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Selectivity data for probe BAY-474 and control BAY-827


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BAY-474


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 2.16
Beta3 ADRB3 21.09
GABAA/BZP -23.90
GABAA -22.27
GABA/PBR -12.35
D4 DRD4 24.01
D5 DRD5 5.40
DAT SLC6A3 -13.90
H4 HRH4 -11.27
KOR OPRK1 8.26
MOR OPRM1 2.64
NET SLC6A2 -28.09
5-HT1A HTR1A -5.32
5-HT1B HTR1B 0.48
5-HT1D HTR1D -14.86
5-HT1E HTR1E 8.21
5-HT2A HTR2A 8.75
5-HT2B HTR2B -10.38
5-HT6 HTR6 20.68
5-HT7A HTR7 -0.97
D1 DRD1 6.92
D2 DRD2 -7.07
D3 DRD3 18.05
Alpha1A ADRA1A 15.58
Alpha1B ADRA1B 1.79
Alpha1D ADRA1D 2.50
Alpha2A ADRA2A -3.48
Alpha2B ADRA2B 8.04
Sigma 1 SIGMAR1 -9.08
Sigma 2 TMEM97 23.88
5-HT2C HTR2C 22.40
5-HT3 HTR3A 32.97
5-HT5A HTR5A -11.19
Beta2 ADRB2 20.19
DOR OPRD1 16.94
H1 HRH1 17.68
H2 HRH2 12.59
H3 HRH3 -3.35
M1 CHRM1 13.91
M2 CHRM2 -8.64
M3 CHRM3 -1.54
M4 CHRM4 5.33
M5 CHRM5 5.48
SERT SLC6A4 -3.41
Alpha2C ADRA2C -4.65

BAY-827


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 2.67
5-HT1B HTR1B 17.18
5-HT1D HTR1D 4.20
5-HT1E HTR1E -3.84
5-HT2A HTR2A 5.76
5-HT2B HTR2B -7.44
5-HT2C HTR2C 71.80 > 10000.00 average (n=2) < 5.00
5-HT3 HTR3A 2.60
5-HT5A HTR5A 4.53
5-HT6 HTR6 55.70 674.00 6.20
5-HT7A HTR7 8.19
D1 DRD1 6.70
D2 DRD2 10.59
D3 DRD3 -18.43
D4 DRD4 5.34
D5 DRD5 58.14 > 10000.00 < 5.00
SERT SLC6A4 -11.33
NET SLC6A2 8.56
DAT SLC6A3 -10.51
MOR OPRM1 -0.02
DOR OPRD1 33.38
KOR OPRK1 -15.98
GABAA -7.24
H2 HRH2 14.05
H3 HRH3 -19.62
Alpha1A ADRA1A -10.97
Alpha1B ADRA1B 21.66
Alpha2A ADRA2A 7.83
Alpha2B ADRA2B 4.71
Alpha2C ADRA2C -1.57
Beta1 ADRB1 4.66
Beta2 ADRB2 -0.81
M1 CHRM1 8.17
M2 CHRM2 18.81
M3 CHRM3 8.81
M4 CHRM4 12.97
M5 CHRM5 9.95
Beta3 ADRB3 24.29
GABAA/BZP 16.89
GABA/PBR 69.55 2396.50 average (n=2) 5.67
Alpha1D ADRA1D 7.73
Sigma 2 TMEM97 23.36
Sigma 1 SIGMAR1 14.56

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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

