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Selectivity data for probe BI-4394 and control BI-4395


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BI-4394


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT3 HTR3A 34.84
5-HT5A HTR5A 14.80
5-HT6 HTR6 4.01
5-HT7A HTR7 5.88
D1 DRD1 -5.02
D2 DRD2 -28.97
Alpha1A ADRA1A -6.15
Alpha1B ADRA1B -1.29
D3 DRD3 2.74
D4 DRD4 -19.32
D5 DRD5 59.61 > 10000.00 average (n=3) < 5.00
DAT SLC6A3 2.26
H1 HRH1 9.64
H3 HRH3 8.18
H4 HRH4 -1.52
M1 CHRM1 -17.39
M2 CHRM2 -17.17
M4 CHRM4 -6.49
M5 CHRM5 7.64
NET SLC6A2 -21.09
GABA/PBR -1.91
5-HT1A HTR1A -13.46
5-HT1B HTR1B 6.12
5-HT1D HTR1D 3.64
5-HT2A HTR2A 19.07
5-HT2B HTR2B 8.13
Alpha1D ADRA1D -10.59
Alpha2A ADRA2A 12.34
Alpha2B ADRA2B 16.43
Alpha2C ADRA2C -7.04
Beta2 ADRB2 -7.76
GABAA/BZP 1.07
DOR OPRD1 -9.42
MOR OPRM1 0.37
Sigma 1 SIGMAR1 14.57
5-HT1E HTR1E 6.37
H2 HRH2 -14.40
GABAA 15.32
M3 CHRM3 4.89
SERT SLC6A4 -0.14
Sigma 2 TMEM97 -10.33
5-HT2C HTR2C 3.56
KOR OPRK1 27.17
Beta1 ADRB1 -5.04
Beta3 ADRB3 -6.63

BI-4395


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 -18.85
Beta3 ADRB3 2.13
5-HT3 HTR3A 23.47
5-HT5A HTR5A 0.78
5-HT6 HTR6 8.85
5-HT7A HTR7 -4.31
D1 DRD1 -19.57
D2 DRD2 -14.39
Alpha1A ADRA1A -13.83
Alpha1B ADRA1B -6.10
D3 DRD3 1.67
D4 DRD4 -8.91
D5 DRD5 73.87 > 10000.00 average (n=2) < 5.00
DAT SLC6A3 -16.91
H1 HRH1 8.74
H3 HRH3 -4.12
H4 HRH4 -6.14
M1 CHRM1 -23.29
M2 CHRM2 -8.35
M4 CHRM4 0.05
M5 CHRM5 -7.43
NET SLC6A2 -21.36
GABA/PBR 6.39
5-HT1A HTR1A 22.66
5-HT1B HTR1B 5.48
5-HT1D HTR1D 10.11
5-HT2A HTR2A 23.57
5-HT2B HTR2B -2.75
Alpha1D ADRA1D -18.75
Alpha2A ADRA2A -14.17
Alpha2B ADRA2B 6.00
Alpha2C ADRA2C -7.92
Beta2 ADRB2 6.74
GABAA/BZP 29.08
DOR OPRD1 0.80
MOR OPRM1 2.90
Sigma 1 SIGMAR1 1.99
5-HT1E HTR1E 10.34
H2 HRH2 8.57
GABAA 26.65
M3 CHRM3 -0.66
SERT SLC6A4 5.30
Sigma 2 TMEM97 -10.81
5-HT2C HTR2C -9.67
KOR OPRK1 16.83

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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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BI-4394


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 100
ABL1 ABL1-phosphorylated 94.0 100
ABL2 ABL2 100.0 100
ACVR1 ACVR1 84.0 100
ACVR1B ACVR1B 86.0 100
ACVR2A ACVR2A 59.0 100
ACVR2B ACVR2B 91.0 100
ACVRL1 ACVRL1 68.0 100
COQ8A ADCK3 100.0 100
COQ8B ADCK4 100.0 100
AKT1 AKT1 100.0 100
AKT2 AKT2 100.0 100
AKT3 AKT3 86.0 100
ALK ALK(L1196M) 98.0 100
PRKAA1 AMPK-alpha1 100.0 100
PRKAA2 AMPK-alpha2 88.0 100
ANKK1 ANKK1 100.0 100
NUAK1 ARK5 100.0 100
MAP3K5 ASK1 98.0 100
MAP3K6 ASK2 79.0 100
AURKA AURKA 90.0 100
AURKB AURKB 100.0 100
AURKC AURKC 100.0 100
AXL AXL 89.0 100
BMP2K BIKE 100.0 100
BLK BLK 99.0 100
BMPR1A BMPR1A 87.0 100
BMPR1B BMPR1B 96.0 100
