Selectivity data for probe PF-04554878 and control PF-00911705


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PF-04554878


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
M3 CHRM3 23.79
Sigma 1 SIGMAR1 40.13
DAT SLC6A3 -6.06
M2 CHRM2 19.53
SERT SLC6A4 2.45
5-HT1A HTR1A -9.76
GABAA/BZP -7.85
D3 DRD3 11.35
D4 DRD4 7.80
D5 DRD5 -7.46
GABAA -23.32
H1 HRH1 -3.38
H2 HRH2 30.19
KOR OPRK1 10.82
MOR OPRM1 -10.65
5-HT1B HTR1B 12.54
5-HT1D HTR1D -15.19
5-HT1E HTR1E 18.19
5-HT6 HTR6 -8.99
5-HT7A HTR7 5.31
Beta2 ADRB2 -13.22
D1 DRD1 -53.29 > 10000.00 < 5.00
D2 DRD2 -33.27
DOR OPRD1 -0.28
H3 HRH3 -7.94
M1 CHRM1 19.29
M5 CHRM5 5.41
Beta1 ADRB1 -0.83
Beta3 ADRB3 4.63
H4 HRH4 -19.63
5-HT2A HTR2A 0.93
5-HT2B HTR2B 5.73
5-HT2C HTR2C 16.90
5-HT3 HTR3A 6.50
5-HT5A HTR5A -1.91
Alpha1A ADRA1A -4.42
Alpha1B ADRA1B -0.22
Alpha1D ADRA1D 4.13
Alpha2A ADRA2A 9.61
Alpha2B ADRA2B 5.76
Alpha2C ADRA2C 4.73
M4 CHRM4 -19.39
NET SLC6A2 7.81
Sigma 2 TMEM97 48.11
GABA/PBR 31.42

PF-00911705


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
M2 CHRM2 -2.08
Sigma 2 TMEM97 60.30 2123.24 5.67
5-HT1D HTR1D 0.19
5-HT2A HTR2A 4.75
5-HT2B HTR2B 13.50
5-HT6 HTR6 11.07
5-HT7A HTR7 -4.55
Alpha1B ADRA1B 0.50
Alpha1D ADRA1D 15.94
Alpha2A ADRA2A 0.40
Alpha2B ADRA2B -4.21
5-HT2C HTR2C 8.11
5-HT3 HTR3A 1.24
Alpha1A ADRA1A -3.55
DOR OPRD1 -6.88
KOR OPRK1 -31.13
5-HT1A HTR1A -13.08
D3 DRD3 -11.78
D4 DRD4 2.34
D5 DRD5 -0.97
GABAA 10.28
H3 HRH3 12.94
H4 HRH4 -22.64
M3 CHRM3 -4.64
M4 CHRM4 8.94
M5 CHRM5 -6.47
GABA/PBR 62.09 1479.11 5.83
Sigma 1 SIGMAR1 23.12
5-HT1B HTR1B 5.78
5-HT1E HTR1E -26.40
5-HT5A HTR5A 1.82
GABAA/BZP 29.52
D1 DRD1 0.76
DAT SLC6A3 -11.64
M1 CHRM1 -6.58
MOR OPRM1 0.77
NET SLC6A2 3.15
Beta2 ADRB2 15.30
Beta1 ADRB1 16.45
Beta3 ADRB3 1.64
D2 DRD2 9.12
H1 HRH1 21.39
H2 HRH2 1.75
SERT SLC6A4 33.55
Alpha2C ADRA2C 4.91

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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

PF-04554878


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 80.0 100
ABL1 ABL1-phosphorylated 100.0 100
ABL2 ABL2 93.0 100
ACVR1 ACVR1 100.0 100
ACVR1B ACVR1B 69.0 100
ACVR2A ACVR2A 90.0 100
ACVR2B ACVR2B 100.0 100
ACVRL1 ACVRL1 100.0 100
COQ8A ADCK3 98.0 100
COQ8B ADCK4 88.0 100
AKT1 AKT1 100.0 100
AKT2 AKT2 77.0 100
AKT3 AKT3 36.0 100
ALK ALK(L1196M) 85.0 100
PRKAA1 AMPK-alpha1 84.0 100
PRKAA2 AMPK-alpha2 100.0 100
ANKK1 ANKK1 88.0 100
NUAK1 ARK5 31.0 100
MAP3K5 ASK1 100.0 100
MAP3K6 ASK2 90.0 100
AURKA AURKA 50.0 100
AURKB AURKB 73.0 100
AURKC AURKC 47.0 100
AXL AXL 51.0 100
BMP2K BIKE 81.0 100
BLK BLK 78.0 100
BMPR1A BMPR1A 100.0 100
BMPR1B BMPR1B 65.0 100
BMPR2 BMPR2 91.0 100