BAY-827


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 82.9 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 79.0 1000
COQ8A ADCK3 97.8 1000
COQ8B ADCK4 78.8 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 82.8 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 95.3 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 83.2 1000
AURKA AURKA 100.0 1000
AURKB AURKB 82.9 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 98.6 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 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 99.9 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 98.5 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 82.1 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 31.8 1000
CAMKK1 CAMKK1 93.7 1000
CAMKK2 CAMKK2 86.5 1000
CASK CASK 66.2 1000
CDK11B CDC2L1 91.6 1000
CDK11A CDC2L2 90.0 1000
CDK13 CDC2L5 86.6 1000
CDK19 CDK11 66.8 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 93.2 1000
CDK9 CDK9 96.9 1000
CDKL1 CDKL1 77.1 1000
CDKL2 CDKL2 97.9 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 88.5 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 100.0 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 64.7 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 91.7 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 79.2 1000
DCLK2 DCAMKL2 97.9 1000
DCLK3 DCAMKL3 71.3 1000
DDR1 DDR1 84.5 1000
DDR2 DDR2 99.4 1000
MAP3K12 DLK 72.2 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 93.6 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 50.1 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 96.4 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 91.2 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 63.9 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 89.6 1000
MAPK7 ERK5 90.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 97.9 1000
FES FES 100.0 1000
FGFR1 FGFR1 86.6 1000
FGFR2 FGFR2 74.3 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 100.0 1000
FLT4 FLT4 89.5 1000
FRK FRK 100.0 1000
FYN FYN 69.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 89.9 1000
GRK1 GRK1 65.5 1000
GRK2 GRK2 88.1 1000
GRK3 GRK3 85.3 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 69.6 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 56.7 1000
HIPK2 HIPK2 86.1 1000
HIPK3 HIPK3 89.5 1000
HIPK4 HIPK4 88.1 1000
MAP4K1 HPK1 93.1 1000
HUNK HUNK 81.4 1000
CILK1 ICK 76.2 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 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 96.4 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 97.2 1000
JAK1 JAK1(JH2domain-pseudokinase) 38.2 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 65.2 1000
MAPK9 JNK2 89.5 1000
MAPK10 JNK3 68.8 1000
KIT KIT-autoinhibited 71.2 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 91.1 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 79.5 1000
LTK LTK 100.0 1000
LYN LYN 96.8 1000
MAP3K13 LZK 100.0 1000
MAK MAK 85.1 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 72.2 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 67.9 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 54.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 91.1 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 53.5 1000
MAP2K4 MEK4 71.5 1000
MAP2K5 MEK5 49.9 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 52.6 1000
MINK1 MINK 77.0 1000
MAP2K7 MKK7 92.2 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 90.6 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 90.4 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 82.2 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 70.2 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 79.6 1000
MUSK MUSK 100.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 91.4 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 78.0 1000
STK38 NDR1 92.3 1000
STK38L NDR2 100.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 59.6 1000
NEK11 NEK11 62.4 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 90.1 1000
NEK5 NEK5 80.3 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 87.4 1000
NEK9 NEK9 95.6 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 78.9 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 99.8 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 58.6 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 88.9 1000
CDK17 PCTK2 87.2 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 98.2 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 92.5 1000
CDK15 PFTAIRE2 75.4 1000
CDK14 PFTK1 94.4 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 93.9 1000
PIK3CA PIK3CA(Q546K) 93.7 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 95.1 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 99.5 1000
PIP4K2B PIP5K2B 69.3 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 96.7 1000
PRKACB PKAC-beta 81.5 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 91.4 1000
PKN2 PKN2 74.6 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 77.5 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 86.3 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 96.1 1000
PRKCI PRKCI 99.4 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 81.1 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 86.9 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 74.1 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 73.8 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 94.6 1000
RIPK2 RIPK2 92.0 1000
RIPK4 RIPK4 71.8 1000
DSTYK RIPK5 100.0 1000
ROCK1 ROCK1 68.5 1000
ROCK2 ROCK2 91.9 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) 86.2 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 77.4 1000
RPS6KB1 S6K1 62.2 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 84.5 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 92.7 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 90.9 1000
STK35 STK35 100.0 1000
STK36 STK36 95.9 1000
STK39 STK39 90.7 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 58.7 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 62.4 1000
TGFBR2 TGFBR2 74.6 1000
TIE1 TIE1 76.4 1000
TEK TIE2 74.5 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 65.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 94.3 1000
NTRK1 TRKA 84.6 1000
NTRK2 TRKB 85.2 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 75.7 1000
TXK TXK 88.1 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 74.4 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 88.3 1000
KDR VEGFR2 96.3 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 91.2 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 93.6 1000
ZAP70 ZAP70 85.4 1000

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BAY-474

Results are significant for > 50 % inhibition.

