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Selectivity data for probe ABT-100 and control A-108


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ABT-100


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A 10.76
5-HT1B HTR1B -4.28
5-HT1D HTR1D -0.93
5-HT1E HTR1E 1.11
5-HT2A HTR2A -0.43
5-HT2B HTR2B -5.75
5-HT2C HTR2C 0.26
5-HT3 HTR3A 17.64
5-HT5A HTR5A 1.81
5-HT6 HTR6 6.74
5-HT7A HTR7 9.15
D1 DRD1 4.35
D2 DRD2 -16.51
D3 DRD3 -9.46
D4 DRD4 -1.32
D5 DRD5 4.79
SERT SLC6A4 1.25
NET SLC6A2 21.68
DAT SLC6A3 9.99
MOR OPRM1 16.41
DOR OPRD1 -0.18
KOR OPRK1 -7.18
GABAA 6.85
H1 HRH1 88.75 > 10000.00 < 5.00
H2 HRH2 14.45
H3 HRH3 5.92
H4 HRH4 -6.36
Alpha1A ADRA1A -7.74
Alpha1B ADRA1B 16.65
Alpha2A ADRA2A 32.18
Alpha2B ADRA2B 8.46
Alpha2C ADRA2C 5.00
Beta1 ADRB1 4.25
Beta2 ADRB2 0.08
M1 CHRM1 -4.07
M2 CHRM2 -1.19
M3 CHRM3 23.29
M4 CHRM4 6.81
M5 CHRM5 -4.82
Beta3 ADRB3 32.89
GABAA/BZP 2.72
GABA/PBR -1.86
Alpha1D ADRA1D -8.65
Sigma 2 TMEM97 40.26
Sigma 1 SIGMAR1 42.52

A-108


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 -16.49
Beta3 ADRB3 -5.85
H1 HRH1 43.48
H2 HRH2 5.38
5-HT1A HTR1A -6.52
5-HT1B HTR1B 3.34
5-HT1D HTR1D 6.65
Sigma 1 SIGMAR1 92.33 91.64 average (n=2) 7.04
Sigma 2 TMEM97 37.82
5-HT1E HTR1E 7.11
5-HT2A HTR2A -4.18
5-HT2B HTR2B 18.59
5-HT2C HTR2C 17.12
5-HT3 HTR3A -0.62
5-HT5A HTR5A 0.81
5-HT6 HTR6 14.17
5-HT7A HTR7 14.98
GABAA/BZP 6.36
D1 DRD1 18.98
D2 DRD2 7.47
D3 DRD3 18.15
D4 DRD4 6.23
DAT SLC6A3 6.63
DOR OPRD1 2.40
KOR OPRK1 1.27
MOR OPRM1 -3.25
Alpha1A ADRA1A 4.51
Alpha1B ADRA1B 5.97
Alpha1D ADRA1D -18.57
Alpha2A ADRA2A 3.37
Alpha2B ADRA2B 19.97
Alpha2C ADRA2C 8.51
D5 DRD5 -12.44
M1 CHRM1 25.81
M3 CHRM3 2.79
M4 CHRM4 -9.70
M5 CHRM5 1.23
NET SLC6A2 5.18
GABA/PBR 9.56
H3 HRH3 17.82
M2 CHRM2 -11.95
SERT SLC6A4 -7.91
Beta2 ADRB2 23.12
H4 HRH4 -3.79
GABAA -12.50

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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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ABT-100