BMX BMX 71.0 100
BRAF BRAF(V600E) 100.0 100
PTK6 BRK 100.0 100
BRSK1 BRSK1 100.0 100
BRSK2 BRSK2 100.0 100
BTK BTK 83.0 100
BUB1 BUB1 100.0 100
CAMK1 CAMK1 100.0 100
PNCK CAMK1B 100.0 100
CAMK1D CAMK1D 100.0 100
CAMK1G CAMK1G 89.0 100
CAMK2A CAMK2A 83.0 100
CAMK2B CAMK2B 86.0 100
CAMK2D CAMK2D 83.0 100
CAMK2G CAMK2G 79.0 100
CAMK4 CAMK4 100.0 100
CAMKK1 CAMKK1 75.0 100
CAMKK2 CAMKK2 68.0 100
CASK CASK 88.0 100
CDK11B CDC2L1 95.0 100
CDK11A CDC2L2 77.0 100
CDK13 CDC2L5 94.0 100
CDK19 CDK11 100.0 100
CDK2 CDK2 97.0 100
CDK3 CDK3 100.0 100
CDK4 CDK4-cyclinD3 100.0 100
CDK5 CDK5 81.0 100
CDK7 CDK7 59.0 100
CDK8 CDK8 50.0 100
CDK9 CDK9 86.0 100
CDKL1 CDKL1 82.0 100
CDKL2 CDKL2 79.0 100
CDKL3 CDKL3 92.0 100
CDKL5 CDKL5 100.0 100
CHEK1 CHEK1 100.0 100
CHEK2 CHEK2 100.0 100
CIT CIT 68.0 100
CLK1 CLK1 23.0 100
CLK2 CLK2 0.0 100
CLK3 CLK3 97.0 100
CLK4 CLK4 25.0 100
CSF1R CSF1R-autoinhibited 76.0 100
CSK CSK 100.0 100
CSNK1A1 CSNK1A1 94.0 100
CSNK1A1L CSNK1A1L 77.0 100
CSNK1D CSNK1D 98.0 100
CSNK1E CSNK1E 100.0 100
CSNK1G1 CSNK1G1 82.0 100
CSNK1G2 CSNK1G2 99.0 100
CSNK1G3 CSNK1G3 100.0 100
CSNK2A1 CSNK2A1 61.0 100
CSNK2A2 CSNK2A2 28.0 100
MATK CTK 37.0 100
DAPK1 DAPK1 82.0 100
DAPK2 DAPK2 68.0 100
DAPK3 DAPK3 75.0 100
DCLK1 DCAMKL1 99.0 100
DCLK2 DCAMKL2 71.0 100
DCLK3 DCAMKL3 67.0 100
DDR1 DDR1 100.0 100
DDR2 DDR2 100.0 100
MAP3K12 DLK 83.0 100
DMPK DMPK 16.0 100
CDC42BPG DMPK2 80.0 100
STK17A DRAK1 19.0 100
STK17B DRAK2 100.0 100
DYRK1A DYRK1A 71.0 100
DYRK1B DYRK1B 79.0 100
DYRK2 DYRK2 76.0 100
EGFR EGFR(T790M) 99.0 100
EIF2AK1 EIF2AK1 85.0 100
EPHA1 EPHA1 98.0 100
EPHA2 EPHA2 86.0 100
EPHA3 EPHA3 82.0 100
EPHA4 EPHA4 99.0 100
EPHA5 EPHA5 64.0 100
EPHA6 EPHA6 85.0 100
EPHA7 EPHA7 68.0 100
EPHA8 EPHA8 87.0 100
EPHB1 EPHB1 87.0 100
EPHB2 EPHB2 76.0 100
EPHB3 EPHB3 87.0 100
EPHB4 EPHB4 94.0 100
EPHB6 EPHB6 100.0 100
ERBB2 ERBB2 100.0 100
ERBB3 ERBB3 93.0 100
ERBB4 ERBB4 84.0 100
MAPK3 ERK1 86.0 100
MAPK1 ERK2 76.0 100
MAPK6 ERK3 71.0 100
MAPK4 ERK4 87.0 100
MAPK7 ERK5 87.0 100
MAPK15 ERK8 40.0 100
ERN1 ERN1 75.0 100
PTK2 FAK 0.2 100
FER FER 83.0 100
FES FES 82.0 100
FGFR1 FGFR1 89.0 100
FGFR2 FGFR2 100.0 100
FGFR3 FGFR3(G697C) 100.0 100
FGFR4 FGFR4 95.0 100
FGR FGR 81.0 100
FLT1 FLT1 63.0 100
FLT3 FLT3-autoinhibited 74.0 100
FLT4 FLT4 39.0 100
FRK FRK 100.0 100
FYN FYN 100.0 100
GAK GAK 69.0 100
EIF2AK4 GCN2(Kin.Dom.2,S808G) 27.0 100
GRK1 GRK1 99.0 100
GRK2 GRK2 89.0 100
GRK3 GRK3 80.0 100
GRK4 GRK4 98.0 100
GRK7 GRK7 97.0 100
GSK3A GSK3A 83.0 100
GSK3B GSK3B 87.0 100
HASPIN HASPIN 100.0 100
HCK HCK 100.0 100
HIPK1 HIPK1 27.0 100
HIPK2 HIPK2 37.0 100
HIPK3 HIPK3 47.0 100
HIPK4 HIPK4 54.0 100
