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Selectivity data for probe BAY-784 and control BAY-786


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BAY-784


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
M3 CHRM3 18.10
Sigma 1 SIGMAR1 17.78
DAT SLC6A3 -20.22
M2 CHRM2 8.38
SERT SLC6A4 -5.40
5-HT1A HTR1A -17.29
GABAA/BZP -9.68
D3 DRD3 9.45
D4 DRD4 1.57
D5 DRD5 19.12
GABAA -16.13
H1 HRH1 24.62
H2 HRH2 14.59
MOR OPRM1 29.14
5-HT1B HTR1B -6.19
5-HT1D HTR1D -13.28
5-HT1E HTR1E 10.40
5-HT6 HTR6 -13.80
5-HT7A HTR7 -8.16
Beta2 ADRB2 -16.76
D1 DRD1 -38.22
D2 DRD2 -35.70
DOR OPRD1 -0.34
H3 HRH3 -8.26
KOR OPRK1 14.38
M1 CHRM1 -2.96
M5 CHRM5 -6.43
Beta1 ADRB1 -0.08
Beta3 ADRB3 -2.87
H4 HRH4 -9.53
5-HT2A HTR2A -4.70
5-HT2B HTR2B -2.53
5-HT2C HTR2C 9.65
5-HT3 HTR3A 1.44
5-HT5A HTR5A -8.25
Alpha1A ADRA1A -0.32
Alpha1B ADRA1B -4.46
Alpha1D ADRA1D 4.13
Alpha2A ADRA2A -5.62
Alpha2B ADRA2B 13.46
Alpha2C ADRA2C 12.83
M4 CHRM4 -13.00
NET SLC6A2 1.03
Sigma 2 TMEM97 74.87 1107.90 5.96
GABA/PBR 7.97

BAY-786


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABA/PBR -27.95
Beta1 ADRB1 -1.82
Beta3 ADRB3 -0.77
H4 HRH4 -6.68
5-HT1B HTR1B -2.74
5-HT1D HTR1D -16.28
5-HT1E HTR1E -1.55
5-HT6 HTR6 -11.24
5-HT7A HTR7 -4.83
Beta2 ADRB2 -16.25
D1 DRD1 -42.59 > 10000.00 < 5.00
D2 DRD2 -8.40
DOR OPRD1 -2.65
H3 HRH3 6.92
M1 CHRM1 -3.70
M5 CHRM5 -1.92
5-HT1A HTR1A -13.18
GABAA/BZP -18.51
D3 DRD3 3.82
D4 DRD4 -5.22
D5 DRD5 -0.49
GABAA -10.40
H1 HRH1 8.01
H2 HRH2 16.47
KOR OPRK1 4.54
MOR OPRM1 13.14
5-HT2A HTR2A 5.01
5-HT2B HTR2B -2.32
5-HT2C HTR2C 16.89
5-HT3 HTR3A -1.68
5-HT5A HTR5A -10.80
Alpha1A ADRA1A 1.70
Alpha1B ADRA1B -8.58
Alpha1D ADRA1D -3.69
Alpha2A ADRA2A 6.57
Alpha2B ADRA2B -1.68
Alpha2C ADRA2C 15.69
M4 CHRM4 -13.38
NET SLC6A2 3.76
Sigma 2 TMEM97 52.73 2001.24 5.70
DAT SLC6A3 -4.64
M2 CHRM2 12.53
SERT SLC6A4 -4.88
Sigma 1 SIGMAR1 37.57
M3 CHRM3 14.45

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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-784


