DGIdb - SILDENAFIL Drug Record

SILDENAFIL chembl:CHEMBL192 Approved

Alternate Names:

VIAGRA
VIZARSIN
HIP-0908
HIP0908
SILDENAFIL
UK-92480
REVATIO
NIPATRA
5-[2-ETHOXY-5-(4-METHYLPIPERAZIN-1-YLSULFONYL)PHENYL]-1-METHYL-3-PROPYL-1H-PYRAZOLO[4,3-D]PYRIMIDIN-7(6H)-ONE
5-[2-ETHOXY-5-(4-METHYL-PIPERAZINE-1-SULFONYL)-PHENYL]-1-METHYL-3-PROPYL-1,6-DIHYDRO-PYRAZOLO[4,3-D]PYRIMIDIN-7-ONE
1-{[3-(4,7-DIHYDRO-1-METHYL-7-OXO-3-PROPYL-1H-PYRAZOLO[4,3-D]PYRIMIDIN-5-YL)-4-ETHOXYPHENYL]SULFONYL}-4-METHYLPIPERAZINE
rxcui:136411
chembl:CHEMBL192
pubchem.compound:5212
drugbank:00203
chemidplus:139755-83-2

Drug Info:

Year of Approval	1998
Drug Class	anti-impotence agents
Drug Indications	for treatment of erectile dysfucntion,antihypertensive agent
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	for treatment of erectile dysfunction

(2 More Sources)

Publications:

Rybalkin et al., 2003, PDE5 is converted to an activated state upon cGMP binding to the GAF A domain., EMBO J.
Zoraghi et al., 2007, Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors., Biochemistry
Wang et al., 2008, Conformational variations of both phosphodiesterase-5 and inhibitors provide the structural basis for the physiological effects of vardenafil and sildenafil., Mol. Pharmacol.
Corbin et al., 2002, Phosphodiesterase type 5 as a pharmacologic target in erectile dysfunction., Urology
Wang et al., 1999, [Mode of action of sildenafil]., Zhongguo Yi Xue Ke Xue Yuan Xue Bao
Kruuse et al., 2003, Migraine can be induced by sildenafil without changes in middle cerebral artery diameter., Brain
Wang et al., 2006, Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development., J. Biol. Chem.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Carson, 2003, Long-term use of sildenafil., Expert Opin Pharmacother
Eisenhardt A et al., 2003, ACE gene I/D and NOS3 G894T polymorphisms and response to sildenafil in men with erectile dysfunction., Urology
de Denus S et al., 2018, CYP3A4 genotype is associated with sildenafil concentrations in patients with heart failure with preserved ejection fraction., Pharmacogenomics J
Sperling H et al., 2003, Sildenafil response is influenced by the G protein beta 3 subunit GNB3 C825T polymorphism: a pilot study., J Urol
Muniz JJ et al., 2013, Endothelial nitric oxide synthase genotypes and haplotypes modify the responses to sildenafil in patients with erectile dysfunction., Pharmacogenomics J
Lacchini R et al., 2013, VEGF genetic polymorphisms affect the responsiveness to sildenafil in clinical and postoperative erectile dysfunction., Pharmacogenomics J
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

SILDENAFIL PDE5A

Interaction Score: 2.9

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12554648 17979301 17959709 12414329 12567500 12477710 16735511 11752352 12614192

Sources:
TdgClinicalTrial TEND GuideToPharmacology
SILDENAFIL PDE6C

Interaction Score: 1.93

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
SILDENAFIL GNB3

Interaction Score: 0.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12576843

Sources:
PharmGKB
SILDENAFIL ABCC5

Interaction Score: 0.72

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
SILDENAFIL NOS3

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22064666

Sources:
PharmGKB
SILDENAFIL VEGFA

Interaction Score: 0.31

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23007311

Sources:
PharmGKB
SILDENAFIL SLCO2B1

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
SILDENAFIL SLCO1B3

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
SILDENAFIL ACE

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12837457

Sources:
PharmGKB
SILDENAFIL CYP3A5

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
SILDENAFIL CYP3A4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28440343

Sources:
DTC PharmGKB

TEND: SILDENAFIL
- Version: 01-August-2011
Alternate Names:

SILDENAFIL Primary Drug Name

Drug Info:

Drug Class anti-impotence agents

Year of Approval 1998

Publications:
TdgClinicalTrial: SILDENAFIL
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications for treatment of erectile dysfunction

Drug Class Small Molecule

FDA Approval approved

Publications:

PharmGKB: sildenafil

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

de Denus S et al., 2018, CYP3A4 genotype is associated with sildenafil concentrations in patients with heart failure with preserved ejection fraction., Pharmacogenomics J

Eisenhardt A et al., 2003, ACE gene I/D and NOS3 G894T polymorphisms and response to sildenafil in men with erectile dysfunction., Urology

DTC: SILDENAFIL
- Version: 02-September-2020
Alternate Names:

CHEMBL192 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178101454
- Version: 29-September-2020
Alternate Names:

SILDENAFIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL192
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Direct Interaction?	True
Endogenous Drug?	False
Specific Action of the Ligand	Inhibition

SILDENAFIL Drug Record

SILDENAFIL chembl:CHEMBL192 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 12554648 17979301 17959709 12414329 12567500 12477710 16735511 11752352 12614192

Sources: TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12576843

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22064666

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23007311

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12837457

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28440343

Sources: DTC PharmGKB

TEND: SILDENAFIL

Alternate Names: SILDENAFIL Primary Drug Name

Drug Info: Drug Class anti-impotence agents Year of Approval 1998

Publications:

TdgClinicalTrial: SILDENAFIL

Alternate Names:

Drug Info: Drug Indications for treatment of erectile dysfunction Drug Class Small Molecule FDA Approval approved

Publications:

PharmGKB: sildenafil

Alternate Names:

Drug Info:

DTC: SILDENAFIL

Alternate Names: CHEMBL192 ChEMBL Drug ID

Drug Info:

Publications:

GuideToPharmacology: 178101454

Alternate Names: SILDENAFIL GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL192

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
12554648 17979301 17959709 12414329 12567500 12477710 16735511 11752352 12614192

Sources:
TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
12576843

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22064666

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23007311

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
12837457

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
28440343

Sources:
DTC PharmGKB

Alternate Names:

SILDENAFIL Primary Drug Name

Drug Info:

Drug Class anti-impotence agents

Year of Approval 1998

Drug Info:

Drug Indications for treatment of erectile dysfunction

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL192 ChEMBL Drug ID

Alternate Names:

SILDENAFIL GuideToPharmacology Ligand Name