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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

A) Progression of a Novartis HAT program from a screening hit to brain-penetrant leads. This program started from an HTS screen of 3M compounds, resulting in a singleton hit (Figure 17). Figure 18. B) Results from a computational model of brain-penetration correlated well with actual K p ’s across the series.

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