BMPR2 BMPR2 82.0 100
BMX BMX 82.0 100
BRAF BRAF(V600E) 100.0 100
PTK6 BRK 98.0 100
BRSK1 BRSK1 100.0 100
BRSK2 BRSK2 67.0 100
BTK BTK 77.0 100
BUB1 BUB1 100.0 100
CAMK1 CAMK1 87.0 100
PNCK CAMK1B 97.0 100
CAMK1D CAMK1D 100.0 100
CAMK1G CAMK1G 100.0 100
CAMK2A CAMK2A 76.0 100
CAMK2B CAMK2B 96.0 100
CAMK2D CAMK2D 91.0 100
CAMK2G CAMK2G 100.0 100
CAMK4 CAMK4 95.0 100
CAMKK1 CAMKK1 100.0 100
CAMKK2 CAMKK2 95.0 100
CASK CASK 71.0 100
CDK11B CDC2L1 98.0 100
CDK11A CDC2L2 100.0 100
CDK13 CDC2L5 83.0 100
CDK19 CDK11 0.0 100
CDK2 CDK2 90.0 100
CDK3 CDK3 43.0 100
CDK4 CDK4-cyclinD3 74.0 100
CDK5 CDK5 94.0 100
CDK7 CDK7 76.0 100
CDK8 CDK8 62.0 100
CDK9 CDK9 97.0 100
CDKL1 CDKL1 77.0 100
CDKL2 CDKL2 88.0 100
CDKL3 CDKL3 0.0 100
CDKL5 CDKL5 87.0 100
CHEK1 CHEK1 100.0 100
CHEK2 CHEK2 100.0 100
CIT CIT 100.0 100
CLK1 CLK1 100.0 100
CLK2 CLK2 96.0 100
CLK3 CLK3 83.0 100
CLK4 CLK4 89.0 100
CSF1R CSF1R-autoinhibited 94.0 100
CSK CSK 74.0 100
CSNK1A1 CSNK1A1 88.0 100
CSNK1A1L CSNK1A1L 100.0 100
CSNK1D CSNK1D 81.0 100
CSNK1E CSNK1E 100.0 100
CSNK1G1 CSNK1G1 100.0 100
CSNK1G2 CSNK1G2 79.0 100
CSNK1G3 CSNK1G3 100.0 100
CSNK2A1 CSNK2A1 81.0 100
CSNK2A2 CSNK2A2 87.0 100
MATK CTK 96.0 100
DAPK1 DAPK1 84.0 100
DAPK2 DAPK2 92.0 100
DAPK3 DAPK3 98.0 100
DCLK1 DCAMKL1 86.0 100
DCLK2 DCAMKL2 100.0 100
DCLK3 DCAMKL3 73.0 100
DDR1 DDR1 100.0 100
DDR2 DDR2 76.0 100
MAP3K12 DLK 79.0 100
DMPK DMPK 87.0 100
CDC42BPG DMPK2 93.0 100
STK17A DRAK1 97.0 100
STK17B DRAK2 100.0 100
DYRK1A DYRK1A 90.0 100
DYRK1B DYRK1B 100.0 100
DYRK2 DYRK2 76.0 100
EGFR EGFR(T790M) 89.0 100
EIF2AK1 EIF2AK1 91.0 100
EPHA1 EPHA1 100.0 100
EPHA2 EPHA2 100.0 100
EPHA3 EPHA3 100.0 100
EPHA4 EPHA4 96.0 100
EPHA5 EPHA5 100.0 100
EPHA6 EPHA6 94.0 100
EPHA7 EPHA7 97.0 100
EPHA8 EPHA8 100.0 100
EPHB1 EPHB1 100.0 100
EPHB2 EPHB2 100.0 100
EPHB3 EPHB3 90.0 100
EPHB4 EPHB4 99.0 100
EPHB6 EPHB6 77.0 100
ERBB2 ERBB2 99.0 100
ERBB3 ERBB3 81.0 100
ERBB4 ERBB4 96.0 100
MAPK3 ERK1 88.0 100
MAPK1 ERK2 99.0 100
MAPK6 ERK3 97.0 100
MAPK4 ERK4 86.0 100
MAPK7 ERK5 100.0 100
MAPK15 ERK8 100.0 100
ERN1 ERN1 90.0 100
PTK2 FAK 94.0 100
FER FER 100.0 100
FES FES 94.0 100
FGFR1 FGFR1 86.0 100
FGFR2 FGFR2 89.0 100
FGFR3 FGFR3(G697C) 92.0 100
FGFR4 FGFR4 68.0 100
FGR FGR 94.0 100
FLT1 FLT1 97.0 100
FLT3 FLT3-autoinhibited 98.0 100
FLT4 FLT4 97.0 100
FRK FRK 100.0 100
FYN FYN 100.0 100
GAK GAK 85.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 100
GRK1 GRK1 95.0 100
GRK2 GRK2 100.0 100
GRK3 GRK3 96.0 100
GRK4 GRK4 100.0 100
GRK7 GRK7 86.0 100
GSK3A GSK3A 100.0 100
GSK3B GSK3B 95.0 100
HASPIN HASPIN 77.0 100
HCK HCK 100.0 100
HIPK1 HIPK1 91.0 100
HIPK2 HIPK2 82.0 100
HIPK3 HIPK3 81.0 100
HIPK4 HIPK4 87.0 100
MAP4K1 HPK1 100.0 100
HUNK HUNK 100.0 100
