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Selectivity data for probe A-079 and control A-226


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A-079


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta2 ADRB2 6.61
GABAA 14.65
M3 CHRM3 -6.83
M4 CHRM4 18.21
5-HT1A HTR1A 6.81
5-HT1B HTR1B 7.88
5-HT1D HTR1D 13.86
5-HT1E HTR1E 6.66
5-HT5A HTR5A 3.01
5-HT6 HTR6 15.60
D2 DRD2 -8.66
D3 DRD3 14.50
Sigma 1 SIGMAR1 83.99 505.48 average (n=2) 6.34
Sigma 2 TMEM97 22.65
D1 DRD1 13.44
5-HT2B HTR2B 24.66
5-HT2C HTR2C 32.73
5-HT3 HTR3A -4.62
5-HT7A HTR7 8.18
Alpha2A ADRA2A 5.31
Alpha2B ADRA2B 15.12
Alpha2C ADRA2C 8.29
DAT SLC6A3 -15.06
DOR OPRD1 -7.17
H1 HRH1 9.24
H3 HRH3 4.32
KOR OPRK1 15.67
M1 CHRM1 15.25
M2 CHRM2 9.31
M5 CHRM5 6.68
MOR OPRM1 -5.90
NET SLC6A2 -2.32
GABA/PBR 11.89
SERT SLC6A4 13.02
5-HT2A HTR2A 21.73
H2 HRH2 0.46
H4 HRH4 9.43
Beta1 ADRB1 -23.77
Beta3 ADRB3 -0.54
D4 DRD4 19.54
Alpha1A ADRA1A -9.69
Alpha1B ADRA1B 3.80
Alpha1D ADRA1D -4.38
D5 DRD5 12.19
GABAA/BZP 21.46

A-226


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 1.12
5-HT1B HTR1B -1.04
5-HT1D HTR1D 4.54
5-HT1E HTR1E 4.47
5-HT5A HTR5A -3.24
5-HT6 HTR6 -3.93
D2 DRD2 -6.57
D3 DRD3 8.60
Sigma 1 SIGMAR1 86.81 528.76 average (n=2) 6.30
Sigma 2 TMEM97 33.37
D1 DRD1 -0.91
5-HT2B HTR2B 43.76
5-HT2C HTR2C 26.96
5-HT3 HTR3A 0.44
5-HT7A HTR7 -0.42
Alpha2A ADRA2A 2.82
Alpha2B ADRA2B 33.10
Alpha2C ADRA2C 15.65
DAT SLC6A3 -18.86
DOR OPRD1 2.53
H1 HRH1 15.25
H3 HRH3 -0.30
KOR OPRK1 8.60
M1 CHRM1 -2.46
M2 CHRM2 14.28
M5 CHRM5 2.77
MOR OPRM1 -1.52
GABA/PBR 50.59 3690.01 average (n=2) 5.44
SERT SLC6A4 8.28
NET SLC6A2 -0.42
5-HT2A HTR2A 40.80
H2 HRH2 -11.21
H4 HRH4 10.76
Beta1 ADRB1 10.15
Beta3 ADRB3 11.05
D4 DRD4 18.59
Alpha1A ADRA1A -8.35
Alpha1B ADRA1B 0.56
Alpha1D ADRA1D -3.74
D5 DRD5 11.78
M3 CHRM3 -5.75
M4 CHRM4 15.37
Beta2 ADRB2 -1.29
GABAA 16.70
GABAA/BZP 20.29

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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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A-079


