Donated Chemical Probes

Selectivity data for probe BAY-386 and control BAY-448

BAY-386

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)	Ki [nM] (Secondary experimental value)	pKi
5-HT1A	HTR1A	14.71
5-HT1B	HTR1B	30.84
5-HT1D	HTR1D	5.17
5-HT5A	HTR5A	10.03
5-HT6	HTR6	2.78
D2	DRD2	-0.71
D3	DRD3	5.09
Sigma 1	SIGMAR1	40.26
Sigma 2	TMEM97	67.73	1203.22 average (n=2)	5.94
D1	DRD1	3.20
5-HT2B	HTR2B	17.07
5-HT2C	HTR2C	-4.94
5-HT3	HTR3A	-15.80
5-HT7A	HTR7	-0.77
Alpha2A	ADRA2A	-0.34
Alpha2B	ADRA2B	2.41
Alpha2C	ADRA2C	11.61
DAT	SLC6A3	0.01
DOR	OPRD1	-2.63
H1	HRH1	-5.32
H3	HRH3	-6.71
KOR	OPRK1	1.29
M1	CHRM1	2.07
M2	CHRM2	-9.14
M5	CHRM5	4.10
MOR	OPRM1	-4.38
NET	SLC6A2	-1.24
GABA/PBR		14.95
SERT	SLC6A4	8.68
5-HT2A	HTR2A	10.54
H2	HRH2	9.25
H4	HRH4	-4.72
5-HT1E	HTR1E	-20.33
Beta1	ADRB1	-29.99
Beta3	ADRB3	-18.14
D4	DRD4	5.24
Alpha1A	ADRA1A	-5.00
Alpha1B	ADRA1B	14.15
Alpha1D	ADRA1D	2.45
D5	DRD5	9.95
M3	CHRM3	-2.11
M4	CHRM4	-17.01
Beta2	ADRB2	11.80
GABAA		-2.64
GABAA/BZP		-7.39

BAY-448

Compound concentration: 10 µM

Receptor	HGNC target name	Inhibition [%] (Primary experimental value)
Beta1	ADRB1	3.66
Beta3	ADRB3	19.29
GABA/PBR		7.20
GABAA/BZP		3.61
Alpha1A	ADRA1A	-4.12
Alpha1B	ADRA1B	-1.18
Alpha1D	ADRA1D	-1.84
Alpha2A	ADRA2A	6.96
Alpha2B	ADRA2B	-2.77
Sigma 1	SIGMAR1	-18.38
Sigma 2	TMEM97	42.39
5-HT1A	HTR1A	-4.52
5-HT1B	HTR1B	4.16
5-HT1D	HTR1D	-9.27
5-HT1E	HTR1E	21.52
5-HT2A	HTR2A	-2.96
5-HT2B	HTR2B	16.83
5-HT6	HTR6	27.70
5-HT7A	HTR7	21.75
D2	DRD2	-0.15
D3	DRD3	-2.97
5-HT2C	HTR2C	37.07
5-HT3	HTR3A	12.85
5-HT5A	HTR5A	-14.58
Beta2	ADRB2	23.99
D1	DRD1	10.59
DOR	OPRD1	-0.62
H1	HRH1	11.54
H2	HRH2	-11.85
H3	HRH3	5.78
M1	CHRM1	-7.31
M2	CHRM2	39.47
M3	CHRM3	-1.45
M4	CHRM4	-0.58
M5	CHRM5	-1.71
SERT	SLC6A4	5.57
D4	DRD4	6.30
D5	DRD5	22.61
DAT	SLC6A3	5.46
H4	HRH4	-2.74
KOR	OPRK1	7.69
MOR	OPRM1	2.23
NET	SLC6A2	-20.16
Alpha2C	ADRA2C	10.52
GABAA		28.42

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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.

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Jump to control KinomeScan data

