TABLE 2

Kinase selectivity profile of PF-3644022

IC50 values are shown for the kinases that were inhibited >50% at 1 μM PF-3644022 against a 200 human kinase selectivity panel (see Supplemental Table 1). CMGC includes the CDK, MAPK, GSK3, and CLK families of kinases. STE is named for yeast sterile-phenotype kinases. TK, tyrosine kinases; TKL, tyrosine kinase-like.

KinaseGroupIC50Selectivitya
nM-fold
MK2CAMK5
AMPKCAMK11723
BrSK1CAMK18737
BrSK2CAMK9018
CaMKIICAMK7014
DRAK1CAMK7114
MK3CAMK5310
MNK2CAMK14830
PhKγ2CAMK528106
Pim1CAMK8818
PRAKCAMK51
CDK1/cycBCMGC35471
CDK5/p35CMGC902180
ASK1STE6012
AxlTK42886
MerTK7615
RIPK2TKL590118
  • AMPK, AMP-activated protein kinase; BrSK1, brain Ser/Thr kinase 1; BrSK2, brain Ser/Thr kinase 2; CaMKII, calcium/calmodulin-dependent protein kinase type II; DRAK1, DAP kinase-related apoptosis-inducing protein kinase 1; MNK2, MAPK-interacting kinase 2; PhKγ2, phosphorylase kinase testis/liver γ 2; CDK1/cycB, cyclin-dependent kinase 1/cyclin B complex; CDK5/p35, cyclin-dependent kinase 5/p35 complex; ASK1, apoptosis signal-regulating kinase 1; RIPK2, receptor-interacting protein kinase 2.

  • a Fold selectivity was relative to MK2 IC50 value.