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Selectivity data for probe BAY-3827 and control BAY-974


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BAY-3827


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 1.59
Beta3 ADRB3 10.32
H4 HRH4 -10.83
5-HT1B HTR1B 9.48
5-HT1D HTR1D 4.65
5-HT1E HTR1E 2.66
5-HT6 HTR6 9.23
5-HT7A HTR7 13.86
Beta2 ADRB2 1.11
D1 DRD1 67.39 634.31 6.20
D2 DRD2 -10.36
DOR OPRD1 20.48
H3 HRH3 -10.83
KOR OPRK1 16.12
M1 CHRM1 2.81
M5 CHRM5 17.88
5-HT1A HTR1A 5.20
GABAA/BZP -16.29
D3 DRD3 10.41
D4 DRD4 -0.18
D5 DRD5 8.47
GABAA -7.98
H1 HRH1 6.23
H2 HRH2 12.65
MOR OPRM1 30.50
5-HT2A HTR2A 14.85
5-HT2B HTR2B 32.47
5-HT2C HTR2C 20.02
5-HT3 HTR3A 2.79
5-HT5A HTR5A 19.90
Alpha1A ADRA1A 6.85
Alpha1B ADRA1B -9.38
Alpha1D ADRA1D 2.75
Alpha2A ADRA2A 5.01
Alpha2B ADRA2B 10.59
Alpha2C ADRA2C 10.00
M4 CHRM4 8.27
NET SLC6A2 2.80
Sigma 2 TMEM97 78.28 2843.81 average (n=2) 5.55
DAT SLC6A3 -11.27
M2 CHRM2 5.10
SERT SLC6A4 -6.24
Sigma 1 SIGMAR1 30.47
M3 CHRM3 22.48
GABA/PBR 85.63 222.40 6.66

BAY-974


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABA/PBR 96.35 20.99 average (n=2) 7.69
M3 CHRM3 9.49
Sigma 1 SIGMAR1 37.89
DAT SLC6A3 -13.16
M2 CHRM2 -2.08
SERT SLC6A4 -6.29
5-HT1A HTR1A 8.55
GABAA/BZP -1.23
D3 DRD3 2.48
D4 DRD4 0.21
D5 DRD5 14.56
GABAA -0.80
H1 HRH1 0.94
H2 HRH2 8.70
MOR OPRM1 13.65
5-HT1B HTR1B 4.12
5-HT1D HTR1D 2.45
5-HT1E HTR1E 11.42
5-HT6 HTR6 2.21
5-HT7A HTR7 6.72
Beta2 ADRB2 -7.25
D1 DRD1 -27.69
D2 DRD2 -13.67
DOR OPRD1 17.66
H3 HRH3 1.89
KOR OPRK1 21.64
M1 CHRM1 -1.37
M5 CHRM5 6.82
Beta1 ADRB1 -7.79
Beta3 ADRB3 -3.33
H4 HRH4 -12.98
5-HT2A HTR2A 8.41
5-HT2B HTR2B 11.39
5-HT2C HTR2C 22.53
5-HT3 HTR3A 9.93
5-HT5A HTR5A 0.04
Alpha1A ADRA1A 1.96
Alpha1B ADRA1B -4.61
Alpha1D ADRA1D 4.71
Alpha2A ADRA2A 14.42
Alpha2B ADRA2B 20.70
Alpha2C ADRA2C 10.22
M4 CHRM4 6.87
NET SLC6A2 2.85
Sigma 2 TMEM97 51.17 4470.95 5.35

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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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BAY-3827


