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Selectivity data for probe PF-04457845 and control PF-04875474


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PF-04457845


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
Beta1 ADRB1 16.50
Beta3 ADRB3 0.69
H4 HRH4 17.33
5-HT1B HTR1B 24.44
5-HT1D HTR1D 42.13
5-HT1E HTR1E 18.99
5-HT6 HTR6 40.65
5-HT7A HTR7 37.46
Beta2 ADRB2 0.51
D1 DRD1 -3.23
D2 DRD2 1.84
DOR OPRD1 12.26
H3 HRH3 8.73
M1 CHRM1 29.51
M5 CHRM5 23.53
5-HT1A HTR1A 20.19
GABAA/BZP 7.35
D3 DRD3 4.08
D4 DRD4 -6.93
D5 DRD5 29.27
GABAA -12.82
H1 HRH1 27.24
H2 HRH2 17.27
KOR OPRK1 30.51
MOR OPRM1 17.53
5-HT2A HTR2A 82.92 248.71 6.60
5-HT2B HTR2B 55.67 1338.44 5.87
5-HT2C HTR2C 64.56 1659.20 5.78
5-HT3 HTR3A 10.69
5-HT5A HTR5A 28.40
Alpha1A ADRA1A 10.35
Alpha1B ADRA1B 0.40
Alpha1D ADRA1D 3.84
Alpha2A ADRA2A 34.45
Alpha2B ADRA2B 40.05
Alpha2C ADRA2C 79.30 595.66 6.22
M4 CHRM4 7.38
NET SLC6A2 7.86
Sigma 2 TMEM97 91.31 436.72 6.36
DAT SLC6A3 -30.34
M2 CHRM2 20.77
SERT SLC6A4 20.21
Sigma 1 SIGMAR1 88.52 472.06 6.33
M3 CHRM3 27.49
GABA/PBR 59.63 1140.08 average (n=2) 5.94

PF-04875474


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
M2 CHRM2 20.71
Sigma 2 TMEM97 69.05 8412.01 5.08
5-HT1D HTR1D -2.98
5-HT2A HTR2A -3.55
5-HT2B HTR2B 2.28
5-HT6 HTR6 7.76
5-HT7A HTR7 1.18
Alpha1B ADRA1B 0.27
Alpha1D ADRA1D -10.56
Alpha2A ADRA2A 0.68
Alpha2B ADRA2B -14.99
5-HT2C HTR2C 1.89
5-HT3 HTR3A -0.28
Alpha1A ADRA1A -14.26
DOR OPRD1 -16.28
KOR OPRK1 -16.25
5-HT1A HTR1A -25.01
D3 DRD3 -9.59
D4 DRD4 12.34
D5 DRD5 4.50
GABAA 23.74
H1 HRH1 30.90
H3 HRH3 17.28
H4 HRH4 -20.15
M3 CHRM3 0.26
M4 CHRM4 -7.53
M5 CHRM5 -0.59
GABA/PBR 25.58
Sigma 1 SIGMAR1 32.18
5-HT1B HTR1B 4.80
5-HT1E HTR1E 0.84
5-HT5A HTR5A 7.85
GABAA/BZP 17.30
D1 DRD1 1.14
DAT SLC6A3 -12.39
M1 CHRM1 -6.78
MOR OPRM1 1.18
Beta2 ADRB2 16.77
Beta1 ADRB1 1.97
Beta3 ADRB3 -10.05
D2 DRD2 13.70
NET SLC6A2 -1.00
H2 HRH2 -3.96
SERT SLC6A4 32.70
Alpha2C ADRA2C 0.34

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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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PF-04457845


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 74.0 1000
ABL1 ABL1-phosphorylated 93.0 1000
ABL2 ABL2 99.0 1000
ACVR1 ACVR1 92.0 1000
ACVR1B ACVR1B 88.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 98.0 1000
ACVRL1 ACVRL1 77.0 1000
COQ8A ADCK3 78.0 1000
COQ8B ADCK4 81.0 1000
AKT1 AKT1 93.0 1000
AKT2 AKT2 81.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 100.0 1000
PRKAA1 AMPK-alpha1 88.0 1000
PRKAA2 AMPK-alpha2 100.0 1000
ANKK1 ANKK1 96.0 1000
NUAK1 ARK5 86.0 1000
MAP3K5 ASK1 100.0 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 100.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 88.0 1000
BMPR2 BMPR2 100.0 1000
BMX BMX 71.0 1000
BRAF BRAF(V600E) 100.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 73.0 1000
