Assay Detail
Binding
CHEMBL2390132
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE4B (152 to 564 amino acids) using cAMP as substrate after 30 mins by plate reader analysis
28
Total Activities
28
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 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.99 | 9.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.31 |
| CHEMBL2385759 | — | — | 1 | 8.33 |
| CHEMBL2385757 | — | — | 1 | 8.18 |
| CHEMBL2385755 | — | — | 1 | 8.12 |
| CHEMBL2385758 | — | — | 1 | 7.96 |
| CHEMBL2385753 | — | — | 1 | 7.80 |
| CHEMBL2385756 | — | — | 1 | 7.66 |
| CHEMBL2385749 | — | — | 1 | 7.60 |
| CHEMBL2385754 | — | — | 1 | 7.57 |
| CHEMBL2385750 | — | — | 1 | 7.55 |
| CHEMBL2385559 | — | — | 1 | 7.54 |
| CHEMBL2385573 | — | — | 1 | 7.54 |
| CHEMBL2385761 | — | — | 1 | 7.48 |
| CHEMBL2385760 | — | — | 1 | 7.37 |
| CHEMBL2385563 | — | — | 1 | 6.85 |
| CHEMBL2385558 | — | — | 1 | 6.82 |
| CHEMBL2385560 | — | — | 1 | 6.72 |
| CHEMBL2385572 | — | — | 1 | 6.64 |
| CHEMBL2385751 | — | — | 1 | 6.55 |
| CHEMBL2385567 | — | — | 1 | 6.37 |
| CHEMBL2385570 | — | — | 1 | 6.32 |
| CHEMBL2385566 | — | — | 1 | 6.21 |
| CHEMBL2385565 | — | — | 1 | 6.10 |
| CHEMBL2385569 | — | — | 1 | 5.66 |
| CHEMBL2385564 | — | — | 1 | 5.60 |
| CHEMBL2385562 | — | — | 1 | 5.52 |
| CHEMBL2385561 | — | — | 1 | 5.30 |
| CHEMBL2385752 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.49 | nM | 9.31 |
| CHEMBL2385759 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2385757 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2385755 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL2385758 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2385753 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2385756 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2385749 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2385754 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2385750 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2385559 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2385573 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2385761 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2385760 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2385563 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2385558 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2385560 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2385572 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2385751 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2385567 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2385570 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2385566 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2385565 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL2385569 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2385564 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2385562 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2385561 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2385752 | — | IC50 | = | 7900.0 | nM | 5.10 |