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Selectivity data for probe BAY-899 and control BAY-897


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BAY-899


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT7A HTR7 2.63
Alpha2B ADRA2B 9.66
D1 DRD1 23.66
DAT SLC6A3 -39.30
H1 HRH1 5.89
H4 HRH4 -4.41
M1 CHRM1 7.56
M3 CHRM3 -12.35
M4 CHRM4 22.81
M5 CHRM5 11.97
Sigma 2 TMEM97 53.17 2051.16 5.69
5-HT1B HTR1B 36.40
5-HT2B HTR2B 37.60
5-HT2C HTR2C 18.28
Alpha1A ADRA1A -3.50
Alpha1B ADRA1B -4.40
Alpha1D ADRA1D 8.01
D3 DRD3 -4.36
M2 CHRM2 -5.10
5-HT1A HTR1A -8.97
5-HT5A HTR5A -11.21
5-HT6 HTR6 -3.59
Alpha2A ADRA2A 9.77
Alpha2C ADRA2C 8.55
D2 DRD2 1.65
GABAA 19.37
H3 HRH3 -8.41
MOR OPRM1 28.12
NET SLC6A2 10.22
Sigma 1 SIGMAR1 64.42 1431.53 5.84
D4 DRD4 43.75
D5 DRD5 10.05
DOR OPRD1 -10.33
KOR OPRK1 56.27 7634.84 5.12
GABA/PBR 44.56
5-HT1D HTR1D 4.38
5-HT1E HTR1E -8.08
5-HT2A HTR2A 8.72
Beta1 ADRB1 11.30
Beta2 ADRB2 25.28
5-HT3 HTR3A 45.75
Beta3 ADRB3 -13.70
H2 HRH2 2.75
SERT SLC6A4 25.50
GABAA/BZP 25.98

BAY-897


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABAA/BZP 22.45
Beta2 ADRB2 25.60
Beta3 ADRB3 29.37
Beta1 ADRB1 -7.28
H2 HRH2 7.29
SERT SLC6A4 21.08
5-HT1D HTR1D 43.28
5-HT1E HTR1E 1.61
5-HT2A HTR2A 54.49 3674.51 5.43
5-HT3 HTR3A 4.70
D4 DRD4 0.29
D5 DRD5 29.13
DOR OPRD1 32.71
KOR OPRK1 79.29 3134.73 5.50
GABA/PBR 33.44
5-HT1A HTR1A -3.56
5-HT5A HTR5A 7.18
5-HT6 HTR6 16.91
Alpha2A ADRA2A 7.16
Alpha2C ADRA2C 8.47
D1 DRD1 39.11
D2 DRD2 -3.97
GABAA 26.88
H3 HRH3 3.57
NET SLC6A2 32.50
Sigma 1 SIGMAR1 73.44 2398.28 5.62
5-HT1B HTR1B 18.80
5-HT2B HTR2B 52.42 5254.12 5.28
5-HT2C HTR2C 68.41 1082.93 5.97
Alpha1A ADRA1A 16.25
Alpha1B ADRA1B 12.21
Alpha1D ADRA1D 34.05
M2 CHRM2 -1.78
5-HT7A HTR7 -11.79
Alpha2B ADRA2B 49.57
D3 DRD3 -2.66
DAT SLC6A3 -22.83
H1 HRH1 15.89
H4 HRH4 7.56
M1 CHRM1 -2.98
M3 CHRM3 -3.47
M4 CHRM4 9.29
M5 CHRM5 -1.70
Sigma 2 TMEM97 80.82 675.62 6.17
MOR OPRM1 37.15

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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-899


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 91.0 1000
ABL1 ABL1-phosphorylated 94.0 1000
ABL2 ABL2 78.0 1000
ACVR1 ACVR1 97.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 83.0 1000
ACVR2B ACVR2B 85.0 1000
ACVRL1 ACVRL1 99.0 1000
COQ8A ADCK3 95.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 78.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 88.0 1000
PRKAA2 AMPK-alpha2 79.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 95.0 1000
MAP3K5 ASK1 84.0 1000
MAP3K6 ASK2 94.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 80.0 1000
AURKC AURKC 81.0 1000
AXL AXL 76.0 1000
BMP2K BIKE 93.0 1000
BLK BLK 80.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 98.0 1000
BMPR2 BMPR2 88.0 1000
BMX BMX 94.0 1000
BRAF BRAF(V600E) 83.0 1000
PTK6 BRK 98.0 1000
BRSK1 BRSK1 87.0 1000
BRSK2 BRSK2 89.0 1000
BTK BTK 92.0 1000
BUB1 BUB1 92.0 1000
CAMK1 CAMK1 73.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 97.0 1000
CAMK2A CAMK2A 92.0 1000
CAMK2B CAMK2B 92.0 1000
CAMK2D CAMK2D 92.0 1000
CAMK2G CAMK2G 80.0 1000
CAMK4 CAMK4 97.0 1000
CAMKK1 CAMKK1 92.0 1000
CAMKK2 CAMKK2 93.0 1000
CASK CASK 94.0 1000
CDK11B CDC2L1 94.0 1000
CDK11A CDC2L2 91.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 75.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 89.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 70.0 1000
CDK9 CDK9 93.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 33.0 1000