BAY-386

HGNC target name	DiscoverX gene symbol of kinase	% Control	Compound Concentration [nM]
AAK1	AAK1	99.0	1000
ABL1	ABL1-phosphorylated	92.0	1000
ABL2	ABL2	100.0	1000
ACVR1	ACVR1	100.0	1000
ACVR1B	ACVR1B	100.0	1000
ACVR2A	ACVR2A	98.0	1000
ACVR2B	ACVR2B	86.0	1000
ACVRL1	ACVRL1	100.0	1000
COQ8A	ADCK3	100.0	1000
COQ8B	ADCK4	73.0	1000
AKT1	AKT1	96.0	1000
AKT2	AKT2	90.0	1000
AKT3	AKT3	100.0	1000
ALK	ALK(L1196M)	65.0	1000
PRKAA1	AMPK-alpha1	100.0	1000
PRKAA2	AMPK-alpha2	100.0	1000
ANKK1	ANKK1	100.0	1000
NUAK1	ARK5	97.0	1000
MAP3K5	ASK1	100.0	1000
MAP3K6	ASK2	91.0	1000
AURKA	AURKA	100.0	1000
AURKB	AURKB	100.0	1000
AURKC	AURKC	99.0	1000
AXL	AXL	100.0	1000
BMP2K	BIKE	97.0	1000
BLK	BLK	100.0	1000
BMPR1A	BMPR1A	89.0	1000
BMPR1B	BMPR1B	82.0	1000
BMPR2	BMPR2	100.0	1000
BMX	BMX	100.0	1000
BRAF	BRAF(V600E)	100.0	1000
PTK6	BRK	100.0	1000
BRSK1	BRSK1	100.0	1000
BRSK2	BRSK2	100.0	1000
BTK	BTK	100.0	1000
BUB1	BUB1	100.0	1000
CAMK1	CAMK1	100.0	1000
PNCK	CAMK1B	100.0	1000
CAMK1D	CAMK1D	91.0	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	91.0	1000
CAMKK1	CAMKK1	100.0	1000
CAMKK2	CAMKK2	100.0	1000
CASK	CASK	100.0	1000
CDK11B	CDC2L1	100.0	1000
CDK11A	CDC2L2	0.0	1000
CDK13	CDC2L5	100.0	1000
CDK19	CDK11	100.0	1000
CDK2	CDK2	100.0	1000
CDK3	CDK3	96.0	1000
CDK4	CDK4-cyclinD3	88.0	1000
CDK5	CDK5	83.0	1000
CDK7	CDK7	100.0	1000
CDK8	CDK8	100.0	1000
CDK9	CDK9	100.0	1000
CDKL1	CDKL1	100.0	1000
CDKL2	CDKL2	100.0	1000
CDKL3	CDKL3	93.0	1000
CDKL5	CDKL5	100.0	1000
CHEK1	CHEK1	100.0	1000
CHEK2	CHEK2	100.0	1000
CIT	CIT	100.0	1000
CLK1	CLK1	98.0	1000
CLK2	CLK2	100.0	1000
CLK3	CLK3	100.0	1000
CLK4	CLK4	100.0	1000
CSF1R	CSF1R-autoinhibited	100.0	1000
CSK	CSK	100.0	1000
CSNK1A1	CSNK1A1	100.0	1000
CSNK1A1L	CSNK1A1L	100.0	1000
CSNK1D	CSNK1D	100.0	1000
CSNK1E	CSNK1E	100.0	1000
CSNK1G1	CSNK1G1	100.0	1000
CSNK1G2	CSNK1G2	89.0	1000
CSNK1G3	CSNK1G3	100.0	1000
CSNK2A1	CSNK2A1	100.0	1000
CSNK2A2	CSNK2A2	100.0	1000
MATK	CTK	100.0	1000
DAPK1	DAPK1	92.0	1000
DAPK2	DAPK2	100.0	1000
DAPK3	DAPK3	100.0	1000
DCLK1	DCAMKL1	100.0	1000
DCLK2	DCAMKL2	0.0	1000
DCLK3	DCAMKL3	100.0	1000
DDR1	DDR1	100.0	1000
DDR2	DDR2	100.0	1000
MAP3K12	DLK	0.0	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	93.0	1000
DYRK2	DYRK2	100.0	1000
EGFR	EGFR(T790M)	100.0	1000
EIF2AK1	EIF2AK1	90.0	1000
EPHA1	EPHA1	100.0	1000
EPHA2	EPHA2	100.0	1000
EPHA3	EPHA3	100.0	1000
EPHA4	EPHA4	100.0	1000
EPHA5	EPHA5	96.0	1000
EPHA6	EPHA6	100.0	1000
EPHA7	EPHA7	96.0	1000
EPHA8	EPHA8	100.0	1000
EPHB1	EPHB1	100.0	1000
EPHB2	EPHB2	100.0	1000
EPHB3	EPHB3	100.0	1000
EPHB4	EPHB4	100.0	1000
EPHB6	EPHB6	100.0	1000
ERBB2	ERBB2	100.0	1000
ERBB3	ERBB3	100.0	1000
ERBB4	ERBB4	95.0	1000
MAPK3	ERK1	94.0	1000
MAPK1	ERK2	95.0	1000
MAPK6	ERK3	100.0	1000
MAPK4	ERK4	100.0	1000
MAPK7	ERK5	100.0	1000
MAPK15	ERK8	100.0	1000
ERN1	ERN1	96.0	1000
PTK2	FAK	93.0	1000
FER	FER	100.0	1000
FES	FES	100.0	1000
FGFR1	FGFR1	100.0	1000
FGFR2	FGFR2	94.0	1000
FGFR3	FGFR3(G697C)	100.0	1000
FGFR4	FGFR4	100.0	1000
FGR	FGR	100.0	1000
FLT1	FLT1	100.0	1000
FLT3	FLT3-autoinhibited	81.0	1000
FLT4	FLT4	100.0	1000
FRK	FRK	100.0	1000
FYN	FYN	80.0	1000
GAK	GAK	100.0	1000
EIF2AK4	GCN2(Kin.Dom.2,S808G)	100.0	1000
GRK1	GRK1	92.0	1000
GRK2	GRK2	66.0	1000
GRK3	GRK3	100.0	1000
GRK4	GRK4	100.0	1000
GRK7	GRK7	100.0	1000
GSK3A	GSK3A	100.0	1000
GSK3B	GSK3B	100.0	1000
HASPIN	HASPIN	95.0	1000
HCK	HCK	100.0	1000
HIPK1	HIPK1	100.0	1000
HIPK2	HIPK2	100.0	1000
HIPK3	HIPK3	100.0	1000
HIPK4	HIPK4	85.0	1000
MAP4K1	HPK1	100.0	1000
HUNK	HUNK	100.0	1000
CILK1	ICK	100.0	1000
IGF1R	IGF1R	100.0	1000
CHUK	IKK-alpha	97.0	1000
IKBKB	IKK-beta	77.0	1000
IKBKE	IKK-epsilon	100.0	1000
INSR	INSR	94.0	1000
INSRR	INSRR	97.0	1000
IRAK1	IRAK1	92.0	1000
IRAK3	IRAK3	100.0	1000
IRAK4	IRAK4	80.0	1000
ITK	ITK	100.0	1000
JAK1	JAK1(JH2domain-pseudokinase)	100.0	1000
JAK2	JAK2(JH1domain-catalytic)	75.0	1000
JAK3	JAK3(JH1domain-catalytic)	100.0	1000
MAPK8	JNK1	82.0	1000
MAPK9	JNK2	84.0	1000
MAPK10	JNK3	79.0	1000
KIT	KIT-autoinhibited	100.0	1000
LATS1	LATS1	100.0	1000
LATS2	LATS2	100.0	1000
LCK	LCK	100.0	1000
LIMK1	LIMK1	100.0	1000
LIMK2	LIMK2	95.0	1000
STK11	LKB1	92.0	1000
STK10	LOK	100.0	1000
LRRK2	LRRK2(G2019S)	100.0	1000
LTK	LTK	100.0	1000
LYN	LYN	85.0	1000
MAP3K13	LZK	98.0	1000
MAK	MAK	100.0	1000
MAP3K1	MAP3K1	100.0	1000
MAP3K15	MAP3K15	100.0	1000
MAP3K2	MAP3K2	100.0	1000
MAP3K3	MAP3K3	100.0	1000
MAP3K4	MAP3K4	83.0	1000
MAP4K2	MAP4K2	94.0	1000
MAP4K3	MAP4K3	100.0	1000
