Donated Chemical Probes

Selectivity data for probe ABT-724 and control A-769

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Primary results are shown as '% Ctrl', i.e. the negative control (DMSO) is equal 100% control and the positive control (control compound) is equal 0% control. For compounds showing less than 50% of control in the primary screening assay, a Kd will be determined. Note: It cannot be excluded that 0 % control values are due to assay artefacts.

View assay details

Jump to control KinomeScan data

ABT-724

HGNC target name	DiscoverX gene symbol of kinase	% Control	Compound Concentration [nM]
AAK1	AAK1	100.0	1000
ABL1	ABL1-phosphorylated	100.0	1000
ABL2	ABL2	100.0	1000
ACVR1	ACVR1	100.0	1000
ACVR1B	ACVR1B	85.0	1000
ACVR2A	ACVR2A	100.0	1000
ACVR2B	ACVR2B	100.0	1000
ACVRL1	ACVRL1	95.0	1000
COQ8A	ADCK3	98.0	1000
COQ8B	ADCK4	100.0	1000
AKT1	AKT1	90.0	1000
AKT2	AKT2	100.0	1000
AKT3	AKT3	100.0	1000
ALK	ALK(L1196M)	97.0	1000
PRKAA1	AMPK-alpha1	100.0	1000
PRKAA2	AMPK-alpha2	100.0	1000
ANKK1	ANKK1	100.0	1000
NUAK1	ARK5	89.0	1000
MAP3K5	ASK1	93.0	1000
MAP3K6	ASK2	98.0	1000
AURKA	AURKA	89.0	1000
AURKB	AURKB	18.0	1000
AURKC	AURKC	100.0	1000
AXL	AXL	100.0	1000
BMP2K	BIKE	100.0	1000
BLK	BLK	100.0	1000
BMPR1A	BMPR1A	86.0	1000
BMPR1B	BMPR1B	100.0	1000
BMPR2	BMPR2	100.0	1000
BMX	BMX	100.0	1000
BRAF	BRAF(V600E)	100.0	1000
PTK6	BRK	100.0	1000
BRSK1	BRSK1	91.0	1000
BRSK2	BRSK2	100.0	1000
BTK	BTK	96.0	1000
BUB1	BUB1	100.0	1000
CAMK1	CAMK1	100.0	1000
PNCK	CAMK1B	0.0	1000
CAMK1D	CAMK1D	96.0	1000
CAMK1G	CAMK1G	100.0	1000
CAMK2A	CAMK2A	100.0	1000
CAMK2B	CAMK2B	100.0	1000
CAMK2D	CAMK2D	91.0	1000
CAMK2G	CAMK2G	100.0	1000
CAMK4	CAMK4	88.0	1000
CAMKK1	CAMKK1	98.0	1000
CAMKK2	CAMKK2	91.0	1000
CASK	CASK	97.0	1000
CDK11B	CDC2L1	100.0	1000
CDK11A	CDC2L2	100.0	1000
CDK13	CDC2L5	100.0	1000
CDK19	CDK11	87.0	1000
CDK2	CDK2	100.0	1000
CDK3	CDK3	100.0	1000
CDK4	CDK4-cyclinD3	100.0	1000
CDK5	CDK5	100.0	1000
CDK7	CDK7	48.0	1000
CDK8	CDK8	100.0	1000
CDK9	CDK9	100.0	1000
CDKL1	CDKL1	78.0	1000
CDKL2	CDKL2	100.0	1000
CDKL3	CDKL3	100.0	1000
CDKL5	CDKL5	100.0	1000
CHEK1	CHEK1	100.0	1000
CHEK2	CHEK2	100.0	1000
CIT	CIT	88.0	1000
CLK1	CLK1	100.0	1000
CLK2	CLK2	89.0	1000
CLK3	CLK3	100.0	1000
CLK4	CLK4	82.0	1000
CSF1R	CSF1R-autoinhibited	100.0	1000
CSK	CSK	100.0	1000
CSNK1A1	CSNK1A1	93.0	1000
CSNK1A1L	CSNK1A1L	100.0	1000
CSNK1D	CSNK1D	95.0	1000
CSNK1E	CSNK1E	100.0	1000
CSNK1G1	CSNK1G1	100.0	1000
CSNK1G2	CSNK1G2	100.0	1000
CSNK1G3	CSNK1G3	100.0	1000
CSNK2A1	CSNK2A1	97.0	1000
