Assay Detail
ADMET
CHEMBL4397197
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvate kinase/lactate dehydrogenase-coupled fluorescence assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.65 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4476440 | — | — | 1 | 7.96 |
| CHEMBL4570605 | — | — | 1 | 7.62 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.62 |
| CHEMBL4459298 | — | — | 1 | 7.37 |
| CHEMBL4564798 | — | — | 1 | 7.36 |
| CHEMBL4544243 | — | — | 1 | 7.32 |
| CHEMBL4449185 | — | — | 1 | 7.24 |
| CHEMBL4437670 | — | — | 1 | 7.24 |
| CHEMBL4561428 | — | — | 1 | 7.01 |
| CHEMBL4434783 | — | — | 1 | 6.98 |
| CHEMBL4593524 | — | — | 1 | 6.89 |
| CHEMBL4553222 | — | — | 1 | 6.87 |
| CHEMBL4567525 | — | — | 1 | 6.86 |
| CHEMBL4569780 | — | — | 1 | 6.78 |
| CHEMBL4573171 | — | — | 1 | 6.65 |
| CHEMBL3315270 | — | — | 1 | 6.62 |
| CHEMBL4518460 | — | — | 1 | 6.45 |
| CHEMBL4440664 | — | — | 1 | 6.25 |
| CHEMBL4458210 | — | — | 1 | 6.23 |
| CHEMBL3315269 | — | — | 1 | 6.11 |
| CHEMBL4472119 | — | — | 1 | 6.02 |
| CHEMBL3315275 | — | — | 1 | 5.96 |
| CHEMBL4455430 | — | — | 1 | 5.85 |
| CHEMBL4520584 | — | — | 1 | 5.79 |
| CHEMBL4541964 | ZATOLMILAST | 3.0 | 1 | 5.70 |
| CHEMBL4533457 | — | — | 1 | 5.48 |
| CHEMBL4549467 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4476440 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4570605 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL514800 | APREMILAST | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4459298 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4564798 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4544243 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4449185 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4437670 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4561428 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4434783 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4593524 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL4553222 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4567525 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4569780 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL4573171 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL3315270 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4518460 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4440664 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL4458210 | — | IC50 | = | 584.0 | nM | 6.23 |
| CHEMBL3315269 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL4472119 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL3315275 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4455430 | — | IC50 | = | 1419.0 | nM | 5.85 |
| CHEMBL4520584 | — | IC50 | = | 1642.0 | nM | 5.79 |
| CHEMBL4541964 | ZATOLMILAST | IC50 | = | 2013.0 | nM | 5.70 |
| CHEMBL4533457 | — | IC50 | = | 3287.0 | nM | 5.48 |
| CHEMBL4549467 | — | IC50 | = | 3830.0 | nM | 5.42 |