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Selectivity data for probe BI-2545 and control BI-3017


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BI-2545


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT3 HTR3A 8.82
5-HT5A HTR5A 33.21
5-HT6 HTR6 28.85
5-HT7A HTR7 18.98
D1 DRD1 8.68
D2 DRD2 7.71
Alpha1A ADRA1A 4.06
Alpha1B ADRA1B 33.38
D3 DRD3 6.61
D4 DRD4 6.75
D5 DRD5 21.62
DAT SLC6A3 -2.65
H1 HRH1 12.75
H3 HRH3 -5.26
H4 HRH4 39.55
M1 CHRM1 -2.87
M2 CHRM2 7.11
M3 CHRM3 -25.53
M4 CHRM4 14.19
M5 CHRM5 15.28
NET SLC6A2 15.48
GABA/PBR 63.72 2555.91 average (n=3) 5.62
SERT SLC6A4 -9.34
5-HT1A HTR1A 0.91
5-HT1B HTR1B 17.87
5-HT1D HTR1D 43.20
5-HT2A HTR2A 51.43 8676.68 average (n=3) 5.06
5-HT2B HTR2B 45.94
Alpha1D ADRA1D -1.41
Alpha2A ADRA2A 14.35
Alpha2B ADRA2B 25.22
Alpha2C ADRA2C 18.97
Beta2 ADRB2 -10.67
GABAA/BZP -4.02
DOR OPRD1 19.65
MOR OPRM1 42.95
Sigma 1 SIGMAR1 51.22 3551.58 average (n=3) 5.45
5-HT1E HTR1E 33.65
H2 HRH2 28.07
GABAA 1.13
Sigma 2 TMEM97 44.85
5-HT2C HTR2C 41.54
KOR OPRK1 27.84
Beta1 ADRB1 13.34
Beta3 ADRB3 31.46

BI-3017


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT3 HTR3A 16.38
5-HT5A HTR5A 13.15
5-HT6 HTR6 26.14
5-HT7A HTR7 9.56
D1 DRD1 -9.63
D2 DRD2 -13.13
Alpha1A ADRA1A -3.15
Alpha1B ADRA1B 30.19
D3 DRD3 1.07
D4 DRD4 -0.15
D5 DRD5 16.44
DAT SLC6A3 -17.64
H1 HRH1 18.06
H3 HRH3 9.03
H4 HRH4 7.45
M1 CHRM1 -23.87
M2 CHRM2 -5.60
M3 CHRM3 -15.26
M4 CHRM4 16.12
M5 CHRM5 -9.70
NET SLC6A2 -7.15
GABA/PBR -4.40
SERT SLC6A4 -3.25
5-HT1A HTR1A -7.66
5-HT1B HTR1B 4.40
5-HT1D HTR1D 22.99
5-HT2A HTR2A 7.65
5-HT2B HTR2B 27.06
Alpha1D ADRA1D -6.43
Alpha2A ADRA2A 2.20
Alpha2B ADRA2B 1.15
Alpha2C ADRA2C 3.82
Beta2 ADRB2 -9.93
GABAA/BZP 14.18
DOR OPRD1 -1.41
MOR OPRM1 12.11
Sigma 1 SIGMAR1 3.21
5-HT1E HTR1E 31.76
H2 HRH2 -0.15
GABAA 9.85
Sigma 2 TMEM97 -2.90
5-HT2C HTR2C 31.08
KOR OPRK1 9.47
Beta1 ADRB1 12.38
Beta3 ADRB3 -6.02

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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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BI-2545


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 96.0 1000
ABL1 ABL1-phosphorylated 100.0 1000
ABL2 ABL2 98.0 1000
ACVR1 ACVR1 100.0 1000
ACVR1B ACVR1B 100.0 1000
ACVR2A ACVR2A 92.0 1000
ACVR2B ACVR2B 100.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 100.0 1000
COQ8B ADCK4 94.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 87.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 73.0 1000
NUAK1 ARK5 87.0 1000
MAP3K5 ASK1 13.0 1000
MAP3K6 ASK2 81.0 1000
AURKA AURKA 93.0 1000
AURKB AURKB 84.0 1000
AURKC AURKC 91.0 1000
AXL AXL 87.0 1000
BMP2K BIKE 85.0 1000
BLK BLK 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 95.0 1000
BMPR2 BMPR2 90.0 1000
BMX BMX 81.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 96.0 1000
BRSK1 BRSK1 89.0 1000
BRSK2 BRSK2 96.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 61.0 1000
CAMK1 CAMK1 77.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 91.0 1000
CAMK2B CAMK2B 100.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 85.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 91.0 1000
CAMKK2 CAMKK2 91.0 1000
CASK CASK 70.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 85.0 1000
CDK19 CDK11 89.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 94.0 1000