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 87.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 83.0 1000
ACVR1 ACVR1 78.0 1000
ACVR1B ACVR1B 87.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 92.0 1000
COQ8B ADCK4 72.0 1000
AKT1 AKT1 84.0 1000
AKT2 AKT2 81.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 99.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 81.0 1000
MAP3K5 ASK1 77.0 1000
MAP3K6 ASK2 76.0 1000
AURKA AURKA 95.0 1000
AURKB AURKB 100.0 1000 > 10000.0
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 97.0 1000
BLK BLK 90.0 1000
BMPR1A BMPR1A 91.0 1000
BMPR1B BMPR1B 77.0 1000
BMPR2 BMPR2 89.0 1000
BMX BMX 75.0 1000
BRAF BRAF(V600E) 82.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 73.0 1000
BRSK2 BRSK2 48.0 1000 > 10000.0
BTK BTK 92.0 1000
BUB1 BUB1 85.0 1000
CAMK1 CAMK1 99.0 1000
PNCK CAMK1B 60.0 1000 > 10000.0
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 96.0 1000
CAMK2A CAMK2A 95.0 1000
CAMK2B CAMK2B 85.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 94.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 77.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 83.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 67.0 1000
CDK19 CDK11 84.0 1000
CDK2 CDK2 95.0 1000
CDK3 CDK3 71.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 92.0 1000
CDK7 CDK7 95.0 1000 > 10000.0
CDK8 CDK8 66.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 82.0 1000
CDKL2 CDKL2 88.0 1000
CDKL3 CDKL3 87.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 97.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 77.0 1000
CLK1 CLK1 70.0 1000
CLK2 CLK2 87.0 1000
CLK3 CLK3 75.0 1000
CLK4 CLK4 94.0 1000
CSF1R CSF1R-autoinhibited 93.0 1000
CSK CSK 82.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 74.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 77.0 1000
CSNK1G1 CSNK1G1 90.0 1000
CSNK1G2 CSNK1G2 78.0 1000
CSNK1G3 CSNK1G3 71.0 1000
CSNK2A1 CSNK2A1 63.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 98.0 1000
DAPK1 DAPK1 84.0 1000
DAPK2 DAPK2 82.0 1000
DAPK3 DAPK3 88.0 1000
DCLK1 DCAMKL1 94.0 1000
DCLK2 DCAMKL2 98.0 1000
DCLK3 DCAMKL3 99.0 1000
DDR1 DDR1 97.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 98.0 1000
CDC42BPG DMPK2 85.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 64.0 1000
DYRK1A DYRK1A 81.0 1000
DYRK1B DYRK1B 58.0 1000
DYRK2 DYRK2 52.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 38.0 1000 > 10000.0
EPHA2 EPHA2 62.0 1000
EPHA3 EPHA3 90.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 97.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 91.0 1000
EPHA8 EPHA8 72.0 1000
EPHB1 EPHB1 98.0 1000
EPHB2 EPHB2 94.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 98.0 1000
EPHB6 EPHB6 95.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 87.0 1000
ERBB4 ERBB4 81.0 1000
MAPK3 ERK1 90.0 1000
MAPK1 ERK2 90.0 1000
MAPK6 ERK3 85.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 93.0 1000
MAPK15 ERK8 58.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 77.0 1000
FER FER 83.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 62.0 1000
FGFR2 FGFR2 86.0 1000
FGFR3 FGFR3(G697C) 60.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 98.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 77.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 97.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 99.0 1000
GRK1 GRK1 95.0 1000
GRK2 GRK2 74.0 1000
GRK3 GRK3 48.0 1000 > 10000.0
GRK4 GRK4 62.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 62.0 1000
GSK3B GSK3B 93.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 100.0 1000
HIPK2 HIPK2 100.0 1000 > 10000.0
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 86.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 68.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 92.0 1000
CHUK IKK-alpha 86.0 1000
IKBKB IKK-beta 87.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 100.0 1000
INSRR INSRR 93.0 1000
IRAK1 IRAK1 83.0 1000
IRAK3 IRAK3 71.0 1000
IRAK4 IRAK4 75.0 1000
ITK ITK 91.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 70.0 1000
JAK2 JAK2(JH1domain-catalytic) 91.0 1000
JAK3 JAK3(JH1domain-catalytic) 72.0 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 89.0 1000
MAPK10 JNK3 70.0 1000
KIT KIT-autoinhibited 95.0 1000
LATS1 LATS1 87.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 82.0 1000
LIMK1 LIMK1 89.0 1000
LIMK2 LIMK2 72.0 1000
STK11 LKB1 71.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 92.0 1000
LTK LTK 91.0 1000
LYN LYN 90.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 90.0 1000
MAP3K15 MAP3K15 90.0 1000
MAP3K2 MAP3K2 77.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 90.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 63.0 1000
MAPKAPK5 MAPKAPK5 90.0 1000