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 81.0 1000
ABL1 ABL1-phosphorylated 88.0 1000
ABL2 ABL2 92.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 99.0 1000
ACVRL1 ACVRL1 75.0 1000
COQ8A ADCK3 84.0 1000
COQ8B ADCK4 96.0 1000
AKT1 AKT1 75.0 1000
AKT2 AKT2 95.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 83.0 1000
PRKAA1 AMPK-alpha1 7.5 1000
PRKAA2 AMPK-alpha2 0.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 33.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 51.0 1000
AURKB AURKB 88.0 1000
AURKC AURKC 29.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 87.0 1000
BMPR1B BMPR1B 96.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 96.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 55.0 1000
BRSK2 BRSK2 36.0 1000
BTK BTK 99.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 76.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 87.0 1000
CAMK1G CAMK1G 90.0 1000
CAMK2A CAMK2A 47.0 1000
CAMK2B CAMK2B 73.0 1000
CAMK2D CAMK2D 78.0 1000
CAMK2G CAMK2G 79.0 1000
CAMK4 CAMK4 56.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 95.0 1000
CASK CASK 81.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 86.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 88.0 1000
CDK4 CDK4-cyclinD3 75.0 1000
CDK5 CDK5 89.0 1000
CDK7 CDK7 90.0 1000
CDK8 CDK8 71.0 1000
CDK9 CDK9 94.0 1000
CDKL1 CDKL1 87.0 1000
CDKL2 CDKL2 94.0 1000
CDKL3 CDKL3 87.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 91.0 1000
CHEK2 CHEK2 70.0 1000
CIT CIT 90.0 1000
CLK1 CLK1 84.0 1000
CLK2 CLK2 55.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 98.0 1000
CSNK1A1 CSNK1A1 96.0 1000
CSNK1A1L CSNK1A1L 62.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 95.0 1000
CSNK1G2 CSNK1G2 97.0 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 63.0 1000
DAPK3 DAPK3 71.0 1000
DCLK1 DCAMKL1 87.0 1000
DCLK2 DCAMKL2 64.0 1000
DCLK3 DCAMKL3 82.0 1000
DDR1 DDR1 48.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 94.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 93.0 1000
STK17A DRAK1 89.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 82.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 60.0 1000
EPHA2 EPHA2 61.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 87.0 1000
EPHA6 EPHA6 57.0 1000
EPHA7 EPHA7 81.0 1000
EPHA8 EPHA8 79.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 76.0 1000
EPHB3 EPHB3 57.0 1000
EPHB4 EPHB4 51.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 71.0 1000
ERBB3 ERBB3 91.0 1000
ERBB4 ERBB4 84.0 1000
MAPK3 ERK1 95.0 1000
MAPK1 ERK2 86.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 96.0 1000
MAPK7 ERK5 86.0 1000
MAPK15 ERK8 81.0 1000
ERN1 ERN1 70.0 1000
PTK2 FAK 82.0 1000
FER FER 90.0 1000
FES FES 68.0 1000
FGFR1 FGFR1 97.0 1000
FGFR2 FGFR2 83.0 1000
FGFR3 FGFR3(G697C) 74.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 51.0 1000
FLT1 FLT1 72.0 1000
FLT3 FLT3-autoinhibited 88.0 1000
FLT4 FLT4 85.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 82.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 43.0 1000
GRK1 GRK1 43.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 54.0 1000
GSK3A GSK3A 90.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 99.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 73.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 87.0 1000
CHUK IKK-alpha 87.0 1000
IKBKB IKK-beta 94.0 1000
IKBKE IKK-epsilon 68.0 1000
INSR INSR 100.0 1000
INSRR INSRR 99.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 98.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 86.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 91.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 79.0 1000
MAPK8 JNK1 71.0 1000
MAPK9 JNK2 67.0 1000
MAPK10 JNK3 92.0 1000
KIT KIT-autoinhibited 100.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 67.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 99.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 94.0 1000
LYN LYN 86.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 96.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 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 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 36.0 1000
MARK2 MARK2 40.0 1000
MARK3 MARK3 30.0 1000
MARK4 MARK4 51.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 97.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 98.0 1000
MELK MELK 43.0 1000
MERTK MERTK 80.0 1000
MET MET(Y1235D) 16.0 1000
MINK1 MINK 99.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 98.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 92.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 88.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 98.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 80.0 1000
STK24 MST3 90.0 1000
STK26 MST4 98.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 83.0 1000
MYLK MYLK 55.0 1000
MYLK2 MYLK2 80.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 68.0 1000
MYO3B MYO3B 77.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 82.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 87.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 75.0 1000
NEK7 NEK7 83.0 1000
NEK9 NEK9 93.0 1000
MAP3K14 NIK 75.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 91.0 1000
MAPK13 p38-delta 96.0 1000
MAPK12 p38-gamma 76.0 1000
PAK1 PAK1 82.0 1000
PAK2 PAK2 75.0 1000
PAK3 PAK3 86.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 93.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 93.0 1000
CDK18 PCTK3 75.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 82.0 1000
PDPK1 PDPK1 86.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 95.0 1000
CDK14 PFTK1 83.0 1000
PHKG1 PHKG1 44.0 1000
PHKG2 PHKG2 81.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 95.0 1000
PIK3CA PIK3CA(Q546K) 39.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 90.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 99.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 56.0 1000
PIP4K2B PIP5K2B 91.0 1000
PIP4K2C PIP5K2C 77.0 1000
PRKACA PKAC-alpha 89.0 1000
PRKACB PKAC-beta 99.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 85.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 97.0 1000
PLK3 PLK3 100.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 55.0 1000
PRKCE PRKCE 19.0 1000
PRKCH PRKCH 32.0 1000
PRKCI PRKCI 82.0 1000
PRKCQ PRKCQ 15.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 87.0 1000
PRKD3 PRKD3 88.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 88.0 1000
PRPF4B PRP4 72.0 1000
PTK2B PYK2 92.0 1000
SIK3 QSK 74.0 1000
RAF1 RAF1 63.0 1000
RET RET(V804M) 11.0 1000
RIOK1 RIOK1 82.0 1000
RIOK2 RIOK2 93.0 1000
RIOK3 RIOK3 45.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 92.0 1000
DSTYK RIPK5 95.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 98.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 90.0 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 80.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 73.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 91.0 1000
SIK1 SIK 66.0 1000
SIK2 SIK2 69.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 40.0 1000
SNRK SNRK 100.0 1000
SRC SRC 94.0 1000
SRMS SRMS 94.0 1000
SRPK1 SRPK1 89.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 79.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 92.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 96.0 1000
TAOK3 TAOK3 38.0 1000
TBK1 TBK1 77.0 1000
TEC TEC 91.0 1000
TESK1 TESK1 96.0 1000
TGFBR1 TGFBR1 58.0 1000
TGFBR2 TGFBR2 82.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 91.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 78.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 81.0 1000
TNNI3K TNNI3K 87.0 1000
NTRK1 TRKA 97.0 1000
NTRK2 TRKB 100.0 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 84.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 29.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 82.0 1000
KDR VEGFR2 88.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 82.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 90.0 1000
WNK4 WNK4 94.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 98.0 1000
STK32C YANK3 100.0 1000
YES1 YES 86.0 1000
STK25 YSK1 80.0 1000
MAP3K19 YSK4 74.0 1000
MAP3K20 ZAK 90.0 1000
ZAP70 ZAP70 100.0 1000

