Article
Demonstration of In Vitro to In Vivo Translation of a TYK2 Inhibitor That Shows Cross Species Potency Differences.
Scientific reports - 2 Jun 2020
Gerstenberger Brian S, Banker Mary Ellen, Clark James D, Dowty Martin E, Fensome Andrew, Gifford Roger, Griffor Matthew C, Hegen Martin, Hollingshead Brett D, Knafels John D, Lin Tsung H, Smith James F, Vajdos Felix F
Abstract excerpt
Translation of modulation of drug target activity to therapeutic effect is a critical aspect for all drug discovery programs. In this work we describe the profiling of a non-receptor tyrosine-protein kinase (TYK2) inhibitor which shows a functionally relevant potency shift between human and preclinical species (e.g. murine, dog, macaque) in both biochemical and cellular assays. Comparison of the structure and...
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