Transforming Discovery into Opportunity

Screening

Head, Tom Pfeifer, PhD (bio)

The process of finding a new drug against a chosen target for a particular disease involves screening large libraries of chemicals for their ability to modify the target. This Division has an extensive set of screening libraries of pure chemicals and natural product fractions to ensure sampling of a wide diversity of compounds for potential drug activity. The chemicals identified as ‘hits’ against individual targets serve as useful tools to study biological processes and human diseases, and as potential lead compounds for drug development.

The Screening Division assists PI’s in developing assays to measure the activity of molecules against the chosen target. Medium- to high-throughput compound screening can be carried out using in-vitro and cell-based systems to identify hits for drug development. CDRD has liquid-handling robots and a suite of instruments for the automated detection of biological and biochemical activity.

Screening Libraries:
  • 230,000 compounds including contributions by chemists
  • 200,000 pre-fractionated Natural Product library (NatureBank) and 5,000 Actinomycete crude extracts
  • 1,000 compound fragment library
  • Selected libraries of known drugs, active agents, kinase inhibitors and metabolites
Capabilities and Expertise Assay Development:
  • Rational biochemical and cell-based assay design for target analysis and phenotypic screening
  • Most detection methodologies available including high throughput microscopy
  • Assay refinement and optimization to 384 well plates for screening for testing of assays in a Pilot screen
High Throughput/Content Screening:
  • Full suite of liquid handlers and dispensers with stackers
  • Both HTS and HCS systems available
  • Automated multi-format system utilizing CatalystExpress robotics
  • Data analysis software for activity relationships
Hit Confirmation:
  • Active compound confirmation and establishment of concentration curves
  • Analogue by catalogue analysis for preliminary structure activity relationships
  • Secondary assay verification

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