MAP4K1 HPK1 18.0 100
HUNK HUNK 100.0 100
CILK1 ICK 68.0 100
IGF1R IGF1R 84.0 100
CHUK IKK-alpha 98.0 100
IKBKB IKK-beta 100.0 100
IKBKE IKK-epsilon 99.0 100
INSR INSR 91.0 100
INSRR INSRR 95.0 100
IRAK1 IRAK1 77.0 100
IRAK3 IRAK3 70.0 100
IRAK4 IRAK4 92.0 100
ITK ITK 80.0 100
JAK1 JAK1(JH2domain-pseudokinase) 29.0 100
JAK2 JAK2(JH1domain-catalytic) 4.8 100
JAK3 JAK3(JH1domain-catalytic) 8.2 100
MAPK8 JNK1 100.0 100
MAPK9 JNK2 95.0 100
MAPK10 JNK3 100.0 100
KIT KIT-autoinhibited 100.0 100
LATS1 LATS1 96.0 100
LATS2 LATS2 65.0 100
LCK LCK 87.0 100
LIMK1 LIMK1 100.0 100
LIMK2 LIMK2 87.0 100
STK11 LKB1 100.0 100
STK10 LOK 77.0 100
LRRK2 LRRK2(G2019S) 65.0 100
LTK LTK 89.0 100
LYN LYN 85.0 100
MAP3K13 LZK 98.0 100
MAK MAK 85.0 100
MAP3K1 MAP3K1 100.0 100
MAP3K15 MAP3K15 95.0 100
MAP3K2 MAP3K2 65.0 100
MAP3K3 MAP3K3 81.0 100
MAP3K4 MAP3K4 100.0 100
MAP4K2 MAP4K2 100.0 100
MAP4K3 MAP4K3 95.0 100
MAP4K4 MAP4K4 98.0 100
MAP4K5 MAP4K5 100.0 100
MAPKAPK2 MAPKAPK2 100.0 100
MAPKAPK5 MAPKAPK5 76.0 100
MARK1 MARK1 100.0 100
MARK2 MARK2 66.0 100
MARK3 MARK3 90.0 100
MARK4 MARK4 83.0 100
MAST1 MAST1 100.0 100
MAP2K1 MEK1 100.0 100
MAP2K2 MEK2 100.0 100
MAP2K3 MEK3 48.0 100
MAP2K4 MEK4 71.0 100
MAP2K5 MEK5 89.0 100
MAP2K6 MEK6 77.0 100
MELK MELK 23.0 100
MERTK MERTK 54.0 100
MET MET(Y1235D) 71.0 100
MINK1 MINK 44.0 100
MAP2K7 MKK7 97.0 100
MKNK1 MKNK1 83.0 100
MKNK2 MKNK2 100.0 100
MYLK3 MLCK 100.0 100
MAP3K9 MLK1 44.0 100
MAP3K10 MLK2 68.0 100
MAP3K11 MLK3 35.0 100
CDC42BPA MRCKA 98.0 100
CDC42BPB MRCKB 90.0 100
STK4 MST1 97.0 100
MST1R MST1R 100.0 100
STK3 MST2 68.0 100
STK24 MST3 54.0 100
STK26 MST4 95.0 100
MTOR MTOR 100.0 100
MUSK MUSK 100.0 100
MYLK MYLK 75.0 100
MYLK2 MYLK2 63.0 100
MYLK4 MYLK4 100.0 100
MYO3A MYO3A 100.0 100
MYO3B MYO3B 100.0 100
STK38 NDR1 86.0 100
STK38L NDR2 73.0 100
NEK1 NEK1 75.0 100
NEK10 NEK10 100.0 100
NEK11 NEK11 89.0 100
NEK2 NEK2 75.0 100
NEK3 NEK3 100.0 100
NEK4 NEK4 76.0 100
NEK5 NEK5 100.0 100
NEK6 NEK6 81.0 100
NEK7 NEK7 70.0 100
NEK9 NEK9 80.0 100
MAP3K14 NIK 92.0 100
NIM1K NIM1 100.0 100
NLK NLK 100.0 100
OXSR1 OSR1 100.0 100
MAPK14 p38-alpha 100.0 100
MAPK11 p38-beta 76.0 100
MAPK13 p38-delta 91.0 100
MAPK12 p38-gamma 67.0 100
PAK1 PAK1 75.0 100
PAK2 PAK2 72.0 100
PAK3 PAK3 100.0 100
PAK4 PAK4 58.0 100
PAK6 PAK6 100.0 100
PAK5 PAK7 62.0 100
CDK16 PCTK1 99.0 100
CDK17 PCTK2 88.0 100
CDK18 PCTK3 68.0 100
PDGFRA PDGFRA 77.0 100
PDGFRB PDGFRB 83.0 100
PDPK1 PDPK1 81.0 100
CDPK1 PFCDPK1(P.falciparum) 85.0 100
PK5 PFPK5(P.falciparum) 89.0 100
CDK15 PFTAIRE2 67.0 100
CDK14 PFTK1 88.0 100
PHKG1 PHKG1 100.0 100
PHKG2 PHKG2 75.0 100
PIK3C2B PIK3C2B 87.0 100
PIK3C2G PIK3C2G 92.0 100