BAY-974


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 90.0 1000
ABL1 ABL1-phosphorylated 66.0 1000
ABL2 ABL2 99.0 1000
ACVR1 ACVR1 99.0 1000
ACVR1B ACVR1B 80.0 1000
ACVR2A ACVR2A 97.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 97.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 94.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 93.0 1000
ALK ALK(L1196M) 80.0 1000
PRKAA1 AMPK-alpha1 77.0 1000
PRKAA2 AMPK-alpha2 99.0 1000
ANKK1 ANKK1 92.0 1000
NUAK1 ARK5 95.0 1000
MAP3K5 ASK1 89.0 1000
MAP3K6 ASK2 71.0 1000
AURKA AURKA 61.0 1000
AURKB AURKB 66.0 1000
AURKC AURKC 97.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 82.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 91.0 1000
BMPR2 BMPR2 79.0 1000
BMX BMX 85.0 1000
BRAF BRAF(V600E) 62.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 92.0 1000
BTK BTK 85.0 1000
BUB1 BUB1 74.0 1000
CAMK1 CAMK1 98.0 1000
PNCK CAMK1B 85.0 1000
CAMK1D CAMK1D 93.0 1000
CAMK1G CAMK1G 99.0 1000
CAMK2A CAMK2A 90.0 1000
CAMK2B CAMK2B 86.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 70.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 67.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 87.0 1000
CDK19 CDK11 74.0 1000
CDK2 CDK2 86.0 1000
CDK3 CDK3 99.0 1000
CDK4 CDK4-cyclinD3 79.0 1000
CDK5 CDK5 87.0 1000
CDK7 CDK7 58.0 1000
CDK8 CDK8 97.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 72.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 79.0 1000
CDKL5 CDKL5 79.0 1000
CHEK1 CHEK1 81.0 1000
CHEK2 CHEK2 74.0 1000
CIT CIT 55.0 1000
CLK1 CLK1 87.0 1000
CLK2 CLK2 75.0 1000
CLK3 CLK3 94.0 1000
CLK4 CLK4 76.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 85.0 1000
CSNK1A1 CSNK1A1 70.0 1000
CSNK1A1L CSNK1A1L 97.0 1000
CSNK1D CSNK1D 89.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 95.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 63.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 79.0 1000
DAPK1 DAPK1 89.0 1000
DAPK2 DAPK2 98.0 1000
DAPK3 DAPK3 88.0 1000
DCLK1 DCAMKL1 79.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 89.0 1000
DDR1 DDR1 74.0 1000
DDR2 DDR2 86.0 1000
MAP3K12 DLK 80.0 1000
DMPK DMPK 99.0 1000
CDC42BPG DMPK2 92.0 1000
STK17A DRAK1 82.0 1000
STK17B DRAK2 88.0 1000
DYRK1A DYRK1A 97.0 1000
DYRK1B DYRK1B 63.0 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 88.0 1000
EPHA2 EPHA2 82.0 1000
EPHA3 EPHA3 99.0 1000
EPHA4 EPHA4 93.0 1000
EPHA5 EPHA5 77.0 1000
EPHA6 EPHA6 89.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 99.0 1000
EPHB2 EPHB2 86.0 1000
EPHB3 EPHB3 99.0 1000
EPHB4 EPHB4 97.0 1000
EPHB6 EPHB6 81.0 1000
ERBB2 ERBB2 86.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 65.0 1000
MAPK3 ERK1 94.0 1000
MAPK1 ERK2 80.0 1000
MAPK6 ERK3 97.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 89.0 1000
ERN1 ERN1 84.0 1000
PTK2 FAK 94.0 1000
FER FER 88.0 1000
FES FES 84.0 1000
FGFR1 FGFR1 97.0 1000
FGFR2 FGFR2 97.0 1000
FGFR3 FGFR3(G697C) 93.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 92.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 96.0 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) 61.0 1000
GRK1 GRK1 88.0 1000
GRK2 GRK2 91.0 1000
GRK3 GRK3 93.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 70.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 81.0 1000
HASPIN HASPIN 71.0 1000
HCK HCK 66.0 1000
HIPK1 HIPK1 71.0 1000
HIPK2 HIPK2 73.0 1000
HIPK3 HIPK3 73.0 1000
HIPK4 HIPK4 80.0 1000
MAP4K1 HPK1 81.0 1000
HUNK HUNK 78.0 1000
CILK1 ICK 97.0 1000
IGF1R IGF1R 96.0 1000
CHUK IKK-alpha 77.0 1000
IKBKB IKK-beta 95.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 75.0 1000
IRAK3 IRAK3 79.0 1000
IRAK4 IRAK4 7.5 1000
ITK ITK 97.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 90.0 1000
JAK2 JAK2(JH1domain-catalytic) 77.0 1000
JAK3 JAK3(JH1domain-catalytic) 83.0 1000
MAPK8 JNK1 88.0 1000
MAPK9 JNK2 73.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 77.0 1000
LATS1 LATS1 85.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 81.0 1000
LIMK1 LIMK1 94.0 1000
LIMK2 LIMK2 99.0 1000
STK11 LKB1 89.0 1000
STK10 LOK 68.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 70.0 1000
LYN LYN 89.0 1000
MAP3K13 LZK 99.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 51.0 1000
MAP3K15 MAP3K15 96.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 77.0 1000
MAP3K4 MAP3K4 84.0 1000
MAP4K2 MAP4K2 99.0 1000
MAP4K3 MAP4K3 80.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 84.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 99.0 1000
MARK3 MARK3 92.0 1000
MARK4 MARK4 94.0 1000
MAST1 MAST1 92.0 1000
MAP2K1 MEK1 87.0 1000
