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Selectivity data for probe MLi-2 and control MLi-2-NC


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MLi-2


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 -20.58
Beta3 ADRB3 -5.99
H4 HRH4 -19.75
5-HT1B HTR1B 1.16
5-HT1D HTR1D -7.94
5-HT1E HTR1E -7.52
5-HT6 HTR6 -13.64
5-HT7A HTR7 -12.93
Beta2 ADRB2 26.40
D1 DRD1 -17.43
D2 DRD2 -14.40
DOR OPRD1 6.66
H3 HRH3 -17.27
KOR OPRK1 -0.60
M1 CHRM1 3.04
M5 CHRM5 1.00
5-HT1A HTR1A 4.44
GABAA/BZP 7.14
D3 DRD3 -0.66
D4 DRD4 -4.87
D5 DRD5 16.09
GABAA -35.27
H1 HRH1 -6.46
H2 HRH2 6.26
MOR OPRM1 -12.29
5-HT2A HTR2A 2.75
5-HT2B HTR2B 41.43
5-HT2C HTR2C 7.65
5-HT3 HTR3A 4.35
5-HT5A HTR5A -4.76
Alpha1A ADRA1A 3.49
Alpha1B ADRA1B -12.52
Alpha1D ADRA1D 3.26
Alpha2A ADRA2A -2.84
Alpha2B ADRA2B 6.10
Alpha2C ADRA2C 7.85
M4 CHRM4 -4.79
NET SLC6A2 7.45
Sigma 2 TMEM97 50.36 4600.45 5.34
DAT SLC6A3 -24.37
M2 CHRM2 25.89
SERT SLC6A4 -2.29
Sigma 1 SIGMAR1 35.87
M3 CHRM3 7.93
GABA/PBR 5.96

MLi-2-NC


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABA/PBR 46.07
M3 CHRM3 6.03
Sigma 1 SIGMAR1 58.18 1593.68 5.80
DAT SLC6A3 -24.44
M2 CHRM2 21.01
SERT SLC6A4 -3.49
5-HT1A HTR1A 18.11
GABAA/BZP 2.92
D3 DRD3 2.71
D4 DRD4 -2.65
D5 DRD5 3.61
GABAA -28.09
H1 HRH1 11.93
H2 HRH2 18.41
MOR OPRM1 13.25
5-HT1B HTR1B 7.83
5-HT1D HTR1D 4.11
5-HT1E HTR1E -0.18
5-HT6 HTR6 -11.32
5-HT7A HTR7 -0.40
Beta2 ADRB2 13.78
D1 DRD1 -26.64
D2 DRD2 -0.18
DOR OPRD1 23.26
H3 HRH3 -6.25
KOR OPRK1 13.09
M1 CHRM1 -1.02
M5 CHRM5 2.87
Beta1 ADRB1 5.75
Beta3 ADRB3 11.81
H4 HRH4 -16.24
5-HT2A HTR2A 3.31
5-HT2B HTR2B 26.74
5-HT2C HTR2C 18.70
5-HT3 HTR3A -3.11
5-HT5A HTR5A -6.76
Alpha1A ADRA1A -3.60
Alpha1B ADRA1B 3.72
Alpha1D ADRA1D 10.21
Alpha2A ADRA2A 12.86
Alpha2B ADRA2B 27.19
Alpha2C ADRA2C 15.06
M4 CHRM4 10.63
NET SLC6A2 30.55
Sigma 2 TMEM97 90.38 1074.98 5.97

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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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Jump to control KinomeScan data

