Assay Detail
Binding
CHEMBL5153773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE5 using [3H]cGMP as substrate incubated for 10 mins by liquid scintillation counter analysis
31
Total Activities
31
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
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Computational design, synthesis and biological evaluation of PDE5 inhibitors based on N<sup>2</sup>,N<sup>4</sup>-diaminoquinazoline and N<sup>2</sup>,N<sup>6</sup>-diaminopurine scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.80 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.85 |
| CHEMBL4445920 | — | — | 1 | 7.00 |
| CHEMBL5175706 | — | — | 1 | 6.82 |
| CHEMBL5178863 | — | — | 1 | 6.66 |
| CHEMBL5194921 | — | — | 1 | 6.54 |
| CHEMBL5187496 | — | — | 1 | 6.44 |
| CHEMBL5194783 | — | — | 1 | 6.39 |
| CHEMBL5184989 | — | — | 1 | 6.37 |
| CHEMBL5203939 | — | — | 1 | 6.31 |
| CHEMBL5186856 | — | — | 1 | 6.30 |
| CHEMBL5195499 | — | — | 1 | 6.28 |
| CHEMBL5191104 | — | — | 1 | 6.22 |
| CHEMBL5200202 | — | — | 1 | 5.99 |
| CHEMBL5199387 | — | — | 1 | 5.84 |
| CHEMBL5188731 | — | — | 1 | 5.79 |
| CHEMBL5177893 | — | — | 1 | 5.70 |
| CHEMBL5195434 | — | — | 1 | 5.47 |
| CHEMBL5171693 | — | — | 1 | 5.40 |
| CHEMBL5183230 | — | — | 1 | 5.35 |
| CHEMBL5208363 | — | — | 1 | 5.28 |
| CHEMBL5193660 | — | — | 1 | 5.28 |
| CHEMBL5196307 | — | — | 1 | 5.03 |
| CHEMBL5183757 | — | — | 1 | 4.72 |
| CHEMBL5206939 | — | — | 1 | 4.64 |
| CHEMBL5195857 | — | — | 1 | 4.54 |
| CHEMBL5193806 | — | — | 1 | 4.48 |
| CHEMBL5188011 | — | — | 1 | 4.42 |
| CHEMBL5200266 | — | — | 1 | 4.37 |
| CHEMBL5170729 | — | — | 1 | - |
| CHEMBL5191329 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4445920 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5175706 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5178863 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL5194921 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5187496 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5194783 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5184989 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5203939 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5186856 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5195499 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5191104 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5200202 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL5199387 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL5188731 | — | IC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL5177893 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5195434 | — | IC50 | = | 3410.0 | nM | 5.47 |
| CHEMBL5171693 | — | IC50 | = | 3970.0 | nM | 5.40 |
| CHEMBL5183230 | — | IC50 | = | 4460.0 | nM | 5.35 |
| CHEMBL5208363 | — | IC50 | = | 5230.0 | nM | 5.28 |
| CHEMBL5193660 | — | IC50 | = | 5280.0 | nM | 5.28 |
| CHEMBL5196307 | — | IC50 | = | 9390.0 | nM | 5.03 |
| CHEMBL5183757 | — | IC50 | = | 18880.0 | nM | 4.72 |
| CHEMBL5206939 | — | IC50 | = | 23010.0 | nM | 4.64 |
| CHEMBL5195857 | — | IC50 | = | 28540.0 | nM | 4.54 |
| CHEMBL5193806 | — | IC50 | = | 33260.0 | nM | 4.48 |
| CHEMBL5188011 | — | IC50 | = | 38370.0 | nM | 4.42 |
| CHEMBL5200266 | — | IC50 | = | 43160.0 | nM | 4.37 |
| CHEMBL5170729 | — | IC50 | - | — | - | |
| CHEMBL5191329 | — | IC50 | - | — | - | |
| CHEMBL5180347 | — | IC50 | - | — | - |