MARK1 MARK1 57.0 1000
MARK2 MARK2 95.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 56.0 1000
MAST1 MAST1 92.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 94.0 1000
MAP2K3 MEK3 78.0 1000
MAP2K4 MEK4 89.0 1000
MAP2K5 MEK5 83.0 1000
MAP2K6 MEK6 76.0 1000
MELK MELK 74.0 1000
MERTK MERTK 84.0 1000
MET MET(Y1235D) 78.0 1000
MINK1 MINK 94.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 68.0 1000
MKNK2 MKNK2 85.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 81.0 1000
MAP3K10 MLK2 55.0 1000
MAP3K11 MLK3 86.0 1000
CDC42BPA MRCKA 78.0 1000
CDC42BPB MRCKB 76.0 1000
STK4 MST1 86.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 77.0 1000
STK24 MST3 90.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 57.0 1000
MUSK MUSK 93.0 1000
MYLK MYLK 88.0 1000
MYLK2 MYLK2 78.0 1000
MYLK4 MYLK4 93.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 71.0 1000
STK38 NDR1 75.0 1000
STK38L NDR2 65.0 1000
NEK1 NEK1 80.0 1000
NEK10 NEK10 83.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 96.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 72.0 1000
NEK6 NEK6 95.0 1000
NEK7 NEK7 46.0 1000 > 10000.0
NEK9 NEK9 72.0 1000
MAP3K14 NIK 88.0 1000
NIM1K NIM1 87.0 1000
NLK NLK 89.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 90.0 1000
MAPK13 p38-delta 87.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 93.0 1000
PAK3 PAK3 96.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 98.0 1000
PAK5 PAK7 94.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 90.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 87.0 1000
CDPK1 PFCDPK1(P.falciparum) 88.0 1000
PK5 PFPK5(P.falciparum) 77.0 1000
CDK15 PFTAIRE2 59.0 1000
CDK14 PFTK1 86.0 1000
PHKG1 PHKG1 63.0 1000
PHKG2 PHKG2 92.0 1000
PIK3C2B PIK3C2B 89.0 1000
PIK3C2G PIK3C2G 81.0 1000
PIK3CA PIK3CA(Q546K) 82.0 1000
PIK3CB PIK3CB 96.0 1000
PIK3CD PIK3CD 79.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 94.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 96.0 1000
PIM2 PIM2 84.0 1000
PIM3 PIM3 89.0 1000
PIP5K1A PIP5K1A 91.0 1000
PIP5K1C PIP5K1C 93.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 87.0 1000
PRKACA PKAC-alpha 81.0 1000
PRKACB PKAC-beta 93.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 97.0 1000
PLK1 PLK1 77.0 1000
PLK2 PLK2 94.0 1000
PLK3 PLK3 89.0 1000
PLK4 PLK4 94.0 1000
PRKCD PRKCD 66.0 1000
PRKCE PRKCE 79.0 1000
PRKCH PRKCH 94.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 79.0 1000
PRKD1 PRKD1 99.0 1000
PRKD2 PRKD2 84.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 91.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 87.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 62.0 1000
SIK3 QSK 67.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 99.0 1000
RIOK1 RIOK1 72.0 1000
RIOK2 RIOK2 83.0 1000
RIOK3 RIOK3 95.0 1000
RIPK1 RIPK1 79.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 90.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 94.0 1000
ROS1 ROS1 89.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 76.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 76.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 87.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 85.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 93.0 1000
RPS6KB1 S6K1 96.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 76.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 95.0 1000
SIK2 SIK2 95.0 1000
SLK SLK 90.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 81.0 1000
SRMS SRMS 79.0 1000
SRPK1 SRPK1 70.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 53.0 1000
STK16 STK16 99.0 1000
STK33 STK33 74.0 1000
STK35 STK35 100.0 1000
STK36 STK36 80.0 1000
STK39 STK39 50.0 1000
SYK SYK 95.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 87.0 1000
TAOK2 TAOK2 98.0 1000
TAOK3 TAOK3 87.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 93.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 81.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 85.0 1000
TEK TIE2 92.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 81.0 1000
TNK1 TNK1 56.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 82.0 1000
NTRK1 TRKA 91.0 1000
NTRK2 TRKB 92.0 1000
NTRK3 TRKC 80.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 98.0 1000
TTK TTK 100.0 1000
TXK TXK 87.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 61.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 88.0 1000
KDR VEGFR2 96.0 1000
PIK3C3 VPS34 91.0 1000
VRK2 VRK2 70.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 84.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 67.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 84.0 1000
YES1 YES 94.0 1000
STK25 YSK1 91.0 1000
MAP3K19 YSK4 63.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 78.0 1000

