Selectivity data for probe BAY-1797 and control BAY-207


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BAY-1797


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 14.31
Beta3 ADRB3 46.33
GABAA/BZP 0.73
GABAA -11.81
GABA/PBR 5.06
D4 DRD4 28.45
D5 DRD5 27.71
DAT SLC6A3 36.99
H4 HRH4 -3.13
KOR OPRK1 20.32
MOR OPRM1 19.34
NET SLC6A2 0.53
Alpha1A ADRA1A 5.04
Alpha1B ADRA1B -0.38
Alpha1D ADRA1D 2.32
Alpha2A ADRA2A 6.31
Alpha2B ADRA2B 56.60 4285.88 average (n=2) 5.37
Sigma 1 SIGMAR1 -8.20
Sigma 2 TMEM97 59.47 4344.21 average (n=2) 5.38
5-HT1A HTR1A -1.77
5-HT1B HTR1B -2.93
5-HT1D HTR1D 1.74
5-HT1E HTR1E -12.68
5-HT2A HTR2A -2.50
5-HT2B HTR2B 30.18
5-HT6 HTR6 17.21
5-HT7A HTR7 35.22
D1 DRD1 21.62
D2 DRD2 -7.81
D3 DRD3 0.87
5-HT2C HTR2C 55.36 6519.91 average (n=2) 5.23
5-HT3 HTR3A 19.90
5-HT5A HTR5A 1.47
Beta2 ADRB2 18.88
DOR OPRD1 20.47
H1 HRH1 15.66
H2 HRH2 -4.85
H3 HRH3 -10.87
M1 CHRM1 11.38
M2 CHRM2 -8.33
M3 CHRM3 -0.53
M4 CHRM4 10.21
M5 CHRM5 16.73
SERT SLC6A4 22.68
Alpha2C ADRA2C 18.19

BAY-207


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 -3.09
Beta3 ADRB3 -5.77
H4 HRH4 0.09
5-HT1B HTR1B 4.81
5-HT1D HTR1D 6.75
5-HT1E HTR1E -1.46
5-HT6 HTR6 -4.73
5-HT7A HTR7 17.33
Beta2 ADRB2 -10.67
D1 DRD1 3.57
D2 DRD2 -9.74
DOR OPRD1 41.61
H3 HRH3 3.87
KOR OPRK1 21.18
M1 CHRM1 -3.55
M5 CHRM5 14.65
5-HT1A HTR1A 4.89
GABAA/BZP 3.19
D3 DRD3 10.53
D4 DRD4 26.99
D5 DRD5 20.83
GABAA -10.82
H1 HRH1 17.89
H2 HRH2 11.49
MOR OPRM1 40.25
5-HT2A HTR2A 11.27
5-HT2B HTR2B 21.09
5-HT2C HTR2C 19.53
5-HT3 HTR3A 3.19
5-HT5A HTR5A 5.57
Alpha1A ADRA1A 15.13
Alpha1B ADRA1B -8.97
Alpha1D ADRA1D 6.88
Alpha2A ADRA2A 40.81
Alpha2B ADRA2B 43.40
Alpha2C ADRA2C 89.61 654.33 6.18
M4 CHRM4 -1.95
NET SLC6A2 22.40
Sigma 2 TMEM97 82.02 1941.33 5.71
DAT SLC6A3 -12.86
M2 CHRM2 2.03
SERT SLC6A4 8.86
Sigma 1 SIGMAR1 18.61
M3 CHRM3 17.95
GABA/PBR 87.47 250.13 average (n=2) 6.62

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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-1797


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 88.0 1000
ABL1 ABL1-phosphorylated 75.0 1000
ABL2 ABL2 87.0 1000
ACVR1 ACVR1 84.0 1000
ACVR1B ACVR1B 98.0 1000
ACVR2A ACVR2A 95.0 1000
ACVR2B ACVR2B 75.0 1000
ACVRL1 ACVRL1 99.0 1000
COQ8A ADCK3 94.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 62.0 1000
PRKAA1 AMPK-alpha1 71.0 1000
PRKAA2 AMPK-alpha2 82.0 1000
ANKK1 ANKK1 78.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 72.0 1000
AURKA AURKA 69.0 1000
AURKB AURKB 58.0 1000
AURKC AURKC 100.0 1000
AXL AXL 93.0 1000
BMP2K BIKE 94.0 1000
BLK BLK 68.0 1000
BMPR1A BMPR1A 69.0 1000
BMPR1B BMPR1B 94.0 1000
BMPR2 BMPR2 73.0 1000
BMX BMX 94.0 1000
BRAF BRAF(V600E) 89.0 1000
PTK6 BRK 96.0 1000
BRSK1 BRSK1 91.0 1000
BRSK2 BRSK2 91.0 1000
BTK BTK 76.0 1000
BUB1 BUB1 1.6 1000
CAMK1 CAMK1 90.0 1000
PNCK CAMK1B 83.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 84.0 1000
CAMK2A CAMK2A 96.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 97.0 1000
CAMK2G CAMK2G 86.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 91.0 1000
CASK CASK 86.0 1000
CDK11B CDC2L1 71.0 1000
CDK11A CDC2L2 95.0 1000
CDK13 CDC2L5 92.0 1000
CDK19 CDK11 91.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 92.0 1000
CDK4 CDK4-cyclinD3 71.0 1000
CDK5 CDK5 61.0 1000
CDK7 CDK7 64.0 1000
CDK8 CDK8 68.0 1000
CDK9 CDK9 92.0 1000
CDKL1 CDKL1 98.0 1000
CDKL2 CDKL2 99.0 1000
CDKL3 CDKL3 95.0 1000
