Assay Detail
Binding
CHEMBL4200907
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE5A1 catalytic domain (535 to 860 residues) expressed in Escherichia coli BL21 using 3H-cGMP as substrate after 15 mins by liquid scintillation counting
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 | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.65 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218772 | — | — | 1 | 9.49 |
| CHEMBL4204687 | — | — | 1 | 9.41 |
| CHEMBL4217826 | — | — | 1 | 9.28 |
| CHEMBL4209550 | — | — | 1 | 9.10 |
| CHEMBL4215845 | — | — | 1 | 8.98 |
| CHEMBL4206819 | — | — | 1 | 8.85 |
| CHEMBL4209964 | — | — | 1 | 8.80 |
| CHEMBL4214877 | — | — | 1 | 8.79 |
| CHEMBL4218349 | — | — | 1 | 8.68 |
| CHEMBL4206105 | — | — | 1 | 8.62 |
| CHEMBL4205598 | — | — | 1 | 8.62 |
| CHEMBL4210468 | — | — | 1 | 8.58 |
| CHEMBL4214882 | — | — | 1 | 8.58 |
| CHEMBL4209958 | — | — | 1 | 8.52 |
| CHEMBL4202694 | — | — | 1 | 8.42 |
| CHEMBL4207041 | — | — | 1 | 8.39 |
| CHEMBL4206520 | — | — | 1 | 8.36 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.29 |
| CHEMBL4218777 | — | — | 1 | 8.17 |
| CHEMBL4214353 | — | — | 1 | 8.02 |
| CHEMBL4210889 | — | — | 1 | 7.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218772 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4204687 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL4217826 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL4209550 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4215845 | — | IC50 | = | 1.05 | nM | 8.98 |
| CHEMBL4206819 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL4209964 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4214877 | — | IC50 | = | 1.63 | nM | 8.79 |
| CHEMBL4218349 | — | IC50 | = | 2.09 | nM | 8.68 |
| CHEMBL4206105 | — | IC50 | = | 2.37 | nM | 8.62 |
| CHEMBL4205598 | — | IC50 | = | 2.38 | nM | 8.62 |
| CHEMBL4210468 | — | IC50 | = | 2.64 | nM | 8.58 |
| CHEMBL4214882 | — | IC50 | = | 2.64 | nM | 8.58 |
| CHEMBL4209958 | — | IC50 | = | 3.04 | nM | 8.52 |
| CHEMBL4202694 | — | IC50 | = | 3.82 | nM | 8.42 |
| CHEMBL4207041 | — | IC50 | = | 4.03 | nM | 8.39 |
| CHEMBL4206520 | — | IC50 | = | 4.38 | nM | 8.36 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4218777 | — | IC50 | = | 6.82 | nM | 8.17 |
| CHEMBL4214353 | — | IC50 | = | 9.63 | nM | 8.02 |
| CHEMBL4210889 | — | IC50 | = | 17.0 | nM | 7.77 |