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Selectivity data for probe MSD-M1PAM and control MSD-M1PAM-NC


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MSD-M1PAM


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT7A HTR7 -26.97 > 10000.00 < 5.00
Alpha2A ADRA2A -25.74
Alpha2B ADRA2B -6.86
D3 DRD3 -7.39
H1 HRH1 28.43
H4 HRH4 -11.40
M1 CHRM1 -1.00
M3 CHRM3 -6.58
M4 CHRM4 -2.36
M5 CHRM5 4.74
Sigma 2 TMEM97 5.17
5-HT1A HTR1A 21.04
5-HT1B HTR1B 2.72
5-HT1E HTR1E -10.11
5-HT2A HTR2A -16.96
5-HT2B HTR2B 3.23
5-HT2C HTR2C 10.49
Alpha1A ADRA1A -33.20
Alpha1B ADRA1B 6.68
Alpha1D ADRA1D -5.73
M2 CHRM2 -8.07
5-HT5A HTR5A -20.02
5-HT6 HTR6 -20.04
Alpha2C ADRA2C -13.95
D1 DRD1 -10.73
D2 DRD2 -16.84
GABAA 20.16
H3 HRH3 4.08
NET SLC6A2 24.71
Sigma 1 SIGMAR1 29.12
D4 DRD4 -8.33
D5 DRD5 -2.87
DOR OPRD1 -20.87
KOR OPRK1 47.32
GABA/PBR 7.88
5-HT1D HTR1D -4.55
5-HT3 HTR3A 12.00
Beta2 ADRB2 13.90
MOR OPRM1 18.49
Beta3 ADRB3 -5.05
Beta1 ADRB1 16.22
DAT SLC6A3 -7.27
H2 HRH2 11.73
SERT SLC6A4 19.01
GABAA/BZP 8.92

MSD-M1PAM-NC


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABAA/BZP 21.76
Beta1 ADRB1 -5.76
Beta2 ADRB2 15.77
Beta3 ADRB3 17.43
DAT SLC6A3 18.60
H2 HRH2 3.10
SERT SLC6A4 -12.04
MOR OPRM1 34.99
5-HT3 HTR3A 6.59
D4 DRD4 -8.64
D5 DRD5 -18.34
DOR OPRD1 -0.84
KOR OPRK1 46.83
GABA/PBR 46.49
5-HT5A HTR5A -19.81
D1 DRD1 -15.09
D2 DRD2 -5.66
GABAA 23.19
H3 HRH3 11.22
NET SLC6A2 40.55
Sigma 1 SIGMAR1 16.27
5-HT1A HTR1A 26.72
5-HT1B HTR1B 13.03
5-HT1D HTR1D 14.60
5-HT1E HTR1E -3.26
5-HT2A HTR2A -15.68
5-HT2B HTR2B 5.44
5-HT2C HTR2C -2.49
Alpha1A ADRA1A -26.36
Alpha1B ADRA1B 1.36
Alpha1D ADRA1D -10.25
5-HT6 HTR6 2.79
5-HT7A HTR7 -22.82
Alpha2A ADRA2A -15.67
Alpha2B ADRA2B -2.99
Alpha2C ADRA2C 1.13
D3 DRD3 -12.76
H1 HRH1 9.70
H4 HRH4 -13.53
M1 CHRM1 -2.01
M2 CHRM2 -14.00
M3 CHRM3 -12.89
M4 CHRM4 -8.87
M5 CHRM5 0.56
Sigma 2 TMEM97 24.14

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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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MSD-M1PAM


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 96.0 1000
ACVR1B ACVR1B 94.0 1000
ACVR2A ACVR2A 95.0 1000
ACVR2B ACVR2B 97.0 1000
ACVRL1 ACVRL1 95.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 90.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 73.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 68.0 1000
NUAK1 ARK5 98.0 1000
MAP3K5 ASK1 75.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 76.0 1000
AURKC AURKC 94.0 1000
AXL AXL 91.0 1000
BMP2K BIKE 95.0 1000
BLK BLK 49.0 1000
BMPR1A BMPR1A 97.0 1000
BMPR1B BMPR1B 67.0 1000
BMPR2 BMPR2 89.0 1000
BMX BMX 88.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 76.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 83.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 84.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 98.0 1000
CDK19 CDK11 82.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 99.0 1000
CDK4 CDK4-cyclinD3 82.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 58.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 99.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 89.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 87.0 1000
CIT CIT 98.0 1000
CLK1 CLK1 80.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 100.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 96.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 91.0 1000
CSNK1G3 CSNK1G3 93.0 1000
CSNK2A1 CSNK2A1 86.0 1000
CSNK2A2 CSNK2A2 86.0 1000
MATK CTK 84.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 99.0 1000
DAPK3 DAPK3 95.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 89.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 93.0 1000
DMPK DMPK 97.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 97.0 1000
DYRK1B DYRK1B 98.0 1000
DYRK2 DYRK2 95.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 86.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 83.0 1000
EPHA3 EPHA3 75.0 1000
EPHA4 EPHA4 79.0 1000
EPHA5 EPHA5 89.0 1000
EPHA6 EPHA6 86.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 92.0 1000
EPHB4 EPHB4 83.0 1000
EPHB6 EPHB6 73.0 1000
ERBB2 ERBB2 96.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 72.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 94.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 81.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 99.0 1000
FGFR1 FGFR1 98.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 94.0 1000
FLT1 FLT1 92.0 1000
FLT3 FLT3-autoinhibited 80.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 99.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 84.0 1000
GRK2 GRK2 93.0 1000
GRK3 GRK3 95.0 1000
GRK4 GRK4 68.0 1000
GRK7 GRK7 77.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 100.0 1000
HIPK2 HIPK2 66.0 1000
HIPK3 HIPK3 84.0 1000
