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BAY-549

HGNC target name	DiscoverX gene symbol of kinase	% Control	Compound Concentration [nM]	Kd [nM]
AAK1	AAK1	99.0	100
ABL1	ABL1-phosphorylated	97.0	100
ABL2	ABL2	86.0	100
ACVR1	ACVR1	94.0	100
ACVR1B	ACVR1B	87.0	100
ACVR2A	ACVR2A	94.0	100
ACVR2B	ACVR2B	100.0	100
ACVRL1	ACVRL1	100.0	100
COQ8A	ADCK3	100.0	100
COQ8B	ADCK4	88.0	100
AKT1	AKT1	100.0	100
AKT2	AKT2	98.0	100
AKT3	AKT3	78.0	100
ALK	ALK(L1196M)	99.0	100
PRKAA1	AMPK-alpha1	100.0	100
PRKAA2	AMPK-alpha2	89.0	100
ANKK1	ANKK1	85.0	100
NUAK1	ARK5	91.0	100
MAP3K5	ASK1	98.0	100
MAP3K6	ASK2	100.0	100
AURKA	AURKA	94.0	100
AURKB	AURKB	82.0	100
AURKC	AURKC	72.0	100
AXL	AXL	93.0	100
BMP2K	BIKE	100.0	100
BLK	BLK	90.0	100
BMPR1A	BMPR1A	85.0	100
BMPR1B	BMPR1B	68.0	100
BMPR2	BMPR2	95.0	100
BMX	BMX	100.0	100
BRAF	BRAF(V600E)	98.0	100
PTK6	BRK	100.0	100
BRSK1	BRSK1	96.0	100
BRSK2	BRSK2	92.0	100
BTK	BTK	96.0	100
BUB1	BUB1	75.0	100
CAMK1	CAMK1	92.0	100
PNCK	CAMK1B	94.0	100
CAMK1D	CAMK1D	94.0	100
CAMK1G	CAMK1G	97.0	100
CAMK2A	CAMK2A	70.0	100
CAMK2B	CAMK2B	85.0	100
CAMK2D	CAMK2D	90.0	100
CAMK2G	CAMK2G	96.0	100
CAMK4	CAMK4	100.0	100
CAMKK1	CAMKK1	99.0	100
CAMKK2	CAMKK2	98.0	100
CASK	CASK	98.0	100
CDK11B	CDC2L1	80.0	100
CDK11A	CDC2L2	100.0	100
CDK13	CDC2L5	73.0	100
CDK19	CDK11	80.0	100
CDK2	CDK2	99.0	100
CDK3	CDK3	97.0	100
CDK4	CDK4-cyclinD3	100.0	100
CDK5	CDK5	94.0	100
CDK7	CDK7	91.0	100
CDK8	CDK8	69.0	100
CDK9	CDK9	78.0	100
CDKL1	CDKL1	100.0	100
CDKL2	CDKL2	93.0	100
CDKL3	CDKL3	100.0	100
CDKL5	CDKL5	73.0	100
CHEK1	CHEK1	100.0	100
CHEK2	CHEK2	89.0	100
CIT	CIT	100.0	100
CLK1	CLK1	83.0	100
CLK2	CLK2	86.0	100
CLK3	CLK3	91.0	100
CLK4	CLK4	86.0	100
CSF1R	CSF1R-autoinhibited	100.0	100
CSK	CSK	87.0	100
CSNK1A1	CSNK1A1	96.0	100
CSNK1A1L	CSNK1A1L	89.0	100
CSNK1D	CSNK1D	100.0	100
CSNK1E	CSNK1E	64.0	100
CSNK1G1	CSNK1G1	100.0	100
CSNK1G2	CSNK1G2	94.0	100
CSNK1G3	CSNK1G3	100.0	100
CSNK2A1	CSNK2A1	100.0	100
CSNK2A2	CSNK2A2	86.0	100
MATK	CTK	88.0	100
DAPK1	DAPK1	98.0	100
DAPK2	DAPK2	89.0	100
DAPK3	DAPK3	97.0	100
DCLK1	DCAMKL1	65.0	100
DCLK2	DCAMKL2	100.0	100
DCLK3	DCAMKL3	97.0	100
DDR1	DDR1	100.0	100
DDR2	DDR2	57.0	100
MAP3K12	DLK	98.0	100
DMPK	DMPK	56.0	100
CDC42BPG	DMPK2	68.0	100
STK17A	DRAK1	100.0	100
STK17B	DRAK2	100.0	100
DYRK1A	DYRK1A	88.0	100
DYRK1B	DYRK1B	100.0	100
DYRK2	DYRK2	100.0	100
EGFR	EGFR(T790M)	75.0	100
EIF2AK1	EIF2AK1	77.0	100
EPHA1	EPHA1	100.0	100
EPHA2	EPHA2	100.0	100
EPHA3	EPHA3	97.0	100
EPHA4	EPHA4	100.0	100
EPHA5	EPHA5	92.0	100
EPHA6	EPHA6	100.0	100
EPHA7	EPHA7	82.0	100
EPHA8	EPHA8	87.0	100
EPHB1	EPHB1	86.0	100
EPHB2	EPHB2	99.0	100
EPHB3	EPHB3	100.0	100
EPHB4	EPHB4	100.0	100
EPHB6	EPHB6	96.0	100
ERBB2	ERBB2	99.0	100
ERBB3	ERBB3	65.0	100
ERBB4	ERBB4	100.0	100
MAPK3	ERK1	90.0	100
MAPK1	ERK2	99.0	100
MAPK6	ERK3	95.0	100
MAPK4	ERK4	81.0	100
MAPK7	ERK5	82.0	100
MAPK15	ERK8	100.0	100
ERN1	ERN1	68.0	100
PTK2	FAK	100.0	100
FER	FER	100.0	100
FES	FES	100.0	100
FGFR1	FGFR1	100.0	100
FGFR2	FGFR2	100.0	100
FGFR3	FGFR3(G697C)	100.0	100
FGFR4	FGFR4	100.0	100
FGR	FGR	100.0	100
FLT1	FLT1	100.0	100
