Assay Detail
Binding
CHEMBL763044
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Inhibition of recombinant human PDE4A expressed in Sf9 cells
13
Total Activities
13
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 | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.18 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL127944 | — | — | 1 | 10.15 |
| CHEMBL339083 | — | — | 1 | 9.70 |
| CHEMBL419236 | — | — | 1 | 9.40 |
| CHEMBL318502 | — | — | 1 | 9.22 |
| CHEMBL127994 | — | — | 1 | 8.57 |
| CHEMBL127201 | — | — | 1 | 8.48 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.40 |
| CHEMBL419416 | — | — | 1 | 8.05 |
| CHEMBL123576 | — | — | 1 | 7.82 |
| CHEMBL124575 | — | — | 1 | 7.55 |
| CHEMBL126587 | — | — | 1 | 7.46 |
| CHEMBL340379 | — | — | 1 | 6.60 |
| CHEMBL32442 | CDP840 | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL127944 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL339083 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL419236 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL318502 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL127994 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL127201 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL419416 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL123576 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL124575 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL126587 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL340379 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL32442 | CDP840 | IC50 | = | 10000.0 | nM | 5.00 |