HIPK4 HIPK4 95.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 75.0 1000
IGF1R IGF1R 89.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 88.0 1000
INSR INSR 74.0 1000
INSRR INSRR 97.0 1000
IRAK1 IRAK1 77.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 83.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 84.0 1000
JAK2 JAK2(JH1domain-catalytic) 96.0 1000
JAK3 JAK3(JH1domain-catalytic) 95.0 1000
MAPK8 JNK1 85.0 1000
MAPK9 JNK2 83.0 1000
MAPK10 JNK3 82.0 1000
KIT KIT-autoinhibited 87.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 95.0 1000
LCK LCK 97.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 100.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 78.0 1000
MAK MAK 97.0 1000
MAP3K1 MAP3K1 98.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 76.0 1000
MAP3K3 MAP3K3 77.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 81.0 1000
MAP4K3 MAP4K3 80.0 1000
MAP4K4 MAP4K4 87.0 1000
MAP4K5 MAP4K5 87.0 1000
MAPKAPK2 MAPKAPK2 75.0 1000
MAPKAPK5 MAPKAPK5 56.0 1000
MARK1 MARK1 94.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 98.0 1000
MAST1 MAST1 50.0 1000
MAP2K1 MEK1 95.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 73.0 1000
MAP2K4 MEK4 85.0 1000
MAP2K5 MEK5 62.0 1000
MAP2K6 MEK6 99.0 1000
MELK MELK 55.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 99.0 1000
MINK1 MINK 92.0 1000
MAP2K7 MKK7 95.0 1000
MKNK1 MKNK1 85.0 1000
MKNK2 MKNK2 85.0 1000
MYLK3 MLCK 87.0 1000
MAP3K9 MLK1 92.0 1000
MAP3K10 MLK2 97.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 96.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 98.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 90.0 1000
MUSK MUSK 96.0 1000
MYLK MYLK 87.0 1000
MYLK2 MYLK2 94.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 93.0 1000
STK38L NDR2 80.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 93.0 1000
NEK11 NEK11 89.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 66.0 1000
NEK4 NEK4 100.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 73.0 1000
NIM1K NIM1 69.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 79.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 78.0 1000
PAK1 PAK1 86.0 1000
PAK2 PAK2 77.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 96.0 1000
CDK16 PCTK1 67.0 1000
CDK17 PCTK2 96.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 90.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 88.0 1000
PK5 PFPK5(P.falciparum) 68.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 97.0 1000
PIK3C2G PIK3C2G 97.0 1000
PIK3CA PIK3CA(Q546K) 58.0 1000
PIK3CB PIK3CB 36.0 1000
PIK3CD PIK3CD 91.0 1000
PIK3CG PIK3CG 91.0 1000
PI4KB PIK4CB 74.0 1000
PIKFYVE PIKFYVE 97.0 1000
PIM1 PIM1 99.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 89.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 99.0 1000
PRKACA PKAC-alpha 88.0 1000
PRKACB PKAC-beta 92.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 88.0 1000
PLK1 PLK1 70.0 1000
PLK2 PLK2 80.0 1000
PLK3 PLK3 85.0 1000
PLK4 PLK4 90.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 96.0 1000
PRKD1 PRKD1 87.0 1000
PRKD2 PRKD2 99.0 1000
PRKD3 PRKD3 98.0 1000
PRKG1 PRKG1 98.0 1000
PRKG2 PRKG2 95.0 1000
EIF2AK2 PRKR 95.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 97.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 92.0 1000
RIOK1 RIOK1 88.0 1000
RIOK2 RIOK2 92.0 1000
RIOK3 RIOK3 96.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 92.0 1000
RIPK4 RIPK4 80.0 1000
DSTYK RIPK5 75.0 1000
ROCK1 ROCK1 86.0 1000
ROCK2 ROCK2 85.0 1000
ROS1 ROS1 90.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 65.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 83.0 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) 97.0 1000
RPS6KB1 S6K1 96.0 1000
SBK1 SBK1 83.0 1000
SGK1 SGK 87.0 1000
SBK3 SgK110 72.0 1000
SGK2 SGK2 86.0 1000
SGK3 SGK3 74.0 1000
SIK1 SIK 92.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 99.0 1000
NUAK2 SNARK 77.0 1000
SNRK SNRK 76.0 1000
SRC SRC 100.0 1000
SRMS SRMS 93.0 1000
SRPK1 SRPK1 100.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 95.0 1000
STK16 STK16 100.0 1000
STK33 STK33 56.0 1000
STK35 STK35 94.0 1000
STK36 STK36 100.0 1000
STK39 STK39 56.0 1000
SYK SYK 92.0 1000
MAP3K7 TAK1 90.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 97.0 1000
TAOK3 TAOK3 78.0 1000
TBK1 TBK1 98.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 41.0 1000
TGFBR2 TGFBR2 93.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 95.0 1000
TLK1 TLK1 97.0 1000
TLK2 TLK2 98.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 93.0 1000
TNK2 TNK2 99.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 88.0 1000
NTRK2 TRKB 84.0 1000
NTRK3 TRKC 70.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 74.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 88.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 93.0 1000