CDK4 CDK4-cyclinD3 97.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 92.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 91.0 1000
CDKL1 CDKL1 84.0 1000
CDKL2 CDKL2 95.0 1000
CDKL3 CDKL3 87.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 92.0 1000
CHEK2 CHEK2 86.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 87.0 1000
CLK2 CLK2 86.0 1000
CLK3 CLK3 78.0 1000
CLK4 CLK4 98.0 1000
CSF1R CSF1R-autoinhibited 95.0 1000
CSK CSK 96.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 86.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 97.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 89.0 1000
CSNK2A1 CSNK2A1 84.0 1000
CSNK2A2 CSNK2A2 92.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 93.0 1000
DAPK2 DAPK2 85.0 1000
DAPK3 DAPK3 94.0 1000
DCLK1 DCAMKL1 94.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 83.0 1000
DDR2 DDR2 82.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 94.0 1000
CDC42BPG DMPK2 90.0 1000
STK17A DRAK1 95.0 1000
STK17B DRAK2 91.0 1000
DYRK1A DYRK1A 86.0 1000
DYRK1B DYRK1B 86.0 1000
DYRK2 DYRK2 77.0 1000
EGFR EGFR(T790M) 78.0 1000
EIF2AK1 EIF2AK1 91.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 79.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 82.0 1000
EPHA5 EPHA5 100.0 1000
EPHA6 EPHA6 69.0 1000
EPHA7 EPHA7 96.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 81.0 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 100.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 88.0 1000
MAPK4 ERK4 80.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 77.0 1000
PTK2 FAK 100.0 1000
FER FER 97.0 1000
FES FES 95.0 1000
FGFR1 FGFR1 90.0 1000
FGFR2 FGFR2 100.0 1000
FGFR3 FGFR3(G697C) 92.0 1000
FGFR4 FGFR4 82.0 1000
FGR FGR 88.0 1000
FLT1 FLT1 82.0 1000
FLT3 FLT3-autoinhibited 91.0 1000
FLT4 FLT4 88.0 1000
FRK FRK 83.0 1000
FYN FYN 85.0 1000
GAK GAK 91.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 84.0 1000
GRK1 GRK1 90.0 1000
GRK2 GRK2 71.0 1000
GRK3 GRK3 90.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 99.0 1000
GSK3B GSK3B 98.0 1000
HASPIN HASPIN 84.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 85.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 89.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 83.0 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 88.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 83.0 1000
INSRR INSRR 83.0 1000
IRAK1 IRAK1 98.0 1000
IRAK3 IRAK3 84.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 69.0 1000
MAPK8 JNK1 90.0 1000
MAPK9 JNK2 100.0 1000
MAPK10 JNK3 90.0 1000
KIT KIT-autoinhibited 90.0 1000
LATS1 LATS1 96.0 1000
LATS2 LATS2 86.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 83.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 91.0 1000
LTK LTK 98.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 86.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 71.0 1000
MAP3K15 MAP3K15 53.0 1000
MAP3K2 MAP3K2 80.0 1000
MAP3K3 MAP3K3 94.0 1000
MAP3K4 MAP3K4 91.0 1000
MAP4K2 MAP4K2 92.0 1000
MAP4K3 MAP4K3 89.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 97.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 86.0 1000
MARK1 MARK1 98.0 1000
MARK2 MARK2 89.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 94.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 83.0 1000
MAP2K2 MEK2 84.0 1000
MAP2K3 MEK3 93.0 1000
