Assay Detail
Binding
CHEMBL998833
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Inhibition of human recombinant PDE5A1 expressed in COS7 cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.96 | 7.13 |
| Inhibition | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL498486 | — | — | 1 | 7.13 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 7.12 |
| CHEMBL497293 | ICARISIDE II | — | 1 | 6.80 |
| CHEMBL504656 | — | — | 1 | 6.44 |
| CHEMBL193059 | — | — | 1 | 6.16 |
| CHEMBL371562 | — | — | 1 | 5.89 |
| CHEMBL498485 | ICARITIN | 3.0 | 1 | 5.66 |
| CHEMBL553204 | ICARIIN | 3.0 | 1 | 5.23 |
| CHEMBL460647 | SOPHORAFLAVANONE B | — | 1 | 4.79 |
| CHEMBL497654 | — | — | 1 | 4.34 |
| CHEMBL293492 | CINNAMALDEHYDE | -1.0 | 1 | - |
| CHEMBL465040 | FERUTININ | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL498486 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL497293 | ICARISIDE II | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL504656 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL193059 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL371562 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL498485 | ICARITIN | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL553204 | ICARIIN | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL460647 | SOPHORAFLAVANONE B | IC50 | = | 16230.0 | nM | 4.79 |
| CHEMBL497654 | — | IC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL293492 | CINNAMALDEHYDE | Inhibition | = | -16.0 | % | - |
| CHEMBL465040 | FERUTININ | Inhibition | = | -7.0 | % | - |