Selectivity data for probe BI-1950 and control BI-9446


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BI-1950


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT3 HTR3A -2.51
5-HT5A HTR5A 6.14
5-HT6 HTR6 6.67
5-HT7A HTR7 -4.31
D1 DRD1 1.26
D2 DRD2 7.62
Alpha1A ADRA1A -8.89
Alpha1B ADRA1B 2.35
D3 DRD3 -3.54
D4 DRD4 -2.68
D5 DRD5 14.04
DAT SLC6A3 -14.81
H1 HRH1 3.20
H3 HRH3 1.43
H4 HRH4 9.55
M1 CHRM1 -11.67
M2 CHRM2 -13.37
M3 CHRM3 -20.45
M4 CHRM4 12.11
M5 CHRM5 -11.77
NET SLC6A2 -2.81
GABA/PBR 13.13
SERT SLC6A4 -4.33
5-HT1A HTR1A -9.74
5-HT1B HTR1B 16.50
5-HT1D HTR1D 12.04
5-HT2A HTR2A 9.30
5-HT2B HTR2B 17.25
Alpha1D ADRA1D -18.52
Alpha2A ADRA2A -16.74
Alpha2B ADRA2B -3.79
Alpha2C ADRA2C 0.16
Beta2 ADRB2 -9.72
GABAA/BZP 4.90
DOR OPRD1 -0.33
MOR OPRM1 17.40
Sigma 1 SIGMAR1 -6.44
5-HT1E HTR1E 17.68
H2 HRH2 11.84
GABAA -4.17
Sigma 2 TMEM97 25.85
5-HT2C HTR2C 24.33
KOR OPRK1 9.67
Beta1 ADRB1 24.11
Beta3 ADRB3 12.45

BI-9446


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT3 HTR3A 17.89
5-HT5A HTR5A 2.14
5-HT6 HTR6 16.11
5-HT7A HTR7 4.18
D1 DRD1 18.58
D2 DRD2 16.44
Alpha1A ADRA1A -1.65
Alpha1B ADRA1B 23.75
D3 DRD3 9.55
D4 DRD4 13.60
D5 DRD5 7.21
DAT SLC6A3 -16.00
H1 HRH1 10.26
H3 HRH3 19.99
H4 HRH4 27.64
M1 CHRM1 -8.37
M2 CHRM2 -8.35
M3 CHRM3 -17.91
M4 CHRM4 21.59
M5 CHRM5 -8.46
NET SLC6A2 -16.93
GABA/PBR -15.22
SERT SLC6A4 5.35
5-HT1A HTR1A -16.56
5-HT1B HTR1B 17.52
5-HT1D HTR1D 22.43
5-HT2A HTR2A 31.89
5-HT2B HTR2B 15.54
Alpha1D ADRA1D 8.28
Alpha2A ADRA2A 12.13
Alpha2B ADRA2B 14.99
Alpha2C ADRA2C 9.30
Beta2 ADRB2 -7.08
GABAA/BZP -11.51
DOR OPRD1 8.30
MOR OPRM1 31.08
Sigma 1 SIGMAR1 -16.18
5-HT1E HTR1E 31.49
H2 HRH2 10.99
GABAA -8.68
Sigma 2 TMEM97 58.05 557.65 average (n=2) 6.30
5-HT2C HTR2C 32.93
KOR OPRK1 12.55
Beta1 ADRB1 29.73
Beta3 ADRB3 -16.36

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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.
View assay details