CSNK2A2	CSNK2A2	100.0	1000
MATK	CTK	100.0	1000
DAPK1	DAPK1	100.0	1000
DAPK2	DAPK2	86.0	1000
DAPK3	DAPK3	91.0	1000
DCLK1	DCAMKL1	100.0	1000
DCLK2	DCAMKL2	98.0	1000
DCLK3	DCAMKL3	93.0	1000
DDR1	DDR1	100.0	1000
DDR2	DDR2	100.0	1000
MAP3K12	DLK	97.0	1000
DMPK	DMPK	100.0	1000
CDC42BPG	DMPK2	100.0	1000
STK17A	DRAK1	100.0	1000
STK17B	DRAK2	100.0	1000
DYRK1A	DYRK1A	100.0	1000
DYRK1B	DYRK1B	100.0	1000
DYRK2	DYRK2	100.0	1000
EGFR	EGFR(T790M)	99.0	1000
EIF2AK1	EIF2AK1	100.0	1000
EPHA1	EPHA1	100.0	1000
EPHA2	EPHA2	100.0	1000
EPHA3	EPHA3	100.0	1000
EPHA4	EPHA4	100.0	1000
EPHA5	EPHA5	100.0	1000
EPHA6	EPHA6	100.0	1000
EPHA7	EPHA7	100.0	1000
EPHA8	EPHA8	100.0	1000
EPHB1	EPHB1	100.0	1000
EPHB2	EPHB2	98.0	1000
EPHB3	EPHB3	100.0	1000
EPHB4	EPHB4	100.0	1000
EPHB6	EPHB6	75.0	1000
ERBB2	ERBB2	78.0	1000
ERBB3	ERBB3	91.0	1000
ERBB4	ERBB4	95.0	1000
MAPK3	ERK1	100.0	1000
MAPK1	ERK2	100.0	1000
MAPK6	ERK3	100.0	1000
MAPK4	ERK4	100.0	1000
MAPK7	ERK5	100.0	1000
MAPK15	ERK8	100.0	1000
ERN1	ERN1	100.0	1000
PTK2	FAK	86.0	1000
FER	FER	100.0	1000
FES	FES	100.0	1000
FGFR1	FGFR1	100.0	1000
FGFR2	FGFR2	96.0	1000
FGFR3	FGFR3(G697C)	100.0	1000
FGFR4	FGFR4	93.0	1000
FGR	FGR	100.0	1000
FLT1	FLT1	100.0	1000
FLT3	FLT3-autoinhibited	100.0	1000
FLT4	FLT4	100.0	1000
FRK	FRK	100.0	1000
FYN	FYN	100.0	1000
GAK	GAK	100.0	1000
EIF2AK4	GCN2(Kin.Dom.2,S808G)	65.0	1000
GRK1	GRK1	92.0	1000
GRK2	GRK2	90.0	1000
GRK3	GRK3	67.0	1000
GRK4	GRK4	100.0	1000
GRK7	GRK7	100.0	1000
GSK3A	GSK3A	66.0	1000
GSK3B	GSK3B	93.0	1000
HASPIN	HASPIN	100.0	1000
HCK	HCK	100.0	1000
HIPK1	HIPK1	99.0	1000
HIPK2	HIPK2	26.0	1000
HIPK3	HIPK3	100.0	1000
HIPK4	HIPK4	91.0	1000
MAP4K1	HPK1	100.0	1000
HUNK	HUNK	100.0	1000
CILK1	ICK	100.0	1000
IGF1R	IGF1R	100.0	1000
CHUK	IKK-alpha	100.0	1000
IKBKB	IKK-beta	100.0	1000
IKBKE	IKK-epsilon	100.0	1000
INSR	INSR	100.0	1000
INSRR	INSRR	97.0	1000
IRAK1	IRAK1	100.0	1000
IRAK3	IRAK3	100.0	1000
IRAK4	IRAK4	100.0	1000
ITK	ITK	100.0	1000
JAK1	JAK1(JH2domain-pseudokinase)	76.0	1000
JAK2	JAK2(JH1domain-catalytic)	100.0	1000
JAK3	JAK3(JH1domain-catalytic)	100.0	1000
MAPK8	JNK1	100.0	1000
MAPK9	JNK2	100.0	1000
MAPK10	JNK3	100.0	1000
KIT	KIT-autoinhibited	100.0	1000
LATS1	LATS1	100.0	1000
LATS2	LATS2	75.0	1000
LCK	LCK	100.0	1000
LIMK1	LIMK1	100.0	1000
LIMK2	LIMK2	100.0	1000
STK11	LKB1	70.0	1000
STK10	LOK	100.0	1000
LRRK2	LRRK2(G2019S)	100.0	1000
LTK	LTK	100.0	1000
LYN	LYN	100.0	1000
MAP3K13	LZK	86.0	1000
MAK	MAK	100.0	1000
MAP3K1	MAP3K1	99.0	1000
MAP3K15	MAP3K15	100.0	1000
MAP3K2	MAP3K2	100.0	1000
MAP3K3	MAP3K3	100.0	1000