CDKL3 CDKL3 77.0 1000
CDKL5 CDKL5 89.0 1000
CHEK1 CHEK1 84.0 1000
CHEK2 CHEK2 92.0 1000
CIT CIT 88.0 1000
CLK1 CLK1 80.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 88.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 93.0 1000
MARK3 MARK3 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 85.0 1000
CSNK1A1L CSNK1A1L 82.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 66.0 1000
CSNK1G1 CSNK1G1 99.0 1000
CSNK1G2 CSNK1G2 96.0 1000
CSNK1G3 CSNK1G3 87.0 1000
CSNK2A1 CSNK2A1 93.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 80.0 1000
DAPK1 DAPK1 78.0 1000
DAPK2 DAPK2 91.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 83.0 1000
DCLK2 DCAMKL2 90.0 1000
DCLK3 DCAMKL3 96.0 1000
DDR1 DDR1 95.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 98.0 1000
CDC42BPG DMPK2 98.0 1000
STK17A DRAK1 85.0 1000
STK17B DRAK2 92.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 78.0 1000
DYRK2 DYRK2 81.0 1000
EGFR EGFR(T790M) 91.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 99.0 1000
EPHA3 EPHA3 82.0 1000
EPHA4 EPHA4 88.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 88.0 1000
EPHA8 EPHA8 88.0 1000
EPHB1 EPHB1 83.0 1000
EPHB2 EPHB2 87.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 80.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 97.0 1000
MAPK3 ERK1 92.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 95.0 1000
MAPK7 ERK5 96.0 1000
MAPK15 ERK8 93.0 1000
ERN1 ERN1 85.0 1000
PTK2 FAK 100.0 1000
FER FER 93.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 82.0 1000
FGFR2 FGFR2 98.0 1000
FGFR3 FGFR3(G697C) 89.0 1000
FGFR4 FGFR4 98.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 88.0 1000
FLT3 FLT3-autoinhibited 90.0 1000
FLT4 FLT4 96.0 1000
FRK FRK 98.0 1000
FYN FYN 100.0 1000
GAK GAK 94.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 85.0 1000
GRK1 GRK1 91.0 1000
GRK2 GRK2 90.0 1000
GRK3 GRK3 96.0 1000
GRK4 GRK4 67.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 93.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 93.0 1000
HCK HCK 96.0 1000
HIPK1 HIPK1 70.0 1000
HIPK2 HIPK2 91.0 1000
HIPK3 HIPK3 90.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 92.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 98.0 1000
INSR INSR 81.0 1000
INSRR INSRR 84.0 1000
IRAK1 IRAK1 88.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 95.0 1000
ITK ITK 90.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 96.0 1000
JAK2 JAK2(JH1domain-catalytic) 84.0 1000
JAK3 JAK3(JH1domain-catalytic) 91.0 1000
MAPK8 JNK1 83.0 1000
MAPK9 JNK2 85.0 1000
MAPK10 JNK3 88.0 1000
KIT KIT-autoinhibited 81.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 99.0 1000
LCK LCK 83.0 1000
LIMK1 LIMK1 99.0 1000
LIMK2 LIMK2 97.0 1000
STK11 LKB1 75.0 1000
STK10 LOK 94.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 93.0 1000
LYN LYN 82.0 1000
MAP3K13 LZK 88.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 89.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 99.0 1000
MAP3K3 MAP3K3 97.0 1000
MAP3K4 MAP3K4 89.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 87.0 1000
MAP4K4 MAP4K4 86.0 1000
MAP4K5 MAP4K5 77.0 1000
MAPKAPK2 MAPKAPK2 80.0 1000
MAPKAPK5 MAPKAPK5 91.0 1000
MARK1 MARK1 71.0 1000
MARK2 MARK2 90.0 1000
MARK4 MARK4 91.0 1000
MAST1 MAST1 96.0 1000
MAP2K1 MEK1 93.0 1000
MAP2K2 MEK2 93.0 1000
MAP2K3 MEK3 76.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 83.0 1000
MAP2K6 MEK6 77.0 1000
