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

Ligand: anagrelide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997), EMA (2004)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.
Published in: J Med Chem

Ligand: anagrelide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997), EMA (2004)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): 3,4-Dihydroquinolin-2(1H)-ones as combined inhibitors of thromboxane A2 synthase and cAMP phosphodiesterase.
Published in: J Med Chem

Ligand: anagrelide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997), EMA (2004)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.
Published in: J Med Chem

Ligand: cilostamide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.
Published in: Biochem Pharmacol

Ligand: cilostazol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1999)
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.
Published in: Biochem Pharmacol

Ligand: cyclic GMP (Metabolite)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -

Ligand: enoximone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: UK
Primary target: yes
Median affinity: 5.420000076293945 pIC50
Reference (Journal): Inhibitors of cyclic AMP phosphodiesterase. 2. Structural variations of N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro- 2-oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide (RS-82856).
Published in: J Med Chem

Ligand: ensifentrine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): The pharmacology of two novel long-acting phosphodiesterase 3/4 inhibitors, RPL554 [9,10-dimethoxy-2(2,4,6-trimethylphenylimino)-3-(n-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one] and RPL565 [6,7-dihydro-2-(2,6-diisopropylphenoxy)-9,10-dimethoxy-4H-pyrimido[6,1-a]isoquinolin-4-one].
Published in: J Pharmacol Exp Ther

Ligand: ibudilast (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 3.5199999809265137 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: inamrinone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1984)
Primary target: yes
Median affinity: 4.800000190734863 pIC50
Reference (Journal): Cardiotonic agents. 9. Synthesis and biological evaluation of a series of (E)-4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]ethenyl]-3 (2H)-pyridazinones: a novel class of compounds with positive inotropic, antithrombotic, and vasodilatory activities for the treatment of congestive heart failure.
Published in: J Med Chem

Ligand: milrinone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: milrinone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.
Published in: Biochem Pharmacol

Ligand: papaverine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 6.039999961853027 pIC50
Reference (Journal): Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
Published in: Eur J Med Chem