Assay Detail
Binding
CHEMBL5339426
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE4D2 (unknown origin)
4
Total Activities
4
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
Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.87 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.40 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 6.30 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.23 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL514800 | APREMILAST | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 2800.0 | nM | 5.55 |