CDKL5 CDKL5 83.0 1000
CHEK1 CHEK1 99.0 1000
CHEK2 CHEK2 81.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 67.0 1000
CLK2 CLK2 91.0 1000
CLK3 CLK3 83.0 1000
CLK4 CLK4 83.0 1000
CSF1R CSF1R-autoinhibited 51.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 93.0 1000
CSNK1A1L CSNK1A1L 74.0 1000
CSNK1D CSNK1D 93.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 89.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 74.0 1000
CSNK2A1 CSNK2A1 96.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 68.0 1000
DAPK1 DAPK1 90.0 1000
DAPK2 DAPK2 90.0 1000
DAPK3 DAPK3 95.0 1000
DCLK1 DCAMKL1 86.0 1000
DCLK2 DCAMKL2 99.0 1000
DCLK3 DCAMKL3 92.0 1000
DDR1 DDR1 94.0 1000
DDR2 DDR2 87.0 1000
MAP3K12 DLK 80.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 94.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 95.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 83.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 91.0 1000
EPHA3 EPHA3 78.0 1000
EPHA4 EPHA4 97.0 1000
EPHA5 EPHA5 62.0 1000
EPHA6 EPHA6 83.0 1000
EPHA7 EPHA7 92.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 93.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 94.0 1000
EPHB4 EPHB4 98.0 1000
EPHB6 EPHB6 92.0 1000
ERBB2 ERBB2 87.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 56.0 1000
MAPK3 ERK1 94.0 1000
MAPK1 ERK2 71.0 1000
MAPK6 ERK3 98.0 1000
MAPK4 ERK4 91.0 1000
MAPK7 ERK5 83.0 1000
MAPK15 ERK8 68.0 1000
ERN1 ERN1 73.0 1000
PTK2 FAK 96.0 1000
FER FER 73.0 1000
FES FES 92.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 61.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 95.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 80.0 1000
FLT3 FLT3-autoinhibited 90.0 1000
FLT4 FLT4 79.0 1000
FRK FRK 98.0 1000
FYN FYN 69.0 1000
GAK GAK 99.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 83.0 1000
GRK2 GRK2 97.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 77.0 1000
GSK3A GSK3A 93.0 1000
GSK3B GSK3B 80.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 54.0 1000
HIPK1 HIPK1 80.0 1000
HIPK2 HIPK2 62.0 1000
HIPK3 HIPK3 84.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 91.0 1000
HUNK HUNK 84.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 63.0 1000
IKBKB IKK-beta 91.0 1000
IKBKE IKK-epsilon 69.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 73.0 1000
IRAK3 IRAK3 87.0 1000
IRAK4 IRAK4 91.0 1000
ITK ITK 87.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 87.0 1000
JAK2 JAK2(JH1domain-catalytic) 73.0 1000
JAK3 JAK3(JH1domain-catalytic) 96.0 1000
MAPK8 JNK1 69.0 1000
MAPK9 JNK2 83.0 1000
MAPK10 JNK3 89.0 1000
KIT KIT-autoinhibited 87.0 1000
LATS1 LATS1 79.0 1000
LATS2 LATS2 94.0 1000
LCK LCK 70.0 1000
LIMK1 LIMK1 87.0 1000
LIMK2 LIMK2 88.0 1000
STK11 LKB1 51.0 1000
STK10 LOK 65.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 87.0 1000
LYN LYN 99.0 1000
MAP3K13 LZK 73.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 66.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 84.0 1000
MAP3K3 MAP3K3 71.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 84.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 71.0 1000
MAP4K5 MAP4K5 72.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 59.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 85.0 1000
MAP2K1 MEK1 97.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 83.0 1000
MAP2K4 MEK4 82.0 1000
MAP2K5 MEK5 88.0 1000
MAP2K6 MEK6 99.0 1000
