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Synonyms: BMS-986165 | BMS986165 | compound 11 [PMID: 31318208} | Sotyktu® | Tyk2-IN-4
deucravacitinib is an approved drug (FDA (2022), EMA (2023))
Compound class: Synthetic organic
Comment: Deucravacitinib (BMS-986165) is a selective, orally active, allosteric inhibitor of the Janus kinase family enzyme, tyrosine kinase 2 (TYK2) [2,5]. The deuteromethyl amide group confers selectivity by virtue of binding to a pocket in the TYK2 JH2 pseudokinase domain.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Burke JR, Cheng L, Gillooly KM, Strnad J, Zupa-Fernandez A, Catlett IM, Zhang Y, Heimrich EM, McIntyre KW, Cunningham MD et al.. (2019)
Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.
Sci Transl Med, 11 (502). DOI: 10.1126/scitranslmed.aaw1736 [PMID:31341059]
2. Chang Y, Xu S, Ding K. (2019)
Tyrosine Kinase 2 (TYK2) Allosteric Inhibitors To Treat Autoimmune Diseases.
J Med Chem, 62 (20): 8951-8952. [PMID:31603320]
3. Papp K, Gordon K, Thaçi D, Morita A, Gooderham M, Foley P, Girgis IG, Kundu S, Banerjee S. (2018)
Phase 2 Trial of Selective Tyrosine Kinase 2 Inhibition in Psoriasis.
N Engl J Med, 379 (14): 1313-1321. [PMID:30205746]
4. Schlapbach C, Conrad C. (2022)
TYK-ing all the boxes in psoriasis.
J Allergy Clin Immunol, 149 (6): 1936-1939. [PMID:35341877]
5. Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L et al.. (2019)
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
J Med Chem, 62 (20): 8973-8995. [PMID:31318208]