FLT3	FLT3-autoinhibited	75.0	100
FLT4	FLT4	98.0	100
FRK	FRK	100.0	100
FYN	FYN	100.0	100
GAK	GAK	100.0	100
EIF2AK4	GCN2(Kin.Dom.2,S808G)	100.0	100
GRK1	GRK1	82.0	100
GRK2	GRK2	98.0	100
GRK3	GRK3	78.0	100
GRK4	GRK4	100.0	100
GRK7	GRK7	68.0	100
GSK3A	GSK3A	95.0	100
GSK3B	GSK3B	98.0	100
HASPIN	HASPIN	61.0	100
HCK	HCK	100.0	100
HIPK1	HIPK1	100.0	100
HIPK2	HIPK2	90.0	100
HIPK3	HIPK3	92.0	100
HIPK4	HIPK4	100.0	100
MAP4K1	HPK1	73.0	100
HUNK	HUNK	100.0	100
CILK1	ICK	79.0	100
IGF1R	IGF1R	86.0	100
CHUK	IKK-alpha	66.0	100
IKBKB	IKK-beta	69.0	100
IKBKE	IKK-epsilon	93.0	100
INSR	INSR	80.0	100
INSRR	INSRR	91.0	100
IRAK1	IRAK1	90.0	100
IRAK3	IRAK3	85.0	100
IRAK4	IRAK4	85.0	100
ITK	ITK	81.0	100
JAK1	JAK1(JH2domain-pseudokinase)	84.0	100
JAK2	JAK2(JH1domain-catalytic)	75.0	100
JAK3	JAK3(JH1domain-catalytic)	92.0	100
MAPK8	JNK1	80.0	100
MAPK9	JNK2	93.0	100
MAPK10	JNK3	81.0	100
KIT	KIT-autoinhibited	77.0	100
LATS1	LATS1	42.0	100
LATS2	LATS2	0.7	100
LCK	LCK	100.0	100
LIMK1	LIMK1	87.0	100
LIMK2	LIMK2	79.0	100
STK11	LKB1	100.0	100
STK10	LOK	100.0	100
LRRK2	LRRK2(G2019S)	100.0	100
LTK	LTK	99.0	100
LYN	LYN	81.0	100
MAP3K13	LZK	81.0	100
MAK	MAK	84.0	100
MAP3K1	MAP3K1	82.0	100
MAP3K15	MAP3K15	94.0	100
MAP3K2	MAP3K2	89.0	100
MAP3K3	MAP3K3	99.0	100
MAP3K4	MAP3K4	100.0	100
MAP4K2	MAP4K2	69.0	100
MAP4K3	MAP4K3	91.0	100
MAP4K4	MAP4K4	94.0	100
MAP4K5	MAP4K5	93.0	100
MAPKAPK2	MAPKAPK2	100.0	100
MAPKAPK5	MAPKAPK5	81.0	100
MARK1	MARK1	82.0	100
MARK2	MARK2	100.0	100
MARK3	MARK3	74.0	100
MARK4	MARK4	100.0	100
MAST1	MAST1	100.0	100
MAP2K1	MEK1	81.0	100
MAP2K2	MEK2	91.0	100
MAP2K3	MEK3	100.0	100
MAP2K4	MEK4	99.0	100
MAP2K5	MEK5	82.0	100
MAP2K6	MEK6	99.0	100
MELK	MELK	57.0	100
MERTK	MERTK	100.0	100
MET	MET(Y1235D)	88.0	100
MINK1	MINK	100.0	100
MAP2K7	MKK7	67.0	100
MKNK1	MKNK1	100.0	100
MKNK2	MKNK2	90.0	100
MYLK3	MLCK	91.0	100
MAP3K9	MLK1	89.0	100
MAP3K10	MLK2	100.0	100
MAP3K11	MLK3	100.0	100
CDC42BPA	MRCKA	98.0	100
CDC42BPB	MRCKB	70.0	100
STK4	MST1	100.0	100
MST1R	MST1R	74.0	100
STK3	MST2	69.0	100
STK24	MST3	100.0	100
STK26	MST4	100.0	100
MTOR	MTOR	85.0	100
MUSK	MUSK	96.0	100
MYLK	MYLK	80.0	100
MYLK2	MYLK2	98.0	100
MYLK4	MYLK4	100.0	100
MYO3A	MYO3A	95.0	100
MYO3B	MYO3B	91.0	100
STK38	NDR1	89.0	100
STK38L	NDR2	87.0	100
NEK1	NEK1	96.0	100
NEK10	NEK10	75.0	100
NEK11	NEK11	75.0	100
NEK2	NEK2	97.0	100
NEK3	NEK3	75.0	100
NEK4	NEK4	90.0	100
NEK5	NEK5	97.0	100
NEK6	NEK6	99.0	100
NEK7	NEK7	100.0	100
NEK9	NEK9	96.0	100
MAP3K14	NIK	92.0	100
NIM1K	NIM1	75.0	100
NLK	NLK	100.0	100
OXSR1	OSR1	92.0	100
MAPK14	p38-alpha	100.0	100
MAPK11	p38-beta	97.0	100
MAPK13	p38-delta	89.0	100
MAPK12	p38-gamma	100.0	100
PAK1	PAK1	100.0	100
PAK2	PAK2	99.0	100
PAK3	PAK3	86.0	100
PAK4	PAK4	100.0	100
PAK6	PAK6	82.0	100
PAK5	PAK7	92.0	100
CDK16	PCTK1	99.0	100
CDK17	PCTK2	81.0	100
CDK18	PCTK3	100.0	100
PDGFRA	PDGFRA	84.0	100
PDGFRB	PDGFRB	83.0	100
PDPK1	PDPK1	100.0	100
CDPK1	PFCDPK1(P.falciparum)	91.0	100
PK5	PFPK5(P.falciparum)	72.0	100
CDK15	PFTAIRE2	76.0	100
CDK14	PFTK1	100.0	100
PHKG1	PHKG1	100.0	100
PHKG2	PHKG2	89.0	100
PIK3C2B	PIK3C2B	88.0	100
