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Publications A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

Application Notes Automating a Cell-Based Target-Compound Assay for Methyltransferase and Bromodomain Proteins using the InCELL Hunter Platform

Histone modifications are essential in eukaryotic gene expression and regulation, and are driven by histone writer, eraser, and reader proteins.…

Scientific Posters PathHunter® β-Arrestin Assays: Determination of Pharmacology Differences Between Human and Ortholog GPCRs

DiscoveRx previously introduced a protein-protein interaction system using enzyme fragment complementation that provides a robust, HTS friendly format for monitoring…

Brochures & Flyers InCELL Pulse™ Target Engagement Kinase Reference Set

View validation data for diverse kinases. Cellular target engagement potency data for multiple kinase inhibitors Dose response curves for under-studied…

Brochures & Flyers GPCR Reference Guide

As more is learned about the intricacies of GPCR signaling, the harder it becomes to accurately describe ligand activity using…

Presentations Advancing Therapeutics Targeting Cytokines with Functional Cell-based Assays

Jennifer Lin-Jones, Ph.D., Associate Director of Assay Development R&D Department, Eurofins DiscoverX

Publications Discovery of Potent Agonists for the Predominant Variant of the Orphan MAS-Related GPCR X4 (MRGPRX4)

The MAS-related Gq protein-coupled receptor X4 (MRGPRX4) is poorly investigated. MRGPRX4 has been proposed to be involved in pain transmission,…

Publications Cell-Based Protein Stabilization Assays for the Detection of Interactions between Small-Molecule Inhibitors and BRD4

Bromodomain protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) proteinfamily, acts as a central element in transcriptional…

Publications MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities

Mast cells play key roles in allergy, anaphylaxis/anaphylactoid reactions, and defense against pathogens/toxins. These cells contain cytoplasmic granules with a…

Publications The SUMOylation inhibitor subasumstat potentiates rituximab activity by IFN1-dependent macrophage and NK cell stimulation

Small ubiquitin-like modifier (SUMO) is a member of a ubiquitin-like protein superfamily. SUMOylation is a reversible posttranslational modification that has…

Publications The First WHO International Standard for Harmonizing the Biological Activity of Bevacizumab

Several Bevacizumab products are approved for clinical use, with many others in late-stage clinical development worldwide. To aid the harmonization…

Blogs & Articles Ligand Bias: Increasing specificity and Reducing Side Effects of Drug Compounds

Ligand bias is the ability of compounds to exert differential signal transduction responses on activation of a GPCR. This is…

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