MELK MELK 59.0 1000
MERTK MERTK 82.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 90.0 1000
MAP2K7 MKK7 91.0 1000
MKNK1 MKNK1 79.0 1000
MKNK2 MKNK2 86.0 1000
MYLK3 MLCK 89.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 98.0 1000
MAP3K11 MLK3 78.0 1000
CDC42BPA MRCKA 91.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 86.0 1000
MST1R MST1R 97.0 1000
STK3 MST2 78.0 1000
STK24 MST3 82.0 1000
STK26 MST4 99.0 1000
MTOR MTOR 92.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 73.0 1000
MYLK2 MYLK2 81.0 1000
MYLK4 MYLK4 93.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 90.0 1000
STK38L NDR2 100.0 1000
NEK1 NEK1 93.0 1000
NEK10 NEK10 89.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 89.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 98.0 1000
NEK5 NEK5 77.0 1000
NEK6 NEK6 98.0 1000
NEK7 NEK7 86.0 1000
NEK9 NEK9 83.0 1000
MAP3K14 NIK 67.0 1000
NIM1K NIM1 62.0 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 88.0 1000
PAK2 PAK2 91.0 1000
PAK3 PAK3 85.0 1000
PAK4 PAK4 87.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 63.0 1000
CDK16 PCTK1 92.0 1000
CDK17 PCTK2 88.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 80.0 1000
PDGFRB PDGFRB 76.0 1000
PDPK1 PDPK1 95.0 1000
CDPK1 PFCDPK1(P.falciparum) 91.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 88.0 1000
CDK14 PFTK1 95.0 1000
PHKG1 PHKG1 87.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 91.0 1000
PIK3C2G PIK3C2G 72.0 1000
PIK3CA PIK3CA(Q546K) 92.0 1000
PIK3CB PIK3CB 84.0 1000
PIK3CD PIK3CD 93.0 1000
PIK3CG PIK3CG 77.0 1000
PI4KB PIK4CB 55.0 1000
PIKFYVE PIKFYVE 95.0 1000
PIM1 PIM1 89.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 96.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 89.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 94.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 96.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 90.0 1000
PKNB PKNB(M.tuberculosis) 89.0 1000
PLK1 PLK1 73.0 1000
PLK2 PLK2 73.0 1000
PLK3 PLK3 87.0 1000
PLK4 PLK4 92.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 87.0 1000
PRKCH PRKCH 93.0 1000
PRKCI PRKCI 93.0 1000
PRKCQ PRKCQ 74.0 1000
PRKD1 PRKD1 96.0 1000
PRKD2 PRKD2 85.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 86.0 1000
EIF2AK2 PRKR 80.0 1000
PRKX PRKX 91.0 1000
PRPF4B PRP4 97.0 1000
PTK2B PYK2 79.0 1000
SIK3 QSK 87.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 93.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 73.0 1000
RIPK1 RIPK1 81.0 1000
RIPK2 RIPK2 94.0 1000
RIPK4 RIPK4 83.0 1000
DSTYK RIPK5 83.0 1000
ROCK1 ROCK1 88.0 1000
ROCK2 ROCK2 98.0 1000
ROS1 ROS1 81.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 90.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 75.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 59.0 1000
RPS6KB1 S6K1 69.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 87.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 85.0 1000
SGK3 SGK3 83.0 1000
SIK1 SIK 93.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 66.0 1000
NUAK2 SNARK 91.0 1000
SNRK SNRK 100.0 1000
SRC SRC 90.0 1000
SRMS SRMS 78.0 1000
SRPK1 SRPK1 62.0 1000
SRPK2 SRPK2 88.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 95.0 1000
STK33 STK33 100.0 1000
STK35 STK35 99.0 1000
STK36 STK36 100.0 1000
STK39 STK39 86.0 1000
SYK SYK 66.0 1000
MAP3K7 TAK1 75.0 1000
TAOK1 TAOK1 93.0 1000
TAOK2 TAOK2 76.0 1000