Conclusion: Clean panel.

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [nM] Assay ID
Adenosine A1 ADORA1 Homo sapiens 10 µM -2.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 7.0 CGS-Z1680 130.00 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM 13.0 IB-MECA 200720
Adrenergic alpha1A ADRA1A Rattus sp. 10 µM 1.0 Prazosin 0.69 203100
Adrenergic alpha1B ADRA1B Rattus sp. 10 µM -1.0 Prazosin 0.27 203200
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM -9.0 Prazosin 0.88 203400
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM -16.0 Yohimbine 203630
Adrenergic beta1 ADRB1 Homo sapiens 10 µM 0.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM 4.0 S(-)-Propranolol 0.78 204110
Androgen (Testosterone) AR AR Rattus sp. 10 µM 12.0 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 -10.0 Bradykinin 1.80 212620
Calcium Channel L-Type, Benzothiazepine CACNA1C Rattus sp. 10 µM -9.0 Diltiazem 0.04 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM 0.0 Nitrendipine 0.72 214600
Calcium Channel N-Type CACNA1B Rattus sp. 10 µM 6.0 omega-Conotoxin GVIA 0.03 216000
Cannabinoid CB1 CNR1 Homo sapiens 10 µM 17.0 R(+)-WIN-55,Z1Z-Z 200.00 217030
Dopamine D1 DRD1 Homo sapiens 10 µM 3.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2S DRD2 Homo sapiens 10 µM 2.0 Spiperone 0.25 219700
Dopamine D3 DRD3 Homo sapiens 10 µM 12.0 Spiperone 0.36 219800
Dopamine D4.2 DRD4 Homo sapiens 10 µM -2.0 Spiperone 29.00 219900
Endothelin ETA EDNRA Homo sapiens 10 µM 7.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM 18.0 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 2.0 Diethylstilbestrol 0.77 226010
GABAA, Flunitrazepam, Central Rattus sp. 10 µM -2.0 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 0.0 Cgp-54626 6.40 228610
Glucocorticoid NR3C1 Homo sapiens 10 µM 12.0 Dexamethasone 4.10 232020
Glutamate, Kainate GRIK2 Rattus sp. 10 µM -4.0 L-Glutamic acid 240.00 232700
Glutamate, NMDA, Agonism Rattus sp. 10 µM -18.0 L-Glutamic acid 410.00 232810
Glutamate, NMDA, Glycine Rattus sp. 10 µM 9.0 MDL 105,519 22.00 232910
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM 4.0 Dizolcipine ((+)-MK- 801) 5.10 233000
Histamine H1 HRH1 Homo sapiens 10 µM 1.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM -21.0 Tiotidine 22.00 239710
Histamine H3 HRH3 Homo sapiens 10 µM -6.0 (R)-alpha-Methylhistamine 2.30 239820
Imidazoline I2, Central Rattus sp. 10 µM 5.0 Idazoxan 12.00 241000
Interleukin IL-1 Mus musculus 10 µM 0.0 IL-1 beta 0.19 243520
Leukotriene, Cysteinyl CysLT1 CYSLTR1 Homo sapiens 10 µM 8.0 Leukotriene D4 0.70 250460
Melatonin MT1 MTNR1A Homo sapiens 10 µM 2.0 Melatonin 0.21 251600
Muscarinic M1 CHRM1 Homo sapiens 10 µM 0.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 10 µM 0.0 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 3.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Nicotinic Acetylcholine Homo sapiens 10 µM -1.0 Epibatidine 0.08 258590
Nicotinic Acetylcholine alpha1, Bungarotoxin CHRNA1 Homo sapiens 10 µM 0.0 alpha-Bungarotoxin 1.10 258700
Opiate delta1 (OP1, DOP) OPRD1 Homo sapiens 10 µM 9.0 Naltrindole 0.91 260130
Opiate kappa (OPZ, KOP) OPRK1 Homo sapiens 10 µM 7.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM -9.0 DAMGO 20.00 260410
Phorbol Ester Mus musculus 10 µM 4.0 Phorbol myristate acetate 0.79 264500
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM 6.0 PAF 0.28 265010
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM 9.0 Glyburide 5.70 265600
Potassium Channel hERG KCNH2 Homo sapiens 10 µM 7.0 Astemizole 265900
Prostanoid EP4 PTGER4 Homo sapiens 10 µM 19.0 Prostaglandin E2 0.11 268420
Purinergic P2X Oryctolagus cuniculus 10 µM -1.0 alpha,beta-Methylene ATP 82.00 268700
Purinergic P2Y Rattus sp. 10 µM -16.0 ATP 18.00 268810
Rolipram Rattus sp. 10 µM 10.0 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 4.0 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM -7.0 MDL-72222 11.00 271910
Sigma 1 SIGMAR1 Homo sapiens 10 µM 15.0 Haloperidol 21.00 278110
Sodium Channel, Site 2 Rattus sp. 10 µM -1.0 Dibucaine 61.00 279510
Tachykinin NK1 TACR1 Homo sapiens 10 µM -4.0 L-703606 3.60 255520
Thyroid Hormone Rattus sp. 10 µM -16.0 Liothyronine 0.03 285900
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 0.0 GBR-1Z909 1.70 220320
Transporter, GABA Rattus sp. 10 µM 1.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 6.0 Desipramine 0.93 204410
Transporter, Serotonin (5-Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 9.0 Fluoxetine 8.60 274030
 