BRSK2 BRSK2 90.0 1000
BTK BTK 100.0 1000
BUB1 BUB1 100.0 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 100.0 1000
CAMK1D CAMK1D 97.0 1000
CAMK1G CAMK1G 95.0 1000
CAMK2A CAMK2A 72.0 1000
CAMK2B CAMK2B 89.0 1000
CAMK2D CAMK2D 82.0 1000
CAMK2G CAMK2G 74.0 1000
CAMK4 CAMK4 63.0 1000
CAMKK1 CAMKK1 92.0 1000
CAMKK2 CAMKK2 73.0 1000
CASK CASK 92.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 82.0 1000
CDK13 CDC2L5 100.0 1000
CDK19 CDK11 100.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 96.0 1000
CDK5 CDK5 92.0 1000
CDK7 CDK7 100.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 93.0 1000
CDKL1 CDKL1 86.0 1000
CDKL2 CDKL2 92.0 1000
CDKL3 CDKL3 81.0 1000
CDKL5 CDKL5 100.0 1000
CHEK1 CHEK1 78.0 1000
CHEK2 CHEK2 94.0 1000
CIT CIT 79.0 1000
CLK1 CLK1 95.0 1000
CLK2 CLK2 66.0 1000
CLK3 CLK3 100.0 1000
CLK4 CLK4 70.0 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 100.0 1000
CSNK1A1L CSNK1A1L 76.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 92.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 100.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 100.0 1000
DAPK1 DAPK1 100.0 1000
DAPK2 DAPK2 69.0 1000
DAPK3 DAPK3 79.0 1000
DCLK1 DCAMKL1 100.0 1000
DCLK2 DCAMKL2 81.0 1000
DCLK3 DCAMKL3 85.0 1000
DDR1 DDR1 79.0 1000
DDR2 DDR2 100.0 1000
MAP3K12 DLK 100.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 84.0 1000
STK17A DRAK1 79.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 100.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 81.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 81.0 1000
EPHA3 EPHA3 100.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 98.0 1000
EPHA6 EPHA6 78.0 1000
EPHA7 EPHA7 95.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 81.0 1000
EPHB4 EPHB4 69.0 1000
EPHB6 EPHB6 100.0 1000
ERBB2 ERBB2 72.0 1000
ERBB3 ERBB3 84.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 100.0 1000
MAPK1 ERK2 92.0 1000
MAPK6 ERK3 90.0 1000
MAPK4 ERK4 95.0 1000
MAPK7 ERK5 100.0 1000
MAPK15 ERK8 83.0 1000
ERN1 ERN1 92.0 1000
PTK2 FAK 100.0 1000
FER FER 74.0 1000
FES FES 76.0 1000
FGFR1 FGFR1 100.0 1000
FGFR2 FGFR2 96.0 1000
FGFR3 FGFR3(G697C) 100.0 1000
FGFR4 FGFR4 100.0 1000
FGR FGR 63.0 1000
FLT1 FLT1 100.0 1000
FLT3 FLT3-autoinhibited 97.0 1000
FLT4 FLT4 80.0 1000
FRK FRK 100.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 87.0 1000
GRK1 GRK1 89.0 1000
GRK2 GRK2 100.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 97.0 1000
GRK7 GRK7 100.0 1000
GSK3A GSK3A 100.0 1000
GSK3B GSK3B 100.0 1000
HASPIN HASPIN 100.0 1000
HCK HCK 98.0 1000
HIPK1 HIPK1 100.0 1000
HIPK2 HIPK2 100.0 1000
HIPK3 HIPK3 100.0 1000
HIPK4 HIPK4 100.0 1000
MAP4K1 HPK1 80.0 1000
HUNK HUNK 87.0 1000
CILK1 ICK 91.0 1000
IGF1R IGF1R 87.0 1000
CHUK IKK-alpha 93.0 1000
IKBKB IKK-beta 83.0 1000
IKBKE IKK-epsilon 100.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 100.0 1000
