Assay Detail
Binding
CHEMBL2340160
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30 mins by colorimetric assay method
11
Total Activities
11
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
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.65 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.10 |
| CHEMBL2335411 | — | — | 1 | 6.63 |
| CHEMBL2335415 | — | — | 1 | 6.58 |
| CHEMBL2335414 | — | — | 1 | 6.57 |
| CHEMBL2335413 | — | — | 1 | 6.56 |
| CHEMBL2335412 | — | — | 1 | 6.55 |
| CHEMBL2335410 | — | — | 1 | 6.41 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 6.30 |
| CHEMBL82318 | — | — | 1 | 6.28 |
| CHEMBL2335409 | — | — | 1 | 6.22 |
| CHEMBL2335408 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2335411 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL2335415 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL2335414 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL2335413 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL2335412 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL2335410 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL82318 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2335409 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL2335408 | — | IC50 | = | 1093.0 | nM | 5.96 |