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Lead generation cellular assays

In the case that the functional cellular target of the lead hits is known and validated, determine the in vitro biochemical half-maximal inhibitory concentrations (IC50) with an accepted assay method. If the capacity for generating this data does not exist institutionally, many fee-for-service resources are available. Without a known target but knowledge of the signaling pathway modulated by the lead hits, a cellular reporter assay can be used in lieu of a biochemical assay however, it is important to keep in mind that compensatory and multimodal effects can confound SAR efforts in cellular systems. These on-target biochemical and cellular assay profiles will serve as potency benchmarks for later SAR and optimization studies. [Pg.215]


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See also in sourсe #XX -- [ Pg.89 ]




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