TYRO3 TYRO3 98.0 1000
ULK1 ULK1 76.0 1000
ULK2 ULK2 93.0 1000
ULK3 ULK3 89.0 1000
KDR VEGFR2 79.0 1000
PIK3C3 VPS34 70.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 99.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 97.0 1000
WNK2 WNK2 79.0 1000
WNK3 WNK3 99.0 1000
WNK4 WNK4 75.0 1000
STK32A YANK1 90.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 72.0 1000
YES1 YES 94.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 77.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 100.0 1000

MSD-M1PAM-NC


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 89.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 83.0 1000
ACVR1B ACVR1B 69.0 1000
ACVR2A ACVR2A 78.0 1000
ACVR2B ACVR2B 75.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 85.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 91.0 1000
AKT2 AKT2 84.0 1000
AKT3 AKT3 74.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 79.0 1000
NUAK1 ARK5 86.0 1000
MAP3K5 ASK1 80.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 90.0 1000
AURKB AURKB 92.0 1000
AURKC AURKC 88.0 1000
AXL AXL 78.0 1000
BMP2K BIKE 92.0 1000
BLK BLK 73.0 1000
BMPR1A BMPR1A 74.0 1000
BMPR1B BMPR1B 95.0 1000
BMPR2 BMPR2 92.0 1000
BMX BMX 84.0 1000
BRAF BRAF(V600E) 99.0 1000
PTK6 BRK 82.0 1000
BRSK1 BRSK1 87.0 1000
BRSK2 BRSK2 77.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 90.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 84.0 1000
CAMK2B CAMK2B 89.0 1000
CAMK2D CAMK2D 97.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 96.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 100.0 1000
CDK11B CDC2L1 80.0 1000
CDK11A CDC2L2 93.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 75.0 1000
CDK2 CDK2 86.0 1000
CDK3 CDK3 79.0 1000
CDK4 CDK4-cyclinD3 98.0 1000
CDK5 CDK5 92.0 1000
CDK7 CDK7 82.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 88.0 1000
CDKL1 CDKL1 78.0 1000
CDKL2 CDKL2 93.0 1000
CDKL3 CDKL3 78.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 90.0 1000
CHEK2 CHEK2 92.0 1000
CIT CIT 99.0 1000
CLK1 CLK1 85.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 99.0 1000
CLK4 CLK4 97.0 1000
CSF1R CSF1R-autoinhibited 86.0 1000
CSK CSK 91.0 1000
CSNK1A1 CSNK1A1 79.0 1000
CSNK1A1L CSNK1A1L 91.0 1000
CSNK1D CSNK1D 74.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 79.0 1000
CSNK1G2 CSNK1G2 76.0 1000
CSNK1G3 CSNK1G3 76.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 98.0 1000
MATK CTK 76.0 1000
DAPK1 DAPK1 89.0 1000
DAPK2 DAPK2 94.0 1000
DAPK3 DAPK3 86.0 1000
DCLK1 DCAMKL1 91.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 85.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 90.0 1000
CDC42BPG DMPK2 88.0 1000
STK17A DRAK1 96.0 1000
STK17B DRAK2 93.0 1000
DYRK1A DYRK1A 94.0 1000
DYRK1B DYRK1B 53.0 1000
DYRK2 DYRK2 100.0 1000
EGFR EGFR(T790M) 90.0 1000
EIF2AK1 EIF2AK1 83.0 1000
EPHA1 EPHA1 83.0 1000
EPHA2 EPHA2 86.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 89.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 91.0 1000
EPHB2 EPHB2 77.0 1000
EPHB3 EPHB3 90.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 95.0 1000
ERBB3 ERBB3 93.0 1000
ERBB4 ERBB4 85.0 1000
MAPK3 ERK1 91.0 1000
MAPK1 ERK2 98.0 1000
MAPK6 ERK3 79.0 1000
MAPK4 ERK4 76.0 1000
MAPK7 ERK5 63.0 1000
MAPK15 ERK8 92.0 1000
ERN1 ERN1 100.0 1000
PTK2 FAK 89.0 1000
FER FER 89.0 1000
FES FES 99.0 1000
FGFR1 FGFR1 93.0 1000
FGFR2 FGFR2 91.0 1000
FGFR3 FGFR3(G697C) 98.0 1000
FGFR4 FGFR4 90.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 98.0 1000
FLT4 FLT4 86.0 1000
FRK FRK 80.0 1000
FYN FYN 83.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 78.0 1000
GRK1 GRK1 85.0 1000
GRK2 GRK2 82.0 1000
GRK3 GRK3 77.0 1000
GRK4 GRK4 86.0 1000
GRK7 GRK7 87.0 1000
GSK3A GSK3A 72.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 77.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 97.0 1000
HIPK4 HIPK4 67.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 79.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 88.0 1000
CHUK IKK-alpha 94.0 1000
IKBKB IKK-beta 99.0 1000
IKBKE IKK-epsilon 94.0 1000
INSR INSR 88.0 1000
INSRR INSRR 93.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 95.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 85.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 96.0 1000
MAPK9 JNK2 97.0 1000
MAPK10 JNK3 96.0 1000
KIT KIT-autoinhibited 100.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 93.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 98.0 1000
LIMK2 LIMK2 82.0 1000
STK11 LKB1 77.0 1000
STK10 LOK 95.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 90.0 1000
LYN LYN 99.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 93.0 1000
MAP3K1 MAP3K1 98.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 92.0 1000
MAP3K4 MAP3K4 90.0 1000
MAP4K2 MAP4K2 96.0 1000
MAP4K3 MAP4K3 81.0 1000
