TABLE 1

Potency and selectivity profile of RN486 in enzymatic assays

BtkSLKTECFGRITKABL1YESLCKJAK1
Kd. μM0.000310.0430.0640.10.240.290.380.865.1
Selectivity11392063237749351226277416,452
  • TEC, Tec nonreceptor kinase; FGR, tyrosine-protein kinase Fgr; ITK, IL2-inducible T-cell kinase; ABL-1, c-abl oncogene 1, nonreceptor tyrosine kinase; YES, Yamaguchi sarcoma viral (v-yes) oncogene homolog 1 (kinase); LCK, lymphocyte-specific protein tyrosine kinase.