Table 2.

Summary of TR-FRET assay (IC50, shaded region) and Biacore data (unshaded region) for SCH772984 binding to both active/inactive wild-type ERK1 and active/inactive ERK1G186D mutant, showing weaker binding for ERK1G186D

ActiveInactive
IC50 (nmol/L)KD (nmol/L)kon (M−1s−1) 106koff (s−1) 10−4t1/2 (min)KD (nM)kon (M−1s−1) 106koff (s−1) 10−4t1/2 (min)
ERK1 WT0.04 ± 0.020.491.24 ± 0.016.04 ± 0.01190.0751.55 ± 0.011.16 ± 0.001100
ERK1 G186D37 ± 14590aRapidRapid<0.01b141.36 ± 0.01187 ± 10.6
  • aSee Supplementary Fig. S3.

  • bUpper limit estimate based on detection limit of Biacore instrument.