MAP4K4	MAP4K4	100.0	1000
MAP4K5	MAP4K5	100.0	1000
MAPKAPK2	MAPKAPK2	100.0	1000
MAPKAPK5	MAPKAPK5	94.0	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	91.0	1000
MAP2K2	MEK2	100.0	1000
MAP2K3	MEK3	100.0	1000
MAP2K4	MEK4	95.0	1000
MAP2K5	MEK5	100.0	1000
MAP2K6	MEK6	100.0	1000
MELK	MELK	100.0	1000
MERTK	MERTK	100.0	1000
MET	MET(Y1235D)	100.0	1000
MINK1	MINK	99.0	1000
MAP2K7	MKK7	100.0	1000
MKNK1	MKNK1	100.0	1000
MKNK2	MKNK2	94.0	1000
MYLK3	MLCK	79.0	1000
MAP3K9	MLK1	100.0	1000
MAP3K10	MLK2	99.0	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	97.0	1000
STK26	MST4	94.0	1000
MTOR	MTOR	100.0	1000
MUSK	MUSK	100.0	1000
MYLK	MYLK	100.0	1000
MYLK2	MYLK2	100.0	1000
MYLK4	MYLK4	100.0	1000
MYO3A	MYO3A	100.0	1000
MYO3B	MYO3B	89.0	1000
STK38	NDR1	100.0	1000
STK38L	NDR2	100.0	1000
NEK1	NEK1	100.0	1000
NEK10	NEK10	81.0	1000
NEK11	NEK11	100.0	1000
NEK2	NEK2	100.0	1000
NEK3	NEK3	100.0	1000
NEK4	NEK4	100.0	1000
NEK5	NEK5	98.0	1000
NEK6	NEK6	98.0	1000
NEK7	NEK7	100.0	1000
NEK9	NEK9	100.0	1000
MAP3K14	NIK	87.0	1000
NIM1K	NIM1	93.0	1000
NLK	NLK	100.0	1000
OXSR1	OSR1	100.0	1000
MAPK14	p38-alpha	100.0	1000
MAPK11	p38-beta	100.0	1000
MAPK13	p38-delta	100.0	1000
MAPK12	p38-gamma	100.0	1000
PAK1	PAK1	100.0	1000
PAK2	PAK2	90.0	1000
PAK3	PAK3	100.0	1000
PAK4	PAK4	100.0	1000
PAK6	PAK6	100.0	1000
PAK5	PAK7	100.0	1000
CDK16	PCTK1	100.0	1000
CDK17	PCTK2	98.0	1000
CDK18	PCTK3	0.0	1000
PDGFRA	PDGFRA	100.0	1000
PDGFRB	PDGFRB	100.0	1000
PDPK1	PDPK1	94.0	1000
CDPK1	PFCDPK1(P.falciparum)	92.0	1000
PK5	PFPK5(P.falciparum)	100.0	1000
CDK15	PFTAIRE2	100.0	1000
CDK14	PFTK1	100.0	1000
PHKG1	PHKG1	94.0	1000
PHKG2	PHKG2	100.0	1000
PIK3C2B	PIK3C2B	100.0	1000
PIK3C2G	PIK3C2G	93.0	1000
PIK3CA	PIK3CA(Q546K)	83.0	1000
PIK3CB	PIK3CB	66.0	1000
PIK3CD	PIK3CD	97.0	1000
PIK3CG	PIK3CG	100.0	1000
PI4KB	PIK4CB	100.0	1000
PIKFYVE	PIKFYVE	100.0	1000
PIM1	PIM1	100.0	1000
PIM2	PIM2	100.0	1000
PIM3	PIM3	100.0	1000
PIP5K1A	PIP5K1A	100.0	1000
PIP5K1C	PIP5K1C	100.0	1000
PIP4K2B	PIP5K2B	73.0	1000
PIP4K2C	PIP5K2C	96.0	1000
PRKACA	PKAC-alpha	100.0	1000
PRKACB	PKAC-beta	100.0	1000
PKMYT1	PKMYT1	100.0	1000
PKN1	PKN1	100.0	1000
PKN2	PKN2	100.0	1000
PKNB	PKNB(M.tuberculosis)	100.0	1000
PLK1	PLK1	91.0	1000
PLK2	PLK2	100.0	1000
PLK3	PLK3	98.0	1000
PLK4	PLK4	100.0	1000
PRKCD	PRKCD	100.0	1000
PRKCE	PRKCE	97.0	1000
PRKCH	PRKCH	100.0	1000
PRKCI	PRKCI	100.0	1000
PRKCQ	PRKCQ	86.0	1000
PRKD1	PRKD1	100.0	1000
PRKD2	PRKD2	100.0	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	97.0	1000
PTK2B	PYK2	99.0	1000
SIK3	QSK	77.0	1000
RAF1	RAF1	100.0	1000
RET	RET(V804M)	100.0	1000
RIOK1	RIOK1	100.0	1000
RIOK2	RIOK2	100.0	1000
RIOK3	RIOK3	85.0	1000
RIPK1	RIPK1	100.0	1000
RIPK2	RIPK2	90.0	1000
RIPK4	RIPK4	97.0	1000
DSTYK	RIPK5	100.0	1000
ROCK1	ROCK1	94.0	1000
ROCK2	ROCK2	98.0	1000
ROS1	ROS1	100.0	1000
RPS6KA4	RPS6KA4(Kin.Dom.2-C-terminal)	82.0	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	100.0	1000
SBK1	SBK1	90.0	1000
SGK1	SGK	91.0	1000
SBK3	SgK110	98.0	1000
SGK2	SGK2	76.0	1000
SGK3	SGK3	100.0	1000
SIK1	SIK	99.0	1000
SIK2	SIK2	100.0	1000
SLK	SLK	100.0	1000
NUAK2	SNARK	100.0	1000
SNRK	SNRK	93.0	1000
SRC	SRC	97.0	1000
SRMS	SRMS	100.0	1000
SRPK1	SRPK1	100.0	1000
SRPK2	SRPK2	100.0	1000
SRPK3	SRPK3	100.0	1000
STK16	STK16	100.0	1000
STK33	STK33	99.0	1000
STK35	STK35	100.0	1000
STK36	STK36	100.0	1000
STK39	STK39	100.0	1000
SYK	SYK	100.0	1000
MAP3K7	TAK1	100.0	1000
TAOK1	TAOK1	100.0	1000
TAOK2	TAOK2	100.0	1000
TAOK3	TAOK3	100.0	1000
TBK1	TBK1	94.0	1000
TEC	TEC	100.0	1000
TESK1	TESK1	100.0	1000
TGFBR1	TGFBR1	100.0	1000
TGFBR2	TGFBR2	100.0	1000
TIE1	TIE1	100.0	1000
TEK	TIE2	100.0	1000
TLK1	TLK1	94.0	1000
TLK2	TLK2	100.0	1000
TNIK	TNIK	75.0	1000
TNK1	TNK1	100.0	1000
TNK2	TNK2	97.0	1000
TNNI3K	TNNI3K	100.0	1000
NTRK1	TRKA	87.0	1000
NTRK2	TRKB	94.0	1000
NTRK3	TRKC	100.0	1000
TRPM6	TRPM6	100.0	1000
TSSK1B	TSSK1B	95.0	1000
TSSK3	TSSK3	100.0	1000
TTK	TTK	82.0	1000
TXK	TXK	100.0	1000
TYK2	TYK2(JH2domain-pseudokinase)	94.0	1000
TYRO3	TYRO3	98.0	1000
ULK1	ULK1	100.0	1000
ULK2	ULK2	75.0	1000
ULK3	ULK3	93.0	1000
KDR	VEGFR2	88.0	1000
PIK3C3	VPS34	100.0	1000
VRK2	VRK2	90.0	1000
WEE1	WEE1	100.0	1000
WEE2	WEE2	100.0	1000
WNK1	WNK1	100.0	1000
WNK2	WNK2	73.0	1000
WNK3	WNK3	99.0	1000
WNK4	WNK4	100.0	1000
STK32A	YANK1	89.0	1000
STK32B	YANK2	100.0	1000
STK32C	YANK3	93.0	1000
YES1	YES	96.0	1000
STK25	YSK1	93.0	1000
MAP3K19	YSK4	58.0	1000
MAP3K20	ZAK	100.0	1000
ZAP70	ZAP70	90.0	1000