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 99.0 1000
ABL1 ABL1-phosphorylated 71.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 94.0 1000
ACVR2A ACVR2A 86.0 1000
ACVR2B ACVR2B 90.0 1000
ACVRL1 ACVRL1 98.0 1000
COQ8A ADCK3 96.0 1000
COQ8B ADCK4 83.0 1000
AKT1 AKT1 96.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 76.0 1000
PRKAA1 AMPK-alpha1 39.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 89.0 1000
NUAK1 ARK5 83.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 83.0 1000
AURKA AURKA 97.0 1000
AURKB AURKB 66.0 1000
AURKC AURKC 82.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 96.0 1000
BLK BLK 78.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 93.0 1000
BMPR2 BMPR2 80.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 84.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 64.0 1000
BUB1 BUB1 68.0 1000
CAMK1 CAMK1 84.0 1000
PNCK CAMK1B 91.0 1000
CAMK1D CAMK1D 85.0 1000
CAMK1G CAMK1G 98.0 1000
CAMK2A CAMK2A 94.0 1000
CAMK2B CAMK2B 98.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 86.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 75.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 88.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 85.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 88.0 1000
CDK5 CDK5 0.0 1000
CDK7 CDK7 64.0 1000
CDK8 CDK8 80.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 90.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 78.0 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 86.0 1000
CLK4 CLK4 0.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 97.0 1000
CSNK1A1 CSNK1A1 92.0 1000
CSNK1A1L CSNK1A1L 95.0 1000
CSNK1D CSNK1D 85.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 86.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 66.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 73.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 99.0 1000
DAPK3 DAPK3 90.0 1000
DCLK1 DCAMKL1 83.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 92.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 78.0 1000
MAP3K12 DLK 82.0 1000
DMPK DMPK 93.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 85.0 1000
DYRK1A DYRK1A 88.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 95.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 86.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 97.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 80.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 70.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 81.0 1000
MAPK6 ERK3 87.0 1000
MAPK4 ERK4 91.0 1000
MAPK7 ERK5 99.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 78.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 49.0 1000
FGFR2 FGFR2 86.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 98.0 1000
FLT3 FLT3-autoinhibited 95.0 1000
FLT4 FLT4 92.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 97.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 88.0 1000
GRK1 GRK1 80.0 1000
GRK2 GRK2 56.0 1000
GRK3 GRK3 99.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 80.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 87.0 1000
HASPIN HASPIN 87.0 1000
HCK HCK 69.0 1000
HIPK1 HIPK1 83.0 1000
HIPK2 HIPK2 81.0 1000
HIPK3 HIPK3 82.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 84.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 77.0 1000
IKBKB IKK-beta 92.0 1000
IKBKE IKK-epsilon 77.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 82.0 1000
IRAK3 IRAK3 99.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 87.0 1000
JAK2 JAK2(JH1domain-catalytic) 80.0 1000
JAK3 JAK3(JH1domain-catalytic) 79.0 1000
MAPK8 JNK1 87.0 1000
MAPK9 JNK2 76.0 1000
MAPK10 JNK3 88.0 1000
KIT KIT-autoinhibited 76.0 1000
LATS1 LATS1 91.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 100.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 54.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 87.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 0.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 63.0 1000
MAP3K15 MAP3K15 96.0 1000
MAP3K2 MAP3K2 66.0 1000
MAP3K3 MAP3K3 74.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 91.0 1000
