CNX-774 is an irreversible, orally active, and highly selective inhibitor of Bruton’s tyrosine kinase (BTK) and can be used for the treatment of rheumatoid arthritis (RA).
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].
[1]. akinleye a, chen y, mukhi n, et al. ibrutinib and novel btk inhibitors in clinical development. j hematol oncol, 2013, 6: 59.