MAP4K4 MAP4K4 87.0 1000
MAP4K5 MAP4K5 75.0 1000
MAPKAPK2 MAPKAPK2 84.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 87.0 1000
MARK4 MARK4 90.0 1000
MAST1 MAST1 82.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 91.0 1000
MAP2K3 MEK3 81.0 1000
MAP2K4 MEK4 83.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 98.0 1000
MELK MELK 78.0 1000
MERTK MERTK 86.0 1000
MET MET(Y1235D) 97.0 1000
MINK1 MINK 89.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 96.0 1000
MYLK3 MLCK 76.0 1000
MAP3K9 MLK1 72.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 89.0 1000
CDC42BPA MRCKA 84.0 1000
CDC42BPB MRCKB 63.0 1000
STK4 MST1 88.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 92.0 1000
STK24 MST3 87.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 58.0 1000
MUSK MUSK 90.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 87.0 1000
MYLK4 MYLK4 95.0 1000
MYO3A MYO3A 80.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 64.0 1000
STK38L NDR2 90.0 1000
NEK1 NEK1 91.0 1000
NEK10 NEK10 96.0 1000
NEK11 NEK11 63.0 1000
NEK2 NEK2 95.0 1000
NEK3 NEK3 83.0 1000
NEK4 NEK4 88.0 1000
NEK5 NEK5 82.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 82.0 1000
NEK9 NEK9 99.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 95.0 1000
NLK NLK 92.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 86.0 1000
MAPK11 p38-beta 76.0 1000
MAPK13 p38-delta 89.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 93.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 82.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 97.0 1000
PDGFRB PDGFRB 86.0 1000
PDPK1 PDPK1 81.0 1000
CDPK1 PFCDPK1(P.falciparum) 84.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 85.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 85.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 73.0 1000
PIK3CA PIK3CA(Q546K) 94.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 61.0 1000
PIK3CG PIK3CG 75.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 76.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 77.0 1000
PIM3 PIM3 99.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 68.0 1000
PIP4K2B PIP5K2B 62.0 1000
PIP4K2C PIP5K2C 58.0 1000
PRKACA PKAC-alpha 88.0 1000
PRKACB PKAC-beta 54.0 1000
PKMYT1 PKMYT1 79.0 1000
PKN1 PKN1 91.0 1000
PKN2 PKN2 88.0 1000
PKNB PKNB(M.tuberculosis) 92.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 100.0 1000
PLK4 PLK4 87.0 1000
PRKCD PRKCD 95.0 1000
PRKCE PRKCE 79.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 87.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 95.0 1000
PRKD2 PRKD2 85.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 88.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 96.0 1000
PRPF4B PRP4 78.0 1000
PTK2B PYK2 86.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 95.0 1000
RIOK1 RIOK1 95.0 1000
RIOK2 RIOK2 95.0 1000
RIOK3 RIOK3 90.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 83.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 80.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 72.0 1000
ROS1 ROS1 97.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 90.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 86.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KB1 S6K1 34.0 1000
SBK1 SBK1 89.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 82.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 91.0 1000
SRC SRC 56.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 85.0 1000
SRPK2 SRPK2 84.0 1000
SRPK3 SRPK3 82.0 1000
STK16 STK16 100.0 1000
STK33 STK33 62.0 1000
STK35 STK35 96.0 1000
STK36 STK36 98.0 1000
STK39 STK39 75.0 1000
SYK SYK 92.0 1000
MAP3K7 TAK1 99.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 100.0 1000
TBK1 TBK1 99.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 90.0 1000
TGFBR1 TGFBR1 72.0 1000
TGFBR2 TGFBR2 93.0 1000
TIE1 TIE1 98.0 1000
TEK TIE2 85.0 1000
TLK1 TLK1 85.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 72.0 1000
TNK2 TNK2 85.0 1000
TNNI3K TNNI3K 89.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 93.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 80.0 1000
TSSK1B TSSK1B 98.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 98.0 1000
TXK TXK 91.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 78.0 1000
ULK1 ULK1 91.0 1000
ULK2 ULK2 92.0 1000
ULK3 ULK3 96.0 1000
KDR VEGFR2 92.0 1000
PIK3C3 VPS34 89.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 74.0 1000
WEE2 WEE2 91.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 94.0 1000
WNK4 WNK4 81.0 1000
STK32A YANK1 98.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 84.0 1000
STK25 YSK1 97.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 95.0 1000
ZAP70 ZAP70 100.0 1000

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MSD-M1PAM

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 MDS Pharma Services).