MAP3K4	MAP3K4	100.0	1000
MAP4K2	MAP4K2	100.0	1000
MAP4K3	MAP4K3	100.0	1000
MAP4K4	MAP4K4	100.0	1000
MAP4K5	MAP4K5	100.0	1000
MAPKAPK2	MAPKAPK2	100.0	1000
MAPKAPK5	MAPKAPK5	100.0	1000
MARK1	MARK1	100.0	1000
MARK2	MARK2	100.0	1000
MARK3	MARK3	100.0	1000
MARK4	MARK4	100.0	1000
MAST1	MAST1	65.0	1000
MAP2K1	MEK1	100.0	1000
MAP2K2	MEK2	100.0	1000
MAP2K3	MEK3	96.0	1000
MAP2K4	MEK4	100.0	1000
MAP2K5	MEK5	83.0	1000
MAP2K6	MEK6	100.0	1000
MELK	MELK	100.0	1000
MERTK	MERTK	90.0	1000
MET	MET(Y1235D)	100.0	1000
MINK1	MINK	100.0	1000
MAP2K7	MKK7	100.0	1000
MKNK1	MKNK1	91.0	1000
MKNK2	MKNK2	100.0	1000
MYLK3	MLCK	100.0	1000
MAP3K9	MLK1	100.0	1000
MAP3K10	MLK2	93.0	1000
MAP3K11	MLK3	100.0	1000
CDC42BPA	MRCKA	100.0	1000
CDC42BPB	MRCKB	100.0	1000
STK4	MST1	100.0	1000
MST1R	MST1R	100.0	1000
STK3	MST2	100.0	1000
STK24	MST3	100.0	1000
STK26	MST4	100.0	1000
MTOR	MTOR	100.0	1000
MUSK	MUSK	100.0	1000
MYLK	MYLK	80.0	1000
MYLK2	MYLK2	91.0	1000
MYLK4	MYLK4	97.0	1000
MYO3A	MYO3A	100.0	1000
MYO3B	MYO3B	95.0	1000
STK38	NDR1	89.0	1000
STK38L	NDR2	72.0	1000
NEK1	NEK1	100.0	1000
NEK10	NEK10	100.0	1000
NEK11	NEK11	100.0	1000
NEK2	NEK2	100.0	1000
NEK3	NEK3	100.0	1000
NEK4	NEK4	100.0	1000
NEK5	NEK5	100.0	1000
NEK6	NEK6	100.0	1000
NEK7	NEK7	100.0	1000
NEK9	NEK9	100.0	1000
MAP3K14	NIK	94.0	1000
NIM1K	NIM1	100.0	1000
NLK	NLK	100.0	1000
OXSR1	OSR1	100.0	1000
MAPK14	p38-alpha	89.0	1000
MAPK11	p38-beta	88.0	1000
MAPK13	p38-delta	100.0	1000
MAPK12	p38-gamma	74.0	1000
PAK1	PAK1	94.0	1000
PAK2	PAK2	100.0	1000
PAK3	PAK3	100.0	1000
PAK4	PAK4	93.0	1000
PAK6	PAK6	100.0	1000
PAK5	PAK7	100.0	1000
CDK16	PCTK1	100.0	1000
CDK17	PCTK2	100.0	1000
CDK18	PCTK3	94.0	1000
PDGFRA	PDGFRA	100.0	1000
PDGFRB	PDGFRB	100.0	1000
PDPK1	PDPK1	89.0	1000
CDPK1	PFCDPK1(P.falciparum)	99.0	1000
PK5	PFPK5(P.falciparum)	100.0	1000
CDK15	PFTAIRE2	95.0	1000
CDK14	PFTK1	100.0	1000
PHKG1	PHKG1	100.0	1000
PHKG2	PHKG2	82.0	1000
PIK3C2B	PIK3C2B	85.0	1000
PIK3C2G	PIK3C2G	100.0	1000
PIK3CA	PIK3CA(Q546K)	100.0	1000
PIK3CB	PIK3CB	100.0	1000
PIK3CD	PIK3CD	69.0	1000
PIK3CG	PIK3CG	100.0	1000
PI4KB	PIK4CB	100.0	1000
PIKFYVE	PIKFYVE	100.0	1000
PIM1	PIM1	90.0	1000
PIM2	PIM2	85.0	1000
PIM3	PIM3	100.0	1000
PIP5K1A	PIP5K1A	79.0	1000
PIP5K1C	PIP5K1C	93.0	1000
PIP4K2B	PIP5K2B	100.0	1000
PIP4K2C	PIP5K2C	86.0	1000
PRKACA	PKAC-alpha	91.0	1000
PRKACB	PKAC-beta	93.0	1000
PKMYT1	PKMYT1	100.0	1000
PKN1	PKN1	88.0	1000
PKN2	PKN2	100.0	1000
PKNB	PKNB(M.tuberculosis)	87.0	1000
PLK1	PLK1	100.0	1000
PLK2	PLK2	100.0	1000
PLK3	PLK3	100.0	1000
PLK4	PLK4	99.0	1000
