Assay Detail
Binding
CHEMBL762819
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Inhibitory activity against phosphodiesterase 5 from human platelets
75
Total Activities
75
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 75 | 6.04 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539033 | — | — | 1 | 9.28 |
| CHEMBL545518 | — | — | 1 | 8.64 |
| CHEMBL557022 | — | — | 1 | 8.59 |
| CHEMBL539806 | — | — | 1 | 8.55 |
| CHEMBL544347 | — | — | 1 | 8.00 |
| CHEMBL555218 | — | — | 1 | 7.85 |
| CHEMBL555463 | — | — | 1 | 7.80 |
| CHEMBL544816 | — | — | 1 | 7.58 |
| CHEMBL542707 | — | — | 1 | 7.14 |
| CHEMBL538031 | — | — | 1 | 6.98 |
| CHEMBL554051 | — | — | 1 | 6.96 |
| CHEMBL553819 | — | — | 1 | 6.92 |
| CHEMBL545749 | — | — | 1 | 6.78 |
| CHEMBL116818 | — | — | 1 | 6.72 |
| CHEMBL117583 | — | — | 1 | 6.68 |
| CHEMBL554946 | — | — | 1 | 6.64 |
| CHEMBL118944 | — | — | 1 | 6.58 |
| CHEMBL118462 | — | — | 1 | 6.51 |
| CHEMBL72650 | — | — | 1 | 6.50 |
| CHEMBL541847 | — | — | 1 | 6.44 |
| CHEMBL118812 | — | — | 1 | 6.38 |
| CHEMBL119841 | — | — | 1 | 6.35 |
| CHEMBL555184 | — | — | 1 | 6.32 |
| CHEMBL544818 | — | — | 1 | 6.27 |
| CHEMBL540318 | — | — | 1 | 6.20 |
| CHEMBL117108 | — | — | 1 | 6.14 |
| CHEMBL118781 | — | — | 1 | 6.13 |
| CHEMBL541845 | — | — | 1 | 6.12 |
| CHEMBL333093 | — | — | 1 | 6.10 |
| CHEMBL118717 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539033 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL545518 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL557022 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL539806 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL544347 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL555218 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL555463 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL544816 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL542707 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL538031 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL554051 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL553819 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL545749 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL116818 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL117583 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL554946 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL118944 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL118462 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL72650 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL541847 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL118812 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL119841 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL555184 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL544818 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL540318 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL117108 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL118781 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL541845 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL333093 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL118717 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL120099 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL555171 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL553820 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL118376 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL118481 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL116890 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL332732 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL341679 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL544348 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL117509 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL118538 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL544584 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL118217 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL119506 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL118415 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL118209 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL545523 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL552952 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL119309 | — | IC50 | = | 3600.0 | nM | 5.44 |