CILK1 ICK 85.0 100
IGF1R IGF1R 82.0 100
CHUK IKK-alpha 100.0 100
IKBKB IKK-beta 100.0 100
IKBKE IKK-epsilon 66.0 100
INSR INSR 81.0 100
INSRR INSRR 77.0 100
IRAK1 IRAK1 85.0 100
IRAK3 IRAK3 100.0 100
IRAK4 IRAK4 91.0 100
ITK ITK 100.0 100
JAK1 JAK1(JH2domain-pseudokinase) 94.0 100
JAK2 JAK2(JH1domain-catalytic) 95.0 100
JAK3 JAK3(JH1domain-catalytic) 82.0 100
MAPK8 JNK1 96.0 100
MAPK9 JNK2 96.0 100
MAPK10 JNK3 100.0 100
KIT KIT-autoinhibited 83.0 100
LATS1 LATS1 97.0 100
LATS2 LATS2 74.0 100
LCK LCK 94.0 100
LIMK1 LIMK1 100.0 100
LIMK2 LIMK2 96.0 100
STK11 LKB1 100.0 100
STK10 LOK 100.0 100
LRRK2 LRRK2(G2019S) 83.0 100
LTK LTK 100.0 100
LYN LYN 100.0 100
MAP3K13 LZK 74.0 100
MAK MAK 100.0 100
MAP3K1 MAP3K1 90.0 100
MAP3K15 MAP3K15 100.0 100
MAP3K2 MAP3K2 100.0 100
MAP3K3 MAP3K3 94.0 100
MAP3K4 MAP3K4 91.0 100
MAP4K2 MAP4K2 84.0 100
MAP4K3 MAP4K3 89.0 100
MAP4K4 MAP4K4 95.0 100
MAP4K5 MAP4K5 93.0 100
MAPKAPK2 MAPKAPK2 72.0 100
MAPKAPK5 MAPKAPK5 92.0 100
MARK1 MARK1 76.0 100
MARK2 MARK2 100.0 100
MARK3 MARK3 93.0 100
MARK4 MARK4 79.0 100
MAST1 MAST1 87.0 100
MAP2K1 MEK1 90.0 100
MAP2K2 MEK2 83.0 100
MAP2K3 MEK3 100.0 100
MAP2K4 MEK4 93.0 100
MAP2K5 MEK5 82.0 100
MAP2K6 MEK6 100.0 100
MELK MELK 100.0 100
MERTK MERTK 100.0 100
MET MET(Y1235D) 86.0 100
MINK1 MINK 94.0 100
MAP2K7 MKK7 97.0 100
MKNK1 MKNK1 75.0 100
MKNK2 MKNK2 92.0 100
MYLK3 MLCK 89.0 100
MAP3K9 MLK1 100.0 100
MAP3K10 MLK2 70.0 100
MAP3K11 MLK3 88.0 100
CDC42BPA MRCKA 100.0 100
CDC42BPB MRCKB 88.0 100
STK4 MST1 100.0 100
MST1R MST1R 100.0 100
STK3 MST2 96.0 100
STK24 MST3 92.0 100
STK26 MST4 81.0 100
MTOR MTOR 100.0 100
MUSK MUSK 64.0 100
MYLK MYLK 100.0 100
MYLK2 MYLK2 89.0 100
MYLK4 MYLK4 100.0 100
MYO3A MYO3A 100.0 100
MYO3B MYO3B 84.0 100
STK38 NDR1 95.0 100
STK38L NDR2 72.0 100
NEK1 NEK1 100.0 100
NEK10 NEK10 90.0 100
NEK11 NEK11 77.0 100
NEK2 NEK2 99.0 100
NEK3 NEK3 88.0 100
NEK4 NEK4 81.0 100
NEK5 NEK5 100.0 100
NEK6 NEK6 95.0 100
NEK7 NEK7 100.0 100
NEK9 NEK9 98.0 100
MAP3K14 NIK 58.0 100
NIM1K NIM1 79.0 100
NLK NLK 86.0 100
OXSR1 OSR1 100.0 100
MAPK14 p38-alpha 100.0 100
MAPK11 p38-beta 98.0 100
MAPK13 p38-delta 100.0 100
MAPK12 p38-gamma 77.0 100
PAK1 PAK1 92.0 100
PAK2 PAK2 100.0 100
PAK3 PAK3 77.0 100
PAK4 PAK4 100.0 100
PAK6 PAK6 99.0 100
PAK5 PAK7 95.0 100
CDK16 PCTK1 75.0 100
CDK17 PCTK2 100.0 100
CDK18 PCTK3 100.0 100
PDGFRA PDGFRA 86.0 100
PDGFRB PDGFRB 86.0 100
PDPK1 PDPK1 92.0 100
CDPK1 PFCDPK1(P.falciparum) 100.0 100
PK5 PFPK5(P.falciparum) 65.0 100
CDK15 PFTAIRE2 93.0 100
CDK14 PFTK1 100.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 100.0 100
PIK3C2B PIK3C2B 93.0 100
PIK3C2G PIK3C2G 100.0 100
PIK3CA PIK3CA(Q546K) 95.0 100
PIK3CB PIK3CB 88.0 100
PIK3CD PIK3CD 65.0 100
PIK3CG PIK3CG 90.0 100
