Selectivity data for probe SM311 and control SM311-NC


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SM311

Compound SM311 was tested at 1 µM against 192 kinases in HEK293T cells.

Conclusion: Six targets > 50 %: LIMK1 (91 %), CDKL2 (85 %), NLK and TXK (73 %), AAK1 (66 %),MAPK9 (JNK2) (65 %).

Target protein HGNC name Species % occupancy at 1 µM
AAK1 AAK1 Homo sapiens 66.0
ABL2 ABL2 Homo sapiens 19.3
AKT2 AKT2 Homo sapiens 12.0
AURKA AURKA Homo sapiens 16.2
AURKB AURKB Homo sapiens 18.0
AURKC AURKC Homo sapiens 11.9
AXL AXL Homo sapiens 7.3
BMP2K BMP2K Homo sapiens 59.6
BMX BMX Homo sapiens 49.8
BRAF(V600E) BRAF Homo sapiens 7.6
BRSK1 BRSK1 Homo sapiens 16.6
BRSK2 BRSK2 Homo sapiens 16.7
BTK BTK Homo sapiens 3.2
CAMK1 CAMK1 Homo sapiens 11.5
CAMK2A CAMK2A Homo sapiens 13.0
CAMK2D CAMK2D Homo sapiens 22.2
CDK1 CDK1 Homo sapiens 36.5
CDK10 CDK10 Homo sapiens 4.1
CDK14 CDK14 Homo sapiens 9.2
CDK15 CDK15 Homo sapiens 9.5
CDK16 CDK16 Homo sapiens 36.4
CDK17 CDK17 Homo sapiens 34.7
CDK18 CDK18 Homo sapiens 14.8
CDK2 CDK2 Homo sapiens 43.3
CDK20 CDK20 Homo sapiens 24.0
CDK3 CDK3 Homo sapiens 47.3
CDK4 CDK4 Homo sapiens 17.4
CDK5 CDK5 Homo sapiens 23.4
CDK6 CDK6 Homo sapiens 15.3
CDK7 CDK7 Homo sapiens 12.4
CDK9 CDK9 Homo sapiens 27.1
CDKL1 CDKL1 Homo sapiens 28.4
CDKL2 CDKL2 Homo sapiens 84.9
CDKL3 CDKL3 Homo sapiens 46.3
CDKL5 CDKL5 Homo sapiens 46.7
CHEK2 CHEK2 Homo sapiens -194.1
CLK1 CLK1 Homo sapiens 15.5
CLK2 CLK2 Homo sapiens 14.8
CLK4 CLK4 Homo sapiens 39.4
CSNK1A1L CSNK1A1L Homo sapiens 4.0
CSNK1D CSNK1D Homo sapiens 16.3
CSNK1G2 CSNK1G2 Homo sapiens 4.5
CSNK2A1 CSNK2A1 Homo sapiens -4.4
CSNK2A2 CSNK2A2 Homo sapiens -1.4
DAPK2 DAPK2 Homo sapiens 28.5
DCLK3 DCLK3 Homo sapiens 25.3
DYRK1A DYRK1A Homo sapiens 2.3
DYRK1B DYRK1B Homo sapiens 5.1
EPHA1 EPHA1 Homo sapiens 19.9
EPHA4 EPHA4 Homo sapiens 41.9
EPHA6 EPHA6 Homo sapiens 13.8
EPHA7 EPHA7 Homo sapiens 22.2
EPHB1 EPHB1 Homo sapiens 36.4
EPHB4 EPHB4 Homo sapiens 31.8
ERN1 ERN1 Homo sapiens 9.9