BAY-474

Kinase selectivity profiling has been performed at 1 µM probe concentration.

Conclusion: The selectivity is >1,000 fold vs all other tested kinases with an IC50 >10 µM for all kinases except for RSK2 (IC50 = 0.9 µM).

Target protein HGNC name Species % inhibition at 1 µM IC50 [µM]
Abl (h) ABL1 Homo sapiens -2.0
ACK1 (h) TNK2 Homo sapiens 2.0
ALK (h) ALK Homo sapiens -11.0
ALK4 (h) ACVR1B Homo sapiens 4.0
Arg (h) ABL2 Homo sapiens 26.0
ARK5 (h) NUAK1 Homo sapiens 22.0
ASK1 (h) MAP3K5 Homo sapiens -6.0
Aurora-A( h) AURKA Homo sapiens 40.0
Axl (h) AXL Homo sapiens 12.0
Bmx (h) BLK Homo sapiens -7.0
BRK (h) BMX Homo sapiens -7.0
BrSK1 (h) BRSK1 Homo sapiens 9.0
BrSK2 (h) BRSK2 Homo sapiens 21.0
BTK (h) BTK Homo sapiens -8.0
CaMKI (h) CAMK1 Homo sapiens -8.0
CaMKIIbeta (h) CAMK2B Homo sapiens 4.0
CaMKIIgamma (h) CAMK2G Homo sapiens 2.0
CaMKIIdelta (h) CAMK2D Homo sapiens 3.0
CaMKIV (h) CAMK4 Homo sapiens -1.0
CDK1/cyclinB( h) CDK1 Homo sapiens 16.0
CDK2/cyclinE (h) CDK2 Homo sapiens 9.0
CDK3/cyclinE (h) CDK3 Homo sapiens -4.0
CDK5/p35 (h) CDK5 Homo sapiens -1.0
CDK6/cyclinD3 (h) CDK6 Homo sapiens -25.0
CDK7/cyclinH/MAT1 (h) CDK7 Homo sapiens -1.0
CDK9/cyclin T1 (h) CDK9 Homo sapiens -10.0
CHK1 (h) CHEK1 Homo sapiens -22.0
CHK2 (h) CHEK2 Homo sapiens 4.0
CK1gamma1 (h) CSNK1G1 Homo sapiens -9.0
CK1gamma2 (h) CSNK1G2 Homo sapiens 19.0
CK1gamma3 (h) CSNK1G3 Homo sapiens 21.0
CK1delta (h) CSNK1D Homo sapiens 3.0
CK2 (h) CSNK2A1 Homo sapiens -8.0
CK2alpha2 (h) CSNK2A2 Homo sapiens -2.0
CLK3 (h) CLK3 Homo sapiens -1.0
cKit (h) KIT Homo sapiens -7.0
c-RAF (h) RAF1 Homo sapiens 1.0
CSK (h) CSK Homo sapiens -14.0
cSRC (h) SRC Homo sapiens 8.0
DAPK1 (h) DAPK1 Homo sapiens 0.0
DAPK2 (h) DAPK2 Homo sapiens -4.0
DCAMKL2 (h) DCLK2 Homo sapiens -5.0
DDR2 (h) DDR2 Homo sapiens 12.0
DMPK (h) DMPK Homo sapiens 3.0
DRAK1 (h) STK17A Homo sapiens -6.0
DYRK2 (h) STK17B Homo sapiens -8.0
