ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.

BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.

Apremilast(CC10004) is a novel small molecule inhibitor of PDE4 with an IC50 value of 74 nM.

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.

Milrinone(Primacor) is a a potent and selective phosphodiesterase 3 inhibitor with an IC50 of 0.42 μM for the inhibition of FIII PDE

PAT-347 is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood.

Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.

Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

Roflumilast (Daxas) is a selective inhibitor of PDE4 with IC50 of 0.2-4.3 nM.

PF-2545920 a highly selective and potent PDE10A inhibitor with an IC50 of 0.37 nM.

Olprinone Hcl(Loprinone Hcl) is a selective phosphodiesterase 3 (PDE3) inhibitor.

E6005 potently and selectively inhibited human PDE4 activity with an IC50 of 2.8 nM and suppressed the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM.

AN-2728 is a topically administered, boron-containing, anti-inflammatory compound that inhibits PDE4 activity and thereby suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors.

PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke.

Phenacaine (Holocaine) is a local anesthetic. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca2+-ATPase and cyclic nucleotide phosphodiesterases from brain and heart.

(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine, is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases.

Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM.

Roflupram is a selective, orally active and brain-penetrant PDE4 inhibitor, with an IC50 of 26.2 nM for core catalytic domains of human PDE4. Roflupram can reverse cognitive deficits and reduce the production of pro-inflammatory factors.

PF-8380 is a potent and specofic autotaxin inhibitor with an IC50 value of 2.8 nM.

T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.

SEP-0372814 is a potent PDE10 inhibitor.

Sildenafil citrate, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.

TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.

PF-04827736 ((S)-PF-04677490) is a potent, selective PDE1 inhibitor with IC50 of 42, 9.1 and 38 nM for PDE1A, PDE1B and PDE1C, respectively; displays >10-fold selectivity over PDE10A1, and >45-fold selectivity over other PDE isoforms.

LY2775240 (LY-2775240) is a highly selective, potent and orally active inhibitor of phosphodiesterase 4 (PDE4) with IC50 of 0.09/0.09/2.4/0.14 nM for PDE4A/B/C/D.LY2775240 displays >200-fold selectivity over PDE10A, and >5000-fold selectivity over other PDE isoforms (IC50>10 uM).LY2775240 potently inhibits TNFα secreted induced by Toll‐like receptor 4 agonist LPS in a human whole blood assay, inhibited LPS‐stimulated TNFα but has no effect with the media‐only control.LY2775240 is more potent than apremilast (IC50, 18 nM vs. 290 nM), also affects E‐selectin, secreted IgG, plasminogen activator inhibitor‐1, and secreted IL‐10.

CPL500036 (CPL-500036) is a highly potent, selective and orally bioavailable PDE10A inhibitor with IC50 of 35 nM.CPL500036 is highly selective for PDE10A over other PDEs and common off-targets.CPL500036 effectively penetrates the brain where increases cAMP/cGMP levels and phosphorylates effector proteins like AMPA subunits.CPL500036 reduced sensorimotor deficits in 6-OHDA-lesioned rats.Acute and chronic CPL500036 did not reduce effects of L-DOPA in sensorimotor tests.Chronic CPL500036 treatment did not decrease L-DOPA-induced contralateral rotation.