Assay Detail
Binding
CHEMBL4198913
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human recombinant N-terminal GST-tagged PDE5A1 expressed in baculovirus infected sf9 cells using cGMP as substrate after 30 mins by fluorescence assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.76 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4216635 | — | — | 1 | 9.00 |
| CHEMBL4209220 | — | — | 1 | 8.70 |
| CHEMBL4203481 | — | — | 1 | 8.70 |
| CHEMBL4217166 | — | — | 1 | 8.52 |
| CHEMBL4214135 | — | — | 1 | 8.52 |
| CHEMBL4214699 | — | — | 1 | 8.52 |
| CHEMBL4202521 | — | — | 1 | 8.15 |
| CHEMBL4212445 | — | — | 1 | 8.00 |
| CHEMBL4204952 | — | — | 1 | 8.00 |
| CHEMBL4212186 | — | — | 1 | 7.96 |
| CHEMBL4213615 | — | — | 1 | 7.89 |
| CHEMBL4210653 | — | — | 1 | 7.85 |
| CHEMBL4212866 | — | — | 1 | 7.82 |
| CHEMBL4207538 | — | — | 1 | 7.70 |
| CHEMBL4207409 | — | — | 1 | 7.57 |
| CHEMBL4209025 | — | — | 1 | 7.51 |
| CHEMBL4218554 | — | — | 1 | 7.44 |
| CHEMBL4216348 | — | — | 1 | 7.33 |
| CHEMBL4217821 | — | — | 1 | 7.32 |
| CHEMBL4206296 | — | — | 1 | 7.28 |
| CHEMBL4207836 | — | — | 1 | 7.10 |
| CHEMBL4205788 | — | — | 1 | 6.84 |
| CHEMBL4204679 | — | — | 1 | 6.84 |
| CHEMBL4204146 | — | — | 1 | 6.83 |
| CHEMBL4217999 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4216635 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4209220 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4203481 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4217166 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4214135 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4214699 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4202521 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4212445 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4204952 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4212186 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4213615 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4210653 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4212866 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4207538 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4207409 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4209025 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4218554 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4216348 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4217821 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4206296 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4207836 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4205788 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4204679 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4204146 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4217999 | — | IC50 | = | 190.0 | nM | 6.72 |