Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

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Malerich JP, Lam JS, Hart B, Fine RM, Klebansky B, Tanga MJ, D'Andrea A

Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7454-7. doi: 10.1016/j.bmcl.2010.10.026. Epub 2010 Oct 13.

PubMed ID

21106455 [ View in PubMed

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Abstract

Tyrosine kinase 2 (TYK2) is required for signaling of interleukin-23 (IL-23), which plays a key role in rheumatoid arthritis. Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibitory activity against the Janus associated kinases TYK2 and JAKs 1-3.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Ruxolitinib	Tyrosine-protein kinase JAK2	IC 50 (nM)	3	N/A	N/A	Details
Tofacitinib	Non-receptor tyrosine-protein kinase TYK2	Kd (nM)	620	N/A	N/A	Details
Tofacitinib	Tyrosine-protein kinase JAK2	Kd (nM)	5	N/A	N/A	Details
Tofacitinib	Tyrosine-protein kinase JAK3	Kd (nM)	2.2	N/A	N/A	Details