Menu

Selectivity data for probe FHT-2344 and control FHT-5908


Jump to control PDSP data

FHT-2344


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1B HTR1B 17.56
5-HT1D HTR1D 16.66
5-HT3 HTR3A 5.62
5-HT6 HTR6 8.90
5-HT1A HTR1A 29.68
5-HT2A HTR2A 4.18
5-HT5A HTR5A 11.19
5-HT7A HTR7 3.33
Alpha1A ADRA1A 12.27
Alpha1B ADRA1B -5.17
Alpha1D ADRA1D 30.45
Alpha2A ADRA2A 5.84
Alpha2B ADRA2B 6.88
Alpha2C ADRA2C 10.25
Beta1 ADRB1 1.40
D2 DRD2 6.68
D3 DRD3 13.04
D4 DRD4 1.52
DAT SLC6A3 -87.78 > 10000.00 average (n=2) < 5.00
DOR OPRD1 9.17
H1 HRH1 1.95
H2 HRH2 22.59
H3 HRH3 7.45
H4 HRH4 -0.33
KOR OPRK1 10.66
M1 CHRM1 -37.13
M2 CHRM2 6.19
M3 CHRM3 9.46
M4 CHRM4 4.13
M5 CHRM5 0.52
MOR OPRM1 18.79
SERT SLC6A4 27.54
Sigma 1 SIGMAR1 1.62
5-HT1E HTR1E -10.82
5-HT2B HTR2B 48.20
5-HT2C HTR2C 14.18
Beta2 ADRB2 1.42
GABAA/BZP 15.99
D1 DRD1 30.86
D5 DRD5 -11.93
GABAA -25.99
NET SLC6A2 45.53
GABA/PBR 47.54
Sigma 2 TMEM97 5.91
Beta3 ADRB3 -3.49

FHT-5908


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1E HTR1E -0.87
5-HT2B HTR2B 86.81 507.65 average (n=2) 6.31
5-HT2C HTR2C 18.28
Beta2 ADRB2 -5.95
GABAA/BZP 31.54
D1 DRD1 38.89
D5 DRD5 -10.11
GABAA 49.39
NET SLC6A2 69.81 8271.80 5.08
GABA/PBR 64.56 1583.39 average (n=2) 5.81
Sigma 2 TMEM97 2.43
5-HT1A HTR1A 23.04
5-HT2A HTR2A -5.53
5-HT5A HTR5A 13.94
5-HT7A HTR7 23.03
Alpha1A ADRA1A 15.19
Alpha1B ADRA1B 8.00
Alpha1D ADRA1D 41.99
Alpha2A ADRA2A 10.47
Alpha2B ADRA2B 14.58
Alpha2C ADRA2C 11.16
Beta1 ADRB1 3.85
D2 DRD2 6.41
D3 DRD3 28.16
D4 DRD4 6.59
DAT SLC6A3 -151.28 > 10000.00 average (n=2) < 5.00
DOR OPRD1 12.37
H1 HRH1 12.46
H2 HRH2 4.24
H3 HRH3 0.34
H4 HRH4 -11.28
KOR OPRK1 4.84
M1 CHRM1 23.22
M2 CHRM2 16.34
M3 CHRM3 40.13
M4 CHRM4 7.09
M5 CHRM5 4.67
MOR OPRM1 8.54
SERT SLC6A4 17.27
Sigma 1 SIGMAR1 83.25 416.90 average (n=2) 6.39
5-HT3 HTR3A 3.44
5-HT6 HTR6 16.39
5-HT1B HTR1B 27.37
5-HT1D HTR1D 36.03
Beta3 ADRB3 -20.16

Jump to PDSP top

FHT-2344

For the DSF screen 10 µM compound and 2 µM recombinant protein kinase domain was used. Temperature-dependent protein unfolding profiles were measured using the QuantStudio™ 5 realtime PCR machine (Thermo Fisher). Excitation and emission filters were set to 465 nm and 590 nm, respectively. The temperature was raised with a step rate of 3°C per minute. Data points were analysed with the internal software (Thermal Shift SoftwareTM Version 1.4, Thermo Fisher) using the Boltzmann equation to determine the inflection point of the transition curve.

