL39 | SEROTONIN | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL351752 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL349542 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL162437 | — | Ki | = | 660.0 | nM | 6.18 |
| CHEMBL165721 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL166214 | — | Ki | > | 550.0 | nM | - |
| CHEMBL165861 | — | Ki | > | 17000.0 | nM | - |
| CHEMBL162219 | — | Ki | > | 550.0 | nM | - |