Assay Detail
Binding
CHEMBL2161156
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Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.79 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158056 | — | — | 1 | 7.96 |
| CHEMBL1232082 | — | — | 1 | 7.66 |
| CHEMBL74078 | — | — | 1 | 7.54 |
| CHEMBL77826 | — | — | 1 | 6.54 |
| CHEMBL315815 | PYRIDOPYRIDAZINONE | — | 1 | 6.47 |
| CHEMBL2158057 | — | — | 1 | 6.47 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 6.26 |
| CHEMBL2158064 | — | — | 1 | 6.14 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.08 |
| CHEMBL2158061 | — | — | 1 | 6.00 |
| CHEMBL19449 | IBUDILAST | 4.0 | 1 | 5.89 |
| CHEMBL356323 | CIPAMFYLLINE | 2.0 | 1 | 5.80 |
| CHEMBL2158062 | — | — | 1 | 5.62 |
| CHEMBL2158063 | — | — | 1 | 5.37 |
| CHEMBL18701 | RO-201724 | — | 1 | 5.37 |
| CHEMBL325795 | S-ROLIPRAM | — | 1 | 5.37 |
| CHEMBL2158070 | — | — | 1 | 5.27 |
| CHEMBL2158068 | — | — | 1 | 5.21 |
| CHEMBL2158067 | — | — | 1 | 5.19 |
| CHEMBL2158003 | — | — | 1 | 5.19 |
| CHEMBL2158069 | — | — | 1 | 5.09 |
| CHEMBL2158059 | — | — | 1 | 4.92 |
| CHEMBL2158060 | — | — | 1 | 4.62 |
| CHEMBL2158065 | — | — | 1 | 4.42 |
| CHEMBL2158066 | — | — | 1 | 4.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158056 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1232082 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL74078 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL77826 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL315815 | PYRIDOPYRIDAZINONE | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2158057 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL2158064 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL2158061 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL19449 | IBUDILAST | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL356323 | CIPAMFYLLINE | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2158062 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2158063 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL18701 | RO-201724 | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL325795 | S-ROLIPRAM | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2158070 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL2158068 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL2158067 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2158003 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2158069 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL2158059 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2158060 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL2158065 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL2158066 | — | IC50 | = | 44000.0 | nM | 4.36 |