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

Target protein HGNC name Species Cmp. conc. % inhibition Reference compound name Reference compound IC50 [nM] Assay ID
Adenosine A1 ADORA1 Homo sapiens 10 µM -11.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 6.0 CGS-Z1680 130.00 200610
Adenosine A3 ADORA3 Homo sapiens 10 µM -3.0 IB-MECA 0.78 200720
Adrenergic alpha1, Non-Selective Rattus sp. 10 µM -4.0 Prazosin 0.37 203500
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM -12.0 Prazosin 0.88 203400
Adrenergic alpha2, Non-Selective Rattus sp. 10 µM -7.0 Yohimbine 19.00 203900
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM -11.0 Yohimbine 8.40 203620
Adrenergic alpha2B ADRA2B Homo sapiens 10 µM -8.0 Yohimbine 14.00 203710
Adrenergic alpha2C ADRA2C Homo sapiens 10 µM 15.0 Yohimbine 75.00 203800
Adrenergic beta1 ADRB1 Homo sapiens 10 µM 2.0 S(-)-Propranolol 2.50 204010
Adrenergic beta2 ADRB2 Homo sapiens 10 µM -4.0 S(-)-Propranolol 0.78 204110
Adrenergic beta3 ADRB3 Homo sapiens 10 µM -5.0 Alprenolol 180.00 204200
Androgen (Testosterone) AR AR Rattus sp. 10 µM -3.0 Testosterone 6.50 285010
Angiotensin AT1 AGTR1 Homo sapiens 10 µM -8.0 Saralasin 0.64 210020
Angiotensin AT2 AGTR2 Homo sapiens 10 µM -2.0 Saralasin 0.28 210110
Atrial Natriuretic Factor (ANF) Cavia porcellus 10 µM 1.0 ANF (rat) 0.40 211000
Bombesin, Non-Selective Rattus sp. 10 µM 6.0 Bombesin 0.70 211500
Bradykinin B1 BDKRB1 Homo sapiens 10 µM -6.0 (Des-Arg10)-Kallidin 0.13 800460
Bradykinin B2 BDKRB2 Homo sapiens 10 µM -20.0 Bradykinin 0.89 212610
Calcitonin CALCR Homo sapiens 10 µM -5.0 Calcitonin (salmon) 0.39 213610
Calcitonin Gene-Related Peptide CGRP1 CALCA Homo sapiens 10 µM -6.0 alpha-CGRP (human) 0.07 214010
Calcium Channel L-Type, Benzothiazepine CACNA1C Rattus sp. 10 µM -2.0 Diltiazem 0.04 214510
Calcium Channel L-Type, Dihydropyridine CACNA1C Rattus sp. 10 µM -12.0 Nitrendipine 0.72 214600
Calcium Channel L-Type, Phenylalkylamine CACNA1C Rattus sp. 10 µM 2.0 Methoxyverapamil (D-600) 22.00 215000
Calcium Channel N-Type CACNA1B Rattus sp. 10 µM -3.0 ω-Conotoxin GVIA 0.03 216000
Cannabinoid CB1 CNR1 Homo sapiens 10 µM -3.0 R(+)-WIN-55,212-2 12.00 217020
Cannabinoid CB2 CNR2 Homo sapiens 10 µM 0.0 R(+)-WIN-55,Z1Z-Z 5.80 217100
Chemokine CCR1 CCR1 Homo sapiens 10 µM 8.0 MCP-3 1.10 217500
Chemokine CCR5 CCR5 Homo sapiens 10 µM -16.0 MIP-1beta 0.07 217700
Chemokine CXCR2 (IL-8RB) CXCR2 Homo sapiens 10 µM 0.0 IL-8 0.18 244500
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM -19.0 Devazepide (L-364,718) 0.18 218020
Cholecystokinin CCK2 (CCKB) CCKBR Homo sapiens 10 µM -3.0 Sincalide 0.14 218120
Dopamine D1 DRD1 Homo sapiens 10 µM 6.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2S DRD2 Homo sapiens 10 µM -9.0 Spiperone 0.25 219700
Dopamine D3 DRD3 Homo sapiens 10 µM -9.0 Spiperone 0.36 219800
Dopamine D4.4 DRD4 Homo sapiens 10 µM 2.0 Spiperone 0.76 220000
Dopamine D5 DRD5 Homo sapiens 10 µM 3.0 R(+)-SCH-23390 1.50 220200
Endothelin ETA EDNRA Homo sapiens 10 µM -1.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM -10.0 Endothelin-1 0.13 224110
Epidermal Growth Factor (EGF) EGFR Homo sapiens 10 µM -7.0 EGF (human) 1.60 225510
Estrogen ERalpha ESR1 Homo sapiens 10 µM -1.0 Diethylstilbestrol 0.77 226010
Estrogen ERbeta ESR2 Homo sapiens 10 µM 8.0 Diethylstilbestrol 0.61 226050