MAP2K2 MEK2 82.0 1000
MAP2K3 MEK3 91.0 1000
MAP2K4 MEK4 79.0 1000
MAP2K5 MEK5 79.0 1000
MAP2K6 MEK6 95.0 1000
MELK MELK 81.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 74.0 1000
MINK1 MINK 96.0 1000
MAP2K7 MKK7 65.0 1000
MKNK1 MKNK1 70.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 86.0 1000
MAP3K9 MLK1 96.0 1000
MAP3K10 MLK2 69.0 1000
MAP3K11 MLK3 96.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 80.0 1000
MST1R MST1R 95.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 75.0 1000
MUSK MUSK 98.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 89.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 86.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 96.0 1000
STK38L NDR2 98.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 90.0 1000
NEK11 NEK11 96.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 94.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 96.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 69.0 1000
NIM1K NIM1 86.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 83.0 1000
MAPK14 p38-alpha 88.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 79.0 1000
MAPK12 p38-gamma 68.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 67.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 93.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 86.0 1000
PDGFRB PDGFRB 94.0 1000
PDPK1 PDPK1 77.0 1000
CDPK1 PFCDPK1(P.falciparum) 98.0 1000
PK5 PFPK5(P.falciparum) 84.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 91.0 1000
PHKG2 PHKG2 89.0 1000
PIK3C2B PIK3C2B 76.0 1000
PIK3C2G PIK3C2G 61.0 1000
PIK3CA PIK3CA(Q546K) 87.0 1000
PIK3CB PIK3CB 86.0 1000
PIK3CD PIK3CD 71.0 1000
PIK3CG PIK3CG 84.0 1000
PI4KB PIK4CB 30.0 1000
PIKFYVE PIKFYVE 87.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 91.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 91.0 1000
PIP4K2B PIP5K2B 83.0 1000
PIP4K2C PIP5K2C 92.0 1000
PRKACA PKAC-alpha 77.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 99.0 1000
PKN1 PKN1 78.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 97.0 1000
PLK1 PLK1 85.0 1000
PLK2 PLK2 74.0 1000
PLK3 PLK3 80.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 85.0 1000
PRKCH PRKCH 94.0 1000
PRKCI PRKCI 66.0 1000
PRKCQ PRKCQ 55.0 1000
PRKD1 PRKD1 92.0 1000
PRKD2 PRKD2 95.0 1000
PRKD3 PRKD3 72.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 72.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 76.0 1000
PRPF4B PRP4 77.0 1000
PTK2B PYK2 83.0 1000
SIK3 QSK 81.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 91.0 1000
RIOK1 RIOK1 93.0 1000
RIOK2 RIOK2 65.0 1000
RIOK3 RIOK3 87.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 78.0 1000
DSTYK RIPK5 72.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 93.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 87.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 94.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 94.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 83.0 1000
RPS6KB1 S6K1 74.0 1000
SBK1 SBK1 98.0 1000
SGK1 SGK 89.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 73.0 1000
SGK3 SGK3 95.0 1000
SIK1 SIK 88.0 1000
SIK2 SIK2 93.0 1000
SLK SLK 88.0 1000
NUAK2 SNARK 81.0 1000
SNRK SNRK 100.0 1000
SRC SRC 89.0 1000
SRMS SRMS 57.0 1000
SRPK1 SRPK1 89.0 1000
SRPK2 SRPK2 88.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 83.0 1000
STK33 STK33 100.0 1000
STK35 STK35 86.0 1000
STK36 STK36 87.0 1000
STK39 STK39 92.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 74.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 70.0 1000
TAOK3 TAOK3 80.0 1000
TBK1 TBK1 69.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 96.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 99.0 1000
TIE1 TIE1 94.0 1000
TEK TIE2 98.0 1000
TLK1 TLK1 88.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 98.0 1000
TNK1 TNK1 76.0 1000
TNK2 TNK2 86.0 1000
TNNI3K TNNI3K 96.0 1000
NTRK1 TRKA 77.0 1000
NTRK2 TRKB 72.0 1000
NTRK3 TRKC 83.0 1000
TRPM6 TRPM6 91.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 80.0 1000
TTK TTK 82.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 82.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 86.0 1000
ULK2 ULK2 72.0 1000
ULK3 ULK3 84.0 1000
KDR VEGFR2 80.0 1000
PIK3C3 VPS34 87.0 1000
VRK2 VRK2 72.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 82.0 1000
WNK2 WNK2 75.0 1000
WNK3 WNK3 82.0 1000
WNK4 WNK4 95.0 1000
STK32A YANK1 95.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 79.0 1000
YES1 YES 88.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 82.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 90.0 1000