A-108


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 94.0 1000
ABL1 ABL1-phosphorylated 96.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 98.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 78.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 87.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 91.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 76.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 90.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 79.0 1000
BLK BLK 71.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 96.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 64.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 86.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 82.0 1000
BUB1 BUB1 98.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 85.0 1000
CAMK2A CAMK2A 84.0 1000
CAMK2B CAMK2B 90.0 1000
CAMK2D CAMK2D 95.0 1000
CAMK2G CAMK2G 98.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 97.0 1000
CASK CASK 92.0 1000
CDK11B CDC2L1 92.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 87.0 1000
CDK19 CDK11 64.0 1000
CDK2 CDK2 89.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 92.0 1000
CDK5 CDK5 96.0 1000
CDK7 CDK7 63.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 89.0 1000
CDKL2 CDKL2 93.0 1000
CDKL3 CDKL3 81.0 1000
CDKL5 CDKL5 93.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 96.0 1000
CIT CIT 97.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 90.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 96.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 78.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 94.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 91.0 1000
CSNK1G2 CSNK1G2 64.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 97.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 87.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 94.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 95.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 94.0 1000
CDC42BPG DMPK2 96.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 84.0 1000
DYRK1A DYRK1A 99.0 1000
DYRK1B DYRK1B 38.0 1000
DYRK2 DYRK2 89.0 1000
EGFR EGFR(T790M) 68.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 93.0 1000
EPHA2 EPHA2 89.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 12.0 1000
EPHA5 EPHA5 67.0 1000
EPHA6 EPHA6 3.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 6.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 94.0 1000
ERBB3 ERBB3 89.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 83.0 1000
MAPK1 ERK2 91.0 1000
MAPK6 ERK3 93.0 1000
MAPK4 ERK4 90.0 1000
MAPK7 ERK5 93.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 95.0 1000
PTK2 FAK 97.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 97.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 83.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 90.0 1000
FRK FRK 100.0 1000
FYN FYN 97.0 1000
GAK GAK 91.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 95.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 56.0 1000
GRK7 GRK7 81.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 79.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 97.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 75.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 84.0 1000
INSRR INSRR 96.0 1000
IRAK1 IRAK1 73.0 1000
IRAK3 IRAK3 91.0 1000
IRAK4 IRAK4 80.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 92.0 1000
JAK2 JAK2(JH1domain-catalytic) 65.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 77.0 1000
MAPK9 JNK2 92.0 1000
MAPK10 JNK3 75.0 1000
KIT KIT-autoinhibited 90.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 82.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 91.0 1000
LTK LTK 100.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 72.0 1000
MAK MAK 99.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 83.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 81.0 1000
MAP3K4 MAP3K4 80.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 61.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 93.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 89.0 1000
MAP2K2 MEK2 74.0 1000
MAP2K3 MEK3 100.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 88.0 1000
MAP2K6 MEK6 94.0 1000
MELK MELK 79.0 1000
MERTK MERTK 69.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 96.0 1000