eEF-2K (h) EEF2K Homo sapiens -5.0
EGFR (h) EGFR Homo sapiens -24.0
EphA1 (h) EPHA1 Homo sapiens 0.0
EphA2 (h) EPHA2 Homo sapiens 13.0
EphA3 (h) EPHA3 Homo sapiens -22.0
EphA4 (h) EPHA4 Homo sapiens -5.0
EphA5 (h) EPHA5 Homo sapiens -1.0
EphA7 (h) EPHA7 Homo sapiens -2.0
EphA8 (h) EPHA8 Homo sapiens -1.0
EphB2 (h) EPHB2 Homo sapiens -15.0
EphB1 (h) EPHB1 Homo sapiens -15.0
EphB3 (h) EPHB3 Homo sapiens -5.0
EphB4 (h) EPHB4 Homo sapiens -4.0
ErbB4 (h) ERBB4 Homo sapiens -21.0
FAK (h) PTK2 Homo sapiens 11.0
Fer (h) FER Homo sapiens 22.0
Fes (h) FES Homo sapiens -36.0
FGFR1 (h) FGFR1 Homo sapiens 23.0
FGFR2 (h) FGFR2 Homo sapiens 17.0
FGFR3 (h) FGFR3 Homo sapiens 10.0
FGFR4 (h) FGFR4 Homo sapiens 18.0
Fgr (h) FGR Homo sapiens 14.0
Flt1 (h) FLT1 Homo sapiens 69.0
Flt3 (h) FLT3 Homo sapiens -11.0
Flt4 (h) FLT4 Homo sapiens 26.0
Fms (h) Homo sapiens -20.0
Fyn (h) FYN Homo sapiens -11.0
GCK (h) GCK Homo sapiens 1.0
GRK5 (h) GRK5 Homo sapiens 0.0
GRK6 (h) GRK6 Homo sapiens -2.0
GRK7 (h) GRK7 Homo sapiens -20.0
GSK3alpha (h) GSK3A Homo sapiens -3.0
GSK3beta (h) GSK3B Homo sapiens -15.0
Haspin (h) HASPIN Homo sapiens 2.0
Hck (h) HCK Homo sapiens 16.0
HIPK1 (h) HIPK1 Homo sapiens -5.0
HIPK2 (h) HIPK2 Homo sapiens -11.0
HIPK3 (h) HIPK3 Homo sapiens -4.0
IGF-1R (h) IGF1R Homo sapiens -40.0
IKKalpha (h) CHUK Homo sapiens -17.0
IKKbeta (h) IKBKB Homo sapiens -13.0
IR (h) INSR Homo sapiens -9.0
IRR (h) INSRR Homo sapiens 2.0
IRAK1 (h) IRAK1 Homo sapiens -14.0
IRAK4 (h) IRAK4 Homo sapiens 0.0
Itk (h) ITK Homo sapiens -14.0
JAK2 (h) JAK2 Homo sapiens -20.0
JAK3 (h) JAK3 Homo sapiens -7.0
JNK1alpha1 (h) MAPK8 Homo sapiens -8.0
JNK2alpha2 (h) MAPK9 Homo sapiens 17.0
JNK3 (h) MAPK10 Homo sapiens -23.0
KDR (h) KDR Homo sapiens 4.0
Lck (h) LCK Homo sapiens -14.0
LIMK1 (h) LIMK1 Homo sapiens 2.0
LKB1 (h) STK11 Homo sapiens -8.0
LOK (h) STK10 Homo sapiens 26.0
Lyn (h) LYN Homo sapiens -1.0