PIK3C2G	PIK3C2G	100.0	100
PIK3CA	PIK3CA(Q546K)	76.0	100
PIK3CB	PIK3CB	76.0	100
PIK3CD	PIK3CD	51.0	100
PIK3CG	PIK3CG	88.0	100
PI4KB	PIK4CB	97.0	100
PIKFYVE	PIKFYVE	98.0	100
PIM1	PIM1	100.0	100
PIM2	PIM2	100.0	100
PIM3	PIM3	100.0	100
PIP5K1A	PIP5K1A	68.0	100
PIP5K1C	PIP5K1C	78.0	100
PIP4K2B	PIP5K2B	90.0	100
PIP4K2C	PIP5K2C	100.0	100
PRKACA	PKAC-alpha	28.0	100
PRKACB	PKAC-beta	36.0	100
PKMYT1	PKMYT1	98.0	100
PKN1	PKN1	72.0	100
PKN2	PKN2	100.0	100
PKNB	PKNB(M.tuberculosis)	98.0	100
PLK1	PLK1	75.0	100
PLK2	PLK2	59.0	100
PLK3	PLK3	83.0	100
PLK4	PLK4	82.0	100
PRKCD	PRKCD	100.0	100
PRKCE	PRKCE	96.0	100
PRKCH	PRKCH	74.0	100
PRKCI	PRKCI	100.0	100
PRKCQ	PRKCQ	66.0	100
PRKD1	PRKD1	55.0	100
PRKD2	PRKD2	94.0	100
PRKD3	PRKD3	100.0	100
PRKG1	PRKG1	49.0	100
PRKG2	PRKG2	90.0	100
EIF2AK2	PRKR	100.0	100
PRKX	PRKX	77.0	100
PRPF4B	PRP4	89.0	100
PTK2B	PYK2	90.0	100
SIK3	QSK	100.0	100
RAF1	RAF1	75.0	100
RET	RET(V804M)	100.0	100
RIOK1	RIOK1	100.0	100
RIOK2	RIOK2	85.0	100
RIOK3	RIOK3	93.0	100
RIPK1	RIPK1	100.0	100
RIPK2	RIPK2	92.0	100
RIPK4	RIPK4	84.0	100
DSTYK	RIPK5	67.0	100
ROCK1	ROCK1	0.6	100
ROCK2	ROCK2	0.9	100
ROS1	ROS1	96.0	100
RPS6KA4	RPS6KA4(Kin.Dom.2-C-terminal)	83.0	100
RPS6KA5	RPS6KA5(Kin.Dom.2-C-terminal)	93.0	100
RPS6KA1	RSK1(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA3	RSK2(Kin.Dom.2-C-terminal)	73.0	100
RPS6KA2	RSK3(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA6	RSK4(Kin.Dom.2-C-terminal)	99.0	100
RPS6KB1	S6K1	85.0	100
SBK1	SBK1	94.0	100
SGK1	SGK	74.0	100
SBK3	SgK110	87.0	100
SGK2	SGK2	69.0	100
SGK3	SGK3	88.0	100
SIK1	SIK	98.0	100
SIK2	SIK2	100.0	100
SLK	SLK	97.0	100
NUAK2	SNARK	85.0	100
SNRK	SNRK	77.0	100
SRC	SRC	100.0	100
SRMS	SRMS	100.0	100
SRPK1	SRPK1	100.0	100
SRPK2	SRPK2	75.0	100
SRPK3	SRPK3	100.0	100
STK16	STK16	87.0	100
STK33	STK33	85.0	100
STK35	STK35	94.0	100
STK36	STK36	85.0	100
STK39	STK39	94.0	100
SYK	SYK	100.0	100
MAP3K7	TAK1	92.0	100
TAOK1	TAOK1	84.0	100
TAOK2	TAOK2	100.0	100
TAOK3	TAOK3	100.0	100
TBK1	TBK1	96.0	100
TEC	TEC	86.0	100
TESK1	TESK1	100.0	100
TGFBR1	TGFBR1	81.0	100
TGFBR2	TGFBR2	100.0	100
TIE1	TIE1	94.0	100
TEK	TIE2	95.0	100
TLK1	TLK1	100.0	100
TLK2	TLK2	95.0	100
TNIK	TNIK	100.0	100
TNK1	TNK1	100.0	100
TNK2	TNK2	95.0	100
TNNI3K	TNNI3K	98.0	100
NTRK1	TRKA	81.0	100
NTRK2	TRKB	94.0	100
NTRK3	TRKC	86.0	100
TRPM6	TRPM6	83.0	100
TSSK1B	TSSK1B	95.0	100
TSSK3	TSSK3	100.0	100
TTK	TTK	96.0	100
TXK	TXK	100.0	100
TYK2	TYK2(JH2domain-pseudokinase)	89.0	100
TYRO3	TYRO3	100.0	100
ULK1	ULK1	92.0	100
ULK2	ULK2	89.0	100
ULK3	ULK3	88.0	100
KDR	VEGFR2	81.0	100
PIK3C3	VPS34	67.0	100
VRK2	VRK2	76.0	100
WEE1	WEE1	100.0	100
WEE2	WEE2	91.0	100
WNK1	WNK1	90.0	100
WNK2	WNK2	96.0	100
WNK3	WNK3	90.0	100
WNK4	WNK4	100.0	100
STK32A	YANK1	86.0	100
STK32B	YANK2	71.0	100
STK32C	YANK3	93.0	100
YES1	YES	96.0	100
STK25	YSK1	100.0	100
MAP3K19	YSK4	74.0	100
MAP3K20	ZAK	100.0	100
ZAP70	ZAP70	100.0	100

BAY-4900

HGNC target name	DiscoverX gene symbol of kinase	% Control	Compound Concentration [nM]	Kd [nM]
AAK1	AAK1	100.0	100
ABL1	ABL1-phosphorylated	97.0	100
ABL2	ABL2	99.0	100
