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Selectivity data for probe THPP-1 and control THPP-1-NC


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THPP-1


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1A HTR1A -0.41
5-HT1B HTR1B 23.34
5-HT1D HTR1D 8.09
5-HT1E HTR1E 6.95
5-HT2B HTR2B 3.25
Alpha1A ADRA1A 12.68
Alpha1B ADRA1B 10.80
H1 HRH1 23.93
M1 CHRM1 -4.03
D4 DRD4 15.66
D5 DRD5 -3.46
DAT SLC6A3 -16.55
M2 CHRM2 19.34
M3 CHRM3 3.95
M4 CHRM4 2.00
Sigma 1 SIGMAR1 38.15
5-HT2A HTR2A -1.40
5-HT2C HTR2C 13.34
5-HT3 HTR3A -13.60
5-HT6 HTR6 -4.55
Alpha1D ADRA1D -4.48
Alpha2A ADRA2A -10.23
Alpha2B ADRA2B -2.32
Alpha2C ADRA2C 1.30
Beta2 ADRB2 -0.65
D1 DRD1 -8.34
DOR OPRD1 6.52
KOR OPRK1 -1.56
MOR OPRM1 -0.32
H4 HRH4 -6.39
5-HT7A HTR7 42.33
Beta1 ADRB1 16.77
Beta3 ADRB3 1.51
D2 DRD2 -32.49
H3 HRH3 5.45
M5 CHRM5 7.79
NET SLC6A2 -6.81
GABAA/BZP 24.89
D3 DRD3 -6.15
GABAA 15.03
H2 HRH2 -0.24
5-HT5A HTR5A -7.27
Sigma 2 TMEM97 55.63 3350.43 5.47
SERT SLC6A4 2.72
GABA/PBR 26.10

THPP-1-NC


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
GABA/PBR 40.96
5-HT5A HTR5A -10.29
Sigma 2 TMEM97 78.75 707.78 6.15
GABAA/BZP -3.36
D3 DRD3 5.44
GABAA -4.66
H2 HRH2 3.39
5-HT7A HTR7 64.49 577.70 6.24
Beta1 ADRB1 29.47
Beta3 ADRB3 12.34
D2 DRD2 -26.49
H3 HRH3 18.34
M5 CHRM5 7.59
NET SLC6A2 -16.55
H4 HRH4 -7.78
5-HT1A HTR1A -0.56
5-HT1B HTR1B 12.89
5-HT1D HTR1D 22.64
5-HT1E HTR1E -5.76
5-HT2B HTR2B 7.85
Alpha1A ADRA1A -1.11
Alpha1B ADRA1B 17.47
H1 HRH1 12.55
M1 CHRM1 4.18
D4 DRD4 7.93
D5 DRD5 19.37
DAT SLC6A3 15.28
M2 CHRM2 18.25
M3 CHRM3 13.48
M4 CHRM4 3.58
Sigma 1 SIGMAR1 49.42
5-HT2A HTR2A 3.00
5-HT2C HTR2C -6.28
5-HT3 HTR3A -4.38
5-HT6 HTR6 0.81
Alpha1D ADRA1D -22.32
Alpha2A ADRA2A 48.38
Alpha2B ADRA2B 29.01
Alpha2C ADRA2C 47.95
Beta2 ADRB2 5.63
D1 DRD1 18.46
DOR OPRD1 8.22
KOR OPRK1 37.98
MOR OPRM1 -0.75
SERT SLC6A4 -16.74

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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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THPP-1


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 100
ABL1 ABL1-phosphorylated 68.0 100
ABL2 ABL2 100.0 100
ACVR1 ACVR1 100.0 100
ACVR1B ACVR1B 86.0 100
ACVR2A ACVR2A 98.0 100
ACVR2B ACVR2B 93.0 100
ACVRL1 ACVRL1 100.0 100
COQ8A ADCK3 100.0 100
COQ8B ADCK4 100.0 100
AKT1 AKT1 82.0 100
AKT2 AKT2 100.0 100
AKT3 AKT3 47.0 100
ALK ALK(L1196M) 100.0 100
PRKAA1 AMPK-alpha1 100.0 100
PRKAA2 AMPK-alpha2 100.0 100
ANKK1 ANKK1 100.0 100
NUAK1 ARK5 100.0 100
MAP3K5 ASK1 84.0 100
MAP3K6 ASK2 100.0 100
AURKA AURKA 81.0 100
AURKB AURKB 97.0 100
AURKC AURKC 95.0 100
AXL AXL 90.0 100
BMP2K BIKE 90.0 100
BLK BLK 75.0 100
BMPR1A BMPR1A 82.0 100
BMPR1B BMPR1B 100.0 100
BMPR2 BMPR2 100.0 100
BMX BMX 100.0 100
BRAF BRAF(V600E) 100.0 100
PTK6 BRK 100.0 100
BRSK1 BRSK1 100.0 100
BRSK2 BRSK2 93.0 100
BTK BTK 100.0 100
BUB1 BUB1 82.0 100
CAMK1 CAMK1 100.0 100
PNCK CAMK1B 100.0 100
CAMK1D CAMK1D 100.0 100
CAMK1G CAMK1G 100.0 100
CAMK2A CAMK2A 100.0 100
CAMK2B CAMK2B 100.0 100
CAMK2D CAMK2D 100.0 100
CAMK2G CAMK2G 100.0 100
CAMK4 CAMK4 100.0 100
CAMKK1 CAMKK1 100.0 100
CAMKK2 CAMKK2 100.0 100
CASK CASK 95.0 100
CDK11B CDC2L1 100.0 100
CDK11A CDC2L2 100.0 100
CDK13 CDC2L5 100.0 100
CDK19 CDK11 63.0 100
CDK2 CDK2 82.0 100
CDK3 CDK3 100.0 100
CDK4 CDK4-cyclinD3 93.0 100
CDK5 CDK5 100.0 100
CDK7 CDK7 77.0 100
CDK8 CDK8 100.0 100
CDK9 CDK9 100.0 100
CDKL1 CDKL1 61.0 100
CDKL2 CDKL2 98.0 100
CDKL3 CDKL3 96.0 100
CDKL5 CDKL5 100.0 100
CHEK1 CHEK1 100.0 100
CHEK2 CHEK2 100.0 100
CIT CIT 92.0 100
CLK1 CLK1 100.0 100
