|
ABL(ABL1)
|
ponatinib, bosutinib, dasatinib, imatinib |
|
|
AKT1
|
GSK690693 |
|
|
AKT2
|
GSK690693 |
|
|
ALK
|
alectinib, crizotinib |
|
|
ALK[G1202R]
|
lorlatinib |
|
|
ALK[L1196M]
|
brigatinib, crizotinib |
|
|
AurA
(AURKA)
|
MK-5108, pan-Aurora inhibitors |
|
|
AurB(AURKB)／INCENP
*
|
MK-5108, pan-Aurora inhibitors |
|
|
AXL
|
crizotinib, sunitinib |
|
|
BMX
|
bosutinib, dasatinib |
|
|
BRAF
|
dabrafenib, vemurafenib |
|
|
BRK(PTK6)
*
|
ibrutinib |
|
|
BTK
*
|
ponatinib, ibrutinib, dasatinib |
|
|
BTK[non-activated]
|
ponatinib, ibrutinib, dasatinib |
|
|
BTK[C481S]
*
|
fenebrutinib |
|
|
BTK[C481S][non-activated]
|
fenebrutinib, ibrutinib |
|
|
BTK[T316A]
*
|
fenebrutinib, ibrutinib |
|
|
BTK[T316A][non-activated]
|
fenebrutinib, acalabrutinib |
|
|
BTK[T474I]
*
|
ARQ-531, ibrutinib |
|
|
BTK[T474I][non-activated]
|
ibrutinib |
|
|
BTK[T474S]
*
|
ARQ-531, ibrutinib |
|
|
BTK[T474S][non-activated]
|
ibrutinib |
|
|
CDK1(CDC2)／CycA2
|
staurosporine |
|
|
CDK2／CycA2
|
PHA-793887, dinaciclib |
|
|
CDK2／CycE1
|
SNS-032 |
|
|
CDK4／CycD1
|
dinaciclib |
|
|
CDK4／CycD3
|
dinaciclib, palbociclib, ribociclib, abemaciclib |
|
|
CDK5／p25
|
SNS-032, dinaciclib |
|
|
CDK6／CycD1
|
dinaciclib |
|
|
CDK7／CycH／MAT1
|
dinaciclib, pan-CDK inhibitors |
|
|
CDK8／CycC
|
staurosporine |
|
|
CDK9／CycK
|
PHA-739887, dinaciclib |
|
|
CDK9／CycT1
|
dinaciclib, pan-CDK inhibitors |
|
|
CDK9／CycT2
|
staurosporine, dinaciclib |
|
|
CHK1(CHEK1)
|
bosutinib, sunitinib |
|
|
DDR2
*
|
ponatinib, dasatinib, imatinib, sorafenib |
|
|
EGFR
|
afatinib, erlotinib, gefitinib |
|
|
EGFR[d746-750]
|
gefitinib, erlotinib, afatinib |
|
|
EGFR[d746-750／C797S]
|
gefitinib, erlotinib, afatinib |
|
|
EGFR[L858R]
|
afatinib |
|
|
EGFR[T790M]
|
afatinib |
|
|
EGFR[T790M／L858R]
|
osimertinib |
|
|
EPHA2
*
|
BMS-777607, dasatinib, staurosporine, |
|
|
FAK(PTK2)
|
crizotinib |
|
|
FGFR1
*
|
infigratinib, ponatinib |
|
|
FGFR1[non-activated]
|
infigratinib, ponatinib |
|
|
FGFR3
*
|
infigratinib, sunitinib |
|
|
FGFR4
|
infigratinib, sunitinib |
|
|
FLT3
*
|
imatinib, dasatinib |
|
|
FMS(CSF1R)[non-activated]
|
dasatinib |
|
|
FYN [isoform a]
|
dasatinib, ponatinib, regorafenib |
|
|
GCN2(EIF2AK4)
|
A-92 |
|
|
GSK3β(GSK3B)
|
abemaciclib, staurosporine |
|
|
HPK1(MAP4K1)
|
bosutinib |
|
|
IGF1R
*
|
GSK-1838705, staurosporine, cabozantinib |
|
|
IKKα(CHUK)
|
IKKβ inhibitor |
|
|
