Assay Detail
Binding
CHEMBL1833211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE4A4 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.26 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1830646 | — | — | 1 | 9.52 |
| CHEMBL1830643 | — | — | 1 | 9.30 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.23 |
| CHEMBL1828652 | — | — | 1 | 9.05 |
| CHEMBL1830638 | — | — | 1 | 8.32 |
| CHEMBL1830641 | — | — | 1 | 8.30 |
| CHEMBL1830644 | — | — | 1 | 8.30 |
| CHEMBL1830790 | — | — | 1 | 8.21 |
| CHEMBL1830636 | — | — | 1 | 7.79 |
| CHEMBL1830635 | — | — | 1 | 7.70 |
| CHEMBL1830647 | — | — | 1 | 7.66 |
| CHEMBL1830642 | — | — | 1 | 7.55 |
| CHEMBL1830640 | — | — | 1 | 7.44 |
| CHEMBL1830645 | — | — | 1 | 7.21 |
| CHEMBL1830639 | — | — | 1 | - |
| CHEMBL1830637 | — | — | 1 | - |
| CHEMBL1830634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1830646 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1830643 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL1828652 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1830638 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1830641 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1830644 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1830790 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1830636 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL1830635 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1830647 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1830642 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1830640 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1830645 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1830639 | — | IC50 | - | — | - | |
| CHEMBL1830637 | — | IC50 | - | — | - | |
| CHEMBL1830634 | — | IC50 | - | — | - |