Assay Detail
Binding
CHEMBL765476
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Inhibitory activity against human PDE4A expressed isoform using construct representing the common region of spliced variants as GST-fusion protein in Sf9 cells.
24
Total Activities
22
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 aminopyridines as potent and selective phosphodiesterase-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.41 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL165889 | — | — | 1 | 9.52 |
| CHEMBL165687 | — | — | 1 | 9.22 |
| CHEMBL162485 | — | — | 1 | 9.10 |
| CHEMBL351187 | — | — | 3 | 9.10 |
| CHEMBL354931 | — | — | 1 | 8.92 |
| CHEMBL349635 | — | — | 1 | 8.92 |
| CHEMBL323312 | — | — | 1 | 8.89 |
| CHEMBL444865 | — | — | 1 | 8.82 |
| CHEMBL166299 | — | — | 1 | 8.77 |
| CHEMBL164564 | — | — | 1 | 8.64 |
| CHEMBL164199 | — | — | 1 | 8.64 |
| CHEMBL286224 | — | — | 1 | 8.38 |
| CHEMBL351007 | — | — | 1 | 8.24 |
| CHEMBL423252 | — | — | 1 | 8.11 |
| CHEMBL166245 | — | — | 1 | 8.08 |
| CHEMBL166297 | — | — | 1 | 8.03 |
| CHEMBL163311 | — | — | 1 | 7.92 |
| CHEMBL162870 | — | — | 1 | 7.80 |
| CHEMBL350627 | — | — | 1 | 7.75 |
| CHEMBL164800 | — | — | 1 | 7.51 |
| CHEMBL165298 | — | — | 1 | 7.51 |
| CHEMBL165773 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL165889 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL165687 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL162485 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL351187 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL354931 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL349635 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL323312 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL444865 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL351187 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL166299 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL164199 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL164564 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL286224 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL351007 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL423252 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL166245 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL166297 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL163311 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL162870 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL350627 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL351187 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL164800 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL165298 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL165773 | — | IC50 | = | 33.0 | nM | 7.48 |