Category: Assay Development and Screening

1376-B - The Transcreener® ADP2 Assay: A Universal Kinase Assay for Both HTS and Lead Discovery

Monday, February 5, 2018
5:00 PM - 6:00 PM

Kinases are one of the most highly validated target families, yet only a small fraction of the kinome has been exploited therapeutically. ADP detection provides a generic assay method that has been broadly adopted for HTS efforts targeting kinases. The Transcreener ADP2 Kinase assay uses homogenous detection of ADP with a choice of FP, FI, or TR-FRET readouts. Although other methods of ADP detection are available, Transcreener is the only with direct detection of ADP. Alternative assays use complex coupling mechanisms making them prone to assay interference, generating false positives that are painstaking to triage. The assay is sensitive at low ADP concentrations used under initial velocity conditions, critical for screening such a diverse class of targets Compatibility with 1536 well-miniaturized formats along with outstanding overnight and reagent signal stability provide flexibility in liquid handling while gathering data that produces dependable results. And while Transcreener’s flexibility and simplicity make it an excellent fit for HTS, the assay also has distinct advantages in SAR and MOA studies. Sensitivity affords use of the assay at low enzyme concentrations and helps determine accurate IC50 measurements for potent inhibitors. Transcreener can also be used kinetic mode, which simplifies early stage assay development and is used while assessing drug-target residence time. Here we demonstrate the Transcreener ADP2 Kinase Assay as a universal HTS approach to discovering, evaluating, selecting, and improving small molecule enzymatic inhibitors as potential new therapeutics for disease.

Justin Brink

Director of Marketing
BellBrook Labs
Madison, Wisconsin

With years of assay development experience, I am currently working to find applications and technology to advance drug discovery. My goal is to discover areas of research where we can leverage current technology platforms to enhance the process of finding new treatments for disease. In my current role with BellBrook Labs, we work every day to accelerate drug discovery by providing HTS solutions to our academic and biotech collaborators. My hope is that this work will provide lasting benefit, and treatments for a multitude of ailments for people worldwide.