PIK3CA PIK3CA(Q546K) 17.0 100
PIK3CB PIK3CB 45.0 100
PIK3CD PIK3CD 90.0 100
PIK3CG PIK3CG 100.0 100
PI4KB PIK4CB 99.0 100
PIKFYVE PIKFYVE 100.0 100
PIM1 PIM1 93.0 100
PIM2 PIM2 100.0 100
PIM3 PIM3 82.0 100
PIP5K1A PIP5K1A 98.0 100
PIP5K1C PIP5K1C 100.0 100
PIP4K2B PIP5K2B 91.0 100
PIP4K2C PIP5K2C 40.0 100
PRKACA PKAC-alpha 100.0 100
PRKACB PKAC-beta 93.0 100
PKMYT1 PKMYT1 94.0 100
PKN1 PKN1 100.0 100
PKN2 PKN2 37.0 100
PKNB PKNB(M.tuberculosis) 69.0 100
PLK1 PLK1 84.0 100
PLK2 PLK2 77.0 100
PLK3 PLK3 91.0 100
PLK4 PLK4 79.0 100
PRKCD PRKCD 100.0 100
PRKCE PRKCE 100.0 100
PRKCH PRKCH 86.0 100
PRKCI PRKCI 84.0 100
PRKCQ PRKCQ 89.0 100
PRKD1 PRKD1 100.0 100
PRKD2 PRKD2 100.0 100
PRKD3 PRKD3 100.0 100
PRKG1 PRKG1 100.0 100
PRKG2 PRKG2 100.0 100
EIF2AK2 PRKR 100.0 100
PRKX PRKX 95.0 100
PRPF4B PRP4 69.0 100
PTK2B PYK2 8.3 100
SIK3 QSK 82.0 100
RAF1 RAF1 97.0 100
RET RET(V804M) 30.0 100
RIOK1 RIOK1 100.0 100
RIOK2 RIOK2 85.0 100
RIOK3 RIOK3 55.0 100
RIPK1 RIPK1 100.0 100
RIPK2 RIPK2 100.0 100
RIPK4 RIPK4 89.0 100
DSTYK RIPK5 87.0 100
ROCK1 ROCK1 100.0 100
ROCK2 ROCK2 100.0 100
ROS1 ROS1 58.0 100
STK25 YSK1 85.0 100
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 57.0 100
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 80.0 100
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 71.0 100
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 100.0 100
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 61.0 100
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 49.0 100
RPS6KB1 S6K1 96.0 100
SBK1 SBK1 67.0 100
SGK1 SGK 56.0 100
SBK3 SgK110 100.0 100
SGK2 SGK2 96.0 100
SGK3 SGK3 85.0 100
SIK1 SIK 90.0 100
SIK2 SIK2 100.0 100
SLK SLK 53.0 100
NUAK2 SNARK 53.0 100
SNRK SNRK 100.0 100
SRC SRC 79.0 100
SRMS SRMS 96.0 100
SRPK1 SRPK1 51.0 100
SRPK2 SRPK2 100.0 100
SRPK3 SRPK3 100.0 100
STK16 STK16 7.7 100
STK33 STK33 68.0 100
STK35 STK35 100.0 100
STK36 STK36 89.0 100
STK39 STK39 100.0 100
SYK SYK 66.0 100
MAP3K7 TAK1 57.0 100
TAOK1 TAOK1 50.0 100
TAOK2 TAOK2 92.0 100
TAOK3 TAOK3 26.0 100
TBK1 TBK1 75.0 100
TEC TEC 100.0 100
TESK1 TESK1 96.0 100
TGFBR1 TGFBR1 87.0 100
TGFBR2 TGFBR2 100.0 100
TIE1 TIE1 47.0 100
TEK TIE2 69.0 100
TLK1 TLK1 73.0 100
TLK2 TLK2 90.0 100
TNIK TNIK 65.0 100
TNK1 TNK1 100.0 100
TNK2 TNK2 100.0 100
TNNI3K TNNI3K 100.0 100
NTRK1 TRKA 13.0 100
NTRK2 TRKB 21.0 100
NTRK3 TRKC 41.0 100
TRPM6 TRPM6 98.0 100
TSSK1B TSSK1B 64.0 100
TSSK3 TSSK3 77.0 100
TTK TTK 8.3 100
TXK TXK 98.0 100
TYK2 TYK2(JH2domain-pseudokinase) 87.0 100
TYRO3 TYRO3 100.0 100
ULK1 ULK1 47.0 100
ULK2 ULK2 75.0 100
ULK3 ULK3 75.0 100
KDR VEGFR2 73.0 100
PIK3C3 VPS34 100.0 100
VRK2 VRK2 85.0 100
