Assay Detail
Binding
CHEMBL3374901
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Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF 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 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel Roflumilast analogs as soft PDE4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.51 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.40 |
| CHEMBL3327321 | — | — | 1 | 8.74 |
| CHEMBL3327323 | — | — | 1 | 8.40 |
| CHEMBL3327325 | — | — | 1 | 8.33 |
| CHEMBL3327315 | — | — | 1 | 8.27 |
| CHEMBL3327322 | — | — | 1 | 8.26 |
| CHEMBL3327326 | — | — | 1 | 8.06 |
| CHEMBL3327317 | — | — | 1 | 7.96 |
| CHEMBL3327316 | — | — | 1 | 7.92 |
| CHEMBL3327328 | — | — | 1 | 7.68 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 7.28 |
| CHEMBL3327327 | — | — | 1 | 7.06 |
| CHEMBL3327324 | — | — | 1 | 6.75 |
| CHEMBL3327318 | — | — | 1 | 6.13 |
| CHEMBL3327329 | — | — | 1 | 6.04 |
| CHEMBL3327319 | — | — | 1 | 5.77 |
| CHEMBL3327320 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3327321 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3327323 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3327325 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3327315 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3327322 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3327326 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL3327317 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3327316 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3327328 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3327327 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3327324 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3327318 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3327329 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3327319 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3327320 | — | IC50 | = | 2700.0 | nM | 5.57 |