Assay Detail
Functional
CHEMBL5509703
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Antagonist activity at human 5-HT2CR expressed in HEK293 cells assessed as inhibition of 5-HT induced response incubated for 5 mins by Fluo-4 AM dye based Ca2+ imaging assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT<sub>2A</sub> Receptor Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.18 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5531940 | — | — | 1 | 6.50 |
| CHEMBL5560448 | — | — | 1 | 6.19 |
| CHEMBL5557122 | — | — | 1 | 6.07 |
| CHEMBL5558376 | — | — | 1 | 5.96 |
| CHEMBL5556242 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5531940 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5560448 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5557122 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5558376 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5556242 | — | IC50 | ~ | 15000.0 | nM | - |