Assay Detail
Binding
CHEMBL4372113
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat lung PDE5 using [3H]cGMP as substrate measured after 10 mins by scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL4567) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Design, synthesis and evaluation of N<sup>2</sup>,N<sup>4</sup>-diaminoquinazoline based inhibitors of phosphodiesterase type 5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.49 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.70 |
| CHEMBL4445920 | — | — | 1 | 7.14 |
| CHEMBL4570769 | — | — | 1 | 7.05 |
| CHEMBL4529354 | — | — | 1 | 6.94 |
| CHEMBL4434898 | — | — | 1 | 6.75 |
| CHEMBL4544782 | — | — | 1 | 6.66 |
| CHEMBL4460740 | — | — | 1 | 6.65 |
| CHEMBL4540726 | — | — | 1 | 6.55 |
| CHEMBL4516390 | — | — | 1 | 6.54 |
| CHEMBL4452377 | — | — | 1 | 6.46 |
| CHEMBL4526365 | — | — | 1 | 6.35 |
| CHEMBL4534674 | — | — | 1 | 6.29 |
| CHEMBL4453311 | — | — | 1 | 6.28 |
| CHEMBL4450878 | — | — | 1 | 6.26 |
| CHEMBL4567109 | — | — | 1 | 6.11 |
| CHEMBL4558761 | — | — | 1 | 6.02 |
| CHEMBL4469064 | — | — | 1 | 5.90 |
| CHEMBL597248 | — | — | 1 | 5.86 |
| CHEMBL4525521 | — | — | 1 | 5.84 |
| CHEMBL4552918 | — | — | 1 | 5.43 |
| CHEMBL4565213 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL192 | SILDENAFIL | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4445920 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4570769 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4529354 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4434898 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4544782 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL4460740 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL4540726 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL4516390 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4452377 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4526365 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL4534674 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL4453311 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL4450878 | — | IC50 | = | 555.0 | nM | 6.26 |
| CHEMBL4567109 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL4558761 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL4469064 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL597248 | — | IC50 | = | 1376.0 | nM | 5.86 |
| CHEMBL4525521 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL4552918 | — | IC50 | = | 3706.0 | nM | 5.43 |
| CHEMBL4565213 | — | IC50 | > | 10000.0 | nM | - |