CLK2 CLK2 100.0 100
CLK3 CLK3 100.0 100
CLK4 CLK4 100.0 100
CSF1R CSF1R-autoinhibited 100.0 100
CSK CSK 100.0 100
CSNK1A1 CSNK1A1 98.0 100
CSNK1A1L CSNK1A1L 100.0 100
CSNK1D CSNK1D 84.0 100
CSNK1E CSNK1E 100.0 100
CSNK1G1 CSNK1G1 100.0 100
CSNK1G2 CSNK1G2 94.0 100
CSNK1G3 CSNK1G3 100.0 100
CSNK2A1 CSNK2A1 99.0 100
CSNK2A2 CSNK2A2 100.0 100
MATK CTK 100.0 100
DAPK1 DAPK1 100.0 100
DAPK2 DAPK2 100.0 100
DAPK3 DAPK3 100.0 100
DCLK1 DCAMKL1 100.0 100
DCLK2 DCAMKL2 100.0 100
DCLK3 DCAMKL3 100.0 100
DDR1 DDR1 100.0 100
DDR2 DDR2 100.0 100
MAP3K12 DLK 97.0 100
DMPK DMPK 72.0 100
CDC42BPG DMPK2 100.0 100
STK17A DRAK1 79.0 100
STK17B DRAK2 62.0 100
DYRK1A DYRK1A 78.0 100
DYRK1B DYRK1B 83.0 100
DYRK2 DYRK2 100.0 100
EGFR EGFR(T790M) 61.0 100
EIF2AK1 EIF2AK1 100.0 100
EPHA1 EPHA1 100.0 100
EPHA2 EPHA2 100.0 100
EPHA3 EPHA3 96.0 100
EPHA4 EPHA4 100.0 100
EPHA5 EPHA5 99.0 100
EPHA6 EPHA6 100.0 100
EPHA7 EPHA7 100.0 100
EPHA8 EPHA8 100.0 100
EPHB1 EPHB1 100.0 100
EPHB2 EPHB2 79.0 100
EPHB3 EPHB3 100.0 100
EPHB4 EPHB4 100.0 100
EPHB6 EPHB6 78.0 100
ERBB2 ERBB2 82.0 100
ERBB3 ERBB3 65.0 100
ERBB4 ERBB4 80.0 100
MAPK3 ERK1 89.0 100
MAPK1 ERK2 95.0 100
MAPK6 ERK3 100.0 100
MAPK4 ERK4 100.0 100
MAPK7 ERK5 100.0 100
MAPK15 ERK8 100.0 100
ERN1 ERN1 100.0 100
PTK2 FAK 99.0 100
FER FER 100.0 100
FES FES 100.0 100
FGFR1 FGFR1 100.0 100
FGFR2 FGFR2 100.0 100
FGFR3 FGFR3(G697C) 100.0 100
FGFR4 FGFR4 90.0 100
FGR FGR 100.0 100
FLT1 FLT1 87.0 100
FLT3 FLT3-autoinhibited 100.0 100
FLT4 FLT4 88.0 100
FRK FRK 100.0 100
FYN FYN 100.0 100
GAK GAK 100.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 100
GRK1 GRK1 100.0 100
GRK2 GRK2 100.0 100
GRK3 GRK3 100.0 100
GRK4 GRK4 73.0 100
GRK7 GRK7 91.0 100
GSK3A GSK3A 100.0 100
GSK3B GSK3B 100.0 100
HASPIN HASPIN 100.0 100
HCK HCK 100.0 100
HIPK1 HIPK1 90.0 100
HIPK2 HIPK2 100.0 100
HIPK3 HIPK3 100.0 100
HIPK4 HIPK4 83.0 100
MAP4K1 HPK1 92.0 100
HUNK HUNK 78.0 100
CILK1 ICK 100.0 100
IGF1R IGF1R 82.0 100
CHUK IKK-alpha 100.0 100
IKBKB IKK-beta 100.0 100
IKBKE IKK-epsilon 100.0 100
INSR INSR 76.0 100
INSRR INSRR 100.0 100
IRAK1 IRAK1 100.0 100
IRAK3 IRAK3 100.0 100
IRAK4 IRAK4 100.0 100
ITK ITK 100.0 100
JAK1 JAK1(JH2domain-pseudokinase) 76.0 100
JAK2 JAK2(JH1domain-catalytic) 100.0 100
JAK3 JAK3(JH1domain-catalytic) 93.0 100
MAPK8 JNK1 100.0 100
MAPK9 JNK2 76.0 100
MAPK10 JNK3 91.0 100
KIT KIT-autoinhibited 100.0 100
LATS1 LATS1 70.0 100
LATS2 LATS2 68.0 100
LCK LCK 100.0 100
LIMK1 LIMK1 100.0 100
LIMK2 LIMK2 100.0 100
STK11 LKB1 100.0 100
STK10 LOK 100.0 100
LRRK2 LRRK2(G2019S) 100.0 100
LTK LTK 100.0 100
LYN LYN 73.0 100
MAP3K13 LZK 87.0 100
MAK MAK 100.0 100
MAP3K1 MAP3K1 100.0 100
MAP3K15 MAP3K15 100.0 100
MAP3K2 MAP3K2 92.0 100
MAP3K3 MAP3K3 96.0 100
MAP3K4 MAP3K4 100.0 100
MAP4K2 MAP4K2 100.0 100
MAP4K3 MAP4K3 100.0 100
MAP4K4 MAP4K4 73.0 100
MAP4K5 MAP4K5 91.0 100
MAPKAPK2 MAPKAPK2 73.0 100
MAPKAPK5 MAPKAPK5 100.0 100
MARK1 MARK1 100.0 100
MARK2 MARK2 100.0 100
MARK3 MARK3 100.0 100
MARK4 MARK4 100.0 100
MAST1 MAST1 100.0 100
MAP2K1 MEK1 100.0 100
MAP2K2 MEK2 100.0 100
MAP2K3 MEK3 93.0 100
MAP2K4 MEK4 100.0 100
MAP2K5 MEK5 100.0 100
MAP2K6 MEK6 100.0 100
MELK MELK 65.0 100
MERTK MERTK 89.0 100
MET MET(Y1235D) 100.0 100
MINK1 MINK 100.0 100
MAP2K7 MKK7 95.0 100
MKNK1 MKNK1 77.0 100
MKNK2 MKNK2 100.0 100
MYLK3 MLCK 83.0 100
MAP3K9 MLK1 100.0 100
MAP3K10 MLK2 100.0 100
MAP3K11 MLK3 100.0 100
CDC42BPA MRCKA 100.0 100
CDC42BPB MRCKB 100.0 100
STK4 MST1 100.0 100
MST1R MST1R 100.0 100
STK3 MST2 100.0 100
STK24 MST3 100.0 100
STK26 MST4 100.0 100
