Assay Detail
Binding
CHEMBL5580831
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 insect cells using FAM-cyclic-3',5'-AMP as substrate measured after 1 hr by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 7-alkoxybenzofurans as PDE4 inhibitors with hepatoprotective activity in D-GalN/LPS-induced hepatic sepsis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.57 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 8.00 |
| CHEMBL5594814 | — | — | 1 | 7.86 |
| CHEMBL5594063 | — | — | 1 | 7.82 |
| CHEMBL5591341 | — | — | 1 | 7.74 |
| CHEMBL5595424 | — | — | 1 | 7.73 |
| CHEMBL5595946 | — | — | 1 | 7.59 |
| CHEMBL5568942 | — | — | 1 | 7.33 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL514800 | APREMILAST | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5594814 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL5594063 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL5591341 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL5595424 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL5595946 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL5568942 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 326.0 | nM | 6.49 |