MELK MELK 66.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 93.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 95.0 1000
MKNK1 MKNK1 95.0 1000
MKNK2 MKNK2 94.0 1000
MYLK3 MLCK 89.0 1000
MAP3K9 MLK1 92.0 1000
MAP3K10 MLK2 77.0 1000
MAP3K11 MLK3 83.0 1000
CDC42BPA MRCKA 96.0 1000
CDC42BPB MRCKB 73.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 77.0 1000
STK26 MST4 90.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 86.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 90.0 1000
MYLK4 MYLK4 88.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 91.0 1000
STK38L NDR2 75.0 1000
NEK1 NEK1 84.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 92.0 1000
NEK3 NEK3 67.0 1000
NEK4 NEK4 79.0 1000
NEK5 NEK5 90.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 84.0 1000
NEK9 NEK9 90.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 90.0 1000
NLK NLK 73.0 1000
OXSR1 OSR1 93.0 1000
MAPK14 p38-alpha 79.0 1000
MAPK11 p38-beta 84.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 96.0 1000
PAK1 PAK1 71.0 1000
PAK2 PAK2 59.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 82.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 95.0 1000
CDK16 PCTK1 75.0 1000
CDK17 PCTK2 97.0 1000
CDK18 PCTK3 96.0 1000
PDGFRA PDGFRA 93.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 97.0 1000
CDPK1 PFCDPK1(P.falciparum) 95.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 93.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 96.0 1000
PIK3C2B PIK3C2B 95.0 1000
PIK3C2G PIK3C2G 97.0 1000
PIK3CA PIK3CA(Q546K) 95.0 1000
PIK3CB PIK3CB 84.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 85.0 1000
PI4KB PIK4CB 89.0 1000
PIKFYVE PIKFYVE 63.0 1000
PIM1 PIM1 91.0 1000
PIM2 PIM2 94.0 1000
PIM3 PIM3 82.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 86.0 1000
PRKACA PKAC-alpha 82.0 1000
PRKACB PKAC-beta 85.0 1000
PKMYT1 PKMYT1 80.0 1000
PKN1 PKN1 95.0 1000
PKN2 PKN2 78.0 1000
PKNB PKNB(M.tuberculosis) 90.0 1000
PLK1 PLK1 80.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 87.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 87.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 76.0 1000
PRKCI PRKCI 98.0 1000
PRKCQ PRKCQ 94.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 85.0 1000
PRKD3 PRKD3 84.0 1000
PRKG1 PRKG1 89.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 73.0 1000
PRKX PRKX 93.0 1000
PRPF4B PRP4 90.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 86.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 94.0 1000
RIOK1 RIOK1 89.0 1000
RIOK2 RIOK2 96.0 1000
RIOK3 RIOK3 89.0 1000
RIPK1 RIPK1 99.0 1000
RIPK2 RIPK2 93.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 100.0 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) 74.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 76.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 82.0 1000
RPS6KB1 S6K1 89.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 75.0 1000
SBK3 SgK110 90.0 1000
SGK2 SGK2 79.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 88.0 1000
SIK2 SIK2 89.0 1000
SLK SLK 82.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 90.0 1000
SRC SRC 93.0 1000
SRMS SRMS 95.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 69.0 1000
STK35 STK35 71.0 1000
STK36 STK36 91.0 1000
STK39 STK39 77.0 1000
SYK SYK 84.0 1000
MAP3K7 TAK1 90.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 87.0 1000
TAOK3 TAOK3 100.0 1000
TBK1 TBK1 87.0 1000
TEC TEC 89.0 1000