MTOR MTOR 97.0 100
MUSK MUSK 100.0 100
MYLK MYLK 70.0 100
MYLK2 MYLK2 94.0 100
MYLK4 MYLK4 100.0 100
MYO3A MYO3A 100.0 100
MYO3B MYO3B 67.0 100
STK38 NDR1 100.0 100
STK38L NDR2 100.0 100
NEK1 NEK1 100.0 100
NEK10 NEK10 100.0 100
NEK11 NEK11 100.0 100
NEK2 NEK2 100.0 100
NEK3 NEK3 100.0 100
NEK4 NEK4 100.0 100
NEK5 NEK5 100.0 100
NEK6 NEK6 100.0 100
NEK7 NEK7 100.0 100
NEK9 NEK9 100.0 100
MAP3K14 NIK 100.0 100
NIM1K NIM1 100.0 100
NLK NLK 100.0 100
OXSR1 OSR1 100.0 100
MAPK14 p38-alpha 100.0 100
MAPK11 p38-beta 100.0 100
MAPK13 p38-delta 100.0 100
MAPK12 p38-gamma 72.0 100
PAK1 PAK1 100.0 100
PAK2 PAK2 100.0 100
PAK3 PAK3 100.0 100
PAK4 PAK4 100.0 100
PAK6 PAK6 100.0 100
PAK5 PAK7 100.0 100
CDK16 PCTK1 100.0 100
CDK17 PCTK2 100.0 100
CDK18 PCTK3 100.0 100
PDGFRA PDGFRA 100.0 100
PDGFRB PDGFRB 100.0 100
PDPK1 PDPK1 90.0 100
CDPK1 PFCDPK1(P.falciparum) 100.0 100
PK5 PFPK5(P.falciparum) 100.0 100
CDK15 PFTAIRE2 100.0 100
CDK14 PFTK1 100.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 100.0 100
PIK3C2B PIK3C2B 100.0 100
PIK3C2G PIK3C2G 100.0 100
PIK3CA PIK3CA(Q546K) 87.0 100
PIK3CB PIK3CB 100.0 100
PIK3CD PIK3CD 94.0 100
PIK3CG PIK3CG 100.0 100
PI4KB PIK4CB 100.0 100
PIKFYVE PIKFYVE 90.0 100
PIM1 PIM1 100.0 100
PIM2 PIM2 98.0 100
PIM3 PIM3 100.0 100
PIP5K1A PIP5K1A 100.0 100
PIP5K1C PIP5K1C 67.0 100
PIP4K2B PIP5K2B 59.0 100
PIP4K2C PIP5K2C 92.0 100
PRKACA PKAC-alpha 82.0 100
PRKACB PKAC-beta 73.0 100
PKMYT1 PKMYT1 100.0 100
PKN1 PKN1 100.0 100
PKN2 PKN2 55.0 100
PKNB PKNB(M.tuberculosis) 86.0 100
PLK1 PLK1 100.0 100
PLK2 PLK2 100.0 100
PLK3 PLK3 100.0 100
PLK4 PLK4 85.0 100
PRKCD PRKCD 100.0 100
PRKCE PRKCE 89.0 100
PRKCH PRKCH 97.0 100
PRKCI PRKCI 100.0 100
PRKCQ PRKCQ 100.0 100
PRKD1 PRKD1 90.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 94.0 100
PRKG1 PRKG1 87.0 100
PRKG2 PRKG2 100.0 100
EIF2AK2 PRKR 100.0 100
PRKX PRKX 100.0 100
PRPF4B PRP4 100.0 100
PTK2B PYK2 100.0 100
SIK3 QSK 100.0 100
RAF1 RAF1 97.0 100
RET RET(V804M) 89.0 100
RIOK1 RIOK1 93.0 100
RIOK2 RIOK2 100.0 100
RIOK3 RIOK3 100.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 100.0 100
DSTYK RIPK5 100.0 100
ROCK1 ROCK1 93.0 100
ROCK2 ROCK2 76.0 100
ROS1 ROS1 100.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 82.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 100
RPS6KB1 S6K1 100.0 100
SBK1 SBK1 100.0 100
SGK1 SGK 91.0 100
SBK3 SgK110 100.0 100
SGK2 SGK2 88.0 100
SGK3 SGK3 100.0 100
SIK1 SIK 100.0 100
SIK2 SIK2 100.0 100
SLK SLK 100.0 100
NUAK2 SNARK 100.0 100
SNRK SNRK 79.0 100
SRC SRC 95.0 100
SRMS SRMS 100.0 100
SRPK1 SRPK1 86.0 100
SRPK2 SRPK2 100.0 100
SRPK3 SRPK3 66.0 100
STK16 STK16 100.0 100
STK33 STK33 53.0 100
STK35 STK35 100.0 100
STK36 STK36 79.0 100
STK39 STK39 100.0 100
SYK SYK 100.0 100
MAP3K7 TAK1 93.0 100
TAOK1 TAOK1 100.0 100
TAOK2 TAOK2 99.0 100
TAOK3 TAOK3 100.0 100
TBK1 TBK1 68.0 100
TEC TEC 100.0 100
TESK1 TESK1 100.0 100
TGFBR1 TGFBR1 100.0 100
TGFBR2 TGFBR2 94.0 100
TIE1 TIE1 100.0 100
TEK TIE2 100.0 100
TLK1 TLK1 100.0 100
TLK2 TLK2 100.0 100
TNIK TNIK 100.0 100
TNK1 TNK1 100.0 100
TNK2 TNK2 100.0 100
TNNI3K TNNI3K 100.0 100
NTRK1 TRKA 100.0 100
NTRK2 TRKB 100.0 100
NTRK3 TRKC 100.0 100
TRPM6 TRPM6 100.0 100
TSSK1B TSSK1B 100.0 100
TSSK3 TSSK3 100.0 100
TTK TTK 100.0 100
TXK TXK 100.0 100
TYK2 TYK2(JH2domain-pseudokinase) 100.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 92.0 100
ULK2 ULK2 100.0 100
ULK3 ULK3 81.0 100
KDR VEGFR2 100.0 100
PIK3C3 VPS34 100.0 100
VRK2 VRK2 91.0 100
WEE1 WEE1 100.0 100
WEE2 WEE2 100.0 100
WNK1 WNK1 100.0 100