MLi-2


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 100
ABL1 ABL1-phosphorylated 67.0 100
ABL2 ABL2 73.0 100
ACVR1 ACVR1 90.0 100
ACVR1B ACVR1B 90.0 100
ACVR2A ACVR2A 94.0 100
ACVR2B ACVR2B 99.0 100
ACVRL1 ACVRL1 94.0 100
COQ8A ADCK3 85.0 100
COQ8B ADCK4 72.0 100
AKT1 AKT1 87.0 100
AKT2 AKT2 100.0 100
AKT3 AKT3 86.0 100
ALK ALK(L1196M) 78.0 100
PRKAA1 AMPK-alpha1 86.0 100
PRKAA2 AMPK-alpha2 100.0 100
ANKK1 ANKK1 79.0 100
NUAK1 ARK5 92.0 100
MAP3K5 ASK1 88.0 100
MAP3K6 ASK2 59.0 100
AURKA AURKA 94.0 100
AURKB AURKB 73.0 100
AURKC AURKC 100.0 100
AXL AXL 100.0 100
BMP2K BIKE 100.0 100
BLK BLK 83.0 100
BMPR1A BMPR1A 100.0 100
BMPR1B BMPR1B 81.0 100
BMPR2 BMPR2 75.0 100
BMX BMX 80.0 100
BRAF BRAF(V600E) 89.0 100
PTK6 BRK 100.0 100
BRSK1 BRSK1 96.0 100
BRSK2 BRSK2 100.0 100
BTK BTK 73.0 100
BUB1 BUB1 84.0 100
CAMK1 CAMK1 100.0 100
PNCK CAMK1B 67.0 100
CAMK1D CAMK1D 100.0 100
CAMK1G CAMK1G 91.0 100
CAMK2A CAMK2A 100.0 100
CAMK2B CAMK2B 100.0 100
CAMK2D CAMK2D 100.0 100
CAMK2G CAMK2G 100.0 100
CAMK4 CAMK4 78.0 100
CAMKK1 CAMKK1 100.0 100
CAMKK2 CAMKK2 100.0 100
CASK CASK 59.0 100
CDK11B CDC2L1 88.0 100
CDK11A CDC2L2 93.0 100
CDK13 CDC2L5 84.0 100
CDK19 CDK11 70.0 100
CDK2 CDK2 96.0 100
CDK3 CDK3 76.0 100
CDK4 CDK4-cyclinD3 68.0 100
CDK5 CDK5 100.0 100
CDK7 CDK7 56.0 100
CDK8 CDK8 63.0 100
CDK9 CDK9 80.0 100
CDKL1 CDKL1 89.0 100
CDKL2 CDKL2 100.0 100
CDKL3 CDKL3 75.0 100
CDKL5 CDKL5 72.0 100
CHEK1 CHEK1 90.0 100
CHEK2 CHEK2 68.0 100
CIT CIT 69.0 100
CLK1 CLK1 86.0 100
CLK2 CLK2 85.0 100
CLK3 CLK3 94.0 100
CLK4 CLK4 87.0 100
CSF1R CSF1R-autoinhibited 84.0 100
CSK CSK 100.0 100
CSNK1A1 CSNK1A1 73.0 100
CSNK1A1L CSNK1A1L 100.0 100
CSNK1D CSNK1D 80.0 100
CSNK1E CSNK1E 100.0 100
CSNK1G1 CSNK1G1 100.0 100
CSNK1G2 CSNK1G2 100.0 100
CSNK1G3 CSNK1G3 95.0 100
CSNK2A1 CSNK2A1 66.0 100
CSNK2A2 CSNK2A2 100.0 100
MATK CTK 94.0 100
DAPK1 DAPK1 93.0 100
DAPK2 DAPK2 85.0 100
DAPK3 DAPK3 96.0 100
DCLK1 DCAMKL1 81.0 100
DCLK2 DCAMKL2 89.0 100
DCLK3 DCAMKL3 92.0 100
DDR1 DDR1 91.0 100
DDR2 DDR2 82.0 100
MAP3K12 DLK 82.0 100
DMPK DMPK 85.0 100
CDC42BPG DMPK2 89.0 100
STK17A DRAK1 100.0 100
STK17B DRAK2 96.0 100
DYRK1A DYRK1A 95.0 100
DYRK1B DYRK1B 93.0 100
DYRK2 DYRK2 98.0 100
EGFR EGFR(T790M) 100.0 100
EIF2AK1 EIF2AK1 100.0 100
EPHA1 EPHA1 76.0 100
EPHA2 EPHA2 72.0 100
EPHA3 EPHA3 93.0 100
EPHA4 EPHA4 89.0 100
EPHA5 EPHA5 95.0 100
EPHA6 EPHA6 90.0 100
EPHA7 EPHA7 82.0 100
EPHA8 EPHA8 82.0 100
EPHB1 EPHB1 83.0 100
EPHB2 EPHB2 90.0 100
EPHB3 EPHB3 98.0 100
EPHB4 EPHB4 79.0 100
EPHB6 EPHB6 91.0 100
ERBB2 ERBB2 77.0 100
ERBB3 ERBB3 100.0 100
ERBB4 ERBB4 90.0 100
MAPK3 ERK1 87.0 100
MAPK1 ERK2 98.0 100
MAPK6 ERK3 91.0 100
MAPK4 ERK4 83.0 100
MAPK7 ERK5 92.0 100
MAPK15 ERK8 81.0 100
ERN1 ERN1 79.0 100
PTK2 FAK 81.0 100
FER FER 86.0 100
FES FES 87.0 100
FGFR1 FGFR1 100.0 100
FGFR2 FGFR2 96.0 100
FGFR3 FGFR3(G697C) 86.0 100
FGFR4 FGFR4 100.0 100
FGR FGR 89.0 100
FLT1 FLT1 100.0 100
FLT3 FLT3-autoinhibited 87.0 100
FLT4 FLT4 100.0 100
FRK FRK 100.0 100
FYN FYN 100.0 100
GAK GAK 86.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 81.0 100
GRK1 GRK1 83.0 100
GRK2 GRK2 86.0 100
GRK3 GRK3 91.0 100
GRK4 GRK4 100.0 100
GRK7 GRK7 64.0 100
GSK3A GSK3A 100.0 100
GSK3B GSK3B 90.0 100
HASPIN HASPIN 74.0 100
HCK HCK 84.0 100
HIPK1 HIPK1 69.0 100
HIPK2 HIPK2 80.0 100
HIPK3 HIPK3 73.0 100
HIPK4 HIPK4 97.0 100
MAP4K1 HPK1 84.0 100
HUNK HUNK 79.0 100
CILK1 ICK 62.0 100
IGF1R IGF1R 100.0 100
CHUK IKK-alpha 76.0 100
IKBKB IKK-beta 84.0 100
IKBKE IKK-epsilon 74.0 100
INSR INSR 100.0 100
INSRR INSRR 57.0 100
IRAK1 IRAK1 79.0 100
IRAK3 IRAK3 94.0 100
IRAK4 IRAK4 90.0 100
ITK ITK 87.0 100
JAK1 JAK1(JH2domain-pseudokinase) 79.0 100
JAK2 JAK2(JH1domain-catalytic) 77.0 100
JAK3 JAK3(JH1domain-catalytic) 0.0 100
MAPK8 JNK1 63.0 100
MAPK9 JNK2 72.0 100
MAPK10 JNK3 77.0 100
KIT KIT-autoinhibited 70.0 100
LATS1 LATS1 96.0 100
LATS2 LATS2 68.0 100
LCK LCK 100.0 100
LIMK1 LIMK1 86.0 100
LIMK2 LIMK2 91.0 100
STK11 LKB1 83.0 100
STK10 LOK 83.0 100
LRRK2 LRRK2(G2019S) 2.3 100
LTK LTK 84.0 100
LYN LYN 98.0 100
MAP3K13 LZK 0.0 100
MAK MAK 95.0 100
MAP3K1 MAP3K1 63.0 100
MAP3K15 MAP3K15 67.0 100
MAP3K2 MAP3K2 73.0 100
MAP3K3 MAP3K3 64.0 100
MAP3K4 MAP3K4 100.0 100
MAP4K2 MAP4K2 76.0 100
MAP4K3 MAP4K3 88.0 100
MAP4K4 MAP4K4 98.0 100
MAP4K5 MAP4K5 100.0 100
MAPKAPK2 MAPKAPK2 96.0 100
MAPKAPK5 MAPKAPK5 93.0 100
MARK1 MARK1 100.0 100
MARK2 MARK2 100.0 100
MARK3 MARK3 73.0 100