ACVR1	ACVR1	85.0	100
ACVR1B	ACVR1B	98.0	100
ACVR2A	ACVR2A	87.0	100
ACVR2B	ACVR2B	79.0	100
ACVRL1	ACVRL1	93.0	100
COQ8A	ADCK3	100.0	100
COQ8B	ADCK4	89.0	100
AKT1	AKT1	75.0	100
AKT2	AKT2	100.0	100
AKT3	AKT3	98.0	100
ALK	ALK(L1196M)	100.0	100
PRKAA1	AMPK-alpha1	100.0	100
PRKAA2	AMPK-alpha2	97.0	100
ANKK1	ANKK1	83.0	100
NUAK1	ARK5	96.0	100
MAP3K5	ASK1	97.0	100
MAP3K6	ASK2	100.0	100
AURKA	AURKA	100.0	100
AURKB	AURKB	78.0	100
AURKC	AURKC	97.0	100
AXL	AXL	100.0	100
BMP2K	BIKE	100.0	100
BLK	BLK	96.0	100
BMPR1A	BMPR1A	95.0	100
BMPR1B	BMPR1B	86.0	100
BMPR2	BMPR2	100.0	100
BMX	BMX	97.0	100
BRAF	BRAF(V600E)	100.0	100
PTK6	BRK	86.0	100
BRSK1	BRSK1	100.0	100
BRSK2	BRSK2	100.0	100
BTK	BTK	84.0	100
BUB1	BUB1	82.0	100
CAMK1	CAMK1	100.0	100
PNCK	CAMK1B	90.0	100
CAMK1D	CAMK1D	100.0	100
CAMK1G	CAMK1G	100.0	100
CAMK2A	CAMK2A	82.0	100
CAMK2B	CAMK2B	100.0	100
CAMK2D	CAMK2D	95.0	100
CAMK2G	CAMK2G	100.0	100
CAMK4	CAMK4	96.0	100
CAMKK1	CAMKK1	100.0	100
CAMKK2	CAMKK2	99.0	100
CASK	CASK	100.0	100
CDK11B	CDC2L1	100.0	100
CDK11A	CDC2L2	100.0	100
CDK13	CDC2L5	77.0	100
CDK19	CDK11	88.0	100
CDK2	CDK2	100.0	100
CDK3	CDK3	100.0	100
CDK4	CDK4-cyclinD3	100.0	100
CDK5	CDK5	100.0	100
CDK7	CDK7	100.0	100
CDK8	CDK8	97.0	100
CDK9	CDK9	100.0	100
CDKL1	CDKL1	100.0	100
CDKL2	CDKL2	100.0	100
CDKL3	CDKL3	96.0	100
CDKL5	CDKL5	78.0	100
CHEK1	CHEK1	100.0	100
CHEK2	CHEK2	94.0	100
CIT	CIT	100.0	100
CLK1	CLK1	96.0	100
CLK2	CLK2	87.0	100
CLK3	CLK3	91.0	100
CLK4	CLK4	100.0	100
CSF1R	CSF1R-autoinhibited	89.0	100
CSK	CSK	100.0	100
CSNK1A1	CSNK1A1	93.0	100
CSNK1A1L	CSNK1A1L	98.0	100
CSNK1D	CSNK1D	100.0	100
CSNK1E	CSNK1E	98.0	100
CSNK1G1	CSNK1G1	100.0	100
CSNK1G2	CSNK1G2	83.0	100
CSNK1G3	CSNK1G3	100.0	100
CSNK2A1	CSNK2A1	98.0	100
CSNK2A2	CSNK2A2	89.0	100
MATK	CTK	97.0	100
DAPK1	DAPK1	100.0	100
DAPK2	DAPK2	100.0	100
DAPK3	DAPK3	100.0	100
DCLK1	DCAMKL1	85.0	100
DCLK2	DCAMKL2	100.0	100
DCLK3	DCAMKL3	89.0	100
DDR1	DDR1	100.0	100
DDR2	DDR2	66.0	100
MAP3K12	DLK	100.0	100
DMPK	DMPK	86.0	100
CDC42BPG	DMPK2	100.0	100
STK17A	DRAK1	94.0	100
STK17B	DRAK2	84.0	100
DYRK1A	DYRK1A	98.0	100
DYRK1B	DYRK1B	82.0	100
DYRK2	DYRK2	100.0	100
EGFR	EGFR(T790M)	88.0	100
EIF2AK1	EIF2AK1	100.0	100
EPHA1	EPHA1	100.0	100
EPHA2	EPHA2	100.0	100
EPHA3	EPHA3	83.0	100
EPHA4	EPHA4	100.0	100
EPHA5	EPHA5	100.0	100
EPHA6	EPHA6	100.0	100
EPHA7	EPHA7	96.0	100
EPHA8	EPHA8	100.0	100
EPHB1	EPHB1	96.0	100
EPHB2	EPHB2	100.0	100
EPHB3	EPHB3	100.0	100
EPHB4	EPHB4	100.0	100
EPHB6	EPHB6	100.0	100
ERBB2	ERBB2	95.0	100
ERBB3	ERBB3	75.0	100
ERBB4	ERBB4	97.0	100
MAPK3	ERK1	98.0	100
MAPK1	ERK2	100.0	100
MAPK6	ERK3	100.0	100
MAPK4	ERK4	100.0	100
MAPK7	ERK5	100.0	100
MAPK15	ERK8	100.0	100
ERN1	ERN1	76.0	100
PTK2	FAK	100.0	100
FER	FER	100.0	100
FES	FES	100.0	100
FGFR1	FGFR1	100.0	100
FGFR2	FGFR2	98.0	100
FGFR3	FGFR3(G697C)	100.0	100
FGFR4	FGFR4	86.0	100
FGR	FGR	100.0	100
FLT1	FLT1	100.0	100
FLT3	FLT3-autoinhibited	83.0	100
FLT4	FLT4	96.0	100
FRK	FRK	81.0	100
FYN	FYN	80.0	100
GAK	GAK	100.0	100
EIF2AK4	GCN2(Kin.Dom.2,S808G)	100.0	100
GRK1	GRK1	92.0	100
GRK2	GRK2	81.0	100
GRK3	GRK3	83.0	100