IRAK3 IRAK3 86.0 1000
IRAK4 IRAK4 97.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 100.0 1000
JAK2 JAK2(JH1domain-catalytic) 100.0 1000
JAK3 JAK3(JH1domain-catalytic) 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 100.0 1000
LATS2 LATS2 84.0 1000
LCK LCK 80.0 1000
LIMK1 LIMK1 88.0 1000
LIMK2 LIMK2 88.0 1000
STK11 LKB1 100.0 1000
STK10 LOK 74.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 74.0 1000
LYN LYN 100.0 1000
MAP3K13 LZK 100.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 100.0 1000
MAP3K15 MAP3K15 100.0 1000
MAP3K2 MAP3K2 100.0 1000
MAP3K3 MAP3K3 100.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 100.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 100.0 1000
MAPKAPK2 MAPKAPK2 87.0 1000
MAPKAPK5 MAPKAPK5 100.0 1000
MARK1 MARK1 84.0 1000
MARK2 MARK2 100.0 1000
MARK3 MARK3 89.0 1000
MARK4 MARK4 76.0 1000
MAST1 MAST1 100.0 1000
MAP2K1 MEK1 100.0 1000
MAP2K2 MEK2 100.0 1000
MAP2K3 MEK3 100.0 1000
MAP2K4 MEK4 100.0 1000
MAP2K5 MEK5 100.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 81.0 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 100.0 1000
MAP3K9 MLK1 100.0 1000
MAP3K10 MLK2 100.0 1000
MAP3K11 MLK3 74.0 1000
CDC42BPA MRCKA 95.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 77.0 1000
MST1R MST1R 92.0 1000
STK3 MST2 100.0 1000
STK24 MST3 100.0 1000
STK26 MST4 100.0 1000
MTOR MTOR 87.0 1000
MUSK MUSK 100.0 1000
MYLK MYLK 100.0 1000
MYLK2 MYLK2 88.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 100.0 1000
STK38L NDR2 84.0 1000
NEK1 NEK1 98.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 98.0 1000
NEK5 NEK5 97.0 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 100.0 1000
MAPK14 p38-alpha 100.0 1000
MAPK11 p38-beta 83.0 1000
MAPK13 p38-delta 86.0 1000
MAPK12 p38-gamma 100.0 1000
PAK1 PAK1 72.0 1000
PAK2 PAK2 83.0 1000
PAK3 PAK3 73.0 1000
PAK4 PAK4 77.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 100.0 1000
CDK16 PCTK1 100.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 76.0 1000
PDGFRA PDGFRA 100.0 1000
PDGFRB PDGFRB 97.0 1000
PDPK1 PDPK1 85.0 1000
CDPK1 PFCDPK1(P.falciparum) 93.0 1000
PK5 PFPK5(P.falciparum) 100.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 89.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 88.0 1000
PIK3C2B PIK3C2B 91.0 1000
PIK3C2G PIK3C2G 95.0 1000
PIK3CA PIK3CA(Q546K) 45.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 81.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 100.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 85.0 1000
PIM2 PIM2 97.0 1000
PIM3 PIM3 79.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 66.0 1000
PIP4K2B PIP5K2B 83.0 1000
PIP4K2C PIP5K2C 75.0 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 100.0 1000
PKNB PKNB(M.tuberculosis) 95.0 1000
PLK1 PLK1 100.0 1000
PLK2 PLK2 100.0 1000
PLK3 PLK3 100.0 1000