MAP4K5 MAP4K5 82.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 89.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 54.0 1000
MAP2K1 MEK1 98.0 1000
MAP2K2 MEK2 88.0 1000
MAP2K3 MEK3 71.0 1000
MAP2K4 MEK4 75.0 1000
MAP2K5 MEK5 69.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 54.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 90.0 1000
MAP2K7 MKK7 72.0 1000
MKNK1 MKNK1 74.0 1000
MKNK2 MKNK2 83.0 1000
MYLK3 MLCK 79.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 87.0 1000
MST1R MST1R 99.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 77.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 74.0 1000
STK38 NDR1 92.0 1000
STK38L NDR2 91.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 94.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 89.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 99.0 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 83.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 87.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 99.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 91.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 90.0 1000
PDGFRB PDGFRB 92.0 1000
PDPK1 PDPK1 91.0 1000
CDPK1 PFCDPK1(P.falciparum) 85.0 1000
PK5 PFPK5(P.falciparum) 94.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 96.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 75.0 1000
PIK3CA PIK3CA(Q546K) 76.0 1000
PIK3CB PIK3CB 68.0 1000
PIK3CD PIK3CD 67.0 1000
PIK3CG PIK3CG 82.0 1000
PI4KB PIK4CB 78.0 1000
PIKFYVE PIKFYVE 84.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 94.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 89.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 86.0 1000
PRKACB PKAC-beta 96.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 70.0 1000
PKNB PKNB(M.tuberculosis) 96.0 1000
PLK1 PLK1 86.0 1000
PLK2 PLK2 76.0 1000
PLK3 PLK3 92.0 1000
PLK4 PLK4 92.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 69.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 81.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 93.0 1000
PRKD2 PRKD2 98.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 77.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 88.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 77.0 1000
RIOK3 RIOK3 69.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 93.0 1000
DSTYK RIPK5 76.0 1000
ROCK1 ROCK1 94.0 1000
ROCK2 ROCK2 95.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 99.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 99.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 87.0 1000
RPS6KB1 S6K1 64.0 1000
SBK1 SBK1 97.0 1000
SGK1 SGK 79.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 83.0 1000
SGK3 SGK3 99.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 96.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 81.0 1000
SNRK SNRK 77.0 1000
SRC SRC 98.0 1000
SRMS SRMS 71.0 1000
SRPK1 SRPK1 72.0 1000
SRPK2 SRPK2 91.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 88.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 84.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 80.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 81.0 1000
TAOK3 TAOK3 99.0 1000
TBK1 TBK1 80.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 91.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 96.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 88.0 1000
TNK2 TNK2 85.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 80.0 1000
NTRK2 TRKB 60.0 1000
NTRK3 TRKC 84.0 1000
TRPM6 TRPM6 81.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 87.0 1000
TTK TTK 78.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 79.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 90.0 1000
ULK2 ULK2 58.0 1000
ULK3 ULK3 85.0 1000
KDR VEGFR2 83.0 1000
PIK3C3 VPS34 86.0 1000
VRK2 VRK2 95.0 1000
WEE1 WEE1 82.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 90.0 1000
WNK2 WNK2 97.0 1000
WNK3 WNK3 86.0 1000
WNK4 WNK4 91.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 90.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 73.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 84.0 1000

