Assay Detail
Binding
CHEMBL4397243
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged PDE4D3 UCR1 S54D 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
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 3 | 7.89 | 8.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4541964 | ZATOLMILAST | 3.0 | 1 | 8.13 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.64 |
| CHEMBL4593524 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4541964 | ZATOLMILAST | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL514800 | APREMILAST | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4593524 | — | IC50 | - | — | - |