PLK4 PLK4 100.0 1000
PRKCD PRKCD 93.0 1000
PRKCE PRKCE 82.0 1000
PRKCH PRKCH 77.0 1000
PRKCI PRKCI 81.0 1000
PRKCQ PRKCQ 67.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 94.0 1000
PRKD3 PRKD3 83.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 100.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 87.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 97.0 1000
SIK3 QSK 83.0 1000
RAF1 RAF1 63.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 100.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 97.0 1000
RIPK2 RIPK2 94.0 1000
RIPK4 RIPK4 100.0 1000
DSTYK RIPK5 69.0 1000
ROCK1 ROCK1 100.0 1000
ROCK2 ROCK2 100.0 1000
ROS1 ROS1 80.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 100.0 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) 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 100.0 1000
SGK3 SGK3 93.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 74.0 1000
NUAK2 SNARK 88.0 1000
SNRK SNRK 100.0 1000
SRC SRC 88.0 1000
SRMS SRMS 95.0 1000
SRPK1 SRPK1 97.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 81.0 1000
STK16 STK16 90.0 1000
STK33 STK33 100.0 1000
STK35 STK35 100.0 1000
STK36 STK36 100.0 1000
STK39 STK39 100.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 100.0 1000
TAOK1 TAOK1 100.0 1000
TAOK2 TAOK2 100.0 1000
TAOK3 TAOK3 42.0 1000
TBK1 TBK1 100.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 91.0 1000
TGFBR1 TGFBR1 61.0 1000
TGFBR2 TGFBR2 76.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 94.0 1000
TLK1 TLK1 100.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 100.0 1000
TNK1 TNK1 98.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 100.0 1000
NTRK2 TRKB 100.0 1000
NTRK3 TRKC 100.0 1000
TRPM6 TRPM6 98.0 1000
TSSK1B TSSK1B 82.0 1000
TSSK3 TSSK3 100.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 100.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 84.0 1000
ULK2 ULK2 100.0 1000
ULK3 ULK3 100.0 1000
KDR VEGFR2 88.0 1000
PIK3C3 VPS34 100.0 1000
VRK2 VRK2 100.0 1000
WEE1 WEE1 97.0 1000
WEE2 WEE2 77.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 92.0 1000
WNK3 WNK3 100.0 1000
WNK4 WNK4 96.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 82.0 1000
STK32C YANK3 100.0 1000
YES1 YES 100.0 1000
STK25 YSK1 100.0 1000
MAP3K19 YSK4 85.0 1000
MAP3K20 ZAK 95.0 1000
ZAP70 ZAP70 100.0 1000

PF-04875474


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 100.0 1000
ABL1 ABL1-phosphorylated 82.0 1000
ABL2 ABL2 100.0 1000
ACVR1 ACVR1 92.0 1000
ACVR1B ACVR1B 79.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 98.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 96.0 1000
COQ8B ADCK4 94.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 100.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 82.0 1000
PRKAA1 AMPK-alpha1 100.0 1000
PRKAA2 AMPK-alpha2 96.0 1000
ANKK1 ANKK1 73.0 1000