Jump to control KinomeScan data

BI-1950


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
CSNK1D CSNK1D 100.0 1000
ABL2 ABL2 83.0 1000
ACVR1 ACVR1 97.0 1000
ACVR1B ACVR1B 99.0 1000
ACVR2A ACVR2A 92.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 60.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 99.0 1000
MAP3K5 ASK1 92.0 1000
MAP3K6 ASK2 100.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 98.0 1000
BMPR1A BMPR1A 98.0 1000
BMPR1B BMPR1B 99.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 77.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 92.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 96.0 1000
PNCK CAMK1B 83.0 1000
CAMK1D CAMK1D 99.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 96.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 100.0 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 100.0 1000
CDK19 CDK11 81.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 100.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 94.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 73.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 86.0 1000
CLK2 CLK2 97.0 1000
CLK3 CLK3 96.0 1000
CLK4 CLK4 88.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1E CSNK1E 82.0 1000
CSNK1G1 CSNK1G1 99.0 1000
CSNK1G2 CSNK1G2 90.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 81.0 1000
CSNK2A2 CSNK2A2 99.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 97.0 1000
DCLK1 DCAMKL1 89.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 67.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 98.0 1000
EGFR EGFR(T790M) 95.0 1000
EIF2AK1 EIF2AK1 93.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 75.0 1000
EPHA3 EPHA3 88.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 84.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 85.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 100.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 91.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 96.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 68.0 1000
FYN FYN 70.0 1000
GAK GAK 92.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 97.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 99.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 90.0 1000
IKBKE IKK-epsilon 89.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 83.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 81.0 1000
MAPK9 JNK2 92.0 1000
MAPK10 JNK3 91.0 1000
KIT KIT-autoinhibited 100.0 1000
LATS1 LATS1 100.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 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 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 76.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 97.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 94.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 96.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 92.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 92.0 1000
MAP2K2 MEK2 90.0 1000
MAP2K3 MEK3 80.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 80.0 1000
MELK MELK 86.0 1000
MERTK MERTK 99.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 93.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 98.0 1000
MTOR MTOR 96.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 98.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 96.0 1000
STK38L NDR2 49.0 1000
NEK1 NEK1 59.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 95.0 1000
NEK3 NEK3 100.0 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 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 94.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 95.0 1000
PAK2 PAK2 92.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 96.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 91.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 85.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 97.0 1000
PIK3CB PIK3CB 99.0 1000
PIK3CD PIK3CD 95.0 1000
PIK3CG PIK3CG 86.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 80.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 75.0 1000
PKMYT1 PKMYT1 79.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 63.0 1000
PKNB PKNB(M.tuberculosis) 100.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 75.0 1000
PLK3 PLK3 81.0 1000
PLK4 PLK4 88.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 90.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 62.0 1000
PRKG2 PRKG2 85.0 1000
EIF2AK2 PRKR 34.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 77.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 76.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 68.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 87.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 92.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 94.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 100.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 94.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 100.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 81.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 88.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 24.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 97.0 1000
TAOK1 TAOK1 86.0 1000
TAOK2 TAOK2 92.0 1000
TAOK3 TAOK3 88.0 1000
TBK1 TBK1 97.0 1000
TEC TEC 75.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 82.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 91.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 59.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 88.0 1000
TNK2 TNK2 94.0 1000
TNNI3K TNNI3K 65.0 1000
NTRK1 TRKA 98.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 100.0 1000
TSSK1B TSSK1B 79.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 90.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 99.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 78.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 83.0 1000
STK32B YANK2 80.0 1000
STK32C YANK3 100.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 100.0 1000

BI-9446


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 78.0 1000
ACVR1 ACVR1 89.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 92.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 90.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 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 100.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 82.0 1000
AURKA AURKA 92.0 1000
AURKB AURKB 100.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 40.0 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 93.0 1000
PNCK CAMK1B 65.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 89.0 1000
CAMK2B CAMK2B 90.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 100.0 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 100.0 1000
CDK19 CDK11 76.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 93.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 100.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 90.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 100.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 97.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 98.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 89.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 92.0 1000
CSNK1G2 CSNK1G2 91.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 91.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 84.0 1000
DAPK3 DAPK3 94.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 88.0 1000
DDR1 DDR1 81.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 91.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 99.0 1000
DYRK1B DYRK1B 80.0 1000
DYRK2 DYRK2 93.0 1000
EGFR EGFR(T790M) 86.0 1000
NEK10 NEK10 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 56.0 1000
EPHA3 EPHA3 83.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 88.0 1000
EPHA7 EPHA7 92.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 87.0 1000
EPHB2 EPHB2 94.0 1000
EPHB3 EPHB3 99.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 96.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 86.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 100.0 1000
MAPK4 ERK4 100.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 82.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 100.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 96.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 99.0 1000
FLT3 FLT3-autoinhibited 100.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 81.0 1000
FYN FYN 89.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 100.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 100.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 100.0 1000
IKBKE IKK-epsilon 80.0 1000
INSR INSR 89.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 92.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 100.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 100.0 1000
LATS1 LATS1 96.0 1000
LATS2 LATS2 92.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 90.0 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 95.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 81.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 78.0 1000
MAP4K4 MAP4K4 91.0 1000
MAP4K5 MAP4K5 93.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 85.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 97.0 1000
MAP2K2 MEK2 99.0 1000
MAP2K3 MEK3 89.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 80.0 1000
MELK MELK 89.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 100.0 1000
MKNK2 MKNK2 100.0 1000
MYLK3 MLCK 87.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 92.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 100.0 1000
STK24 MST3 93.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 91.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 100.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 99.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 48.0 1000
NEK1 NEK1 48.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 83.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 12.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 86.0 1000
MAP3K14 NIK 100.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 84.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 100.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 99.0 1000
PAK2 PAK2 64.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 98.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 97.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 100.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 97.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 100.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 88.0 1000
PIK3CB PIK3CB 97.0 1000
PIK3CD PIK3CD 73.0 1000
PIK3CG PIK3CG 95.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 100.0 1000
PIM2 PIM2 98.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 97.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 75.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 96.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 98.0 1000
PLK3 PLK3 100.0 1000
PLK4 PLK4 90.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 87.0 1000
PRKCQ PRKCQ 98.0 1000
PRKD1 PRKD1 86.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 87.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 56.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 91.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 98.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 91.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 95.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 99.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KB1 S6K1 100.0 1000
SBK1 SBK1 95.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 100.0 1000
SRC SRC 98.0 1000
SRMS SRMS 100.0 1000
SRPK1 SRPK1 94.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 91.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 96.0 1000
TAOK1 TAOK1 97.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 91.0 1000
TBK1 TBK1 95.0 1000
TEC TEC 92.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 99.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 92.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 97.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 93.0 1000
TNK2 TNK2 86.0 1000
TNNI3K TNNI3K 72.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 0.0 1000
TSSK1B TSSK1B 76.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 94.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 100.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 100.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 99.0 1000
WNK2 WNK2 100.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 99.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 90.0 1000

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BI-1950

Conclusion: Closest hit is the Ca2+ ion channel DHPSI with 72 % inhibition at 10 µM.