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 89.0 1000
ABL1 ABL1-phosphorylated 66.0 1000
ABL2 ABL2 82.0 1000
ACVR1 ACVR1 80.0 1000
ACVR1B ACVR1B 77.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 91.0 1000
ACVRL1 ACVRL1 76.0 1000
COQ8A ADCK3 78.0 1000
COQ8B ADCK4 84.0 1000
AKT1 AKT1 82.0 1000
AKT2 AKT2 88.0 1000
AKT3 AKT3 83.0 1000
ALK ALK(L1196M) 71.0 1000
PRKAA1 AMPK-alpha1 99.0 1000
PRKAA2 AMPK-alpha2 88.0 1000
ANKK1 ANKK1 79.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 93.0 1000
MAP3K6 ASK2 63.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 68.0 1000
AURKC AURKC 80.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 80.0 1000
BLK BLK 87.0 1000
BMPR1A BMPR1A 86.0 1000
BMPR1B BMPR1B 87.0 1000
BMPR2 BMPR2 81.0 1000
BMX BMX 83.0 1000
BRAF BRAF(V600E) 77.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 78.0 1000
BUB1 BUB1 88.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 82.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 97.0 1000
CAMK2A CAMK2A 81.0 1000
CAMK2B CAMK2B 97.0 1000
CAMK2D CAMK2D 99.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 69.0 1000
CAMKK1 CAMKK1 98.0 1000
CAMKK2 CAMKK2 98.0 1000
CASK CASK 70.0 1000
CDK11B CDC2L1 89.0 1000
CDK11A CDC2L2 94.0 1000
CDK13 CDC2L5 95.0 1000
CDK19 CDK11 79.0 1000
CDK2 CDK2 82.0 1000
CDK3 CDK3 84.0 1000
CDK4 CDK4-cyclinD3 74.0 1000
CDK5 CDK5 68.0 1000
CDK7 CDK7 60.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 93.0 1000
CDKL1 CDKL1 81.0 1000
CDKL2 CDKL2 92.0 1000
CDKL3 CDKL3 80.0 1000
CDKL5 CDKL5 82.0 1000
CHEK1 CHEK1 83.0 1000
CHEK2 CHEK2 85.0 1000
CIT CIT 70.0 1000
CLK1 CLK1 79.0 1000
CLK2 CLK2 78.0 1000
CLK3 CLK3 73.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 74.0 1000
CSNK1A1L CSNK1A1L 78.0 1000
CSNK1D CSNK1D 81.0 1000
CSNK1E CSNK1E 99.0 1000
CSNK1G1 CSNK1G1 99.0 1000
CSNK1G2 CSNK1G2 87.0 1000
CSNK1G3 CSNK1G3 98.0 1000
CSNK2A1 CSNK2A1 74.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 72.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 97.0 1000
DAPK3 DAPK3 87.0 1000
DCLK1 DCAMKL1 93.0 1000
DCLK2 DCAMKL2 96.0 1000
DCLK3 DCAMKL3 77.0 1000
DDR1 DDR1 89.0 1000
DDR2 DDR2 91.0 1000
MAP3K12 DLK 76.0 1000
DMPK DMPK 88.0 1000
CDC42BPG DMPK2 73.0 1000
STK17A DRAK1 98.0 1000
STK17B DRAK2 74.0 1000
DYRK1A DYRK1A 91.0 1000
DYRK1B DYRK1B 57.0 1000
DYRK2 DYRK2 94.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 82.0 1000
EPHA2 EPHA2 84.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 74.0 1000
EPHA5 EPHA5 64.0 1000
EPHA6 EPHA6 67.0 1000
EPHA7 EPHA7 86.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 76.0 1000
EPHB3 EPHB3 75.0 1000
EPHB4 EPHB4 73.0 1000
EPHB6 EPHB6 95.0 1000
ERBB2 ERBB2 83.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 66.0 1000
MAPK3 ERK1 69.0 1000
MAPK1 ERK2 71.0 1000
MAPK6 ERK3 73.0 1000
MAPK4 ERK4 75.0 1000
MAPK7 ERK5 88.0 1000
MAPK15 ERK8 95.0 1000
ERN1 ERN1 77.0 1000
PTK2 FAK 82.0 1000
FER FER 74.0 1000
FES FES 73.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 93.0 1000
FGFR3 FGFR3(G697C) 84.0 1000
FGFR4 FGFR4 96.0 1000
FGR FGR 67.0 1000
FLT1 FLT1 87.0 1000
