Assay Detail
Functional
CHEMBL3364798
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human 5-HT7 expressed in HEK-293 cells assessed as inhibition in serotonin-induced increase in cAMP level after 45 mins by HTRF assay
3
Total Activities
3
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
The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.95 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | 2.0 | 1 | 6.54 |
| CHEMBL3321794 | — | — | 1 | 5.66 |
| CHEMBL3321798 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL12314 | MESULERGINE | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3321794 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3321798 | — | IC50 | = | 2300.0 | nM | 5.64 |