TAOK3 TAOK3 75.0 1000
TBK1 TBK1 68.0 1000
TEC TEC 96.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 87.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 90.0 1000
TLK1 TLK1 99.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 93.0 1000
TNK1 TNK1 74.0 1000
TNK2 TNK2 79.0 1000
TNNI3K TNNI3K 91.0 1000
NTRK1 TRKA 73.0 1000
NTRK2 TRKB 66.0 1000
NTRK3 TRKC 87.0 1000
TRPM6 TRPM6 84.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 87.0 1000
TTK TTK 91.0 1000
TXK TXK 92.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 67.0 1000
TYRO3 TYRO3 76.0 1000
ULK1 ULK1 88.0 1000
ULK2 ULK2 52.0 1000
ULK3 ULK3 74.0 1000
KDR VEGFR2 77.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 75.0 1000
WEE2 WEE2 78.0 1000
WNK1 WNK1 89.0 1000
WNK2 WNK2 0.0 1000
WNK3 WNK3 78.0 1000
WNK4 WNK4 0.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 86.0 1000
STK25 YSK1 88.0 1000
MAP3K19 YSK4 78.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 87.0 1000

BAY-207


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 88.0 1000
ABL2 ABL2 80.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 89.0 1000
ACVR2A ACVR2A 96.0 1000
ACVR2B ACVR2B 90.0 1000
ACVRL1 ACVRL1 45.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 63.0 1000
AKT1 AKT1 78.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 79.0 1000
ALK ALK(L1196M) 85.0 1000
PRKAA1 AMPK-alpha1 80.0 1000
PRKAA2 AMPK-alpha2 87.0 1000
ANKK1 ANKK1 97.0 1000
NUAK1 ARK5 95.0 1000
MAP3K5 ASK1 88.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 84.0 1000
AURKC AURKC 63.0 1000
AXL AXL 89.0 1000
BMP2K BIKE 74.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 90.0 1000
BMPR1B BMPR1B 81.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 87.0 1000
BRAF BRAF(V600E) 74.0 1000
PTK6 BRK 99.0 1000
BRSK1 BRSK1 82.0 1000
BRSK2 BRSK2 87.0 1000
BTK BTK 88.0 1000
BUB1 BUB1 95.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 97.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 97.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 93.0 1000
CAMK4 CAMK4 43.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 89.0 1000
CASK CASK 89.0 1000
CDK11B CDC2L1 83.0 1000
CDK11A CDC2L2 73.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 85.0 1000
CDK2 CDK2 82.0 1000
CDK3 CDK3 90.0 1000
CDK4 CDK4-cyclinD3 70.0 1000
CDK5 CDK5 74.0 1000
CDK7 CDK7 82.0 1000
CDK8 CDK8 91.0 1000
CDK9 CDK9 78.0 1000
CDKL1 CDKL1 99.0 1000
CDKL2 CDKL2 94.0 1000
CDKL3 CDKL3 77.0 1000
CDKL5 CDKL5 95.0 1000
CHEK1 CHEK1 80.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 78.0 1000
CLK1 CLK1 59.0 1000
CLK2 CLK2 97.0 1000
CLK3 CLK3 72.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 84.0 1000
CSNK1D CSNK1D 83.0 1000
CSNK1E CSNK1E 64.0 1000
CSNK1G1 CSNK1G1 90.0 1000
CSNK1G2 CSNK1G2 82.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 98.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 68.0 1000
DCLK2 DCAMKL2 74.0 1000
DCLK3 DCAMKL3 56.0 1000
DDR1 DDR1 83.0 1000
DDR2 DDR2 96.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 79.0 1000
CDC42BPG DMPK2 82.0 1000
STK17A DRAK1 85.0 1000
STK17B DRAK2 97.0 1000
DYRK1A DYRK1A 90.0 1000
DYRK1B DYRK1B 86.0 1000
DYRK2 DYRK2 81.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 95.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 80.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 79.0 1000
EPHA6 EPHA6 54.0 1000
EPHA7 EPHA7 82.0 1000