FLT3 FLT3-autoinhibited 86.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 99.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 70.0 1000
GRK1 GRK1 79.0 1000
GRK2 GRK2 98.0 1000
GRK3 GRK3 92.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 85.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 79.0 1000
HASPIN HASPIN 65.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 80.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 78.0 1000
HIPK4 HIPK4 79.0 1000
MAP4K1 HPK1 92.0 1000
HUNK HUNK 76.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 79.0 1000
CHUK IKK-alpha 67.0 1000
IKBKB IKK-beta 83.0 1000
IKBKE IKK-epsilon 94.0 1000
INSR INSR 100.0 1000
INSRR INSRR 83.0 1000
IRAK1 IRAK1 79.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 90.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 88.0 1000
JAK2 JAK2(JH1domain-catalytic) 71.0 1000
JAK3 JAK3(JH1domain-catalytic) 80.0 1000
MAPK8 JNK1 86.0 1000
MAPK9 JNK2 92.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 80.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 82.0 1000
LIMK1 LIMK1 78.0 1000
LIMK2 LIMK2 80.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 76.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 87.0 1000
LYN LYN 87.0 1000
MAP3K13 LZK 96.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 63.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 85.0 1000
MAP3K3 MAP3K3 86.0 1000
MAP3K4 MAP3K4 99.0 1000
MAP4K2 MAP4K2 97.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 97.0 1000
MAP4K5 MAP4K5 80.0 1000
MAPKAPK2 MAPKAPK2 69.0 1000
MAPKAPK5 MAPKAPK5 91.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 86.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 71.0 1000
MAP2K1 MEK1 95.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 94.0 1000
MAP2K4 MEK4 75.0 1000
MAP2K5 MEK5 98.0 1000
MAP2K6 MEK6 98.0 1000
MELK MELK 96.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 85.0 1000
MINK1 MINK 98.0 1000
MAP2K7 MKK7 79.0 1000
MKNK1 MKNK1 56.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 86.0 1000
MAP3K9 MLK1 77.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 88.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 78.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 81.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 90.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 81.0 1000
MYLK4 MYLK4 94.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 94.0 1000
STK38L NDR2 95.0 1000
NEK1 NEK1 94.0 1000
NEK10 NEK10 95.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 83.0 1000
NEK5 NEK5 84.0 1000
NEK6 NEK6 87.0 1000
NEK7 NEK7 85.0 1000
NEK9 NEK9 79.0 1000
MAP3K14 NIK 84.0 1000
NIM1K NIM1 94.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 80.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 82.0 1000
MAPK13 p38-delta 92.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 88.0 1000
PAK2 PAK2 82.0 1000
PAK3 PAK3 89.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 86.0 1000
CDK17 PCTK2 90.0 1000
CDK18 PCTK3 89.0 1000
PDGFRA PDGFRA 78.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 87.0 1000
CDPK1 PFCDPK1(P.falciparum) 87.0 1000
