Apoptosis Signal-regulating Kinase 1 (ASK1) is one of the key mediators of the cellular stress response and modulation of this pathway with the small molecule, ATP-competitive inhibitor Selonsertib is being tested in the clinic for the treatment of liver fibrosis. Inhibition of ASK1 may also be beneficial in the treatment of neurological diseases and to investigate the potential therapeutic value of modulating this pathway in the CNS we have identified novel brain-penetrant inhibitors following a structure based drug design approach. The results from this systematic optimization effort will be presented.

Discovery of potent, selective, and brain-penetrant apoptosis signal-regulating kinase 1 (ASK1) inhibitors

2019 Fall National Meeting

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