Assay Detail
Binding
CHEMBL1065787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE3A by fluorescence microplate reader
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of 6-(benzyloxy)-4-methylquinolin-2(1H)-one derivatives as PDE3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.86 | 6.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL592243 | — | — | 1 | 6.37 |
| CHEMBL592057 | — | — | 1 | 6.19 |
| CHEMBL592242 | — | — | 1 | 6.18 |
| CHEMBL591997 | — | — | 1 | 6.08 |
| CHEMBL591114 | — | — | 1 | 5.90 |
| CHEMBL592241 | — | — | 1 | 5.87 |
| CHEMBL603613 | — | — | 1 | 5.87 |
| CHEMBL589984 | — | — | 1 | 5.84 |
| CHEMBL601295 | — | — | 1 | 5.78 |
| CHEMBL591059 | — | — | 1 | 5.75 |
| CHEMBL592059 | — | — | 1 | 5.55 |
| CHEMBL17423 | VESNARINONE | 2.0 | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL592243 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL592057 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL592242 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL591997 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL591114 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL592241 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL603613 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL589984 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL601295 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL591059 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL592059 | — | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL17423 | VESNARINONE | IC50 | = | 10700.0 | nM | 4.97 |