MARK4 MARK4 100.0 100
MAST1 MAST1 70.0 100
MAP2K1 MEK1 88.0 100
MAP2K2 MEK2 85.0 100
MAP2K3 MEK3 71.0 100
MAP2K4 MEK4 73.0 100
MAP2K5 MEK5 90.0 100
MAP2K6 MEK6 100.0 100
MELK MELK 88.0 100
MERTK MERTK 97.0 100
MET MET(Y1235D) 92.0 100
MINK1 MINK 84.0 100
MAP2K7 MKK7 77.0 100
MKNK1 MKNK1 67.0 100
MKNK2 MKNK2 74.0 100
MYLK3 MLCK 87.0 100
MAP3K9 MLK1 100.0 100
MAP3K10 MLK2 100.0 100
MAP3K11 MLK3 100.0 100
CDC42BPA MRCKA 90.0 100
CDC42BPB MRCKB 93.0 100
STK4 MST1 83.0 100
MST1R MST1R 100.0 100
STK3 MST2 78.0 100
STK24 MST3 96.0 100
STK26 MST4 76.0 100
MTOR MTOR 99.0 100
MUSK MUSK 56.0 100
MYLK MYLK 56.0 100
MYLK2 MYLK2 91.0 100
MYLK4 MYLK4 100.0 100
MYO3A MYO3A 100.0 100
MYO3B MYO3B 89.0 100
STK38 NDR1 87.0 100
STK38L NDR2 85.0 100
NEK1 NEK1 100.0 100
NEK10 NEK10 69.0 100
NEK11 NEK11 100.0 100
NEK2 NEK2 86.0 100
NEK3 NEK3 76.0 100
NEK4 NEK4 84.0 100
NEK5 NEK5 100.0 100
NEK6 NEK6 100.0 100
NEK7 NEK7 100.0 100
NEK9 NEK9 100.0 100
MAP3K14 NIK 64.0 100
NIM1K NIM1 72.0 100
NLK NLK 100.0 100
OXSR1 OSR1 72.0 100
MAPK14 p38-alpha 95.0 100
MAPK11 p38-beta 89.0 100
MAPK13 p38-delta 96.0 100
MAPK12 p38-gamma 96.0 100
PAK1 PAK1 97.0 100
PAK2 PAK2 95.0 100
PAK3 PAK3 83.0 100
PAK4 PAK4 97.0 100
PAK6 PAK6 100.0 100
PAK5 PAK7 86.0 100
CDK16 PCTK1 85.0 100
CDK17 PCTK2 89.0 100
CDK18 PCTK3 100.0 100
PDGFRA PDGFRA 75.0 100
PDGFRB PDGFRB 73.0 100
PDPK1 PDPK1 78.0 100
CDPK1 PFCDPK1(P.falciparum) 94.0 100
PK5 PFPK5(P.falciparum) 80.0 100
CDK15 PFTAIRE2 100.0 100
CDK14 PFTK1 100.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 91.0 100
PIK3C2B PIK3C2B 66.0 100
PIK3C2G PIK3C2G 69.0 100
PIK3CA PIK3CA(Q546K) 69.0 100
PIK3CB PIK3CB 59.0 100
PIK3CD PIK3CD 68.0 100
PIK3CG PIK3CG 72.0 100
PI4KB PIK4CB 100.0 100
PIKFYVE PIKFYVE 90.0 100
PIM1 PIM1 100.0 100
PIM2 PIM2 88.0 100
PIM3 PIM3 100.0 100
PIP5K1A PIP5K1A 100.0 100
PIP5K1C PIP5K1C 92.0 100
PIP4K2B PIP5K2B 81.0 100
PIP4K2C PIP5K2C 90.0 100
PRKACA PKAC-alpha 85.0 100
PRKACB PKAC-beta 91.0 100
PKMYT1 PKMYT1 96.0 100
PKN1 PKN1 91.0 100
PKN2 PKN2 89.0 100
PKNB PKNB(M.tuberculosis) 95.0 100
PLK1 PLK1 68.0 100
PLK2 PLK2 76.0 100
PLK3 PLK3 84.0 100
PLK4 PLK4 71.0 100
PRKCD PRKCD 100.0 100
PRKCE PRKCE 95.0 100
PRKCH PRKCH 92.0 100
PRKCI PRKCI 80.0 100
PRKCQ PRKCQ 74.0 100
PRKD1 PRKD1 84.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 82.0 100
PRKG1 PRKG1 100.0 100
PRKG2 PRKG2 79.0 100
EIF2AK2 PRKR 100.0 100
PRKX PRKX 86.0 100
PRPF4B PRP4 83.0 100
PTK2B PYK2 100.0 100
SIK3 QSK 74.0 100
RAF1 RAF1 100.0 100
RET RET(V804M) 97.0 100
RIOK1 RIOK1 100.0 100
RIOK2 RIOK2 68.0 100
RIOK3 RIOK3 100.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 48.0 100
DSTYK RIPK5 77.0 100
ROCK1 ROCK1 80.0 100
ROCK2 ROCK2 89.0 100
ROS1 ROS1 100.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 75.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 89.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 93.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 85.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 85.0 100
RPS6KB1 S6K1 73.0 100
SBK1 SBK1 88.0 100
SGK1 SGK 89.0 100
SBK3 SgK110 100.0 100
SGK2 SGK2 84.0 100
SGK3 SGK3 84.0 100
SIK1 SIK 100.0 100
SIK2 SIK2 87.0 100
SLK SLK 98.0 100
NUAK2 SNARK 79.0 100
SNRK SNRK 94.0 100
SRC SRC 81.0 100
SRMS SRMS 59.0 100
SRPK1 SRPK1 100.0 100
SRPK2 SRPK2 79.0 100
SRPK3 SRPK3 100.0 100
STK16 STK16 100.0 100
STK33 STK33 86.0 100
STK35 STK35 85.0 100
STK36 STK36 86.0 100
STK39 STK39 85.0 100
SYK SYK 96.0 100
MAP3K7 TAK1 70.0 100
TAOK1 TAOK1 86.0 100
TAOK2 TAOK2 73.0 100
TAOK3 TAOK3 69.0 100
TBK1 TBK1 68.0 100
TEC TEC 74.0 100
TESK1 TESK1 75.0 100
TGFBR1 TGFBR1 100.0 100
TGFBR2 TGFBR2 100.0 100
TIE1 TIE1 67.0 100
TEK TIE2 100.0 100
TLK1 TLK1 94.0 100
TLK2 TLK2 100.0 100
TNIK TNIK 100.0 100
TNK1 TNK1 76.0 100
TNK2 TNK2 79.0 100
TNNI3K TNNI3K 78.0 100
NTRK1 TRKA 73.0 100
NTRK2 TRKB 67.0 100
NTRK3 TRKC 86.0 100
TRPM6 TRPM6 64.0 100
TSSK1B TSSK1B 72.0 100
TSSK3 TSSK3 79.0 100
TTK TTK 74.0 100
TXK TXK 80.0 100
TYK2 TYK2(JH2domain-pseudokinase) 76.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 80.0 100
ULK2 ULK2 69.0 100
ULK3 ULK3 78.0 100
KDR VEGFR2 82.0 100
PIK3C3 VPS34 100.0 100
VRK2 VRK2 65.0 100
WEE1 WEE1 97.0 100
WEE2 WEE2 100.0 100
WNK1 WNK1 89.0 100
WNK2 WNK2 84.0 100
WNK3 WNK3 73.0 100
WNK4 WNK4 94.0 100
STK32A YANK1 92.0 100
STK32B YANK2 92.0 100
STK32C YANK3 89.0 100
YES1 YES 80.0 100
STK25 YSK1 100.0 100
MAP3K19 YSK4 84.0 100
MAP3K20 ZAK 92.0 100
ZAP70 ZAP70 83.0 100