GRK4	GRK4	100.0	100
GRK7	GRK7	82.0	100
GSK3A	GSK3A	99.0	100
GSK3B	GSK3B	90.0	100
HASPIN	HASPIN	74.0	100
HCK	HCK	100.0	100
HIPK1	HIPK1	100.0	100
HIPK2	HIPK2	100.0	100
HIPK3	HIPK3	80.0	100
HIPK4	HIPK4	100.0	100
MAP4K1	HPK1	82.0	100
HUNK	HUNK	100.0	100
CILK1	ICK	100.0	100
IGF1R	IGF1R	97.0	100
CHUK	IKK-alpha	85.0	100
IKBKB	IKK-beta	87.0	100
IKBKE	IKK-epsilon	100.0	100
INSR	INSR	90.0	100
INSRR	INSRR	100.0	100
IRAK1	IRAK1	95.0	100
IRAK3	IRAK3	97.0	100
IRAK4	IRAK4	90.0	100
ITK	ITK	97.0	100
JAK1	JAK1(JH2domain-pseudokinase)	83.0	100
JAK2	JAK2(JH1domain-catalytic)	72.0	100
JAK3	JAK3(JH1domain-catalytic)	94.0	100
MAPK8	JNK1	76.0	100
MAPK9	JNK2	86.0	100
MAPK10	JNK3	80.0	100
KIT	KIT-autoinhibited	78.0	100
LATS1	LATS1	69.0	100
LATS2	LATS2	91.0	100
LCK	LCK	100.0	100
LIMK1	LIMK1	90.0	100
LIMK2	LIMK2	100.0	100
STK11	LKB1	100.0	100
STK10	LOK	100.0	100
LRRK2	LRRK2(G2019S)	100.0	100
LTK	LTK	87.0	100
LYN	LYN	99.0	100
MAP3K13	LZK	99.0	100
MAK	MAK	97.0	100
MAP3K1	MAP3K1	76.0	100
MAP3K15	MAP3K15	84.0	100
MAP3K2	MAP3K2	79.0	100
MAP3K3	MAP3K3	90.0	100
MAP3K4	MAP3K4	100.0	100
MAP4K2	MAP4K2	81.0	100
MAP4K3	MAP4K3	100.0	100
MAP4K4	MAP4K4	86.0	100
MAP4K5	MAP4K5	91.0	100
MAPKAPK2	MAPKAPK2	100.0	100
MAPKAPK5	MAPKAPK5	100.0	100
MARK1	MARK1	100.0	100
MARK2	MARK2	100.0	100
MARK3	MARK3	83.0	100
MARK4	MARK4	100.0	100
MAST1	MAST1	100.0	100
MAP2K1	MEK1	90.0	100
MAP2K2	MEK2	100.0	100
MAP2K3	MEK3	94.0	100
MAP2K4	MEK4	80.0	100
MAP2K5	MEK5	100.0	100
MAP2K6	MEK6	100.0	100
MELK	MELK	89.0	100
MERTK	MERTK	90.0	100
MET	MET(Y1235D)	91.0	100
MINK1	MINK	93.0	100
MAP2K7	MKK7	84.0	100
MKNK1	MKNK1	100.0	100
MKNK2	MKNK2	90.0	100
MYLK3	MLCK	94.0	100
MAP3K9	MLK1	96.0	100
MAP3K10	MLK2	100.0	100
MAP3K11	MLK3	100.0	100
CDC42BPA	MRCKA	84.0	100
CDC42BPB	MRCKB	100.0	100
STK4	MST1	94.0	100
MST1R	MST1R	87.0	100
STK3	MST2	92.0	100
STK24	MST3	100.0	100
STK26	MST4	92.0	100
MTOR	MTOR	85.0	100
MUSK	MUSK	100.0	100
MYLK	MYLK	95.0	100
MYLK2	MYLK2	99.0	100
MYLK4	MYLK4	91.0	100
MYO3A	MYO3A	100.0	100
MYO3B	MYO3B	57.0	100
STK38	NDR1	87.0	100
STK38L	NDR2	100.0	100
NEK1	NEK1	100.0	100
NEK10	NEK10	66.0	100
NEK11	NEK11	85.0	100
NEK2	NEK2	100.0	100
NEK3	NEK3	91.0	100
NEK4	NEK4	84.0	100
NEK5	NEK5	100.0	100
NEK6	NEK6	100.0	100
NEK7	NEK7	100.0	100
NEK9	NEK9	100.0	100
MAP3K14	NIK	100.0	100
NIM1K	NIM1	93.0	100
NLK	NLK	100.0	100
OXSR1	OSR1	93.0	100
MAPK14	p38-alpha	100.0	100
MAPK11	p38-beta	100.0	100
MAPK13	p38-delta	95.0	100
MAPK12	p38-gamma	100.0	100
PAK1	PAK1	100.0	100
PAK2	PAK2	100.0	100
PAK3	PAK3	100.0	100
PAK4	PAK4	100.0	100
PAK6	PAK6	100.0	100
PAK5	PAK7	90.0	100
CDK16	PCTK1	100.0	100
CDK17	PCTK2	100.0	100
CDK18	PCTK3	100.0	100
PDGFRA	PDGFRA	98.0	100
PDGFRB	PDGFRB	96.0	100
PDPK1	PDPK1	61.0	100
CDPK1	PFCDPK1(P.falciparum)	88.0	100
PK5	PFPK5(P.falciparum)	68.0	100
CDK15	PFTAIRE2	94.0	100
CDK14	PFTK1	100.0	100
PHKG1	PHKG1	100.0	100
PHKG2	PHKG2	100.0	100
PIK3C2B	PIK3C2B	83.0	100
PIK3C2G	PIK3C2G	100.0	100
PIK3CA	PIK3CA(Q546K)	76.0	100
PIK3CB	PIK3CB	82.0	100
PIK3CD	PIK3CD	51.0	100
PIK3CG	PIK3CG	82.0	100
PI4KB	PIK4CB	100.0	100
PIKFYVE	PIKFYVE	91.0	100
PIM1	PIM1	100.0	100
