Assay Detail
ADMET
CHEMBL4397441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human PDE6C expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (CHEMBL3977) ↗| 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 | 3 | 7.18 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4462192 | — | — | 1 | 7.70 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 7.44 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4462192 | — | IC50 | = | 19.8 | nM | 7.70 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 36.42 | nM | 7.44 |
| CHEMBL779 | TADALAFIL | IC50 | = | 402.0 | nM | 6.40 |