MKNK1 MKNK1 81.0 1000
MKNK2 MKNK2 74.0 1000
MYLK3 MLCK 96.0 1000
MAP3K9 MLK1 98.0 1000
MAP3K10 MLK2 98.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 81.0 1000
CDC42BPB MRCKB 95.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 95.0 1000
STK24 MST3 100.0 1000
STK26 MST4 99.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 99.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 97.0 1000
MYO3A MYO3A 98.0 1000
MYO3B MYO3B 55.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 87.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 84.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 95.0 1000
NEK3 NEK3 87.0 1000
NEK4 NEK4 90.0 1000
NEK5 NEK5 98.0 1000
NEK6 NEK6 95.0 1000
NEK7 NEK7 99.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 92.0 1000
NIM1K NIM1 97.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 75.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 96.0 1000
MAPK13 p38-delta 90.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 96.0 1000
PAK3 PAK3 91.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 85.0 1000
CDK17 PCTK2 95.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 97.0 1000
PDPK1 PDPK1 96.0 1000
CDPK1 PFCDPK1(P.falciparum) 75.0 1000
PK5 PFPK5(P.falciparum) 69.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 95.0 1000
PHKG2 PHKG2 92.0 1000
PIK3C2B PIK3C2B 95.0 1000
PIK3C2G PIK3C2G 61.0 1000
PIK3CA PIK3CA(Q546K) 85.0 1000
PIK3CB PIK3CB 75.0 1000
PIK3CD PIK3CD 84.0 1000
PIK3CG PIK3CG 69.0 1000
PI4KB PIK4CB 80.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 87.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 96.0 1000
PRKACA PKAC-alpha 94.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 85.0 1000
PKNB PKNB(M.tuberculosis) 78.0 1000
PLK1 PLK1 83.0 1000
PLK2 PLK2 86.0 1000
PLK3 PLK3 88.0 1000
PLK4 PLK4 84.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 95.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 98.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 98.0 1000
PRKG1 PRKG1 94.0 1000
PRKG2 PRKG2 87.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 94.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 97.0 1000
RAF1 RAF1 85.0 1000
RET RET(V804M) 98.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 90.0 1000
RIPK1 RIPK1 90.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 94.0 1000
DSTYK RIPK5 100.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 96.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 93.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 81.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 72.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 98.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 94.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 92.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 87.0 1000
SRC SRC 100.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 97.0 1000
SRPK2 SRPK2 55.0 1000
SRPK3 SRPK3 56.0 1000
STK16 STK16 99.0 1000
STK33 STK33 69.0 1000
STK35 STK35 100.0 1000
STK36 STK36 93.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 67.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 98.0 1000
TAOK3 TAOK3 100.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 92.0 1000
TGFBR1 TGFBR1 78.0 1000
TGFBR2 TGFBR2 96.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 92.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 97.0 1000
TNIK TNIK 99.0 1000
TNK1 TNK1 88.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 91.0 1000
NTRK2 TRKB 88.0 1000
NTRK3 TRKC 99.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 70.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 85.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 95.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 78.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 95.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 84.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 85.0 1000
STK32A YANK1 75.0 1000
STK32B YANK2 97.0 1000
STK32C YANK3 80.0 1000
YES1 YES 100.0 1000
STK25 YSK1 95.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 85.0 1000
ZAP70 ZAP70 100.0 1000

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ABT-100

Results are expressed as percent inhibition of control specific binding (mean values; n=2).

Conclusion: Closest off-target is PCP with 97 % inhibtion at 3 µM.