WNK2 WNK2 100.0 100
WNK3 WNK3 100.0 100
WNK4 WNK4 100.0 100
STK32A YANK1 83.0 100
STK32B YANK2 100.0 100
STK32C YANK3 100.0 100
YES1 YES 100.0 100
STK25 YSK1 100.0 100
MAP3K19 YSK4 100.0 100
MAP3K20 ZAK 100.0 100
ZAP70 ZAP70 95.0 100

THPP-1-NC


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 100
ABL1 ABL1-phosphorylated 66.0 100
ABL2 ABL2 100.0 100
ACVR1 ACVR1 100.0 100
ACVR1B ACVR1B 89.0 100
ACVR2A ACVR2A 97.0 100
ACVR2B ACVR2B 100.0 100
ACVRL1 ACVRL1 99.0 100
COQ8A ADCK3 100.0 100
COQ8B ADCK4 100.0 100
AKT1 AKT1 92.0 100
AKT2 AKT2 100.0 100
AKT3 AKT3 64.0 100
ALK ALK(L1196M) 100.0 100
PRKAA1 AMPK-alpha1 100.0 100
PRKAA2 AMPK-alpha2 100.0 100
ANKK1 ANKK1 100.0 100
NUAK1 ARK5 100.0 100
MAP3K5 ASK1 91.0 100
MAP3K6 ASK2 100.0 100
AURKA AURKA 72.0 100
AURKB AURKB 92.0 100
AURKC AURKC 100.0 100
AXL AXL 63.0 100
BMP2K BIKE 99.0 100
BLK BLK 84.0 100
BMPR1A BMPR1A 93.0 100
BMPR1B BMPR1B 100.0 100
BMPR2 BMPR2 99.0 100
BMX BMX 100.0 100
BRAF BRAF(V600E) 100.0 100
PTK6 BRK 100.0 100
BRSK1 BRSK1 100.0 100
BRSK2 BRSK2 94.0 100
BTK BTK 100.0 100
BUB1 BUB1 78.0 100
CAMK1 CAMK1 100.0 100
PNCK CAMK1B 100.0 100
CAMK1D CAMK1D 100.0 100
CAMK1G CAMK1G 100.0 100
CAMK2A CAMK2A 100.0 100
CAMK2B CAMK2B 100.0 100
CAMK2D CAMK2D 100.0 100
CAMK2G CAMK2G 100.0 100
CAMK4 CAMK4 100.0 100
CAMKK1 CAMKK1 100.0 100
CAMKK2 CAMKK2 100.0 100
CASK CASK 81.0 100
CDK11B CDC2L1 100.0 100
CDK11A CDC2L2 100.0 100
CDK13 CDC2L5 100.0 100
CDK19 CDK11 62.0 100
CDK2 CDK2 80.0 100
CDK3 CDK3 100.0 100
CDK4 CDK4-cyclinD3 100.0 100
CDK5 CDK5 100.0 100
CDK7 CDK7 65.0 100
CDK8 CDK8 82.0 100
CDK9 CDK9 100.0 100
CDKL1 CDKL1 63.0 100
CDKL2 CDKL2 87.0 100
CDKL3 CDKL3 89.0 100
CDKL5 CDKL5 100.0 100
CHEK1 CHEK1 100.0 100
CHEK2 CHEK2 100.0 100
CIT CIT 100.0 100
CLK1 CLK1 100.0 100
CLK2 CLK2 100.0 100
CLK3 CLK3 100.0 100
CLK4 CLK4 92.0 100
CSF1R CSF1R-autoinhibited 100.0 100
CSK CSK 100.0 100
CSNK1A1 CSNK1A1 73.0 100
CSNK1A1L CSNK1A1L 100.0 100
CSNK1D CSNK1D 83.0 100
CSNK1E CSNK1E 100.0 100
CSNK1G1 CSNK1G1 100.0 100
CSNK1G2 CSNK1G2 86.0 100
CSNK1G3 CSNK1G3 100.0 100
CSNK2A1 CSNK2A1 100.0 100
CSNK2A2 CSNK2A2 88.0 100
MATK CTK 100.0 100
DAPK1 DAPK1 100.0 100
DAPK2 DAPK2 100.0 100
DAPK3 DAPK3 100.0 100
DCLK1 DCAMKL1 100.0 100
DCLK2 DCAMKL2 100.0 100
DCLK3 DCAMKL3 100.0 100
DDR1 DDR1 100.0 100
DDR2 DDR2 97.0 100
MAP3K12 DLK 90.0 100
DMPK DMPK 87.0 100
CDC42BPG DMPK2 100.0 100
STK17A DRAK1 96.0 100
STK17B DRAK2 91.0 100
DYRK1A DYRK1A 78.0 100
DYRK1B DYRK1B 77.0 100
DYRK2 DYRK2 84.0 100
EGFR EGFR(T790M) 74.0 100
EIF2AK1 EIF2AK1 100.0 100
EPHA1 EPHA1 100.0 100
EPHA2 EPHA2 100.0 100
EPHA3 EPHA3 100.0 100
EPHA4 EPHA4 100.0 100
EPHA5 EPHA5 89.0 100
EPHA6 EPHA6 100.0 100
EPHA7 EPHA7 99.0 100
EPHA8 EPHA8 100.0 100
EPHB1 EPHB1 100.0 100
EPHB2 EPHB2 80.0 100
EPHB3 EPHB3 100.0 100
EPHB4 EPHB4 100.0 100
EPHB6 EPHB6 91.0 100
ERBB2 ERBB2 82.0 100
ERBB3 ERBB3 73.0 100
ERBB4 ERBB4 94.0 100
MAPK3 ERK1 88.0 100
MAPK1 ERK2 93.0 100
MAPK6 ERK3 100.0 100
MAPK4 ERK4 100.0 100
MAPK7 ERK5 100.0 100
MAPK15 ERK8 100.0 100
ERN1 ERN1 100.0 100
PTK2 FAK 92.0 100
FER FER 100.0 100
FES FES 100.0 100
FGFR1 FGFR1 100.0 100
FGFR2 FGFR2 100.0 100
FGFR3 FGFR3(G697C) 100.0 100
FGFR4 FGFR4 98.0 100
FGR FGR 99.0 100
FLT1 FLT1 100.0 100
FLT3 FLT3-autoinhibited 100.0 100
FLT4 FLT4 100.0 100
FRK FRK 100.0 100
FYN FYN 100.0 100
GAK GAK 100.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 100
GRK1 GRK1 100.0 100
GRK2 GRK2 100.0 100
GRK3 GRK3 100.0 100
GRK4 GRK4 75.0 100
GRK7 GRK7 74.0 100
GSK3A GSK3A 100.0 100
GSK3B GSK3B 100.0 100
HASPIN HASPIN 100.0 100