BAY-448

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	100.0	1000
ACVR2A	ACVR2A	100.0	1000
ACVR2B	ACVR2B	100.0	1000
ACVRL1	ACVRL1	100.0	1000
COQ8A	ADCK3	91.0	1000
COQ8B	ADCK4	100.0	1000
AKT1	AKT1	90.0	1000
AKT2	AKT2	96.0	1000
AKT3	AKT3	100.0	1000
ALK	ALK(L1196M)	100.0	1000
PRKAA1	AMPK-alpha1	100.0	1000
PRKAA2	AMPK-alpha2	66.0	1000
ANKK1	ANKK1	100.0	1000
NUAK1	ARK5	100.0	1000
MAP3K5	ASK1	100.0	1000
MAP3K6	ASK2	92.0	1000
AURKA	AURKA	85.0	1000
AURKB	AURKB	100.0	1000
AURKC	AURKC	100.0	1000
AXL	AXL	100.0	1000
BMP2K	BIKE	100.0	1000
BLK	BLK	100.0	1000
BMPR1A	BMPR1A	100.0	1000
BMPR1B	BMPR1B	100.0	1000
BMPR2	BMPR2	100.0	1000
BMX	BMX	100.0	1000
BRAF	BRAF(V600E)	89.0	1000
PTK6	BRK	100.0	1000
BRSK1	BRSK1	100.0	1000
BRSK2	BRSK2	100.0	1000
BTK	BTK	96.0	1000
BUB1	BUB1	100.0	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	95.0	1000
CAMKK1	CAMKK1	100.0	1000
CAMKK2	CAMKK2	100.0	1000
CASK	CASK	93.0	1000
CDK11B	CDC2L1	100.0	1000
CDK11A	CDC2L2	100.0	1000
CDK13	CDC2L5	96.0	1000
CDK19	CDK11	100.0	1000
CDK2	CDK2	100.0	1000
CDK3	CDK3	100.0	1000
CDK4	CDK4-cyclinD3	100.0	1000
CDK5	CDK5	100.0	1000
CDK7	CDK7	89.0	1000
CDK8	CDK8	100.0	1000
CDK9	CDK9	100.0	1000
CDKL1	CDKL1	100.0	1000
CDKL2	CDKL2	100.0	1000
CDKL3	CDKL3	81.0	1000
CDKL5	CDKL5	100.0	1000
CHEK1	CHEK1	100.0	1000
CHEK2	CHEK2	100.0	1000
CIT	CIT	98.0	1000
CLK1	CLK1	100.0	1000
CLK2	CLK2	100.0	1000
CLK3	CLK3	100.0	1000
CLK4	CLK4	83.0	1000
CSF1R	CSF1R-autoinhibited	100.0	1000
CSK	CSK	100.0	1000
CSNK1A1	CSNK1A1	70.0	1000
CSNK1A1L	CSNK1A1L	100.0	1000
CSNK1D	CSNK1D	100.0	1000
CSNK1E	CSNK1E	100.0	1000
CSNK1G1	CSNK1G1	100.0	1000
CSNK1G2	CSNK1G2	100.0	1000
CSNK1G3	CSNK1G3	100.0	1000
CSNK2A1	CSNK2A1	86.0	1000
CSNK2A2	CSNK2A2	90.0	1000
MATK	CTK	100.0	1000
DAPK1	DAPK1	100.0	1000
DAPK2	DAPK2	100.0	1000
DAPK3	DAPK3	100.0	1000
DCLK1	DCAMKL1	75.0	1000
DCLK2	DCAMKL2	100.0	1000
DCLK3	DCAMKL3	100.0	1000
DDR1	DDR1	100.0	1000
DDR2	DDR2	74.0	1000
MAP3K12	DLK	92.0	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	76.0	1000
DYRK2	DYRK2	100.0	1000
EGFR	EGFR(T790M)	77.0	1000
EIF2AK1	EIF2AK1	100.0	1000
EPHA1	EPHA1	89.0	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	100.0	1000
EPHB3	EPHB3	100.0	1000
EPHB4	EPHB4	100.0	1000
EPHB6	EPHB6	73.0	1000
ERBB2	ERBB2	100.0	1000
ERBB3	ERBB3	100.0	1000
ERBB4	ERBB4	100.0	1000
MAPK3	ERK1	100.0	1000
MAPK1	ERK2	100.0	1000
MAPK6	ERK3	100.0	1000
MAPK4	ERK4	100.0	1000
MAPK7	ERK5	87.0	1000
MAPK15	ERK8	100.0	1000
ERN1	ERN1	100.0	1000
PTK2	FAK	100.0	1000
FER	FER	82.0	1000
FES	FES	100.0	1000
FGFR1	FGFR1	100.0	1000
FGFR2	FGFR2	85.0	1000
FGFR3	FGFR3(G697C)	84.0	1000
FGFR4	FGFR4	100.0	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	94.0	1000
GAK	GAK	97.0	1000
EIF2AK4	GCN2(Kin.Dom.2,S808G)	28.0	1000
GRK1	GRK1	82.0	1000
GRK2	GRK2	83.0	1000
GRK3	GRK3	100.0	1000
GRK4	GRK4	99.0	1000
GRK7	GRK7	100.0	1000
GSK3A	GSK3A	79.0	1000
GSK3B	GSK3B	92.0	1000
HASPIN	HASPIN	100.0	1000
HCK	HCK	100.0	1000
HIPK1	HIPK1	82.0	1000
HIPK2	HIPK2	100.0	1000
HIPK3	HIPK3	96.0	1000
HIPK4	HIPK4	100.0	1000
MAP4K1	HPK1	100.0	1000
HUNK	HUNK	100.0	1000
CILK1	ICK	62.0	1000
IGF1R	IGF1R	100.0	1000
CHUK	IKK-alpha	100.0	1000
IKBKB	IKK-beta	80.0	1000
IKBKE	IKK-epsilon	100.0	1000
INSR	INSR	85.0	1000
INSRR	INSRR	100.0	1000
IRAK1	IRAK1	100.0	1000
IRAK3	IRAK3	100.0	1000
IRAK4	IRAK4	83.0	1000
ITK	ITK	100.0	1000
JAK1	JAK1(JH2domain-pseudokinase)	74.0	1000
JAK2	JAK2(JH1domain-catalytic)	100.0	1000
JAK3	JAK3(JH1domain-catalytic)	100.0	1000
MAPK8	JNK1	77.0	1000
MAPK9	JNK2	99.0	1000
MAPK10	JNK3	88.0	1000
KIT	KIT-autoinhibited	84.0	1000
LATS1	LATS1	100.0	1000
LATS2	LATS2	100.0	1000
LCK	LCK	100.0	1000
LIMK1	LIMK1	100.0	1000
LIMK2	LIMK2	100.0	1000
STK11	LKB1	100.0	1000
STK10	LOK	100.0	1000
LRRK2	LRRK2(G2019S)	94.0	1000
LTK	LTK	100.0	1000
LYN	LYN	100.0	1000
MAP3K13	LZK	100.0	1000
MAK	MAK	100.0	1000
MAP3K1	MAP3K1	100.0	1000
MAP3K15	MAP3K15	100.0	1000
MAP3K2	MAP3K2	99.0	1000
MAP3K3	MAP3K3	84.0	1000
MAP3K4	MAP3K4	72.0	1000
MAP4K2	MAP4K2	100.0	1000
MAP4K3	MAP4K3	100.0	1000
MAP4K4	MAP4K4	100.0	1000
MAP4K5	MAP4K5	100.0	1000
MAPKAPK2	MAPKAPK2	97.0	1000
MAPKAPK5	MAPKAPK5	100.0	1000
MARK1	MARK1	91.0	1000
MARK2	MARK2	100.0	1000
MARK3	MARK3	100.0	1000
MARK4	MARK4	84.0	1000
MAST1	MAST1	100.0	1000
