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Tyrosine Kinase 2 (TYK2) Allosteric Inhibitors To Treat Autoimmune Diseases

Yu Chang, Shilin Xu, Ke Ding

J Med Chem. 2019 Oct 24;62(20):8951-8952.

PMID: 31603320

Abstract:

TYK2 is an emerging drug target for various human autoimmune diseases. However, discovery of selective TYK2 inhibitor over other JAK family members (i.e., JAK1, 2, 3) by targeting the catalytically active site (Janus Homologue 1 (JH1) domain) is challenging. This Viewpoint discusses the discovery of a series of N-methyl pyridazine-3-carboxamides as novel selective pseudokinase (JH2) domain binders of TYK2. A systematic structure-based optimization yielded a highly potent and selective allosteric TYK2 inhibitor candidate that is currently in phase III clinical trial for psoriasis.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
IAR42411949 Tyk2 active human Tyk2 active human Price
IAR42416387 Jak1 active human Jak1 active human Price
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