PRKCD	PRKCD	100.0	1000
PRKCE	PRKCE	100.0	1000
PRKCH	PRKCH	89.0	1000
PRKCI	PRKCI	97.0	1000
PRKCQ	PRKCQ	98.0	1000
PRKD1	PRKD1	95.0	1000
PRKD2	PRKD2	91.0	1000
PRKD3	PRKD3	100.0	1000
PRKG1	PRKG1	100.0	1000
PRKG2	PRKG2	100.0	1000
EIF2AK2	PRKR	100.0	1000
PRKX	PRKX	100.0	1000
PRPF4B	PRP4	57.0	1000
PTK2B	PYK2	100.0	1000
SIK3	QSK	91.0	1000
RAF1	RAF1	100.0	1000
RET	RET(V804M)	100.0	1000
RIOK1	RIOK1	86.0	1000
RIOK2	RIOK2	100.0	1000
RIOK3	RIOK3	100.0	1000
RIPK1	RIPK1	100.0	1000
RIPK2	RIPK2	100.0	1000
RIPK4	RIPK4	100.0	1000
DSTYK	RIPK5	100.0	1000
ROCK1	ROCK1	100.0	1000
ROCK2	ROCK2	100.0	1000
ROS1	ROS1	100.0	1000
RPS6KA4	RPS6KA4(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA5	RPS6KA5(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA1	RSK1(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA3	RSK2(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA2	RSK3(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA6	RSK4(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KB1	S6K1	97.0	1000
SBK1	SBK1	100.0	1000
SGK1	SGK	100.0	1000
SBK3	SgK110	100.0	1000
SGK2	SGK2	100.0	1000
SGK3	SGK3	100.0	1000
SIK1	SIK	100.0	1000
SIK2	SIK2	100.0	1000
SLK	SLK	93.0	1000
NUAK2	SNARK	100.0	1000
SNRK	SNRK	100.0	1000
SRC	SRC	93.0	1000
SRMS	SRMS	94.0	1000
SRPK1	SRPK1	100.0	1000
SRPK2	SRPK2	100.0	1000
SRPK3	SRPK3	100.0	1000
STK16	STK16	87.0	1000
STK33	STK33	97.0	1000
STK35	STK35	100.0	1000
STK36	STK36	84.0	1000
STK39	STK39	100.0	1000
SYK	SYK	100.0	1000
MAP3K7	TAK1	52.0	1000
TAOK1	TAOK1	100.0	1000
TAOK2	TAOK2	83.0	1000
TAOK3	TAOK3	86.0	1000
TBK1	TBK1	77.0	1000
TEC	TEC	100.0	1000
TESK1	TESK1	97.0	1000
TGFBR1	TGFBR1	97.0	1000
TGFBR2	TGFBR2	88.0	1000
TIE1	TIE1	96.0	1000
TEK	TIE2	94.0	1000
TLK1	TLK1	95.0	1000
TLK2	TLK2	100.0	1000
TNIK	TNIK	100.0	1000
TNK1	TNK1	59.0	1000
TNK2	TNK2	100.0	1000
TNNI3K	TNNI3K	100.0	1000
NTRK1	TRKA	100.0	1000
NTRK2	TRKB	100.0	1000
NTRK3	TRKC	87.0	1000
TRPM6	TRPM6	100.0	1000
TSSK1B	TSSK1B	100.0	1000
TSSK3	TSSK3	92.0	1000
TTK	TTK	100.0	1000
TXK	TXK	95.0	1000
TYK2	TYK2(JH2domain-pseudokinase)	100.0	1000
TYRO3	TYRO3	93.0	1000
ULK1	ULK1	100.0	1000
ULK2	ULK2	100.0	1000
ULK3	ULK3	100.0	1000
KDR	VEGFR2	100.0	1000
PIK3C3	VPS34	100.0	1000
VRK2	VRK2	100.0	1000
WEE1	WEE1	100.0	1000
WEE2	WEE2	100.0	1000
WNK1	WNK1	100.0	1000
WNK2	WNK2	100.0	1000
WNK3	WNK3	100.0	1000
WNK4	WNK4	100.0	1000
STK32A	YANK1	100.0	1000
STK32B	YANK2	100.0	1000
STK32C	YANK3	100.0	1000
YES1	YES	100.0	1000
STK25	YSK1	94.0	1000
MAP3K19	YSK4	100.0	1000
MAP3K20	ZAK	92.0	1000
ZAP70	ZAP70	100.0	1000