IKKα(CHUK)[inactive mutant]
|
IKKβ inhibitor |
|
|
IRAK4
|
crizotinib, sunitinib |
|
|
ITK
*
|
crizotinib, sunitinib |
|
|
JAK2
|
staurosporine |
No SPR Data
|
|
KDR(VEGFR2)
|
vandetanib |
|
|
KIT
*
|
pazopanib, masitinib, staurosporine |
|
|
LCK
|
ponatinib, regorafenib |
|
|
LYNa
|
ponatinib, regorafenib, tamatinib |
|
|
MAP2K1[inactive]
|
crizotinib, dasatinib, trametinib |
|
|
MAP3K5
|
staurosporine, bosutinib, sunitinib |
|
|
MER(MERTK)
|
BMS-777607 |
|
|
MET
|
crizotinib |
|
|
p38α(MAPK14)
|
sorafenib, p38 MAPK inhibitors |
|
|
p38α(MAPK14)[inactive]
|
sorafenib, p38 MAPK inhibitors |
|
|
PAK4
|
GSK690693, staurosporine, bosutinib |
|
|
PDGFRα(PDGFRA)
*
|
nintedanib, axitinib, crenolanib, gilteritinib |
|
|
PDGFRα(PDGFRA)[non-activated]
|
nintedanib, axitinib, crenolanib, gilteritinib |
|
|
PDGFRβ(PDGFRB)
*
|
nintedanib, axitinib, crenolanib, gilteritinib |
|
|
PDGFRβ(PDGFRB)[non-activated]
|
nintedanib, axitinib, crenolanib, gilteritinib |
|
|
PIK3CA[E542K]／PIK3R1
|
idelalisib |
|
|
PIK3CA[E545K]／PIK3R1
|
idelalisib |
|
|
PIK3CA[H1047R]／PIK3R1
|
idelalisib |
|
|
PIK3CA[P539R]／PIK3R1
|
idelalisib |
|
|
PIK3CA[R88Q]／PIK3R1
|
idelalisib |
|
|
PIK3CA／PIK3R1
|
pictilisib, dactolisib |
|
|
PIK3CB／PIK3R1
|
apitolisib |
|
|
PIK3CD／PIK3R1
|
idelalisib, duvelisib |
|
|
PIK3CG
|
apitolisib, dactolisib, duvelisib |
|
|
PKACα(PRKACA)
|
A-674563 |
|
|
PKN1
|
GSK690693 |
|
|
PLK1
|
GSK461364 |
|
|
PYK2(PTK2B)
*
|
crizotinib |
|
|
RAF1
(CRAF)
|
dabrafenib |
|
|
RET
|
ponatinib, regorafenib, vandetanib, dasatinib, sorafenib |
|
|
RET[G691S]
*
|
staurosporine |
|
|
RET[M918T]
*
|
staurosporine |
|
|
RET[S891A]
*
|
staurosporine |
|
|
RET[V804M]
*
|
staurosporine |
|
|
RET[V804M][non-activated]
|
staurosporine |
|
|
RET[Y791F]
*
|
staurosporine |
|
|
ROCK1
|
GSK-429286A |
|
|
SRC
|
A-770041, ponatinib, regorafenib |
|
|
SRPK1
|
staurosporine |
|
|
SYK
*
|
staurosporine |
|
|
SYK[non-activated]
|
staurosporine |
|
|
TGFβR1(TGFBR1)
|
SB 431542 |
|
|
TIE2(TEK)
*
|
ponatinib, vandetanib |
|
|
TNIK
|
bosutinib, sunitinib |
|
|
TRKA(NTRK1)
*
|
AZ23, ponatinib |
|
|
TRKA(NTRK1)[non-activated]
|
AZ23, ponatinib |
|
|
TRKB(NTRK2)
*
|
AZ23, ponatinib |
|
|
TRKB(NTRK2)[non-activated]
|
ponatinib |
|
|
TRKC(NTRK3)
*
|
AZ23, sorafenib |
|
|
TYRO3
*
|
BMS-777607 |
|
|
TYRO3[non-activated]
|
BMS-777607 |
|
|
WEE1
|
AZD1775 |
|
|
YES(YES1)
|
staurosporine, saracatinib |
|