MLi-2-NC


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 84.0 1000
ABL1 ABL1-phosphorylated 79.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 96.0 1000
ACVR1B ACVR1B 78.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 98.0 1000
ACVRL1 ACVRL1 63.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 89.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 98.0 1000
PRKAA1 AMPK-alpha1 93.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 67.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 76.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 94.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 95.0 1000
BMPR1A BMPR1A 85.0 1000
BMPR1B BMPR1B 77.0 1000
BMPR2 BMPR2 54.0 1000
BMX BMX 93.0 1000
BRAF BRAF(V600E) 91.0 1000
PTK6 BRK 92.0 1000
BRSK1 BRSK1 97.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 80.0 1000
BUB1 BUB1 89.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 82.0 1000
CAMK2A CAMK2A 98.0 1000
CAMK2B CAMK2B 96.0 1000
CAMK2D CAMK2D 88.0 1000
CAMK2G CAMK2G 90.0 1000
CAMK4 CAMK4 67.0 1000
CAMKK1 CAMKK1 80.0 1000
CAMKK2 CAMKK2 85.0 1000
CASK CASK 93.0 1000
CDK11B CDC2L1 88.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 86.0 1000
CDK19 CDK11 92.0 1000
CDK2 CDK2 73.0 1000
CDK3 CDK3 98.0 1000
CDK4 CDK4-cyclinD3 71.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 84.0 1000
CDKL1 CDKL1 89.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 88.0 1000
CDKL5 CDKL5 64.0 1000
CHEK1 CHEK1 57.0 1000
CHEK2 CHEK2 97.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 86.0 1000
CLK2 CLK2 81.0 1000
CLK3 CLK3 98.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 55.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 78.0 1000
CSNK1D CSNK1D 84.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 89.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 76.0 1000
CSNK2A2 CSNK2A2 86.0 1000
MATK CTK 80.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 89.0 1000
DAPK3 DAPK3 89.0 1000
DCLK1 DCAMKL1 64.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 77.0 1000
DDR1 DDR1 68.0 1000
DDR2 DDR2 79.0 1000
MAP3K12 DLK 61.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 81.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 81.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 83.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 60.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 68.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 99.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 99.0 1000
EPHB2 EPHB2 95.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 80.0 1000
ERBB3 ERBB3 57.0 1000
ERBB4 ERBB4 96.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 97.0 1000
MAPK4 ERK4 93.0 1000
MAPK7 ERK5 76.0 1000
MAPK15 ERK8 72.0 1000
ERN1 ERN1 69.0 1000
PTK2 FAK 95.0 1000
FER FER 100.0 1000
FES FES 93.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 90.0 1000
FLT1 FLT1 95.0 1000
FLT3 FLT3-autoinhibited 77.0 1000
FLT4 FLT4 85.0 1000
FRK FRK 100.0 1000
FYN FYN 98.0 1000
GAK GAK 86.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 68.0 1000
GRK3 GRK3 69.0 1000
GRK4 GRK4 96.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 86.0 1000
GSK3B GSK3B 91.0 1000
HASPIN HASPIN 99.0 1000
HCK HCK 96.0 1000
HIPK1 HIPK1 85.0 1000
HIPK2 HIPK2 74.0 1000
HIPK3 HIPK3 91.0 1000
HIPK4 HIPK4 79.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 78.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 75.0 1000
IKBKB IKK-beta 76.0 1000
IKBKE IKK-epsilon 65.0 1000
INSR INSR 100.0 1000
INSRR INSRR 91.0 1000
IRAK1 IRAK1 67.0 1000
IRAK3 IRAK3 89.0 1000
IRAK4 IRAK4 76.0 1000
ITK ITK 96.0 1000
STK38L NDR2 72.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 84.0 1000
JAK2 JAK2(JH1domain-catalytic) 55.0 1000
JAK3 JAK3(JH1domain-catalytic) 12.0 1000
MAPK8 JNK1 82.0 1000
MAPK9 JNK2 78.0 1000
MAPK10 JNK3 71.0 1000
KIT KIT-autoinhibited 97.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 58.0 1000
LCK LCK 94.0 1000
LIMK1 LIMK1 95.0 1000
LIMK2 LIMK2 92.0 1000
STK11 LKB1 94.0 1000
STK10 LOK 91.0 1000
LRRK2 LRRK2(G2019S) 36.0 1000
LTK LTK 100.0 1000
LYN LYN 82.0 1000
MAP3K13 LZK 91.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 92.0 1000
MAP3K15 MAP3K15 80.0 1000
MAP3K2 MAP3K2 83.0 1000
MAP3K3 MAP3K3 90.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 81.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 93.0 1000
MAPKAPK5 MAPKAPK5 73.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 89.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 74.0 1000
MAP2K2 MEK2 73.0 1000
MAP2K3 MEK3 70.0 1000
MAP2K4 MEK4 82.0 1000
MAP2K5 MEK5 93.0 1000
MAP2K6 MEK6 89.0 1000
MELK MELK 55.0 1000
MERTK MERTK 83.0 1000
MET MET(Y1235D) 87.0 1000
MINK1 MINK 66.0 1000
MAP2K7 MKK7 74.0 1000
MKNK1 MKNK1 79.0 1000
MKNK2 MKNK2 67.0 1000
MYLK3 MLCK 97.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 89.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 79.0 1000
STK26 MST4 74.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 92.0 1000
MYLK MYLK 64.0 1000
MYLK2 MYLK2 87.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 57.0 1000
NEK1 NEK1 83.0 1000
NEK10 NEK10 89.0 1000
NEK11 NEK11 58.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 99.0 1000
NEK4 NEK4 60.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 79.0 1000
NEK9 NEK9 71.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 74.0 1000
NLK NLK 96.0 1000
OXSR1 OSR1 93.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 88.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 76.0 1000
PAK2 PAK2 90.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 93.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 84.0 1000
CDK16 PCTK1 87.0 1000
CDK17 PCTK2 88.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 83.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 83.0 1000
PK5 PFPK5(P.falciparum) 94.0 1000
CDK15 PFTAIRE2 84.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 90.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 70.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 39.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 97.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 89.0 1000
PIKFYVE PIKFYVE 78.0 1000
PIM1 PIM1 77.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 92.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 90.0 1000
PIP4K2B PIP5K2B 84.0 1000
PIP4K2C PIP5K2C 98.0 1000
PRKACA PKAC-alpha 95.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 74.0 1000
PLK2 PLK2 68.0 1000
PLK3 PLK3 84.0 1000
PLK4 PLK4 65.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 91.0 1000
PRKD1 PRKD1 82.0 1000
PRKD2 PRKD2 90.0 1000
PRKD3 PRKD3 64.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 85.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 92.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 77.0 1000
SIK3 QSK 63.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 89.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 98.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 85.0 1000
DSTYK RIPK5 67.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 97.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 81.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 62.0 1000
SGK1 SGK 47.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 58.0 1000
SGK3 SGK3 67.0 1000
SIK1 SIK 96.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 68.0 1000
SNRK SNRK 92.0 1000
SRC SRC 100.0 1000
SRMS SRMS 83.0 1000
SRPK1 SRPK1 88.0 1000
SRPK2 SRPK2 88.0 1000
SRPK3 SRPK3 98.0 1000
STK16 STK16 100.0 1000
STK33 STK33 86.0 1000
STK35 STK35 100.0 1000
STK36 STK36 93.0 1000
STK39 STK39 70.0 1000
SYK SYK 89.0 1000
MAP3K7 TAK1 89.0 1000
TAOK1 TAOK1 82.0 1000
TAOK2 TAOK2 80.0 1000
TAOK3 TAOK3 35.0 1000
TBK1 TBK1 75.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 89.0 1000
TGFBR2 TGFBR2 73.0 1000
TIE1 TIE1 92.0 1000
TEK TIE2 94.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 97.0 1000
TNIK TNIK 80.0 1000
TNK1 TNK1 95.0 1000
TNK2 TNK2 96.0 1000
TNNI3K TNNI3K 71.0 1000
NTRK1 TRKA 76.0 1000
NTRK2 TRKB 65.0 1000
NTRK3 TRKC 65.0 1000
TRPM6 TRPM6 85.0 1000
TSSK1B TSSK1B 99.0 1000
TSSK3 TSSK3 75.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 82.0 1000
TYRO3 TYRO3 93.0 1000
ULK1 ULK1 76.0 1000
ULK2 ULK2 59.0 1000
ULK3 ULK3 67.0 1000
KDR VEGFR2 75.0 1000
PIK3C3 VPS34 86.0 1000
VRK2 VRK2 73.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 96.0 1000
WNK1 WNK1 82.0 1000
WNK2 WNK2 63.0 1000
WNK3 WNK3 91.0 1000
WNK4 WNK4 60.0 1000
STK32A YANK1 78.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 98.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 68.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 100.0 1000

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MLi-2

Results are significant for > 50 % inhibition. Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (ID Business Solutions Ltd., UK). The inhibition constants (Ki) were calculated with the equation of Cheng and Prusoff (Cheng, Y., Prusoff, W.H., Biochem. Pharmacol. 22:3099-3108, 1973) using the observed IC50 value of the tested compound, the concentration of radioligand employed in the assay, and the historical values for the Ki of the ligand (obtained experimentally at Ricerca Biosciences, LLC).

