Assay Detail
Binding
CHEMBL5339428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant PDE4D2 (86 to 413 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation method
19
Total Activities
19
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 | 19 | 7.84 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5400816 | — | — | 1 | 8.85 |
| CHEMBL5431083 | — | — | 1 | 8.85 |
| CHEMBL5407967 | — | — | 1 | 8.46 |
| CHEMBL5408080 | — | — | 1 | 8.28 |
| CHEMBL5421333 | — | — | 1 | 8.19 |
| CHEMBL5420700 | — | — | 1 | 8.11 |
| CHEMBL5440771 | — | — | 1 | 8.09 |
| CHEMBL5435764 | — | — | 1 | 8.03 |
| CHEMBL5434362 | — | — | 1 | 7.99 |
| CHEMBL5434713 | — | — | 1 | 7.97 |
| CHEMBL5438159 | — | — | 1 | 7.93 |
| CHEMBL5410553 | — | — | 1 | 7.91 |
| CHEMBL5405731 | — | — | 1 | 7.70 |
| CHEMBL5437810 | — | — | 1 | 7.60 |
| CHEMBL5428117 | — | — | 1 | 6.69 |
| CHEMBL561643 | MANGOSTANIN | — | 1 | 6.38 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.23 |
| CHEMBL5420621 | — | — | 1 | - |
| CHEMBL5437828 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5400816 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5431083 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5407967 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5408080 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5421333 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5420700 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5440771 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5435764 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5434362 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5434713 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL5438159 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5410553 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5405731 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL5437810 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5428117 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL561643 | MANGOSTANIN | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL5420621 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5437828 | — | IC50 | > | 1000.0 | nM | - |