TESK1 TESK1 91.0 1000
TGFBR1 TGFBR1 90.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 88.0 1000
TEK TIE2 93.0 1000
TLK1 TLK1 90.0 1000
TLK2 TLK2 89.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 97.0 1000
TNK2 TNK2 93.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 75.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 86.0 1000
TTK TTK 86.0 1000
TXK TXK 87.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 88.0 1000
ULK2 ULK2 93.0 1000
ULK3 ULK3 95.0 1000
KDR VEGFR2 88.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 85.0 1000
WEE2 WEE2 95.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 79.0 1000
WNK3 WNK3 93.0 1000
WNK4 WNK4 81.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 87.0 1000
STK32C YANK3 96.0 1000
YES1 YES 98.0 1000
STK25 YSK1 82.0 1000
MAP3K19 YSK4 81.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 93.0 1000

BAY-897


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 95.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 88.0 1000
ACVR1 ACVR1 96.0 1000
ACVR1B ACVR1B 94.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 81.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 92.0 1000
AKT1 AKT1 95.0 1000
AKT2 AKT2 96.0 1000
AKT3 AKT3 95.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 96.0 1000
PRKAA2 AMPK-alpha2 51.0 1000
ANKK1 ANKK1 92.0 1000
NUAK1 ARK5 92.0 1000
MAP3K5 ASK1 87.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 89.0 1000
AURKC AURKC 87.0 1000
AXL AXL 77.0 1000
BMP2K BIKE 94.0 1000
BLK BLK 90.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 87.0 1000
BMPR2 BMPR2 96.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 93.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 95.0 1000
BTK BTK 93.0 1000
BUB1 BUB1 98.0 1000
CAMK1 CAMK1 70.0 1000
PNCK CAMK1B 96.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 88.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 89.0 1000
CAMK2G CAMK2G 96.0 1000
CAMK4 CAMK4 86.0 1000
CAMKK1 CAMKK1 99.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 89.0 1000
CDK11A CDC2L2 92.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 79.0 1000
CDK2 CDK2 90.0 1000
CDK3 CDK3 93.0 1000
CDK4 CDK4-cyclinD3 94.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 77.0 1000
CDK8 CDK8 95.0 1000
CDK9 CDK9 87.0 1000
CDKL1 CDKL1 97.0 1000
CDKL2 CDKL2 77.0 1000
CDKL3 CDKL3 82.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 94.0 1000
CIT CIT 91.0 1000
CLK1 CLK1 86.0 1000
CLK2 CLK2 95.0 1000
CLK3 CLK3 82.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 95.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 97.0 1000
CSNK1A1L CSNK1A1L 92.0 1000
CSNK1D CSNK1D 90.0 1000
CSNK1E CSNK1E 85.0 1000
CSNK1G1 CSNK1G1 90.0 1000
CSNK1G2 CSNK1G2 98.0 1000
CSNK1G3 CSNK1G3 80.0 1000
CSNK2A1 CSNK2A1 99.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 90.0 1000
DAPK1 DAPK1 87.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 87.0 1000
DCLK3 DCAMKL3 93.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 91.0 1000
CDC42BPG DMPK2 93.0 1000
STK17A DRAK1 86.0 1000
STK17B DRAK2 89.0 1000
DYRK1A DYRK1A 95.0 1000
DYRK1B DYRK1B 88.0 1000
DYRK2 DYRK2 84.0 1000
EGFR EGFR(T790M) 87.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 91.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 90.0 1000
EPHA8 EPHA8 92.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 91.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 70.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 82.0 1000