MAP2K4 MEK4 95.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 72.0 1000
MELK MELK 97.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 76.0 1000
MINK1 MINK 72.0 1000
MAP2K7 MKK7 95.0 1000
MKNK1 MKNK1 90.0 1000
MKNK2 MKNK2 90.0 1000
MYLK3 MLCK 98.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 83.0 1000
MAP3K11 MLK3 99.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 87.0 1000
STK24 MST3 90.0 1000
STK26 MST4 76.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 77.0 1000
MYLK MYLK 88.0 1000
MYLK2 MYLK2 97.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 98.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 75.0 1000
STK38L NDR2 45.0 1000
NEK1 NEK1 44.0 1000
NEK10 NEK10 73.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 84.0 1000
NEK5 NEK5 94.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 83.0 1000
NEK9 NEK9 77.0 1000
MAP3K14 NIK 77.0 1000
NIM1K NIM1 100.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 85.0 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 100.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 93.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 97.0 1000
PDGFRB PDGFRB 90.0 1000
PDPK1 PDPK1 96.0 1000
CDPK1 PFCDPK1(P.falciparum) 99.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 75.0 1000
CDK14 PFTK1 96.0 1000
PHKG1 PHKG1 92.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 65.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 78.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 75.0 1000
PIK3CG PIK3CG 76.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 98.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 93.0 1000
PIP5K1C PIP5K1C 98.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 100.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 93.0 1000
PKNB PKNB(M.tuberculosis) 80.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 89.0 1000
PLK3 PLK3 89.0 1000
PLK4 PLK4 82.0 1000
PRKCD PRKCD 93.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 98.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 85.0 1000
PRKD3 PRKD3 83.0 1000
PRKG1 PRKG1 83.0 1000
PRKG2 PRKG2 82.0 1000
EIF2AK2 PRKR 45.0 1000
PRKX PRKX 86.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 85.0 1000
SIK3 QSK 79.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 88.0 1000
RIOK1 RIOK1 69.0 1000
RIOK2 RIOK2 94.0 1000
RIOK3 RIOK3 94.0 1000
RIPK1 RIPK1 89.0 1000
RIPK2 RIPK2 64.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 82.0 1000
ROCK1 ROCK1 85.0 1000
ROCK2 ROCK2 90.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 86.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 83.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 84.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 86.0 1000
RPS6KB1 S6K1 86.0 1000
SBK1 SBK1 97.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 66.0 1000
SGK3 SGK3 84.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 88.0 1000
SNRK SNRK 77.0 1000
SRC SRC 100.0 1000
SRMS SRMS 83.0 1000
SRPK1 SRPK1 81.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 100.0 1000
STK33 STK33 84.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 80.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 94.0 1000
TAOK1 TAOK1 78.0 1000
TAOK2 TAOK2 86.0 1000
TAOK3 TAOK3 88.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 79.0 1000
TGFBR1 TGFBR1 97.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 77.0 1000