MAPK1 (h) MAPK1 Homo sapiens 4.0
MAPK2( h) Homo sapiens 4.0
MAPKAP-K2 (h) MAPKAPK2 Homo sapiens -2.0
MAPKAP-K3 (h) MAPKAPK3 Homo sapiens -5.0
MARK1 (h) MARK1 Homo sapiens 11.0
MEK1 (h) MAP2K1 Homo sapiens -11.0
MELK (h) MELK Homo sapiens 26.0
Mer (h) MERTK Homo sapiens 12.0
Met (h) MET Homo sapiens 82.0
MINK (h) MINK1 Homo sapiens -15.0
MKK4 (m) MAP2K4 Homo sapiens 31.0
MKK6 (h) MAP2K6 Homo sapiens 5.0
MKK7beta (h) MAP2K7 Homo sapiens 13.0
MLCK (h) MYLK3 Homo sapiens 9.0
MLK1 (h) MAP3K9 Homo sapiens -1.0
Mnk2 (h) MKNK2 Homo sapiens -13.0
MRCKalpha (h) CDC42BPA Homo sapiens -10.0
MRCKbeta (h) CDC42BPB Homo sapiens -7.0
MSK1 (h) RPS6KA5 Homo sapiens -1.0
MSK2 (h) RPS6KA4 Homo sapiens -1.0
MSSK1 (h) SRPK3 Homo sapiens -23.0
MST1 (h) STK4 Homo sapiens 19.0
MST2 (h) STK3 Homo sapiens 7.0
MST3 (h) STK24 Homo sapiens 10.0
MuSK (h) MUSK Homo sapiens 19.0
NEK2 (h) NEK2 Homo sapiens -5.0
NEK3 (h) NEK3 Homo sapiens -9.0
NEK6 (h) NEK6 Homo sapiens -10.0
NEK7 (h) NEK7 Homo sapiens -12.0
NEK11 (h) NEK11 Homo sapiens -45.0
NLK (h) NLK Homo sapiens -4.0
p70S6K (h) RPS6KB1 Homo sapiens -3.0
PAK2 (h) PAK2 Homo sapiens -14.0
PAK3 (h) PAK3 Homo sapiens -8.0
PAK4 (h) PAK4 Homo sapiens 3.0
PAK5 (h) PAK5 Homo sapiens -4.0
PAK6 (h) PAK6 Homo sapiens 7.0
PAR-1Balpha (h) MARK2 Homo sapiens 26.0
PASK (h) PASK Homo sapiens 19.0
PDGFRalpha (h) PDGFRA Homo sapiens -2.0
PDGFRbeta(h) PDGFRB Homo sapiens -12.0
PDK1 (h) PDK1 Homo sapiens -17.0
PhKgamma2 (h) PHKG2 Homo sapiens -10.0
Pim-1 (h) PIM1 Homo sapiens -3.0
Pim-2 (h) PIM2 Homo sapiens -3.0
Pim-3 (h) PIM3 Homo sapiens -30.0
PKA (h) PRKACA Homo sapiens -27.0
PKBalpha (h) AKT1 Homo sapiens -13.0
PKBbeta (h) AKT2 Homo sapiens -5.0
PKBgamma (h) AKT3 Homo sapiens -4.0
PKCalpha (h) PRKCA Homo sapiens 18.0
PKCbetaI (h) PRKCB Homo sapiens -4.0
PKCbetaII (h) PRKCB Homo sapiens 7.0
PKCgamma(h) PRKCG Homo sapiens 18.0
PKCdelta (h) PRKCD Homo sapiens 2.0