GABA-alpha5beta3gamma2 Homo sapiens 10 µM 14.0 Diazepam 14.00 800340
GABA-alpha5beta3gamma2 (Muscimol binding) Homo sapiens 10 µM 11.0 GABA 218.00 800360
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 18.0 Picrotoxin 270.00 226810
GABAA, Muscimol, Central Rattus sp. 10 µM -20.0 GABA 32.00 226500
GABAB, Non-Selective GABBR1 Rattus sp. 10 µM -14.0 CGP-546Z6 1.80 228510
Galanin GAL1 GALR1 Homo sapiens 10 µM 2.0 Galanin (human) 0.08 231510
Galanin GAL2 GALR2 Homo sapiens 10 µM 4.0 Galanin (human) 2.40 231600
Glucocorticoid NR3C1 Homo sapiens 10 µM 4.0 Dexamethasone 4.10 232020
Glutamate, AMPA Rattus sp. 10 µM -7.0 L-Glutamic acid 320.00 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 7.0 L-Glutamic acid 240.00 232700
Glutamate, NMDA, Agonism Rattus sp. 10 µM 25.0 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 11.0 Dizolcipine ((+)-MK-801) 5.10 233000
Glutamate, Non-Selective Rattus sp. 10 µM 8.0 L-Glutamic acid 33.00 235010
Glycine, Strychnine-Sensitive Rattus sp. 10 µM 33.0 (-)-Strychnine 8.90 239000
Histamine H1 HRH1 Homo sapiens 10 µM 5.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM -3.0 Tiotidine 22.00 239710
Histamine H3 HRH3 Homo sapiens 10 µM -9.0 R(-)-alpha-Methylhistamine (RAMH) 5.20 239810
Histamine H4 HRH4 Homo sapiens 10 µM 11.0 Histamine 13.00 239900
Inositol Trisphosphate IP3 ITPR1 Rattus sp. 10 µM -3.0 Inositol 1,4,5-trisphosphate 69.00 242500
Insulin INSR Rattus sp. 10 µM 3.0 Insulin 6.10 243000
Leukotriene, Cysteinyl CysLT1 CYSLTR1 Homo sapiens 10 µM -5.0 Leukotriene D4 0.70 250460
Melanocortin MC3 MC3R Homo sapiens 10 µM 1.0 NDP-alpha-MSH 0.15 251300
Melanocortin MC4 MC4R Homo sapiens 10 µM -1.0 NDP-alpha-MSH 0.22 251350
Melanocortin MC5 MC5R Homo sapiens 10 µM 1.0 NDP-alpha-MSH 0.48 251400
Melatonin MT, Non-Selective Gallus gallus 10 µM -6.0 6-Chloromelatonin 1.00 251500
Muscarinic M1 CHRM1 Homo sapiens 10 µM 3.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 10 µM 2.0 4-DAMP 55.00 252710
Muscarinic M3 CHRM3 Homo sapiens 10 µM 3.0 4-DAMP 5.10 252810
Muscarinic M4 CHRM4 Homo sapiens 10 µM 0.0 4-DAMP 15.00 252910
Muscarinic M5 CHRM5 Homo sapiens 10 µM 11.0 4-DAMP 3.20 253010
Neuropeptide Y Y1 NPY1R Homo sapiens 10 µM -1.0 Neuropeptide Y (human, rat) 0.22 257010
Neuropeptide Y Y2 NPY2R Homo sapiens 10 µM -17.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Neurotensin NT1 NTSR1 Homo sapiens 10 µM -13.0 Neurotensin 0.46 800480
Nicotinic Acetylcholine Homo sapiens 10 µM -2.0 Epibatidine 0.08 258590
NMDA-NR1a/NR2a Homo sapiens 10 µM -6.0 7-Chlorokynurenic acid 850.00 800380
Opiate delta (OP1, DOP) OPRD1 Homo sapiens 10 µM 19.0 Naltrindole 0.92 260110
Opiate kappa (OP2, KOP) OPRK1 Homo sapiens 10 µM 2.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 0.0 DAMGO 20.00 260410
Orphanin ORL1 OPRL1 Homo sapiens 10 µM 14.0 Orphanin-FQ 1.50 260600
Oxytocin OXTR Homo sapiens 10 µM -5.0 Oxytocin 1.70 800400
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM -5.0 PAF 0.28 265010
Potassium Channel [KA] Rattus sp. 10 µM 17.0 Dendrotoxin 0.09 265500
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM 1.0 Glyburide 5.70 265600
Potassium Channel [SKCA] Rattus sp. 10 µM -10.0 Apamin 0.01 265800
Potassium Channel hERG KCNH2 Homo sapiens 10 µM 5.0 L-706,000 0.46 800510
PPARalpha PPARA Homo sapiens 10 µM 11.0 L-797773 6.10 800420
