Assay Detail
ADMET
CHEMBL4397195
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Inhibition of recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) 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 | 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 | 6.29 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4476440 | — | — | 1 | 7.57 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.50 |
| CHEMBL4570605 | — | — | 1 | 6.99 |
| CHEMBL4459298 | — | — | 1 | 6.84 |
| CHEMBL4437670 | — | — | 1 | 6.83 |
| CHEMBL4544243 | — | — | 1 | 6.69 |
| CHEMBL4564798 | — | — | 1 | 6.60 |
| CHEMBL4449185 | — | — | 1 | 6.60 |
| CHEMBL4573171 | — | — | 1 | 6.50 |
| CHEMBL4434783 | — | — | 1 | 6.46 |
| CHEMBL3315270 | — | — | 1 | 6.32 |
| CHEMBL4458210 | — | — | 1 | 6.27 |
| CHEMBL4567525 | — | — | 1 | 6.09 |
| CHEMBL4593524 | — | — | 1 | 6.05 |
| CHEMBL4518460 | — | — | 1 | 6.04 |
| CHEMBL4541964 | ZATOLMILAST | 3.0 | 1 | 5.99 |
| CHEMBL4569780 | — | — | 1 | 5.89 |
| CHEMBL4553222 | — | — | 1 | 5.78 |
| CHEMBL4561428 | — | — | 1 | 5.70 |
| CHEMBL4440664 | — | — | 1 | 5.68 |
| CHEMBL4472119 | — | — | 1 | 5.61 |
| CHEMBL3315269 | — | — | 1 | 5.39 |
| CHEMBL4455430 | — | — | 1 | 5.20 |
| CHEMBL4533457 | — | — | 1 | - |
| CHEMBL4549467 | — | — | 1 | - |
| CHEMBL4520584 | — | — | 1 | - |
| CHEMBL3315275 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4476440 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL514800 | APREMILAST | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4570605 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4459298 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4437670 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4544243 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4564798 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL4449185 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4573171 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4434783 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL3315270 | — | IC50 | = | 482.0 | nM | 6.32 |
| CHEMBL4458210 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL4567525 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4593524 | — | IC50 | = | 885.0 | nM | 6.05 |
| CHEMBL4518460 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL4541964 | ZATOLMILAST | IC50 | = | 1018.0 | nM | 5.99 |
| CHEMBL4569780 | — | IC50 | = | 1283.0 | nM | 5.89 |
| CHEMBL4553222 | — | IC50 | = | 1665.0 | nM | 5.78 |
| CHEMBL4561428 | — | IC50 | = | 1991.0 | nM | 5.70 |
| CHEMBL4440664 | — | IC50 | = | 2111.0 | nM | 5.68 |
| CHEMBL4472119 | — | IC50 | = | 2431.0 | nM | 5.61 |
| CHEMBL3315269 | — | IC50 | = | 4040.0 | nM | 5.39 |
| CHEMBL4455430 | — | IC50 | = | 6325.0 | nM | 5.20 |
| CHEMBL4533457 | — | IC50 | - | — | - | |
| CHEMBL4549467 | — | IC50 | - | — | - | |
| CHEMBL4520584 | — | IC50 | - | — | - | |
| CHEMBL3315275 | — | IC50 | > | 10000.0 | nM | - |