HCK HCK 94.0 100
HIPK1 HIPK1 64.0 100
HIPK2 HIPK2 100.0 100
HIPK3 HIPK3 100.0 100
HIPK4 HIPK4 61.0 100
MAP4K1 HPK1 93.0 100
HUNK HUNK 86.0 100
CILK1 ICK 100.0 100
IGF1R IGF1R 83.0 100
CHUK IKK-alpha 100.0 100
IKBKB IKK-beta 100.0 100
IKBKE IKK-epsilon 100.0 100
INSR INSR 84.0 100
INSRR INSRR 100.0 100
IRAK1 IRAK1 100.0 100
IRAK3 IRAK3 100.0 100
IRAK4 IRAK4 100.0 100
ITK ITK 100.0 100
JAK1 JAK1(JH2domain-pseudokinase) 71.0 100
JAK2 JAK2(JH1domain-catalytic) 100.0 100
JAK3 JAK3(JH1domain-catalytic) 98.0 100
MAPK8 JNK1 100.0 100
MAPK9 JNK2 72.0 100
MAPK10 JNK3 78.0 100
KIT KIT-autoinhibited 100.0 100
LATS1 LATS1 67.0 100
LATS2 LATS2 94.0 100
LCK LCK 100.0 100
LIMK1 LIMK1 100.0 100
LIMK2 LIMK2 100.0 100
STK11 LKB1 100.0 100
STK10 LOK 100.0 100
LRRK2 LRRK2(G2019S) 100.0 100
LTK LTK 91.0 100
LYN LYN 88.0 100
MAP3K13 LZK 66.0 100
MAK MAK 99.0 100
MAP3K1 MAP3K1 100.0 100
MAP3K15 MAP3K15 100.0 100
MAP3K2 MAP3K2 100.0 100
MAP3K3 MAP3K3 77.0 100
MAP3K4 MAP3K4 100.0 100
MAP4K2 MAP4K2 100.0 100
MAP4K3 MAP4K3 95.0 100
MAP4K4 MAP4K4 84.0 100
MAP4K5 MAP4K5 93.0 100
MAPKAPK2 MAPKAPK2 92.0 100
MAPKAPK5 MAPKAPK5 100.0 100
MARK1 MARK1 92.0 100
MARK2 MARK2 100.0 100
MARK3 MARK3 100.0 100
MARK4 MARK4 100.0 100
MAST1 MAST1 100.0 100
MAP2K1 MEK1 100.0 100
MAP2K2 MEK2 100.0 100
MAP2K3 MEK3 100.0 100
MAP2K4 MEK4 97.0 100
MAP2K5 MEK5 98.0 100
MAP2K6 MEK6 100.0 100
MELK MELK 67.0 100
MERTK MERTK 100.0 100
MET MET(Y1235D) 100.0 100
MINK1 MINK 100.0 100
MAP2K7 MKK7 79.0 100
MKNK1 MKNK1 69.0 100
MKNK2 MKNK2 73.0 100
MYLK3 MLCK 98.0 100
MAP3K9 MLK1 91.0 100
MAP3K10 MLK2 96.0 100
MAP3K11 MLK3 100.0 100
CDC42BPA MRCKA 100.0 100
CDC42BPB MRCKB 99.0 100
STK4 MST1 100.0 100
MST1R MST1R 100.0 100
STK3 MST2 100.0 100
STK24 MST3 100.0 100
STK26 MST4 100.0 100
MTOR MTOR 89.0 100
MUSK MUSK 100.0 100
MYLK MYLK 86.0 100
MYLK2 MYLK2 96.0 100
MYLK4 MYLK4 100.0 100
MYO3A MYO3A 96.0 100
MYO3B MYO3B 78.0 100
STK38 NDR1 100.0 100
STK38L NDR2 95.0 100
NEK1 NEK1 100.0 100
NEK10 NEK10 100.0 100
NEK11 NEK11 98.0 100
NEK2 NEK2 100.0 100
NEK3 NEK3 100.0 100
NEK4 NEK4 100.0 100
NEK5 NEK5 100.0 100
NEK6 NEK6 100.0 100
NEK7 NEK7 100.0 100
NEK9 NEK9 100.0 100
MAP3K14 NIK 100.0 100
NIM1K NIM1 100.0 100
NLK NLK 100.0 100
OXSR1 OSR1 100.0 100
MAPK14 p38-alpha 100.0 100
MAPK11 p38-beta 100.0 100
MAPK13 p38-delta 100.0 100
MAPK12 p38-gamma 79.0 100
PAK1 PAK1 100.0 100
PAK2 PAK2 100.0 100
PAK3 PAK3 100.0 100
PAK4 PAK4 100.0 100
PAK6 PAK6 100.0 100
PAK5 PAK7 100.0 100
CDK16 PCTK1 100.0 100
CDK17 PCTK2 100.0 100
CDK18 PCTK3 100.0 100
PDGFRA PDGFRA 98.0 100
PDGFRB PDGFRB 100.0 100
PDPK1 PDPK1 100.0 100
CDPK1 PFCDPK1(P.falciparum) 100.0 100
PK5 PFPK5(P.falciparum) 100.0 100
CDK15 PFTAIRE2 100.0 100
CDK14 PFTK1 100.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 100.0 100
PIK3C2B PIK3C2B 100.0 100
PIK3C2G PIK3C2G 100.0 100
PIK3CA PIK3CA(Q546K) 97.0 100
PIK3CB PIK3CB 100.0 100
PIK3CD PIK3CD 82.0 100
PIK3CG PIK3CG 100.0 100
PI4KB PIK4CB 100.0 100
PIKFYVE PIKFYVE 91.0 100
PIM1 PIM1 100.0 100
PIM2 PIM2 100.0 100
PIM3 PIM3 100.0 100
PIP5K1A PIP5K1A 100.0 100
PIP5K1C PIP5K1C 85.0 100
PIP4K2B PIP5K2B 61.0 100
PIP4K2C PIP5K2C 96.0 100
PRKACA PKAC-alpha 89.0 100
PRKACB PKAC-beta 82.0 100
PKMYT1 PKMYT1 92.0 100
PKN1 PKN1 100.0 100
PKN2 PKN2 80.0 100
PKNB PKNB(M.tuberculosis) 97.0 100
PLK1 PLK1 100.0 100
PLK2 PLK2 100.0 100
PLK3 PLK3 100.0 100
PLK4 PLK4 70.0 100
PRKCD PRKCD 100.0 100
PRKCE PRKCE 100.0 100
PRKCH PRKCH 94.0 100
PRKCI PRKCI 100.0 100
PRKCQ PRKCQ 100.0 100
PRKD1 PRKD1 87.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 100.0 100
