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We systematically validated a robust 96‐well Caco‐2 assay via an extended set of 93 marketed drugs with diverse transport mechanisms and quantified by LC/MS/MS, to investigate its predictive utility while dealing with challenging discovery compounds. Utilizing nonlinear fit, the validation led to a good correlation (R2 = 0.76) between absorptive permeability, log Papp(A–B), from in vitro Caco‐2 assay...
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