A-769

HGNC target name	DiscoverX gene symbol of kinase	% Control	Compound Concentration [nM]
AAK1	AAK1	100.0	1000
ABL1	ABL1-phosphorylated	78.0	1000
ABL2	ABL2	98.0	1000
ACVR1	ACVR1	100.0	1000
ACVR1B	ACVR1B	100.0	1000
ACVR2A	ACVR2A	69.0	1000
ACVR2B	ACVR2B	98.0	1000
ACVRL1	ACVRL1	100.0	1000
COQ8A	ADCK3	100.0	1000
COQ8B	ADCK4	100.0	1000
AKT1	AKT1	100.0	1000
AKT2	AKT2	98.0	1000
AKT3	AKT3	92.0	1000
ALK	ALK(L1196M)	100.0	1000
PRKAA1	AMPK-alpha1	83.0	1000
PRKAA2	AMPK-alpha2	100.0	1000
ANKK1	ANKK1	92.0	1000
NUAK1	ARK5	100.0	1000
MAP3K5	ASK1	98.0	1000
MAP3K6	ASK2	92.0	1000
AURKA	AURKA	74.0	1000
AURKB	AURKB	67.0	1000
AURKC	AURKC	100.0	1000
AXL	AXL	100.0	1000
BMP2K	BIKE	100.0	1000
BLK	BLK	96.0	1000
BMPR1A	BMPR1A	100.0	1000
BMPR1B	BMPR1B	80.0	1000
BMPR2	BMPR2	80.0	1000
BMX	BMX	100.0	1000
BRAF	BRAF(V600E)	85.0	1000
PTK6	BRK	88.0	1000
BRSK1	BRSK1	100.0	1000
BRSK2	BRSK2	100.0	1000
BTK	BTK	79.0	1000
BUB1	BUB1	90.0	1000
CAMK1	CAMK1	100.0	1000
PNCK	CAMK1B	100.0	1000
CAMK1D	CAMK1D	100.0	1000
CAMK1G	CAMK1G	100.0	1000
CAMK2A	CAMK2A	100.0	1000
CAMK2B	CAMK2B	100.0	1000
CAMK2D	CAMK2D	100.0	1000
CAMK2G	CAMK2G	100.0	1000
CAMK4	CAMK4	100.0	1000
CAMKK1	CAMKK1	100.0	1000
CAMKK2	CAMKK2	100.0	1000
CASK	CASK	100.0	1000
CDK11B	CDC2L1	100.0	1000
CDK11A	CDC2L2	100.0	1000
CDK13	CDC2L5	85.0	1000
CDK19	CDK11	96.0	1000
CDK2	CDK2	95.0	1000
CDK3	CDK3	100.0	1000
CDK4	CDK4-cyclinD3	82.0	1000
CDK5	CDK5	99.0	1000
CDK7	CDK7	61.0	1000
CDK8	CDK8	87.0	1000
CDK9	CDK9	97.0	1000
CDKL1	CDKL1	100.0	1000
CDKL2	CDKL2	84.0	1000
CDKL3	CDKL3	100.0	1000
CDKL5	CDKL5	76.0	1000
CHEK1	CHEK1	94.0	1000
CHEK2	CHEK2	96.0	1000
CIT	CIT	100.0	1000
CLK1	CLK1	80.0	1000
CLK2	CLK2	100.0	1000
CLK3	CLK3	85.0	1000
CLK4	CLK4	100.0	1000
CSF1R	CSF1R-autoinhibited	73.0	1000
CSK	CSK	100.0	1000
CSNK1A1	CSNK1A1	72.0	1000
CSNK1A1L	CSNK1A1L	100.0	1000
CSNK1D	CSNK1D	100.0	1000
CSNK1E	CSNK1E	91.0	1000
CSNK1G1	CSNK1G1	100.0	1000
CSNK1G2	CSNK1G2	99.0	1000
CSNK1G3	CSNK1G3	86.0	1000
CSNK2A1	CSNK2A1	81.0	1000
CSNK2A2	CSNK2A2	100.0	1000
MATK	CTK	45.0	1000
DAPK1	DAPK1	100.0	1000
DAPK2	DAPK2	100.0	1000
DAPK3	DAPK3	100.0	1000
DCLK1	DCAMKL1	82.0	1000
DCLK2	DCAMKL2	100.0	1000
DCLK3	DCAMKL3	100.0	1000
DDR1	DDR1	100.0	1000
DDR2	DDR2	89.0	1000
MAP3K12	DLK	74.0	1000
DMPK	DMPK	81.0	1000
CDC42BPG	DMPK2	100.0	1000
STK17A	DRAK1	98.0	1000
STK17B	DRAK2	100.0	1000
DYRK1A	DYRK1A	79.0	1000
DYRK1B	DYRK1B	91.0	1000
DYRK2	DYRK2	81.0	1000
EGFR	EGFR(T790M)	85.0	1000
EIF2AK1	EIF2AK1	93.0	1000
EPHA1	EPHA1	100.0	1000
EPHA2	EPHA2	100.0	1000
EPHA3	EPHA3	100.0	1000
EPHA4	EPHA4	100.0	1000
EPHA5	EPHA5	100.0	1000
EPHA6	EPHA6	100.0	1000
EPHA7	EPHA7	93.0	1000
EPHA8	EPHA8	95.0	1000
EPHB1	EPHB1	99.0	1000
EPHB2	EPHB2	99.0	1000
EPHB3	EPHB3	93.0	1000
EPHB4	EPHB4	100.0	1000
EPHB6	EPHB6	89.0	1000
ERBB2	ERBB2	88.0	1000
ERBB3	ERBB3	90.0	1000
ERBB4	ERBB4	83.0	1000
MAPK3	ERK1	99.0	1000
MAPK1	ERK2	93.0	1000
MAPK6	ERK3	100.0	1000
MAPK4	ERK4	100.0	1000
MAPK7	ERK5	100.0	1000
MAPK15	ERK8	82.0	1000
ERN1	ERN1	70.0	1000
PTK2	FAK	100.0	1000
FER	FER	100.0	1000
FES	FES	98.0	1000
FGFR1	FGFR1	100.0	1000
FGFR2	FGFR2	100.0	1000
FGFR3	FGFR3(G697C)	100.0	1000
FGFR4	FGFR4	89.0	1000
FGR	FGR	100.0	1000
