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 WuXi Discovery Services, the Biology Unit is led by a group of leading scientists with significant experience in drug discovery. The Discovery Biology Unit is dedicated to providing open access and integrated platforms to support 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, GTPase (KRAS) polymerase, dehydrogenase/reductase, protease, epigenetic enzymes (HMT, KDM, HDAC, Bromodomain), ligand-receptor (protein) binding and PPI.
  • Example of assay development
Enzymology, Kinase, phosphatase, ATPase, polymerase, protease, and epigenetic enzymes, ATP, titration

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
Enzyme inhibitor analysis, including Vmax, Km, Ki, substrate-inhibitor titration, reversible, time-dependent