Assay Detail
Binding
CHEMBL827930
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Inhibition of human Phosphodiesterase 5 (n=2-3)
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 | Expert |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.71 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 7.70 |
| CHEMBL194081 | — | — | 1 | 7.52 |
| CHEMBL196241 | — | — | 1 | 7.47 |
| CHEMBL196289 | — | — | 1 | 7.41 |
| CHEMBL193746 | — | — | 1 | 7.23 |
| CHEMBL196830 | — | — | 1 | 7.17 |
| CHEMBL372476 | — | — | 1 | 7.12 |
| CHEMBL195584 | — | — | 1 | 7.09 |
| CHEMBL371793 | — | — | 1 | 7.09 |
| CHEMBL193428 | — | — | 1 | 7.05 |
| CHEMBL365943 | — | — | 1 | 7.00 |
| CHEMBL364045 | — | — | 1 | 7.00 |
| CHEMBL382494 | — | — | 1 | 6.80 |
| CHEMBL371451 | — | — | 1 | 6.75 |
| CHEMBL363638 | — | — | 1 | 6.64 |
| CHEMBL193363 | — | — | 1 | 6.57 |
| CHEMBL439862 | — | — | 1 | 6.50 |
| CHEMBL195768 | — | — | 1 | 6.46 |
| CHEMBL195830 | — | — | 1 | 6.37 |
| CHEMBL193995 | — | — | 1 | 6.35 |
| CHEMBL195603 | — | — | 1 | 6.04 |
| CHEMBL195282 | — | — | 1 | 6.01 |
| CHEMBL196493 | — | — | 1 | 5.96 |
| CHEMBL197153 | — | — | 1 | 5.51 |
| CHEMBL364091 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL194081 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL196241 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL196289 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL193746 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL196830 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL372476 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL195584 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL371793 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL193428 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL365943 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL364045 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL382494 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL371451 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL363638 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL193363 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL439862 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL195768 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL195830 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL193995 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL195603 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL195282 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL196493 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL197153 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL364091 | — | IC50 | = | 13000.0 | nM | 4.89 |