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BAY-3827

The test was done at 10 µM ATP concentration. The results are in percentage activity compared to buffer control. Shown are data from PMID: 33492659 (Supplementary Table 1 , IC50 values are from S2) .

Conclusion: Clean panel: Closest off-targets are RPS6KA1 with IC50 = 9 nM, RPS6KA2 with IC50 = 24 nM, RPS6KA5 with IC50 = 43 nM, RPS6KA3 with IC50 = 52 nM and STK24 with IC50 = 94 nM.

Target protein HGNC name Species % residual kinase activity at 1 µM IC50 [nM]
Abl(h) ABL1 Homo sapiens 131.0
ACK1(h) TNK2 Homo sapiens 94.0
ACTR2(h) ACTR2 Homo sapiens 99.0
ALK(h) ALK Homo sapiens 103.0
ALK1(h) ACVRL1 Homo sapiens 138.0
ALK2(h) ACVR1 Homo sapiens 109.0
ALK4(h) ACVR1B Homo sapiens 90.0
ALK6(h) BMPR1B Homo sapiens 99.0
Arg(h) ABL2 Homo sapiens 101.0
AMPKalpha1(h) PRKAA1 Homo sapiens 1.0 10.00
AMPKalpha2(h) PRKAA2 Homo sapiens 0.0 7.00
A-Raf(h) ARAF Homo sapiens 78.0
ARK5(h) NUAK1 Homo sapiens 21.0
ASK1(h) MAP3K5 Homo sapiens 99.0
Aurora-A(h) AURKA Homo sapiens 34.0 480.00
Aurora-B(h) AURKB Homo sapiens 76.0
Aurora-C(h) AURKC Homo sapiens 85.0
Axl(h) AXL Homo sapiens 100.0
Blk(h) BLK Homo sapiens 111.0
BMPR2(h) BMPR2 Homo sapiens 104.0
Bmx(h) BMX Homo sapiens 113.0
BRK(h) PTK6 Homo sapiens 104.0
BrSK1(h) BRSK1 Homo sapiens 64.0
BrSK2(h) BRSK2 Homo sapiens 34.0
BTK(h) BTK Homo sapiens 96.0
B-Raf(h) BRAF Homo sapiens 99.0
CaMKI(h) CAMK1 Homo sapiens 93.0
CaMKIbeta(h) PNCK Homo sapiens 91.0
CaMKIgamma(h) CAMK1G Homo sapiens 92.0
CaMKIIalpha(h) CAMK2A Homo sapiens 81.0
CaMKIIbeta(h) CAMK2B Homo sapiens 100.0
CaMKIIgamma(h) CAMK2G Homo sapiens 79.0
CaMKIdelta(h) CAMK1D Homo sapiens 104.0
CaMKIIdelta(h) CAMK2D Homo sapiens 75.0
CaMKIV(h) CAMK4 Homo sapiens 111.0
CaMKK1(h) CAMKK1 Homo sapiens 95.0
CaMKK2(h) CAMKK2 Homo sapiens 101.0
CDK1/cyclinB(h) CDK1 Homo sapiens 98.0
CDK2/cyclinA(h) CDK2 Homo sapiens 100.0
CDK2/cyclinE(h) CDK2 Homo sapiens 92.0
CDK3/cyclinE(h) CDK3 Homo sapiens 100.0
CDK4/cyclinD3(h) CDK4 Homo sapiens 112.0
CDK5/p25(h) CDK5 Homo sapiens 98.0
CDK5/p35(h) CDK5 Homo sapiens 99.0
CDK6/cyclinD3(h) CDK6 Homo sapiens 110.0
CDK7/cyclinH/MAT1(h) CDK7 Homo sapiens 66.0
CDK9/cyclin T1(h) CDK9 Homo sapiens 91.0
CDK12/cyclinK(h) CDK12 Homo sapiens 85.0
CDK18/cyclinY(h) CDK18 Homo sapiens 106.0
CDKL1(h) CDKL1 Homo sapiens 95.0
ChaK1(h) TRPM7 Homo sapiens 100.0
CHK1(h) CHEK1 Homo sapiens 112.0
CHK2(h) CHEK2 Homo sapiens 100.0
CK1gamma1(h) CSNK1G1 Homo sapiens 101.0
CK1gamma2(h) CSNK1G2 Homo sapiens 98.0
CK1gamma3(h) CSNK1G3 Homo sapiens 105.0
CK1delta(h) CSNK1D Homo sapiens 94.0
CK2(h) CSNK2A1 Homo sapiens 94.0
CK2alpha1(h) CSNK2A1 Homo sapiens 93.0
CK2alpha2(h) CSNK2A2 Homo sapiens 109.0
CLIK1(h) STK35 Homo sapiens 80.0
CLK1(h) CLK1 Homo sapiens 108.0
CLK2(h) CLK2 Homo sapiens 93.0
CLK3(h) CLK3 Homo sapiens 109.0
CLK4(h) CLK4 Homo sapiens 104.0
cKit(h) KIT Homo sapiens 101.0
CSK(h) CSK Homo sapiens 90.0
c-RAF(h) RAF1 Homo sapiens 99.0
cSRC(h) SRC Homo sapiens 85.0
DAPK1(h) DAPK1 Homo sapiens 100.0
DAPK2(h) DAPK2 Homo sapiens 96.0
DCAMKL2(h) DCLK2 Homo sapiens 97.0
DCAMKL3(h) DCLK3 Homo sapiens 100.0
DDR1(h) DDR1 Homo sapiens 32.0
DDR2(h) DDR2 Homo sapiens 92.0
DMPK(h) DMPK Homo sapiens 91.0
DRAK1(h) STK17A Homo sapiens 119.0
DRAK2(h) STK17B Homo sapiens 99.0
DYRK1A(h) DYRK1A Homo sapiens 107.0
DYRK1B(h) DYRK1B Homo sapiens 99.0
DYRK2(h) DYRK2 Homo sapiens 100.0
DYRK3(h) DYRK3 Homo sapiens 97.0
eEF-2K(h) EEF2K Homo sapiens 141.0
EGFR(h) EGFR Homo sapiens 107.0
EphA1(h) EPHA1 Homo sapiens 98.0
EphA2(h) EPHA2 Homo sapiens 88.0
EphA3(h) EPHA3 Homo sapiens 112.0
EphA4(h) EPHA4 Homo sapiens 106.0
EphA5(h) EPHA5 Homo sapiens 89.0
EphA7(h) EPHA7 Homo sapiens 91.0
EphA8(h) EPHA8 Homo sapiens 102.0
EphB2(h) EPHB2 Homo sapiens 98.0
EphB1(h) EPHB1 Homo sapiens 96.0
EphB3(h) EPHB3 Homo sapiens 109.0
EphB4(h) EPHB4 Homo sapiens 77.0
ErbB2(h) ERBB2 Homo sapiens 95.0
ErbB4(h) ERBB4 Homo sapiens 101.0
FAK(h) PTK2 Homo sapiens 84.0
