Table 1.

Kinase inhibitory activity of CH5183284/Debio 1347

ClassEnzymeIC50, nmol/L
Tyrosine kinaseFGFR19.3
FGFR27.6
FGFR322
FGFR4290
PDGFRβ560
FLT11,000
KDR2,100
ABL4,900
EPHA25,000
KIT5,500
SRC5,900
FLT36,400
TIE2>10,000
EGFR>10,000
MET>10,000
INSR>10,000
ALK>10,000
JAK2>10,000
HER2>10,000
EPHB2>10,000
RON>10,000
AXL>10,000
LTK>10,000
FAK>10,000
Serine/threonine kinaseRaf-1>10,000
MEK1>10,000
PKA>10,000
AKT1>10,000
PKACα>10,000
PKACβ1>10,000
PKACβ2>10,000
p38α>10,000
AurA>10,000
CDC2/CycB1>10,000
CHK1>10,000
CHK2>10,000
TBK1>10,000

NOTE: Detailed description of in vitro kinase inhibitory assays in the presence of CH5183284/Debio 1347 is presented in Materials and Methods.