TEK TIE2 89.0 1000
TLK1 TLK1 68.0 1000
TLK2 TLK2 90.0 1000
TNIK TNIK 98.0 1000
TNK1 TNK1 94.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 80.0 1000
NTRK1 TRKA 85.0 1000
NTRK2 TRKB 99.0 1000
NTRK3 TRKC 91.0 1000
TRPM6 TRPM6 92.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 91.0 1000
TXK TXK 84.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 75.0 1000
ULK1 ULK1 92.0 1000
ULK2 ULK2 97.0 1000
ULK3 ULK3 99.0 1000
KDR VEGFR2 96.0 1000
PIK3C3 VPS34 72.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 93.0 1000
WNK1 WNK1 90.0 1000
WNK2 WNK2 84.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 89.0 1000
STK32A YANK1 72.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 90.0 1000
YES1 YES 100.0 1000
STK25 YSK1 95.0 1000
MAP3K19 YSK4 100.0 1000
MAP3K20 ZAK 86.0 1000
ZAP70 ZAP70 60.0 1000

BI-3017


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 95.0 1000
ABL2 ABL2 90.0 1000
ACVR1 ACVR1 95.0 1000
ACVR1B ACVR1B 92.0 1000
ACVR2A ACVR2A 69.0 1000
ACVR2B ACVR2B 91.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 84.0 1000
COQ8B ADCK4 100.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 98.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 93.0 1000
PRKAA1 AMPK-alpha1 92.0 1000
PRKAA2 AMPK-alpha2 97.0 1000
ANKK1 ANKK1 100.0 1000
NUAK1 ARK5 82.0 1000
MAP3K5 ASK1 95.0 1000
MAP3K6 ASK2 78.0 1000
AURKA AURKA 91.0 1000
AURKB AURKB 93.0 1000
AURKC AURKC 100.0 1000
AXL AXL 88.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 93.0 1000
BMPR1A BMPR1A 85.0 1000
BMPR1B BMPR1B 100.0 1000
BMPR2 BMPR2 81.0 1000
BMX BMX 88.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 86.0 1000
BTK BTK 99.0 1000
BUB1 BUB1 90.0 1000
CAMK1 CAMK1 93.0 1000
PNCK CAMK1B 83.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 65.0 1000
CAMK2B CAMK2B 90.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 95.0 1000
CAMKK1 CAMKK1 100.0 1000
CAMKK2 CAMKK2 100.0 1000
CASK CASK 72.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 82.0 1000
CDK19 CDK11 97.0 1000
CDK2 CDK2 77.0 1000
CDK3 CDK3 97.0 1000
CDK4 CDK4-cyclinD3 78.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 78.0 1000
CDK8 CDK8 75.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 81.0 1000
CDKL2 CDKL2 95.0 1000
CDKL3 CDKL3 99.0 1000
CDKL5 CDKL5 87.0 1000
CHEK1 CHEK1 100.0 1000
CHEK2 CHEK2 100.0 1000
CIT CIT 100.0 1000
CLK1 CLK1 100.0 1000
CLK2 CLK2 80.0 1000
CLK3 CLK3 90.0 1000
CLK4 CLK4 97.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 99.0 1000
CSNK1A1 CSNK1A1 86.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 97.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 96.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 81.0 1000
CSNK2A2 CSNK2A2 85.0 1000
MATK CTK 94.0 1000
DAPK1 DAPK1 95.0 1000
DAPK2 DAPK2 82.0 1000
DAPK3 DAPK3 92.0 1000
DCLK1 DCAMKL1 90.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 100.0 1000
DDR2 DDR2 77.0 1000
MAP3K12 DLK 72.0 1000
DMPK DMPK 98.0 1000
CDC42BPG DMPK2 92.0 1000
STK17A DRAK1 79.0 1000
STK17B DRAK2 85.0 1000
DYRK1A DYRK1A 81.0 1000
DYRK1B DYRK1B 99.0 1000
DYRK2 DYRK2 94.0 1000
EGFR EGFR(T790M) 91.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 92.0 1000
EPHA3 EPHA3 93.0 1000
EPHA4 EPHA4 98.0 1000
EPHA5 EPHA5 93.0 1000
EPHA6 EPHA6 98.0 1000
EPHA7 EPHA7 89.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 95.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 99.0 1000