PI4KB PIK4CB 79.0 100
PIKFYVE PIKFYVE 100.0 100
PIM1 PIM1 95.0 100
PIM2 PIM2 96.0 100
PIM3 PIM3 99.0 100
PIP5K1A PIP5K1A 100.0 100
PIP5K1C PIP5K1C 100.0 100
PIP4K2B PIP5K2B 100.0 100
PIP4K2C PIP5K2C 95.0 100
PRKACA PKAC-alpha 85.0 100
PRKACB PKAC-beta 86.0 100
PKMYT1 PKMYT1 100.0 100
PKN1 PKN1 100.0 100
PKN2 PKN2 86.0 100
PKNB PKNB(M.tuberculosis) 100.0 100
PLK1 PLK1 90.0 100
PLK2 PLK2 80.0 100
PLK3 PLK3 70.0 100
PLK4 PLK4 82.0 100
PRKCD PRKCD 90.0 100
PRKCE PRKCE 90.0 100
PRKCH PRKCH 87.0 100
PRKCI PRKCI 87.0 100
PRKCQ PRKCQ 97.0 100
PRKD1 PRKD1 75.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 100.0 100
PRKG1 PRKG1 91.0 100
PRKG2 PRKG2 93.0 100
EIF2AK2 PRKR 100.0 100
PRKX PRKX 100.0 100
PRPF4B PRP4 89.0 100
PTK2B PYK2 100.0 100
SIK3 QSK 100.0 100
RAF1 RAF1 100.0 100
RET RET(V804M) 76.0 100
RIOK1 RIOK1 96.0 100
RIOK2 RIOK2 100.0 100
RIOK3 RIOK3 100.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 82.0 100
DSTYK RIPK5 69.0 100
ROCK1 ROCK1 78.0 100
ROCK2 ROCK2 85.0 100
ROS1 ROS1 97.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 86.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 84.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 80.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 84.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 93.0 100
RPS6KB1 S6K1 88.0 100
SBK1 SBK1 90.0 100
SGK1 SGK 100.0 100
SBK3 SgK110 87.0 100
SGK2 SGK2 100.0 100
SGK3 SGK3 82.0 100
SIK1 SIK 97.0 100
SIK2 SIK2 100.0 100
SLK SLK 98.0 100
NUAK2 SNARK 85.0 100
SNRK SNRK 80.0 100
SRC SRC 93.0 100
SRMS SRMS 90.0 100
SRPK1 SRPK1 75.0 100
SRPK2 SRPK2 100.0 100
SRPK3 SRPK3 100.0 100
STK16 STK16 78.0 100
STK33 STK33 100.0 100
STK35 STK35 94.0 100
STK36 STK36 97.0 100
STK39 STK39 85.0 100
SYK SYK 100.0 100
MAP3K7 TAK1 80.0 100
TAOK1 TAOK1 90.0 100
TAOK2 TAOK2 90.0 100
TAOK3 TAOK3 85.0 100
TBK1 TBK1 84.0 100
TEC TEC 99.0 100
TESK1 TESK1 97.0 100
TGFBR1 TGFBR1 100.0 100
TGFBR2 TGFBR2 66.0 100
TIE1 TIE1 76.0 100
TEK TIE2 83.0 100
TLK1 TLK1 83.0 100
TLK2 TLK2 93.0 100
TNIK TNIK 100.0 100
TNK1 TNK1 88.0 100
TNK2 TNK2 100.0 100
TNNI3K TNNI3K 100.0 100
NTRK1 TRKA 89.0 100
NTRK2 TRKB 91.0 100
NTRK3 TRKC 94.0 100
TRPM6 TRPM6 95.0 100
TSSK1B TSSK1B 100.0 100
TSSK3 TSSK3 91.0 100
TTK TTK 93.0 100
TXK TXK 90.0 100
TYK2 TYK2(JH2domain-pseudokinase) 91.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 87.0 100
ULK2 ULK2 78.0 100
ULK3 ULK3 100.0 100
KDR VEGFR2 81.0 100
PIK3C3 VPS34 80.0 100
VRK2 VRK2 98.0 100
WEE1 WEE1 90.0 100
WEE2 WEE2 100.0 100
WNK1 WNK1 93.0 100
WNK2 WNK2 85.0 100
WNK3 WNK3 96.0 100
WNK4 WNK4 97.0 100
STK32A YANK1 75.0 100
STK32B YANK2 92.0 100
STK32C YANK3 100.0 100
YES1 YES 100.0 100
STK25 YSK1 100.0 100
MAP3K19 YSK4 75.0 100
MAP3K20 ZAK 87.0 100