Fer(h) FER Homo sapiens 100.0
Fes(h) FES Homo sapiens 89.0
FGFR1(h) FGFR1 Homo sapiens 61.0
FGFR2(h) FGFR2 Homo sapiens 58.0
FGFR3(h) FGFR3 Homo sapiens 99.0
FGFR4(h) FGFR4 Homo sapiens 99.0
Fgr(h) FGR Homo sapiens 93.0
Flt1(h) FLT1 Homo sapiens 96.0
Flt3(h) FLT3 Homo sapiens 7.0
Flt4(h) FLT4 Homo sapiens 73.0
Fms(h) CSF1R Homo sapiens 99.0
Fyn(h) FYN Homo sapiens 97.0
GCK(h) GCK Homo sapiens 97.0
GCN2(h) EIF2AK4 Homo sapiens 100.0
GRK1(h) GRK1 Homo sapiens 72.0
GRK2(h) GRK2 Homo sapiens 102.0
GRK3(h) GRK3 Homo sapiens 106.0
GRK5(h) GRK5 Homo sapiens 98.0
GRK6(h) GRK6 Homo sapiens 96.0
GRK7(h) GRK7 Homo sapiens 78.0
GSK3α(h) GSK3A Homo sapiens 83.0
GSK3β(h) GSK3B Homo sapiens 58.0
Haspin(h) HASPIN Homo sapiens 107.0
Hck(h) HCK Homo sapiens 88.0
Hck(h) activated HCK Homo sapiens 109.0
HIPK1(h) HIPK1 Homo sapiens 100.0
HIPK2(h) HIPK2 Homo sapiens 100.0
HIPK3(h) HIPK3 Homo sapiens 100.0
HIPK4(h) HIPK4 Homo sapiens 105.0
HPK1(h) MAP4K1 Homo sapiens 57.0
HRI(h) EIF2AK1 Homo sapiens 100.0
ICK(h) CILK1 Homo sapiens 99.0
IGF-1R(h) IGF1R Homo sapiens 110.0
IGF-1R(h), activated IGF1R Homo sapiens 121.0
IKKalpha(h) CHUK Homo sapiens 107.0
IKKbeta(h) IKBKB Homo sapiens 106.0
IKKepsilon(h) IKBKE Homo sapiens 108.0
IR(h) INSR Homo sapiens 115.0
IR(h), activated INSR Homo sapiens 89.0
IRE1(h) ERN1 Homo sapiens 104.0
IRR(h) INSRR Homo sapiens 101.0
IRAK1(h) IRAK1 Homo sapiens 99.0
IRAK4(h) IRAK4 Homo sapiens 103.0
Itk(h) ITK Homo sapiens 106.0
JAK1(h) JAK1 Homo sapiens 98.0
JAK2(h) JAK2 Homo sapiens 88.0
JAK3(h) JAK3 Homo sapiens 93.0
JNK1alpha1(h) MAPK8 Homo sapiens 72.0
JNK2alpha2(h) MAPK9 Homo sapiens 88.0
JNK3(h) MAPK10 Homo sapiens 72.0
KDR(h) KDR Homo sapiens 90.0
Lck(h) LCK Homo sapiens 93.0
Lck(h) activated LCK Homo sapiens 108.0
LIMK1(h) LIMK1 Homo sapiens 95.0
LKB1(h) STK11 Homo sapiens 90.0
LOK(h) STK10 Homo sapiens 88.0
Lyn(h) LYN Homo sapiens 110.0
LRRK2(h) LRRK2 Homo sapiens 95.0
LTK(h) LTK Homo sapiens 100.0
MAK(h) MAK Homo sapiens 95.0
MAPK1(h) MAPK1 Homo sapiens 95.0
MAPK2(h) MAPK2 Homo sapiens 102.0
MAP4K3(h) MAP4K3 Homo sapiens 78.0
MAP4K4(h) MAP4K4 Homo sapiens 91.0
MAP4K5(h) MAP4K5 Homo sapiens 95.0
MAPKAP-K2(h) MAPKAPK2 Homo sapiens 97.0
MAPKAP-K3(h) MAPKAPK3 Homo sapiens 106.0
MEK1(h) MAP2K1 Homo sapiens 90.0
MEK2(h) MAP2K2 Homo sapiens 112.0
MARK1(h) MARK1 Homo sapiens 66.0
MARK3(h) MARK3 Homo sapiens 70.0
MARK4(h) MARK4 Homo sapiens 65.0
MEKK2(h) MAP3K2 Homo sapiens 103.0
MELK(h) MELK Homo sapiens 39.0
Mer(h) MERTK Homo sapiens 96.0
Met(h) MET Homo sapiens 1.0
MINK(h) MINK1 Homo sapiens 99.0
MKK6(h) MAP2K6 Homo sapiens 94.0
MKK7beta(h) MAP2K7 Homo sapiens 103.0
MLCK(h) MYLK3 Homo sapiens 32.0
MLK1(h) MAP3K9 Homo sapiens 93.0
MLK2(h) MAP3K10 Homo sapiens 94.0
Mnk2(h) MKNK2 Homo sapiens 110.0
MOK(h) MOK Homo sapiens 115.0
MRCKalpha(h) CDC42BPA Homo sapiens 98.0
MRCKbeta(h) CDC42BPB Homo sapiens 109.0
MSK1(h) RPS6KA5 Homo sapiens 10.0 43.00
MSK2(h) RPS6KA4 Homo sapiens 27.0
MSSK1(h) SRPK3 Homo sapiens 39.0
MST1(h) STK4 Homo sapiens 73.0
MST2(h) STK3 Homo sapiens 47.0
MST3(h) STK24 Homo sapiens 17.0 94.00
MST4(h) STK26 Homo sapiens 84.0
mTOR(h) MTOR Homo sapiens 116.0
mTOR/FKBP12(h) MTOR Homo sapiens 98.0
MuSK(h) MUSK Homo sapiens 91.0
MYLK2(h) MYLK2 Homo sapiens 89.0
MYO3B(h) MYO3B Homo sapiens 24.0
NEK1(h) NEK1 Homo sapiens 102.0
NEK2(h) NEK2 Homo sapiens 91.0
NEK3(h) NEK3 Homo sapiens 102.0
NEK6(h) NEK6 Homo sapiens 94.0
NEK7(h) NEK7 Homo sapiens 112.0
NEK9(h) NEK9 Homo sapiens 47.0
NIM1(h) NIM1K Homo sapiens 93.0
NEK11(h) NEK11 Homo sapiens 103.0
NLK(h) NLK Homo sapiens 91.0
NUAK2(h) NUAK2 Homo sapiens 45.0
p70S6K(h) RPS6KB1 Homo sapiens 76.0
PAK1(h) PAK1 Homo sapiens 94.0
PAK2(h) PAK2 Homo sapiens 105.0
PAK4(h) PAK4 Homo sapiens 91.0
PAK3(h) PAK3 Homo sapiens 100.0
PAK5(h) PAK5 Homo sapiens 86.0
PAK6(h) PAK6 Homo sapiens 86.0
PAR-1Balpha(h) MARK2 Homo sapiens 32.0
PASK(h) PASK Homo sapiens 97.0
PEK(h) EIF2AK3 Homo sapiens 101.0