PRKG1 PRKG1 74.0 100
PRKG2 PRKG2 100.0 100
EIF2AK2 PRKR 100.0 100
PRKX PRKX 100.0 100
PRPF4B PRP4 100.0 100
PTK2B PYK2 100.0 100
SIK3 QSK 100.0 100
RAF1 RAF1 100.0 100
RET RET(V804M) 82.0 100
RIOK1 RIOK1 98.0 100
RIOK2 RIOK2 100.0 100
RIOK3 RIOK3 100.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 100.0 100
DSTYK RIPK5 100.0 100
ROCK1 ROCK1 78.0 100
ROCK2 ROCK2 74.0 100
ROS1 ROS1 100.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 67.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 100
RPS6KB1 S6K1 100.0 100
SBK1 SBK1 100.0 100
SGK1 SGK 99.0 100
SBK3 SgK110 100.0 100
SGK2 SGK2 94.0 100
SGK3 SGK3 100.0 100
SIK1 SIK 91.0 100
SIK2 SIK2 100.0 100
SLK SLK 100.0 100
NUAK2 SNARK 100.0 100
SNRK SNRK 84.0 100
SRC SRC 100.0 100
SRMS SRMS 100.0 100
SRPK1 SRPK1 99.0 100
SRPK2 SRPK2 100.0 100
SRPK3 SRPK3 79.0 100
STK16 STK16 100.0 100
STK33 STK33 74.0 100
STK35 STK35 96.0 100
STK36 STK36 78.0 100
STK39 STK39 100.0 100
SYK SYK 100.0 100
MAP3K7 TAK1 78.0 100
TAOK1 TAOK1 100.0 100
TAOK2 TAOK2 97.0 100
TAOK3 TAOK3 100.0 100
TBK1 TBK1 75.0 100
TEC TEC 100.0 100
TESK1 TESK1 100.0 100
TGFBR1 TGFBR1 100.0 100
TGFBR2 TGFBR2 97.0 100
TIE1 TIE1 100.0 100
TEK TIE2 100.0 100
TLK1 TLK1 100.0 100
TLK2 TLK2 100.0 100
TNIK TNIK 100.0 100
TNK1 TNK1 100.0 100
TNK2 TNK2 99.0 100
TNNI3K TNNI3K 100.0 100
NTRK1 TRKA 100.0 100
NTRK2 TRKB 100.0 100
NTRK3 TRKC 100.0 100
TRPM6 TRPM6 100.0 100
TSSK1B TSSK1B 99.0 100
TSSK3 TSSK3 100.0 100
TTK TTK 100.0 100
TXK TXK 100.0 100
TYK2 TYK2(JH2domain-pseudokinase) 100.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 90.0 100
ULK2 ULK2 89.0 100
ULK3 ULK3 89.0 100
KDR VEGFR2 100.0 100
PIK3C3 VPS34 100.0 100
VRK2 VRK2 77.0 100
WEE1 WEE1 100.0 100
WEE2 WEE2 100.0 100
WNK1 WNK1 100.0 100
WNK2 WNK2 100.0 100
WNK3 WNK3 100.0 100
WNK4 WNK4 100.0 100
STK32A YANK1 94.0 100
STK32B YANK2 87.0 100
STK32C YANK3 98.0 100
YES1 YES 100.0 100
STK25 YSK1 100.0 100
MAP3K19 YSK4 100.0 100
MAP3K20 ZAK 100.0 100
ZAP70 ZAP70 91.0 100

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THPP-1

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: A significant inhibition was found for the Adenosine transporter with IC50 = 1.61 µM @ 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 37.0 R(-)-PIA 830.00 200510
Adenosine A2A ADORA2A Homo sapiens 10 µM 17.0 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 8.0 Prazosin 0.27 203200
Adrenergic alpha1D ADRA1D Homo sapiens 10 µM 45.0 Prazosin 0.88 203400
Adrenergic alpha2A ADRA2A Homo sapiens 10 µM -3.0 Yohimbine 8.40 203620
Adrenergic alpha2B ADRA2B Homo sapiens 10 µM 1.0 Yohimbine 14.00 203710
Adrenergic alpha2C ADRA2C Homo sapiens 10 µM 3.0 Yohimbine 75.00 203800
Adrenergic beta1 ADRB1 Homo sapiens 10 µM -3.0 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 1.0 Alprenolol 180.00 204200
Adrenomedullin AM1 ADM Homo sapiens 10 µM -6.0 Adrenomedullin 0.10 204460
Androgen (Testosterone) AR AR Rattus sp. 10 µM 7.0 Testosterone 6.50 285010
Angiotensin AT1 AGTR1 Homo sapiens 10 µM 3.0 Saralasin 0.64 210020
Atrial Natriuretic Factor (ANF) Cavia porcellus 10 µM 0.0 ANF (rat) 0.40 211000
Bradykinin B1 BDKRB1 Homo sapiens 10 µM 28.0 (Des-Arg10)-Kallidin 0.87 212510
Bradykinin B2 BDKRB2 Homo sapiens 10 µM 13.0 Bradykinin 0.89 212610
Cannabinoid CB1 CNR1 Homo sapiens 10 µM 21.0 R(+)-WIN-55,Z1Z-Z 200.00 217030
Cannabinoid CB2 CNR2 Homo sapiens 10 µM 28.0 R(+)-WIN-55,Z1Z-Z 5.80 217100
Chemokine CCR1 CCR1 Homo sapiens 10 µM 11.0 MCP-3 1.10 217500
Chemokine CXCRZ (IL-8RB) CXCR2 Homo sapiens 10 µM -4.0 IL-8 0.18 244500