MAPK3 ERK1 87.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 98.0 1000
MAPK4 ERK4 95.0 1000
MAPK7 ERK5 96.0 1000
MAPK15 ERK8 94.0 1000
ERN1 ERN1 85.0 1000
PTK2 FAK 100.0 1000
FER FER 91.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 93.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 95.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 96.0 1000
FRK FRK 93.0 1000
FYN FYN 89.0 1000
GAK GAK 89.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 91.0 1000
GRK2 GRK2 92.0 1000
GRK3 GRK3 95.0 1000
GRK4 GRK4 93.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 95.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 85.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 96.0 1000
HIPK2 HIPK2 79.0 1000
HIPK3 HIPK3 92.0 1000
HIPK4 HIPK4 96.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 99.0 1000
CILK1 ICK 76.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 89.0 1000
INSR INSR 86.0 1000
INSRR INSRR 94.0 1000
IRAK1 IRAK1 88.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 96.0 1000
ITK ITK 96.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 91.0 1000
MAPK9 JNK2 88.0 1000
MAPK10 JNK3 82.0 1000
KIT KIT-autoinhibited 91.0 1000
LATS1 LATS1 86.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 94.0 1000
LIMK1 LIMK1 85.0 1000
LIMK2 LIMK2 93.0 1000
STK11 LKB1 61.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 86.0 1000
LYN LYN 95.0 1000
MAP3K13 LZK 98.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 87.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 89.0 1000
MAP3K3 MAP3K3 87.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 95.0 1000
MAP4K3 MAP4K3 90.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 91.0 1000
MAPKAPK2 MAPKAPK2 98.0 1000
MAPKAPK5 MAPKAPK5 75.0 1000
MARK1 MARK1 81.0 1000
MARK2 MARK2 82.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 86.0 1000
MAST1 MAST1 79.0 1000
MAP2K1 MEK1 98.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 88.0 1000
MAP2K4 MEK4 86.0 1000
MAP2K5 MEK5 81.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 78.0 1000
MERTK MERTK 96.0 1000
MET MET(Y1235D) 86.0 1000
MINK1 MINK 99.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 95.0 1000
MKNK2 MKNK2 91.0 1000
MYLK3 MLCK 80.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 78.0 1000
CDC42BPA MRCKA 94.0 1000
CDC42BPB MRCKB 88.0 1000
STK4 MST1 99.0 1000
MST1R MST1R 98.0 1000
STK3 MST2 94.0 1000
STK24 MST3 93.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 92.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 97.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 83.0 1000
STK38 NDR1 99.0 1000
STK38L NDR2 76.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 93.0 1000
NEK3 NEK3 64.0 1000
NEK4 NEK4 94.0 1000
NEK5 NEK5 96.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 82.0 1000
NEK9 NEK9 88.0 1000
MAP3K14 NIK 61.0 1000
NIM1K NIM1 80.0 1000
NLK NLK 87.0 1000
OXSR1 OSR1 90.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 96.0 1000
MAPK12 p38-gamma 94.0 1000
PAK1 PAK1 82.0 1000
PAK2 PAK2 52.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 94.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 65.0 1000
CDK17 PCTK2 96.0 1000
CDK18 PCTK3 98.0 1000
PDGFRA PDGFRA 95.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 88.0 1000
CDPK1 PFCDPK1(P.falciparum) 96.0 1000
PK5 PFPK5(P.falciparum) 87.0 1000
CDK15 PFTAIRE2 86.0 1000