Conclusion: Clean panel

Target protein HGNC name Species delta Tm delta Tm Staurosporine positive control
ABL1 ABL1 Homo sapiens 0.4 8.26
BMX BMX Homo sapiens 0.2 7.18
CAMKK2 CAMKK2 Homo sapiens 0.3 24.44
CASK CASK Homo sapiens 0.5 4.91
CSNK1D CSNK1D Homo sapiens 0.6 1.43
CSNK2A1A CSNK2A1 Homo sapiens -0.1 2.85
BMPR2 BMPR2 Homo sapiens 0.4 2.89
CDK2 CDK2 Homo sapiens 0.6 15.50
BRAF BRAF Homo sapiens 0.0 0.63
AAK1 AAK1 Homo sapiens 0.0 11.62
CAMK2B CAMK2B Homo sapiens 0.6 14.50
CAMK2D CAMK2D Homo sapiens 0.2 16.01
CAMK4 CAMK4 Homo sapiens 0.8 8.78
CDC42 CDC42 Homo sapiens 0.6 2.78
CLK3 CLK3 Homo sapiens -0.4 4.89
DYRK2 DYRK2 Homo sapiens 1.4 6.46
CDKL1 CDKL1 Homo sapiens 0.2 5.00
CHEK2 CHEK2 Homo sapiens -0.7 16.68
CLK1 CLK1 Homo sapiens 0.5 10.94
DAPK1 DAPK1 Homo sapiens -0.1 9.19
CSNK2A2A CSNK2A2 Homo sapiens 0.1 4.26
DAPK3 DAPK3 Homo sapiens -1.5 16.19
FES FES Homo sapiens 0.1 8.70
GSG2 HASPIN Homo sapiens -0.2 7.11
TTK TTK Homo sapiens -1.4 8.80
EPHA2 EPHA2 Homo sapiens 0.2 7.67
MAPK1 MAPK1 Homo sapiens 0.8 1.98
MERTK MERTK Homo sapiens 0.5 6.35
MST3 STK24 Homo sapiens -5.5 6.74
DCAMKL1 DCLK1 Homo sapiens 0.2 13.96
DMPK DMPK Homo sapiens 0.6 9.28
EPHA5 EPHA5 Homo sapiens 0.1 8.98
EPHA7 EPHA7 Homo sapiens 1.0 11.54
EPHB3 EPHB3 Homo sapiens -0.3 7.30
FGFR1 FGFR1 Homo sapiens -0.1 5.65
FGFR2 FGFR2 Homo sapiens 0.3 8.53
FGFR3 FGFR3 Homo sapiens 0.4 11.80
GAK GAK Homo sapiens -0.2 8.71
GPRK5 GRK5 Homo sapiens 0.5 6.82
GSK3B GSK3B Homo sapiens 0.2 12.08
MAP2K1 MAP2K1 Homo sapiens -0.1 5.51
MAP2K4 MAP2K4 Homo sapiens 0.4 10.83
MAP2K6 MAP2K6 Homo sapiens 1.5 12.12
MAP3K5 MAP3K5 Homo sapiens 1.1 18.07
MAPK10 MAPK10 Homo sapiens 0.6 7.41
MAPK13 MAPK13 Homo sapiens 0.2 6.96
MAPK14 MAPK14 Homo sapiens -0.1 1.14
MAPK8 MAPK8 Homo sapiens 0.2 7.87
MAPK9 MAPK9 Homo sapiens 0.2 3.96
MARK3 MARK3 Homo sapiens 1.1 19.07
MARK4 MARK4 Homo sapiens 0.5 15.76
MELK MELK Homo sapiens -0.1 13.96
PIM3 PIM3 Homo sapiens 0.1 17.57
FLT1 FLT1 Homo sapiens 0.0 11.11
NEK1 NEK1 Homo sapiens -0.2 -0.58
NEK2 NEK2 Homo sapiens 0.2 3.70
NEK7 NEK7 Homo sapiens 0.1 1.29
OXSR1 OXSR1 Homo sapiens 0.0 5.06
PAK1 PAK1 Homo sapiens -0.2 7.66
MST4 STK26 Homo sapiens -1.1 6.93
PAK4 PAK4 Homo sapiens 0.0 13.41
PHKG2 PHKG2 Homo sapiens 0.2 22.17
PIM1 PIM1 Homo sapiens -0.4 11.92
RPS6KA1 RPS6KA1 Homo sapiens 0.2 3.76
STK10 STK10 Homo sapiens 0.2 22.74
AKT3 AKT3 Homo sapiens 0.0 7.03
BMP2K BMP2K Homo sapiens 0.2 18.68
CAMK1D CAMK1D Homo sapiens 0.2 10.85
CAMK1G CAMK1G Homo sapiens 0.0 13.27
PCTK1 CDK16 Homo sapiens -1.2 7.03
PKMYT1 PKMYT1 Homo sapiens -0.6 -0.19
PLK4 PLK4 Homo sapiens 0.5 19.92
RPS6KA5 RPS6KA5 Homo sapiens 1.2 13.07
SLK SLK Homo sapiens 1.3 12.23
SRC SRC Homo sapiens -0.2 5.50
SRPK1 SRPK1 Homo sapiens 0.7 7.14
STK3 STK3 Homo sapiens 1.3 15.54
STK4 STK4 Homo sapiens 0.0 14.22
STK6 AURKA Homo sapiens 0.9 16.54
STK17A STK17A Homo sapiens 0.6 12.57
STK17B STK17B Homo sapiens -0.1 10.02
STK38L STK38L Homo sapiens 0.5 10.85
STK39 STK39 Homo sapiens 0.2 8.58
BRD4 BRD4 Homo sapiens -0.8 1.04
BRPF1 BRPF1 Homo sapiens -1.2 -0.05
TAF1 TAF1 Homo sapiens 0.0 0.18
TIF1 TRIM24 Homo sapiens 1.4 2.51
ULK1 ULK1 Homo sapiens 0.5 13.45
ULK3 ULK3 Homo sapiens 0.3 18.20
VRK1 VRK1 Homo sapiens 0.3 3.19
WNK1 WNK1 Homo sapiens 0.2 0.64
CSNK1E CSNK1E Homo sapiens 0.5 3.74
EPHA4 EPHA4 Homo sapiens 1.1 6.89
FECH FECH Homo sapiens 0.1 1.69
HIPK2 HIPK2 Homo sapiens 0.2 6.38
MAP2K7 MAP2K7 Homo sapiens 0.2 6.68
EPHB1 EPHB1 Homo sapiens -0.3 6.19
AURKB AURKB Homo sapiens 1.3 13.63
DYRK1A DYRK1A Homo sapiens -0.8 9.30
MAPK15 MAPK15 Homo sapiens 0.9 14.99
MAPKAPK2 MAPKAPK2 Homo sapiens 0.8 3.41
MSSK1 SRPK3 Homo sapiens 0.4 3.67
NQO2 NQO2 Homo sapiens -0.8 -2.91
TLK1 TLK1 Homo sapiens 1.4 9.52
 

