Assay Detail
Binding
CHEMBL1037804
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Displacement of [3H]LY278584 from 5HT3 receptor in rat cortical homogenate
18
Total Activities
18
Compounds Tested
2
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
Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.37 | 9.36 |
| IC50 | 2 | 7.98 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL124886 | — | — | 1 | 9.36 |
| CHEMBL582992 | — | — | 1 | 9.31 |
| CHEMBL566522 | — | — | 1 | 9.17 |
| CHEMBL136978 | — | — | 1 | 9.10 |
| CHEMBL341474 | — | — | 1 | 9.09 |
| CHEMBL18772 | QUIPAZINE | 2.0 | 1 | 9.02 |
| CHEMBL137621 | — | — | 1 | 8.66 |
| CHEMBL571483 | — | — | 1 | 8.65 |
| CHEMBL423899 | — | — | 1 | 8.62 |
| CHEMBL571046 | — | — | 1 | 8.25 |
| CHEMBL136536 | — | — | 1 | 8.06 |
| CHEMBL523497 | — | — | 1 | 7.93 |
| CHEMBL342447 | — | — | 1 | 7.89 |
| CHEMBL578809 | — | — | 1 | 7.75 |
| CHEMBL576046 | — | — | 1 | 7.65 |
| CHEMBL576282 | — | — | 1 | 7.52 |
| CHEMBL570103 | — | — | 1 | 7.35 |
| CHEMBL571475 | — | — | 1 | 6.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL124886 | — | Ki | = | 0.44 | nM | 9.36 |
| CHEMBL582992 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL566522 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL136978 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL341474 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL18772 | QUIPAZINE | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL137621 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL571483 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL423899 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL571046 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL136536 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL523497 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL342447 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL578809 | — | Ki | = | 17.84 | nM | 7.75 |
| CHEMBL576046 | — | Ki | = | 22.21 | nM | 7.65 |
| CHEMBL576282 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL570103 | — | Ki | = | 44.3 | nM | 7.35 |
| CHEMBL571475 | — | Ki | = | 330.2 | nM | 6.48 |