Assay Detail
Binding
CHEMBL832406
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Inhibitory concentration against human phosphodiesterase 10
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL4409) ↗| 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 | 4 | 5.76 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1520 | VARDENAFIL | 4.0 | 1 | 6.10 |
| CHEMBL373102 | — | — | 1 | 5.66 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 5.51 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1520 | VARDENAFIL | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL373102 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL779 | TADALAFIL | IC50 | > | 10000.0 | nM | - |