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Exposed polar surface area (EPSA), which assays PSA experimentally, has emerged as a valuable tool to screen for potentially permeable “beyond rule of 5” (bRo5) compounds —promising candidates for developing treatments targeting previously undruggable sites. As bRo5 drugs play an increasingly crucial role in treating complex diseases but have poor oral pharmacokinetics, it is significantly important to establish a more rapid screening platform for potentially permeable drugs to provide essential guidance for molecular modification.

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