PPARgamma PPARG Homo sapiens 10 µM 10.0 L-797773 4.80 800440
Prostanoid DP PTGDR Homo sapiens 10 µM 29.0 Prostaglandin D2 (PGD2) 2.30 800080
Prostanoid EP1 PTGER1 Homo sapiens 10 µM 14.0 Prostaglandin E2 (PGE2) 7.90 800000
Prostanoid EP3 PTGER3 Homo sapiens 10 µM 3.0 Prostaglandin E2 (PGE2) 0.63 800020
Prostanoid EP4 PTGER4 Homo sapiens 10 µM -4.0 Prostaglandin E2 (PGE2) 2.60 800040
Prostanoid FP PTGFR Homo sapiens 10 µM 12.0 Prostaglandin F2alpha (PGF2alpha) 1.70 800060
Prostanoid IP PTGIR Homo sapiens 10 µM 22.0 Iloprost 16.00 800100
Prostanoid, Thromboxane A2 (TP) TBXA2R Homo sapiens 10 µM 21.0 ICI-192,605 2.10 285510
Purinergic P2X Oryctolagus cuniculus 10 µM -17.0 alpha,beta-Methylene ATP 82.00 268700
Serotonin (5-Hydroxytryptamine) 5-HT1, Non-Selective Rattus sp. 10 µM 5.0 Serotonin (5-HT) 1.10 271000
Serotonin (5-Hydroxytryptamine) 5-HT1A HTR1A Homo sapiens 10 µM 2.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT1B HTR1B Rattus sp. 10 µM -2.0 Serotonin (5-HT) 5.70 271200
Serotonin (5-Hydroxytryptamine) 5-HT2, Non-Selective Rattus sp. 10 µM 0.0 Ketanserin 2.10 271600
Serotonin (5-Hydroxytryptamine) 5-HT2B HTR2B Homo sapiens 10 µM -2.0 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT2C HTR2C Homo sapiens 10 µM -8.0 SBZ4Z084 1.00 271800
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM 17.0 MDL-72222 11.00 271910
Serotonin (5-Hydroxytryptamine) 5-HT4 HTR4 Cavia porcellus 10 µM 6.0 RS-23597-190 90.00 272000
Serotonin (5-Hydroxytryptamine) 5-HT6 HTR6 Homo sapiens 10 µM 11.0 Methiothepin 2.80 272200
Sodium Channel, Site 2 Rattus sp. 10 µM 4.0 Dibucaine 61.00 279510
Somatostatin sst1 SSTR1 Homo sapiens 10 µM -3.0 Somatostatin-14 0.18 800160
Somatostatin sst2 SSTR2 Homo sapiens 10 µM 12.0 Somatostatin-14 0.03 800180
Somatostatin sst3 SSTR3 Homo sapiens 10 µM 2.0 Somatostatin-14 1.10 800200
Somatostatin sst4 SSTR4 Homo sapiens 10 µM -1.0 Somatostatin-14 0.32 800220
Somatostatin sst5 SSTR5 Homo sapiens 10 µM -5.0 Somatostatin-14 0.31 283000
Tachykinin NK1 TACR1 Homo sapiens 10 µM 0.0 L-703,606 25.00 255510
Tachykinin NK2 TACR2 Homo sapiens 10 µM 9.0 MEN-10,376 110.00 255600
Tachykinin NK3 TACR3 Homo sapiens 10 µM 7.0 Senktide 13.00 255710
Thyrotropin Releasing Hormone (TRH) TRHR Rattus sp. 10 µM 13.0 TRH 120.00 286000
Transporter, Adenosine Cavia porcellus 10 µM 2.0 Nitrobenzylthioinosine 0.85 202000
Transporter, Choline SLC5A7 Rattus sp. 10 µM 29.0 Hemicholinium-3 2.40 219000
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM 0.0 GBR-12909 1.70 220320
Transporter, GABA Rattus sp. 10 µM -4.0 NO-711 200.00 226400
Transporter, Monoamine SLC18A2 Oryctolagus cuniculus 10 µM 9.0 Ketanserin 5.60 252010
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 8.0 Desipramine 0.93 204410
Transporter, Serotonin (5- Hydroxytryptamine) (SERT) SLC6A4 Homo sapiens 10 µM 9.0 GBR-12909 110.00 274020
Vasoactive Intestinal Peptide VIP1 VIPR1 Homo sapiens 10 µM 14.0 VIP 0.13 287010
Vasopressin V1A AVPR1A Homo sapiens 10 µM -5.0 (Arg8)-Vasopressin 1.30 287520
Vasopressin V2 AVPR2 Homo sapiens 10 µM -2.0 (Arg8)-Vasopressin 4.30 800540
 

MSD-M1PAM

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 IC50 [µM] Reference compound name Reference compound IC50 [µM] Assay ID
Cholinesterase, Acetyl, ACES ACHE Homo sapiens 10 µM 1.0 Physostigmine 0.12 104010
