Assay Detail
Binding
CHEMBL822071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 5.57 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302299 | — | — | 1 | 6.44 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 6.35 |
| CHEMBL67239 | — | — | 1 | 6.28 |
| CHEMBL932 | DIPYRIDAMOLE | 4.0 | 1 | 6.28 |
| CHEMBL332624 | — | — | 1 | 6.19 |
| CHEMBL331407 | — | — | 1 | 6.11 |
| CHEMBL125435 | — | — | 1 | 6.00 |
| CHEMBL63637 | — | — | 1 | 6.00 |
| CHEMBL126177 | — | — | 1 | 5.89 |
| CHEMBL125164 | — | — | 1 | 5.89 |
| CHEMBL1794860 | — | — | 1 | 5.83 |
| CHEMBL125394 | — | — | 1 | 5.82 |
| CHEMBL123846 | — | — | 1 | 5.82 |
| CHEMBL267475 | FPL-55712 | — | 1 | 5.80 |
| CHEMBL338642 | — | — | 1 | 5.77 |
| CHEMBL332898 | — | — | 1 | 5.75 |
| CHEMBL125992 | — | — | 1 | 5.72 |
| CHEMBL339775 | — | — | 1 | 5.70 |
| CHEMBL123364 | — | — | 1 | 5.70 |
| CHEMBL122909 | — | — | 1 | 5.66 |
| CHEMBL125066 | — | — | 1 | 5.46 |
| CHEMBL122093 | — | — | 1 | 5.40 |
| CHEMBL124544 | — | — | 1 | 5.34 |
| CHEMBL331434 | — | — | 1 | 5.26 |
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 5.06 |
| CHEMBL338276 | — | — | 1 | 5.05 |
| CHEMBL124393 | — | — | 1 | 5.02 |
| CHEMBL121775 | — | — | 1 | 4.96 |
| CHEMBL122059 | — | — | 1 | 4.96 |
| CHEMBL125714 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302299 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL67239 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL932 | DIPYRIDAMOLE | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL332624 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL331407 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL125435 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL63637 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL126177 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL125164 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1794860 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL125394 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL123846 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL267475 | FPL-55712 | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL338642 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL332898 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL125992 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL339775 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL123364 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL122909 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL125066 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL122093 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL124544 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL331434 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL19224 | PAPAVERINE | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL338276 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL124393 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL121775 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL122059 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL125714 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL340289 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL341475 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL124539 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL125163 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125373 | — | IC50 | > | 100000.0 | nM | - |