ZAP70 ZAP70 98.0 100

BI-4395


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 90.0 100
ABL1 ABL1-phosphorylated 62.0 100
ABL2 ABL2 93.0 100
ACVR1 ACVR1 99.0 100
ACVR1B ACVR1B 83.0 100
ACVR2A ACVR2A 98.0 100
ACVR2B ACVR2B 100.0 100
ACVRL1 ACVRL1 97.0 100
COQ8A ADCK3 100.0 100
COQ8B ADCK4 100.0 100
AKT1 AKT1 100.0 100
AKT2 AKT2 96.0 100
AKT3 AKT3 88.0 100
ALK ALK(L1196M) 100.0 100
PRKAA1 AMPK-alpha1 81.0 100
PRKAA2 AMPK-alpha2 91.0 100
ANKK1 ANKK1 100.0 100
NUAK1 ARK5 70.0 100
MAP3K5 ASK1 86.0 100
MAP3K6 ASK2 88.0 100
AURKA AURKA 100.0 100
AURKB AURKB 92.0 100
AURKC AURKC 76.0 100
AXL AXL 89.0 100
BMP2K BIKE 82.0 100
BLK BLK 100.0 100
BMPR1A BMPR1A 94.0 100
BMPR1B BMPR1B 88.0 100
BMPR2 BMPR2 83.0 100
BMX BMX 98.0 100
BRAF BRAF(V600E) 89.0 100
PTK6 BRK 89.0 100
BRSK1 BRSK1 86.0 100
BRSK2 BRSK2 100.0 100
BTK BTK 77.0 100
BUB1 BUB1 83.0 100
CAMK1 CAMK1 95.0 100
PNCK CAMK1B 100.0 100
CAMK1D CAMK1D 95.0 100
CAMK1G CAMK1G 89.0 100
CAMK2A CAMK2A 79.0 100
CAMK2B CAMK2B 91.0 100
CAMK2D CAMK2D 83.0 100
CAMK2G CAMK2G 83.0 100
CAMK4 CAMK4 92.0 100
CAMKK1 CAMKK1 85.0 100
CAMKK2 CAMKK2 80.0 100
CASK CASK 69.0 100
CDK11B CDC2L1 93.0 100
CDK11A CDC2L2 96.0 100
CDK13 CDC2L5 72.0 100
CDK19 CDK11 100.0 100
CDK2 CDK2 91.0 100
CDK3 CDK3 88.0 100
CDK4 CDK4-cyclinD3 88.0 100
CDK5 CDK5 90.0 100
CDK7 CDK7 100.0 100
CDK8 CDK8 100.0 100
CDK9 CDK9 82.0 100
CDKL1 CDKL1 70.0 100
CDKL2 CDKL2 78.0 100
CDKL3 CDKL3 100.0 100
CDKL5 CDKL5 85.0 100
CHEK1 CHEK1 83.0 100
CHEK2 CHEK2 100.0 100
CIT CIT 59.0 100
CLK1 CLK1 80.0 100
CLK2 CLK2 100.0 100
CLK3 CLK3 95.0 100
CLK4 CLK4 69.0 100
CSF1R CSF1R-autoinhibited 98.0 100
CSK CSK 94.0 100
CSNK1A1 CSNK1A1 81.0 100
CSNK1A1L CSNK1A1L 94.0 100
CSNK1D CSNK1D 84.0 100
CSNK1E CSNK1E 80.0 100
CSNK1G1 CSNK1G1 91.0 100
CSNK1G2 CSNK1G2 90.0 100
CSNK1G3 CSNK1G3 94.0 100
CSNK2A1 CSNK2A1 68.0 100
CSNK2A2 CSNK2A2 100.0 100
MATK CTK 86.0 100
DAPK1 DAPK1 97.0 100
DAPK2 DAPK2 96.0 100
DAPK3 DAPK3 86.0 100
DCLK1 DCAMKL1 88.0 100
DCLK2 DCAMKL2 92.0 100
DCLK3 DCAMKL3 96.0 100
DDR1 DDR1 89.0 100
DDR2 DDR2 75.0 100
MAP3K12 DLK 100.0 100
DMPK DMPK 76.0 100
CDC42BPG DMPK2 100.0 100
STK17A DRAK1 92.0 100
STK17B DRAK2 91.0 100
DYRK1A DYRK1A 98.0 100
DYRK1B DYRK1B 100.0 100
DYRK2 DYRK2 100.0 100
EGFR EGFR(T790M) 100.0 100
EIF2AK1 EIF2AK1 90.0 100
EPHA1 EPHA1 95.0 100
EPHA2 EPHA2 95.0 100
EPHA3 EPHA3 89.0 100
EPHA4 EPHA4 100.0 100
EPHA5 EPHA5 92.0 100
EPHA6 EPHA6 100.0 100
EPHA7 EPHA7 82.0 100
EPHA8 EPHA8 92.0 100
EPHB1 EPHB1 87.0 100
EPHB2 EPHB2 100.0 100
EPHB3 EPHB3 100.0 100
EPHB4 EPHB4 100.0 100
EPHB6 EPHB6 96.0 100
ERBB2 ERBB2 92.0 100
ERBB3 ERBB3 77.0 100
ERBB4 ERBB4 98.0 100
MAPK3 ERK1 94.0 100
MAPK1 ERK2 94.0 100
MAPK6 ERK3 100.0 100
MAPK4 ERK4 89.0 100