Conclusion: The closest off-target is Serotonin (5-Hydroxytryptamine) 5-HT2B (HTR2B) with IC50 = 1.17 µM at 10 µM.

Target protein HGNC name Species Cmp. conc. % inhibition IC50 [µM] Ki [µM] Reference compound name Reference compound IC50 [nM] Assay ID
Adenosine A1 ADORA1 Homo sapiens 10 µM 29.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 1.0 CGS-Z1680 130.00 200610
Adrenergic alpha1A ADRA1A Rattus sp. 10 µM 9.0 Prazosin 0.69 203100
Adrenergic alpha1B ADRA1B Rattus sp. 10 µM -2.0 Prazosin 0.27 203200
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM 1.0 Prazosin 0.88 203400
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM 6.0 Yohimbine 8.40 203620
Adrenergic alpha2B ADRA2B Homo sapiens 10 µM 2.0 Yohimbine 14.00 203710
Adrenergic alpha2C ADRA2C Homo sapiens 10 µM 14.0 Yohimbine 75.00 203800
Adrenergic beta1 ADRB1 Homo sapiens 10 µM -7.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM 16.0 S(-)-Propranolol 0.78 204110
Adrenergic beta3 ADRB3 Homo sapiens 10 µM 21.0 Alprenolol 180.00 204200
Adrenomedullin AM1 ADM Homo sapiens 10 µM -8.0 Adrenomedullin 0.10 204460
Androgen (Testosterone) AR AR Rattus sp. 10 µM 9.0 Testosterone 6.50 285010
Angiotensin AT1 AGTR1 Homo sapiens 10 µM 8.0 Saralasin 0.92 210030
Atrial Natriuretic Factor (ANF) Cavia porcellus 10 µM -2.0 ANF (rat) 0.40 211000
Bradykinin B1 BDKRB1 Homo sapiens 10 µM 8.0 212510
Bradykinin B2 BDKRB2 Homo sapiens 10 µM 7.0 Bradykinin 1.80 212620
Cannabinoid CB1 CNR1 Homo sapiens 10 µM 20.0 R(+)-WIN-55,212-2 200.00 217030
Cannabinoid CB2 CNR2 Homo sapiens 10 µM 2.0 R(+)-WIN-55,212-2 5.80 217100
Chemokine CCR1 CCR1 Homo sapiens 10 µM -3.0 MCP-3 0.27 217510
Chemokine CXCR2 (IL-8RB) CXCR2 Homo sapiens 10 µM 1.0 IL-8 0.18 244500
Chemokine CXCR4 CXCR4 Homo sapiens 10 µM 3.0 SDF-1alpha 0.12 244550
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM -4.0 Devazepide (L-364,718) 0.18 218020
Cholecystokinin CCK2 (CCKB) CCKBR Homo sapiens 10 µM 15.0 Sincalide 0.06 218130
Corticotropin Releasing Factor CRF1 CRHR1 Homo sapiens 10 µM 6.0 Sauvagine (frog) 0.85 219150
Dopamine D1 DRD1 Homo sapiens 10 µM 12.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2S DRD2 Homo sapiens 10 µM 11.0 Spiperone 0.25 219700
Endothelin ETA EDNRA Homo sapiens 10 µM 23.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM -1.0 Endothelin-1 0.13 224110
Estrogen ERalpa ESR1 Homo sapiens 10 µM 8.0 Diethylstilbestrol 0.77 226010
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 35.0 Picrotoxin 270.00 226810
GABAA, Ro-15-1788, Hippocampus Rattus sp. 10 µM 1.0 Diazepam 46.00 226630
GABAB, Non-Selective GABBR1 Rattus sp. 10 µM -3.0 CGP-546Z6 1.80 228510
Glucocorticoid NR3C1 Homo sapiens 10 µM 19.0 Dexamethasone 3.80 232030
Glutamate, AMPA Rattus sp. 10 µM -2.0 L-Glutamic acid 320.00 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 12.0 L-Glutamic acid 240.00 232700
Glutamate, Metabotropic, mGlu5 GRM5 Homo sapiens 10 µM 0.0 L-Glutamic acid 1500.00 237000
Glutamate, NMDA, Agonism Rattus sp. 10 µM 5.0 L-Glutamic acid 410.00 232810
Glutamate, NMDA, Glycine Rattus sp. 10 µM 4.0 MDL 105,519 22.00 232910
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM -1.0 Dizolcipine ((+)-MK- 801) 5.10 233000
Glutamate, NMDA, Polyamine Rattus sp. 10 µM 19.0 Ifenprodil 23.00 234000
Glycine, Strychnine-Sensitive Rattus sp. 10 µM -22.0 (-)-Strychnine 8.90 239000
Histamine H1 HRH1 Homo sapiens 10 µM -4.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM 2.0 Tiotidine 22.00 239710
Histamine H3 HRH3 Homo sapiens 10 µM -12.0 R(-)-alpha-Methylhistamine (RAMH) 2.30 239820
Histamine H4 HRH4 Homo sapiens 10 µM -4.0 Histamine 13.00 239900
Leukotriene, Cysteinyl CysLT2 CYSLTR2 Homo sapiens 10 µM -20.0 LTC4 4.10 250480
Melanin-Concentrating Hormone MCH1 (SLC1) MCHR1 Homo sapiens 10 µM 1.0 MCH (human, mouse, rat) 0.67 251010
Melanocortin MC1 MC1R Homo sapiens 10 µM -1.0 NDP-alpha-MSH 0.06 251100
Melanocortin MC3 MC3R Homo sapiens 10 µM -2.0 NDP-alpha-MSH 0.15 251300
Melanocortin MC4 MC4R Homo sapiens 10 µM -6.0 NDP-alpha-MSH 0.22 251350
Melanocortin MC5 MC5R Homo sapiens 10 µM -3.0 NDP-alpha-MSH 0.48 251400
Muscarinic M1 CHRM1 Homo sapiens 10 µM 12.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 0.01 µM 11.0 6.42 2.70 4-DAMP 55.00 252710
Muscarinic M3 CHRM3 Homo sapiens 10 µM 26.0 4-DAMP 5.10 252810
Muscarinic M4 CHRM4 Homo sapiens 10 µM 26.0 4-DAMP 15.00 252910
Muscarinic M5 CHRM5 Homo sapiens 10 µM -8.0 4-DAMP 3.20 253010
Neuropeptide Y Y1 NPY1R Homo sapiens 10 µM 0.0 Neuropeptide Y (human, rat) 0.22 257010
Neuropeptide Y Y2 NPY2R Homo sapiens 10 µM 1.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Neurotensin NT1 NTSR1 Homo sapiens 10 µM -2.0 Neurotensin 1.20 258010
Nicotinic Acetylcholine Homo sapiens 10 µM -12.0 Epibatidine 0.08 258590
Nicotinic Acetylcholine D1, Bungarotoxin CHRNA1 Homo sapiens 10 µM 6.0 alpha-Bungarotoxin 1.10 258700
Opiate kappa (OP2, KOP) OPRK1 Homo sapiens 10 µM 19.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 17.0 DAMGO 20.00 260410
Orphanin ORL1 OPRL1 Homo sapiens 10 µM 7.0 Orphanin-FQ 1.50 260600
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM 33.0 PAF 0.28 265010
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM 18.0 Glyburide 5.70 265600
PPARalpha PPARA Homo sapiens 10 µM 10.0 L-797773 6.10 800420
PPARgamma PPARG Homo sapiens 0.01 µM 6.0 6.52 1.19 L-797773 4.80 800440
Progesterone PR-B PGR Homo sapiens 10 µM 30.0 Progesterone 1.50 268020
Prostanoid EP1 PTGER1 Homo sapiens 10 µM 16.0 Prostaglandin E2 (PGE2) 1.60 268110
Prostanoid EP3 PTGER3 Homo sapiens 10 µM -4.0 Prostaglandin E2 (PGE2) 0.63 800020
Prostanoid FP PTGFR Homo sapiens 10 µM -11.0 Dinoprost 3.10 268510
Prostanoid IP PTGIR Homo sapiens 10 µM -9.0 268600
Purinergic P2Y Rattus sp. 10 µM -16.0 ATP 18.00 268810
Retinoid X Receptor RXRalpha RXRA Homo sapiens 10 µM 4.0 9-cis-Retinoic acid 11.00 269500
Serotonin (5-Hydroxytryptamine) 5-HT1A HTR1A Homo sapiens 10 µM -6.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT1B HTR1B Rattus sp. 10 µM 0.0 Serotonin (5-HT) 5.70 271200
Serotonin (5-Hydroxytryptamine) 5-HT2A HTR2A Homo sapiens 10 µM 6.0 Ketanserin 271650
Serotonin (5-Hydroxytryptamine) 5-HT2B HTR2B Homo sapiens 0.01 µM -7.0 1.17 0.75 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT2C HTR2C Homo sapiens 10 µM -7.0 SBZ4Z084 1.00 271800
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM -9.0 MDL-72222 11.00 271910
Serotonin (5-Hydroxytryptamine) 5-HT6 HTR6 Homo sapiens 10 µM 3.0 Methiothepin 2.80 272200
Somatostatin sst2 SSTR2 Homo sapiens 10 µM 13.0 Somatostatin-14 0.01 282700
Tachykinin NK1 TACR1 Homo sapiens 10 µM 22.0 L-703606 3.60 255520
Tachykinin NK2 TACR2 Homo sapiens 10 µM 27.0 MEN-10,376 110.00 255600
Thyrotropin Releasing Hormone (TRH) TRHR Rattus sp. 10 µM -14.0 TRH 120.00 286000
Transporter, Adenosine Cavia porcellus 0.01 µM 2.0 9.70 3.32 Nitrobenzylthioinosine 0.85 202000
Transporter, Choline SLC5A7 Rattus sp. 10 µM 18.0 Hemicholinium-3 2.40 219000
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 16.0 GBR-1Z909 1.70 220320
Transporter, GABA Rattus sp. 10 µM 0.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 0.01 µM 6.0 3.82 3.79 Desipramine 0.93 204410
Transporter, Serotonin (5-Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 2.0 Fluoxetine 8.60 274030
Vasoactive Intestinal Peptide VIP1 VIPR1 Homo sapiens 10 µM 3.0 VIP 0.13 287010
Vasopressin V1A AVPR1A Homo sapiens 10 µM -9.0 (Arg8)-Vasopressin 0.33 287530
Vasopressin V1B AVPR1B Homo sapiens 10 µM 1.0 (Arg8)-Vasopressin 0.66 287560
Vasopressin V2 AVPR2 Homo sapiens 10 µM 9.0 (Arg8)-Vasopressin 4.50 287610
 

