Assay Detail
Binding
CHEMBL5638042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of his-tagged recombinant human PDE4D catalytic domain (T86 to S413 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as substrate incubated for 10 mins by SPA assay
13
Total Activities
13
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 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Drug repurposing and structure-based discovery of new PDE4 and PDE5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.33 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.41 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.49 |
| CHEMBL1316965 | ETHAVERINE HYDROCHLORIDE | -1.0 | 1 | 6.39 |
| CHEMBL80713 | — | — | 1 | 6.38 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.34 |
| CHEMBL5646602 | — | — | 1 | 6.03 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 6.00 |
| CHEMBL562318 | MARDEPODECT | 2.0 | 1 | 5.76 |
| CHEMBL5647232 | — | — | 1 | 5.75 |
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 5.75 |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | 5.68 |
| CHEMBL5639763 | — | — | 1 | 5.65 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL514800 | APREMILAST | IC50 | = | 32.44 | nM | 7.49 |
| CHEMBL1316965 | ETHAVERINE HYDROCHLORIDE | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL80713 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5646602 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL562318 | MARDEPODECT | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL5647232 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL1236962 | OMIPALISIB | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL388590 | BENZBROMARONE | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5639763 | — | IC50 | = | 2250.0 | nM | 5.65 |
| CHEMBL460702 | BMS-777607 | IC50 | = | 2460.0 | nM | 5.61 |