Assay Detail
Binding
CHEMBL3095679
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]5-HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.26 | 7.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092753 | — | — | 1 | 7.91 |
| CHEMBL3092759 | — | — | 1 | 7.75 |
| CHEMBL294951 | PIZOTYLINE | 2.0 | 1 | 7.60 |
| CHEMBL3092755 | — | — | 1 | 7.38 |
| CHEMBL3092756 | — | — | 1 | 6.84 |
| CHEMBL3092758 | — | — | 1 | 6.73 |
| CHEMBL3092760 | — | — | 1 | 6.62 |
| CHEMBL3092763 | — | — | 1 | - |
| CHEMBL3092762 | — | — | 1 | - |
| CHEMBL3092761 | — | — | 1 | - |
| CHEMBL3092757 | — | — | 1 | - |
| CHEMBL3092754 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092753 | — | Ki | = | 12.4 | nM | 7.91 |
| CHEMBL3092759 | — | Ki | = | 17.6 | nM | 7.75 |
| CHEMBL294951 | PIZOTYLINE | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3092755 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3092756 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL3092758 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL3092760 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL3092763 | — | Ki | > | 100.0 | nM | - |
| CHEMBL3092762 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3092761 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3092757 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3092754 | — | Ki | > | 100.0 | nM | - |