NUAK1 ARK5 100.0 1000
MAP3K5 ASK1 98.0 1000
MAP3K6 ASK2 60.0 1000
AURKA AURKA 100.0 1000
AURKB AURKB 59.0 1000
AURKC AURKC 100.0 1000
AXL AXL 100.0 1000
BMP2K BIKE 100.0 1000
BLK BLK 65.0 1000
BMPR1A BMPR1A 100.0 1000
BMPR1B BMPR1B 91.0 1000
BMPR2 BMPR2 76.0 1000
BMX BMX 100.0 1000
BRAF BRAF(V600E) 85.0 1000
PTK6 BRK 91.0 1000
BRSK1 BRSK1 100.0 1000
BRSK2 BRSK2 100.0 1000
BTK BTK 59.0 1000
BUB1 BUB1 1.4 1000
CAMK1 CAMK1 100.0 1000
PNCK CAMK1B 63.0 1000
CAMK1D CAMK1D 100.0 1000
CAMK1G CAMK1G 100.0 1000
CAMK2A CAMK2A 100.0 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 64.0 1000
CDK11B CDC2L1 100.0 1000
CDK11A CDC2L2 100.0 1000
CDK13 CDC2L5 98.0 1000
CDK19 CDK11 84.0 1000
CDK2 CDK2 100.0 1000
CDK3 CDK3 100.0 1000
CDK4 CDK4-cyclinD3 94.0 1000
CDK5 CDK5 100.0 1000
CDK7 CDK7 81.0 1000
CDK8 CDK8 100.0 1000
CDK9 CDK9 100.0 1000
CDKL1 CDKL1 100.0 1000
CDKL2 CDKL2 100.0 1000
CDKL3 CDKL3 95.0 1000
CDKL5 CDKL5 73.0 1000
CHEK1 CHEK1 100.0 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 98.0 1000
CSF1R CSF1R-autoinhibited 87.0 1000
CSK CSK 100.0 1000
CSNK1A1 CSNK1A1 88.0 1000
CSNK1A1L CSNK1A1L 100.0 1000
CSNK1D CSNK1D 100.0 1000
CSNK1E CSNK1E 100.0 1000
CSNK1G1 CSNK1G1 100.0 1000
CSNK1G2 CSNK1G2 100.0 1000
CSNK1G3 CSNK1G3 100.0 1000
CSNK2A1 CSNK2A1 72.0 1000
CSNK2A2 CSNK2A2 100.0 1000
MATK CTK 59.0 1000
DAPK1 DAPK1 98.0 1000
DAPK2 DAPK2 100.0 1000
DAPK3 DAPK3 100.0 1000
DCLK1 DCAMKL1 84.0 1000
DCLK2 DCAMKL2 100.0 1000
DCLK3 DCAMKL3 100.0 1000
DDR1 DDR1 99.0 1000
DDR2 DDR2 80.0 1000
MAP3K12 DLK 83.0 1000
DMPK DMPK 100.0 1000
CDC42BPG DMPK2 100.0 1000
STK17A DRAK1 100.0 1000
STK17B DRAK2 100.0 1000
DYRK1A DYRK1A 75.0 1000
DYRK1B DYRK1B 100.0 1000
DYRK2 DYRK2 81.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 100.0 1000
EPHA1 EPHA1 100.0 1000
EPHA2 EPHA2 100.0 1000
EPHA3 EPHA3 95.0 1000
EPHA4 EPHA4 100.0 1000
EPHA5 EPHA5 85.0 1000
EPHA6 EPHA6 100.0 1000
EPHA7 EPHA7 100.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 100.0 1000
EPHB2 EPHB2 100.0 1000
EPHB3 EPHB3 100.0 1000
EPHB4 EPHB4 100.0 1000
EPHB6 EPHB6 87.0 1000
ERBB2 ERBB2 83.0 1000
ERBB3 ERBB3 99.0 1000
ERBB4 ERBB4 100.0 1000
MAPK3 ERK1 99.0 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 67.0 1000
PTK2 FAK 100.0 1000
FER FER 100.0 1000
FES FES 91.0 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 86.0 1000
FLT4 FLT4 100.0 1000
FRK FRK 82.0 1000
FYN FYN 100.0 1000
GAK GAK 100.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 97.0 1000
GRK1 GRK1 82.0 1000
GRK2 GRK2 96.0 1000
GRK3 GRK3 100.0 1000
GRK4 GRK4 100.0 1000
GRK7 GRK7 85.0 1000
GSK3A GSK3A 92.0 1000
GSK3B GSK3B 77.0 1000
HASPIN HASPIN 79.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 88.0 1000
HIPK2 HIPK2 89.0 1000
HIPK3 HIPK3 74.0 1000
HIPK4 HIPK4 92.0 1000
MAP4K1 HPK1 98.0 1000
HUNK HUNK 89.0 1000
CILK1 ICK 80.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 69.0 1000
