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Selectivity data for probe BAY-293 and control BAY-294


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BAY-293


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
H1 HRH1 49.37
H2 HRH2 100.01 139.82 average (n=2) 6.86
5-HT1A HTR1A 56.47 3629.42 average (n=2) 5.48
5-HT1B HTR1B 66.11 1407.51 average (n=2) 5.87
5-HT1D HTR1D 98.14 181.12 average (n=2) 6.77
Sigma 1 SIGMAR1 22.56
Sigma 2 TMEM97 94.79 179.81 average (n=2) 6.75
5-HT1E HTR1E 5.81
5-HT2A HTR2A 98.54 133.44 average (n=2) 6.96
5-HT2B HTR2B 86.94 623.09 average (n=2) 6.21
5-HT2C HTR2C 73.71 3399.46 average (n=2) 5.54
5-HT3 HTR3A 17.12
5-HT5A HTR5A 68.47 2549.48 average (n=2) 5.67
5-HT6 HTR6 -1.41
5-HT7A HTR7 76.22 1734.98 average (n=2) 5.77
GABAA/BZP 12.31
D1 DRD1 82.72 1266.19 5.90
D2 DRD2 32.33
D3 DRD3 56.82 936.32 average (n=2) 6.03
D4 DRD4 56.71 2660.95 average (n=2) 5.58
DAT SLC6A3 77.24 522.03 average (n=3) 6.32
DOR OPRD1 5.63
KOR OPRK1 26.95
MOR OPRM1 46.82
Alpha1A ADRA1A 71.58 428.25 6.37
Alpha1B ADRA1B 85.77 264.61 6.58
Alpha1D ADRA1D 74.98 337.65 average (n=2) 6.47
Alpha2A ADRA2A 91.74 381.33 6.42
Alpha2B ADRA2B 64.20 1226.87 5.91
Alpha2C ADRA2C 94.20 130.87 average (n=2) 6.89
D5 DRD5 32.47
M1 CHRM1 88.77 237.75 average (n=2) 6.68
M3 CHRM3 56.45 972.03 average (n=2) 6.02
M4 CHRM4 43.11
M5 CHRM5 64.75 956.13 average (n=2) 6.03
NET SLC6A2 84.01 982.16 average (n=2) 6.06
GABA/PBR 13.08
H3 HRH3 26.73
M2 CHRM2 74.19 511.68 6.29
SERT SLC6A4 47.44
Beta2 ADRB2 12.05
H4 HRH4 42.13
Beta1 ADRB1 -11.17
Beta3 ADRB3 19.97
GABAA 0.89

BAY-294


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABAA -1.27
Beta2 ADRB2 18.20
H4 HRH4 66.95 1885.82 5.72
SERT SLC6A4 56.17 4231.56 5.37
M2 CHRM2 65.43 1474.01 5.83
H1 HRH1 56.74 1365.75 average (n=2) 5.87
H2 HRH2 100.93 21.13 average (n=2) 7.68
5-HT1A HTR1A 93.75 390.80 average (n=2) 6.41
5-HT1B HTR1B 75.02 1757.20 average (n=2) 5.76
5-HT1D HTR1D 98.91 93.49 average (n=2) 7.04
Sigma 1 SIGMAR1 48.99
Sigma 2 TMEM97 83.20 637.88 average (n=2) 6.22
5-HT1E HTR1E 10.83
5-HT2A HTR2A 99.18 69.37 average (n=2) 7.16
5-HT2B HTR2B 97.29 74.56 average (n=2) 7.13
5-HT2C HTR2C 71.78 706.49 average (n=3) 6.16
5-HT3 HTR3A 15.99
5-HT5A HTR5A 78.10 1057.57 average (n=2) 6.01
5-HT6 HTR6 20.19
5-HT7A HTR7 70.65 699.54 average (n=2) 6.16
GABAA/BZP 9.67
D1 DRD1 89.17 717.65 average (n=3) 6.25
D2 DRD2 50.60 2333.64 average (n=2) 5.70
D3 DRD3 64.75 868.61 average (n=2) 6.06
D4 DRD4 31.01
DAT SLC6A3 70.33 1672.13 average (n=3) 5.85
DOR OPRD1 10.53
KOR OPRK1 64.43 841.37 average (n=2) 6.09
MOR OPRM1 67.32 854.25 average (n=2) 6.12
Alpha1A ADRA1A 83.44 453.53 average (n=2) 6.36
Alpha1B ADRA1B 94.74 95.26 average (n=2) 7.07
Alpha1D ADRA1D 81.17 397.13 average (n=2) 6.41
Alpha2A ADRA2A 93.51 127.42 average (n=2) 6.90
Alpha2B ADRA2B 82.93 846.75 average (n=2) 6.09
Alpha2C ADRA2C 94.20 95.18 average (n=2) 7.04
D5 DRD5 36.60
M1 CHRM1 89.09 314.14 average (n=3) 6.65
M3 CHRM3 48.01
M4 CHRM4 59.37 303.26 average (n=2) 6.54
M5 CHRM5 54.07 523.93 average (n=2) 6.28
NET SLC6A2 69.28 2083.21 average (n=2) 5.68
GABA/PBR -11.42
H3 HRH3 24.64
Beta1 ADRB1 -10.87
Beta3 ADRB3 38.21

