Assay Detail
Binding
CHEMBL5118310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT<sub>6</sub>R antagonists: Design, synthesis, biological evaluation, and early in vivo cognition-enhancing studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 9.36 | 10.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5189271 | — | — | 1 | 10.07 |
| CHEMBL5177311 | — | — | 1 | 9.74 |
| CHEMBL5169546 | — | — | 1 | 9.68 |
| CHEMBL5206617 | — | — | 1 | 9.59 |
| CHEMBL5170650 | — | — | 1 | 9.59 |
| CHEMBL96745 | — | — | 1 | 9.59 |
| CHEMBL5187350 | — | — | 1 | 9.48 |
| CHEMBL5208122 | — | — | 1 | 9.37 |
| CHEMBL5206037 | — | — | 1 | 9.34 |
| CHEMBL5203370 | — | — | 1 | 9.26 |
| CHEMBL5194574 | — | — | 1 | 9.19 |
| CHEMBL5201308 | — | — | 1 | 9.17 |
| CHEMBL5201491 | — | — | 1 | 9.08 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 1 | 9.08 |
| CHEMBL5183606 | — | — | 1 | 9.06 |
| CHEMBL5171917 | — | — | 1 | 8.89 |
| CHEMBL5187416 | — | — | 1 | 8.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5189271 | — | Ki | = | 0.085 | nM | 10.07 |
| CHEMBL5177311 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL5169546 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL5206617 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL5170650 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL96745 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL5187350 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL5208122 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL5206037 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL5203370 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL5194574 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL5201308 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL5201491 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL3286580 | IDALOPIRDINE | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL5183606 | — | Ki | = | 0.87 | nM | 9.06 |
| CHEMBL5171917 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL5187416 | — | Ki | = | 1.3 | nM | 8.89 |