Drug Discovery Part I: Screening for Compounds Jim Wells ...

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Assay formats: Biochemical • Use a puri�ed protein and an activity you can visualize substrate • Use when enzyme enzyme • You know what protein you want to inhibit • You can express and purify the protein • Selectivity among similar proteins is important Assay formats: Cell-based • Screen in whole cells when • Molecular target known, but not isolable from cell • Goal is to alter a cellular phenotype • Pathway is known, best target is not known Assay formats: Cell-based • Results read out by • Whole well �uorescence/ luminescence • Cell-by-cell properties
Demo • Biochemical assays - Light-box fluorophore High-content cells screens: Quantitative microscopy • Demo High-content screens: Quantitative microscopy
Page 1 and 2: Drug Discovery Part I: Screening fo
Page 3 and 4: Target ID: what’s causing disease
Page 5 and 6: Goals for oral drugs (chemical prop
Page 7: Start with libraries of drug-like m
Page 11: Introduction to Drug Discovery Than

Drug Discovery Part I: Screening for Compounds Jim Wells ...

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