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 |
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 |