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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-293


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 95.0 1000
ABL1 ABL1-phosphorylated 97.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 91.0 1000
ACVR2A ACVR2A 94.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 87.0 1000
COQ8A ADCK3 92.0 1000
COQ8B ADCK4 65.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 72.0 1000
AKT3 AKT3 92.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 97.0 1000
ANKK1 ANKK1 76.0 1000
NUAK1 ARK5 97.0 1000
MAP3K5 ASK1 91.0 1000
MAP3K6 ASK2 99.0 1000
AURKA AURKA 73.0 1000
AURKB AURKB 77.0 1000
AURKC AURKC 92.0 1000
AXL AXL 93.0 1000
BMP2K BIKE 87.0 1000
BLK BLK 91.0 1000
BMPR1A BMPR1A 91.0 1000
BMPR1B BMPR1B 83.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 49.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 87.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 90.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 95.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 93.0 1000
CAMK2A CAMK2A 99.0 1000
CAMK2B CAMK2B 92.0 1000
CAMK2D CAMK2D 99.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 88.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 81.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 91.0 1000
CDK13 CDC2L5 89.0 1000
CDK19 CDK11 85.0 1000
CDK2 CDK2 82.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 90.0 1000
CDK5 CDK5 78.0 1000
CDK7 CDK7 63.0 1000
CDK8 CDK8 68.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 93.0 1000
CDKL2 CDKL2 99.0 1000
CDKL3 CDKL3 99.0 1000
CDKL5 CDKL5 94.0 1000
CHEK1 CHEK1 92.0 1000
CHEK2 CHEK2 76.0 1000
CIT CIT 92.0 1000
CLK1 CLK1 98.0 1000
CLK2 CLK2 98.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 73.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 82.0 1000
CSNK1E CSNK1E 99.0 1000
CSNK1G1 CSNK1G1 88.0 1000
CSNK1G2 CSNK1G2 98.0 1000
CSNK1G3 CSNK1G3 99.0 1000
CSNK2A1 CSNK2A1 83.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 57.0 1000
DAPK1 DAPK1 99.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 86.0 1000
DCLK2 DCAMKL2 99.0 1000
DCLK3 DCAMKL3 95.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 92.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 86.0 1000
CDC42BPG DMPK2 98.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 92.0 1000
DYRK1A DYRK1A 88.0 1000
DYRK1B DYRK1B 64.0 1000
DYRK2 DYRK2 92.0 1000
EGFR EGFR(T790M) 68.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 79.0 1000
EPHA2 EPHA2 76.0 1000
EPHA3 EPHA3 87.0 1000
EPHA4 EPHA4 79.0 1000
EPHA5 EPHA5 88.0 1000
EPHA6 EPHA6 96.0 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 99.0 1000
EPHB6 EPHB6 98.0 1000
ERBB2 ERBB2 84.0 1000
ERBB3 ERBB3 76.0 1000
ERBB4 ERBB4 97.0 1000
MAPK3 ERK1 94.0 1000
MAPK1 ERK2 78.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 94.0 1000
MAPK7 ERK5 97.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 86.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 85.0 1000
FGFR3 FGFR3(G697C) 85.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 87.0 1000
