Assay Detail
Binding
CHEMBL4425316
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged PDE4B 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
11
Total Activities
11
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 4B (CHEMBL275) ↗| 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 | 11 | 6.84 | 10.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 10.39 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.60 |
| CHEMBL1230564 | — | — | 1 | 7.48 |
| CHEMBL519827 | — | — | 1 | 7.25 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 7.08 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 6.64 |
| CHEMBL603830 | DAXALIPRAM | 2.0 | 1 | 6.38 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.26 |
| CHEMBL590754 | FILAMINAST | 2.0 | 1 | 6.02 |
| CHEMBL168949 | — | — | 1 | 5.42 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | IC50 | = | 0.041 | nM | 10.39 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1230564 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL519827 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL603830 | DAXALIPRAM | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL590754 | FILAMINAST | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL168949 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 20000.0 | nM | 4.70 |