MAPK7 ERK5 87.0 100
MAPK15 ERK8 98.0 100
ERN1 ERN1 83.0 100
PTK2 FAK 85.0 100
FER FER 93.0 100
FES FES 95.0 100
FGFR1 FGFR1 84.0 100
FGFR2 FGFR2 87.0 100
FGFR3 FGFR3(G697C) 82.0 100
FGFR4 FGFR4 100.0 100
FGR FGR 87.0 100
FLT1 FLT1 89.0 100
FLT3 FLT3-autoinhibited 95.0 100
FLT4 FLT4 43.0 100
FRK FRK 100.0 100
FYN FYN 98.0 100
GAK GAK 90.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 94.0 100
GRK1 GRK1 100.0 100
GRK2 GRK2 98.0 100
GRK3 GRK3 81.0 100
GRK4 GRK4 96.0 100
GRK7 GRK7 100.0 100
GSK3A GSK3A 61.0 100
GSK3B GSK3B 78.0 100
HASPIN HASPIN 77.0 100
HCK HCK 81.0 100
HIPK1 HIPK1 85.0 100
HIPK2 HIPK2 97.0 100
HIPK3 HIPK3 88.0 100
HIPK4 HIPK4 100.0 100
MAP4K1 HPK1 97.0 100
HUNK HUNK 65.0 100
CILK1 ICK 72.0 100
IGF1R IGF1R 91.0 100
CHUK IKK-alpha 90.0 100
IKBKB IKK-beta 93.0 100
IKBKE IKK-epsilon 100.0 100
INSR INSR 100.0 100
INSRR INSRR 98.0 100
IRAK1 IRAK1 93.0 100
IRAK3 IRAK3 83.0 100
IRAK4 IRAK4 71.0 100
ITK ITK 85.0 100
JAK1 JAK1(JH2domain-pseudokinase) 84.0 100
JAK2 JAK2(JH1domain-catalytic) 90.0 100
JAK3 JAK3(JH1domain-catalytic) 65.0 100
MAPK8 JNK1 88.0 100
MAPK9 JNK2 60.0 100
MAPK10 JNK3 76.0 100
KIT KIT-autoinhibited 90.0 100
LATS1 LATS1 100.0 100
LATS2 LATS2 100.0 100
LCK LCK 75.0 100
LIMK1 LIMK1 100.0 100
LIMK2 LIMK2 100.0 100
STK11 LKB1 100.0 100
STK10 LOK 80.0 100
LRRK2 LRRK2(G2019S) 70.0 100
LTK LTK 81.0 100
LYN LYN 100.0 100
MAP3K13 LZK 78.0 100
MAK MAK 92.0 100
MAP3K1 MAP3K1 65.0 100
MAP3K15 MAP3K15 91.0 100
MAP3K2 MAP3K2 75.0 100
MAP3K3 MAP3K3 78.0 100
MAP3K4 MAP3K4 86.0 100
MAP4K2 MAP4K2 85.0 100
MAP4K3 MAP4K3 97.0 100
MAP4K4 MAP4K4 92.0 100
MAP4K5 MAP4K5 96.0 100
MAPKAPK2 MAPKAPK2 55.0 100
MAPKAPK5 MAPKAPK5 89.0 100
MARK1 MARK1 100.0 100
MARK2 MARK2 100.0 100
MARK3 MARK3 81.0 100
MARK4 MARK4 100.0 100
MAST1 MAST1 100.0 100
MAP2K1 MEK1 91.0 100
MAP2K2 MEK2 85.0 100
MAP2K3 MEK3 93.0 100
MAP2K4 MEK4 79.0 100
MAP2K5 MEK5 63.0 100
MAP2K6 MEK6 100.0 100
MELK MELK 86.0 100
MERTK MERTK 40.0 100
MET MET(Y1235D) 100.0 100
MINK1 MINK 95.0 100
MAP2K7 MKK7 95.0 100
MKNK1 MKNK1 100.0 100
MKNK2 MKNK2 96.0 100
MYLK3 MLCK 100.0 100
MAP3K9 MLK1 100.0 100
MAP3K10 MLK2 100.0 100
MAP3K11 MLK3 87.0 100
CDC42BPA MRCKA 79.0 100
CDC42BPB MRCKB 100.0 100
STK4 MST1 80.0 100
MST1R MST1R 100.0 100
STK3 MST2 91.0 100
STK24 MST3 97.0 100
STK26 MST4 95.0 100
MTOR MTOR 31.0 100
MUSK MUSK 95.0 100
MYLK MYLK 62.0 100
MYLK2 MYLK2 83.0 100
MYLK4 MYLK4 76.0 100
MYO3A MYO3A 95.0 100
MYO3B MYO3B 100.0 100
STK38 NDR1 92.0 100
STK38L NDR2 99.0 100
NEK1 NEK1 100.0 100
NEK10 NEK10 58.0 100
NEK11 NEK11 83.0 100
NEK2 NEK2 95.0 100
NEK3 NEK3 100.0 100
NEK4 NEK4 84.0 100
NEK5 NEK5 48.0 100
NEK6 NEK6 91.0 100
NEK7 NEK7 98.0 100
NEK9 NEK9 99.0 100
MAP3K14 NIK 85.0 100
NIM1K NIM1 78.0 100
