Selectivity data for probe BAY-678 and control BAY-677


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BAY-678


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 50.00 4976.50 average (n=2) 5.31
5-HT1B HTR1B 6.69
5-HT1D HTR1D 10.86
5-HT1E HTR1E 7.74
5-HT2A HTR2A -0.43
5-HT2B HTR2B 6.06
5-HT2C HTR2C -2.88
5-HT3 HTR3A -7.63
5-HT5A HTR5A 4.22
5-HT6 HTR6 -6.02
5-HT7A HTR7 3.93
D1 DRD1 -8.40
D2 DRD2 0.57
D3 DRD3 -17.68
D4 DRD4 15.94
D5 DRD5 0.74
SERT SLC6A4 -2.61
NET SLC6A2 -17.51
DAT SLC6A3 -0.34
MOR OPRM1 -5.41
DOR OPRD1 -6.02
KOR OPRK1 -13.57
GABAA 11.88
H1 HRH1 34.10
H2 HRH2 14.54
H3 HRH3 50.00 3068.50 average (n=2) 5.55
H4 HRH4 25.92
Alpha1A ADRA1A -14.21
Alpha1B ADRA1B -1.17
Alpha2A ADRA2A 10.49
Alpha2B ADRA2B -1.73
Alpha2C ADRA2C 20.20
Beta1 ADRB1 60.03 5454.00 5.30
Beta2 ADRB2 24.33
M1 CHRM1 -4.65
M2 CHRM2 -12.45
M3 CHRM3 10.38
M4 CHRM4 -6.72
M5 CHRM5 -6.78
Beta3 ADRB3 -0.55
GABAA/BZP 9.75
GABA/PBR 19.99
Alpha1D ADRA1D 3.11
Sigma 2 TMEM97 35.90
Sigma 1 SIGMAR1 -18.64

BAY-677


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT2C HTR2C 28.97
5-HT3 HTR3A 23.69
5-HT5A HTR5A 8.86
Beta2 ADRB2 21.57
DOR OPRD1 4.95
H1 HRH1 5.28
H2 HRH2 3.40
H3 HRH3 -11.23
M4 CHRM4 2.88
M5 CHRM5 2.19
SERT SLC6A4 2.85
Sigma 1 SIGMAR1 -15.49
5-HT1A HTR1A 3.63
5-HT1B HTR1B 6.75
5-HT1D HTR1D -16.45
5-HT1E HTR1E -20.95
5-HT2A HTR2A -6.25
5-HT2B HTR2B 15.84
5-HT6 HTR6 14.92
5-HT7A HTR7 13.87
D1 DRD1 -12.62
D2 DRD2 -1.53
D3 DRD3 -6.43
Alpha1A ADRA1A -5.26
Alpha1B ADRA1B -8.10
Alpha1D ADRA1D 7.70
Alpha2A ADRA2A -8.89
Alpha2B ADRA2B 11.77
Alpha2C ADRA2C 10.96
M1 CHRM1 -19.40
M2 CHRM2 -9.21
M3 CHRM3 27.28
Sigma 2 TMEM97 20.94
D4 DRD4 5.84
D5 DRD5 5.12
DAT SLC6A3 1.88
H4 HRH4 -0.78
KOR OPRK1 -8.67
MOR OPRM1 2.02
NET SLC6A2 -8.06
GABAA/BZP 14.73
GABAA -5.84
GABA/PBR -17.79
Beta1 ADRB1 8.09
Beta3 ADRB3 17.24

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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-678