MAP2K1	MEK1	100.0	1000
MAP2K2	MEK2	90.0	1000
MAP2K3	MEK3	98.0	1000
MAP2K4	MEK4	100.0	1000
MAP2K5	MEK5	78.0	1000
MAP2K6	MEK6	100.0	1000
MELK	MELK	100.0	1000
MERTK	MERTK	100.0	1000
MET	MET(Y1235D)	100.0	1000
MINK1	MINK	100.0	1000
MAP2K7	MKK7	100.0	1000
MKNK1	MKNK1	99.0	1000
MKNK2	MKNK2	100.0	1000
MYLK3	MLCK	100.0	1000
MAP3K9	MLK1	100.0	1000
MAP3K10	MLK2	96.0	1000
MAP3K11	MLK3	86.0	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	74.0	1000
MTOR	MTOR	92.0	1000
MUSK	MUSK	100.0	1000
MYLK	MYLK	87.0	1000
MYLK2	MYLK2	100.0	1000
MYLK4	MYLK4	100.0	1000
MYO3A	MYO3A	100.0	1000
MYO3B	MYO3B	100.0	1000
STK38	NDR1	100.0	1000
STK38L	NDR2	100.0	1000
NEK1	NEK1	100.0	1000
NEK10	NEK10	84.0	1000
NEK11	NEK11	100.0	1000
NEK2	NEK2	100.0	1000
NEK3	NEK3	73.0	1000
NEK4	NEK4	82.0	1000
NEK5	NEK5	100.0	1000
NEK6	NEK6	100.0	1000
NEK7	NEK7	100.0	1000
NEK9	NEK9	100.0	1000
MAP3K14	NIK	91.0	1000
NIM1K	NIM1	100.0	1000
NLK	NLK	70.0	1000
OXSR1	OSR1	89.0	1000
MAPK14	p38-alpha	79.0	1000
MAPK11	p38-beta	100.0	1000
MAPK13	p38-delta	100.0	1000
MAPK12	p38-gamma	100.0	1000
PAK1	PAK1	79.0	1000
PAK2	PAK2	87.0	1000
PAK3	PAK3	100.0	1000
PAK4	PAK4	100.0	1000
PAK6	PAK6	100.0	1000
PAK5	PAK7	100.0	1000
CDK16	PCTK1	100.0	1000
CDK17	PCTK2	100.0	1000
CDK18	PCTK3	97.0	1000
PDGFRA	PDGFRA	100.0	1000
PDGFRB	PDGFRB	100.0	1000
PDPK1	PDPK1	95.0	1000
CDPK1	PFCDPK1(P.falciparum)	82.0	1000
PK5	PFPK5(P.falciparum)	80.0	1000
CDK15	PFTAIRE2	100.0	1000
CDK14	PFTK1	100.0	1000
PHKG1	PHKG1	100.0	1000
PHKG2	PHKG2	100.0	1000
PIK3C2B	PIK3C2B	66.0	1000
PIK3C2G	PIK3C2G	90.0	1000
PIK3CA	PIK3CA(Q546K)	100.0	1000
PIK3CB	PIK3CB	99.0	1000
PIK3CD	PIK3CD	100.0	1000
PIK3CG	PIK3CG	85.0	1000
PI4KB	PIK4CB	93.0	1000
PIKFYVE	PIKFYVE	100.0	1000
PIM1	PIM1	100.0	1000
PIM2	PIM2	100.0	1000
PIM3	PIM3	91.0	1000
PIP5K1A	PIP5K1A	88.0	1000
PIP5K1C	PIP5K1C	100.0	1000
PIP4K2B	PIP5K2B	100.0	1000
PIP4K2C	PIP5K2C	89.0	1000
PRKACA	PKAC-alpha	100.0	1000
PRKACB	PKAC-beta	100.0	1000
PKMYT1	PKMYT1	100.0	1000
PKN1	PKN1	100.0	1000
PKN2	PKN2	100.0	1000
PKNB	PKNB(M.tuberculosis)	82.0	1000
PLK1	PLK1	81.0	1000
PLK2	PLK2	100.0	1000
PLK3	PLK3	88.0	1000
PLK4	PLK4	88.0	1000
PRKCD	PRKCD	100.0	1000
PRKCE	PRKCE	100.0	1000
PRKCH	PRKCH	95.0	1000
PRKCI	PRKCI	100.0	1000
PRKCQ	PRKCQ	87.0	1000
PRKD1	PRKD1	100.0	1000
PRKD2	PRKD2	100.0	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	72.0	1000
PTK2B	PYK2	100.0	1000
SIK3	QSK	78.0	1000
RAF1	RAF1	100.0	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	68.0	1000
DSTYK	RIPK5	94.0	1000
ROCK1	ROCK1	100.0	1000
ROCK2	ROCK2	100.0	1000
ROS1	ROS1	86.0	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)	92.0	1000
RPS6KA6	RSK4(Kin.Dom.2-C-terminal)	100.0	1000
RPS6KB1	S6K1	75.0	1000
SBK1	SBK1	100.0	1000
SGK1	SGK	100.0	1000
SBK3	SgK110	84.0	1000
SGK2	SGK2	100.0	1000
SGK3	SGK3	100.0	1000
SIK1	SIK	100.0	1000
SIK2	SIK2	100.0	1000
SLK	SLK	98.0	1000
NUAK2	SNARK	100.0	1000
SNRK	SNRK	100.0	1000
SRC	SRC	96.0	1000
SRMS	SRMS	89.0	1000
SRPK1	SRPK1	100.0	1000
SRPK2	SRPK2	100.0	1000
SRPK3	SRPK3	100.0	1000
STK16	STK16	100.0	1000
STK33	STK33	100.0	1000
STK35	STK35	99.0	1000
STK36	STK36	100.0	1000
STK39	STK39	95.0	1000
SYK	SYK	96.0	1000
MAP3K7	TAK1	100.0	1000
TAOK1	TAOK1	100.0	1000
TAOK2	TAOK2	76.0	1000
TAOK3	TAOK3	100.0	1000
TBK1	TBK1	68.0	1000
TEC	TEC	100.0	1000
TESK1	TESK1	91.0	1000
TGFBR1	TGFBR1	100.0	1000
TGFBR2	TGFBR2	100.0	1000
TIE1	TIE1	89.0	1000
TEK	TIE2	100.0	1000
TLK1	TLK1	100.0	1000
TLK2	TLK2	100.0	1000
TNIK	TNIK	99.0	1000
TNK1	TNK1	100.0	1000
TNK2	TNK2	100.0	1000
TNNI3K	TNNI3K	100.0	1000
NTRK1	TRKA	90.0	1000
NTRK2	TRKB	83.0	1000
NTRK3	TRKC	100.0	1000
TRPM6	TRPM6	100.0	1000
TSSK1B	TSSK1B	100.0	1000
TSSK3	TSSK3	100.0	1000
TTK	TTK	100.0	1000
TXK	TXK	92.0	1000
TYK2	TYK2(JH2domain-pseudokinase)	100.0	1000
TYRO3	TYRO3	100.0	1000
ULK1	ULK1	85.0	1000
ULK2	ULK2	100.0	1000
ULK3	ULK3	77.0	1000
KDR	VEGFR2	100.0	1000
PIK3C3	VPS34	90.0	1000
VRK2	VRK2	91.0	1000
WEE1	WEE1	100.0	1000
WEE2	WEE2	100.0	1000
WNK1	WNK1	86.0	1000
WNK2	WNK2	100.0	1000
WNK3	WNK3	76.0	1000
WNK4	WNK4	100.0	1000
STK32A	YANK1	100.0	1000
STK32B	YANK2	68.0	1000
STK32C	YANK3	100.0	1000
YES1	YES	100.0	1000
STK25	YSK1	89.0	1000
MAP3K19	YSK4	77.0	1000
MAP3K20	ZAK	87.0	1000
ZAP70	ZAP70	100.0	1000