Chemokine CXCR4 CXCR4 Homo sapiens 10 µM 4.0 SDF-1alpha 0.12 244550
Cholecystokinin CCK1 (CCKA) CCKAR Homo sapiens 10 µM 5.0 Devazepide (L-364,718) 0.18 218020
Cholecystokinin CCK2 (CCKB) CCKBR Homo sapiens 10 µM -8.0 Sincalide 0.14 218120
Corticotropin Releasing Factor CRF1 CRHR1 Homo sapiens 10 µM 12.0 Sauvagine (frog) 0.85 219150
Dopamine D1 DRD1 Homo sapiens 10 µM 6.0 R(+)-SCH-Z3390 1.40 219500
Dopamine D2S DRD2 Homo sapiens 10 µM 3.0 Spiperone 0.25 219700
Endothelin ETA EDNRA Homo sapiens 10 µM 1.0 Endothelin-1 0.23 224010
Endothelin ETB EDNRB Homo sapiens 10 µM 0.0 Endothelin-1 0.13 224110
Estrogen ERalpha ESR1 Homo sapiens 10 µM -1.0 Diethylstilbestrol 0.77 226010
GABAA, Chloride Channel, TBOB Rattus sp. 10 µM 4.0 Picrotoxin 270.00 226810
GABAA, Ro-15-1788, Hippocampus Rattus sp. 10 µM 37.0 Diazepam 46.00 226630
GABAB, Non-Selective GABBR1 Rattus sp. 10 µM -5.0 CGP-546Z6 1.80 228510
Glucocorticoid NR3C1 Homo sapiens 10 µM -6.0 Dexamethasone 4.10 232020
Glutamate, AMPA Rattus sp. 10 µM -10.0 L-Glutamic acid 320.00 232600
Glutamate, Kainate GRIK2 Rattus sp. 10 µM 9.0 L-Glutamic acid 240.00 232700
Glutamate, Metabotropic, mGlu5 GRM5 Homo sapiens 10 µM 22.0 L-Glutamic acid 1500.00 237000
Glutamate, NMDA, Agonism Rattus sp. 10 µM 0.0 L-Glutamic acid 410.00 232810
Glutamate, NMDA, Glycine Rattus sp. 10 µM 3.0 MDL 105,519 22.00 232910
Glutamate, NMDA, Phencyclidine Rattus sp. 10 µM -10.0 Dizolcipine ((+)-MK- 801) 5.10 233000
Glutamate, NMDA, Polyamine Rattus sp. 10 µM 11.0 Ifenprodil 23.00 234000
Glycine, Strychnine-Sensitive Rattus sp. 10 µM 15.0 (-)-Strychnine 8.90 239000
Histamine H1 HRH1 Homo sapiens 10 µM 0.0 Pyrilamine 3.30 239610
Histamine H2 HRH2 Homo sapiens 10 µM 2.0 Tiotidine 22.00 239710
Histamine H3 HRH3 Homo sapiens 10 µM -1.0 R(-)-alpha-Methylhistamine (RAMH) 5.20 239810
Histamine H4 HRH4 Homo sapiens 10 µM 1.0 Histamine 13.00 239900
Leukotriene, Cysteinyl CysLT2 CYSLTR2 Homo sapiens 10 µM 8.0 LTC4 4.10 250480
Melanin-Concentrating Hormone MCH1 (SLC1) MCHR1 Homo sapiens 10 µM 4.0 MCH (human, mouse, rat) 0.67 251010
Melanocortin MC1 MC1R Homo sapiens 10 µM 23.0 NDP-alpha-MSH 0.06 251100
Melanocortin MC3 MC3R Homo sapiens 10 µM 0.0 NDP-alpha-MSH 0.15 251300
Melanocortin MC4 MC4R Homo sapiens 10 µM 8.0 NDP-alpha-MSH 0.22 251350
Melanocortin MC5 MC5R Homo sapiens 10 µM 6.0 NDP-alpha-MSH 0.48 251400
Muscarinic M1 CHRM1 Homo sapiens 10 µM 6.0 4-DAMP 4.50 252610
Muscarinic M2 CHRM2 Homo sapiens 10 µM 5.0 4-DAMP 55.00 252710
Muscarinic M3 CHRM3 Homo sapiens 10 µM -6.0 4-DAMP 5.10 252810
Muscarinic M4 CHRM4 Homo sapiens 10 µM 5.0 4-DAMP 15.00 252910
Muscarinic M5 CHRM5 Homo sapiens 10 µM 1.0 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 1.0 Neuropeptide Y (13-36) (porcine) 0.21 257110
Neurotensin NT1 NTSR1 Homo sapiens 10 µM 10.0 Neurotensin 1.20 258010
Nicotinic Acetylcholine Homo sapiens 10 µM -7.0 Epibatidine 0.08 258590
Nicotinic Acetylcholine alpha1, Bungarotoxin CHRNA1 Homo sapiens 10 µM -3.0 alpha-Bungarotoxin 1.10 258700
NMDA-NR1a/NRZa Homo sapiens 10 µM -7.0 7-Chlorokynurenic acid 850.00 800380
Opiate kappa (OPZ, KOP) OPRK1 Homo sapiens 10 µM 2.0 U-69593 16.00 260210
Opiate µ (OP3, MOP) OPRM1 Homo sapiens 10 µM 2.0 DAMGO 20.00 260410
Orphanin ORL1 OPRL1 Homo sapiens 10 µM 5.0 Orphanin-FQ 1.50 260600
Platelet Activating Factor (PAF) PTAFR Homo sapiens 10 µM -4.0 PAF 0.28 265010
Potassium Channel [KATP] KCNJ11 Cricetinae 10 µM -4.0 Glyburide 5.70 265600
PPARalpha PPARA Homo sapiens 10 µM 4.0 L-797773 6.10 800420