FLT1	FLT1	100.0	1000
FLT3	FLT3-autoinhibited	91.0	1000
FLT4	FLT4	100.0	1000
FRK	FRK	92.0	1000
FYN	FYN	100.0	1000
GAK	GAK	99.0	1000
EIF2AK4	GCN2(Kin.Dom.2,S808G)	100.0	1000
GRK1	GRK1	100.0	1000
GRK2	GRK2	93.0	1000
GRK3	GRK3	31.0	1000
GRK4	GRK4	88.0	1000
GRK7	GRK7	87.0	1000
GSK3A	GSK3A	100.0	1000
GSK3B	GSK3B	78.0	1000
HASPIN	HASPIN	100.0	1000
HCK	HCK	82.0	1000
HIPK1	HIPK1	78.0	1000
HIPK2	HIPK2	62.0	1000
HIPK3	HIPK3	96.0	1000
HIPK4	HIPK4	100.0	1000
MAP4K1	HPK1	100.0	1000
HUNK	HUNK	100.0	1000
CILK1	ICK	68.0	1000
IGF1R	IGF1R	100.0	1000
CHUK	IKK-alpha	98.0	1000
IKBKB	IKK-beta	86.0	1000
IKBKE	IKK-epsilon	81.0	1000
INSR	INSR	85.0	1000
INSRR	INSRR	94.0	1000
IRAK1	IRAK1	73.0	1000
IRAK3	IRAK3	94.0	1000
IRAK4	IRAK4	74.0	1000
ITK	ITK	97.0	1000
JAK1	JAK1(JH2domain-pseudokinase)	80.0	1000
JAK2	JAK2(JH1domain-catalytic)	65.0	1000
JAK3	JAK3(JH1domain-catalytic)	100.0	1000
MAPK8	JNK1	77.0	1000
MAPK9	JNK2	68.0	1000
MAPK10	JNK3	66.0	1000
KIT	KIT-autoinhibited	72.0	1000
LATS1	LATS1	100.0	1000
LATS2	LATS2	94.0	1000
LCK	LCK	100.0	1000
LIMK1	LIMK1	100.0	1000
LIMK2	LIMK2	100.0	1000
STK11	LKB1	100.0	1000
STK10	LOK	87.0	1000
LRRK2	LRRK2(G2019S)	92.0	1000
LTK	LTK	89.0	1000
LYN	LYN	95.0	1000
MAP3K13	LZK	82.0	1000
MAK	MAK	100.0	1000
MAP3K1	MAP3K1	70.0	1000
MAP3K15	MAP3K15	67.0	1000
MAP3K2	MAP3K2	82.0	1000
MAP3K3	MAP3K3	83.0	1000
MAP3K4	MAP3K4	100.0	1000
MAP4K2	MAP4K2	100.0	1000
MAP4K3	MAP4K3	100.0	1000
MAP4K4	MAP4K4	95.0	1000
MAP4K5	MAP4K5	100.0	1000
MAPKAPK2	MAPKAPK2	80.0	1000
MAPKAPK5	MAPKAPK5	84.0	1000
MARK1	MARK1	100.0	1000
MARK2	MARK2	100.0	1000
MARK3	MARK3	98.0	1000
MARK4	MARK4	100.0	1000
MAST1	MAST1	100.0	1000
MAP2K1	MEK1	79.0	1000
MAP2K2	MEK2	70.0	1000
MAP2K3	MEK3	100.0	1000
MAP2K4	MEK4	89.0	1000
MAP2K5	MEK5	72.0	1000
MAP2K6	MEK6	100.0	1000
MELK	MELK	46.0	1000
MERTK	MERTK	80.0	1000
MET	MET(Y1235D)	89.0	1000
MINK1	MINK	89.0	1000
MAP2K7	MKK7	92.0	1000
MKNK1	MKNK1	98.0	1000
MKNK2	MKNK2	75.0	1000
MYLK3	MLCK	100.0	1000
MAP3K9	MLK1	100.0	1000
MAP3K10	MLK2	100.0	1000
MAP3K11	MLK3	100.0	1000
CDC42BPA	MRCKA	100.0	1000
CDC42BPB	MRCKB	100.0	1000
STK4	MST1	85.0	1000
MST1R	MST1R	100.0	1000
STK3	MST2	87.0	1000
STK24	MST3	100.0	1000
STK26	MST4	95.0	1000
MTOR	MTOR	100.0	1000
MUSK	MUSK	100.0	1000
MYLK	MYLK	94.0	1000
MYLK2	MYLK2	100.0	1000
MYLK4	MYLK4	100.0	1000
MYO3A	MYO3A	100.0	1000
MYO3B	MYO3B	100.0	1000
STK38	NDR1	88.0	1000
STK38L	NDR2	100.0	1000
NEK1	NEK1	100.0	1000
NEK10	NEK10	78.0	1000
NEK11	NEK11	79.0	1000
NEK2	NEK2	96.0	1000
NEK3	NEK3	88.0	1000
NEK4	NEK4	88.0	1000
NEK5	NEK5	100.0	1000
NEK6	NEK6	98.0	1000
NEK7	NEK7	100.0	1000
NEK9	NEK9	100.0	1000
MAP3K14	NIK	100.0	1000
NIM1K	NIM1	84.0	1000
NLK	NLK	100.0	1000
OXSR1	OSR1	78.0	1000
MAPK14	p38-alpha	100.0	1000
MAPK11	p38-beta	100.0	1000
MAPK13	p38-delta	100.0	1000
MAPK12	p38-gamma	98.0	1000
PAK1	PAK1	100.0	1000
PAK2	PAK2	100.0	1000
PAK3	PAK3	87.0	1000
PAK4	PAK4	100.0	1000
PAK6	PAK6	100.0	1000
PAK5	PAK7	97.0	1000
CDK16	PCTK1	81.0	1000
CDK17	PCTK2	100.0	1000
CDK18	PCTK3	100.0	1000
PDGFRA	PDGFRA	89.0	1000
PDGFRB	PDGFRB	100.0	1000
PDPK1	PDPK1	99.0	1000
CDPK1	PFCDPK1(P.falciparum)	89.0	1000
PK5	PFPK5(P.falciparum)	92.0	1000
CDK15	PFTAIRE2	100.0	1000