ERBB2 ERBB2 99.0 1000
ERBB3 ERBB3 59.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 92.0 1000
MAPK1 ERK2 100.0 1000
MAPK6 ERK3 93.0 1000
MAPK4 ERK4 94.0 1000
MAPK7 ERK5 98.0 1000
MAPK15 ERK8 100.0 1000
ERN1 ERN1 90.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 99.0 1000
FGFR1 FGFR1 91.0 1000
FGFR2 FGFR2 78.0 1000
FGFR3 FGFR3(G697C) 97.0 1000
FGFR4 FGFR4 81.0 1000
FGR FGR 100.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 93.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 84.0 1000
GRK1 GRK1 100.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 70.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 88.0 1000
GSK3A GSK3A 82.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 91.0 1000
HCK HCK 99.0 1000
HIPK1 HIPK1 82.0 1000
HIPK2 HIPK2 81.0 1000
HIPK3 HIPK3 76.0 1000
HIPK4 HIPK4 84.0 1000
MAP4K1 HPK1 100.0 1000
HUNK HUNK 81.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 93.0 1000
CHUK IKK-alpha 100.0 1000
IKBKB IKK-beta 96.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 84.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 81.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 87.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 85.0 1000
JAK2 JAK2(JH1domain-catalytic) 93.0 1000
JAK3 JAK3(JH1domain-catalytic) 96.0 1000
MAPK8 JNK1 84.0 1000
MAPK9 JNK2 95.0 1000
MAPK10 JNK3 100.0 1000
KIT KIT-autoinhibited 79.0 1000
LATS1 LATS1 89.0 1000
LATS2 LATS2 97.0 1000
LCK LCK 94.0 1000
LIMK1 LIMK1 100.0 1000
LIMK2 LIMK2 92.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 82.0 1000
LTK LTK 93.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 65.0 1000
MAK MAK 98.0 1000
MAP3K1 MAP3K1 85.0 1000
MAP3K15 MAP3K15 95.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 91.0 1000
MAP3K4 MAP3K4 94.0 1000
MAP4K2 MAP4K2 84.0 1000
MAP4K3 MAP4K3 66.0 1000
MAP4K4 MAP4K4 99.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 72.0 1000
MAPKAPK5 MAPKAPK5 97.0 1000
MARK1 MARK1 84.0 1000
MARK2 MARK2 97.0 1000
MARK3 MARK3 95.0 1000
MARK4 MARK4 85.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 92.0 1000
MAP2K2 MEK2 84.0 1000
MAP2K3 MEK3 84.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 92.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 100.0 1000
MKNK1 MKNK1 91.0 1000
MKNK2 MKNK2 90.0 1000
MYLK3 MLCK 97.0 1000
MAP3K9 MLK1 89.0 1000
MAP3K10 MLK2 85.0 1000
MAP3K11 MLK3 100.0 1000
CDC42BPA MRCKA 100.0 1000
CDC42BPB MRCKB 82.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 100.0 1000
STK3 MST2 97.0 1000
STK24 MST3 90.0 1000
STK26 MST4 77.0 1000
MTOR MTOR 96.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 90.0 1000
MYLK4 MYLK4 89.0 1000
MYO3A MYO3A 99.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 70.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 92.0 1000
NEK11 NEK11 88.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 79.0 1000
NEK5 NEK5 87.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 66.0 1000
NIM1K NIM1 87.0 1000
NLK NLK 41.0 1000
OXSR1 OSR1 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 94.0 1000
MAPK13 p38-delta 98.0 1000
MAPK12 p38-gamma 79.0 1000
PAK1 PAK1 92.0 1000
PAK2 PAK2 100.0 1000
PAK3 PAK3 75.0 1000
PAK4 PAK4 100.0 1000
PAK6 PAK6 95.0 1000
PAK5 PAK7 92.0 1000
CDK16 PCTK1 78.0 1000
CDK17 PCTK2 90.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 80.0 1000
