CNX-774 is an orally active and selective inhibitor of BTK with IC50 value of <1 nM.
Bruton’s tyrosine kinase (BTK) is an important enzyme in the B-cell antigen receptor (BCR) signaling pathway and also plays an important role in mast cell activation and B cell maturation.
CNX-774 is an orally active, irreversible and selective BTK inhibitor with IC50 value of <1 nM. CNX-774 formed covalent bond with the Cys481 residue within the ATP binding site of BTK. In cellular assays, CNX-774 inhibited BTK with IC50 values of 1-10 nM [1].
Reference:
[1]. Akinleye A, Chen Y, Mukhi N, et al. Ibrutinib and novel BTK inhibitors in clinical development. J Hematol Oncol, 2013, 6: 59.