Assay Detail
Binding
CHEMBL765478
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells.
18
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.95 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL323312 | — | — | 5 | 8.89 |
| CHEMBL408345 | — | — | 1 | 8.57 |
| CHEMBL286224 | — | — | 1 | 8.38 |
| CHEMBL32442 | CDP840 | — | 1 | 8.38 |
| CHEMBL103635 | — | — | 1 | 8.36 |
| CHEMBL105164 | — | — | 1 | 7.75 |
| CHEMBL103859 | — | — | 1 | 7.57 |
| CHEMBL102718 | — | — | 1 | 7.50 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.42 |
| CHEMBL105243 | — | — | 1 | 7.42 |
| CHEMBL102784 | — | — | 2 | 7.41 |
| CHEMBL319858 | — | — | 1 | 7.38 |
| CHEMBL318108 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL323312 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL323312 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL323312 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL408345 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL32442 | CDP840 | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL323312 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL286224 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL103635 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL105164 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL323312 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL103859 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL102718 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL105243 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL102784 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL102784 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL319858 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL318108 | — | IC50 | = | 57.0 | nM | 7.24 |