ERN2 ERN2 Homo sapiens 13.1
FER FER Homo sapiens 1.3
FES FES Homo sapiens 28.7
FGFR1 FGFR1 Homo sapiens 34.0
FGFR2 FGFR2 Homo sapiens 41.4
FGFR3 FGFR3 Homo sapiens 9.1
FGFR4 FGFR4 Homo sapiens 14.6
FLT3 FLT3 Homo sapiens 14.5
FYN FYN Homo sapiens 29.6
GAK GAK Homo sapiens 27.0
HIPK2 HIPK2 Homo sapiens -5.8
HIPK3 HIPK3 Homo sapiens 11.1
HIPK4 HIPK4 Homo sapiens 25.6
ICK CILK1 Homo sapiens 17.1
IGF1R IGF1R Homo sapiens 0.2
IKBKE IKBKE Homo sapiens 18.1
INSR INSR Homo sapiens -5.6
IRAK3 IRAK3 Homo sapiens -0.2
IRAK4 IRAK4 Homo sapiens 9.0
ITK ITK Homo sapiens 19.4
JAK2 (V617F) JAK2 Homo sapiens 30.8
JAK3 JAK3 Homo sapiens 10.2
JNK3 MAPK10 Homo sapiens 26.4
LATS1 LATS1 Homo sapiens -4.1
LATS2 LATS2 Homo sapiens -17.0
LCK LCK Homo sapiens 26.5
LIMK1 LIMK1 Homo sapiens 91.4
LIMK2 LIMK2 Homo sapiens 46.9
LRRK2 LRRK2 Homo sapiens 21.4
LTK LTK Homo sapiens -2.3
MAP3K10 MAP3K10 Homo sapiens -3.7
MAP3K11 MAP3K11 Homo sapiens -3.5
MAP3K12 MAP3K12 Homo sapiens 10.2
MAP3K19 MAP3K19 Homo sapiens 71.1
MAP3K2 MAP3K2 Homo sapiens 25.2
MAP3K21 MAP3K21 Homo sapiens 18.6
MAP3K3 MAP3K3 Homo sapiens 14.0
MAP3K4 MAP3K4 Homo sapiens 15.0
MAP3K9 MAP3K9 Homo sapiens 11.2
MAP4K1 MAP4K1 Homo sapiens 1.6
MAP4K2 MAP4K2 Homo sapiens -13.0
MAP4K3 MAP4K3 Homo sapiens -6.7
MAP4K5 MAP4K5 Homo sapiens 40.5
MAPK11 MAPK11 Homo sapiens 0.1
MAPK14 MAPK14 Homo sapiens 19.8
MAPK4 MAPK4 Homo sapiens 3.8
MAPK6 MAPK6 Homo sapiens -6.3
MAPK8 MAPK8 Homo sapiens 43.2
MAPK9 MAPK9 Homo sapiens 64.9
MARK2 MARK2 Homo sapiens 19.4
MARK4 MARK4 Homo sapiens 15.4
MAST3 MAST3 Homo sapiens 27.0
MAST4 MAST4 Homo sapiens 4.9
MELK MELK Homo sapiens -2.5
MERTK MERTK Homo sapiens -6.3
MET MET Homo sapiens -5.0
MKNK2 MKNK2 Homo sapiens 24.2
MLTK MAP3K20 Homo sapiens 13.3
MUSK MUSK Homo sapiens 13.9
MYLK2 MYLK2 Homo sapiens 0.6
MYLK3 MYLK3 Homo sapiens -2.5
MYLK4 MYLK4 Homo sapiens 16.1
NEK1 NEK1 Homo sapiens 1.0
NEK11 NEK11 Homo sapiens 14.7
NEK2 NEK2 Homo sapiens 5.8
NEK3 NEK3 Homo sapiens 10.3
NEK4 NEK4 Homo sapiens -8.7
NEK5 NEK5 Homo sapiens 29.5