BAY-786


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 86.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 97.0 1000
ACVR1B ACVR1B 87.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 72.0 1000
COQ8A ADCK3 90.0 1000
COQ8B ADCK4 85.0 1000
AKT1 AKT1 94.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 86.0 1000
ALK ALK(L1196M) 87.0 1000
PRKAA1 AMPK-alpha1 97.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 76.0 1000
NUAK1 ARK5 88.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 68.0 1000
AURKA AURKA 81.0 1000
AURKB AURKB 66.0 1000
AURKC AURKC 80.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 76.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 85.0 1000
BMPR2 BMPR2 73.0 1000
BMX BMX 92.0 1000
BRAF BRAF(V600E) 90.0 1000
PTK6 BRK 94.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 73.0 1000
BUB1 BUB1 1.9 1000
CAMK1 CAMK1 97.0 1000
PNCK CAMK1B 96.0 1000
CAMK1D CAMK1D 99.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 90.0 1000
CAMK2B CAMK2B 92.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 84.0 1000
CAMK4 CAMK4 71.0 1000
CAMKK1 CAMKK1 72.0 1000
CAMKK2 CAMKK2 83.0 1000
CASK CASK 64.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 89.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 41.0 1000
CDK4 CDK4-cyclinD3 88.0 1000
CDK5 CDK5 89.0 1000
CDK7 CDK7 56.0 1000
CDK8 CDK8 63.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 67.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 97.0 1000
CIT CIT 84.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 82.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 74.0 1000
CSK CSK 96.0 1000
CSNK1A1 CSNK1A1 81.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 93.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 90.0 1000
CSNK1G2 CSNK1G2 85.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 67.0 1000
CSNK2A2 CSNK2A2 72.0 1000
MATK CTK 74.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 90.0 1000
DAPK3 DAPK3 89.0 1000
DCLK1 DCAMKL1 74.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 69.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 67.0 1000
MAP3K12 DLK 87.0 1000
DMPK DMPK 86.0 1000
CDC42BPG DMPK2 93.0 1000
STK17A DRAK1 73.0 1000
STK17B DRAK2 87.0 1000
DYRK1A DYRK1A 85.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 90.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 94.0 1000
EPHA1 EPHA1 86.0 1000
EPHA2 EPHA2 84.0 1000
EPHA3 EPHA3 67.0 1000
EPHA4 EPHA4 97.0 1000
EPHA5 EPHA5 77.0 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 94.0 1000
EPHB6 EPHB6 94.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 72.0 1000
MAPK3 ERK1 83.0 1000
MAPK1 ERK2 83.0 1000
MAPK6 ERK3 86.0 1000
MAPK4 ERK4 89.0 1000
MAPK7 ERK5 97.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 65.0 1000
PTK2 FAK 95.0 1000
FER FER 100.0 1000
FES FES 93.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 98.0 1000
FGFR3 FGFR3(G697C) 80.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 93.0 1000
FLT1 FLT1 82.0 1000
FLT3 FLT3-autoinhibited 94.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 99.0 1000
FYN FYN 70.0 1000
GAK GAK 96.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 79.0 1000
GRK2 GRK2 80.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 65.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 90.0 1000
HASPIN HASPIN 77.0 1000
HCK HCK 86.0 1000
HIPK1 HIPK1 70.0 1000
HIPK2 HIPK2 72.0 1000
HIPK3 HIPK3 81.0 1000
HIPK4 HIPK4 97.0 1000
MAP4K1 HPK1 89.0 1000
HUNK HUNK 85.0 1000
CILK1 ICK 97.0 1000
IGF1R IGF1R 88.0 1000
CHUK IKK-alpha 84.0 1000
IKBKB IKK-beta 86.0 1000
IKBKE IKK-epsilon 82.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 77.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 90.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 85.0 1000
JAK2 JAK2(JH1domain-catalytic) 70.0 1000
JAK3 JAK3(JH1domain-catalytic) 93.0 1000
MAPK8 JNK1 55.0 1000
MAPK9 JNK2 82.0 1000
MAPK10 JNK3 73.0 1000
KIT KIT-autoinhibited 82.0 1000
LATS1 LATS1 97.0 1000
LATS2 LATS2 99.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 91.0 1000
LIMK2 LIMK2 94.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 94.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 81.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 0.0 1000
MAK MAK 89.0 1000
MAP3K1 MAP3K1 68.0 1000
MAP3K15 MAP3K15 78.0 1000
MAP3K2 MAP3K2 88.0 1000
MAP3K3 MAP3K3 60.0 1000
MAP3K4 MAP3K4 84.0 1000
MAP4K2 MAP4K2 91.0 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 100.0 1000