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BAY-386

Results are significant for > 50 % inhibition.

Conclusion: Closest off-target is Cannabinoid CB₁ with 88 % inhibition at 10 µM.

Target protein	HGNC name	Species	Cmp. conc.	% inhibition	Reference compound name	Reference compound IC50 [nM]	Assay ID
Adenosine A1	ADORA1	Homo sapiens	10 µM	-6.0	R(-)-PIA	830.00	200510
Adenosine A2A	ADORA2A	Homo sapiens	10 µM	0.0	CGS-Z1680	130.00	200610
Adenosine A3	ADORA3	Homo sapiens	10 µM	12.0	IB-MECA		200720
Adrenergic alpha1A	ADRA1A	Rattus sp.	10 µM	1.0	Prazosin	0.69	203100
Adrenergic alpha1B	ADRA1B	Rattus sp.	10 µM	9.0	Prazosin	0.27	203200
Adrenergic alpha1D	ADRA1D	Homo sapiens	10 µM	-4.0	Prazosin	0.88	203400
Adrenergic alpha2A	ADRA2A	Homo sapiens	10 µM	8.0	Yohimbine	8.40	203620
Adrenergic beta1	ADRB1	Homo sapiens	10 µM	-13.0	S(-)-Propranolol	2.50	204010
Adrenergic beta2	ADRB2	Homo sapiens	10 µM	0.0	S(-)-Propranolol	0.78	204110
Androgen (Testosterone) AR	AR	Rattus sp.	10 µM	11.0	Testosterone	6.50	285010
Bradykinin B1	BDKRB1	Homo sapiens	10 µM	6.0	(Des-Arg10)-Kallidin	0.87	212510
Bradykinin B2	BDKRB2	Homo sapiens	10 µM	11.0	Bradykinin	0.89	212610
Calcium Channel L-Type, Benzothiazepine	CACNA1C	Rattus sp.	10 µM	16.0	Diltiazem	0.04	214510
Calcium Channel L-Type, Dihydropyridine	CACNA1C	Rattus sp.	10 µM	14.0	Nitrendipine	0.72	214600
Calcium Channel N-Type	CACNA1B	Rattus sp.	10 µM	3.0	omega-Conotoxin GVIA	0.03	216000
Cannabinoid CB1	CNR1	Homo sapiens	10 µM	88.0	R(+)-WIN-55,Z1Z-Z	200.00	217030
Dopamine D1	DRD1	Homo sapiens	10 µM	4.0	R(+)-SCH-Z3390	1.40	219500
Dopamine D2S	DRD2	Homo sapiens	10 µM	1.0	Spiperone	0.25	219700
Dopamine D3	DRD3	Homo sapiens	10 µM	-1.0	Spiperone	0.36	219800
Dopamine D4.2	DRD4	Homo sapiens	10 µM	-9.0	Spiperone	29.00	219900
Endothelin ETA	EDNRA	Homo sapiens	10 µM	2.0	Endothelin-1	0.23	224010
Endothelin ETB	EDNRB	Homo sapiens	10 µM	-4.0	Endothelin-1	0.13	224110
Epidermal Growth Factor (EGF)	EGFR	Homo sapiens	10 µM	-7.0	EGF (human)	1.60	225510
Estrogen ERalpha	ESR1	Homo sapiens	10 µM	-1.0	Diethylstilbestrol	0.77	226010
GABAA, Flunitrazepam, Central		Rattus sp.	10 µM	-3.0	Hydrogen diazepam chloride	16.00	226600
GABAA, Muscimol, Central		Rattus sp.	10 µM	10.0	GABA	32.00	226500
GABAB1A	GABBR1	Homo sapiens	10 µM	10.0	Cgp-54626	6.40	228610
Glucocorticoid	NR3C1	Homo sapiens	10 µM	9.0	Dexamethasone	4.10	232020
Glutamate, Kainate	GRIK2	Rattus sp.	10 µM	15.0	L-Glutamic acid	240.00	232700
Glutamate, NMDA, Agonism		Rattus sp.	10 µM	-2.0	L-Glutamic acid	410.00	232810
Glutamate, NMDA, Glycine		Rattus sp.	10 µM	12.0	MDL 105,519	22.00	232910
Glutamate, NMDA, Phencyclidine		Rattus sp.	10 µM	0.0	Dizolcipine ((+)-MK- 801)	5.10	233000
Histamine H1	HRH1	Homo sapiens	10 µM	0.0	Pyrilamine	3.30	239610
Histamine H2	HRH2	Homo sapiens	10 µM	-3.0	Tiotidine	22.00	239710
Histamine H3	HRH3	Homo sapiens	10 µM	-3.0	R(-)-alpha-Methylhistamine (RAMH)	5.20	239810
Imidazoline I2, Central		Rattus sp.	10 µM	0.0	Idazoxan	12.00	241000
Interleukin IL-1		Mus musculus	10 µM	16.0	IL-1 beta	0.19	243520
Leukotriene, Cysteinyl CysLT1	CYSLTR1	Homo sapiens	10 µM	1.0	Leukotriene D4	0.70	250460
Melatonin MT1	MTNR1A	Homo sapiens	10 µM	14.0	Melatonin	0.21	251600
Muscarinic M1	CHRM1	Homo sapiens	10 µM	-3.0	4-DAMP	4.50	252610
Muscarinic M2	CHRM2	Homo sapiens	10 µM	-3.0	4-DAMP	55.00	252710
Muscarinic M3	CHRM3	Homo sapiens	10 µM	-2.0	4-DAMP	5.10	252810
Neuropeptide Y Y1	NPY1R	Homo sapiens	10 µM	1.0	Neuropeptide Y (human, rat)	0.22	257010
Neuropeptide Y Y2	NPY2R	Homo sapiens	10 µM	2.0	Neuropeptide Y (13-36) (porcine)	0.21	257110
Nicotinic Acetylcholine		Homo sapiens	10 µM	-4.0	Epibatidine	0.08	258590
Nicotinic Acetylcholine alpha1, Bungarotoxin	CHRNA1	Homo sapiens	10 µM	-2.0	alpha-Bungarotoxin	1.10	258700
Opiate delta (OP1, DOP)	OPRD1	Homo sapiens	10 µM	-17.0	Naltrindole	0.92	260110
Opiate kappa (OPZ, KOP)	OPRK1	Homo sapiens	10 µM	-3.0	U-69593	16.00	260210
Opiate µ (OP3, MOP)	OPRM1	Homo sapiens	10 µM	6.0	DAMGO	20.00	260410
Phorbol Ester		Mus musculus	10 µM	5.0	Phorbol myristate acetate	0.79	264500
Platelet Activating Factor (PAF)	PTAFR	Homo sapiens	10 µM	0.0	PAF	0.28	265010
Potassium Channel [KATP]	KCNJ11	Cricetinae	10 µM	4.0	Glyburide	5.70	265600
Potassium Channel hERG	KCNH2	Homo sapiens	10 µM	22.0	Astemizole		265900
Prostanoid EP4	PTGER4	Homo sapiens	10 µM	1.0	Prostaglandin E2	0.11	268420
Purinergic P2X		Oryctolagus cuniculus	10 µM	9.0	alpha,beta-Methylene ATP	82.00	268700
Purinergic P2Y		Rattus sp.	10 µM	12.0	ATP	18.00	268810
Rolipram		Rattus sp.	10 µM	3.0	Rolipram	5.70	270000
Serotonin (5-Hydroxytryptamine) 5-HT1A	HTR1A	Homo sapiens	10 µM	-9.0	Metergoline	4.10	271110
Serotonin (5-Hydroxytryptamine) 5-HT2B	HTR2B	Homo sapiens	10 µM	-18.0	Ketanserin	290.00	271700
Serotonin (5-Hydroxytryptamine) 5-HT3	HTR3A	Homo sapiens	10 µM	16.0	MDL-72222	11.00	271910
Sigma 1	SIGMAR1	Homo sapiens	10 µM	12.0	Haloperidol	21.00	278110
Sodium Channel, Site 2		Rattus sp.	10 µM	55.0	Dibucaine	61.00	279510
Tachykinin NK1	TACR1	Homo sapiens	10 µM	-2.0	L-703,606	25.00	255510
Thyroid Hormone		Rattus sp.	10 µM	11.0	Liothyronine	0.03	285900
Transporter, Dopamine (DAT)	SLC6A3	Homo sapiens	10 µM	10.0	GBR-1Z909	1.70	220320
Transporter, GABA		Rattus sp.	10 µM	14.0	NO-711	200.00	226400
Transporter, Norepinephrine (NET)	SLC6A2	Homo sapiens	10 µM	17.0	Desipramine	0.93	204410
Transporter, Serotonin (5-Hydroxytryptamine) (SERT)	SLC6A4	Homo sapiens	10 µM	3.0	Fluoxetine	8.60	274030

