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Drug Discovery & Development

Our group aims to facilitate colleagues from the College of Medicine and beyond to translate their research findings towards commercial outcomes. Atlhough our primary focus is small molecule drug discovery we also provide support for other activities such as diagnostic assay development. We are an experienced team with backgrounds in the pharmaceutical and biotechnology industries, and currently work on a number of drug discovery programmes across several target classes and disease indications. Our most advanced programme has successfully moved beyond the discovery phase towards clinical development.

Drug Discovery

Our expertise ranges from assay development and screening through to hit-to-lead optimisation and pre-clinical profiling. We provide the following support:

  • Protein overexpression in E. coli and yeast
  • Protein purification
  • Protein crystallisation
  • Expression in mammalian cells
  • Assay development
  • Enzymology
  • Small molecule library screening
  • Medicinal chemistry advice
  • ADMET profiling
  • Metabolite profiling
  • In vivo PK/PD profiling
  • Disease model profiling

ADMET Profiling

We provide a range of validated in vitro Absorption, Distribution, Metabolism, Excretion and Toxicology (ADMET) assays that are required during the drug discovery process. These are facilitated by our close association with the Biomedical Mass Spectrometry Core. Assays include:

  • Metabolic stability in pooled liver microsomes (human, primate, dog, pig, rat and mouse)
  • CYP450 inhibition - luminescence and LC-MS assays for 1A2, 2C9, 2C19, 2D6 and 3A4
  • Plasma protein binding (human, rat)
  • Cytoxicity
  • Compound stability in simulated gastric fluid and simulated intestinal fluid
  • Intestinal metabolism in pooled human intestinal microsomes or rat jejunum and duodenum

Instrumentation

Our laboratory is equipped with a range of equiment to support our activities, including:

  • Tecan M1000 tunable microplate reader (FLINT, FP, FRET, HTRF, luminescence, absorbance readouts, 1-1536 well microplates)
  • Molecular Devices tunable microplate reader (absorbance)
  • GE Healthcare AKTA Purifier

We also have access to robotics, radiometric detection (suitable for SPA) and mass spectrometry allowing a broad spectrum of assays to be deployed.

For further enquiries contact Dr Scott Webster

Location: E3.01, QMRI

Telephone: +44 (0)131 242 6738

Email: scott.webster@ed.ac.uk