MARK2 MARK2 63.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 61.0 1000
MAP2K1 MEK1 91.0 1000
MAP2K2 MEK2 78.0 1000
MAP2K3 MEK3 73.0 1000
MAP2K4 MEK4 76.0 1000
MAP2K5 MEK5 90.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 85.0 1000
MAP2K7 MKK7 79.0 1000
MKNK1 MKNK1 78.0 1000
MKNK2 MKNK2 76.0 1000
MYLK3 MLCK 76.0 1000
MAP3K9 MLK1 77.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 86.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 87.0 1000
STK24 MST3 100.0 1000
STK26 MST4 82.0 1000
MTOR MTOR 92.0 1000
MUSK MUSK 79.0 1000
MYLK MYLK 74.0 1000
MYLK2 MYLK2 83.0 1000
MYLK4 MYLK4 95.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 84.0 1000
STK38L NDR2 94.0 1000
NEK1 NEK1 96.0 1000
NEK10 NEK10 83.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 88.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 99.0 1000
NEK5 NEK5 86.0 1000
NEK6 NEK6 95.0 1000
NEK7 NEK7 65.0 1000
NEK9 NEK9 72.0 1000
MAP3K14 NIK 71.0 1000
NIM1K NIM1 78.0 1000
NLK NLK 89.0 1000
OXSR1 OSR1 71.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 86.0 1000
MAPK12 p38-gamma 94.0 1000
PAK1 PAK1 80.0 1000
PAK2 PAK2 84.0 1000
PAK3 PAK3 89.0 1000
PAK4 PAK4 89.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 74.0 1000
CDK16 PCTK1 80.0 1000
CDK17 PCTK2 99.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 87.0 1000
PDGFRB PDGFRB 77.0 1000
PDPK1 PDPK1 92.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 97.0 1000
CDK15 PFTAIRE2 69.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 84.0 1000
PIK3C2B PIK3C2B 90.0 1000
PIK3C2G PIK3C2G 75.0 1000
PIK3CA PIK3CA(Q546K) 72.0 1000
PIK3CB PIK3CB 75.0 1000
PIK3CD PIK3CD 67.0 1000
PIK3CG PIK3CG 95.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 73.0 1000
PIM1 PIM1 74.0 1000
PIM2 PIM2 92.0 1000
PIM3 PIM3 85.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 94.0 1000
PIP4K2B PIP5K2B 89.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 98.0 1000
PRKACB PKAC-beta 85.0 1000
PKMYT1 PKMYT1 92.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 68.0 1000
PKNB PKNB(M.tuberculosis) 84.0 1000
PLK1 PLK1 82.0 1000
PLK2 PLK2 74.0 1000
PLK3 PLK3 82.0 1000
PLK4 PLK4 92.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 76.0 1000
PRKCH PRKCH 96.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 95.0 1000
PRKD1 PRKD1 76.0 1000
PRKD2 PRKD2 90.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 89.0 1000
EIF2AK2 PRKR 97.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 84.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 72.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 78.0 1000
RIOK2 RIOK2 77.0 1000
RIOK3 RIOK3 72.0 1000
RIPK1 RIPK1 30.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 72.0 1000
DSTYK RIPK5 78.0 1000
ROCK1 ROCK1 82.0 1000
ROCK2 ROCK2 93.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 84.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 97.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 82.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 72.0 1000
SBK1 SBK1 92.0 1000
SGK1 SGK 77.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 77.0 1000
SGK3 SGK3 83.0 1000
SIK1 SIK 89.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 75.0 1000
SNRK SNRK 96.0 1000
SRC SRC 98.0 1000
SRMS SRMS 60.0 1000
SRPK1 SRPK1 96.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 99.0 1000
STK33 STK33 86.0 1000
STK35 STK35 93.0 1000
STK36 STK36 100.0 1000
STK39 STK39 77.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 63.0 1000
TAOK1 TAOK1 91.0 1000
TAOK2 TAOK2 64.0 1000
TAOK3 TAOK3 80.0 1000
TBK1 TBK1 84.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 85.0 1000
TGFBR1 TGFBR1 84.0 1000
TGFBR2 TGFBR2 71.0 1000
TIE1 TIE1 95.0 1000
TEK TIE2 96.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 71.0 1000
TNK1 TNK1 88.0 1000
TNK2 TNK2 84.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 75.0 1000
NTRK2 TRKB 71.0 1000
NTRK3 TRKC 71.0 1000
TRPM6 TRPM6 92.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 97.0 1000
TTK TTK 100.0 1000
TXK TXK 83.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 73.0 1000
TYRO3 TYRO3 84.0 1000
ULK1 ULK1 80.0 1000
ULK2 ULK2 54.0 1000
ULK3 ULK3 69.0 1000
KDR VEGFR2 80.0 1000
PIK3C3 VPS34 89.0 1000
VRK2 VRK2 98.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 79.0 1000
WNK2 WNK2 0.0 1000
WNK3 WNK3 70.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 99.0 1000
STK32B YANK2 96.0 1000
STK32C YANK3 100.0 1000
YES1 YES 93.0 1000
STK25 YSK1 99.0 1000
MAP3K19 YSK4 69.0 1000
MAP3K20 ZAK 92.0 1000
ZAP70 ZAP70 72.0 1000