BAY-386

Cellular agonist effect was calculated as a % of control response to a known reference agonist for each target and cellular antagonist effect was calculated as a % inhibition of control reference agonist response for each target. Results showing an inhibition higher than 50 % are considered to represent significant effects of the probe. The results are expressed as a percent of control agonist response: (measured response/ control response ) * 100 or as a percent inhibition of control agonist response 100-((measured response/ control response) * 100).

Conclusion: Off target inhibition of Human CB1 in a cell based antagonist effect assay at 10 µM is 80.7 % and inhibition of M1 is 57%.

Target protein	HGNC name	Species	Cmp. conc.	Mean [% Inhibition of Control Agonist Response]	First measurement	Second measurement	Assay ID
A2B (h)	ADORA2B	Homo sapiens	10 µM	-0.3	12.90	-13.60	Cerep_455
A2B (h)	ADORA2B	Homo sapiens	10 µM	3.5	3.60	3.30	Cerep_452
A3 (h)	ADORA3	Homo sapiens	10 µM	-13.1	-9.90	-16.40	Cerep_983
A3 (h)	ADORA3	Homo sapiens	10 µM	2.5	1.80	3.20	Cerep_982
alpha1A (h)	ADRA1A	Homo sapiens	10 µM	18.8	12.10	25.50	Cerep_1501
alpha1A (h)	ADRA1A	Homo sapiens	10 µM	11.5	13.00	10.00	Cerep_1500
alpha2A (h)	ADRA2A	Homo sapiens	10 µM	-1.7	-13.50	10.00	Cerep_4317
alpha2A (h)	ADRA2A	Homo sapiens	10 µM	6.3	2.50	10.00	Cerep_4316
beta1 (h)	ADRB1	Homo sapiens	10 µM	-0.2	8.70	-9.20	Cerep_1606
beta1 (h)	ADRB1	Homo sapiens	10 µM	3.4	3.60	3.20	Cerep_1605
beta2 (h)	ADRB2	Homo sapiens	10 µM	-6.9	-20.30	6.50	Cerep_1977
beta2 (h)	ADRB2	Homo sapiens	10 µM	-1.7	-3.50		Cerep_1976
CB1 (h)	CNR1	Homo sapiens	10 µM	80.7	87.90	73.60	Cerep_1745
CB1 (h)	CNR1	Homo sapiens	10 µM	-266.7	-315.00	-218.40	Cerep_1744
D1 (h)	DRD1	Homo sapiens	10 µM	-31.6	-32.60	-30.60	Cerep_1686
D1 (h)	DRD1	Homo sapiens	10 µM	-1.4	0.40	-3.20	Cerep_1685
D2s (h)	DRD2	Homo sapiens	10 µM	6.6	5.60	7.60	Old_Cerep_45
D2s (h)	DRD2	Homo sapiens	10 µM	4.0	3.10	4.90	Old_Cerep_44
H1 (h)	HRH1	Homo sapiens	10 µM	6.9	7.20	6.60	Cerep_2543
H1 (h)	HRH1	Homo sapiens	10 µM	4.1	2.60	5.70	Cerep_2542
H2 (h)	HRH2	Homo sapiens	10 µM	9.6	12.10	7.10	Cerep_1696
H2 (h)	HRH2	Homo sapiens	10 µM	-0.7	-2.50	1.10	Cerep_1695
H3 (h)	HRH3	Homo sapiens	10 µM	-3.7	-5.10	-2.20	Cerep_1801
H3 (h)	HRH3	Homo sapiens	10 µM	6.2	8.10	4.20	Cerep_1800
MC4 (h)	MC4R	Homo sapiens	10 µM	-8.1	0.20	-16.50	Cerep_700
MC4 (h)	MC4R	Homo sapiens	10 µM	-1.2	0.10	-2.50	Cerep_699
motilin (h)	MLN	Homo sapiens	10 µM	29.2	30.20	28.10	Cerep_1894
motilin (h)	MLN	Homo sapiens	10 µM	16.7	16.60	16.80	Cerep_1321
M1 (h)	CHRM1	Homo sapiens	10 µM	57.0	56.40	57.60	Cerep_1474
M1 (h)	CHRM1	Homo sapiens	10 µM	12.8	12.70	12.90	Cerep_1262
M4 (h)	CHRM4	Homo sapiens	10 µM	5.8	4.90	6.70	Cerep_1671
M4 (h)	CHRM4	Homo sapiens	10 µM	-15.0	-4.70	-25.40	Cerep_1670
NK1 (h)	TACR1	Homo sapiens	10 µM	23.3	22.70	24.00	Cerep_2192
NK1 (h)	TACR1	Homo sapiens	10 µM	1.8	1.70	1.80	Cerep_2190
kappa(KOP) (h)	OPRK1	Homo sapiens	10 µM	4.5	3.40	5.50	Cerep_4460
kappa(KOP) (h)	OPRK1	Homo sapiens	10 µM	20.6	16.50	24.70	Cerep_4459
my(MOP) (h)	OPRM1	Homo sapiens	10 µM	3.7	6.60	0.70	Cerep_1393
my(MOP) (h)	OPRM1	Homo sapiens	10 µM	1.0	20.20	-18.20	Cerep_1392
EP3 (h)	PTGER3	Homo sapiens	10 µM	-8.0	-11.20	-4.90	Cerep_4331
EP3 (h)	PTGER3	Homo sapiens	10 µM	4.5	6.20	2.80	Cerep_4330
P2Y2 (h)	P2RY2	Homo sapiens	10 µM	41.9	51.20	32.50	Cerep_2167
P2Y2 (h)	P2RY2	Homo sapiens	10 µM	0.7	-0.80	2.30	Cerep_2164
5-HT1A (h)	HTR1A	Homo sapiens	10 µM	25.6	32.50	18.70	Cerep_4333
5-HT1A (h)	HTR1A	Homo sapiens	10 µM	-0.2	0.90	-1.40	Cerep_4332
5-HT2B (h)	HTR2B	Homo sapiens	10 µM	7.0	10.20	3.90	Cerep_3345
5-HT2B (h)	HTR2B	Homo sapiens	10 µM	1.6	0.30	2.90	Cerep_3344
5-HT6 (h)	HTR6	Homo sapiens	10 µM	21.1	16.20	26.00	Cerep_1628
5-HT6 (h)	HTR6	Homo sapiens	10 µM	2.8	8.20	-2.60	Cerep_1627
sst4 (h)	SSTR4	Homo sapiens	10 µM	-3.3	-4.90	-1.70	Cerep_2103
sst4 (h)	SSTR4	Homo sapiens	10 µM	-13.0	-20.80	-5.10	Cerep_2095

BAY-448

Conclusion: Clean panel.

