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Advancements in hit identification for membrane protein drug discovery

Drug Target Review

Advancements in screening technologies for small-molecule drug discovery including cellular assays, computational screening, and biophysics-based methods enhanced by structural biology breakthroughs have improved screening hit rates and facilitated the identification of drug candidates for previously undruggable targets.

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How to Get Drugs Into the Brain

Drug Hunter

Overall, only a few prodrugs for CNS disorders have even reached clinical trials , so for the most part traditional property-based drug design remains the best bet for the vast majority of programs. A) Progression of a Novartis HAT program from a screening hit to brain-penetrant leads. What is K p,uu ? Figure 18.

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