WEE1 WEE1 95.0 100
WEE2 WEE2 97.0 100
WNK1 WNK1 100.0 100
WNK2 WNK2 94.0 100
WNK3 WNK3 100.0 100
WNK4 WNK4 81.0 100
STK32A YANK1 71.0 100
STK32B YANK2 97.0 100
STK32C YANK3 100.0 100
YES1 YES 100.0 100
MAP3K19 YSK4 1.7 100
MAP3K20 ZAK 100.0 100
ZAP70 ZAP70 100.0 100

PF-00911705


HGNC target name DiscoverX gene symbol of kinase % Control Compound Concentration [nM] Kd [nM]
AAK1 AAK1 27.0 1000
ABL1 ABL1-phosphorylated 40.0 1000
ABL2 ABL2 75.0 1000
ACVR1 ACVR1 91.0 1000
ACVR1B ACVR1B 26.0 1000
ACVR2A ACVR2A 100.0 1000
ACVR2B ACVR2B 73.0 1000
ACVRL1 ACVRL1 100.0 1000
COQ8A ADCK3 79.0 1000
COQ8B ADCK4 84.0 1000
AKT1 AKT1 100.0 1000
AKT2 AKT2 82.0 1000
AKT3 AKT3 100.0 1000
ALK ALK(L1196M) 65.0 1000
PRKAA1 AMPK-alpha1 80.0 1000
PRKAA2 AMPK-alpha2 87.0 1000
ANKK1 ANKK1 84.0 1000
NUAK1 ARK5 21.0 1000
MAP3K5 ASK1 100.0 1000
MAP3K6 ASK2 73.0 1000
AURKA AURKA 14.0 1000
AURKB AURKB 9.9 1000
AURKC AURKC 14.0 1000
AXL AXL 21.0 1000
BMP2K BIKE 2.3 1000
BLK BLK 40.0 1000
BMPR1A BMPR1A 89.0 1000
BMPR1B BMPR1B 3.6 1000
BMPR2 BMPR2 60.0 1000
BMX BMX 80.0 1000
BRAF BRAF(V600E) 68.0 1000
PTK6 BRK 100.0 1000
BRSK1 BRSK1 43.0 1000
BRSK2 BRSK2 97.0 1000
BTK BTK 63.0 1000
BUB1 BUB1 91.0 1000
CAMK1 CAMK1 72.0 1000
PNCK CAMK1B 66.0 1000
CAMK1D CAMK1D 79.0 1000
CAMK1G CAMK1G 95.0 1000
CAMK2A CAMK2A 67.0 1000
CAMK2B CAMK2B 86.0 1000
CAMK2D CAMK2D 100.0 1000
CAMK2G CAMK2G 100.0 1000
CAMK4 CAMK4 100.0 1000
CAMKK1 CAMKK1 90.0 1000
CAMKK2 CAMKK2 69.0 1000
CASK CASK 85.0 1000
CDK11B CDC2L1 91.0 1000
CDK11A CDC2L2 94.0 1000
CDK13 CDC2L5 82.0 1000
CDK19 CDK11 84.0 1000
CDK2 CDK2 89.0 1000
CDK3 CDK3 90.0 1000
CDK4 CDK4-cyclinD3 63.0 1000
CDK5 CDK5 79.0 1000
CDK7 CDK7 3.5 1000
CDK8 CDK8 97.0 1000
CDK9 CDK9 84.0 1000
CDKL1 CDKL1 61.0 1000
CDKL2 CDKL2 84.0 1000
CDKL3 CDKL3 78.0 1000
CDKL5 CDKL5 87.0 1000
CHEK1 CHEK1 57.0 1000
CHEK2 CHEK2 0.0 1000
CIT CIT 99.0 1000
CLK1 CLK1 4.4 1000
CLK2 CLK2 0.0 1000
CLK3 CLK3 12.0 1000
CLK4 CLK4 1.4 1000
CSF1R CSF1R-autoinhibited 100.0 1000
CSK CSK 74.0 1000
CSNK1A1 CSNK1A1 81.0 1000
CSNK1A1L CSNK1A1L 81.0 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 26.0 1000
CSNK2A2 CSNK2A2 6.7 1000
MATK CTK 65.0 1000
DAPK1 DAPK1 15.0 1000
DAPK2 DAPK2 58.0 1000
DAPK3 DAPK3 33.0 1000
DCLK1 DCAMKL1 57.0 1000
DCLK2 DCAMKL2 90.0 1000
DCLK3 DCAMKL3 43.0 1000
DDR1 DDR1 80.0 1000
DDR2 DDR2 94.0 1000
MAP3K12 DLK 48.0 1000
DMPK DMPK 23.0 1000
CDC42BPG DMPK2 93.0 1000
STK17A DRAK1 11.0 1000
STK17B DRAK2 48.0 1000
DYRK1A DYRK1A 19.0 1000
DYRK1B DYRK1B 31.0 1000
DYRK2 DYRK2 37.0 1000
EGFR EGFR(T790M) 100.0 1000
EIF2AK1 EIF2AK1 87.0 1000
EPHA1 EPHA1 86.0 1000
EPHA2 EPHA2 80.0 1000
EPHA3 EPHA3 72.0 1000
