Assay Detail
Binding
CHEMBL4844538
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Antagonist activity at human 5-HT3 receptor expressed in CHO-K1 cells assessed as inhibition of 5-HT induced inward currents preincubated for 30 sec followed by 5HT addition for 2 sec at -60 mV holding potential by ion flux automated patch clamp assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| 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 | 7.97 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1189679 | PALONOSETRON | 4.0 | 1 | 8.77 |
| CHEMBL4867565 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1189679 | PALONOSETRON | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4867565 | — | IC50 | = | 67.6 | nM | 7.17 |