EPHA8 EPHA8 80.0 1000
EPHB1 EPHB1 78.0 1000
EPHB2 EPHB2 74.0 1000
EPHB3 EPHB3 62.0 1000
EPHB4 EPHB4 57.0 1000
EPHB6 EPHB6 81.0 1000
ERBB2 ERBB2 49.0 1000
ERBB3 ERBB3 84.0 1000
ERBB4 ERBB4 75.0 1000
MAPK3 ERK1 76.0 1000
MAPK1 ERK2 75.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 87.0 1000
MAPK7 ERK5 92.0 1000
MAPK15 ERK8 65.0 1000
ERN1 ERN1 61.0 1000
PTK2 FAK 87.0 1000
FER FER 83.0 1000
FES FES 64.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 54.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 70.0 1000
FLT4 FLT4 67.0 1000
FRK FRK 99.0 1000
FYN FYN 100.0 1000
GAK GAK 76.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 76.0 1000
GRK1 GRK1 72.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 90.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 96.0 1000
HCK HCK 89.0 1000
HIPK1 HIPK1 91.0 1000
HIPK2 HIPK2 88.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 58.0 1000
MAP4K1 HPK1 66.0 1000
HUNK HUNK 75.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 80.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 70.0 1000
IKBKE IKK-epsilon 70.0 1000
INSR INSR 100.0 1000
INSRR INSRR 95.0 1000
IRAK1 IRAK1 79.0 1000
IRAK3 IRAK3 75.0 1000
IRAK4 IRAK4 61.0 1000
ITK ITK 79.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 76.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 64.0 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 79.0 1000
LATS1 LATS1 69.0 1000
LATS2 LATS2 68.0 1000
LCK LCK 80.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 82.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 69.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 73.0 1000
LYN LYN 83.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 89.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 86.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 94.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 90.0 1000
MAPKAPK5 MAPKAPK5 89.0 1000
MARK1 MARK1 83.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 92.0 1000
MARK4 MARK4 82.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 88.0 1000
MAP2K2 MEK2 89.0 1000
MAP2K3 MEK3 84.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 94.0 1000
MAP2K6 MEK6 96.0 1000
MELK MELK 96.0 1000
MERTK MERTK 70.0 1000
MET MET(Y1235D) 61.0 1000
MINK1 MINK 86.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 99.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 89.0 1000
MAP3K9 MLK1 67.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 79.0 1000
CDC42BPA MRCKA 95.0 1000
CDC42BPB MRCKB 62.0 1000
STK4 MST1 73.0 1000
MST1R MST1R 99.0 1000
STK3 MST2 94.0 1000
STK24 MST3 93.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 77.0 1000
MYLK MYLK 72.0 1000
MYLK2 MYLK2 73.0 1000
MYLK4 MYLK4 94.0 1000
MYO3A MYO3A 93.0 1000
MYO3B MYO3B 29.0 1000
STK38 NDR1 81.0 1000
STK38L NDR2 81.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 89.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 86.0 1000
NEK3 NEK3 95.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 89.0 1000
NEK6 NEK6 81.0 1000
NEK7 NEK7 90.0 1000
NEK9 NEK9 94.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 86.0 1000
NLK NLK 68.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 68.0 1000
MAPK13 p38-delta 88.0 1000
MAPK12 p38-gamma 54.0 1000
PAK1 PAK1 79.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 64.0 1000
PAK4 PAK4 74.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 88.0 1000
