Compound Detail
CHEMBL1339
VARDENAFIL HYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
CCCc1nc(C)c2c(O)nc(-c3cc(S(=O)(=O)N4CCN(CC)CC4)ccc3OCC)nn12.Cl
Basic Information
| ChEMBL ID | CHEMBL1339 |
| Name | VARDENAFIL HYDROCHLORIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | XCMULUAPJXCOHI-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL1520 |
| Active Moiety | CHEMBL1520 |
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
8
Publications
12
Known Names
2
Indications
1
Mechanisms
Molecular Properties
488.6
MW (Da)
2.07
ALogP
8
HBA
1
HBD
112.9
PSA (Ų)
0.52
QED
0
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2003 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Phosphodiesterase 5A inhibitor | INHIBITOR | cGMP-specific 3',5'-cyclic phosphodiesterase | ✓ | ✓ |
Indications
Erectile Dysfunction Erectile Dysfunction
Activity Summary
IC50 2 meas. best 9.15
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| cGMP-specific 3',5'-cyclic phosphodiesterase CHEMBL1827 | IC50 | 9.15 | 9.15 | 0.7 | 1 |
| Phosphodiesterase 1 CHEMBL2097166 | IC50 | 6.75 | 6.75 | 180.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| T1/2 | 4.0 | hr | Homo sapiens |
| Tmax | 0.5 | hr | Homo sapiens |
| Vss | 208.0 | L | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| cGMP-specific 3',5'-cyclic phosphodiesterase | IC50 | = | 0.7 | nM | 9.15 | Inhibition of Phosphodiesterase 5 | 11958981 |
| Phosphodiesterase 1 | IC50 | = | 180.0 | nM | 6.75 | Inhibition of Phosphodiesterase 1 | 11958981 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 11958981 | 10.1016/s0960-894x(02)00030-6 | Phosphodiesterase 1 | 1 |
| 11958981 | 10.1016/s0960-894x(02)00030-6 | cGMP-specific 3',5'-cyclic phosphodiesterase | 1 |
| 11958981 | 10.1016/s0960-894x(02)00030-6 | Phosphodiesterase 3 | 1 |
| 11958981 | 10.1016/s0960-894x(02)00030-6 | Phosphodiesterase 4 | 1 |
| 11958981 | 10.1016/s0960-894x(02)00030-6 | Oryctolagus cuniculus | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine