Wednesday, June 19, 2013

instrumentsFree Application Guide: High Throughput Screening Applications

What is Smarter Screening?
High throughput screening (HTS), or the process by which libraries of small molecule compounds are individually assessed for binding, activating or inactivating biological activity in drug target molecules, has been part of the drug discovery process for more than two decades. Its primary purpose is to rapidly select which compounds possess the desired activity and thereby undergo further testing and optimization. Since its inception, HTS methods have undergone significant change: the early dependence on “home-brewed” assay chemistries and basic research instruments evolved into industrialized methods incorporating millions of compounds that could be screened against purified drug targets using sophisticated liquid handling, detection and robotics.
In this Application Guide, we describe key liquid handling and detection instrumentation for HTS methods and provide four HTS case studies. The case studies use commercially available compound libraries and assay chemistries suitable for nuclear receptor, GPCR, cellular kinase, as well as epigenetic drug targets.

This Application Guide covers:

  • Androgen Receptor Agonist/Antagonist Studies using the Cell-based Human AR Reporter Assay System from INDIGO Biosciences
  • GLP-1 Ligand Binding Analysis using a Cell-Based HTRF® Tag-lite® Assay
  • Quantification of Endogenous Cellular Kinase Activity using a Cell-Based HTRF Phospho-STAT3 (Tyr705) Protein Kinase Assay
  • Assessment of Histone Deacetylase 1 Inhibition using the Bioluminescent HDAC-Glo™ I/II Assay

Tag-lite and HTRF are registered trademarks of Cisbio Bioassays.
HDAC-Glo is a trademark of Promega Corporation. 

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