CDK18 PCTK3 69.0 1000
PDGFRA PDGFRA 81.0 1000
PDGFRB PDGFRB 90.0 1000
PDPK1 PDPK1 85.0 1000
CDPK1 PFCDPK1(P.falciparum) 89.0 1000
PK5 PFPK5(P.falciparum) 93.0 1000
CDK15 PFTAIRE2 98.0 1000
CDK14 PFTK1 63.0 1000
PHKG1 PHKG1 89.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 84.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 99.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 75.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 94.0 1000
PIM2 PIM2 76.0 1000
PIM3 PIM3 88.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 48.0 1000
PIP4K2B PIP5K2B 62.0 1000
PIP4K2C PIP5K2C 62.0 1000
PRKACA PKAC-alpha 94.0 1000
PRKACB PKAC-beta 88.0 1000
PKMYT1 PKMYT1 70.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 83.0 1000
PKNB PKNB(M.tuberculosis) 90.0 1000
PLK1 PLK1 92.0 1000
PLK2 PLK2 84.0 1000
PLK3 PLK3 86.0 1000
PLK4 PLK4 87.0 1000
PRKCD PRKCD 89.0 1000
PRKCE PRKCE 65.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 98.0 1000
PRKCQ PRKCQ 88.0 1000
PRKD1 PRKD1 65.0 1000
PRKD2 PRKD2 87.0 1000
PRKD3 PRKD3 85.0 1000
PRKG1 PRKG1 91.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 77.0 1000
PRPF4B PRP4 68.0 1000
PTK2B PYK2 91.0 1000
SIK3 QSK 87.0 1000
RAF1 RAF1 81.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 84.0 1000
RIOK2 RIOK2 89.0 1000
RIOK3 RIOK3 73.0 1000
RIPK1 RIPK1 93.0 1000
RIPK2 RIPK2 93.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 93.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 82.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 89.0 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) 92.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 96.0 1000
RPS6KB1 S6K1 81.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 74.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 90.0 1000
SIK1 SIK 71.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 79.0 1000
NUAK2 SNARK 80.0 1000
SNRK SNRK 100.0 1000
SRC SRC 88.0 1000
SRMS SRMS 77.0 1000
SRPK1 SRPK1 71.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 80.0 1000
STK16 STK16 100.0 1000
STK33 STK33 100.0 1000
STK35 STK35 94.0 1000
STK36 STK36 99.0 1000
STK39 STK39 100.0 1000
SYK SYK 70.0 1000
MAP3K7 TAK1 98.0 1000
TAOK1 TAOK1 91.0 1000
TAOK2 TAOK2 82.0 1000
TAOK3 TAOK3 100.0 1000
TBK1 TBK1 62.0 1000
TEC TEC 81.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 82.0 1000
TGFBR2 TGFBR2 64.0 1000
TIE1 TIE1 85.0 1000
TEK TIE2 69.0 1000
TLK1 TLK1 99.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 82.0 1000
TNNI3K TNNI3K 72.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 88.0 1000
TRPM6 TRPM6 95.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 90.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 80.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 89.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 83.0 1000
KDR VEGFR2 74.0 1000
PIK3C3 VPS34 89.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 91.0 1000
WEE2 WEE2 74.0 1000
WNK1 WNK1 88.0 1000
WNK2 WNK2 88.0 1000
WNK3 WNK3 78.0 1000
WNK4 WNK4 81.0 1000
STK32A YANK1 90.0 1000
STK32B YANK2 91.0 1000
STK32C YANK3 100.0 1000
YES1 YES 90.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 70.0 1000
MAP3K20 ZAK 99.0 1000
ZAP70 ZAP70 100.0 1000

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BAY-1797

Results are significant for > 50 % inhibition.

Conclusion: Closest off-target is SLC6A3 with 60 % inhibition at 3 µM (IC50 = 2.17 µM).

