Assay Detail
Functional
CHEMBL4844560
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Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NG108-15 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT<sub>3</sub> and 5-HT<sub>6</sub> Receptor Antagonist with Antipsychotic and Procognitive Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 7.78 | 8.55 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | 3.0 | 1 | 8.55 |
| CHEMBL1210710 | SB-399885 | — | 1 | 7.01 |
| CHEMBL4867565 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083390 | INTEPIRDINE | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1210710 | SB-399885 | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4867565 | — | Activity | - | — | - |