Assay Detail
Binding
CHEMBL4196372
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Inhibition of human GST-tagged PDE7A expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase 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 | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 4.70 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL484928 | — | — | 1 | 5.68 |
| CHEMBL4209680 | — | — | 1 | 5.50 |
| CHEMBL4215783 | — | — | 1 | 5.42 |
| CHEMBL4218055 | — | — | 1 | 5.14 |
| CHEMBL4205843 | — | — | 1 | 5.09 |
| CHEMBL4207233 | — | — | 1 | 5.02 |
| CHEMBL4211991 | — | — | 1 | 4.98 |
| CHEMBL4207258 | — | — | 1 | 4.93 |
| CHEMBL4203371 | — | — | 1 | 4.56 |
| CHEMBL4210386 | — | — | 1 | 4.47 |
| CHEMBL4213966 | — | — | 1 | 4.31 |
| CHEMBL4217007 | — | — | 1 | 4.28 |
| CHEMBL4203545 | — | — | 1 | 4.25 |
| CHEMBL4205157 | — | — | 1 | 4.16 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 4.07 |
| CHEMBL4204397 | — | — | 1 | 4.05 |
| CHEMBL4209377 | — | — | 1 | 4.03 |
| CHEMBL4214592 | — | — | 1 | - |
| CHEMBL4217546 | — | — | 1 | - |
| CHEMBL4214541 | — | — | 1 | - |
| CHEMBL4207716 | — | — | 1 | - |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | - |
| CHEMBL4216676 | — | — | 1 | - |
| CHEMBL4214256 | — | — | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
| CHEMBL4218669 | — | — | 1 | - |
| CHEMBL4213058 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL484928 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4209680 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4215783 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4218055 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4205843 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4207233 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL4211991 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL4207258 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4203371 | — | IC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL4210386 | — | IC50 | = | 33600.0 | nM | 4.47 |
| CHEMBL4213966 | — | IC50 | = | 48900.0 | nM | 4.31 |
| CHEMBL4217007 | — | IC50 | = | 52800.0 | nM | 4.28 |
| CHEMBL4203545 | — | IC50 | = | 56100.0 | nM | 4.25 |
| CHEMBL4205157 | — | IC50 | = | 69800.0 | nM | 4.16 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | IC50 | = | 85600.0 | nM | 4.07 |
| CHEMBL4204397 | — | IC50 | = | 89300.0 | nM | 4.05 |
| CHEMBL4209377 | — | IC50 | = | 92900.0 | nM | 4.03 |
| CHEMBL4214592 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4217546 | — | IC50 | = | 115900.0 | nM | - |
| CHEMBL4214541 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4207716 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL63 | ROLIPRAM | IC50 | > | 200000.0 | nM | - |
| CHEMBL4216676 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4214256 | — | IC50 | = | 140900.0 | nM | - |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | > | 200000.0 | nM | - |
| CHEMBL4218669 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4213058 | — | IC50 | > | 200000.0 | nM | - |