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Description: Deucravacitinib (BMS986165; Tyk2-IN-4) is a novel, highly potent, orally bioavailable, selective and allosteric inhibitor of TYK2 (tyrosine kinase 2) in Phase 3 clinical studies across multiple immune-mediated diseases such as psoriatic arthritis, lupus and inflammatory bowel disease. BMS-986165 is able to block Il-12, IL-23 and type I interferon signaling. BMS-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).
References: WO2018183649A1.; WO2018183656A1.; WO2014074661A1.
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