Assay Detail
Binding
CHEMBL4397198
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His6-tagged PDE4D7 UCR1 S129D 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 | 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 | 27 | 7.74 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4476440 | — | — | 1 | 9.70 |
| CHEMBL4570605 | — | — | 1 | 9.30 |
| CHEMBL4593524 | — | — | 1 | 9.10 |
| CHEMBL4437670 | — | — | 1 | 8.96 |
| CHEMBL4573171 | — | — | 1 | 8.77 |
| CHEMBL4449185 | — | — | 1 | 8.74 |
| CHEMBL4458210 | — | — | 1 | 8.70 |
| CHEMBL4459298 | — | — | 1 | 8.59 |
| CHEMBL4544243 | — | — | 1 | 8.30 |
| CHEMBL4541964 | ZATOLMILAST | 3.0 | 1 | 8.11 |
| CHEMBL4567525 | — | — | 1 | 8.07 |
| CHEMBL4440664 | — | — | 1 | 8.05 |
| CHEMBL4434783 | — | — | 1 | 7.92 |
| CHEMBL4564798 | — | — | 1 | 7.66 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.58 |
| CHEMBL4569780 | — | — | 1 | 7.46 |
| CHEMBL4472119 | — | — | 1 | 7.46 |
| CHEMBL4553222 | — | — | 1 | 7.38 |
| CHEMBL4518460 | — | — | 1 | 7.29 |
| CHEMBL3315275 | — | — | 1 | 7.02 |
| CHEMBL4561428 | — | — | 1 | 6.88 |
| CHEMBL3315270 | — | — | 1 | 6.67 |
| CHEMBL4455430 | — | — | 1 | 6.65 |
| CHEMBL4549467 | — | — | 1 | 6.32 |
| CHEMBL3315269 | — | — | 1 | 6.17 |
| CHEMBL4533457 | — | — | 1 | 6.13 |
| CHEMBL4520584 | — | — | 1 | 5.93 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4476440 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4570605 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4593524 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4437670 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4573171 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4449185 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4458210 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4459298 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4544243 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4541964 | ZATOLMILAST | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4567525 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4440664 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4434783 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4564798 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL514800 | APREMILAST | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4569780 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4472119 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4553222 | — | IC50 | = | 42.1 | nM | 7.38 |
| CHEMBL4518460 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3315275 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4561428 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL3315270 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4455430 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4549467 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL3315269 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL4533457 | — | IC50 | = | 733.0 | nM | 6.13 |
| CHEMBL4520584 | — | IC50 | = | 1165.0 | nM | 5.93 |