BMS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM). BMS-986165 potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional responses (IC50 range 2-14 nM). BMS-986165 was approximately 200-fold selective against JAK1/3-dependent signaling in IL-2-stimulated T cells and >3,000-fold selective over JAK2-dependent EPO-induced signaling in TF-1 cells.
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