NLK NLK 100.0 100
OXSR1 OSR1 88.0 100
MAPK14 p38-alpha 100.0 100
MAPK11 p38-beta 86.0 100
MAPK13 p38-delta 91.0 100
MAPK12 p38-gamma 90.0 100
PAK1 PAK1 86.0 100
PAK2 PAK2 23.0 100
PAK3 PAK3 82.0 100
PAK4 PAK4 86.0 100
PAK6 PAK6 96.0 100
PAK5 PAK7 62.0 100
CDK16 PCTK1 93.0 100
CDK17 PCTK2 77.0 100
CDK18 PCTK3 97.0 100
PDGFRA PDGFRA 100.0 100
PDGFRB PDGFRB 96.0 100
PDPK1 PDPK1 100.0 100
CDPK1 PFCDPK1(P.falciparum) 73.0 100
PK5 PFPK5(P.falciparum) 74.0 100
CDK15 PFTAIRE2 95.0 100
CDK14 PFTK1 100.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 86.0 100
PIK3C2B PIK3C2B 78.0 100
PIK3C2G PIK3C2G 100.0 100
PIK3CA PIK3CA(Q546K) 76.0 100
PIK3CB PIK3CB 82.0 100
PIK3CD PIK3CD 97.0 100
PIK3CG PIK3CG 64.0 100
PI4KB PIK4CB 70.0 100
PIKFYVE PIKFYVE 100.0 100
PIM1 PIM1 91.0 100
PIM2 PIM2 81.0 100
PIM3 PIM3 91.0 100
PIP5K1A PIP5K1A 63.0 100
PIP5K1C PIP5K1C 91.0 100
PIP4K2B PIP5K2B 93.0 100
PIP4K2C PIP5K2C 63.0 100
PRKACA PKAC-alpha 100.0 100
PRKACB PKAC-beta 98.0 100
PKMYT1 PKMYT1 93.0 100
PKN1 PKN1 90.0 100
PKN2 PKN2 100.0 100
PKNB PKNB(M.tuberculosis) 76.0 100
PLK1 PLK1 95.0 100
PLK2 PLK2 100.0 100
PLK3 PLK3 94.0 100
PLK4 PLK4 61.0 100
PRKCD PRKCD 89.0 100
PRKCE PRKCE 64.0 100
PRKCH PRKCH 84.0 100
PRKCI PRKCI 80.0 100
PRKCQ PRKCQ 99.0 100
PRKD1 PRKD1 95.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 89.0 100
PRKG1 PRKG1 100.0 100
PRKG2 PRKG2 78.0 100
EIF2AK2 PRKR 84.0 100
PRKX PRKX 71.0 100
PRPF4B PRP4 100.0 100
PTK2B PYK2 96.0 100
SIK3 QSK 94.0 100
RAF1 RAF1 70.0 100
RET RET(V804M) 91.0 100
RIOK1 RIOK1 76.0 100
RIOK2 RIOK2 100.0 100
RIOK3 RIOK3 83.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 68.0 100
DSTYK RIPK5 96.0 100
ROCK1 ROCK1 93.0 100
ROCK2 ROCK2 82.0 100
ROS1 ROS1 74.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 81.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 95.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 70.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 98.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 85.0 100
RPS6KB1 S6K1 91.0 100
SBK1 SBK1 77.0 100
SGK1 SGK 88.0 100
SBK3 SgK110 79.0 100
SGK2 SGK2 54.0 100
SGK3 SGK3 96.0 100
SIK1 SIK 100.0 100
SIK2 SIK2 90.0 100
SLK SLK 65.0 100
NUAK2 SNARK 87.0 100
SNRK SNRK 92.0 100
SRC SRC 100.0 100
SRMS SRMS 81.0 100
SRPK1 SRPK1 33.0 100
SRPK2 SRPK2 85.0 100
SRPK3 SRPK3 100.0 100
STK16 STK16 86.0 100
STK33 STK33 87.0 100
STK35 STK35 94.0 100
STK36 STK36 93.0 100
STK39 STK39 90.0 100
SYK SYK 81.0 100
MAP3K7 TAK1 95.0 100
TAOK1 TAOK1 91.0 100
TAOK2 TAOK2 82.0 100
TAOK3 TAOK3 83.0 100
TBK1 TBK1 77.0 100
TEC TEC 89.0 100
TESK1 TESK1 92.0 100
TGFBR1 TGFBR1 97.0 100
TGFBR2 TGFBR2 100.0 100
TIE1 TIE1 93.0 100
TEK TIE2 82.0 100
TLK1 TLK1 100.0 100
TLK2 TLK2 89.0 100
TNIK TNIK 97.0 100
