Assay Detail
Binding
CHEMBL4425320
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged PDE4D catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method
10
Total Activities
10
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
3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.13 | 10.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 10.68 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.17 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.96 |
| CHEMBL1230564 | — | — | 1 | 7.68 |
| CHEMBL1230397 | — | — | 1 | 6.80 |
| CHEMBL1794670 | — | — | 1 | 6.57 |
| CHEMBL313842 | ZARDAVERINE | 2.0 | 1 | 6.41 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.26 |
| CHEMBL1230268 | — | — | 1 | 5.70 |
| CHEMBL506972 | — | — | 1 | 4.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | IC50 | = | 0.021 | nM | 10.68 |
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1230564 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1230397 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1794670 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL313842 | ZARDAVERINE | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1230268 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL506972 | — | IC50 | = | 82000.0 | nM | 4.09 |