Profiling PDEs with the Transcreener AMP²/GMP² Phosphodiesterase Assay

Transcreener AMP2/GMP2 Phosphodiesterase Assay Kit

Detect any AMP or GMP producing enzyme (e.g., ligases, synthetases, phosphodiesterases) using any precursor substrate, including cAMP, cGMP, ATP, or NAD. It is the only activity assay method for direct detection of unlabeled AMP or GMP; i.e. without using coupling enzymes. The method is simple and HTS-proven: run your enzyme reaction, add detection reagents, and read the far red FP or TR-FRET signal on any multimode plate reader.

XMP enzyme products, including AMP, GMP, and CMP displace a fluorescent tracer from a highly selective antibody resulting in a change in fluorescence. Both assays use a far-red tracer, which reduces compound interference and provides a robust ratiometric readout. Make measuring cyclic nucleotide phosphodiesterase activity easy with a simple, proven, HTS-ready assay.

Universal AMP/GMP Detection for Phosphodiesterases

Phosphodiesterase Assay Kit Schematic AMP GMP Assay FP
Phosphodiesterase Assay Kit Schematic AMP GMP Assay TR-FRET

One Assay … Hundreds of Targets

Along with PDEs the kit can also be used with:

  • Ligases: Ub and SUMO Ligases, DNA and RNA Ligases
  • Synthetases: Acyl CoA Synthetase, Amino-Acyl tRNA Synthetases, NAD Synthetase
  • Phosphodiesterases: cAMP, cGMP
  • Sialyltransferases: (CMP detection)
  • Protein deAMPylase
  • Ectonucleotidases such as CD39, CD73, and ENPP1


  • Measure Enzymatic Activity
  • Screen Compound Libraries for Inhibitors
  • Determine Inhibitor Selectivity
  • Measure Inhibitor Potency
  • Inhibitor Residence Time Measurement

Measure the Potency of Inhibitors for a Variety of Targets


  • Direct detection of unlabeled AMP or GMP from a PDE reaction
  • Easy to use: one-step, simple mix-and-read format
  • Robust: Z’ > 0.7 for initial velocity reactions
  • Less interference: Far-red fluorescence minimizes compound interference
  • Non-radioactive assay technique
  • Available in FP or TR-FRET readouts
  • Wide substrate concentration range: 1 μM to 1000 µM

Sensitive Assay with Large Window

PDE Assay Services

Interested in moving your program forward, but don't want to bring an assay in-house? Our scientists can help! BellBrook scientists will use their extensive biochemistry and enzymology expertise to work with you and accelerate your PDE program.

Assay Development Services

Lead Discovery Services Include:

  • Inhibitor Screening – To identify or confirm activity with the target.
  • Inhibitor Potency Profiling – Dose-response with target and/or related proteins. Fast IC50 results.
  • Residence Time Measurements – Determination of koff using ‘jump dilution’ enzymatic assay method.
  • Mechanism of Action Studies – Kinetic analysis to define the mode of inhibition.

Contact Us to Learn More

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What's Included

What You Will Need

Far Red FP & TR-FRET Readouts Validated on Major Multimode Readers

Supplier Instrument FP Assays
TR-FRET Assays
bioteklogo TriStar²S LB 942 in review validated
Mithras² LB 943 in review validated
bioteklogo Cytation™ 5 validated validated
Cytation™ 3 validated validated
Cytation™ 1 validated validated
Synergy™ H1 validated validated
Synergy™ 2/H4/4 validated validated
Synergy™ HTX not capable not capable
Synergy™ Neo 2 validated validated
BMGLABTECH Logo POLARstar® Omega validated validated
FLUOstar® Omega not capable validated
PHERAstar® FSX validated validated
PHERAstar® Plus/FS validated validated
CLARIOstar® /Plus validated validated
VANTAstar validated validated
MDS AT logo Analyst® GT/HT validated validated
Gemini® XPS/EM not capable not capable
SpectraMax® M2/M2e not capable not capable
SpectraMax® M5/M5e/FlexStation® 3 not capable validated
SpectraMax® Paradigm validated contact us
SpectraMax® iD3/iD5 in review validated
perkinElmerLogo EnVision®/EnVision® Xcite validated validated
tecanLogo Infinite® M1000/M1000Pro/Safire2™ validated validated
Infinite® M200 not capable not capable
Infinite® F500 validated validated
Infinite® F200/Ultraevolution contact us contact us
Spark™ 10M validated validated

PDE's As Enzyme Drug Targets

Cyclic nucleotide phosphodiesterases are proven drug targets. Most are a focus of inhibition due to their functional properties. Since PDEs degrade cAMP or cGMP, inhibitors can prolong the effects of the cyclic nucleotide in the signaling cascade within the tissues where the individual enzyme is most likely to reside.

PDEs are currently classified into 11 different families. Each is classed based on a number of different factors including the distribution within tissue, and substrate specificity. Some hydrolyze cAMP, while others cGMP. A variety can degrade both cAMP and cGMP. The Transcreener antibody can detect the product AMP or GMP of cyclic nucleotide hydrolysis. This allows the measurement of virtually any PDE's activity.

Substrate Specificity

cAMP4, 7, 8
cGMP5, 6, 9
cAMP & cGMP1, 2, 3, 10, 11

The Transcreener phosphodiesterase assay enables researchers to scour vast compound libraries for potent, yet selective inhibitors for unique PDEs. Follow-up SAR can also be completed to improve upon initial hits and provide a greater probability for success. PDEs have excellent promise in a variety of therapeutic areas including heart disease, dementia, infection, depression, and asthma. New inhibitors can provide better therapeutic potential and can limit off-target effects more effectively.