PK5 PFPK5(P.falciparum) 84.0 1000
CDK15 PFTAIRE2 80.0 1000
CDK14 PFTK1 91.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 90.0 1000
PIK3C2B PIK3C2B 92.0 1000
PIK3C2G PIK3C2G 75.0 1000
PIK3CA PIK3CA(Q546K) 91.0 1000
PIK3CB PIK3CB 99.0 1000
PIK3CD PIK3CD 72.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 50.0 1000
PIKFYVE PIKFYVE 92.0 1000
PIM1 PIM1 85.0 1000
PIM2 PIM2 83.0 1000
PIM3 PIM3 96.0 1000
PIP5K1A PIP5K1A 97.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 91.0 1000
PIP4K2C PIP5K2C 83.0 1000
PRKACA PKAC-alpha 78.0 1000
PRKACB PKAC-beta 89.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 80.0 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 93.0 1000
PLK2 PLK2 78.0 1000
PLK3 PLK3 86.0 1000
PLK4 PLK4 75.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 76.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 74.0 1000
PRKCQ PRKCQ 80.0 1000
PRKD1 PRKD1 71.0 1000
PRKD2 PRKD2 99.0 1000
PRKD3 PRKD3 98.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 79.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 96.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 99.0 1000
SIK3 QSK 68.0 1000
RAF1 RAF1 91.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 80.0 1000
RIOK2 RIOK2 86.0 1000
RIOK3 RIOK3 78.0 1000
RIPK1 RIPK1 82.0 1000
RIPK2 RIPK2 91.0 1000
RIPK4 RIPK4 83.0 1000
DSTYK RIPK5 66.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 98.0 1000
ROS1 ROS1 87.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 81.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 94.0 1000
RPS6KB1 S6K1 66.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 89.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 78.0 1000
SGK3 SGK3 81.0 1000
SIK1 SIK 80.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 91.0 1000
NUAK2 SNARK 73.0 1000
SNRK SNRK 100.0 1000
SRC SRC 91.0 1000
SRMS SRMS 76.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 75.0 1000
SRPK3 SRPK3 91.0 1000
STK16 STK16 97.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 84.0 1000
STK39 STK39 94.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 81.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 94.0 1000
TAOK3 TAOK3 86.0 1000
TBK1 TBK1 75.0 1000
TEC TEC 89.0 1000
TESK1 TESK1 82.0 1000
TGFBR1 TGFBR1 85.0 1000
TGFBR2 TGFBR2 74.0 1000
TIE1 TIE1 63.0 1000
TEK TIE2 89.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 93.0 1000
TNK1 TNK1 66.0 1000
TNK2 TNK2 85.0 1000
TNNI3K TNNI3K 70.0 1000
NTRK1 TRKA 83.0 1000
NTRK2 TRKB 66.0 1000
NTRK3 TRKC 88.0 1000
TRPM6 TRPM6 64.0 1000
TSSK1B TSSK1B 82.0 1000
TSSK3 TSSK3 99.0 1000
TTK TTK 96.0 1000
TXK TXK 81.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 73.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 85.0 1000
ULK2 ULK2 46.0 1000
ULK3 ULK3 74.0 1000
KDR VEGFR2 81.0 1000
PIK3C3 VPS34 83.0 1000
VRK2 VRK2 74.0 1000
WEE1 WEE1 97.0 1000
WEE2 WEE2 83.0 1000
WNK1 WNK1 83.0 1000
WNK2 WNK2 80.0 1000
WNK3 WNK3 75.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 65.0 1000
YES1 YES 87.0 1000
STK25 YSK1 86.0 1000
MAP3K19 YSK4 66.0 1000
MAP3K20 ZAK 84.0 1000
ZAP70 ZAP70 96.0 1000

