Assay Detail
Binding
CHEMBL4397429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.85 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4455533 | — | — | 1 | 9.27 |
| CHEMBL4462192 | — | — | 1 | 9.21 |
| CHEMBL4474634 | — | — | 1 | 9.10 |
| CHEMBL4444940 | — | — | 1 | 9.08 |
| CHEMBL4467125 | — | — | 1 | 9.04 |
| CHEMBL4468620 | — | — | 1 | 9.00 |
| CHEMBL4559488 | — | — | 1 | 8.92 |
| CHEMBL4483406 | — | — | 1 | 8.91 |
| CHEMBL4572238 | — | — | 1 | 8.84 |
| CHEMBL4435186 | — | — | 1 | 8.81 |
| CHEMBL2180945 | — | — | 1 | 8.80 |
| CHEMBL4455861 | — | — | 1 | 8.79 |
| CHEMBL4440789 | — | — | 1 | 8.77 |
| CHEMBL4582221 | — | — | 1 | 8.73 |
| CHEMBL4539785 | — | — | 1 | 8.70 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 8.63 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.37 |
| CHEMBL4522391 | — | — | 1 | 8.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4455533 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4462192 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4474634 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4444940 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL4467125 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL4468620 | — | IC50 | = | 1.01 | nM | 9.00 |
| CHEMBL4559488 | — | IC50 | = | 1.21 | nM | 8.92 |
| CHEMBL4483406 | — | IC50 | = | 1.23 | nM | 8.91 |
| CHEMBL4572238 | — | IC50 | = | 1.46 | nM | 8.84 |
| CHEMBL4435186 | — | IC50 | = | 1.55 | nM | 8.81 |
| CHEMBL2180945 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4455861 | — | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL4440789 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL4582221 | — | IC50 | = | 1.86 | nM | 8.73 |
| CHEMBL4539785 | — | IC50 | = | 2.02 | nM | 8.70 |
| CHEMBL779 | TADALAFIL | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 4.31 | nM | 8.37 |
| CHEMBL4522391 | — | IC50 | = | 5.33 | nM | 8.27 |