PDGFRalpha(h) PDGFRA Homo sapiens 102.0
PDGFRbeta(h) PDGFRB Homo sapiens 108.0
PDHK4(h) PDK4 Homo sapiens 101.0
PDK1(h) PDK1 Homo sapiens 85.0
PhKgamma2(h) PHKG2 Homo sapiens 100.0
Pim-1(h) PIM1 Homo sapiens 119.0
Pim-2(h) PIM2 Homo sapiens 102.0
Pim-3(h) PIM3 Homo sapiens 108.0
PKA(h) PRKACA Homo sapiens 103.0
PKAcβ(h) PRKACB Homo sapiens 90.0
PKBalpha (h) AKT1 Homo sapiens 91.0
PKBbeta (h) AKT2 Homo sapiens 105.0
PKBgamma (h) AKT3 Homo sapiens 78.0
PKCalpha (h) PRKCA Homo sapiens 44.0
PKCbetaI (h) PRKCB Homo sapiens 55.0
PKCbetaII (h) PRKCB Homo sapiens 42.0
PKCgamma(h) PRKCG Homo sapiens 47.0
PKCdelta (h) PRKCD Homo sapiens 69.0
PKCepsilon (h) PRKCE Homo sapiens 62.0
PKCeta (h) PRKCH Homo sapiens 92.0
PKCiota (h) PRKCI Homo sapiens 97.0
PKCmu (h) PRKD1 Homo sapiens 96.0
PKCtheta (h) PRKCQ Homo sapiens 33.0
PKCzeta(h) PRKCZ Homo sapiens 99.0
PKD2(h) PRKD2 Homo sapiens 98.0
PKD3(h) PRKD3 Homo sapiens 97.0
PKG1alpha (h) PRKG1 Homo sapiens 68.0
PKG1beta (h) PRKG1 Homo sapiens 78.0
PKR(h) EIF2AK2 Homo sapiens 96.0
Plk1(h) PLK1 Homo sapiens 102.0
Plk3(h) PLK3 Homo sapiens 127.0
PRAK(h) MAPKAPK5 Homo sapiens 87.0
PRKG2(h) PRKG2 Homo sapiens 79.0
PRK1(h) PKN1 Homo sapiens 74.0
PRK2(h) PKN2 Homo sapiens 93.0
PrKX(h) PRKX Homo sapiens 94.0
PRP4(h) PRPF4B Homo sapiens 96.0
PTK5(h) FRK Homo sapiens 91.0
Pyk2(h) PTK2B Homo sapiens 76.0
Ret(h) RET Homo sapiens 23.0
RIPK2(h) RIPK2 Homo sapiens 115.0
ROCK-I(h) ROCK1 Homo sapiens 104.0
ROCK-II(h) ROCK2 Homo sapiens 97.0
Ron(h) MST1R Homo sapiens 102.0
Ros(h) ROS1 Homo sapiens 100.0
Rse(h) TYRO3 Homo sapiens 105.0
Rsk1(h) RPS6KA1 Homo sapiens 7.0 9.00
Rsk2(h) RPS6KA3 Homo sapiens 0.0 52.00
Rsk3(h) RPS6KA2 Homo sapiens 5.0 24.00
Rsk4(h) RPS6KA6 Homo sapiens 2.0
SAPK2a(h) MAPK14 Homo sapiens 101.0
SAPK2b(h) MAPK11 Homo sapiens 110.0
SAPK3(h) MAPK12 Homo sapiens 106.0
SAPK4(h) MAPK13 Homo sapiens 111.0
SGK(h) SGK1 Homo sapiens 79.0
SGK2(h) SGK2 Homo sapiens 70.0
SGK3(h) SGK3 Homo sapiens 95.0
SIK(h) SIK1 Homo sapiens 86.0
SIK2(h) SIK2 Homo sapiens 68.0
SIK3(h) SIK3 Homo sapiens 84.0
SLK(h) SLK Homo sapiens 101.0
Snk(h) PLK2 Homo sapiens 100.0
SNRK(h) SNRK Homo sapiens 113.0
SRPK1(h) SRPK1 Homo sapiens 84.0
SRPK2(h) SRPK2 Homo sapiens 83.0
STK25(h) STK25 Homo sapiens 43.0
STK33(h) STK33 Homo sapiens 55.0
Syk(h) SYK Homo sapiens 106.0
TAK1(h) MAP3K7 Homo sapiens 104.0
TAO1(h) TAOK1 Homo sapiens 97.0
TAO2(h) TAOK2 Homo sapiens 104.0
TAO3(h) TAOK3 Homo sapiens 102.0
TBK1(h) TBK1 Homo sapiens 106.0
Tec(h) activated TEC Homo sapiens 100.0
TGFBR1(h) TGFBR1 Homo sapiens 99.0
Tie2 (h) TEK Homo sapiens 81.0
TLK1(h) TLK1 Homo sapiens 103.0
TLK2(h) TLK2 Homo sapiens 96.0
TNIK(h) TNIK Homo sapiens 49.0
TrkA(h) NTRK1 Homo sapiens 60.0
TrkB(h) NTRK2 Homo sapiens 103.0
TrkC(h) NTRK3 Homo sapiens 133.0
TSSK1(h) TSSK1B Homo sapiens 84.0
TSSK2(h) TSSK2 Homo sapiens 105.0
TSSK3(h) TSSK3 Homo sapiens 110.0
TSSK4(h) TSSK4 Homo sapiens 103.0
TTBK1(h) TTBK1 Homo sapiens 104.0
TTBK2(h) TTBK2 Homo sapiens 108.0
TTK(h) TTK Homo sapiens 90.0
Txk(h) TXK Homo sapiens 111.0
TYK2(h) TYK2 Homo sapiens 87.0
ULK1(h) ULK1 Homo sapiens 26.0
ULK2(h) ULK2 Homo sapiens 84.0
ULK3(h) ULK3 Homo sapiens 59.0
Wee1(h) WEE1 Homo sapiens 96.0
Wee1B(h) WEE2 Homo sapiens 101.0
WNK2(h) WNK2 Homo sapiens 87.0
WNK3(h) WNK3 Homo sapiens 103.0
VRK2(h) VRK2 Homo sapiens 98.0
Yes(h) YES1 Homo sapiens 90.0
ZAK(h) MAP3K20 Homo sapiens 99.0
ZAP-70(h) ZAP70 Homo sapiens 119.0
ZIPK(h) DAPK3 Homo sapiens 91.0
ATM(h) ATM Homo sapiens 99.0
ATR/ATRIP(h) ATR Homo sapiens 94.0
DNA-PK(h) PRKDC Homo sapiens 94.0
PI3 Kinase(p110b/p85a)(h) PIK3CB Homo sapiens 99.0
PI3 Kinase (p120g)(h) PIK3CG Homo sapiens 99.0
PI3 Kinase(p110d/p85a)(h) PIK3CD Homo sapiens 103.0
PI3 Kinase(p110a/p85a)(h) PIK3CA Homo sapiens 99.0
PI3KC2a(h) PIK3C2A Homo sapiens 103.0
PI3KC2g(h) PIK3C2G Homo sapiens 100.0
PIP4K2a(h) PIP4K2A Homo sapiens 105.0
PIP5K1a(h) PIP5K1A Homo sapiens 100.0
PIP5K1g(h) PIP5K1C Homo sapiens 97.0
 