CDK14	PFTK1	100.0	1000
PHKG1	PHKG1	96.0	1000
PHKG2	PHKG2	100.0	1000
PIK3C2B	PIK3C2B	94.0	1000
PIK3C2G	PIK3C2G	95.0	1000
PIK3CA	PIK3CA(Q546K)	84.0	1000
PIK3CB	PIK3CB	74.0	1000
PIK3CD	PIK3CD	100.0	1000
PIK3CG	PIK3CG	64.0	1000
PI4KB	PIK4CB	73.0	1000
PIKFYVE	PIKFYVE	100.0	1000
PIM1	PIM1	100.0	1000
PIM2	PIM2	96.0	1000
PIM3	PIM3	94.0	1000
PIP5K1A	PIP5K1A	96.0	1000
PIP5K1C	PIP5K1C	100.0	1000
PIP4K2B	PIP5K2B	100.0	1000
PIP4K2C	PIP5K2C	81.0	1000
PRKACA	PKAC-alpha	92.0	1000
PRKACB	PKAC-beta	100.0	1000
PKMYT1	PKMYT1	100.0	1000
PKN1	PKN1	100.0	1000
PKN2	PKN2	62.0	1000
PKNB	PKNB(M.tuberculosis)	87.0	1000
PLK1	PLK1	78.0	1000
PLK2	PLK2	71.0	1000
PLK3	PLK3	80.0	1000
PLK4	PLK4	84.0	1000
PRKCD	PRKCD	100.0	1000
PRKCE	PRKCE	77.0	1000
PRKCH	PRKCH	100.0	1000
PRKCI	PRKCI	100.0	1000
PRKCQ	PRKCQ	100.0	1000
PRKD1	PRKD1	100.0	1000
PRKD2	PRKD2	100.0	1000
PRKD3	PRKD3	100.0	1000
PRKG1	PRKG1	100.0	1000
PRKG2	PRKG2	94.0	1000
EIF2AK2	PRKR	100.0	1000
PRKX	PRKX	100.0	1000
PRPF4B	PRP4	100.0	1000
PTK2B	PYK2	100.0	1000
SIK3	QSK	100.0	1000
RAF1	RAF1	91.0	1000
RET	RET(V804M)	100.0	1000
RIOK1	RIOK1	100.0	1000
RIOK2	RIOK2	100.0	1000
RIOK3	RIOK3	100.0	1000
RIPK1	RIPK1	100.0	1000
RIPK2	RIPK2	100.0	1000
RIPK4	RIPK4	66.0	1000
DSTYK	RIPK5	76.0	1000
ROCK1	ROCK1	93.0	1000
ROCK2	ROCK2	74.0	1000
ROS1	ROS1	100.0	1000
RPS6KA4	RPS6KA4(Kin.Dom.2-C-terminal)	73.0	1000
RPS6KA5	RPS6KA5(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA1	RSK1(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA3	RSK2(Kin.Dom.2-C-terminal)	77.0	1000
RPS6KA2	RSK3(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KA6	RSK4(Kin.Dom.2-C-terminal)	94.0	1000
RPS6KB1	S6K1	87.0	1000
SBK1	SBK1	99.0	1000
SGK1	SGK	82.0	1000
SBK3	SgK110	100.0	1000
SGK2	SGK2	81.0	1000
SGK3	SGK3	95.0	1000
SIK1	SIK	100.0	1000
SIK2	SIK2	100.0	1000
SLK	SLK	100.0	1000
NUAK2	SNARK	100.0	1000
SNRK	SNRK	100.0	1000
SRC	SRC	100.0	1000
SRMS	SRMS	100.0	1000
SRPK1	SRPK1	100.0	1000
SRPK2	SRPK2	59.0	1000
SRPK3	SRPK3	100.0	1000
STK16	STK16	100.0	1000
STK33	STK33	91.0	1000
STK35	STK35	100.0	1000
STK36	STK36	97.0	1000
STK39	STK39	100.0	1000
SYK	SYK	100.0	1000
MAP3K7	TAK1	74.0	1000
TAOK1	TAOK1	100.0	1000
TAOK2	TAOK2	95.0	1000
TAOK3	TAOK3	93.0	1000
TBK1	TBK1	100.0	1000
TEC	TEC	90.0	1000
TESK1	TESK1	100.0	1000
TGFBR1	TGFBR1	100.0	1000
TGFBR2	TGFBR2	99.0	1000
TIE1	TIE1	100.0	1000
TEK	TIE2	100.0	1000
TLK1	TLK1	100.0	1000
TLK2	TLK2	100.0	1000
TNIK	TNIK	100.0	1000
TNK1	TNK1	84.0	1000
TNK2	TNK2	100.0	1000
TNNI3K	TNNI3K	100.0	1000
NTRK1	TRKA	85.0	1000
NTRK2	TRKB	100.0	1000
NTRK3	TRKC	83.0	1000
TRPM6	TRPM6	100.0	1000
TSSK1B	TSSK1B	100.0	1000
TSSK3	TSSK3	98.0	1000
TTK	TTK	98.0	1000
TXK	TXK	100.0	1000
TYK2	TYK2(JH2domain-pseudokinase)	84.0	1000
TYRO3	TYRO3	100.0	1000
ULK1	ULK1	88.0	1000
ULK2	ULK2	94.0	1000
ULK3	ULK3	81.0	1000
KDR	VEGFR2	89.0	1000
PIK3C3	VPS34	94.0	1000
VRK2	VRK2	75.0	1000
WEE1	WEE1	100.0	1000
WEE2	WEE2	100.0	1000
WNK1	WNK1	100.0	1000
WNK2	WNK2	100.0	1000
WNK3	WNK3	100.0	1000
WNK4	WNK4	91.0	1000
STK32A	YANK1	100.0	1000
STK32B	YANK2	100.0	1000
STK32C	YANK3	71.0	1000
YES1	YES	100.0	1000
STK25	YSK1	100.0	1000
MAP3K19	YSK4	72.0	1000
MAP3K20	ZAK	100.0	1000
ZAP70	ZAP70	99.0	1000