PIM2	PIM2	88.0	100
PIM3	PIM3	100.0	100
PIP5K1A	PIP5K1A	70.0	100
PIP5K1C	PIP5K1C	93.0	100
PIP4K2B	PIP5K2B	76.0	100
PIP4K2C	PIP5K2C	96.0	100
PRKACA	PKAC-alpha	90.0	100
PRKACB	PKAC-beta	92.0	100
PKMYT1	PKMYT1	100.0	100
PKN1	PKN1	100.0	100
PKN2	PKN2	75.0	100
PKNB	PKNB(M.tuberculosis)	100.0	100
PLK1	PLK1	83.0	100
PLK2	PLK2	83.0	100
PLK3	PLK3	98.0	100
PLK4	PLK4	83.0	100
PRKCD	PRKCD	100.0	100
PRKCE	PRKCE	91.0	100
PRKCH	PRKCH	98.0	100
PRKCI	PRKCI	100.0	100
PRKCQ	PRKCQ	99.0	100
PRKD1	PRKD1	74.0	100
PRKD2	PRKD2	91.0	100
PRKD3	PRKD3	100.0	100
PRKG1	PRKG1	83.0	100
PRKG2	PRKG2	83.0	100
EIF2AK2	PRKR	100.0	100
PRKX	PRKX	100.0	100
PRPF4B	PRP4	81.0	100
PTK2B	PYK2	100.0	100
SIK3	QSK	100.0	100
RAF1	RAF1	91.0	100
RET	RET(V804M)	95.0	100
RIOK1	RIOK1	100.0	100
RIOK2	RIOK2	100.0	100
RIOK3	RIOK3	93.0	100
RIPK1	RIPK1	100.0	100
RIPK2	RIPK2	83.0	100
RIPK4	RIPK4	100.0	100
DSTYK	RIPK5	98.0	100
ROCK1	ROCK1	76.0	100
ROCK2	ROCK2	83.0	100
ROS1	ROS1	100.0	100
RPS6KA4	RPS6KA4(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA5	RPS6KA5(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA1	RSK1(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA3	RSK2(Kin.Dom.2-C-terminal)	79.0	100
RPS6KA2	RSK3(Kin.Dom.2-C-terminal)	100.0	100
RPS6KA6	RSK4(Kin.Dom.2-C-terminal)	100.0	100
RPS6KB1	S6K1	84.0	100
SBK1	SBK1	97.0	100
SGK1	SGK	80.0	100
SBK3	SgK110	65.0	100
SGK2	SGK2	86.0	100
SGK3	SGK3	90.0	100
SIK1	SIK	100.0	100
SIK2	SIK2	100.0	100
SLK	SLK	98.0	100
NUAK2	SNARK	85.0	100
SNRK	SNRK	86.0	100
SRC	SRC	92.0	100
SRMS	SRMS	100.0	100
SRPK1	SRPK1	85.0	100
SRPK2	SRPK2	78.0	100
SRPK3	SRPK3	100.0	100
STK16	STK16	100.0	100
STK33	STK33	100.0	100
STK35	STK35	99.0	100
STK36	STK36	93.0	100
STK39	STK39	100.0	100
SYK	SYK	100.0	100
MAP3K7	TAK1	100.0	100
TAOK1	TAOK1	97.0	100
TAOK2	TAOK2	100.0	100
TAOK3	TAOK3	100.0	100
TBK1	TBK1	100.0	100
TEC	TEC	100.0	100
TESK1	TESK1	100.0	100
TGFBR1	TGFBR1	93.0	100
TGFBR2	TGFBR2	90.0	100
TIE1	TIE1	100.0	100
TEK	TIE2	100.0	100
TLK1	TLK1	100.0	100
TLK2	TLK2	100.0	100
TNIK	TNIK	96.0	100
TNK1	TNK1	100.0	100
TNK2	TNK2	85.0	100
TNNI3K	TNNI3K	78.0	100
NTRK1	TRKA	74.0	100
NTRK2	TRKB	96.0	100
NTRK3	TRKC	76.0	100
TRPM6	TRPM6	77.0	100
TSSK1B	TSSK1B	100.0	100
TSSK3	TSSK3	100.0	100
TTK	TTK	100.0	100
TXK	TXK	100.0	100
TYK2	TYK2(JH2domain-pseudokinase)	85.0	100
TYRO3	TYRO3	80.0	100
ULK1	ULK1	93.0	100
ULK2	ULK2	100.0	100
ULK3	ULK3	85.0	100
KDR	VEGFR2	93.0	100
PIK3C3	VPS34	75.0	100
VRK2	VRK2	81.0	100
WEE1	WEE1	91.0	100
WEE2	WEE2	93.0	100
WNK1	WNK1	98.0	100
WNK2	WNK2	88.0	100
WNK3	WNK3	95.0	100
WNK4	WNK4	100.0	100
STK32A	YANK1	89.0	100
STK32B	YANK2	99.0	100
STK32C	YANK3	100.0	100
YES1	YES	93.0	100
STK25	YSK1	100.0	100
MAP3K19	YSK4	75.0	100
MAP3K20	ZAK	97.0	100
ZAP70	ZAP70	100.0	100

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BAY-549

The assay has been performed at 10 µM probe concentration.

Conclusion: Closest hits among the tested kinases are Trk-A with IC₅₀ = 252 nM, Flt3 with IC₅₀ = 303 nM and PKA with IC₅₀ = 734 nM. The other kinases with an inhibition > 50% have IC₅₀ values between 1 and 10 µM.

