Assay Detail
Binding
CHEMBL984533
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Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells
18
Total Activities
18
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 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.68 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499477 | — | — | 1 | 10.22 |
| CHEMBL514564 | — | — | 1 | 9.77 |
| CHEMBL519193 | — | — | 1 | 9.47 |
| CHEMBL464804 | — | — | 1 | 9.43 |
| CHEMBL456171 | — | — | 1 | 9.35 |
| CHEMBL484753 | — | — | 1 | 9.21 |
| CHEMBL485547 | — | — | 1 | 9.12 |
| CHEMBL372575 | — | — | 1 | 8.85 |
| CHEMBL456808 | — | — | 1 | 8.81 |
| CHEMBL464600 | — | — | 1 | 8.45 |
| CHEMBL485620 | — | — | 1 | 8.21 |
| CHEMBL485629 | MK-0873 | 2.0 | 1 | 8.17 |
| CHEMBL456172 | — | — | 1 | 8.04 |
| CHEMBL456173 | — | — | 1 | 7.82 |
| CHEMBL511368 | — | — | 1 | 7.18 |
| CHEMBL464803 | — | — | 1 | 6.85 |
| CHEMBL464802 | — | — | 1 | - |
| CHEMBL458106 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499477 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL514564 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL519193 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL464804 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL456171 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL484753 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL485547 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL372575 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL456808 | — | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL464600 | — | IC50 | = | 3.54 | nM | 8.45 |
| CHEMBL485620 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL485629 | MK-0873 | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL456172 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL456173 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL511368 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL464803 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL464802 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL458106 | — | IC50 | > | 1000.0 | nM | - |