NEK9 NEK9 Homo sapiens 28.9
NIM1K NIM1K Homo sapiens 12.5
NLK NLK Homo sapiens 73.1
NTRK1 NTRK1 Homo sapiens 23.9
NTRK2 NTRK2 Homo sapiens 31.5
NUAK1 NUAK1 Homo sapiens 10.6
PAK4 PAK4 Homo sapiens 12.1
PAK6 PAK6 Homo sapiens 26.2
PHKG1 PHKG1 Homo sapiens 15.9
PHKG2 PHKG2 Homo sapiens 29.2
PKMYT1 PKMYT1 Homo sapiens -20.9
PLK2 PLK2 Homo sapiens 6.9
PLK3 PLK3 Homo sapiens 13.0
PLK4 PLK4 Homo sapiens -2.8
PRKAA1 PRKAA1 Homo sapiens 3.4
PRKAA2 PRKAA2 Homo sapiens 0.4
PRKACA PRKACA Homo sapiens 12.4
PRKACB PRKACB Homo sapiens 2.0
PRKCE PRKCE Homo sapiens 5.5
PRKX PRKX Homo sapiens -7.1
PTK2 PTK2 Homo sapiens 11.2
PTK2B PTK2B Homo sapiens 13.1
PTK6 PTK6 Homo sapiens 7.7
RET RET Homo sapiens 7.8
RIOK2 RIOK2 Homo sapiens 16.7
RIPK1 RIPK1 Homo sapiens 10.5
RIPK2 RIPK2 Homo sapiens 26.0
RON MST1R Homo sapiens -3.9
RPS6KA1 RPS6KA1 Homo sapiens -20.4
RPS6KA2 RPS6KA2 Homo sapiens 0.1
RPS6KA3 RPS6KA3 Homo sapiens 1.4
RPS6KA4 RPS6KA4 Homo sapiens -4.7
RPS6KA6 RPS6KA6 Homo sapiens -33.9
SBK3 SBK3 Homo sapiens 15.9
SGK1 SGK1 Homo sapiens 5.9
SIK1 SIK1 Homo sapiens 0.7
SLK SLK Homo sapiens 20.6
SNF1LK2 SIK2 Homo sapiens 7.7
SNRK SNRK Homo sapiens 12.1
SRMS SRMS Homo sapiens 30.1
STK10 STK10 Homo sapiens 28.9
STK11 STK11 Homo sapiens 9.4
STK16 STK16 Homo sapiens 27.3
STK17B STK17B Homo sapiens 19.6
STK3 STK3 Homo sapiens 10.4
STK32B STK32B Homo sapiens 27.4
STK33 STK33 Homo sapiens -8.6
STK35 STK35 Homo sapiens 7.4
STK36 STK36 Homo sapiens 49.9
STK38 STK38 Homo sapiens 4.5
STK38L STK38L Homo sapiens 2.5
STK4 STK4 Homo sapiens 17.4
TBK1 TBK1 Homo sapiens 1.5
TEC TEC Homo sapiens 12.7
TEK TEK Homo sapiens 27.3
TIE1 TIE1 Homo sapiens 15.8
TLK1 TLK1 Homo sapiens 11.4
TLK2 TLK2 Homo sapiens 11.6
TNK1 TNIK Homo sapiens -5.3
TNK2(iso1) TNK2 Homo sapiens 2.5
TNNI3K TNNI3K Homo sapiens -2.8
TXK TXK Homo sapiens 73.4
TYRO3 TYRO3 Homo sapiens -0.5
ULK1 ULK1 Homo sapiens -7.5
ULK2 ULK2 Homo sapiens 10.0
ULK3 ULK3 Homo sapiens 26.1
WEE1 WEE1 Homo sapiens -3.0
WEE2 WEE2 Homo sapiens -3.6
 