IKBKB IKK-beta 94.0 1000
IKBKE IKK-epsilon 77.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 66.0 1000
IRAK3 IRAK3 100.0 1000
IRAK4 IRAK4 100.0 1000
ITK ITK 100.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 95.0 1000
JAK2 JAK2(JH1domain-catalytic) 88.0 1000
JAK3 JAK3(JH1domain-catalytic) 100.0 1000
MAPK8 JNK1 75.0 1000
MAPK9 JNK2 72.0 1000
MAPK10 JNK3 77.0 1000
KIT KIT-autoinhibited 78.0 1000
LATS1 LATS1 91.0 1000
LATS2 LATS2 100.0 1000
LCK LCK 100.0 1000
LIMK1 LIMK1 88.0 1000
LIMK2 LIMK2 95.0 1000
STK11 LKB1 64.0 1000
STK10 LOK 94.0 1000
LRRK2 LRRK2(G2019S) 100.0 1000
LTK LTK 100.0 1000
LYN LYN 97.0 1000
MAP3K13 LZK 0.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 66.0 1000
MAP3K15 MAP3K15 81.0 1000
MAP3K2 MAP3K2 79.0 1000
MAP3K3 MAP3K3 79.0 1000
MAP3K4 MAP3K4 100.0 1000
MAP4K2 MAP4K2 80.0 1000
MAP4K3 MAP4K3 100.0 1000
MAP4K4 MAP4K4 100.0 1000
MAP4K5 MAP4K5 94.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 76.0 1000
MARK1 MARK1 100.0 1000
MARK2 MARK2 80.0 1000
MARK3 MARK3 100.0 1000
MARK4 MARK4 100.0 1000
MAST1 MAST1 58.0 1000
MAP2K1 MEK1 93.0 1000
MAP2K2 MEK2 95.0 1000
MAP2K3 MEK3 72.0 1000
MAP2K4 MEK4 74.0 1000
MAP2K5 MEK5 88.0 1000
MAP2K6 MEK6 100.0 1000
MELK MELK 100.0 1000
MERTK MERTK 100.0 1000
MET MET(Y1235D) 100.0 1000
MINK1 MINK 100.0 1000
MAP2K7 MKK7 91.0 1000
MKNK1 MKNK1 67.0 1000
MKNK2 MKNK2 77.0 1000
MYLK3 MLCK 85.0 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 80.0 1000
STK24 MST3 98.0 1000
STK26 MST4 71.0 1000
MTOR MTOR 100.0 1000
MUSK MUSK 97.0 1000
MYLK MYLK 73.0 1000
MYLK2 MYLK2 87.0 1000
MYLK4 MYLK4 100.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 100.0 1000
STK38 NDR1 99.0 1000
STK38L NDR2 100.0 1000
NEK1 NEK1 100.0 1000
NEK10 NEK10 100.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 100.0 1000
NEK3 NEK3 100.0 1000
NEK4 NEK4 95.0 1000
NEK5 NEK5 100.0 1000
NEK6 NEK6 100.0 1000
NEK7 NEK7 100.0 1000
NEK9 NEK9 100.0 1000
MAP3K14 NIK 77.0 1000
NIM1K NIM1 76.0 1000
NLK NLK 100.0 1000
OXSR1 OSR1 71.0 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 90.0 1000
PAK2 PAK2 95.0 1000
PAK3 PAK3 100.0 1000
PAK4 PAK4 96.0 1000
PAK6 PAK6 100.0 1000
PAK5 PAK7 95.0 1000
CDK16 PCTK1 81.0 1000
CDK17 PCTK2 100.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 80.0 1000
PDGFRB PDGFRB 81.0 1000
PDPK1 PDPK1 97.0 1000
CDPK1 PFCDPK1(P.falciparum) 99.0 1000
PK5 PFPK5(P.falciparum) 93.0 1000
CDK15 PFTAIRE2 100.0 1000
CDK14 PFTK1 100.0 1000
PHKG1 PHKG1 100.0 1000
PHKG2 PHKG2 100.0 1000
PIK3C2B PIK3C2B 93.0 1000
PIK3C2G PIK3C2G 100.0 1000
PIK3CA PIK3CA(Q546K) 92.0 1000
PIK3CB PIK3CB 79.0 1000
PIK3CD PIK3CD 64.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 91.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 91.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 100.0 1000
PIP5K1A PIP5K1A 100.0 1000
PIP5K1C PIP5K1C 100.0 1000