FLT3 FLT3-autoinhibited 88.0 1000
FLT4 FLT4 83.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 88.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 99.0 1000
GRK1 GRK1 99.0 1000
GRK2 GRK2 86.0 1000
GRK3 GRK3 98.0 1000
GRK4 GRK4 80.0 1000
GRK7 GRK7 83.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 90.0 1000
HASPIN HASPIN 98.0 1000
HCK HCK 97.0 1000
HIPK1 HIPK1 78.0 1000
HIPK2 HIPK2 86.0 1000
HIPK3 HIPK3 83.0 1000
HIPK4 HIPK4 86.0 1000
MAP4K1 HPK1 83.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 82.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 94.0 1000
IKBKE IKK-epsilon 71.0 1000
INSR INSR 79.0 1000
INSRR INSRR 95.0 1000
IRAK1 IRAK1 71.0 1000
IRAK3 IRAK3 75.0 1000
IRAK4 IRAK4 76.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 73.0 1000
JAK2 JAK2(JH1domain-catalytic) 67.0 1000
JAK3 JAK3(JH1domain-catalytic) 94.0 1000
MAPK8 JNK1 66.0 1000
MAPK9 JNK2 71.0 1000
MAPK10 JNK3 71.0 1000
KIT KIT-autoinhibited 81.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 98.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 99.0 1000
LIMK2 LIMK2 96.0 1000
STK11 LKB1 96.0 1000
STK10 LOK 95.0 1000
LRRK2 LRRK2(G2019S) 72.0 1000
LTK LTK 97.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 80.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 72.0 1000
MAP3K15 MAP3K15 60.0 1000
MAP3K2 MAP3K2 87.0 1000
MAP3K3 MAP3K3 83.0 1000
MAP3K4 MAP3K4 73.0 1000
MAP4K2 MAP4K2 91.0 1000
MAP4K3 MAP4K3 99.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 83.0 1000
MAPKAPK5 MAPKAPK5 88.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 99.0 1000
MARK3 MARK3 89.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 76.0 1000
MAP2K1 MEK1 86.0 1000
MAP2K2 MEK2 82.0 1000
MAP2K3 MEK3 80.0 1000
MAP2K4 MEK4 86.0 1000
MAP2K5 MEK5 91.0 1000
MAP2K6 MEK6 86.0 1000
MELK MELK 53.0 1000
MERTK MERTK 61.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 57.0 1000
MAP2K7 MKK7 79.0 1000
MKNK1 MKNK1 83.0 1000
MKNK2 MKNK2 63.0 1000
MYLK3 MLCK 96.0 1000
MAP3K9 MLK1 98.0 1000
MAP3K10 MLK2 96.0 1000
MAP3K11 MLK3 99.0 1000
CDC42BPA MRCKA 67.0 1000
CDC42BPB MRCKB 89.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 85.0 1000
STK24 MST3 100.0 1000
STK26 MST4 99.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 93.0 1000
MYLK MYLK 84.0 1000
MYLK2 MYLK2 91.0 1000
MYLK4 MYLK4 99.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 47.0 1000
STK38 NDR1 60.0 1000
STK38L NDR2 86.0 1000
NEK1 NEK1 91.0 1000
NEK10 NEK10 73.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 92.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 83.0 1000
NEK5 NEK5 99.0 1000
NEK6 NEK6 96.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 93.0 1000
NIM1K NIM1 93.0 1000
NLK NLK 84.0 1000
OXSR1 OSR1 67.0 1000
MAPK14 p38-alpha 87.0 1000
MAPK11 p38-beta 86.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 97.0 1000
PAK2 PAK2 88.0 1000
PAK3 PAK3 86.0 1000
PAK4 PAK4 97.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 95.0 1000
CDK16 PCTK1 87.0 1000
CDK17 PCTK2 94.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 84.0 1000
PDGFRB PDGFRB 91.0 1000
