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Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM).

Deucravacitinib (BMS-986165) 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂，用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活，可抑制IL-12/23和 I 型IFN 途径。它选择性结合 TYK2 假激酶 (JH2) 结构域，IC50为1.0 nM。