Target protein	HGNC name	Species	Cmp. conc.	Mean [% Inhibition of Control Agonist Response]	First measurement	Second measurement	Assay ID
A2B (h)	ADORA2B	Homo sapiens	10 µM	-8.5	-0.6	-16.4	Cerep_455
A2B (h)	ADORA2B	Homo sapiens	10 µM	1.5	2.0	1.0	Cerep_452
A3 (h)	ADORA3	Homo sapiens	10 µM	12.2	8.9	15.4	Cerep_983
A3 (h)	ADORA3	Homo sapiens	10 µM	19.2	21.7	16.7	Cerep_982
alpha1A (h)	ADRA1A	Homo sapiens	10 µM	4.3	1.6	7.1	Cerep_1501
alpha1A (h)	ADRA1A	Homo sapiens	10 µM	-0.4	-0.2	-0.6	Cerep_1500
alpha2A (h)	ADRA2A	Homo sapiens	10 µM	-13.5	-13.5	-13.5	Cerep_4317
alpha2A (h)	ADRA2A	Homo sapiens	10 µM	2.5	0.7	4.4	Cerep_4316
beta1 (h)	ADRB1	Homo sapiens	10 µM	6.8	6.8	6.7	Cerep_1606
beta1 (h)	ADRB1	Homo sapiens	10 µM	0.3	-2.1	2.7	Cerep_1605
beta2 (h)	ADRB2	Homo sapiens	10 µM	10.2	13.0	7.3	Cerep_1977
beta2 (h)	ADRB2	Homo sapiens	10 µM	2.3	2.2	2.3	Cerep_1976
CB1 (h)	CNR1	Homo sapiens	10 µM	-0.6	4.4	-3.7	Cerep_1745
CB1 (h)	CNR1	Homo sapiens	10 µM	-17.6	-26.4	-8.9	Cerep_1744
D1 (h)	DRD1	Homo sapiens	10 µM	13.9	11.0	16.8	Cerep_1686
D1 (h)	DRD1	Homo sapiens	10 µM	-1.2	-3.5	1.1	Cerep_1685
D2s (h)	DRD2	Homo sapiens	10 µM	8.6	7.6	9.6	Old_Cerep_45
D2s (h)	DRD2	Homo sapiens	10 µM	3.1	3.1	3.1	Old_Cerep_44
H1 (h)	HRH1	Homo sapiens	10 µM	-14.6	-18.6	-10.5	Cerep_2543
H1 (h)	HRH1	Homo sapiens	10 µM	0.3	-1.3	1.8	Cerep_2542
H2 (h)	HRH2	Homo sapiens	10 µM	-2.8	9.1	-14.7	Cerep_1696
H2 (h)	HRH2	Homo sapiens	10 µM	2.6	0.9	4.4	Cerep_1695
H3 (h)	HRH3	Homo sapiens	10 µM	-4.2	-6.1	-2.2	Cerep_1801
H3 (h)	HRH3	Homo sapiens	10 µM	13.9	32.4	-4.5	Cerep_1800
MC4 (h)	MC4R	Homo sapiens	10 µM	14.3	16.0	12.6	Cerep_700
MC4 (h)	MC4R	Homo sapiens	10 µM	-1.8	-1.5	-2.1	Cerep_699
motilin (h)	MLN	Homo sapiens	10 µM	0.9	-0.3	2.1	Cerep_1894
motilin (h)	MLN	Homo sapiens	10 µM	6.9	7.9	6.0	Cerep_1321
M1 (h)	CHRM1	Homo sapiens	10 µM	10.2	2.4	18.0	Cerep_1474
M1 (h)	CHRM1	Homo sapiens	10 µM	1.2	1.5	1.0	Cerep_1262
M4 (h)	CHRM4	Homo sapiens	10 µM	1.9	2.7	1.1	Cerep_1671
M4 (h)	CHRM4	Homo sapiens	10 µM	25.1	24.9	25.2	Cerep_1670
NK1 (h)	TACR1	Homo sapiens	10 µM	2.1	1.3	2.8	Cerep_2192
NK1 (h)	TACR1	Homo sapiens	10 µM	0.3	0.9	-0.3	Cerep_2190
kappa (KOP) (h)	OPRK1	Homo sapiens	10 µM	1.3	4.2	-1.6	Cerep_4460
kappa (KOP) (h)	OPRK1	Homo sapiens	10 µM	9.0	10.9	7.0	Cerep_4459
mu (MOP) (h)	OPRM1	Homo sapiens	10 µM	-4.8	-5.1	-4.6	Cerep_1393
mu (MOP) (h)	OPRM1	Homo sapiens	10 µM	36.0	34.4	37.5	Cerep_1392
EP3 (h)	PTGER3	Homo sapiens	10 µM	0.6	-0.2	1.4	Cerep_4331
EP3 (h)	PTGER3	Homo sapiens	10 µM	-0.6	-1.2	-0.1	Cerep_4330
P2Y2 (h)	P2RY2	Homo sapiens	10 µM	29.1	24.0	34.1	Cerep_2167
P2Y2 (h)	P2RY2	Homo sapiens	10 µM	-4.2	-3.7	-4.7	Cerep_2164
5-HT1A (h)	HTR1A	Homo sapiens	10 µM	-23.0	-25.4	-20.7	Cerep_4333
5-HT1A (h)	HTR1A	Homo sapiens	10 µM	1.1	2.5	-0.4	Cerep_4332
5-HT2B (h)	HTR2B	Homo sapiens	10 µM	-3.0	-0.6	-5.4	Cerep_3345
5-HT2B (h)	HTR2B	Homo sapiens	10 µM	0.4	0.2	0.6	Cerep_3344
5-HT6 (h)	HTR6	Homo sapiens	10 µM	2.1	3.4	0.7	Cerep_1628
5-HT6 (h)	HTR6	Homo sapiens	10 µM	1.4	0.5	2.3	Cerep_1627
sst4 (h)	SSTR4	Homo sapiens	10 µM	1.2	4.1	-1.6	Cerep_2103
sst4 (h)	SSTR4	Homo sapiens	10 µM	-2.0	-3.7	-0.3	Cerep_2095

Selectivity data for probe BAY-386 and control BAY-448

PDSP data

BAY-386

BAY-448

DiscoverX KinomeScan data

BAY-386

BAY-448

Eurofins-Panlabs radioligand binding assay

BAY-386

Eurofins-Cerep Cellular and Nuclear Receptor Functional Assays

BAY-386

BAY-448