Target protein HGNC name Species Cmp. conc. % inhibition IC50 [µM] Ki [µM] Reference compound name Reference compound IC50 [nM] Assay ID
Adenosine A1 ADORA1 Homo sapiens 10 µM 35.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 14.0 CGS-Z1680 130.00 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM 47.0 IB-MECA 200720
Adrenergic alpha1A ADRA1A Rattus sp. 10 µM 16.0 Prazosin 0.69 203100
Adrenergic alpha1B ADRA1B Rattus sp. 10 µM 9.0 Prazosin 0.27 203200
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM 5.0 Prazosin 0.88 203400
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM 26.0 Yohimbine 203630
Adrenergic beta1 ADRB1 Homo sapiens 10 µM 3.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM 2.0 S(-)-Propranolol 0.78 204110
Androgen (Testosterone) AR AR Rattus sp. 10 µM 17.0 Testosterone 6.50 285010
Bradykinin B1 BDKRB1 Homo sapiens 10 µM 11.0 (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 17.0 Diltiazem 0.04 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM 21.0 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 44.0 R(+)-WIN-55,Z1Z-Z 200.00 217030
Dopamine D1 DRD1 Homo sapiens 10 µM 11.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2S DRD2 Homo sapiens 10 µM 15.0 Spiperone 0.25 219700
Dopamine D3 DRD3 Homo sapiens 10 µM 28.0 Spiperone 0.36 219800
Dopamine D4.2 DRD4 Homo sapiens 10 µM 4.0 Spiperone 29.00 219900
Endothelin ETA EDNRA Homo sapiens 10 µM 3.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM -1.0 Endothelin-1 0.13 224110
Epidermal Growth Factor (EGF) EGFR Homo sapiens 10 µM 2.0 EGF (human) 1.60 225510
Estrogen ERalpha ESR1 Homo sapiens 10 µM 5.0 Diethylstilbestrol 0.77 226010
GABAA, Flunitrazepam, Central Rattus sp. 10 µM 0.0 Hydrogen diazepam chloride 16.00 226600
GABAA, Muscimol, Central Rattus sp. 10 µM 15.0 GABA 32.00 226500
GABAB1A GABBR1 Homo sapiens 10 µM 14.0 Cgp-54626 6.40 228610
Glucocorticoid NR3C1 Homo sapiens 10 µM 20.0 Dexamethasone 4.10 232020
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 3.0 L-Glutamic acid 240.00 232700
Glutamate, NMDA, Agonism Rattus sp. 10 µM 23.0 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 -1.0 Dizolcipine ((+)-MK- 801) 5.10 233000
Histamine H1 HRH1 Homo sapiens 10 µM 15.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM -15.0 Tiotidine 22.00 239710
Histamine H3 HRH3 Homo sapiens 10 µM 0.0 (R)-alpha-Methylhistamine 2.30 239820
Imidazoline I2, Central Rattus sp. 10 µM 10.0 Idazoxan 12.00 241000
Interleukin IL-1 Mus musculus 10 µM 24.0 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 13.0 Melatonin 0.21 251600
Muscarinic M1 CHRM1 Homo sapiens 10 µM -6.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 10 µM 4.0 4-DAMP 55.00 252710
Muscarinic M3 CHRM3 Homo sapiens 10 µM -12.0 4-DAMP 5.10 252810
Neuropeptide Y Y1 NPY1R Homo sapiens 10 µM 9.0 Neuropeptide Y (human, rat) 0.22 257010
Neuropeptide Y Y2 NPY2R Homo sapiens 10 µM 8.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Nicotinic Acetylcholine Homo sapiens 10 µM -11.0 Epibatidine 0.08 258590
Nicotinic Acetylcholine alpha1, Bungarotoxin CHRNA1 Homo sapiens 10 µM -4.0 alpha-Bungarotoxin 1.10 258700
Opiate delta1 (OP1, DOP) OPRD1 Homo sapiens 10 µM 4.0 Naltrindole 0.91 260130
Opiate kappa (OPZ, KOP) OPRK1 Homo sapiens 10 µM 10.0 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 -2.0 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 8.0 Astemizole 265900
Prostanoid EP4 PTGER4 Homo sapiens 10 µM 21.0 Prostaglandin E2 0.11 268420
Purinergic P2X Oryctolagus cuniculus 10 µM 5.0 alpha,beta-Methylene ATP 82.00 268700
Purinergic P2Y Rattus sp. 10 µM 14.0 ATP 18.00 268810
Rolipram Rattus sp. 10 µM 8.0 Rolipram 5.70 270000
Serotonin (5-Hydroxytryptamine) 5-HT1A HTR1A Homo sapiens 10 µM 7.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM 3.0 MDL-72222 11.00 271910
Sigma 1 SIGMAR1 Homo sapiens 10 µM 19.0 Haloperidol 21.00 278110
Sodium Channel, Site 2 Rattus sp. 10 µM 57.0 Dibucaine 61.00 279510
Tachykinin NK1 TACR1 Homo sapiens 10 µM 4.0 L-703606 3.60 255520
Thyroid Hormone Rattus sp. 10 µM 2.0 Liothyronine 0.03 285900
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 3 µM 60.0 2.17 1.73 GBR-1Z909 1.70 220320
Transporter, GABA Rattus sp. 10 µM -10.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 47.0 Desipramine 0.93 204410
Transporter, Serotonin (5-Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 4.0 Fluoxetine 8.60 274030