PDPK1 PDPK1 92.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 76.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 83.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 86.0 1000
PIK3C2G PIK3C2G 59.0 1000
PIK3CA PIK3CA(Q546K) 89.0 1000
PIK3CB PIK3CB 96.0 1000
PIK3CD PIK3CD 75.0 1000
PIK3CG PIK3CG 67.0 1000
PI4KB PIK4CB 82.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 97.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 83.0 1000
PIP5K1A PIP5K1A 75.0 1000
PIP5K1C PIP5K1C 88.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 92.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 93.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 89.0 1000
PKNB PKNB(M.tuberculosis) 76.0 1000
PLK1 PLK1 80.0 1000
PLK2 PLK2 82.0 1000
PLK3 PLK3 91.0 1000
PLK4 PLK4 74.0 1000
PRKCD PRKCD 98.0 1000
PRKCE PRKCE 74.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 90.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 92.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 85.0 1000
EIF2AK2 PRKR 90.0 1000
PRKX PRKX 67.0 1000
PRPF4B PRP4 96.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 90.0 1000
RAF1 RAF1 70.0 1000
RET RET(V804M) 90.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 94.0 1000
RIPK1 RIPK1 97.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 91.0 1000
DSTYK RIPK5 83.0 1000
ROCK1 ROCK1 91.0 1000
ROCK2 ROCK2 93.0 1000
ROS1 ROS1 84.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 76.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 86.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 81.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 95.0 1000
SGK3 SGK3 78.0 1000
SIK1 SIK 91.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 97.0 1000
NUAK2 SNARK 97.0 1000
SNRK SNRK 78.0 1000
SRC SRC 100.0 1000
SRMS SRMS 92.0 1000
SRPK1 SRPK1 90.0 1000
SRPK2 SRPK2 61.0 1000
SRPK3 SRPK3 84.0 1000
STK16 STK16 97.0 1000
STK33 STK33 45.0 1000
STK35 STK35 91.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 70.0 1000
TAOK1 TAOK1 95.0 1000
TAOK2 TAOK2 86.0 1000
TAOK3 TAOK3 83.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 83.0 1000
TGFBR1 TGFBR1 74.0 1000
TGFBR2 TGFBR2 91.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 87.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 90.0 1000
TNIK TNIK 85.0 1000
TNK1 TNK1 64.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 87.0 1000
NTRK2 TRKB 88.0 1000
NTRK3 TRKC 88.0 1000
TRPM6 TRPM6 91.0 1000
TSSK1B TSSK1B 59.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 97.0 1000
TXK TXK 76.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 71.0 1000
TYRO3 TYRO3 89.0 1000
ULK1 ULK1 88.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 78.0 1000
KDR VEGFR2 93.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 89.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 88.0 1000
WNK2 WNK2 72.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 76.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 60.0 1000
YES1 YES 100.0 1000
STK25 YSK1 89.0 1000
MAP3K19 YSK4 71.0 1000
MAP3K20 ZAK 75.0 1000
ZAP70 ZAP70 87.0 1000

