Assay Detail
Binding
CHEMBL4268472
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE5 (unknown origin)
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.47 | 9.28 |
| Ki | 7 | 8.45 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4212630 | — | — | 1 | 9.28 |
| CHEMBL4209716 | — | — | 1 | 9.22 |
| CHEMBL1520 | VARDENAFIL | 4.0 | 1 | 9.15 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.80 |
| CHEMBL4214135 | — | — | 1 | 8.52 |
| CHEMBL4214699 | — | — | 1 | 8.52 |
| CHEMBL163905 | — | — | 1 | 8.40 |
| CHEMBL1963681 | AVANAFIL | 4.0 | 1 | 8.30 |
| CHEMBL337587 | — | — | 1 | 8.30 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 8.28 |
| CHEMBL4277253 | — | — | 1 | 8.10 |
| CHEMBL133285 | — | — | 1 | 8.10 |
| CHEMBL4288994 | — | — | 1 | 8.10 |
| CHEMBL4212186 | — | — | 1 | 7.96 |
| CHEMBL4210889 | — | — | 1 | 7.77 |
| CHEMBL4288553 | — | — | 1 | 7.07 |
| CHEMBL4288354 | — | — | 1 | 6.80 |
| CHEMBL4280451 | — | — | 1 | 6.77 |
| CHEMBL4288752 | — | — | 1 | 6.72 |
| CHEMBL4278092 | — | — | 1 | 6.62 |
| CHEMBL4205751 | — | — | 1 | 5.31 |
| CHEMBL501991 | PERLOLYRIN | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4212630 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL4209716 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1520 | VARDENAFIL | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL192 | SILDENAFIL | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4214135 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4214699 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL163905 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1963681 | AVANAFIL | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL337587 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL779 | TADALAFIL | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL4277253 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL133285 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4288994 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4212186 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4210889 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4288553 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4288354 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4280451 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4288752 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4278092 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4205751 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL501991 | PERLOLYRIN | IC50 | = | 9300.0 | nM | 5.03 |