Target protein HGNC name Species % control at 10 µM % control at 3 µM % control at 1 µM % control at 0.3 µM % control at 0.1 µM % control at 0.03 µM Mode of action Assay
5HT1/R Rattus norvegicus 100.0 Radioactive Assay
5HT2/R Rattus norvegicus 98.0 Radioactive Assay
5HT3/HU HTR3A Homo sapiens 134.0 Others
5HT4/GPIG HTR4 Cavia porcellus 83.0 Radioactive Assay
5HT5A/HU HTR5A Homo sapiens 105.0 Others
5HT6/HU HTR6 Homo sapiens 102.0 Others
5HTTRANS/HU SLC6A4 Homo sapiens 119.0 Radioactive Assay
ALPHA1/R Rattus norvegicus 102.0 Others
ALPHA2/R Rattus norvegicus 88.0 Others
AT1 AGTR1 Homo sapiens 90.0 Others
ATP NA+/K+PI ATP1A1 Sus scrofa 109.0 inhibitor Spectrofluorimetry
ATRANS Cavia porcellus 92.0 Radioactive Assay
BETA/R ADRB2 Rattus norvegicus 84.0 Radioactive Assay
CA+/DHPSI/RA CACNA1C Rattus norvegicus 28.0 58.00 81.00 94.00 98.00 97.00 Radioactive Assay
CA+/DILSI/RA CACNA1C Rattus norvegicus 69.0 Radioactive Assay
CA+/N/RA CACNA1B Rattus norvegicus 102.0 Radioactive Assay
CA+/PAASITE CACNA1C Rattus norvegicus 49.5 76.00 86.00 102.00 110.00 109.00 Radioactive Assay
CANHYDRASE CA6 Homo sapiens 86.0 inhibitor absorption of electromagnetic radiation
CGRP/HU CALCA Homo sapiens 105.0 Radioactive Assay
D1/HU DRD1 Homo sapiens 92.0 Radioactive Assay
D2L/H DRD2 Homo sapiens 115.0 Radioactive Assay
D3/HU DRD3 Homo sapiens 88.0 Radioactive Assay
D4.2/H DRD4 Homo sapiens 86.0 Radioactive Assay
D5/HU DRD5 Homo sapiens 86.0 Radioactive Assay
DATRANS/H SLC6A3 Homo sapiens 67.0 inhibitor Radioactive Assay
GABAA MUSCIMOL CENT GABRA1 Rattus norvegicus 96.0 Scintillation counting
GABAACENTR GABRA1 Rattus norvegicus 99.0 Radioactive Assay
GABAACL+ GABRA1 Rattus norvegicus 73.0 Radioactive Assay
GABAB/RA Rattus norvegicus 111.0 inhibitor Radioactive Assay
GLUTAMAT/R GRIN1 Rattus norvegicus 92.0 Radioactive Assay
H1/H HRH1 Homo sapiens 109.0 Radioactive Assay
H2/H HRH2 Homo sapiens 74.0 Radioactive Assay
H3/H HRH3 Homo sapiens 98.0 Radioactive Assay
K+/KA/R KCNA1 Rattus norvegicus 92.0 Radioactive Assay
K+/KATP/HA KCNJ1 Mullus auratus 107.0 Radioactive Assay
K+/SKCA KCNN1 Rattus norvegicus 108.0 Radioactive Assay
MAOA MAOA Homo sapiens 107.0 inhibitor FI - fluorescence intensity
MAOB MAOB Homo sapiens 101.0 inhibitor FI - fluorescence intensity
MUSCARIN/NS Rattus norvegicus 109.0 Radioactive Assay
MUSCARIN/OTM CHRM1 Rattus norvegicus 77.0 Radioactive Assay
NA+/SITE2/RA SCN1B Rattus norvegicus 42.0 67.00 75.00 84.00 86.00 103.00 Radioactive Assay
NACH/H CHRNA1 Homo sapiens 112.0 Radioligand Binding
NETRANS/H SLC6A2 Homo sapiens 72.0 Radioactive Assay
OPIAT/NS Rattus norvegicus 78.0 Radioactive Assay
SIGMA/NS/GP Cavia porcellus 65.0 Radioactive Assay
THRO SYN(HU) TBXAS1 Homo sapiens 47.0 74.00 82.00 91.00 93.00 94.00 Enzyme Immunoassay
VASOPRE_V2 AVPR2 Homo sapiens 85.0 Radioactive Assay