A-226


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 98.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 92.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 82.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 98.0 1000
COQ8A ADCK3 91.0 1000
COQ8B ADCK4 83.0 1000
AKT1 AKT1 98.0 1000
AKT2 AKT2 84.0 1000
AKT3 AKT3 89.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 73.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 96.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 82.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 91.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 80.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 99.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 75.0 1000
BRSK1 BRSK1 99.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 86.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 92.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 90.0 1000
CAMK4 CAMK4 87.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 88.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 95.0 1000
CDK11A CDC2L2 69.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 96.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 86.0 1000
CDK7 CDK7 93.0 1000
CDK8 CDK8 73.0 1000
CDK9 CDK9 96.0 1000
CDKL1 CDKL1 91.0 1000
CDKL2 CDKL2 81.0 1000
CDKL3 CDKL3 86.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 83.0 1000
CHEK2 CHEK2 90.0 1000
CIT CIT 70.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 88.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 97.0 1000
CSF1R CSF1R-autoinhibited 98.0 1000
CSK CSK 96.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 83.0 1000
CSNK1D CSNK1D 92.0 1000
CSNK1E CSNK1E 92.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 73.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 97.0 1000
DAPK2 DAPK2 85.0 1000
DAPK3 DAPK3 98.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 83.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 91.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 72.0 1000
CDC42BPG DMPK2 85.0 1000
STK17A DRAK1 73.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 87.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 83.0 1000
EPHA2 EPHA2 89.0 1000
EPHA3 EPHA3 99.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 79.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 92.0 1000
EPHA8 EPHA8 99.0 1000
EPHB1 EPHB1 90.0 1000
EPHB2 EPHB2 99.0 1000
EPHB3 EPHB3 96.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 91.0 1000
ERBB3 ERBB3 76.0 1000
ERBB4 ERBB4 98.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 92.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 96.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 90.0 1000
PTK2 FAK 100.0 1000
FER FER 80.0 1000
FES FES 93.0 1000
FGFR1 FGFR1 57.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 87.0 1000
FGFR4 FGFR4 83.0 1000
FGR FGR 86.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 80.0 1000
FRK FRK 80.0 1000
FYN FYN 72.0 1000
GAK GAK 96.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 50.0 1000
GRK1 GRK1 88.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 80.0 1000
HIPK1 HIPK1 97.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 91.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 91.0 1000
CILK1 ICK 97.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 95.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 94.0 1000
IRAK4 IRAK4 95.0 1000
ITK ITK 91.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 94.0 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 100.0 1000
LATS1 LATS1 89.0 1000
LATS2 LATS2 75.0 1000
LCK LCK 87.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 90.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 73.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 61.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 23.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 69.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 72.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 98.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 94.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 99.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 88.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 95.0 1000
MAP2K2 MEK2 92.0 1000
MAP2K3 MEK3 100.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 86.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 92.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 75.0 1000
MAP3K11 MLK3 79.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 69.0 1000
STK4 MST1 70.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 86.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 93.0 1000
MYLK2 MYLK2 78.0 1000
MYLK4 MYLK4 99.0 1000
MYO3A MYO3A 94.0 1000
MYO3B MYO3B 67.0 1000
STK38 NDR1 95.0 1000
STK38L NDR2 81.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 67.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 99.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 56.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 82.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 88.0 1000
PAK1 PAK1 70.0 1000
PAK2 PAK2 79.0 1000
PAK3 PAK3 63.0 1000
PAK4 PAK4 76.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 99.0 1000
CDK18 PCTK3 87.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 86.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 85.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 92.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 55.0 1000
PIK3C2G PIK3C2G 98.0 1000
PIK3CA PIK3CA(Q546K) 46.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 100.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 70.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 80.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 78.0 1000
PIP4K2B PIP5K2B 74.0 1000
PIP4K2C PIP5K2C 85.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 61.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 92.0 1000
PLK1 PLK1 82.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 100.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 98.0 1000
PRKCE PRKCE 62.0 1000
PRKCH PRKCH 68.0 1000
PRKCI PRKCI 99.0 1000
PRKCQ PRKCQ 88.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 97.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 94.0 1000
PRPF4B PRP4 85.0 1000
PTK2B PYK2 98.0 1000
SIK3 QSK 89.0 1000
RAF1 RAF1 99.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 73.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 65.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 95.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 88.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 78.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KB1 S6K1 100.0 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 96.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 93.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 98.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 97.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 84.0 1000
STK33 STK33 96.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 76.0 1000
MAP3K7 TAK1 99.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 46.0 1000
TBK1 TBK1 93.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 73.0 1000
TGFBR1 TGFBR1 88.0 1000
TGFBR2 TGFBR2 97.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 85.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 96.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 53.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 90.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 93.0 1000
TXK TXK 73.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 96.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 94.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 78.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 99.0 1000
STK32C YANK3 100.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 98.0 1000
MAP3K20 ZAK 76.0 1000
ZAP70 ZAP70 38.0 1000

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A-079

Ligand profiling has been performed at 10 µM probe concentration. Shown are supplementary data from PMID: 21402443 .

Conclusion: No significant off-target hits identified in CEREP panel.

