Assay Detail
Binding
CHEMBL855487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE4A
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.22 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 8.40 |
| CHEMBL218103 | — | — | 1 | 7.96 |
| CHEMBL217899 | TOFIMILAST | 2.0 | 1 | 7.64 |
| CHEMBL218653 | — | — | 1 | 7.46 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 6.82 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 6.79 |
| CHEMBL218990 | — | — | 1 | 6.60 |
| CHEMBL218793 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL218103 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL217899 | TOFIMILAST | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL218653 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL218990 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL218793 | — | IC50 | = | 770.0 | nM | 6.11 |