MLi-2

Results are significant for > 50 % inhibition. Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQTM (ID Business Solutions Ltd., UK).

Conclusion: No significant inhibition was found for the tested targets.

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [µM] Assay ID
Cholinesterase, Acetyl, ACES ACHE Homo sapiens 10 µM -2.0 Physostigmine 0.12 104010
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM 9.0 Indomethacin 0.04 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM -20.0 Rofecoxib 0.17 118010
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 2.0 Clorgyline 0.00 140010
Monoamine Oxidase MAO-B MAOB Homo sapiens 10 µM 28.0 R(-)-Deprenyl 0.01 140120
Peptidase, CASP3 (Caspase 3) CASP3 Homo sapiens 10 µM 12.0 Ac-DEVD-CHO 0.00 163200
Peptidase, CASP8 (Caspase 8) CASP8 Homo sapiens 10 µM 7.0 Ac-IETD-CHO 0.01 163500
Peptidase, CASP9 (Caspase 9) CASP9 Homo sapiens 10 µM 5.0 Z-LEHD-FMK 0.07 163600
Peptidase, CTSG (Cathepsin G) CTSG Homo sapiens 10 µM 9.0 Chymostatin 2.10 112510
Phosphodiesterase PDE3 Homo sapiens 10 µM 21.0 Cilostamide 0.05 152000
Protein Serine/Threonine Kinase, MAPK14 (p38α) MAPK14 Homo sapiens 10 µM 19.0 SB 202190 0.02 176610
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 10 µM 33.0 Staurosporine 1.60 171000
Protein Serine/Threonine Kinase, MARK3 MARK3 Homo sapiens 10 µM 11.0 Hymenialdisine 0.08 171315
Protein Serine/Threonine Kinase, PKA, Non-Selective Bos taurus 10 µM 16.0 H-7 3.60 177000
Protein Serine/Threonine Kinase, PKC, Non-Selective Rattus sp. 10 µM 26.0 Staurosporine 0.00 178010
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM -14.0 170020
Protein Tyrosine Kinase, Insulin Receptor INSR Homo sapiens 10 µM 9.0 GSK 1838705 0.01 174990
Tyrosine Hydroxylase TH Rattus sp. 10 µM -19.0 alpha-Methyl-L-P-Tyrosine 20.00 195000
 

MLi-2

Results are expressed as percent inhibition.

Conclusion: Clean panel: Closest off-target is CLK4 with IC50 = 255 nM.