Target protein	HGNC name	Species	% inhibition at 10 µM	IC50 [nM]
Abl (h)	ABL1	Homo sapiens	14.0
Abl (m)	ABL1	Mus musculus	33.0
Abl(T315I) (h)	ABL1	Homo sapiens	28.0
ALK (h)	ALK	Homo sapiens	78.0
AMPK (r)		Rattus sp.	8.0
Arg (h)	ABL2	Homo sapiens	37.0
Arg (m)	ABL2	Mus musculus	36.0
Aurora A (h)	AURKA	Homo sapiens	77.0
Axl (h)	AXL	Homo sapiens	85.0
Blk (m)	BLK	Mus musculus	16.0
Bmx (h)	BMX	Homo sapiens	18.0
BTK (h)	BTK	Homo sapiens	1.0
CaMKII (r)	CAMK2G	Rattus sp.	7.0
CaMKIV (h)	CAMK4	Homo sapiens	-8.0
CDK1/ cyclin B (h)	CDK1	Homo sapiens	-22.0
CDK2/ cyclin A (h)	CDK2	Homo sapiens	20.0
CDK2/ cyclin E (h)	CDK2	Homo sapiens	40.0
CDK3/ cyclin E (h)	CDK3	Homo sapiens	33.0
CDK5/ p35 (h)	CDK5	Homo sapiens	7.0
CDK6/ cyclin D3 (h)	CDK6	Homo sapiens	9.0
CDK7/ cyclin H/ MATI (h)	CDK7	Homo sapiens	57.0
CHK1 (h)	CHEK1	Homo sapiens	9.0
CHK2 (h)	CHEK2	Homo sapiens	64.0
CK1delta (h)	CSNK1D	Homo sapiens	65.0
CK1 (y)	CSNK1A1	Saccharomyces cerevisiae	44.0
CK2 (h)	CSNK2A1	Homo sapiens	6.0
c-RAF (h)	RAF1	Homo sapiens	76.0
CSK (h)	CSK	Homo sapiens	-21.0
cSRC (h)	SRC	Homo sapiens	-4.0
EGFR (h)	EGFR	Homo sapiens	-15.0
EphA2 (h)	EPHA2	Homo sapiens	4.0
EphB2 (h)	EPHB2	Homo sapiens	-12.0
EphB4 (h)	EPHB4	Homo sapiens	-9.0
ErbB4 (h)	ERBB4	Homo sapiens	5.0
Fes (h)	FES	Homo sapiens	28.0
FGFR3 (h)	FGFR3	Homo sapiens	12.0
Fgr (h)	FGR	Homo sapiens	27.0
Flt3 (h)	FLT3	Homo sapiens	98.0	303.00
Fms (h)		Homo sapiens	64.0
Fyn (h)	FYN	Homo sapiens	14.0
GSK3alpha (h)	GSK3A	Homo sapiens	13.0
GSK3beta (h)	GSK3B	Homo sapiens	-1.0
IGF-1R (h)	IGF1R	Homo sapiens	41.0
IKKalpha (h)	CHUK	Homo sapiens	-41.0
IKKbeta (h)	IKBKB	Homo sapiens	-28.0
IR (h)	INSR	Homo sapiens	59.0
JNK1alpha1 (h)	MAPK8	Homo sapiens	22.0
JNK2alpha2 (h)	MAPK9	Homo sapiens	16.0
JNK3 (h)	MAPK10	Homo sapiens	8.0
Lck (h)	LCK	Homo sapiens	50.0
Lyn (m)	LYN	Mus musculus	4.0
Lyn (h)	LYN	Homo sapiens	31.0
MAPK1 (h)	MAPK1	Homo sapiens	1.0
MAPK2 (h)		Homo sapiens	17.0
MAPK2 (m)		Mus musculus	21.0
MAPKAP-K2 (h)	MAPKAPK2	Homo sapiens	-6.0
MEKI (h)	MAP2K1	Homo sapiens	9.0
Met (h)	MET	Homo sapiens	82.0
MKK4 (m)	MAP2K4	Mus musculus	-21.0
MKK6 (h)	MAP2K6	Homo sapiens	6.0
MKK7βbeta(h)	MAP2K7	Homo sapiens	20.0
MSK1 (h)	RPS6KA5	Homo sapiens	86.0
MST2 (h)	STK3	Homo sapiens	59.0
NEK2 (h)	NEK2	Homo sapiens	19.0
p70SK6 (h)	RPS6KB1	Homo sapiens	84.0
PAK2 (h)	PAK2	Homo sapiens	2.0
PAR-1Balpha (h)	MARK2	Homo sapiens	33.0
PDGFRalpha (h)	PDGFRA	Homo sapiens	3.0
PDGFRbeta (h)	PDGFRB	Homo sapiens	-28.0
PDK1 (h)	PDK1	Homo sapiens	28.0
Pim-1 (h)	PIM1	Homo sapiens	20.0
PKA (h)	PRKACA	Homo sapiens	95.0	734.00
PKBalpha (h)	AKT1	Homo sapiens	84.0
PKBbeta (h)	AKT2	Homo sapiens	85.0
PKBγgamma(h)	AKT3	Homo sapiens	87.0
PKCalpha (h)	PRKCA	Homo sapiens	6.0
PKCBI (h)	PRKCB	Homo sapiens	8.0
PKCBII(h)	PRKCB	Homo sapiens	9.0
PKCgamma (h)	PRKCG	Homo sapiens	33.0
PKCdelta (h)	PRKCD	Homo sapiens	16.0
PKCepsilon (h)	PRKCE	Homo sapiens	28.0
PKCeta (h)	PRKCH	Homo sapiens	24.0
PKCiota (h)	PRKCI	Homo sapiens	18.0
PKCmu (h)	PRKD1	Homo sapiens	60.0
PKCtheta (h)	PRKCQ	Homo sapiens	42.0
PKCzeta (h)	PRKCZ	Homo sapiens	-7.0
PKD2 (h)	PRKD2	Homo sapiens	28.0
PIK3 (h)		Homo sapiens	-3.0
PRAK (h)	MAPKAPK5	Homo sapiens	36.0
PRK2 (h)	PKN2	Homo sapiens	70.0
Ret (h)	RET	Homo sapiens	52.0
ROCK-2 (h)	ROCK2	Homo sapiens	100.0	1.00
ROCK-2 (r)	ROCK2	Rattus sp.	102.0	< 1.00
Ros (h)	ROS1	Homo sapiens	10.0
Rse (h)	TYRO3	Homo sapiens	15.0
Rsk1 (h)	RPS6KA1	Homo sapiens	72.0
Rsk1 (r)	RPS6KA1	Rattus sp.	79.0
Rsk2 (h)	RPS6KA3	Homo sapiens	61.0
Rsk3 (h)	RPS6KA2	Homo sapiens	48.0
SAPK2a (h)	MAPK14	Homo sapiens	21.0
SAPK2b (h)	MAPK11	Homo sapiens	1.0
SAPK3 (h)	MAPK12	Homo sapiens	4.0
SAPK4 (h)	MAPK13	Homo sapiens	16.0
SGK (h)	SGK1	Homo sapiens	76.0
Syk (h)	SYK	Homo sapiens	20.0
Tie2 (h)	TEK	Homo sapiens	26.0
TrkA (h)	NTRK1	Homo sapiens	99.0	252.00
TrkB (h)	NTRK2	Homo sapiens	84.0
Yes (h)	YES1	Homo sapiens	23.0
ZAP-70 (h)	ZAP70	Homo sapiens	-8.0

 

BAY-549

The measured results was calculated by the following formula:
PG (%)=100 x (Mean F_test - Mean F_time0)/(Mean F_ctrl - Mean F_time0)
If (Mean F_test - Mean F_time0) < 0, then
PG (%)= 100 x (Mean F_test - Mean F_time0)/(Mean F_time0 - Mean F_blank)
Where:

• PG: percent growth
• Mean F_time0 = The average of 2 measured fluorescent intensities of reduced alamarBlue at the time just before exposure of cells to the test substance.
