Assay Detail
Binding
CHEMBL871523
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Inhibition of PDE5
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.92 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378542 | — | — | 1 | 8.08 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 7.70 |
| CHEMBL213060 | — | — | 1 | 7.64 |
| CHEMBL213219 | — | — | 1 | 7.42 |
| CHEMBL438451 | — | — | 1 | 7.40 |
| CHEMBL377563 | — | — | 1 | 7.30 |
| CHEMBL378255 | — | — | 1 | 7.15 |
| CHEMBL215699 | — | — | 1 | 7.10 |
| CHEMBL215756 | — | — | 1 | 7.02 |
| CHEMBL215465 | — | — | 1 | 7.00 |
| CHEMBL377850 | — | — | 1 | 7.00 |
| CHEMBL213113 | — | — | 1 | 6.85 |
| CHEMBL382494 | — | — | 1 | 6.80 |
| CHEMBL213425 | — | — | 1 | 6.75 |
| CHEMBL215700 | — | — | 1 | 6.66 |
| CHEMBL213099 | — | — | 1 | 6.62 |
| CHEMBL213094 | — | — | 1 | 6.43 |
| CHEMBL385683 | — | — | 1 | 6.41 |
| CHEMBL212397 | — | — | 1 | 6.33 |
| CHEMBL377144 | — | — | 1 | 5.85 |
| CHEMBL213265 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378542 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL213060 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL213219 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL438451 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL377563 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL378255 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL215699 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL215756 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL215465 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL377850 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL213113 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL382494 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL213425 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL215700 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL213099 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL213094 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL385683 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL212397 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL377144 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL213265 | — | IC50 | = | 1500.0 | nM | 5.82 |