PDGFRB PDGFRB 84.0 1000
PDPK1 PDPK1 100.0 1000
CDPK1 PFCDPK1(P.falciparum) 100.0 1000
PK5 PFPK5(P.falciparum) 85.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 97.0 1000
PIK3C2B PIK3C2B 97.0 1000
PIK3C2G PIK3C2G 99.0 1000
PIK3CA PIK3CA(Q546K) 85.0 1000
PIK3CB PIK3CB 84.0 1000
PIK3CD PIK3CD 85.0 1000
PIK3CG PIK3CG 89.0 1000
PI4KB PIK4CB 97.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 96.0 1000
PIM2 PIM2 0.0 1000
PIM3 PIM3 97.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 93.0 1000
PIP4K2B PIP5K2B 100.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 88.0 1000
PRKACB PKAC-beta 98.0 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 92.0 1000
PLK2 PLK2 82.0 1000
PLK3 PLK3 73.0 1000
PLK4 PLK4 83.0 1000
PRKCD PRKCD 95.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 98.0 1000
PRKCI PRKCI 100.0 1000
PRKCQ PRKCQ 91.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 92.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 100.0 1000
PRPF4B PRP4 95.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 100.0 1000
RAF1 RAF1 94.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 97.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 86.0 1000
RIPK2 RIPK2 100.0 1000
RIPK4 RIPK4 98.0 1000
DSTYK RIPK5 69.0 1000
ROCK1 ROCK1 71.0 1000
ROCK2 ROCK2 86.0 1000
ROS1 ROS1 100.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 90.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 74.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 96.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 86.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 91.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 95.0 1000
RPS6KB1 S6K1 84.0 1000
SBK1 SBK1 93.0 1000
SGK1 SGK 100.0 1000
SBK3 SgK110 54.0 1000
SGK2 SGK2 100.0 1000
SGK3 SGK3 100.0 1000
SIK1 SIK 98.0 1000
SIK2 SIK2 92.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 100.0 1000
SNRK SNRK 98.0 1000
SRC SRC 100.0 1000
SRMS SRMS 87.0 1000
SRPK1 SRPK1 80.0 1000
SRPK2 SRPK2 77.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 80.0 1000
STK33 STK33 93.0 1000
STK35 STK35 83.0 1000
STK36 STK36 92.0 1000
STK39 STK39 79.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 75.0 1000
TAOK1 TAOK1 85.0 1000
TAOK2 TAOK2 91.0 1000
TAOK3 TAOK3 83.0 1000
TBK1 TBK1 96.0 1000
TEC TEC 94.0 1000
TESK1 TESK1 98.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 90.0 1000
TLK1 TLK1 87.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 66.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 94.0 1000
NTRK1 TRKA 94.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 90.0 1000
TRPM6 TRPM6 85.0 1000
TSSK1B TSSK1B 91.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 89.0 1000
TXK TXK 94.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 93.0 1000
ULK2 ULK2 77.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 80.0 1000
PIK3C3 VPS34 94.0 1000
VRK2 VRK2 29.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 86.0 1000
WNK2 WNK2 79.0 1000
WNK3 WNK3 91.0 1000
WNK4 WNK4 100.0 1000
STK32A YANK1 94.0 1000
STK32B YANK2 97.0 1000
STK32C YANK3 95.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 90.0 1000
MAP3K20 ZAK 90.0 1000
ZAP70 ZAP70 97.0 1000

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BI-2545

Conclusion: Closest hit is the Ca2+ channel DHPSI with 80 % inhibition at 10 µM.