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BAY-784

Results are significant for > 50 % inhibition. Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (ID Business Solutions Ltd., UK). The inhibition constants (Ki) were calculated with the equation of Cheng and Prusoff (Cheng, Y., Prusoff, W.H., Biochem. Pharmacol. 22:3099-3108, 1973) using the observed IC50 value of the tested compound, the concentration of radioligand employed in the assay, and the historical values for the Ki of the ligand (obtained experimentally at MDS Pharma Services).

Conclusion: The closest off-target is the Cannabinoid receptor 1 (CNR1) with IC50 = 3.44. µM at 3 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 15.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 0.0 CGS-Z1680 130.00 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM 9.0 IB-MECA 0.78 200720
Adrenergic alpha1A ADRA1A Rattus sp. 10 µM 7.0 Prazosin 0.69 203100
Adrenergic alpha1B ADRA1B Rattus sp. 10 µM 2.0 Prazosin 0.27 203200
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM 18.0 Prazosin 0.88 203400
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM -1.0 Yohimbine 8.40 203620
Adrenergic alpha2B ADRA2B Homo sapiens 10 µM 4.0 Yohimbine 14.00 203710
Adrenergic alpha2C ADRA2C Homo sapiens 10 µM 3.0 Yohimbine 75.00 203800
Adrenergic beta1 ADRB1 Homo sapiens 10 µM 7.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM -4.0 S(-)-Propranolol 0.78 204110
Adrenergic beta3 ADRB3 Homo sapiens 10 µM 0.0 Alprenolol 180.00 204200
Androgen (Testosterone) AR AR Rattus sp. 10 µM 16.0 Testosterone 6.50 285010
Angiotensin AT2 AGTR2 Homo sapiens 10 µM -5.0 Saralasin 0.35 210120
Atrial Natriuretic Factor (ANF) Cavia porcellus 10 µM 2.0 ANF (rat) 0.40 211000
Bradykinin B2 BDKRB2 Homo sapiens 10 µM 9.0 Bradykinin 1.80 212620
Calcitonin CALCR Homo sapiens 10 µM -22.0 Calcitonin (salmon) 0.39 213610
Calcium Channel L-Type, Benzothiazepine CACNA1C Rattus sp. 10 µM 29.0 Diltiazem 0.04 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM 26.0 Nitrendipine 0.72 214600
Calcium Channel L-Type, Phenylalkylamine CACNA1C Rattus sp. 10 µM 47.0 Methoxyverapamil (D-600) 22.00 215000
Cannabinoid CB1 CNR1 Homo sapiens 3 µM 52.0 3.44 2.57 R(+)-WIN-55,Z1Z-Z 200.00 217030
Chemokine CCR2B CCR2 Homo sapiens 10 µM -1.0 MCP-1 0.07 217550
Chemokine CCR4 CCR4 Homo sapiens 10 µM -20.0 217660
Chemokine CCR5 CCR5 Homo sapiens 10 µM -1.0 217720
Chemokine CXCR2 (IL-8RB) CXCR2 Homo sapiens 10 µM 14.0 IL-8 0.18 244500
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM -3.0 Devazepide (L-364,718) 0.18 218020
Dopamine D1 DRD1 Homo sapiens 10 µM 6.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2L DRD2 Homo sapiens 10 µM 4.0 Spiperone 219600
Dopamine D3 DRD3 Homo sapiens 10 µM 17.0 Spiperone 0.36 219800
Dopamine D4.2 DRD4 Homo sapiens 10 µM 11.0 Spiperone 29.00 219900
Endothelin ETA EDNRA Homo sapiens 10 µM 16.0 Endothelin-1 0.23 224010
Estrogen ERalpha ESR1 Homo sapiens 10 µM 21.0 Diethylstilbestrol 0.77 226010
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 34.0 Picrotoxin 270.00 226810
GABAA, Flunitrazepam, Central Rattus sp. 10 µM -1.0 Hydrogen diazepam chloride 16.00 226600
GABAA, Muscimol, Central Rattus sp. 10 µM 7.0 GABA 32.00 226500
Glucocorticoid NR3C1 Homo sapiens 10 µM 13.0 Dexamethasone 3.80 232030
Glutamate, AMPA Rattus sp. 10 µM 2.0 L-Glutamic acid 320.00 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 1.0 L-Glutamic acid 240.00 232700
