Assay Detail
Binding
CHEMBL831692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human phosphodiesterase 5
35
Total Activities
35
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
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.71 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1520 | VARDENAFIL | 4.0 | 1 | 9.70 |
| CHEMBL193989 | — | — | 1 | 8.64 |
| CHEMBL373102 | — | — | 1 | 8.60 |
| CHEMBL365358 | — | — | 1 | 8.48 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.46 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 8.40 |
| CHEMBL283562 | — | — | 1 | 8.35 |
| CHEMBL365944 | — | — | 1 | 8.28 |
| CHEMBL362938 | — | — | 1 | 8.19 |
| CHEMBL370413 | — | — | 1 | 8.11 |
| CHEMBL197049 | — | — | 1 | 7.85 |
| CHEMBL194341 | — | — | 1 | 7.82 |
| CHEMBL446663 | — | — | 1 | 7.72 |
| CHEMBL193855 | — | — | 1 | 7.70 |
| CHEMBL370241 | — | — | 1 | 7.66 |
| CHEMBL363411 | — | — | 1 | 7.64 |
| CHEMBL372427 | — | — | 1 | 7.55 |
| CHEMBL370118 | — | — | 1 | 7.55 |
| CHEMBL193603 | — | — | 1 | 7.54 |
| CHEMBL372917 | — | — | 1 | 7.50 |
| CHEMBL439673 | — | — | 1 | 7.48 |
| CHEMBL193645 | — | — | 1 | 7.48 |
| CHEMBL372955 | — | — | 1 | 7.46 |
| CHEMBL194056 | — | — | 1 | 7.42 |
| CHEMBL365591 | — | — | 1 | 7.40 |
| CHEMBL194511 | — | — | 1 | 7.40 |
| CHEMBL373320 | — | — | 1 | 7.32 |
| CHEMBL435502 | — | — | 1 | 7.22 |
| CHEMBL364459 | — | — | 1 | 7.22 |
| CHEMBL193364 | — | — | 1 | 7.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1520 | VARDENAFIL | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL193989 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL373102 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL365358 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL779 | TADALAFIL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL283562 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL365944 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL362938 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL370413 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL197049 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL194341 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL446663 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL193855 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL370241 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL363411 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL370118 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL372427 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL193603 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL372917 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL439673 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL193645 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL372955 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL194056 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL365591 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL194511 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL373320 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL435502 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL364459 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL193364 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL68152 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL381886 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL371515 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL196930 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL193477 | — | IC50 | = | 200.0 | nM | 6.70 |