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Enzymes/Biochemical Assays

Overview

Enzyme/biochemical assays are essential tools to screen compounds that bind to target proteins with a defined mechanism. In recent years a large variety of enzyme/biochemical assays have been developed to discover and to optimize compounds that inhibit the activity of these targets.

As part of the WuXi Research Service Division (RSD), the Biology Unit is led by a group of leading scientists with significant experience in drug discovery.The RSD Biology Unit is dedicated to providing open access and integrated platforms for supporting plate-based screening services, including HTS, hit identification, lead optimization, selectivity screening and early safety profiling, up to drug candidate selection.

 

Assay Development

  • Strong expertise relating to enzymology in drug discovery.
  • Capabilities for assay development on diverse targets: kinase, phosphatase, ATPase, polymerase, dehydrogenase/reductase, protease, epigenetic enzymes (HMT, KDM, HDAC, Bromodomain), ligand-receptor (protein) binding and PPI.
  • Example of assay development

 

Assay Formats

  • End-point assay & continuous assays
  • Plate-based screening platform
  • Major assay platforms: TR-FRET, FP, ADP-Glo, Z-Lyte , ELISA, absorbance, LC/MS

 

Compound Profiling

  • Weekly screening service to provide clients high quality, timely data, with the ability to solve problems and communicate effectively 
  • Potency measurements across multiple target classes (IC50, Ki)

 

Inhibitor Characterization

  • Compound evaluation, as a part of SAR, to understand MOA of inhibitors, including mechanism of inhibition, time-dependent inhibition and reversibility of inhibition
  • Example of studying mechanism of inhibition