The criteria used to identify and prioritize the chemical matter from a HTS campaign will be outlined.  Synthetic efforts to optimize the highest priority hits using parallel synthesis, structure-based drug design and multi-parameter optimization will be presented.  Techniques used during this process include library design, protein crystallography, HT-ADME and medicinal chemistry principles.

HTS identification and optimization of Rho Kinase inhibitors

241st National Meeting (2011)

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