CDK14 PFTK1 94.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 96.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 75.0 1000
PIK3CB PIK3CB 77.0 1000
PIK3CD PIK3CD 93.0 1000
PIK3CG PIK3CG 87.0 1000
PI4KB PIK4CB 75.0 1000
PIKFYVE PIKFYVE 95.0 1000
PIM1 PIM1 99.0 1000
PIM2 PIM2 93.0 1000
PIM3 PIM3 79.0 1000
PIP5K1A PIP5K1A 95.0 1000
PIP5K1C PIP5K1C 96.0 1000
PIP4K2B PIP5K2B 97.0 1000
PIP4K2C PIP5K2C 94.0 1000
PRKACA PKAC-alpha 95.0 1000
PRKACB PKAC-beta 83.0 1000
PKMYT1 PKMYT1 63.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 80.0 1000
PKNB PKNB(M.tuberculosis) 86.0 1000
PLK1 PLK1 78.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 87.0 1000
PLK4 PLK4 94.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 93.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 95.0 1000
PRKD1 PRKD1 94.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 98.0 1000
PRKG1 PRKG1 91.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 88.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 89.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 94.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 94.0 1000
RIOK3 RIOK3 96.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 96.0 1000
RIPK4 RIPK4 84.0 1000
DSTYK RIPK5 100.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 93.0 1000
ROS1 ROS1 76.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 73.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 74.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 92.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 97.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 94.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 95.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 89.0 1000
SGK1 SGK 95.0 1000
SBK3 SgK110 70.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 97.0 1000
SIK1 SIK 99.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 82.0 1000
SNRK SNRK 90.0 1000
SRC SRC 91.0 1000
SRMS SRMS 94.0 1000
SRPK1 SRPK1 94.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 50.0 1000
STK35 STK35 80.0 1000
STK36 STK36 89.0 1000
STK39 STK39 82.0 1000
SYK SYK 91.0 1000
MAP3K7 TAK1 89.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 92.0 1000
TBK1 TBK1 81.0 1000
TEC TEC 86.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 85.0 1000
TGFBR2 TGFBR2 91.0 1000
TIE1 TIE1 85.0 1000
TEK TIE2 100.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 96.0 1000
TNK2 TNK2 99.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 85.0 1000
NTRK2 TRKB 84.0 1000
NTRK3 TRKC 68.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 87.0 1000
TSSK3 TSSK3 98.0 1000
TTK TTK 94.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 99.0 1000
ULK1 ULK1 89.0 1000
ULK2 ULK2 98.0 1000
ULK3 ULK3 99.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 92.0 1000
VRK2 VRK2 97.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 96.0 1000
WNK2 WNK2 88.0 1000
WNK3 WNK3 94.0 1000
WNK4 WNK4 85.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 72.0 1000
STK32C YANK3 75.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 88.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 91.0 1000

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BAY-899

The percentage of the mean value obtained when testing in duplicates at a single concentration of 10 µM is reported. Shown are supplementary data (Table S1) from PMID: 31670515 .

Conclusion: No inhibition or activation > 70% at 10 µM compound concentration reveals excellent selectivity within target family.

