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GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].

SYK: 7.1 (pIC₅₀); LCK: 5.4 (pIC₅₀); LRRK2: 5.4 (pIC₅₀); GSK3β: 5.3 (pIC₅₀); JAK2: 5 (pIC₅₀); VEGFR2: 4.5 (pIC₅₀); Aurora B: <4.6 (pIC₅₀); Aurora A: <4.3 (pIC₅₀)

[1] Barker MD, et al. Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3458-3462. DOI:10.1016/j.bmcl.2018.09.022
[2] Ramirez Molina C, et al. GSK2646264, a spleen tyrosine kinase inhibitor, attenuates the release of histamine in ex vivo human skin. Br J Pharmacol. 2019 Apr;176(8):1135-1142. DOI:10.1111/bph.14610