Target protein HGNC name Species % Inhibition at 1 µM IC50 [nM]
ABL1 Y253F ABL1 7.3
ABL1 ABL1 1.1
ABL1 E255K ABL1 4.4
ABL1 G250E ABL1 4.5
ABL1 T315I ABL1 9.3
ABL2 (Arg) ABL2 0.9
ACVR1 (ALK2) ACVR1 10.7
ACVR1B (ALK4) ACVR1B -0.7
ACVR2B ACVR2B -1.2
ADRBK1 (GRK2) GRK2 3.8
ADRBK2 (GRK3) GRK3 -0.2
AKT1 (PKB alpha) AKT1 6.8
AKT2 (PKB beta) AKT2 5.5
AKT3 (PKB gamma) AKT3 7.7
AMPK A1/B1/G1 PRKAA1 -3.8
AMPK A2/B1/G1 PRKAA2 5.7
AURKA (Aurora A) AURKA -0.2
AURKB (Aurora B) AURKB 16.2
AURKC (Aurora C) AURKC 1.9
AXL AXL 4.8
BLK BLK 8.2
BMPR1A (ALK3) BMPR1A 0.8
BMX BMX 14.0
BRAF BRAF 27.1
BRAF V599E BRAF 10.4
BRSK1 (SAD1) BRSK1 4.8
BTK BTK 4.5
CAMK1 (CaMK1) CAMK1 -4.0
CAMK1D (CaMKI delta) CAMK1D 17.4
CAMK2A (CaMKII alpha) CAMK2A 8.0
CAMK2B (CaMKII beta) CAMK2B 12.6
CAMK2D (CaMKII delta) CAMK2D 23.9
CAMK4 (CaMKIV) CAMK4 -20.0
CAMKK1 (CAMKKA) CAMKK1 12.6
CAMKK2 (CaMKK beta) CAMKK2 19.8
CDC42 BPA (MRCKA) CDC42BPA 2.5
CDC42 BPB (MRCKB) CDC42BPB 4.3
CDK1/cyclin B CDK1 1.3
CDK2/cyclin A CDK2 1.1
CDK5/p25 CDK5 -2.7
CDK5/p35 CDK5 -0.5
CDK7/cyclin H/MNAT1 CDK7 -16.5
CDK8/cyclin C CDK8 8.8
CDK9/cyclin K CDK9 -2.2
CDK9/cyclin T1 CDK9 11.3
CHEK1 (CHK1) CHEK1 -0.2
CHEK2 (CHK2) CHEK2 14.9
CHUK (IKK alpha) CHUK 8.2
CLK1 CLK1 15.7
CLK2 CLK2 55.0 605.00
CLK3 CLK3 8.9
CLK4 CLK4 80.1 225.00
CSF1R (FMS) CSF1R 6.9
CSK CSK 5.5
CSNK1A1 (CK1 alpha 1) CSNK1A1 1.9
CSNK1D (CK1 delta) CSNK1D 1.0
CSNK1E (CK1 epsilon) CSNK1E 8.1
CSNK1G1 (CK1 gamma 1) CSNK1G1 -1.8
CSNK1G2 (CK1 gamma 2) CSNK1G2 2.4
CSNK1G3 (CK1 gamma 3) CSNK1G3 2.2
CSNK2A1 (CK2 alpha 1) CSNK2A1 3.5
CSNK2A2 (CK2 alpha 2) CSNK2A2 10.5
DAPK1 DAPK1 -0.6
DAPK3 (ZIPK) DAPK3 5.3
DCAMKL2 (DCK2) DCLK2 5.6
DDR1 DDR1 0.9
DDR2 DDR2 3.6
DMPK DMPK 5.7
DNA-PK PRKDC 21.6
DYRK1A DYRK1A 4.4
DYRK1B DYRK1B 1.8
DYRK3 DYRK3 2.5
DYRK4 DYRK4 1.7
EEF2K EEF2K 4.3
EGFR (ErbB1) EGFR -0.8
EGFR (ErbB1) L858R EGFR -0.5
EGFR (ErbB1) L861Q EGFR 9.2
EGFR (ErbB1) T790M EGFR 3.9
EGFR (ErbB1) T790M L858R EGFR 2.4
EPHA1 EPHA1 7.8
EPHA2 EPHA2 -4.3
EPHA3 EPHA3 -3.3
EPHA4 EPHA4 4.8
EPHA5 EPHA5 5.1
EPHA7 EPHA7 8.1
EPHA8 EPHA8 7.4
EPHB1 EPHB1 3.5
EPHB2 EPHB2 -1.1
EPHB3 EPHB3 9.9
EPHB4 EPHB4 2.2
ERBB2 (HER2) ERBB2 -2.5
ERBB4 (HER4) ERBB4 11.9
FER FER 26.7
FES (FPS) FES 6.0
FGFR1 FGFR1 3.9
FGFR2 FGFR2 -3.3
FGFR3 FGFR3 9.4
FGFR3 K650E FGFR3 3.4
FGFR4 FGFR4 14.8
FGR FGR -2.2
FLT1 (VEGFR1) FLT1 -1.0
FLT3 FLT3 2.5
FLT3 D835Y FLT3 9.6
FLT4 (VEGFR3) FLT4 8.7
FRAP1 (mTOR) MTOR 7.1
FRK (PTK5) FRK 7.1
FYN FYN 11.2
GRK4 GRK4 6.0
GRK5 GRK5 0.1
GRK6 GRK6 6.6
GRK7 GRK7 4.4
GSG2 (Haspin) HASPIN -10.4
GSK3A (GSK3 alpha) GSK3A 0.0
GSK3B (GSK3 beta) GSK3B 3.5
HCK HCK 7.7
HIPK1 (Myak) HIPK1 3.1
HIPK2 HIPK2 5.3
HIPK4 HIPK4 6.2
IGF1R IGF1R 2.0
IKBKB (IKK beta) IKBKB 0.0
IKBKE (IKK epsilon) IKBKE 1.8
INSR INSR -0.9
INSRR (IRR) INSRR 21.1
IRAK1 IRAK1 -14.9
IRAK4 IRAK4 -13.9
ITK ITK 2.0
JAK1 JAK1 -2.5
JAK2 JAK2 5.8
JAK2 JH1 JH2 JAK2 -4.3
JAK2 JH1 JH2 V617F JAK2 -7.8
JAK3 JAK3 7.1
KDR (VEGFR2) KDR 3.6
KIT KIT 5.5
KIT T670I KIT -0.7
KIT V654A KIT 1.1
LCK LCK 10.4
LIMK1 LIMK1 11.0
LIMK2 LIMK2 0.6
LRRK2 LRRK2 95.8
MAP2K1 (MEK1) S218D S222D LRRK2 97.2
LTK (TYK1) LTK 42.4
LYN A LYN 1.1
LYN B LYN 3.9
MAP2K1 (MEK1) MAP2K1 8.3
MAP2K1 (MEK1) S218D S222D MAP2K1 6.9
MAP2K2 (MEK2) MAP2K2 20.3
MAP2K3 (MEK3) MAP2K3 -2.3
MAP2K6 (MKK6) MAP2K6 -2.7
MAP2K6 (MKK6) S207E T211E MAP2K6 -2.0
MAP3K10 (MLK2) MAP3K10 0.7
MAP3K11 (MLK3) MAP3K11 -3.7
MAP3K14 (NIK) MAP3K14 78.8 244.00
MAP3K2 (MEKK2) MAP3K2 7.6