Target protein HGNC name Species Cmp. conc. First measurement [Inhibition (% of control)] Assay ID
A2B ADORA2B Homo sapiens 10 µM 16.0 Cerep_455
A3 ADORA3 Homo sapiens 10 µM -6.0 Cerep_983
alpha 1A ADRA1A Homo sapiens 10 µM 45.0 Cerep_1501
alpha 2A ADRA2A Homo sapiens 10 µM -16.0 Cerep_4317
beta 1 ADRB1 Homo sapiens 10 µM 13.0 Cerep_1606
beta 2 ADRB2 Homo sapiens 10 µM 26.0 Cerep_1977
CB1 CNR1 Homo sapiens 10 µM 4.0 Cerep_1745
D1 DRD1 Homo sapiens 10 µM 15.0 Cerep_1686
D2L DRD2 Homo sapiens 10 µM 67.0 Cerep_4254
H1 HRH1 Homo sapiens 10 µM 4.0 Cerep_2543
H2 HRH2 Homo sapiens 10 µM 34.0 Cerep_1696
H3 HRH3 Homo sapiens 10 µM -19.0 Cerep_1801
MC4 MC4R Homo sapiens 10 µM 11.0 Cerep_700
Motilin MLN Homo sapiens 10 µM 28.0 Cerep_1894
M1 CHRM1 Homo sapiens 10 µM 32.0 Cerep_1474
M4 CHRM4 Homo sapiens 10 µM 2.0 Cerep_1671
NK1 TACR1 Homo sapiens 10 µM 24.0 Cerep_2192
kappa (KOP) OPRK1 Homo sapiens 10 µM -10.0 Cerep_4460
mu (MOP) OPRM1 Homo sapiens 10 µM 8.0 Cerep_1393
EP3 PTGER3 Homo sapiens 10 µM -5.0 Cerep_4331
P2Y2 P2RY2 Homo sapiens 10 µM 8.0 Cerep_2167
5-HT1A HTR1A Homo sapiens 10 µM 0.0 Cerep_4333
5-HT2B HTR2B Homo sapiens 10 µM 18.0 Cerep_3345
5-HT6 HTR6 Homo sapiens 10 µM 12.0 Cerep_1628
sst4 SSTR4 Homo sapiens 10 µM 6.0 Cerep_2103
A2B ADORA2B Homo sapiens 10 µM -1.0 Cerep_452
A3 ADORA3 Homo sapiens 10 µM 25.0 Cerep_982
alpha 1A ADRA1A Homo sapiens 10 µM 2.0 Cerep_1500
alpha 2A ADRA2A Homo sapiens 10 µM -2.0 Cerep_4316
beta 1 ADRB1 Homo sapiens 10 µM -1.0 Cerep_1605
beta 2 ADRB2 Homo sapiens 10 µM -3.0 Cerep_1976
CB1 CNR1 Homo sapiens 10 µM 52.0 Cerep_1744
D1 DRD1 Homo sapiens 10 µM -1.0 Cerep_1685
D2L DRD2 Homo sapiens 10 µM -1.0 Cerep_4253
H1 HRH1 Homo sapiens 10 µM -4.0 Cerep_2542
H2 HRH2 Homo sapiens 10 µM -2.0 Cerep_1695
H3 HRH3 Homo sapiens 10 µM 38.0 Cerep_1800
MC4 MC4R Homo sapiens 10 µM -2.0 Cerep_699
Motilin MLN Homo sapiens 10 µM -1.0 Cerep_1321
M1 CHRM1 Homo sapiens 10 µM 1.0 Cerep_1262
M4 CHRM4 Homo sapiens 10 µM -6.0 Cerep_1670
NK1 TACR1 Homo sapiens 10 µM -3.0 Cerep_2190
kappa (KOP) OPRK1 Homo sapiens 10 µM 56.0 Cerep_4459
mu (MOP) OPRM1 Homo sapiens 10 µM 56.0 Cerep_1392
EP3 PTGER3 Homo sapiens 10 µM -1.0 Cerep_4330
P2Y2 P2RY2 Homo sapiens 10 µM -1.0 Cerep_2164
5-HT1A HTR1A Homo sapiens 10 µM 1.0 Cerep_4332
5-HT2B HTR2B Homo sapiens 10 µM 1.0 Cerep_3344
5-HT6 HTR6 Homo sapiens 10 µM -1.0 Cerep_1627
sst4 SSTR4 Homo sapiens 10 µM 23.0 Cerep_2095