PIP4K2B PIP5K2B 96.0 1000
PIP4K2C PIP5K2C 100.0 1000
PRKACA PKAC-alpha 93.0 1000
PRKACB PKAC-beta 100.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 100.0 1000
PKN2 PKN2 100.0 1000
PKNB PKNB(M.tuberculosis) 87.0 1000
PLK1 PLK1 87.0 1000
PLK2 PLK2 60.0 1000
PLK3 PLK3 80.0 1000
PLK4 PLK4 98.0 1000
PRKCD PRKCD 100.0 1000
PRKCE PRKCE 100.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 96.0 1000
PRKCQ PRKCQ 100.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 100.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 91.0 1000
EIF2AK2 PRKR 100.0 1000
PRKX PRKX 92.0 1000
PRPF4B PRP4 100.0 1000
PTK2B PYK2 100.0 1000
SIK3 QSK 74.0 1000
RAF1 RAF1 100.0 1000
RET RET(V804M) 100.0 1000
RIOK1 RIOK1 100.0 1000
RIOK2 RIOK2 77.0 1000
RIOK3 RIOK3 100.0 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 93.0 1000
RIPK4 RIPK4 74.0 1000
DSTYK RIPK5 65.0 1000
ROCK1 ROCK1 82.0 1000
ROCK2 ROCK2 90.0 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) 92.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 100.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 89.0 1000
RPS6KB1 S6K1 71.0 1000
SBK1 SBK1 89.0 1000
SGK1 SGK 85.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 74.0 1000
SGK3 SGK3 87.0 1000
SIK1 SIK 100.0 1000
SIK2 SIK2 100.0 1000
SLK SLK 100.0 1000
NUAK2 SNARK 73.0 1000
SNRK SNRK 100.0 1000
SRC SRC 100.0 1000
SRMS SRMS 67.0 1000
SRPK1 SRPK1 82.0 1000
SRPK2 SRPK2 100.0 1000
SRPK3 SRPK3 100.0 1000
STK16 STK16 98.0 1000
STK33 STK33 100.0 1000
STK35 STK35 94.0 1000
STK36 STK36 100.0 1000
STK39 STK39 77.0 1000
SYK SYK 100.0 1000
MAP3K7 TAK1 93.0 1000
TAOK1 TAOK1 91.0 1000
TAOK2 TAOK2 66.0 1000
TAOK3 TAOK3 82.0 1000
TBK1 TBK1 72.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 100.0 1000
TGFBR1 TGFBR1 100.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 100.0 1000
TEK TIE2 84.0 1000
TLK1 TLK1 98.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 92.0 1000
TNK1 TNK1 100.0 1000
TNK2 TNK2 100.0 1000
TNNI3K TNNI3K 100.0 1000
NTRK1 TRKA 82.0 1000
NTRK2 TRKB 77.0 1000
NTRK3 TRKC 85.0 1000
TRPM6 TRPM6 73.0 1000
TSSK1B TSSK1B 100.0 1000
TSSK3 TSSK3 98.0 1000
TTK TTK 100.0 1000
TXK TXK 100.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 79.0 1000
TYRO3 TYRO3 100.0 1000
ULK1 ULK1 79.0 1000
ULK2 ULK2 73.0 1000
ULK3 ULK3 82.0 1000
KDR VEGFR2 64.0 1000
PIK3C3 VPS34 88.0 1000
VRK2 VRK2 97.0 1000
WEE1 WEE1 100.0 1000
WEE2 WEE2 100.0 1000
WNK1 WNK1 100.0 1000
WNK2 WNK2 0.0 1000
WNK3 WNK3 84.0 1000
WNK4 WNK4 0.0 1000
STK32A YANK1 100.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 100.0 1000
YES1 YES 100.0 1000
STK25 YSK1 91.0 1000
MAP3K19 YSK4 90.0 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 90.0 1000

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PF-04457845

Ligand profiling has been performed at 10 µM probe concentration with IC50 and Ki follow up for specific targets.