Target protein HGNC name Species Cmp. conc. % Control Assay ID
COX-1 PTGS1 Homo sapiens 10 µM 82.0 Cerep_4173
COX-2 PTGS2 Homo sapiens 10 µM 81.0 Cerep_4186
5HT1A/H HTR1A Homo sapiens 10 µM 83.0 Cerep_131
5HT1B/R HTR1B Rattus norvegicus 10 µM 92.0 Cerep_132
5HT2AH_AGON HTR2A Homo sapiens 10 µM 45.0 Cerep_471
5HT2B/H AG HTR2B Homo sapiens 10 µM 54.0 Cerep_1333
5HT3/H HTR3A Homo sapiens 10 µM 94.0 Cerep_411
A2A/H ADORA2A Homo sapiens 10 µM 107.0 Cerep_4
ACE(HU_AMTCH400) ACHE Homo sapiens 10 µM 109.0 Old_Cerep_363
ALPHA1AH_ANTAG ADRA1A Homo sapiens 10 µM 87.0 Cerep_2338
ALPHA2A/HU ADRA2A Homo sapiens 10 µM 86.0 Cerep_13
ANDROGEN/H AR Homo sapiens 10 µM 103.0 Cerep_933
BETA1/HUM ADRB1 Homo sapiens 10 µM 98.0 Cerep_18
BETA2/HUM ADRB2 Homo sapiens 10 µM 96.0 Cerep_20
BZD/CENTR/R Rattus norvegicus 10 µM 136.0 Cerep_28
CA+/DHPSI/R Rattus norvegicus 10 µM 20.0 Old_Cerep_161
CB1/CENTR/H CNR1 Homo sapiens 10 µM 95.0 Old_Cerep_67
CB2/PERIPH/H CNR2 Homo sapiens 10 µM 77.0 Cerep_37
CCKA/H CCKAR Homo sapiens 10 µM 51.0 Old_Cerep_39
D1/H DRD1 Homo sapiens 10 µM 92.0 Cerep_44
D2SH_AGON DRD2 Homo sapiens 10 µM 97.0 Cerep_1322
DATRANS/HUM SLC6A3 Homo sapiens 10 µM 57.0 Old_Cerep_52
DELTA2/H OPRD1 Homo sapiens 10 µM 82.0 Cerep_114
ETA/H EDNRA Homo sapiens 10 µM 92.0 Cerep_54
GCORTICOID/H NR3C1 Homo sapiens 10 µM 99.0 Old_Cerep_469
H1/PYRIL/HS HRH1 Homo sapiens 10 µM 101.0 Cerep_870
H2/APT/HS HRH2 Homo sapiens 10 µM 110.0 Cerep_1208
HERG_DOFETILIDE KCNH2 Homo sapiens 10 µM 71.0 Cerep_4094
K+/VOLT/RA Rattus norvegicus 10 µM 103.0 Cerep_166
KAPPA/R OPRK1 Rattus norvegicus 10 µM 68.0 Cerep_1971
LCK_CE LCK Homo sapiens 10 µM 96.0 Old_Cerep_2906
M1/H CHRM1 Homo sapiens 10 µM 97.0 Cerep_91
M2/H CHRM2 Homo sapiens 10 µM 100.0 Cerep_93
M3/H CHRM3 Homo sapiens 10 µM 100.0 Cerep_95
MAO-A_ANTAG MAOA Rattus norvegicus 10 µM 70.0 Cerep_443
MU/H OPRM1 Homo sapiens 10 µM 67.0 Cerep_118
NA+/SITE2/R Rattus norvegicus 10 µM 34.0 Old_Cerep_169
NEUP/H SLC6A2 Homo sapiens 10 µM 39.0 Cerep_355
NMDA/R Rattus norvegicus 10 µM 100.0 Cerep_66
N_NEURO_A4B2 CHRNA4
 CHRNB2
 		Homo sapiens 10 µM 111.0 Cerep_3029
PDE3A PDE3A Homo sapiens 10 µM 76.0 Cerep_4072
PDE4D2 PDE4D Homo sapiens 10 µM 98.0 Cerep_4077
SLC6A4/H SCL6A4 Homo sapiens 10 µM 66.0 Cerep_439
V1A/HUM AVPR1A Homo sapiens 10 µM 80.0 Cerep_159