BAY-3827

Proliferation assays were performed in a panel of cells with dysregulated C-MYC (COLO 320DM, LS-174T, Ramos, SNU-16, SU-DHL-10, OCI-LY7 and JJN-3) or N-MYC (IMR-32 and IMR-5/75). Colo201 and SK-N-F1 were used as control cell lines (without C-MYC/N-MYC dysregulation). Cell viability was determined by CellTiter Glo ® after treatment with BAY 3827 for the indicated time. Shown are data from PMID: 33492659 (Table 2 and Supplementary Table 3) .

Conclusion: Strong inhibitory effects were observed for LNCaP and VCaP cells, two prostate cancer cell lines that are responsive to androgen stimulation, whereas no activity was observed in andogen receptor (AR)-negative prostate cancer cell lines. BAY-3827 also inhibited multiple myeloma cell lines. BAY-3827 did not inhibit cell proliferation in cancer cell lines with dysregulated MYC signaling. BAY-974 had no anti-proliferative activity on prostate cancer cell lines (data not shown).

Tumor type Cell line Species Cell Proliferation IC50 [µM] Time [day]
Colon COLO 320 Homo sapiens 22.20 3
Colon LS-174T Homo sapiens 30.00 3
B lymphocyte Ramos Homo sapiens 12.10 3
Stomach SNU-16 Homo sapiens 12.00 3
lymphnode SU-DHL-10 Homo sapiens 12.50 3
B lymphocyte Oci-Ly-7 Homo sapiens 12.20 3
Plasma cell JJN3 Homo sapiens 20.00 3
Colon COLO 201, control Homo sapiens 16.00 3
Brain (neuroblast) IMR-32 Homo sapiens 11.50 6
Brain (neuroblast) IMR-5/75 Homo sapiens 21.30 6
Bone marrow SK-N-F1, control Homo sapiens 21.20 6
B lymphocyte REC-1 Homo sapiens 3.30 3
Lymphoblast RAJI Homo sapiens 33.00 3
Lympoma Daudi Homo sapiens 22.90 3
Plasma cell L-363 Homo sapiens 10.80 3
Plasma-cytoma AMO-1 Homo sapiens 33.00 3
Multiple myeloma LP-1 Homo sapiens 1.90 3
Multiple myeloma OPM-2 Homo sapiens 1.50 3
Bladder SW780 Homo sapiens 10.30 3
Bone U2-OS Homo sapiens 18.70 3
Brain U251 Homo sapiens 20.90 3
Breast MDA-MB- 231 Homo sapiens 30.00 3
Breast MDA-MB- 453 Homo sapiens 14.60 3
Cervix HeLa Homo sapiens 25.70 3
Colon SW480 Homo sapiens 27.80 3
Liver Snu398 Homo sapiens 7.30 3
Lung A549 Homo sapiens 25.80 3
Lung NCI- H292 Homo sapiens 17.10 3
Lung NCI- H460 Homo sapiens 33.00 3
Lung NCI- H520 Homo sapiens 24.10 3
Ovary A2780 Homo sapiens 33.00 3
Pancreas BxPC3 Homo sapiens 11.40 3
Pancreas PANC-1 Homo sapiens 17.10 3
Skin A375 Homo sapiens 22.80 3
Stomach Snu16 Homo sapiens 11.60 3
Prostate LNCaP Homo sapiens 0.28 6
Prostate VCaP Homo sapiens 1.71 6
Prostate 22Rv1 Homo sapiens 5.55 6
Prostate C4-2B Homo sapiens 10.00 6
Prostate PC-3 Homo sapiens 10.00 6
Prostate DU-145 Homo sapiens 10.00 6