Assay Detail
Binding
CHEMBL1006686
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Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
5-hydroxytryptamine receptor 3A (CHEMBL2411) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.03 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523716 | — | — | 1 | 9.10 |
| CHEMBL341474 | — | — | 1 | 9.10 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 9.02 |
| CHEMBL466462 | — | — | 1 | 8.92 |
| CHEMBL445505 | — | — | 1 | 8.68 |
| CHEMBL492395 | — | — | 1 | 8.66 |
| CHEMBL511555 | — | — | 1 | 8.55 |
| CHEMBL523042 | — | — | 1 | 8.52 |
| CHEMBL503987 | — | — | 1 | 8.47 |
| CHEMBL493183 | — | — | 1 | 8.14 |
| CHEMBL468498 | — | — | 1 | 7.95 |
| CHEMBL523497 | — | — | 1 | 7.93 |
| CHEMBL512418 | — | — | 1 | 7.77 |
| CHEMBL494999 | — | — | 1 | 7.36 |
| CHEMBL466456 | — | — | 1 | 7.19 |
| CHEMBL495000 | — | — | 1 | 7.10 |
| CHEMBL466655 | — | — | 1 | 6.90 |
| CHEMBL466662 | — | — | 1 | 6.62 |
| CHEMBL466446 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523716 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL341474 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL466462 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL445505 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL492395 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL511555 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL523042 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL503987 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL493183 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL468498 | — | Ki | = | 11.2 | nM | 7.95 |
| CHEMBL523497 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL512418 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL494999 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL466456 | — | Ki | = | 65.0 | nM | 7.19 |
| CHEMBL495000 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL466655 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL466662 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL466446 | — | Ki | = | 246.0 | nM | 6.61 |