EN CN


Target Based Assays

Return

Phosphodiesterases (PDEs)

Phosphodiesterase Drug Discovery

Phosphodiesterases (PDEs) regulate intracellular levels of cyclic nucleotides such as cAMP and cGMP by catalyzing their hydrolysis. Dysregulated PDE activity is associated with erectile dysfunction, pulmonary hypertension, neurodegenerative disorders, and other diseases.

Selective inhibition of individual PDE isoforms enables modulation of cyclic-nucleotide signaling and provides a foundation for therapeutic development across diverse disease areas.

Assay Principle

Fluorescence-polarization detection of PDE activity

PDE hydrolytic activity is measured by monitoring the breakdown of dye-labeled cyclic nucleotides. PDE-mediated hydrolysis exposes the resulting nucleotide monophosphate, allowing high-affinity beads to bind the product. This interaction changes the motion of the fluorescent molecular complex and generates a measurable fluorescence-polarization (FP) signal. The degree of cyclic-nucleotide hydrolysis reflects PDE activity and supports evaluation of small-molecule inhibitor potency.

Assay Strategy

PDE inhibitor selectivity profiling

01 / ISOFORM COVERAGE

Activity assays are available across a broad range of PDE families and isoforms.

02 / SELECTIVITY

Cross-family and within-subtype profiling supports assessment of inhibitor selectivity, including comparisons across PDE4 targets.

03 / REFERENCE CONTROLS

Reference compounds are available for target-specific assay validation and comparative inhibitor characterization.

Target Coverage

Available PDE activity assays

TargetSynonymsAssay TypeReference Compound
PDE1APDE1A5ActivityBay 60-7550
PDE1BPDE1B1ActivityBay 60-7550
PDE1CHcam3ActivityBay 60-7550
PDE2A
ActivityBay 60-7550
PDE3A
ActivityCilostamide, Anagrelide, IBMX, Milrinone
PDE3BCGIPDE1, CGIP1ActivityCilostamide
PDE4A1APDE4A1ActivityRoflumilast
PDE4A4BPDE4A4, PDE46ActivityRoflumilast, BI 1015550
PDE4A10
ActivityRoflumilast
PDE4B1
ActivityRoflumilast
PDE4B2
ActivityRoflumilast, BI 1015550
PDE4B3
ActivityRoflumilast
PDE4C1
ActivityRoflumilast
PDE4C2
ActivityRoflumilast, BI 1015550
PDE4D2hPDE4D2ActivityML-030, Roflumilast, BI 1015550
PDE4D3hPDE4D4ActivityML-030, Roflumilast
PDE4D7
ActivityRoflumilast
PDE5APDE5ActivitySildenafil citrate
PDE6C
ActivitySildenafil citrate
PDE7AHCP1, TM22ActivityBRL-50481
PDE7BbA472E5.1ActivityDipyridamole
PDE8A1
ActivityDipyridamole
PDE9A2
ActivityBAY-73-6691
PDE10A1
ActivityTP-10
PDE10A2
ActivityTP-10
PDE11A4
ActivityDipyridamole

Contact Us

We value your inquiries and are here to provide you with tailored solutions for your drug discovery and development needs. Whether you have questions, require more information, or are interested in discussing potential collaborations, our team of experts is just a message away.
Feel free to reach out to us.

We are a CRO service organization, not a hospital




Get a quote

Go top