Assay Detail
Binding
CHEMBL4196371
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Inhibition of human GST-tagged PDE4B expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay
28
Total Activities
28
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
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| 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 | 28 | 4.95 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 5.96 |
| CHEMBL4209680 | — | — | 1 | 5.85 |
| CHEMBL4207233 | — | — | 1 | 5.75 |
| CHEMBL4205843 | — | — | 1 | 5.72 |
| CHEMBL4211991 | — | — | 1 | 5.36 |
| CHEMBL4217546 | — | — | 1 | 5.26 |
| CHEMBL4215783 | — | — | 1 | 5.13 |
| CHEMBL4214541 | — | — | 1 | 5.11 |
| CHEMBL4203371 | — | — | 1 | 5.10 |
| CHEMBL4214592 | — | — | 1 | 4.90 |
| CHEMBL4214256 | — | — | 1 | 4.79 |
| CHEMBL4218055 | — | — | 1 | 4.57 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | — | 1 | 4.55 |
| CHEMBL4207258 | — | — | 1 | 4.51 |
| CHEMBL4213966 | — | — | 1 | 4.43 |
| CHEMBL4217007 | — | — | 1 | 4.36 |
| CHEMBL4204397 | — | — | 1 | 4.32 |
| CHEMBL4209377 | — | — | 1 | 4.29 |
| CHEMBL4205157 | — | — | 1 | 4.15 |
| CHEMBL628 | PENTOXIFYLLINE | 4.0 | 1 | - |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | - |
| CHEMBL4213058 | — | — | 1 | - |
| CHEMBL484928 | — | — | 1 | - |
| CHEMBL4210386 | — | — | 1 | - |
| CHEMBL4203545 | — | — | 1 | - |
| CHEMBL4207716 | — | — | 1 | - |
| CHEMBL4216676 | — | — | 1 | - |
| CHEMBL4218669 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4209680 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4207233 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4205843 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4211991 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4217546 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4215783 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL4214541 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL4203371 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4214592 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL4214256 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL4218055 | — | IC50 | = | 26900.0 | nM | 4.57 |
| CHEMBL275084 | ISOBUTYLMETHYLXANTHINE | IC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL4207258 | — | IC50 | = | 31100.0 | nM | 4.51 |
| CHEMBL4213966 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL4217007 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL4204397 | — | IC50 | = | 47800.0 | nM | 4.32 |
| CHEMBL4209377 | — | IC50 | = | 51800.0 | nM | 4.29 |
| CHEMBL4205157 | — | IC50 | = | 70800.0 | nM | 4.15 |
| CHEMBL628 | PENTOXIFYLLINE | IC50 | > | 90000.0 | nM | - |
| CHEMBL1355736 | THEOPHYLLINE | IC50 | > | 200000.0 | nM | - |
| CHEMBL4213058 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL484928 | — | IC50 | = | 175000.0 | nM | - |
| CHEMBL4210386 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4203545 | — | IC50 | = | 116100.0 | nM | - |
| CHEMBL4207716 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4216676 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4218669 | — | IC50 | > | 200000.0 | nM | - |