EPHA4 EPHA4 90.0 1000
EPHA5 EPHA5 82.0 1000
EPHA6 EPHA6 85.0 1000
EPHA7 EPHA7 87.0 1000
EPHA8 EPHA8 100.0 1000
EPHB1 EPHB1 99.0 1000
EPHB2 EPHB2 81.0 1000
EPHB3 EPHB3 95.0 1000
EPHB4 EPHB4 96.0 1000
EPHB6 EPHB6 54.0 1000
ERBB2 ERBB2 100.0 1000
ERBB3 ERBB3 78.0 1000
ERBB4 ERBB4 46.0 1000
MAPK3 ERK1 96.0 1000
MAPK1 ERK2 70.0 1000
MAPK6 ERK3 66.0 1000
MAPK4 ERK4 57.0 1000
MAPK7 ERK5 78.0 1000
MAPK15 ERK8 4.8 1000
ERN1 ERN1 49.0 1000
PTK2 FAK 4.9 1000
FER FER 78.0 1000
FES FES 74.0 1000
FGFR1 FGFR1 82.0 1000
FGFR2 FGFR2 59.0 1000
FGFR3 FGFR3(G697C) 89.0 1000
FGFR4 FGFR4 83.0 1000
FGR FGR 58.0 1000
FLT1 FLT1 69.0 1000
FLT3 FLT3-autoinhibited 64.0 1000
FLT4 FLT4 92.0 1000
FRK FRK 93.0 1000
FYN FYN 59.0 1000
GAK GAK 66.0 1000
EIF2AK4 GCN2(Kin.Dom.2,S808G) 6.7 1000
GRK1 GRK1 74.0 1000
GRK2 GRK2 31.0 1000
GRK3 GRK3 91.0 1000
GRK4 GRK4 10.0 1000
GRK7 GRK7 29.0 1000
GSK3A GSK3A 64.0 1000
GSK3B GSK3B 57.0 1000
HASPIN HASPIN 76.0 1000
HCK HCK 100.0 1000
HIPK1 HIPK1 45.0 1000
HIPK2 HIPK2 54.0 1000
HIPK3 HIPK3 48.0 1000
HIPK4 HIPK4 35.0 1000
MAP4K1 HPK1 33.0 1000
HUNK HUNK 100.0 1000
CILK1 ICK 100.0 1000
IGF1R IGF1R 100.0 1000
CHUK IKK-alpha 57.0 1000
IKBKB IKK-beta 78.0 1000
IKBKE IKK-epsilon 18.0 1000
INSR INSR 100.0 1000
INSRR INSRR 100.0 1000
IRAK1 IRAK1 13.0 1000
IRAK3 IRAK3 11.0 1000
IRAK4 IRAK4 50.0 1000
ITK ITK 93.0 1000
JAK1 JAK1(JH2domain-pseudokinase) 20.0 1000
JAK2 JAK2(JH1domain-catalytic) 3.8 1000
JAK3 JAK3(JH1domain-catalytic) 1.9 1000
MAPK8 JNK1 65.0 1000
MAPK9 JNK2 79.0 1000
MAPK10 JNK3 56.0 1000
KIT KIT-autoinhibited 52.0 1000
LATS1 LATS1 51.0 1000
LATS2 LATS2 42.0 1000
LCK LCK 46.0 1000
LIMK1 LIMK1 97.0 1000
LIMK2 LIMK2 94.0 1000
STK11 LKB1 72.0 1000
STK10 LOK 100.0 1000
LRRK2 LRRK2(G2019S) 7.3 1000
LTK LTK 100.0 1000
LYN LYN 80.0 1000
MAP3K13 LZK 0.0 1000
MAK MAK 100.0 1000
MAP3K1 MAP3K1 49.0 1000
MAP3K15 MAP3K15 92.0 1000
MAP3K2 MAP3K2 9.7 1000
MAP3K3 MAP3K3 44.0 1000
MAP3K4 MAP3K4 91.0 1000
MAP4K2 MAP4K2 39.0 1000
MAP4K3 MAP4K3 87.0 1000
MAP4K4 MAP4K4 82.0 1000
MAP4K5 MAP4K5 72.0 1000
MAPKAPK2 MAPKAPK2 100.0 1000
MAPKAPK5 MAPKAPK5 94.0 1000
MARK1 MARK1 77.0 1000
MARK2 MARK2 47.0 1000
MARK3 MARK3 52.0 1000
MARK4 MARK4 63.0 1000
MAST1 MAST1 69.0 1000
MAP2K1 MEK1 85.0 1000
MAP2K2 MEK2 82.0 1000
MAP2K3 MEK3 58.0 1000
MAP2K4 MEK4 23.0 1000
MAP2K5 MEK5 48.0 1000
MAP2K6 MEK6 83.0 1000
MELK MELK 40.0 1000
MERTK MERTK 21.0 1000
MET MET(Y1235D) 10.0 1000
MINK1 MINK 53.0 1000
MAP2K7 MKK7 73.0 1000
MKNK1 MKNK1 45.0 1000
MKNK2 MKNK2 91.0 1000
MYLK3 MLCK 100.0 1000
MAP3K9 MLK1 41.0 1000
MAP3K10 MLK2 49.0 1000
MAP3K11 MLK3 32.0 1000
CDC42BPA MRCKA 80.0 1000
CDC42BPB MRCKB 100.0 1000
STK4 MST1 100.0 1000
