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Cpds 10 6 s to few. A. Whole cell screening – Target Identification. Cpds 10 6 s to few. Genes 1000s to few. Select developable compounds Confirm antibacterial activity. Determine mode of action: Generate resistant mutants Genome re-sequencing Mechanistic screens. Preclinical candidate
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Cpds 106s to few A. Whole cell screening – Target Identification Cpds 106s to few Genes 1000s to few • Select developable compounds • Confirm antibacterial activity • Determine mode of action: • Generate resistant mutants • Genome re-sequencing • Mechanistic screens • Preclinical candidate • selection • Cpd • series & Target • Whole cell antibacterial assays • HTS / focused screens • Screen for antibacterial activity Assay develop. & Compound screens Med. Chem. & Biology Computational Biol. & Microbiology B. Target specific screening – Target prioritization Genes 1000s to few • Gene expression • Gene essentiality • Spectrum / specificity • Tractability • Known mode of action • Expert scoring • Select developable compounds • Screen for antibacterial activity • Preclinical candidate • selection • Cpd • series & Target • Configure assays • HTS or focused screens • Lab validation • Select for screening • Top • Target list Assay develop. & Compound screens Med. Chem. & Biology Computational Biol. & Microbiology