Target protein HGNC name Species % inhibition at 10 µM % inhibition at 3 µM % inhibition at 1 µM % inhibition at 0.3 µM
A1 (h) ADORA1 Homo sapiens < 10.0
A2a (h) ADORA2A Homo sapiens < 10.0
A3 (h) ADORA3 Homo sapiens < 10.0
alpha1 (non-selective) < 10.0
alpha2 (non-selective) < 10.0
beta1 (h) ADRB1 Homo sapiens 22.0
beta2 (h) ADRB2 Homo sapiens 10.0
NE uptake (h) SLC6A2 Homo sapiens 74.0 45.00
AT1 (h) AGTR1 Homo sapiens < 10.0
AT2 (h) AGTR2 Homo sapiens < 10.0
ANP NPPA < 10.0
BZD (central) < 10.0
BZD (peripheral) 36.0
Bombesin < 10.0
B2 (h) BDKRB2 Homo sapiens < 10.0
CGRP (h) CALCA Homo sapiens < 10.0
CB1 (h) (central) CNR1 Homo sapiens 68.0 45.00 23.00
CB2 (h) (peripheral) CNR2 Homo sapiens < 10.0
CCKA (h) CCKAR Homo sapiens < 10.0
CCKB (h) CCKBR Homo sapiens < 10.0
D1 (h) DRD1 Homo sapiens 31.0
D2 (h) DRD2 Homo sapiens 12.0
D3 (h) DRD3 Homo sapiens 36.0
D4.4 (h) DRD4 Homo sapiens < 10.0
D5 (h) DRD5 Homo sapiens 54.0
DA uptake (h) SLC6A3 Homo sapiens 75.0 41.00 21.00
ETA (h) EDNRA Homo sapiens < 10.0
ETB (h) EDNRB Homo sapiens 21.0
GABA (non selective) < 10.0
GALI (h) GAL Homo sapiens < 10.0
PDGF < 10.0
IL-8A (h) (CXCR1) CXCR1 Homo sapiens < 10.0
TNF-alpha (h) TNF Homo sapiens 24.0
CCR1 (h) CCR1 Homo sapiens < 10.0
H1 (central) HRH1 < 10.0
H2 HRH2 53.0
ML1 MCOLN1 50.0
M1 (h) CHRM1 Homo sapiens < 10.0
M2 (h) CHRM2 Homo sapiens < 10.0
M3 (h) CHRM3 Homo sapiens < 10.0
M4 (h) CHRM4 Homo sapiens < 10.0
M5 (h) CHRM5 Homo sapiens 18.0
NK1 (h) TACR1 Homo sapiens 68.0 31.00
NK2 (h) TACR2 Homo sapiens 81.0 32.00
NK3 (h) TACR3 Homo sapiens 45.0
Y1 (h) NPY1R Homo sapiens < 10.0
Y2 (h) NPY2R Homo sapiens < 10.0
NT1 (h) NTSR1 Homo sapiens < 10.0
Delta (h) OPRD1 Homo sapiens 14.0
Kappa (h) OPRK1 Homo sapiens 36.0
Mu (h) OPRM1 Homo sapiens 18.0
ORL-1 (h) OPRL1 Homo sapiens < 10.0
PACAP-null (h) ADCYAP1 Homo sapiens < 10.0
PCP PRCP 100.0 97.00 75.00 14.00
TXA2/PGH2 (h) TBXA2R Homo sapiens 24.0
PGI2 (h) PTGIR Homo sapiens < 10.0
P2X < 10.0
P2Y < 10.0
5-HT1A (h) HTR1A Homo sapiens 18.0
5-HT1B HTR1B < 10.0
5-HT2A (h) HTR2A Homo sapiens 15.0
5-HT2C (h) HTR2C Homo sapiens < 10.0
5-HT3 (h) HTR3A Homo sapiens 12.0
5-HT5A (h) HTR5A Homo sapiens 30.0
5-HT6 (h) HTR6 Homo sapiens < 10.0
5-HT7 (h) HTR7 Homo sapiens 22.0
Sigma (non selective) 67.0 28.00
Somatostatin 13.0
VIP1 (h) VIPR1 Homo sapiens 60.0 23.00
V1a (h) AVPR1A Homo sapiens < 10.0
Ca2+ channel (L verapamil site) 60.0 37.00 10.00
K+ channel (Volt-dependent) < 10.0
K+ channel (Ca2+ - dependent) < 10.0
Na+ channel (site 2) 58.0 22.00 10.00 15.00
Cl- ionophore 67.0 30.00