MST1R MST1R 72.0 1000
STK3 MST2 46.0 1000
STK24 MST3 93.0 1000
STK26 MST4 46.0 1000
MTOR MTOR 94.0 1000
MUSK MUSK 92.0 1000
MYLK MYLK 71.0 1000
MYLK2 MYLK2 53.0 1000
MYLK4 MYLK4 35.0 1000
MYO3A MYO3A 100.0 1000
MYO3B MYO3B 68.0 1000
STK38 NDR1 65.0 1000
STK38L NDR2 75.0 1000
NEK1 NEK1 51.0 1000
NEK10 NEK10 90.0 1000
NEK11 NEK11 100.0 1000
NEK2 NEK2 83.0 1000
NEK3 NEK3 60.0 1000
NEK4 NEK4 84.0 1000
NEK5 NEK5 63.0 1000
NEK6 NEK6 84.0 1000
NEK7 NEK7 68.0 1000
NEK9 NEK9 63.0 1000
MAP3K14 NIK 65.0 1000
NIM1K NIM1 9.5 1000
NLK NLK 98.0 1000
OXSR1 OSR1 86.0 1000
MAPK14 p38-alpha 92.0 1000
MAPK11 p38-beta 85.0 1000
MAPK13 p38-delta 100.0 1000
MAPK12 p38-gamma 58.0 1000
PAK1 PAK1 73.0 1000
PAK2 PAK2 83.0 1000
PAK3 PAK3 88.0 1000
PAK4 PAK4 52.0 1000
PAK6 PAK6 71.0 1000
PAK5 PAK7 76.0 1000
CDK16 PCTK1 82.0 1000
CDK17 PCTK2 85.0 1000
CDK18 PCTK3 100.0 1000
PDGFRA PDGFRA 58.0 1000
PDGFRB PDGFRB 69.0 1000
PDPK1 PDPK1 54.0 1000
CDPK1 PFCDPK1(P.falciparum) 84.0 1000
PK5 PFPK5(P.falciparum) 75.0 1000
CDK15 PFTAIRE2 63.0 1000
CDK14 PFTK1 86.0 1000
PHKG1 PHKG1 76.0 1000
PHKG2 PHKG2 63.0 1000
PIK3C2B PIK3C2B 79.0 1000
PIK3C2G PIK3C2G 77.0 1000
PIK3CA PIK3CA(Q546K) 93.0 1000
PIK3CB PIK3CB 100.0 1000
PIK3CD PIK3CD 77.0 1000
PIK3CG PIK3CG 100.0 1000
PI4KB PIK4CB 76.0 1000
PIKFYVE PIKFYVE 100.0 1000
PIM1 PIM1 79.0 1000
PIM2 PIM2 100.0 1000
PIM3 PIM3 77.0 1000
PIP5K1A PIP5K1A 12.0 1000
PIP5K1C PIP5K1C 91.0 1000
PIP4K2B PIP5K2B 4.8 1000
PIP4K2C PIP5K2C 42.0 1000
PRKACA PKAC-alpha 81.0 1000
PRKACB PKAC-beta 88.0 1000
PKMYT1 PKMYT1 100.0 1000
PKN1 PKN1 43.0 1000
PKN2 PKN2 22.0 1000
PKNB PKNB(M.tuberculosis) 80.0 1000
PLK1 PLK1 7.6 1000
PLK2 PLK2 0.5 1000
PLK3 PLK3 1.7 1000
PLK4 PLK4 50.0 1000
PRKCD PRKCD 78.0 1000
PRKCE PRKCE 50.0 1000
PRKCH PRKCH 100.0 1000
PRKCI PRKCI 55.0 1000
PRKCQ PRKCQ 55.0 1000
PRKD1 PRKD1 100.0 1000
PRKD2 PRKD2 92.0 1000
PRKD3 PRKD3 100.0 1000
PRKG1 PRKG1 100.0 1000
PRKG2 PRKG2 68.0 1000
EIF2AK2 PRKR 82.0 1000
PRKX PRKX 15.0 1000
PRPF4B PRP4 23.0 1000
PTK2B PYK2 59.0 1000
SIK3 QSK 82.0 1000
RAF1 RAF1 85.0 1000
RET RET(V804M) 31.0 1000
RIOK1 RIOK1 9.7 1000
RIOK2 RIOK2 81.0 1000
RIOK3 RIOK3 8.5 1000
RIPK1 RIPK1 100.0 1000
RIPK2 RIPK2 82.0 1000
RIPK4 RIPK4 6.0 1000
DSTYK RIPK5 53.0 1000
ROCK1 ROCK1 49.0 1000
ROCK2 ROCK2 69.0 1000
ROS1 ROS1 43.0 1000
RPS6KA4 RPS6KA4(Kin.Dom.2-C-terminal) 72.0 1000
RPS6KA5 RPS6KA5(Kin.Dom.2-C-terminal) 78.0 1000
RPS6KA1 RSK1(Kin.Dom.2-C-terminal) 68.0 1000
RPS6KA3 RSK2(Kin.Dom.2-C-terminal) 85.0 1000
RPS6KA2 RSK3(Kin.Dom.2-C-terminal) 95.0 1000
RPS6KA6 RSK4(Kin.Dom.2-C-terminal) 79.0 1000
RPS6KB1 S6K1 50.0 1000
SBK1 SBK1 34.0 1000
SGK1 SGK 66.0 1000
