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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