PKCepsilon (h) PRKCE Homo sapiens 26.0
PKCeta (h) PRKCH Homo sapiens -3.0
PKCiota (h) PRKCI Homo sapiens -7.0
PKCmu (h) PRKD1 Homo sapiens 15.0
PKCtheta (h) PRKCQ Homo sapiens 15.0
PKD2 (h) PRKD2 Homo sapiens 3.0
PKG1alpha (h) PRKG1 Homo sapiens 7.0
PKG1beta (h) PRKG1 Homo sapiens 16.0
Plk3 (h) PLK3 Homo sapiens -13.0
PRAK (h) MAPKAPK5 Homo sapiens 6.0
PRK2 (h) PKN2 Homo sapiens 9.0
PrKX (h) PRKX Homo sapiens -14.0
PTK5 (h) FRK Homo sapiens 2.0
Pyk2 (h) PTK2B Homo sapiens 17.0
Ret (h) RET Homo sapiens -12.0
RIPK2 (h) RIPK2 Homo sapiens 5.0
ROCK-I (h) ROCK1 Homo sapiens 1.0
ROCK-II (h) ROCK2 Homo sapiens -3.0
Ron (h) MST1R Homo sapiens 8.0
Ros (h) ROS1 Homo sapiens 25.0
Rse (h) TYRO3 Homo sapiens 28.0
Rsk1 (h) RPS6KA1 Homo sapiens 46.0
Rsk2 (h) RPS6KA3 Homo sapiens 46.0 0.90
Rsk3 (h) RPS6KA2 Homo sapiens 51.0
Rsk4 (h) RPS6KA6 Homo sapiens 52.0
SAPK2a (h) MAPK14 Homo sapiens 3.0
SAPK2b (h) MAPK11 Homo sapiens -10.0
SAPK3 (h) MAPK12 Homo sapiens 8.0
SAPK4 (h) MAPK13 Homo sapiens 10.0
SGK (h) SGK1 Homo sapiens -2.0
SGK2 (h) SGK2 Homo sapiens -18.0
SGK3 (h) SGK3 Homo sapiens -2.0
SIK (h) SIK1 Homo sapiens -7.0
Snk (h) PLK2 Homo sapiens 3.0
SRPK1 (h) SRPK1 Homo sapiens 11.0
SRPK2 (h) SRPK2 Homo sapiens -28.0
STK33 (h) STK33 Homo sapiens 2.0
Syk (h) SYK Homo sapiens 8.0
TAK1 (h) MAP3K7 Homo sapiens -12.0
TAO1 (h) TAOK1 Homo sapiens -6.0
TAO2 (h) TAOK2 Homo sapiens -2.0
TAO3 (h) TAOK3 Homo sapiens -8.0
TBK1 (h) TBK1 Homo sapiens -6.0
Tie2 (h) TEK Homo sapiens 10.0
TLK2 (h) TLK2 Homo sapiens -30.0
TrkA (h) NTRK1 Homo sapiens 27.0
TrkB (h) NTRK2 Homo sapiens -2.0
TSSK1 (h) TSSK1B Homo sapiens 27.0
TSSK2 (h) TSSK2 Homo sapiens -3.0
ULK3 (h) ULK3 Homo sapiens -5.0
WNK2 (h) WNK2 Homo sapiens -8.0
WNK3 (h) WNK3 Homo sapiens -5.0
VRK2 (h) VRK2 Homo sapiens -20.0
Yes (h) YES1 Homo sapiens -11.0
ZAP-70 (h) ZAP70 Homo sapiens 12.0
ZIPK (h) DAPK3 Homo sapiens -17.0