FHT-5908

Conclusion: Clean panel

Target protein HGNC name Species delta Tm delta Tm Staurosporine positive control
ABL1 ABL1 Homo sapiens 0.2 8.26
BMX BMX Homo sapiens 0.3 7.18
CAMKK2 CAMKK2 Homo sapiens 0.6 24.44
CASK CASK Homo sapiens 0.6 4.91
CSNK1D CSNK1D Homo sapiens 0.8 1.43
CSNK2A1A CSNK2A1 Homo sapiens 0.1 2.85
BMPR2 BMPR2 Homo sapiens 0.4 2.89
CDK2 CDK2 Homo sapiens 0.4 15.50
BRAF BRAF Homo sapiens 0.0 0.63
AAK1 AAK1 Homo sapiens 0.0 11.62
CAMK2B CAMK2B Homo sapiens 0.5 14.50
CAMK2D CAMK2D Homo sapiens 0.1 16.01
CAMK4 CAMK4 Homo sapiens 0.4 8.78
CDC42 CDC42 Homo sapiens -0.2 2.78
CLK3 CLK3 Homo sapiens -0.3 4.89
DYRK2 DYRK2 Homo sapiens 1.8 6.46
CDKL1 CDKL1 Homo sapiens 0.2 5.00
CHEK2 CHEK2 Homo sapiens -1.1 16.68
CLK1 CLK1 Homo sapiens 0.5 10.94
DAPK1 DAPK1 Homo sapiens 0.0 9.19
CSNK2A2 CSNK2A2 Homo sapiens -0.2 4.26
DAPK3 DAPK3 Homo sapiens -1.0 16.19
FES FES Homo sapiens 0.0 8.70
GSG2 HASPIN Homo sapiens -1.1 7.11
TTK TTK Homo sapiens -0.4 8.80
EPHA2 EPHA2 Homo sapiens 0.2 7.67
MAPK1 MAPK1 Homo sapiens 0.4 1.98
MERTK MERTK Homo sapiens 0.3 6.35
MST3 STK24 Homo sapiens -2.0 6.74
DCAMKL1 DCLK1 Homo sapiens 0.0 13.96
DMPK DMPK Homo sapiens -0.3 9.28
EPHA5 EPHA5 Homo sapiens 0.3 8.98
EPHA7 EPHA7 Homo sapiens 1.1 11.54
EPHB3 EPHB3 Homo sapiens -0.4 7.30
FGFR1 FGFR1 Homo sapiens -0.2 5.65
FGFR2 FGFR2 Homo sapiens 0.2 8.53
FGFR3 FGFR3 Homo sapiens 1.8 11.80
GAK GAK Homo sapiens 0.0 8.71
GPRK5 GRK5 Homo sapiens 0.2 6.82
GSK3B GSK3B Homo sapiens 0.7 12.08
MAP2K1 MAP2K1 Homo sapiens -0.1 5.51
MAP2K4 MAP2K4 Homo sapiens 0.3 10.83
MAP2K6 MAP2K6 Homo sapiens 1.6 12.12
MAP3K5 MAP3K5 Homo sapiens 1.2 18.07
MAPK10 MAPK10 Homo sapiens 1.8 7.41
MAPK13 MAPK13 Homo sapiens 0.2 6.96
MAPK14 MAPK14 Homo sapiens -0.1 1.14
MAPK8 MAPK8 Homo sapiens 0.5 7.87
MAPK9 MAPK9 Homo sapiens 0.4 3.96
MARK3 MARK3 Homo sapiens 1.7 19.07