TNK1 TNK1 100.0 100
TNK2 TNK2 100.0 100
TNNI3K TNNI3K 100.0 100
NTRK1 TRKA 74.0 100
NTRK2 TRKB 92.0 100
NTRK3 TRKC 89.0 100
TRPM6 TRPM6 79.0 100
TSSK1B TSSK1B 100.0 100
TSSK3 TSSK3 97.0 100
TTK TTK 88.0 100
TXK TXK 90.0 100
TYK2 TYK2(JH2domain-pseudokinase) 94.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 83.0 100
ULK2 ULK2 98.0 100
ULK3 ULK3 99.0 100
KDR VEGFR2 85.0 100
PIK3C3 VPS34 93.0 100
VRK2 VRK2 91.0 100
WEE1 WEE1 100.0 100
WEE2 WEE2 91.0 100
WNK1 WNK1 100.0 100
WNK2 WNK2 70.0 100
WNK3 WNK3 67.0 100
WNK4 WNK4 100.0 100
STK32A YANK1 92.0 100
STK32B YANK2 100.0 100
STK32C YANK3 100.0 100
YES1 YES 84.0 100
STK25 YSK1 91.0 100
MAP3K19 YSK4 85.0 100
MAP3K20 ZAK 80.0 100
ZAP70 ZAP70 82.0 100

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BI-4394

Conclusion: Closest hits at 10 µM are MAPKAPK2 with 99 % inhibition, RPS6KA3 with 95 % inhibition, GSK3B and MAPK14 with 94 % inhibition.

Target protein HGNC name Species % control at 10 µM Assay
KIT KIT Homo sapiens 77.0
ABL1 ABL1 Homo sapiens 48.0
ACVR1B ACVR1B Homo sapiens 100.0
AKT1 AKT1 Homo sapiens 24.0
AMPK A1B1G1 PRKAA1
 PRKAB1
 PRKAG1
 		Homo sapiens 8.0
BTK BTK Homo sapiens 68.0
CDK1/CYCLINB CDK1 Homo sapiens 88.0
CDK2/CYCLINA CDK2 Homo sapiens 93.0
CHEK1 CHEK1 Homo sapiens 94.0
CSNK1G2 CSNK1G2 Homo sapiens 61.0
CSNK2A1 CSNK2A1 Homo sapiens 89.0
DYRK3 DYRK3 Homo sapiens 28.0
EGFR EGFR Homo sapiens 99.0
EPHA2 EPHA2 Homo sapiens 85.0
ERBB2 ERBB2 Homo sapiens 87.0
FGFR1 FGFR1 Homo sapiens 94.0
FLT3 FLT3 Homo sapiens 64.0
FRAP1 (MTOR) MTOR Homo sapiens 78.0
GSK3B GSK3B Homo sapiens 6.0
IGF1R IGF1R Homo sapiens 88.0
IKBKB IKBKB Homo sapiens 48.0
INSR INSR Homo sapiens 98.0
IRAK4 IRAK4 Homo sapiens 121.0
JAK3 JAK3 Homo sapiens 44.0
KDR KDR Homo sapiens 17.0
LCK LCK Homo sapiens 68.0
MAP2K1 MAP2K1 Homo sapiens 78.0
MAP3K9 MAP3K9 Homo sapiens 93.0
MAP4K4 MAP4K4 Homo sapiens 32.0
MAPK1 MAPK1 Homo sapiens 84.0
MAPK14 MAPK14 Homo sapiens 6.0
MAPK8 MAPK8 Homo sapiens 87.0
MAPKAPK2 MAPKAPK2 Homo sapiens 1.0
MARK2 MARK2 Homo sapiens 107.0
MET MET Homo sapiens 43.0
NEK1 NEK1 Homo sapiens 49.0
NTRK1 NTRK1 Homo sapiens 190.0
PAK4 PAK4 Homo sapiens 75.0
PDGFRB PDGFRB Homo sapiens 96.0
PHKG2 PHKG2 Homo sapiens 82.0
PIK3CAPIK3R1 PIK3CA
 PIK3R1
 		Homo sapiens 133.0 Adapta
PIM1 PIM1 Homo sapiens 14.0
PLK1 PLK1 Homo sapiens 73.0
PRKACA PRKACA Homo sapiens 10.0
PRKCB1 PRKCB Homo sapiens 97.0
PRKCE PRKCE Homo sapiens 115.0
RET RET Homo sapiens 64.0
ROCK1 ROCK1 Homo sapiens 97.0
ROCK2 ROCK2 Homo sapiens 56.0
RPS6KA3 RPS6KA3 Homo sapiens 5.0
RPS6KB1 RPS6KB1 Homo sapiens 89.0
SRC SRC Homo sapiens 25.0
STK6 AURKA Homo sapiens -1.0 Z´-LYTE
SYK SYK Homo sapiens 56.0
TEK TEK Homo sapiens 85.0
ZAP70 ZAP70 Homo sapiens 100.0