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GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases[1][2].

[1] Tasso B, et al. The Development of BTK Inhibitors: A Five-Year Update. Molecules. 2021 Dec 6;26(23):7411. DOI:10.3390/molecules26237411
[2] Brullo C, et al. Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective. Int J Mol Sci. 2021 Jul 16;22(14):7641. DOI:10.3390/ijms22147641