Assay Detail
Functional
CHEMBL5118312
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| IC50 | 7 | 8.01 | 8.44 |
| Kb | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5169546 | — | — | 2 | 8.44 |
| CHEMBL96745 | — | — | 2 | 8.44 |
| CHEMBL5189271 | — | — | 2 | 8.21 |
| CHEMBL5170650 | — | — | 2 | 8.15 |
| CHEMBL5206617 | — | — | 2 | 7.68 |
| CHEMBL3286580 | IDALOPIRDINE | 3.0 | 2 | 7.58 |
| CHEMBL5177311 | — | — | 2 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5169546 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL96745 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5189271 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL5170650 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5206617 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3286580 | IDALOPIRDINE | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5177311 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5169546 | — | Kb | = | 0.56 | nM | - |
| CHEMBL96745 | — | Kb | = | 0.55 | nM | - |
| CHEMBL5177311 | — | Kb | = | 4.5 | nM | - |
| CHEMBL5206617 | — | Kb | = | 3.3 | nM | - |
| CHEMBL5170650 | — | Kb | = | 1.1 | nM | - |
| CHEMBL5189271 | — | Kb | = | 0.99 | nM | - |
| CHEMBL3286580 | IDALOPIRDINE | Kb | = | 4.1 | nM | - |