Conclusion: Clean panel. The closest off-target at 10 µM is HTR2A (Ki = 1.6 µM).

Target protein HGNC name Species % inhibition at 10 µM Ki [µM]
A1 (h) ADORA1 Homo sapiens 3.0
A2A (h) ADORA2A Homo sapiens -11.0
alpha1 (non-selective) -2.0
alpha2A (h) ADRA2A Homo sapiens -4.0
alpha2B (h) ADRA2B Homo sapiens 4.0
beta1 (h) ADRB1 Homo sapiens 1.0
beta2 (h) ADRB2 Homo sapiens -11.0
AT1 (h) AGTR1 Homo sapiens -10.0
BZD (central) 15.0
CB1 (h) CNR1 Homo sapiens 55.0 14.00
CB2 (h) CNR2 Homo sapiens 55.0 5.10
CCKA (h) (CCK1) CCKAR Homo sapiens -10.0
CCKB (h) (CCK2) CCKBR Homo sapiens -6.0
D1 (h) DRD1 Homo sapiens 3.0
D2S (h) DRD2 Homo sapiens -9.0
D3 (h) DRD3 Homo sapiens 3.0
GABAA -4.0
GABAB(1b) (h) GABBR1 Homo sapiens -13.0
AMPA GRIA2 -8.0
Kainate GRIK2 2.0
NMDA -3.0
Glycine (strychnine-insensitive) -2.0
H1 (h) HRH1 Homo sapiens -1.0
H2 (h) HRH2 Homo sapiens -6.0
H3 (h) HRH3 Homo sapiens 10.0
MAO-A MAOA 13.0
M1 (h) CHRM1 Homo sapiens 36.0
M2 (h) CHRM2 Homo sapiens 15.0
M3 (h) CHRM3 Homo sapiens 11.0
N(neuronal) (α-BGTX-insensitive) (α4β2 nicotinic receptor) CHRNA4 8.0
N (h) (muscle-type) CHRNA1 Homo sapiens -25.0
mu (h) (MOP) (agonist site) OPRM1 Homo sapiens 3.0
delta2 (h) (DOP) OPRD1 Homo sapiens 2.0
kappa (KOP) OPRK1 0.0
5-HT1A (h) HTR1A Homo sapiens 6.0
5-HT1B HTR1B -3.0
5-HT2A (h) (agonist site) HTR2A Homo sapiens 57.0 1.60
5-HT2B (h) (agonist site) HTR2B Homo sapiens 35.0
5-HT2C (h) (agonist site) HTR2C Homo sapiens -3.0
5-HT3 (h) HTR3A Homo sapiens -8.0
5-HT4e (h) HTR4 Homo sapiens -8.0
5-HT7 (h) HTR7 Homo sapiens 7.0
Glucocorticoid (h) (GR) NR3C1 Homo sapiens -25.0
V1a (h) AVPR1A Homo sapiens 8.0
Ca2+ channel (L, DHP site) 11.0
Ca2+ channel (L, diltiazem site) (benzothiazepines) 1.0
Ca2+ channel (L, verapamil site) (phenylalkylamines) -5.0
Ca2+ channel (N) -5.0
Na+ channel (site 2) 13.0
CI channel 78.0 3.00
NE transporter (h) SLC6A2 Homo sapiens -5.0
DA transporter (h) SLC6A3 Homo sapiens -1.0
5-HT transporter (h) SLC6A4 Homo sapiens 11.0
GABA transporter SLC6A1 -1.0
Choline transporter (h) (CHT1) SLC5A7 Homo sapiens 18.0
COX2 (h) PTGS2 Homo sapiens -37.0
PDE 3 (h) Homo sapiens 10.0
PDE 4 (h) Homo sapiens 18.0
ACE (h) ACE Homo sapiens -15.0
p38alpha kinase (h) MAPK14 Homo sapiens 1.0
FLT-1 (h) (VEGFR1) FLT1 Homo sapiens 4.0
ATPase (Na+/K+) -2.0
Acetylcholinesterase (h) ACHE Homo sapiens 10.0