PPARgamma PPARG Homo sapiens 10 µM -4.0 L-797773 4.80 800440
Progesterone PR-B PGR Homo sapiens 10 µM 12.0 Progesterone 1.50 268020
Prostanoid EP1 PTGER1 Homo sapiens 10 µM -1.0 Prostaglandin E2 (PGE2) 7.90 800000
Prostanoid EP3 PTGER3 Homo sapiens 10 µM -1.0 Prostaglandin E2 (PGE2) 0.63 800020
Prostanoid FP PTGFR Homo sapiens 10 µM 22.0 Prostaglandin F2alpha (PGF2alpha) 1.70 800060
Prostanoid IP PTGIR Homo sapiens 10 µM -12.0 Iloprost 16.00 800100
Prostanoid, Thromboxane A2(TP) TBXA2R Homo sapiens 10 µM 8.0 ICI-19Z,605 2.10 285510
Purinergic P2Y Rattus sp. 10 µM 5.0 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 8.0 Metergoline 4.10 271110
Serotonin (5-Hydroxytryptamine) 5-HT1B HTR1B Rattus sp. 10 µM 7.0 Serotonin (5-HT) 5.70 271200
Serotonin (5-Hydroxytryptamine) 5-HT2B HTR2B Homo sapiens 10 µM -1.0 Ketanserin 290.00 271700
Serotonin (5-Hydroxytryptamine) 5-HT2C HTR2C Homo sapiens 10 µM 22.0 SBZ4Z084 1.00 271800
Serotonin (5-Hydroxytryptamine) 5-HT3 HTR3A Homo sapiens 10 µM -8.0 MDL-72222 11.00 271910
Serotonin (5-Hydroxytryptamine) 5-HT6 HTR6 Homo sapiens 10 µM 5.0 Methiothepin 2.80 272200
Somatostatin sst2 SSTR2 Homo sapiens 10 µM 0.0 Somatostatin-14 0.01 282700
Tachykinin NK1 TACR1 Homo sapiens 10 µM 8.0 L-703,606 25.00 255510
Tachykinin NK2 TACR2 Homo sapiens 10 µM 18.0 MEN-10,376 110.00 255600
Thyrotropin Releasing Hormone (TRH) TRHR Rattus sp. 10 µM 7.0 TRH 120.00 286000
Transporter, Adenosine Cavia porcellus 0.01 µM -6.0 1.61 0.55 Nitrobenzylthioinosine 0.85 202000
Transporter, Choline SLC5A7 Rattus sp. 10 µM 9.0 Hemicholinium-3 2.40 219000
Transporter, Dopamine (DAT) SLC6A3 Homo sapiens 10 µM -3.0 GBR-1Z909 1.70 220320
Transporter, GABA Rattus sp. 10 µM -9.0 NO-711 200.00 226400
Transporter, Norepinephrine (NET) SLC6A2 Homo sapiens 10 µM 3.0 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 8.0 VIP 0.13 287010
Vasopressin V1A AVPR1A Homo sapiens 10 µM 1.0 (Arg8)-Vasopressin 0.33 287530
Vasopressin V1B AVPR1B Homo sapiens 10 µM 5.0 (Arg8)-Vasopressin 0.66 287560
Vasopressin V2 AVPR2 Homo sapiens 10 µM -2.0 (Arg8)-Vasopressin 4.50 287610
 

THPP-1

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 -1.0 Physostigmine 0.12 104010
Cyclooxygenase COX-1 PTGS1 Homo sapiens 10 µM -11.0 Indomethacin 0.04 116020
Cyclooxygenase COX-2 PTGS2 Homo sapiens 10 µM -10.0 Rofecoxib 0.17 118010
Monoamine Oxidase MAO-A MAOA Homo sapiens 10 µM 42.0 Clorgyline 0.00 140010
Monoamine Oxidase MAO-B MAOB Homo sapiens 10 µM 32.0 R(-)-Deprenyl 0.01 140120
Peptidase, CASP3 (Caspase 3) CASP3 Homo sapiens 10 µM -1.0 Ac-DEVD-CHO 0.00 163200
Peptidase, CASP8 (Caspase 8) CASP8 Homo sapiens 10 µM -3.0 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 17.0 Chymostatin 2.10 112510
Phosphodiesterase PDE3 Homo sapiens 10 µM 45.0 Cilostamide 0.05 152000
Protein Serine/Threonine Kinase, MAPK14 (p38α) MAPK14 Homo sapiens 10 µM -14.0 SB-Z0Z190 0.02 176600
Protein Serine/Threonine Kinase, MAPK3 (ERK1) MAPK3 Homo sapiens 10 µM 6.0 Staurosporine 1.60 171000
Protein Serine/Threonine Kinase, MARK3 MARK3 Homo sapiens 10 µM 7.0 Hymenialdisine 0.08 171315
Protein Serine/Threonine Kinase, PKA, Non-Selective Bos taurus 10 µM -7.0 H-7 3.60 177000
Protein Serine/Threonine Kinase, PKC, Non-Selective Rattus sp. 10 µM 12.0 Staurosporine 0.00 178010
Protein Tyrosine Kinase, EGF Receptor EGFR Homo sapiens 10 µM 6.0 Tyrphostin 47 1.10 170010
Protein Tyrosine Kinase, Insulin Receptor INSR Homo sapiens 10 µM -2.0 Tyrphostin 47 3.10 175000
Tyrosine Hydroxylase TH Rattus sp. 10 µM 4.0 alpha-Methyl-L-P-Tyrosine 20.00 195000