BAY-294


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 94.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 76.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 91.0 1000
COQ8B ADCK4 93.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 90.0 1000
AKT3 AKT3 95.0 1000
ALK ALK(L1196M) 93.0 1000
PRKAA1 AMPK-alpha1 93.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 90.0 1000
NUAK1 ARK5 90.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 73.0 1000
AURKB AURKB 99.0 1000
AURKC AURKC 94.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 79.0 1000
BLK BLK 94.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 58.0 1000
BRAF BRAF(V600E) 84.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 89.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 89.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 96.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 97.0 1000
CAMK2G CAMK2G 90.0 1000
CAMK4 CAMK4 99.0 1000
CAMKK1 CAMKK1 99.0 1000
CAMKK2 CAMKK2 82.0 1000
CASK CASK 71.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 93.0 1000
CDK19 CDK11 88.0 1000
CDK2 CDK2 91.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 96.0 1000
CDK5 CDK5 98.0 1000
CDK7 CDK7 61.0 1000
CDK8 CDK8 84.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 97.0 1000
CDKL5 CDKL5 87.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 87.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 95.0 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 74.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 95.0 1000
CSNK1E CSNK1E 91.0 1000
CSNK1G1 CSNK1G1 92.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 93.0 1000
CSNK2A1 CSNK2A1 91.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 51.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 87.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 94.0 1000
MAP3K12 DLK 97.0 1000
DMPK DMPK 85.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 80.0 1000
DYRK1B DYRK1B 55.0 1000
DYRK2 DYRK2 96.0 1000
EGFR EGFR(T790M) 76.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 80.0 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 87.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 87.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 95.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 92.0 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 91.0 1000
FLT3 FLT3-autoinhibited 93.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 90.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 91.0 1000
GRK4 GRK4 97.0 1000
GRK7 GRK7 89.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 98.0 1000
HIPK1 HIPK1 79.0 1000
HIPK2 HIPK2 76.0 1000
HIPK3 HIPK3 97.0 1000
HIPK4 HIPK4 91.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 86.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 90.0 1000
IKBKB IKK-beta 83.0 1000
IKBKE IKK-epsilon 85.0 1000
INSR INSR 89.0 1000
INSRR INSRR 93.0 1000
IRAK1 IRAK1 80.0 1000
IRAK3 IRAK3 83.0 1000
IRAK4 IRAK4 89.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 68.0 1000
JAK2 JAK2(JH1domain-catalytic) 63.0 1000
JAK3 JAK3(JH1domain-catalytic) 99.0 1000
MAPK8 JNK1 81.0 1000
MAPK9 JNK2 71.0 1000
MAPK10 JNK3 74.0 1000
KIT KIT-autoinhibited 70.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 95.0 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) 84.0 1000
LTK LTK 98.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 91.0 1000
MAK MAK 97.0 1000
MAP3K1 MAP3K1 97.0 1000
MAP3K15 MAP3K15 77.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 87.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 97.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 97.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 80.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 96.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 98.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 87.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 74.0 1000
MERTK MERTK 72.0 1000
MET MET(Y1235D) 98.0 1000
MINK1 MINK 88.0 1000
MAP2K7 MKK7 81.0 1000
MKNK1 MKNK1 91.0 1000
MKNK2 MKNK2 71.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 92.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 89.0 1000
STK24 MST3 100.0 1000
STK26 MST4 97.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 90.0 1000
MYLK MYLK 94.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 87.0 1000
STK38 NDR1 87.0 1000
STK38L NDR2 94.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 78.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 92.0 1000
NEK3 NEK3 87.0 1000
NEK4 NEK4 83.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 90.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 78.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 99.0 1000
PAK2 PAK2 97.0 1000
PAK3 PAK3 87.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 83.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 92.0 1000
PDGFRB PDGFRB 99.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 81.0 1000
PK5 PFPK5(P.falciparum) 71.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 87.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 84.0 1000
PIK3CB PIK3CB 89.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 73.0 1000
PI4KB PIK4CB 74.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 92.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 100.0 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 90.0 1000
PKNB PKNB(M.tuberculosis) 90.0 1000
PLK1 PLK1 85.0 1000
PLK2 PLK2 83.0 1000
PLK3 PLK3 87.0 1000
PLK4 PLK4 76.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 78.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 87.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 99.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 93.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 76.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 78.0 1000
RAF1 RAF1 65.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 96.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 75.0 1000
DSTYK RIPK5 78.0 1000
ROCK1 ROCK1 93.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 82.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 78.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 83.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 91.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 93.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 93.0 1000
SRC SRC 100.0 1000
SRMS SRMS 88.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 52.0 1000
SRPK3 SRPK3 89.0 1000
STK16 STK16 100.0 1000
STK33 STK33 73.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 75.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 90.0 1000
TAOK3 TAOK3 75.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 80.0 1000
TGFBR2 TGFBR2 97.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 99.0 1000
TNK1 TNK1 85.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 87.0 1000
NTRK2 TRKB 98.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 93.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 76.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 91.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 88.0 1000
KDR VEGFR2 91.0 1000
PIK3C3 VPS34 93.0 1000
VRK2 VRK2 73.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 99.0 1000
WNK3 WNK3 98.0 1000
WNK4 WNK4 90.0 1000
STK32A YANK1 91.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 71.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 78.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 100.0 1000

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BAY-293

Results are significant for > 50 % inhibition.