MARK4 MARK4 Homo sapiens 0.5 15.76
MELK MELK Homo sapiens 0.1 13.96
PIM3 PIM3 Homo sapiens 0.7 17.57
FLT1 FLT1 Homo sapiens -0.2 11.11
NEK1 NEK1 Homo sapiens -0.5 -0.58
NEK2 NEK2 Homo sapiens -0.1 3.70
NEK7 NEK7 Homo sapiens 0.0 1.29
OXSR1 OXSR1 Homo sapiens 1.3 5.06
PAK1 PAK1 Homo sapiens 0.4 7.66
MST4 STK26 Homo sapiens -1.3 6.93
PAK4 PAK4 Homo sapiens -0.1 13.41
PHKG2 PHKG2 Homo sapiens 0.2 22.17
PIM1 PIM1 Homo sapiens -0.4 11.92
RPS6KA1 RPS6KA1 Homo sapiens 0.2 3.76
STK10 STK10 Homo sapiens 0.6 22.74
AKT3 AKT3 Homo sapiens 0.2 7.03
BMP2K BMP2K Homo sapiens 0.3 18.68
CAMK1D CAMK1D Homo sapiens 0.5 10.85
CAMK1G CAMK1G Homo sapiens 0.4 13.27
PCTK1 CDK16 Homo sapiens -1.4 7.03
PKMYT1 PKMYT1 Homo sapiens -0.2 -0.19
PLK4 PLK4 Homo sapiens 0.7 19.92
RPS6KA5 RPS6KA5 Homo sapiens -0.1 13.07
SLK SLK Homo sapiens 0.2 12.23
SRC SRC Homo sapiens 0.3 5.50
SRPK1 SRPK1 Homo sapiens 0.0 7.14
STK3 STK3 Homo sapiens 0.3 15.54
STK4 STK4 Homo sapiens 0.0 14.22
STK6 AURKA Homo sapiens 0.2 16.54
STK17A STK17A Homo sapiens 1.0 12.57
STK17B STK17B Homo sapiens -12.2 10.02
STK38L STK38L Homo sapiens 0.2 10.85
STK39 STK39 Homo sapiens 0.3 8.58
BRD4 BRD4 Homo sapiens -0.3 1.04
BRPF1 BRPF1 Homo sapiens -1.2 -0.05
TAF1 TAF1 Homo sapiens -0.2 0.18
TIF1 TRIM24 Homo sapiens 1.2 2.51
ULK1 ULK1 Homo sapiens 0.1 13.45
ULK3 ULK3 Homo sapiens 0.2 18.20
VRK1 VRK1 Homo sapiens 0.3 3.19
WNK1 WNK1 Homo sapiens 0.4 0.64
CSNK1E CSNK1E Homo sapiens 0.7 3.74
EPHA4 EPHA4 Homo sapiens 1.2 6.89
FECH FECH Homo sapiens -0.6 1.69
HIPK2 HIPK2 Homo sapiens 0.2 6.38
MAP2K7 MAP2K7 Homo sapiens 1.0 6.68
EPHB1 EPHB1 Homo sapiens 0.2 6.19
AURKB AURKB Homo sapiens 0.8 13.63
DYRK1A DYRK1A Homo sapiens -0.8 9.30
MAPK15 MAPK15 Homo sapiens 1.1 14.99
MAPKAPK2 MAPKAPK2 Homo sapiens -9.5 3.41
MSSK1 SRPK3 Homo sapiens 0.1 3.67
NQO2 NQO2 Homo sapiens -0.6 -2.91
TLK1 TLK1 Homo sapiens 1.6 9.52