Glutamate, NMDA, Agonism Rattus sp. 10 µM -13.0 L-Glutamic acid 410.00 232810
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM -4.0 Dizolcipine ((+)-MK-801) 5.10 233000
Glycine, Strychnine-Sensitive Rattus sp. 10 µM 4.0 (-)-Strychnine 8.90 239000
Histamine H1 HRH1 Homo sapiens 10 µM 9.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM 1.0 Tiotidine 22.00 239710
Imidazoline I2, Central Rattus sp. 10 µM 10.0 Idazoxan 12.00 241000
Insulin INSR Rattus sp. 10 µM -1.0 Insulin 6.10 243000
Leukotriene, Cysteinyl CysLT1 CYSLTR1 Homo sapiens 10 µM 4.0 Leukotriene D4 0.70 250460
Melanocortin MC3 MC3R Homo sapiens 10 µM -7.0 NDP-alpha-MSH 0.15 251300
Melanocortin MC4 MC4R Homo sapiens 10 µM 12.0 NDP-alpha-MSH 0.22 251350
Melanocortin MC5 MC5R Homo sapiens 10 µM 27.0 NDP-alpha-MSH 0.48 251400
Muscarinic M1 CHRM1 Homo sapiens 10 µM 5.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 10 µM -3.0 4-DAMP 55.00 252710
Muscarinic M3 CHRM3 Homo sapiens 10 µM 1.0 4-DAMP 5.10 252810
Muscarinic M4 CHRM4 Homo sapiens 10 µM 2.0 4-DAMP 15.00 252910
Muscarinic M5 CHRM5 Homo sapiens 10 µM 0.0 4-DAMP 3.20 253010
Neuropeptide Y Y1 NPY1R Homo sapiens 10 µM 17.0 Neuropeptide Y (human, rat) 0.22 257010
Neuropeptide Y Y2 NPY2R Homo sapiens 10 µM 2.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Nicotinic Acetylcholine Homo sapiens 10 µM -15.0 Epibatidine 0.08 258590
Opiate delta (OP1, DOP) OPRD1 Homo sapiens 10 µM 5.0 Naltrindole 0.91 260130
Opiate kappa (OP2, KOP) OPRK1 Homo sapiens 10 µM 7.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 16.0 DAMGO 20.00 260410
Phorbol Ester Mus musculus 10 µM 1.0 Phorbol myristate acetate 0.79 264500
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM 6.0 PAF 0.28 265010
Platelet-Derived Growth Factor (PDGF) Mus musculus 10 µM -4.0 265200
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM 0.0 Glyburide 5.70 265600
Progesterone PGR Bos taurus 10 µM 0.0 268000
Purinergic P2X Oryctolagus cuniculus 10 µM -17.0 alpha,beta-Methylene ATP 82.00 268700
Serotonin (5-Hydroxytryptamine) 5-HT1A HTR1A Homo sapiens 10 µM 0.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT1B HTR1B Rattus sp. 10 µM -24.0 Serotonin (5-HT) 5.70 271200
Serotonin (5-Hydroxytryptamine) 5-HT2B HTR2B Homo sapiens 10 µM 4.0 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT2C HTR2C Homo sapiens 10 µM 9.0 SBZ4Z084 1.00 271800
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM 19.0 MDL-72222 11.00 271910
Serotonin (5-Hydroxytryptamine) 5-HT4 HTR4 Cavia porcellus 10 µM 22.0 RS-23597-190 90.00 272000
Serotonin (5-Hydroxytryptamine) 5-HT6 HTR6 Homo sapiens 10 µM 14.0 Methiothepin 2.80 272200
Sigma 1 SIGMAR1 Homo sapiens 10 µM 15.0 Haloperidol 21.00 278110
Sigma 2 TMEM97 Rattus sp. 10 µM 20.0 Ifenprodil 8.00 278200
Tachykinin NK1 TACR1 Homo sapiens 10 µM 26.0 L-703606 3.60 255520
Tachykinin NK2 TACR2 Homo sapiens 10 µM 7.0 MEN-10,376 110.00 255600
Transporter, Adenosine Cavia porcellus 10 µM 25.0 Nitrobenzylthioinosine 0.85 202000
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 25.0 GBR-12909 1.70 220320
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 14.0 Desipramine 0.93 204410
Transporter, Serotonin (5- Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 10.0 Fluoxetine 8.60 274030
Tumor Necrosis Factor (TNF), Non-Selective Homo sapiens 10 µM 22.0 286510
Vasoactive Intestinal Peptide VIP1 VIPR1 Homo sapiens 10 µM 2.0 VIP 0.13 287010
Vasopressin V1A AVPR1A Homo sapiens 10 µM -11.0 (Arg8)-Vasopressin 0.33 287530
 