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM -18.0 Indomethacin 0.04 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM -17.0 Rofecoxib 0.17 118010
Lipoxygenase 12-LO ALOX12 Homo sapiens 10 µM 13.0 Baicalein 0.73 137010
Lipoxygenase 5-LO ALOX5 Homo sapiens 10 µM -7.0 NDGA 0.13 136010
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 12.0 Clorgyline 0.00 140010
Monoamine Oxidase MAO-B MAOB Homo sapiens 10 µM -5.0 R(-)-Deprenyl 0.01 140120
Nitric Oxide Synthase, Inducible (iNOS) NOS2 Mus musculus 10 µM 0.0 S-Methylisothiourea 2.30 144000
Nitric Oxide Synthase, Neuronal (nNOS) NOS1 Rattus sp. 10 µM -18.0 S-Methylisothiourea 0.53 142000
Peptidase, CASP1 (Caspase 1) CASP1 Homo sapiens 10 µM 7.0 Ac-YVAD-CHO 0.03 163000
Peptidase, CASP3 (Caspase 3) CASP3 Homo sapiens 10 µM 6.0 Ac-DEVD-CHO 0.00 163200
Peptidase, CASP6 (Caspase 6) CASP6 Homo sapiens 10 µM 13.0 Ac-VEID-CHO 0.01 163300
Peptidase, CASP7 (Caspase 7) CASP7 Homo sapiens 10 µM 5.0 Ac-DEVD-CHO 0.01 163400
Peptidase, CASP8 (Caspase 8) CASP8 Homo sapiens 10 µM 9.0 Ac-IETD-CHO 0.01 163500
Peptidase, CTSG (Cathepsin G) CTSG Homo sapiens 10 µM 10.0 Chymostatin 2.10 112510
Peptidase, ELA2 (Neutrophil Elastase 2) ELANE Homo sapiens 10 µM 9.0 N-MeOSuc-Ala-Ala-Pro- Val-Chloromethylketone 0.18 166000
Peptidase, Endothelin Converting Enzyme-1 (ECE-1) ECE1 Homo sapiens 10 µM 45.0 Phosphoramidon 0.00 163950
Peptidase, Matrix Metalloproteinase-1 (MMP-1) MMP1 Homo sapiens 10 µM 15.0 TIMP-2 0.01 114110
Peptidase, Matrix Metalloproteinase-12 (MMP-12) MMP12 Homo sapiens 10 µM 12.0 TIMP-2 0.00 115200
Peptidase, Metalloproteinase, Neutral Endopeptidase MME Homo sapiens 10 µM 3.0 Phosphoramidon 0.01 164000
Phosphodiesterase PDE1 Bos taurus 100 µM 28.0 IBMX 3.80 146000
Phosphodiesterase PDE2 Homo sapiens 100 µM -23.0 EHNA 1.80 148000
Phosphodiesterase PDE3 Homo sapiens 100 µM 1.0 Cilostamide 0.05 152000
Phosphodiesterase PDE4 Homo sapiens 100 µM 8.0 Ro 20-1724 1.10 154000
Phosphodiesterase PDE5 PDE5A Homo sapiens 100 µM 21.0 Zaprinast 1.10 156000
Phosphodiesterase PDE6 Bos taurus 100 µM 5.0 Zaprinast 0.22 156100
Protein Serine/Threonine Kinase, MAPK14 (p38a) MAPK14 Homo sapiens 10 µM -3.0 SB-202190 0.02 176600
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 100 µM -21.0 Staurosporine 1.60 171000
Protein Serine/Threonine Kinase, PKA, Non-Selective Bos taurus 100 µM 24.0 H-7 3.60 177000
Protein Serine/Threonine Kinase, PKC, Non-Selective Rattus sp. 10 µM 9.0 Staurosporine 0.00 178010
Protein Serine/Threonine Kinase, PRKCA (PKCa) PRKCA Homo sapiens 0.1 µM -9.0 91.50 Staurosporine 0.00 180010
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM 5.0 Tyrphostin 47 1.10 170010
Protein Tyrosine Kinase, FLT1 (VEGFR-1) FLT1 Homo sapiens 10 µM 0.0 Staurosporine 0.00 171800
Protein Tyrosine Kinase, Insulin Receptor INSR Homo sapiens 10 µM 1.0 Tyrphostin 47 3.10 175000
Protein Tyrosine Kinase, SRC SRC Homo sapiens 10 µM 0.0 Staurosporine 0.23 176800
Protein Tyrosine Phosphatase, PTPN1 (PTP1B) PTPN1 Homo sapiens 10 µM 34.0 (NH4)6Mo7O24 0.03 192010
Protein Tyrosine Phosphatase, PTPN2 (TCPTP) PTPN2 Homo sapiens 0.01 µM -4.0 10.00 (NH4)6Mo7O24 0.02 193010
Protein Tyrosine Phosphatase, PTPRC (CD45) PTPRC Homo sapiens 10 µM 13.0 (NH4)6Mo7O24 0.04 190010
Tyrosine Hydroxylase TH Rattus sp. 10 µM -2.0 alpha-Methyl-L-P-Tyrosine 20.00 195000