Target family: Phosphodiesterases, 3',5'-cyclic nucleotide (PDEs) (type: enzyme)
Target: phosphodiesterase 5A

Ligand: compound 53 [PMID: 19631533] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.300000190734863 pIC50
Reference (Journal): Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Published in: Bioorg Med Chem Lett

Ligand: gisadenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.899999618530273 pIC50
Reference (Journal): The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics.
Published in: Bioorg Med Chem

Ligand: ibudilast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 3.990000009536743 pIC50
Reference (Journal): Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast.
Published in: Bioorg Med Chem Lett

Ligand: icariside II (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Icariside II, a phosphodiesterase 5 inhibitor, attenuates cerebral ischaemia/reperfusion injury by inhibiting glycogen synthase kinase-3β-mediated activation of autophagy.
Published in: Br J Pharmacol

Ligand: milrinone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1987)
Primary target: no
Median affinity: 7.309999942779541 pIC50

Ligand: nitrosoprodenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): The identification of a nitrosated prodrug of the PDE-5 inhibitor aildenafil in a dietary supplement: a Viagra with a pop.
Published in: J Pharm Biomed Anal

Ligand: PF-00489791 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.149999618530273 pIC50
Reference (Patent): Use of a tetrasubstituted pyrazolo[4,3-d]pyrimidine compound for treating diabetic nephropathy.

Ligand: SCH51866 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.199999809265137 pIC50
Reference (Journal): Antiplatelet and antiproliferative effects of SCH 51866, a novel type 1 and type 5 phosphodiesterase inhibitor.
Published in: J Cardiovasc Pharmacol

Ligand: sildenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1998)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Published in: J Med Chem

Ligand: sildenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (1998)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibition of cyclic GMP-binding cyclic GMP-specific phosphodiesterase (Type 5) by sildenafil and related compounds.
Published in: Mol Pharmacol

Ligand: T0156 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.5 pIC50
Reference (Journal): Enzymological and pharmacological profile of T-0156, a potent and selective phosphodiesterase type 5 inhibitor.
Published in: Eur J Pharmacol

Ligand: tadalafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2002), FDA (2003)
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
Published in: J Med Chem

Ligand: TPN171 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pIC50
Reference (Journal): Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Published in: J Med Chem

Ligand: tunodafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Yonkenafil: a novel phosphodiesterase type 5 inhibitor induces neuronal network potentiation by a cGMP-dependent Nogo-R axis in acute experimental stroke.
Published in: Exp Neurol

Ligand: udenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: South Korea
Primary target: no
Median affinity: 8.079999923706055 pIC50
Reference (Journal): Mechanism of erectogenic effect of the selective phosphodiesterase type 5 inhibitor, DA-8159.
Published in: Arch Pharm Res

Ligand: vardenafil (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA and FDA (2003)
Primary target: yes
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Published in: Bioorg Med Chem Lett

Ligand: zaprinast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Inhibition of cyclic GMP-binding cyclic GMP-specific phosphodiesterase (Type 5) by sildenafil and related compounds.
Published in: Mol Pharmacol