BAY-784

Results are significant for > 50 % inhibition. Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (ID Business Solutions Ltd., UK).

Conclusion: The closest off-targets found at 10 µM are MAPK3 with IC50 = 4.87 µM and MAPK14 with IC50 = 10.7 µM.

Target protein HGNC name Species Cmp. conc. % inhibition IC50 [µM] Reference compound name Reference compound IC50 [µM] Assay ID
Aldose Reductase AKR1B1 Rattus sp. 10 µM 0.0 Quercitrin 0.56 107000
ATPase, Na+/K+, Heart Sus scrofa 10 µM 4.0 Ouabain 2.00 107710
Beta-Lactamase Bacteria 10 µM -2.0 CLAVULANIC ACID 11.00 126000
Carbonic Anhydrase II CA2 Homo sapiens 10 µM -5.0 Acetazolamide 0.03 112020
Cholinesterase, Acetyl, ACES ACHE Homo sapiens 10 µM 56.0 Physostigmine 0.12 104010
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM -12.0 Indomethacin 0.04 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM 4.0 Rofecoxib 0.17 118010
CYP450, 1A2 CYP1A2 Homo sapiens 10 µM -2.0 118050
CYP450, 2C19 CYP2C19 Homo sapiens 10 µM 36.0 118070
CYP450, 2C9 CYP2C9 Homo sapiens 10 µM 32.0 118060
CYP450, 2D6 CYP2D6 Homo sapiens 10 µM 4.0 118080
CYP450, 3A4 CYP3A4 Homo sapiens 10 µM 38.0 118090
HMG-CoA Reductase HMGCR Homo sapiens 10 µM 12.0 Lovastatin 0.07 124010
Leukotriene LTC4 Synthase LTC4S Cavia porcellus 10 µM -9.0 Sulfasalazine 87.00 132000
Lipoxygenase 15-LO ALOX15 Oryctolagus cuniculus 10 µM 11.0 138000
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 3.0 Clorgyline 0.00 140010
Nitric Oxide Synthase, Inducible (iNOS) NOS2 Mus musculus 10 µM 6.0 S-Methylisothiourea 2.30 144000
Nitric Oxide Synthase, Neuronal (nNOS) NOS1 Rattus sp. 10 µM 2.0 S-methylisothiourea 142000
Peptidase, Angiotensin Converting Enzyme ACE Oryctolagus cuniculus 10 µM 0.0 Captopril 0.01 107300
Peptidase, CASP1 (Caspase 1) CASP1 Homo sapiens 10 µM 8.0 Ac-YVAD-CHO 0.03 163000
Peptidase, CTSG (Cathepsin G) CTSG Homo sapiens 10 µM 0.0 Chymostatin 2.10 112510
Peptidase, ELA2 (Neutrophil Elastase 2) ELANE Homo sapiens 30 µM 4.0 N-MeOSuc-Ala-Ala-Pro- Val-Chloromethylketone 0.07 166010
Peptidase, Matrix Metalloproteinase-1 (MMP-1) MMP1 Homo sapiens 10 µM -4.0 GM-6001 114110
Peptidase, Matrix Metalloproteinase-9 (MMP-9) MMP9 Homo sapiens 10 µM 3.0 GM-6001 0.00 114910
Phosphodiesterase PDE3 Homo sapiens 10 µM 9.0 Cilostamide 0.05 152000
Phosphodiesterase PDE4 Homo sapiens 10 µM 2.0 Ro 20-1724 1.10 154000
Phosphodiesterase PDE5 PDE5A Homo sapiens 10 µM -5.0 Zaprinast 156000
Protein Serine/Threonine Kinase, MAPK1 (ERK2) MAPK1 Homo sapiens 10 µM 53.0 Staurosporine 0.47 171120
Protein Serine/Threonine Kinase, MAPK14 (p38α) MAPK14 Homo sapiens 10 µM 50.0 10.70 SB-Z0Z190 0.02 176610
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 10 µM 87.0 4.87 Staurosporine 1.60 171000
Protein Serine/Threonine Kinase, PRKCA (PKCα) PRKCA Homo sapiens 10 µM 16.0 Staurosporine 0.00 180010
Protein Serine/threonine Phosphatase, PPP3CA (Calcineurin, PP2B) PPP3CA Homo sapiens 11 µM -8.0 (NH4)6Mo7O24 25.00 188020
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM -3.0 170020
Protein Tyrosine Kinase, ERBB2 (HER2) ERBB2 Homo sapiens 10 µM 6.0 Staurosporine 1.30 174020
Protein Tyrosine Kinase, Fyn FYN Homo sapiens 10 µM 5.0 Staurosporine 0.20 172020
Protein Tyrosine Kinase, LCK LCK Homo sapiens 10 µM 0.0 TC-S 7003 0.06 176020
Protein Tyrosine Phosphatase, PTPRC (CD45) PTPRC Homo sapiens 10 µM -5.0 (NH4)6Mo7O24 190010
Thromboxane Synthase TBXAS1 Homo sapiens 10 µM 22.0 1-(7-Carboxyheptyl)-Imidazole 0.01 194020