Conclusion: There are many off-targets. The clostest off-targets are 5-HT2A (110 % inhibition), α1A (106 %), KOP (105 %), 5-HT2C(104 %) and 5-HT2B (100 %).

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [nM] Assay ID
Adrenergic alpha1A ADRA1A Rattus sp. 10 µM 106.0 Prazosin 0.69 203100
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM 99.0 Yohimbine 203630
Adrenergic alpha2B ADRA2B Homo sapiens 10 µM 85.0 Yohimbine 14.00 203710
Adrenergic alpha2C ADRA2C Homo sapiens 10 µM 99.0 Yohimbine 203810
Dopamine D1 DRD1 Homo sapiens 10 µM 85.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2L DRD2 Homo sapiens 10 µM 67.0 Spiperone 219600
Dopamine D2S DRD2 Homo sapiens 10 µM 71.0 Spiperone 0.25 219700
Dopamine D3 DRD3 Homo sapiens 10 µM 88.0 Spiperone 0.36 219800
Histamine H2 HRH2 Homo sapiens 10 µM 99.0 Tiotidine 22.00 239710
Muscarinic M1 CHRM1 Homo sapiens 10 µM 94.0 4-DAMP 4.50 252610
Opiate kappa (OPZ, KOP) OPRK1 Homo sapiens 10 µM 105.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 93.0 DAMGO 20.00 260410
Serotonin (5-Hydroxytryptamine) 5-HT1A HTR1A Homo sapiens 10 µM 81.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT2A HTR2A Homo sapiens 10 µM 110.0 Ketanserin 271650
Serotonin (5-Hydroxytryptamine) 5-HT2B HTR2B Homo sapiens 10 µM 100.0 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT2C HTR2C Homo sapiens 10 µM 104.0 SBZ4Z084 1.00 271800
Transporter, Adenosine Cavia porcellus 10 µM 62.0 Nitrobenzylthioinosine 0.85 202000
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 90.0 GBR-1Z909 1.70 220320
Transporter, GABA Rattus sp. 10 µM 71.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 86.0 Desipramine 0.93 204410
 

BAY-293

Results are expressed as percent residual kinase activity. Shown are the top kinases from the 358 kinases tested at 1 µM.

Conclusion: Clean panel: All tested kinases retain activity > 67%.

Target protein HGNC name Species % residual kinase activity at 1 µM
CK2alpha2(h) CSNK2A2 Homo sapiens 67.0
DYRK1A(h) DYRK1A Homo sapiens 68.0
IGF-1R(h) IGF1R Homo sapiens 74.0
LTK(h) LTK Homo sapiens 75.0
Syk(h) SYK Homo sapiens 79.0
TrkB(h) NTRK2 Homo sapiens 79.0
TSSK1(h) TSSK1B Homo sapiens 79.0
CHK2(h) CHEK2 Homo sapiens 80.0
TrkC(h) NTRK3 Homo sapiens 80.0
Ret(h) RET Homo sapiens 81.0
Flt4(h) FLT4 Homo sapiens 82.0
PASK(h) PASK Homo sapiens 84.0
PDHK2(h) PDK2 Homo sapiens 85.0
CDK1/cyclinB(h) CDK1 Homo sapiens 87.0
PEK(h) EIF2AK3 Homo sapiens 87.0
TTBK1(h) TTBK1 Homo sapiens 87.0
Axl(h) AXL Homo sapiens 88.0
Flt1(h) FLT1 Homo sapiens 88.0
Lyn(h) LYN Homo sapiens 88.0
MST4(h) STK26 Homo sapiens 88.0
PAK6(h) PAK6 Homo sapiens 88.0
PKCepsilon(h) PRKCE Homo sapiens 88.0
ATR/ATRIP(h) ATR Homo sapiens 88.0
EphA3(h) EPHA3 Homo sapiens 89.0
PhKgamma2(h) PHKG2 Homo sapiens 89.0
Pim-1(h) PIM1 Homo sapiens 89.0
Rse(h) TYRO3 Homo sapiens 89.0