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 83.3 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 74.5 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 85.7 1000
ACVR2B ACVR2B 87.5 1000
ACVRL1 ACVRL1 71.7 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 90.4 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 90.6 1000
ALK ALK(L1196M) 94.1 1000
PRKAA1 AMPK-alpha1 85.4 1000
PRKAA2 AMPK-alpha2 80.4 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 93.2 1000
MAP3K5 ASK1 94.8 1000
MAP3K6 ASK2 91.2 1000
AURKA AURKA 83.9 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 95.8 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 74.2 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 97.4 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 86.7 1000
PNCK CAMK1B 92.4 1000
CAMK1D CAMK1D 79.4 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 92.5 1000
CAMK2B CAMK2B 95.7 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 54.3 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 95.7 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 96.9 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 79.4 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 90.6 1000
CDK8 CDK8 65.3 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 80.9 1000
CDKL2 CDKL2 75.4 1000
CDKL3 CDKL3 98.5 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 73.2 1000
CHEK2 CHEK2 85.6 1000
CIT CIT 77.6 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 88.3 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 90.0 1000
CSNK1A1 CSNK1A1 91.5 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 94.6 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 94.8 1000
CSNK2A2 CSNK2A2 75.7 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 93.8 1000
DAPK2 DAPK2 79.2 1000
DAPK3 DAPK3 83.8 1000
DCLK1 DCAMKL1 85.1 1000
DCLK2 DCAMKL2 88.0 1000
DCLK3 DCAMKL3 53.9 1000
DDR1 DDR1 71.5 1000
DDR2 DDR2 87.6 1000
MAP3K12 DLK 86.8 1000
DMPK DMPK 86.5 1000
CDC42BPG DMPK2 79.3 1000
STK17A DRAK1 93.7 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 67.2 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 98.2 1000
EPHA6 EPHA6 94.5 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 85.0 1000
ERBB2 ERBB2 95.6 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 90.8 1000
MAPK3 ERK1 97.1 1000
MAPK1 ERK2 98.9 1000
MAPK6 ERK3 75.8 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 100.0 1000
FER FER 96.9 1000
FES FES 84.1 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 86.7 1000
FLT1 FLT1 62.4 1000
FLT3 FLT3-autoinhibited 82.9 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 97.2 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 56.9 1000
GRK1 GRK1 99.2 1000
GRK2 GRK2 89.0 1000
GRK3 GRK3 92.6 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 95.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 87.7 1000
HIPK1 HIPK1 72.6 1000
HIPK2 HIPK2 94.3 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 80.1 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 98.2 1000
INSR INSR 89.3 1000
INSRR INSRR 99.6 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 90.4 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 87.1 1000
JAK3 JAK3(JH1domain-catalytic) 70.5 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 83.8 1000
LATS1 LATS1 67.1 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 70.2 1000
LIMK2 LIMK2 91.7 1000
STK11 LKB1 72.8 1000
STK10 LOK 84.5 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 92.6 1000
LYN LYN 100.0 1000
MAP3K13 LZK 92.4 1000
MAK MAK 82.5 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 83.5 1000
MAP4K4 MAP4K4 99.3 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 82.6 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 96.9 1000
MAP2K1 MEK1 93.3 1000
MAP2K2 MEK2 84.2 1000
MAP2K3 MEK3 95.2 1000
MAP2K4 MEK4 98.1 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 94.6 1000
MELK MELK 88.2 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 84.8 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 94.0 1000
MAP3K10 MLK2 92.1 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 97.5 1000
MST1R MST1R 81.1 1000
STK3 MST2 93.1 1000
STK24 MST3 95.4 1000
STK26 MST4 100.0 1000
MTOR MTOR 92.5 1000
MUSK MUSK 100.0 1000
MYLK MYLK 83.8 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 85.1 1000
MYO3B MYO3B 78.3 1000
STK38 NDR1 94.1 1000
STK38L NDR2 93.6 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 96.4 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 72.0 1000
NEK4 NEK4 93.9 1000
NEK5 NEK5 80.6 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 83.5 1000
NLK NLK 93.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 74.6 1000
MAPK12 p38-gamma 77.4 1000
PAK1 PAK1 91.2 1000
PAK2 PAK2 98.2 1000
PAK3 PAK3 86.3 1000
PAK4 PAK4 97.9 1000
PAK6 PAK6 92.7 1000
PAK5 PAK7 96.2 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 85.1 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 94.0 1000
PDPK1 PDPK1 93.4 1000
CDPK1 PFCDPK1(P.falciparum) 94.8 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 91.7 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 80.8 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 78.2 1000
PIK3CA PIK3CA(Q546K) 100.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 89.8 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 90.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 98.2 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 52.8 1000
PIP4K2C PIP5K2C 80.7 1000
PRKACA PKAC-alpha 92.3 1000
PRKACB PKAC-beta 48.7 1000
PKMYT1 PKMYT1 90.6 1000
PKN1 PKN1 71.1 1000
PKN2 PKN2 96.3 1000
PKNB PKNB(M.tuberculosis) 82.7 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 97.8 1000
PLK3 PLK3 84.2 1000
PLK4 PLK4 82.7 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 73.9 1000
PRKCH PRKCH 91.3 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 83.3 1000
PRKD1 PRKD1 95.7 1000
PRKD2 PRKD2 98.8 1000
PRKD3 PRKD3 78.0 1000
PRKG1 PRKG1 45.5 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 83.4 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 87.5 1000
RIOK2 RIOK2 98.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 85.8 1000
RIPK2 RIPK2 98.7 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 76.9 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 86.1 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 78.8 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 83.4 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 91.5 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 99.2 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 87.7 1000
RPS6KB1 S6K1 93.8 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 87.8 1000
SLK SLK 98.4 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 95.9 1000
SRMS SRMS 97.9 1000
SRPK1 SRPK1 67.5 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 84.6 1000
STK33 STK33 91.6 1000
STK35 STK35 85.9 1000
STK36 STK36 100.0 1000
STK39 STK39 90.8 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 94.4 1000
TAOK3 TAOK3 73.0 1000
TBK1 TBK1 89.5 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 99.2 1000
TGFBR2 TGFBR2 67.8 1000
TIE1 TIE1 89.9 1000
TEK TIE2 100.0 1000
TLK1 TLK1 85.3 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 90.8 1000
TNK1 TNK1 62.1 1000
TNK2 TNK2 78.6 1000
TNNI3K TNNI3K 99.7 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 98.1 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 83.8 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 96.2 1000
TTK TTK 97.9 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 94.9 1000
TYRO3 TYRO3 66.9 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 84.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 77.6 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 89.0 1000
WNK2 WNK2 94.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 94.1 1000
YES1 YES 81.1 1000
STK25 YSK1 89.9 1000
MAP3K19 YSK4 93.0 1000
MAP3K20 ZAK 96.9 1000
ZAP70 ZAP70 88.1 1000

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