Course Outline

Overview of key biological areas and technologies relevant to medicinal chemists.


Biology of the major drug target classes:
Structure, function and relative target tractability.


Key biological tools of the trade/interpretation of the data they generate:

- in vitro compound potency and selectivity: bioassay formats and design, enzyme inhibition, receptor binding modulation, low-throughput screening, high-throughput screening/bioassay automation, micro/nano-bioassays, bioassay in cell culture, virtual screening.

- biostructural (X-ray) analysis of the compound-target protein complex.

- Global Technologies: genomics, structural genomics, proteomics, chemogeomics

- Methods for in vitro ADMET assays: P450 inhibition, metabolic stability, protein binding, permeability, cytotoxicity assays, hERG assay.

 

Animal models of disease.

- selected key animal models, their application and value.


Biological data handling.

- methods for quality assessment and interpretation.

 

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