Assay Detail
Binding
CHEMBL4404704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE4D2 (86 to 413 residues) expressed in Escherichia coli BL21 codon-plus cells using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation counting method
27
Total Activities
27
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 and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.85 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453774 | — | — | 1 | 7.80 |
| CHEMBL4471352 | — | — | 1 | 7.77 |
| CHEMBL4529685 | — | — | 1 | 7.36 |
| CHEMBL4435746 | — | — | 1 | 7.24 |
| CHEMBL4473291 | — | — | 1 | 7.12 |
| CHEMBL4515248 | — | — | 1 | 7.00 |
| CHEMBL4567905 | — | — | 1 | 7.00 |
| CHEMBL4536071 | — | — | 1 | 6.83 |
| CHEMBL4563050 | — | — | 1 | 6.70 |
| CHEMBL561643 | MANGOSTANIN | — | 1 | 6.38 |
| CHEMBL4434646 | — | — | 1 | 6.32 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.27 |
| CHEMBL4524406 | — | — | 1 | 6.21 |
| CHEMBL323197 | MANGOSTIN | — | 1 | 5.88 |
| CHEMBL4468003 | — | — | 1 | - |
| CHEMBL4440868 | — | — | 1 | - |
| CHEMBL4456328 | — | — | 1 | - |
| CHEMBL4468793 | — | — | 1 | - |
| CHEMBL4463249 | — | — | 1 | - |
| CHEMBL4450759 | — | — | 1 | - |
| CHEMBL4474532 | — | — | 1 | - |
| CHEMBL4533012 | — | — | 1 | - |
| CHEMBL4474598 | — | — | 1 | - |
| CHEMBL4514622 | — | — | 1 | - |
| CHEMBL4545698 | — | — | 1 | - |
| CHEMBL4436788 | — | — | 1 | - |
| CHEMBL4551152 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453774 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4471352 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4529685 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4435746 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4473291 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4515248 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4567905 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4536071 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4563050 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL561643 | MANGOSTANIN | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4434646 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4524406 | — | IC50 | = | 622.0 | nM | 6.21 |
| CHEMBL323197 | MANGOSTIN | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4468003 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4440868 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4456328 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4468793 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4463249 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4450759 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4474532 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4533012 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4474598 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4514622 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4545698 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4436788 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4551152 | — | IC50 | > | 10000.0 | nM | - |