MAP3K3 (MEKK3) MAP3K3 -0.7
MAP3K5 (ASK1) MAP3K5 71.9 428.00
MAP3K7/MAP3K7IP1 (TAK1-TAB1) MAP3K7 -4.4
MAP3K8 (COT) MAP3K8 16.3
MAP3K9 (MLK1) MAP3K9 27.3
MAP4K2 (GCK) MAP4K2 30.9
MAP4K4 (HGK) MAP4K4 17.1
MAP4K5 (KHS1) MAP4K5 3.3
MAPK1 (ERK2) MAPK1 -4.0
MAPK10 (JNK3) MAPK10 13.6
MAPK11 (p38 beta) MAPK11 13.0
MAPK12 (p38 gamma) MAPK12 1.0
MAPK13 (p38 delta) MAPK13 4.3
MAPK14 (p38 alpha) MAPK14 -6.5
MAPK14 (p38 alpha) Direct MAPK14 8.1
MAPK3 (ERK1) MAPK3 18.7
MAPK8 (JNK1) MAPK8 -0.1
MAPK9 (JNK2) MAPK9 19.7
MAPKAPK2 MAPKAPK2 2.4
MAPKAPK3 MAPKAPK3 3.7
MAPKAPK5 (PRAK) MAPKAPK5 14.2
MARK1 (MARK) MARK1 8.4
MARK2 MARK2 7.8
MARK3 MARK3 1.6
MARK4 MARK4 15.6
MATK (HYL) MATK 3.3
MELK MELK 5.4
MERTK (cMER) MERTK 4.8
MET (cMet) MET 5.5
MET M1250T MET 2.2
MINK1 MINK1 4.6
MKNK1 (MNK1) MKNK1 -3.2
MKNK2 (MNK2) MKNK2 9.3
MLCK (MLCK2) MYLK2 1.7
MST1R (RON) MST1R 1.5
MST4 STK26 6.9
MUSK MUSK 0.0
MYLK (MLCK) MYLK 10.9
MYLK2 (skMLCK) MYLK2 1.4
NEK1 NEK1 3.5
NEK2 NEK2 -2.6
NEK4 NEK4 6.4
NEK6 NEK6 4.8
NEK7 NEK7 3.7
NEK9 NEK9 -1.0
NLK NLK 4.5
NTRK1 (TRKA) NTRK1 0.8
NTRK2 (TRKB) NTRK2 7.0
NTRK3 (TRKC) NTRK3 14.9
NUAK1 (ARK5) NUAK1 14.5
PAK1 PAK1 6.8
PAK2 (PAK65) PAK2 8.7
PAK3 PAK3 10.9
PAK4 PAK4 -7.3
PAK6 PAK6 1.7
PAK7 (KIAA1264) PAK5 6.0
PASK PASK -0.1
PDGFRA (PDGFR alpha) PDGFRA 0.4
PDGFRA D842V PDGFRA 3.5
PDGFRA T674I PDGFRA 23.5
PDGFRA V561D PDGFRA 8.1
PDGFRB (PDGFR beta) PDGFRB 6.4
PDK1 PDK1 13.6
PDK1 Direct PDK1 -2.4
PHKG1 PHKG1 0.8
PHKG2 PHKG2 1.9
PI4KA (PI4K alpha) PI4KA 5.4
PI4KB (PI4K beta) PI4KB 1.5
PIK3C2A (PI3K-C2 alpha) PIK3C2A -0.7
PIK3C2B (PI3K-C2 beta) PIK3C2B -3.3
PIK3C3 (hVPS34) PIK3C3 19.4
PIK3CA/PIK3R1 (p110 alpha/p85 alpha) PIK3CA 3.2
PIK3CD/PIK3R1 (p110 delta/p85 alpha) PIK3CD 2.1
PIK3CG (p110 gamma) PIK3CG -12.0
PIM1 PIM1 -2.7
PIM2 PIM2 -1.9
PKN1 (PRK1) PKN1 1.5
PLK1 PLK1 7.5
PLK2 PLK2 12.7
PLK3 PLK3 4.9
PRKACA (PKA) PRKACA -2.3
PRKCA (PKC alpha) PRKCA -4.1
PRKCB1 (PKC beta I) PRKCB -7.7
PRKCB2 (PKC beta II) PRKCB 10.4
PRKCD (PKC delta) PRKCD 3.6
PRKCE (PKC epsilon) PRKCE 4.4
PRKCG (PKC gamma) PRKCG 1.2
PRKCH (PKC eta) PRKCH 6.4
PRKCI (PKC iota) PRKCI -0.5
PRKCN (PKD3) PRKD3 21.1
PRKCQ (PKC theta) PRKCQ 2.5
PRKCZ (PKC zeta) PRKCZ -4.0
PRKD1 (PKC mu) PRKD1 13.3
PRKD2 (PKD2) PRKD2 19.0
PRKG1 PRKG1 0.2
PRKG2 (PKG2) PRKG2 1.2
PRKX PRKX 1.5
PTK2 (FAK) PTK2 14.2
PTK2B (FAK2) PTK2B 2.5
PTK6 (Brk) PTK6 2.7
RAF1 (cRAF) Y340D Y341D RAF1 3.0
RET RET 5.8
RET V804L RET 5.7
RET Y791F RET 5.3
RIPK2 RIPK2 0.0
ROCK1 ROCK1 -0.9
ROCK2 ROCK2 10.2
ROS1 ROS1 2.5
RPS6KA1 (RSK1) RPS6KA1 8.7
RPS6KA2 (RSK3) RPS6KA2 7.5
RPS6KA3 (RSK2) RPS6KA3 3.9
RPS6KA4 (MSK2) RPS6KA4 7.7
RPS6KA5 (MSK1) RPS6KA5 0.4
RPS6KA6 (RSK4) RPS6KA6 3.2
RPS6KB1 (p70S6K) RPS6KB1 5.3
SGK (SGK1) SGK1 -1.6
SGK2 SGK2 1.4
SGKL (SGK3) SGK3 0.2
SLK SLK 1.5
SNF1LK2 SIK2 7.1
SPHK1 SPHK1 -15.8
SPHK2 SPHK2 -0.7
SRC SRC 5.0
SRC N1 SRC 5.8
SRMS (Srm) SRMS 11.0
SRPK1 SRPK1 6.2
SRPK2 SRPK2 0.8
STK16 (PKL12) STK16 2.6
STK17A (DRAK1) STK17A -2.3
STK22B (TSSK2) TSSK2 10.2
STK22D (TSSK1) TSSK3 15.8
STK23 (MSSK1) SRPK3 12.0
STK24 (MST3) STK24 7.3
STK25 (YSK1) STK25 2.2
STK3 (MST2) STK3 11.9
STK33 STK33 24.3
STK4 (MST1) STK4 21.8
SYK SYK 2.8
TAOK2 (TAO1) TAOK2 -2.7
TAOK3 (JIK) TAOK3 0.4
TBK1 TBK1 7.8
TEC TEC -2.1
TEK (Tie2) TEK 2.4
TGFBR1 (ALK5) TGFBR1 0.9
TNK2 (ACK) TNK2 22.9
TTK TTK 56.5 935.00
TXK TXK 3.1
TYK2 TYK2 1.2
TYRO3 (RSE) TYRO3 6.1
WEE1 WEE1 3.0
WNK2 WNK2 -1.7
YES1 YES1 5.8
ZAK MAP3K20 4.3
ZAP70 ZAP70 10.2