SBK3 SgK110 100.0 1000
SGK2 SGK2 75.0 1000
SGK3 SGK3 87.0 1000
SIK1 SIK 76.0 1000
SIK2 SIK2 41.0 1000
SLK SLK 41.0 1000
NUAK2 SNARK 7.6 1000
SNRK SNRK 85.0 1000
SRC SRC 60.0 1000
SRMS SRMS 62.0 1000
SRPK1 SRPK1 17.0 1000
SRPK2 SRPK2 40.0 1000
SRPK3 SRPK3 11.0 1000
STK16 STK16 1.5 1000
STK33 STK33 15.0 1000
STK35 STK35 86.0 1000
STK36 STK36 87.0 1000
STK39 STK39 100.0 1000
SYK SYK 5.7 1000
MAP3K7 TAK1 48.0 1000
TAOK1 TAOK1 3.7 1000
TAOK2 TAOK2 58.0 1000
TAOK3 TAOK3 12.0 1000
TBK1 TBK1 21.0 1000
TEC TEC 100.0 1000
TESK1 TESK1 97.0 1000
TGFBR1 TGFBR1 44.0 1000
TGFBR2 TGFBR2 100.0 1000
TIE1 TIE1 17.0 1000
TEK TIE2 50.0 1000
TLK1 TLK1 79.0 1000
TLK2 TLK2 100.0 1000
TNIK TNIK 77.0 1000
TNK1 TNK1 65.0 1000
TNK2 TNK2 86.0 1000
TNNI3K TNNI3K 73.0 1000
NTRK1 TRKA 10.0 1000
NTRK2 TRKB 21.0 1000
NTRK3 TRKC 45.0 1000
TRPM6 TRPM6 86.0 1000
TSSK1B TSSK1B 56.0 1000
TSSK3 TSSK3 80.0 1000
TTK TTK 13.0 1000
TXK TXK 91.0 1000
TYK2 TYK2(JH2domain-pseudokinase) 59.0 1000
TYRO3 TYRO3 99.0 1000
ULK1 ULK1 1.2 1000
ULK2 ULK2 5.4 1000
ULK3 ULK3 25.0 1000
KDR VEGFR2 56.0 1000
PIK3C3 VPS34 84.0 1000
VRK2 VRK2 78.0 1000
WEE1 WEE1 13.0 1000
WEE2 WEE2 28.0 1000
WNK1 WNK1 87.0 1000
WNK2 WNK2 22.0 1000
WNK3 WNK3 79.0 1000
WNK4 WNK4 0.0 1000
STK32A YANK1 72.0 1000
STK32B YANK2 100.0 1000
STK32C YANK3 76.0 1000
YES1 YES 77.0 1000
STK25 YSK1 82.0 1000
MAP3K19 YSK4 0.4 1000
MAP3K20 ZAK 100.0 1000
ZAP70 ZAP70 61.0 1000

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PF-04554878

Kinase selectivity profiling against an Invitrogen panel has been performed at 1 µM probe concentration with IC50 follow up for specific targets. These assays are run at Km ATP for each kinase.

Conclusion: Closest hits are TRK-A with IC50 = 56 nM and MAP3K9 with IC50 = 75.3 nM.

Target protein HGNC name Species % inhibition at 1 µM IC50 [nM]
ABL ABL1 34.0 1640.00
AKT1 AKT1 4.0
Aurora-A AURKA 87.0 135.00
BTK BTK 14.0
CAMK1 CAMK1 0.0
CDK2/cyclinA CDK2 72.0 344.00
CDK6/cyclinD3 CDK6 13.0
CHK1 CHEK1 23.0
CHK2 CHEK2 28.0
CK2 CSNK2A1 43.0
CKLdelta 27.0
CLK1 CLK1 99.0 250.00
ECK EPHA2 18.0
EGFR EGFR 13.0
FGFR1 FGFR1 64.0
GSK3beta GSK3B 83.0 416.00
IKKβ IKBKB 4.0
IKKi IKBKE 8.0
INSR INSR 50.0
JAK3 JAK3 94.0 > 1000.00
LCK LCK 39.0
MAP3K9 MAP3K9 98.0 75.30
MAP4K4 MAP4K4 28.0
MAPK1/ERK2 MAPK1 35.0
MAPKAPK2 MAPKAPK2 2.0
MARK1 MARK1 81.0 448.00
MASK 46.0
MET MET 54.0
MST2 STK3 60.0
MYLK2 MYLK2 8.0
NEK 12.0
PAK4 PAK4 69.0
PDK1 PDK1 25.0
PIM2 PIM2 0.0
PKACa PRKACA 29.0
PKCbeta II PRKCB 15.0
PKCzeta PRKCZ 10.0
ROCK1 ROCK1 20.0
S6K T389D D3E RPS6KB1 18.0
SAPK2A/p38 MAPK14 1.0
SGK SGK1 30.0
SRC SRC 58.0 > 1000.00
TAOK3 TAOK3 66.0
TRK-A NTRK1 97.0 56.00
VEGFR2/Flk1 KDR 68.0