Assay Detail
Binding
CHEMBL4014035
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE5A1 catalytic domain (535 to 860 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method
22
Total Activities
22
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
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.70 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1737 | SILDENAFIL CITRATE | 4.0 | 1 | 8.29 |
| CHEMBL4059555 | — | — | 1 | 8.27 |
| CHEMBL4099219 | — | — | 1 | 8.25 |
| CHEMBL4087872 | — | — | 1 | 7.80 |
| CHEMBL4099081 | — | — | 1 | 7.68 |
| CHEMBL4082746 | — | — | 1 | 7.52 |
| CHEMBL4069398 | — | — | 1 | 7.51 |
| CHEMBL4079069 | — | — | 1 | 7.30 |
| CHEMBL4084753 | — | — | 1 | 7.25 |
| CHEMBL4065489 | — | — | 1 | 7.11 |
| CHEMBL4072265 | — | — | 1 | - |
| CHEMBL4096629 | — | — | 1 | - |
| CHEMBL4060717 | — | — | 1 | - |
| CHEMBL4088934 | — | — | 1 | - |
| CHEMBL4091487 | — | — | 1 | - |
| CHEMBL4086923 | — | — | 1 | - |
| CHEMBL4103327 | — | — | 1 | - |
| CHEMBL4095575 | — | — | 1 | - |
| CHEMBL4068199 | — | — | 1 | - |
| CHEMBL4063667 | — | — | 1 | - |
| CHEMBL4073050 | — | — | 1 | - |
| CHEMBL4099915 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1737 | SILDENAFIL CITRATE | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4059555 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4099219 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4087872 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4099081 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4082746 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4069398 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4079069 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4084753 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4065489 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4072265 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4096629 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4060717 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4088934 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4091487 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4086923 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4103327 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4095575 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4068199 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4063667 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4073050 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL4099915 | — | IC50 | > | 100.0 | nM | - |