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ABT-724

The screen was done at 10 µM compound. Results are expressed as percent inhibition of control specific binding (mean values; n = 2). Shown are supplementary data from PMID: 15087502 (Table 5) .

Conclusion: Closest off-target is the 5-HT1A receptor (Ki =2780 ± 642 nM).

Target protein	HGNC name	% inhibition at 10 µM	Ki [nM]
A1	ADORA1	< 10.0
A2A	ADORA2A	28.0
A3	ADORA3	11.0
a 1		23.0
a 2		21.0
b 1	ADRB1	< 10.0
b 2	ADRB2	13.0
NE transporter	SLC6A2	< 10.0
AT1	AGTR1	< 10.0
AT2	AGTR2	< 10.0
ANP	NPPA	< 10.0
BZD (central)		< 10.0
BZD (peripheral)		< 10.0
Bombesin		< 10.0
B2	BDKRB2	< 10.0
CGRP	CALCA	< 10.0
CB1	CNR1	< 10.0
CB2	CNR2	< 10.0
CCKA (CCK1)	CCKAR	< 10.0
CCKB (CCK2)	CCKBR	17.0
D1	DRD1	24.0
D2	DRD2	< 10.0
D3	DRD3	< 10.0
D4	DRD4	99.0
D5	DRD5	< 10.0
DA transporter	SLC6A3	11.0
ETA	EDNRA	< 10.0
ETB	EDNRB	< 10.0
GABA		< 10.0
GAL1	GALR1	< 10.0
IL-8B (CXCR2)	CXCR2	< 10.0
TNF-a	TNF	< 10.0
CCR1	CCR1	< 10.0
H1	HRH1	17.0
H2	HRH2	< 10.0
ML1	MCOLN1	51.0
M1	CHRM1	< 10.0
M2	CHRM2	< 10.0
M3	CHRM3	< 10.0
M4	CHRM4	< 10.0
M5	CHRM5	< 10.0
NK1	TACR1	< 10.0
NK2	TACR2	15.0
NK3	TACR3	26.0
Y1	NPY1R	< 10.0
Y2	NPY2R	< 10.0
NT1 (NTS1)	NTSR1	< 10.0
delta	OPRD1	< 10.0
kappa	OPRK1	68.0
mu	OPRM1	51.0
ORL1	OPRL1	< 10.0
PACAP	ADCYAP1	< 10.0
PCP	PRCP	18.0
TXA2/PGH2	TBXA2R	< 10.0
PGI2	PTGIR	< 10.0
P2X		< 10.0
P2Y		< 10.0
5-HT1A	HTR1A	73.0	2780.00
5-HT1B	HTR1B	< 10.0
5-HT2A	HTR2A	< 10.0
5-HT2C	HTR2C	10.0
5-HT3	HTR3A	10.0
5-HT5A	HTR5A	21.0
5-HT6	HTR6	< 10.0
5-HT7	HTR7	< 10.0
s		< 10.0
Somatostatin		< 10.0
VIP1 (VPAC1)	VIPR1	< 10.0
V1A	AVPR1A	< 10.0
Ca2+ channel		< 10.0
K+V channel		< 10.0
SK+Ca channel		< 10.0
Na+ channel		< 10.0
Cl- channel		< 10.0

Selectivity data for probe ABT-724 and control A-769

PDSP data

DiscoverX KinomeScan data

ABT-724

A-769

Cerep ligand profiling

ABT-724