SM311

DSF-assay screen against 91 kinases at 20 µM.

Conclusion: Three targets > 3 K: LIMK1 (deltaTm = 8.11 K), MAPK8 (deltaTm =7.36 K) , MAPK10 (deltaTm =8.12 K).

Target protein HGNC name Species delta Tm delta Tm Staurosporine positive control
AAK1 AAK1 Homo sapiens 2.0 13.12
ABL1 ABL1 Homo sapiens 0.1 6.75
AURKB AURKB Homo sapiens 1.1 15.19
BMP2K BMP2K Homo sapiens 0.3 18.42
BMPR2 BMPR2 Homo sapiens 0.5 2.71
BMX BMX Homo sapiens 2.9 7.81
BRAF BRAF Homo sapiens 1.0 0.05
CAMK1D CAMK1D Homo sapiens 1.2 11.43
CAMK2B CAMK2B Homo sapiens -0.1 14.31
CAMK2D CAMK2D Homo sapiens 2.3 19.28
CAMK4 CAMK4 Homo sapiens 0.8 7.87
CAMKK2 CAMKK2 Homo sapiens 0.1 20.76
CASK CASK Homo sapiens -0.4 3.65
CDC42BPA CDC42BPA Homo sapiens 0.2 2.32
CDK2 CDK2 Homo sapiens 1.3 14.22
CDKL1 CDKL1 Homo sapiens 0.5 5.66
CHEK2 CHEK2 Homo sapiens 0.3 18.16
CLK1 CLK1 Homo sapiens 0.7 11.88
CLK3 CLK3 Homo sapiens 0.3 3.74
CSNK1D CSNK1D Homo sapiens -0.1 1.74
CSNK1E CSNK1E Homo sapiens 0.5 3.03
CSNK2A2 CSNK2A2 Homo sapiens 0.3 4.71
DAPK1 DAPK1 Homo sapiens 0.1 9.45
DAPK3 DAPK3 Homo sapiens 0.3 16.56
DCAMKL1 DCLK1 Homo sapiens 0.5 13.08
DMPK1 DMPK Homo sapiens 0.4 10.16
DYRK1 DYRK1A Homo sapiens 0.5 10.29
DYRK2 DYRK2 Homo sapiens 0.7 6.27
EPHA2 EPHA2 Homo sapiens 0.3 7.01
EPHA4 EPHA4 Homo sapiens 0.4 5.98
EPHA5 EPHA5 Homo sapiens 1.4 8.36
EPHA7 EPHA7 Homo sapiens 2.9 13.26
EPHB1 EPHB1 Homo sapiens 0.2 5.45
EPHB3 EPHB3 Homo sapiens 1.1 7.34
FES FES Homo sapiens 0.4 8.31
FGFR1 FGFR1 Homo sapiens 0.6 6.26
FGFR2 FGFR2 Homo sapiens 1.1 8.38
GAK GAK Homo sapiens 1.5 9.41
GPRK5 GRK5 Homo sapiens 0.4 7.72
GSG2 HASPIN Homo sapiens 0.1 8.69
GSK3B GSK3B Homo sapiens 1.1 11.25
HIPK2 HIPK2 Homo sapiens 0.0 3.47
JNK1 MAPK8 Homo sapiens 7.4 6.53
JNK3 MAPK10 Homo sapiens 8.1 6.61
LIMK1 LIMK1 Homo sapiens 8.1
LIMK2 LIMK2 Homo sapiens 1.0
MAP2K1 MAP2K1 Homo sapiens 0.7 6.94
MAP2K4 MAP2K4 Homo sapiens 0.2 11.01
MAP2K6 MAP2K6 Homo sapiens 0.2 11.91
MAP2K7 MAP2K7 Homo sapiens 0.8 6.14
MAP3K5 MAP3K5 Homo sapiens 1.4 17.86
MAPK1 MAPK1 Homo sapiens 0.4 2.14
MAPK13 MAPK13 Homo sapiens -0.1 5.84
MAPK14 MAPK14 Homo sapiens 2.2 3.22
MAPK15 MAPK15 Homo sapiens 0.6 15.77
MAPK9 MAPK9 Homo sapiens 0.9 3.07
MAPKAPK2 MAPKAPK2 Homo sapiens 0.1 3.41
MARK3 MARK3 Homo sapiens -0.1 18.82
MARK4 MARK4 Homo sapiens 1.4 17.74
MELK MELK Homo sapiens 1.0 13.91
MSSK1 SRPK3 Homo sapiens 0.0 3.51
MST3 STK24 Homo sapiens -2.6 2.42
MST4 STK26 Homo sapiens 0.6 6.51
NEK1 NEK1 Homo sapiens 0.0 0.14
NEK2 NEK2 Homo sapiens 0.0 2.38
NEK7 NEK7 Homo sapiens 2.4 1.22
OSR1 OXSR1 Homo sapiens 1.4 7.68
PAK1 PAK1 Homo sapiens 0.7 7.17
PAK4 PAK4 Homo sapiens 1.5 14.88
PCTK1 CDK16 Homo sapiens 0.6 8.88
PIM1 PIM1 Homo sapiens -0.1 21.41
PIM3 PIM3 Homo sapiens 1.2 20.38
PKMYT1 PKMYT1 Homo sapiens 0.1 0.35
PLK4 PLK4 Homo sapiens 0.4 18.91
RPS6KA1 RPS6KA1 Homo sapiens 0.2 3.53
RPS6KA5 RPS6KA5 Homo sapiens 0.3 13.05
SLK SLK Homo sapiens 0.7 16.05
SRC SRC Homo sapiens 0.9 6.42
SRPK1 SRPK1 Homo sapiens -0.2 6.12
STK10 STK10 Homo sapiens 0.9 25.83
STK17A STK17A Homo sapiens -0.1 13.56
STK17B STK17B Homo sapiens 1.8 12.92
STK3 STK3 Homo sapiens 0.1 16.84
STK39 STK39 Homo sapiens 0.5 7.80
STK4 STK4 Homo sapiens -0.7 16.05
STK6 AURKA Homo sapiens 1.6 20.11
TLK1 TLK1 Homo sapiens 0.3 9.95
TTK TTK Homo sapiens 1.8 11.58
ULK1 ULK1 Homo sapiens 0.5 13.23
ULK3 ULK3 Homo sapiens 0.0 17.37
VRK1 VRK1 Homo sapiens 0.2 3.09