• Mean F_test = The average of 2 measured fluorescent intensities of alamarBlue after 72-hour exposure of cells to the test substance.
• Mean F_ctrl = The average of 2 measured fluorescent intensities of alamarBlue after 72-hour incubation without the test substance.
• Mean F_blank = The average of 2 measured fluorescent intensities of alamarBlue in medium without cells after 72-hour incubation.

A decrease of 50 % or more (>= 50 %) in fluorescent intensity relative to vehicle-treated control indicated significant cell growth inhibition, cytostatic or cytotoxic activity, and a semi-quantitative IC₅₀, TGI and LC₅₀ were then determined by nonlinear regression using GraphPad Prism (GraphPad Software, USA).
IC₅₀ (50 % Inhibition Concentration): Test compound concentration where the increase from time0 in the number or mass of treated cells was only 50 % as much as the corresponding increase in the vehicle-control at the end of experiment.
TGI (Total Growth Inhibition): Test compound concentration where the number or mass of treated cells at the end of experiment was equal to that at time0.
LC₅₀ (50 % Lethal Concentration): Test compound concentration where the number or mass of treated cells at the end of experiment was half that at time0.

Conclusion: No significant anti-proliferative activity below 1 µM in the tested tumour cell lines.

Tumor type	Cell line	Species	IC50 [µM]	TGI [µM]	LC50 [µM]	Mean growth ± SEM [%] at 100 µM	Mean growth ± SEM [%] at 10 µM	Mean growth ± SEM [%] at 1 µM	Mean growth ± SEM [%] at 0.1 µM	Mean growth ± SEM [%] at 0.01 µM
Breast	MCF-7	Homo sapiens	11.00	100.00	100.00	6 ± 4	57 ± 2	87 ± 1	89 ± 9	92 ± 3
Breast	T-47D	Homo sapiens	2.90	15.00	75.00	-45 ± 2	-2 ± 4	86 ± 1	97 ± 8	106 ± 6
Colon	DLD-1	Homo sapiens	2.40	100.00	100.00	5 ± 1	24 ± 1	66 ± 4	94 ± 2	101.00
Colon	HT-29	Homo sapiens	2.90	19.00	100.00	-38 ± 9	10 ± 4	75 ± 1	95 ± 1	100 ± 8
Kidney	A-498	Homo sapiens	7.80	70.00	100.00	-1 ± 2	26 ± 2	98 ± 5	93 ± 5	99 ± 2
Kidney	ACHN	Homo sapiens	3.60	32.00	100.00	-25 ± 4	27.00	60 ± 10	106 ± 2	103 ± 1
Leukemia	1-IL-60	Homo sapiens	21.00	100.00	100.00	35 ± 2	53 ± 6	89 ± 5	88 ± 4	98 ± 4
Leukemia	K562	Homo sapiens	8.30	100.00	100.00	32 ± 6	42 ± 3	69 ± 4	92 ± 5	95 ± 7
Liver	HC-4	Homo sapiens	2.10	13.00	82.00	-56 ± 8	12 ± 8	59 ± 5	94 ± 1	102 ± 5
Liver	Hep 3B	Homo sapiens	1.30	45.00	100.00	-4 ± 5	11.00	51 ± 6	82 ± 3	90 ± 8
Liver	HepG2	Homo sapiens	3.10	54.00	100.00	-3 ± 6	18 ± 4	62 ± 2	95 ± 6	101 ± 4
Lung	A549	Homo sapiens	1.50	25.00	100.00	-15 ± 3	7 ± 2	42 ± 2	97 ± 4	103 ± 4
Lung	NCI-1-1460	Homo sapiens	1.10	11.00	100.00	-45 ± 12	2 ± 1	50 ± 2	82 ± 3	98 ± 1
Lung	PC-6	Homo sapiens	4.20	18.00	76.00	-65 ± 6	32 ± 7	70 ± 9	84 ± 5	105 ± 9
Lymphoma	H33HJ-JA1	Homo sapiens	100.00	100.00	100.00	80 ± 7	98 ± 1	97 ± 6	103 ± 5	96 ± 8
Lymphoma	U937	Homo sapiens	14.00	100.00	100.00	17 ± 5	56 ± 7	104 ± 2	103 ± 2	101 ± 1
Melanoma	B16-FO	Homo sapiens	12.00	36.00	100.00	-46 ± 5	53 ± 9	106 ± 1	94 ± 4	98 ± 5
Melanoma	SK-MEL-5	Homo sapiens	16.00	50.00	100.00	-32 ± 1	65 ± 6	98 ± 3	89 ± 8	106 ± 3
Neuroepithelioma	SK-N-MC	Homo sapiens	7.90	20.00	52.00	-72 ± 8	38 ± 3	98 ± 5	103 ± 4	103 ± 6
Pancreas	MIA PaCa-2	Homo sapiens	8.90	48.00	100.00	-23 ± 5	45.00	88 ± 3	98 ± 1	95 ± 3
Pancreas	PANC-1	Homo sapiens	11.00	45.00	100.00	-31 ± 9	55 ± 1	87 ± 2	86 ± 3	98 ± 8
Prostate	PC-3	Homo sapiens	9.40	100.00	100.00	29 ± 3	48 ± 1	58 ± 3	102 ± 5	97 ± 2
Skin	A431	Homo sapiens	5.50	31.00	100.00	-36 ± 5	35 ± 3	77 ± 3	103 ± 6	92 ± 9
Stomach	KATO III	Homo sapiens	3.20	100.00	100.00	19 ± 7	27 ± 7	66 ± 8	99 ± 11	98 ± 7