Target protein HGNC name Species % inhibition at 10 µM
A1 ADORA1 8.0
A3 ADORA3 27.0
alpha 2 -1.0
beta 2 ADRB2 -3.0
AT2 (h) AGTR2 Homo sapiens -9.0
BZD-peripheral 6.0
B2 (h) BDKRB2 Homo sapiens 2.0
CB1 (h) CNR1 Homo sapiens 3.0
CCKB (h) CCKBR Homo sapiens 7.0
D2S (h) DRD2 Homo sapiens 4.0
D4.4 (h) DRD4 Homo sapiens 4.0
ETA (h) EDNRA Homo sapiens 5.0
GABA -3.0
GAL2 (h) GALR2 Homo sapiens -27.0
CXCR2 (h) CXCR2 Homo sapiens -1.0
CCR1 (h) CCR1 Homo sapiens 1.0
H2 (h) HRH2 Homo sapiens 3.0
MT1 (h) MTNR1A Homo sapiens 31.0
M2 (h) CHRM2 Homo sapiens 13.0
M4 (h) CHRM4 Homo sapiens 5.0
NK1 (h) TACR1 Homo sapiens -3.0
NK3 (h) TACR3 Homo sapiens 23.0
Y2 (h) NPY2R Homo sapiens 13.0
delta 2 (h) OPRD1 Homo sapiens 11.0
mu (h) (MOP) OPRM1 Homo sapiens 12.0
PACAP (h) ADCYAP1 Homo sapiens -18.0
TXA2/PGH2 TBXA2R 6.0
P2Y 7.0
5-HT1B HTR1B 14.0
5-HT2C (h) HTR2C Homo sapiens 6.0
5-HT5A (h) HTR5A Homo sapiens 4.0
5-HT7 (h) HTR7 Homo sapiens 17.0
sst -4.0
V1a (h) AVPR1A Homo sapiens -3.0
K+ channel -8.0
Na+ channel 17.0
NE transporter SLC6A2 32.0
5-HT transporter SLC6A4 -20.0
A2A (h) ADORA2A Homo sapiens 8.0
alpha1 6.0
beta1 (h) ADRB1 Homo sapiens -2.0
AT1 (h) AGTR1 Homo sapiens -1.0
BZD (central) 1.0
BB (non-select) -3.0
CGRP (h) CALCA Homo sapiens -22.0
CCKA (h) CCKAR Homo sapiens 29.0
D1 (h) DRD1 Homo sapiens 6.0
D3 (h) DRD3 Homo sapiens 14.0
D5 (h) DRD5 Homo sapiens -8.0
ETB (h) EDNRB Homo sapiens 5.0
GAL1 (h) GALR1 Homo sapiens 5.0
PDGF -6.0
TNF-alpha (h) TNF Homo sapiens 1.0
H1 (h) HRH1 Homo sapiens 4.0
MC4 (h) MC4R Homo sapiens 2.0
M1 (h) CHRM1 Homo sapiens 8.0
M3 (h) CHRM3 Homo sapiens 6.0
M5 (h) CHRM5 Homo sapiens -4.0
NK2 (h) TACR2 Homo sapiens 2.0
Y1 (h) NPY1R Homo sapiens 0.0
NT1 (h) NTSR1 Homo sapiens -5.0
kappa (guinea pig) OPRK1 Cavia porcellus -4.0
ORL1 (h) (NOP) OPRL1 Homo sapiens -5.0
PCP PRCP 2.0
P2X -2.0
5-HT1A (h) HTR1A Homo sapiens -27.0
5-HT2A (h) HTR2A Homo sapiens -1.0
5-HT3 (h) HTR3A Homo sapiens 0.0
5-HT6 (h) HTR6 Homo sapiens 0.0
sigma -2.0
VIP1 (h) VIPR1 Homo sapiens 0.0
Ca2+ channel 3.0
SK+ channel -5.0
Cl- channel 26.0
DA transporter(h) SLC6A3 Homo sapiens 43.0