Selectivity data for probe GNE-2256 and control GNE-6689
Jump to control PDSP data
GNE-2256
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| 5-HT1A | HTR1A | -2.64 | ||
| 5-HT1E | HTR1E | 1.48 | ||
| 5-HT2A | HTR2A | -7.43 | ||
| 5-HT2B | HTR2B | 84.14 | 509.45 | 6.29 |
| 5-HT2C | HTR2C | 1.26 | ||
| 5-HT3 | HTR3A | -0.18 | ||
| 5-HT5A | HTR5A | -0.55 | ||
| 5-HT6 | HTR6 | 7.46 | ||
| 5-HT7A | HTR7 | -24.46 | ||
| Alpha1A | ADRA1A | -13.39 | ||
| Alpha1B | ADRA1B | -5.24 | ||
| Alpha1D | ADRA1D | 6.71 | ||
| Alpha2A | ADRA2A | 9.09 | ||
| Alpha2B | ADRA2B | -0.98 | ||
| Alpha2C | ADRA2C | -8.65 | ||
| Beta1 | ADRB1 | 1.93 | ||
| Beta2 | ADRB2 | 3.53 | ||
| GABAA/BZP | 18.49 | |||
| D1 | DRD1 | -12.31 | ||
| D2 | DRD2 | 3.24 | ||
| D3 | DRD3 | -1.84 | ||
| D4 | DRD4 | -9.22 | ||
| D5 | DRD5 | -6.56 | ||
| DAT | SLC6A3 | 20.04 | ||
| DOR | OPRD1 | -7.48 | ||
| H1 | HRH1 | 17.69 | ||
| H3 | HRH3 | -5.14 | ||
| H4 | HRH4 | 19.48 | ||
| KOR | OPRK1 | -0.13 | ||
| M1 | CHRM1 | -9.03 | ||
| M2 | CHRM2 | -9.33 | ||
| M3 | CHRM3 | -14.74 | ||
| M4 | CHRM4 | -23.88 | ||
| M5 | CHRM5 | -6.70 | ||
| MOR | OPRM1 | 6.20 | ||
| NET | SLC6A2 | 2.12 | ||
| GABA/PBR | -2.15 | |||
| SERT | SLC6A4 | -15.05 | ||
| Sigma 1 | SIGMAR1 | 9.11 | ||
| Sigma 2 | TMEM97 | -0.93 | ||
| 5-HT1B | HTR1B | 32.98 | ||
| 5-HT1D | HTR1D | 33.19 | ||
| Beta3 | ADRB3 | 11.18 | ||
| H2 | HRH2 | -2.71 |
GNE-2256
Data show inhibition of single replicates measured using an ATP concentration at Kmapp. Displayed are supplementary data from PMID: 26110718 (Table S3 and S4).
Conclusion: Closest off-targets (IC50 [nM]) are FLT3 (177), JAK1 (282), JAK2 (486), LRRK2 (198), MAP4K4 (680), MINK1 (879), MAP3K7- TAB1 (TAK1-TAB1) (966), NTRK1 (313), NTRK2 (259)
| Target protein | HGNC name | Species | % Inhibition at 1 µM | IC50 [nM] |
|---|---|---|---|---|
| ACVR1B | ACVR1B | Homo sapiens | -1.0 | |
| ACVR2B | ACVR2B | Homo sapiens | 12.5 | |
| AKT1 | AKT1 | Homo sapiens | 0.5 | |
| AKT2 | AKT2 | Homo sapiens | 7.5 | |
| ALK2 | ACVR1 | Homo sapiens | 8.0 | |
| ARK5 | NUAK1 | Homo sapiens | 23.5 | |
| ASK1 | MAP3K5 | Homo sapiens | 3.5 | |
| Abl | ABL1 | Homo sapiens | 9.8 | |
| Aurora_A | AURKA | Homo sapiens | 20.5 | |
| Aurora_B | AURKB | Homo sapiens | 21.3 | |
| Axl | AXL | Homo sapiens | 17.0 | |
| B-Raf | BRAF | Homo sapiens | -0.5 | |
| BMPR1A | BMPR1A | Homo sapiens | 7.0 | |
| BTK | BTK | Homo sapiens | 42.0 | |
| Blk | BLK | Homo sapiens | 37.5 | |
| Bmx | BMX | Homo sapiens | 33.3 | |
| BrSK1 | BRSK1 | Homo sapiens | 3.0 | |
| Brk | PTK6 | Homo sapiens | 10.5 | |
| CAMKK1 | CAMKK1 | Homo sapiens | 3.5 | |
| CAMKK2 | CAMKK2 | Homo sapiens | 8.5 | |
| CDK1/cyclinB | CDK1 | Homo sapiens | 2.5 | |
| CDK2/cyclinA | CDK2 | Homo sapiens | 3.0 | |
| CDK5/p25 | CDK5 | Homo sapiens | 9.0 | |
| CDK7/cyclinH | CDK7 | Homo sapiens | 4.0 | |
| CDK8/cyclinC | CDK8 | Homo sapiens | 13.5 | |
| CDK9/cyclinT1 | CDK9 | Homo sapiens | 2.5 | |
| CHK1 | CHEK1 | Homo sapiens | 3.0 | |
| CHK2 | CHEK2 | Homo sapiens | 13.0 | |
| CK1_alpha1 | CSNK1A1 | Homo sapiens | -0.5 | |
| CK1_delta | CSNK1D | Homo sapiens | 1.5 | |
| CK1_epsilon1 | CSNK1E | Homo sapiens | 5.5 | |
| CK1_gamma1 | CSNK1G1 | Homo sapiens | -3.5 | |
| CK1_gamma2 | CSNK1G2 | Homo sapiens | 5.0 | |
| CK2_alpha1 | CSNK2A1 | Homo sapiens | 3.5 | |
| CLK1 | CLK1 | Homo sapiens | 7.5 | |
| CLK2 | CLK2 | Homo sapiens | 20.3 | |
| CLK3 | CLK3 | Homo sapiens | 10.0 | |
| CLK4 | CLK4 | Homo sapiens | 47.8 | |
| CSF1R | CSF1R | Homo sapiens | 25.3 | |
| CSK | CSK | Homo sapiens | 22.0 | |
| CaMKI | CAMK1 | Homo sapiens | -5.5 | |
| CaMKII_beta | CAMK2B | Homo sapiens | -5.5 | |
| CaMKI_delta | CAMK1D | Homo sapiens | 2.0 | |
| CamKII_alpha | CAMK2A | Homo sapiens | 2.5 | |
| CamKIV | CAMK4 | Homo sapiens | -6.0 | |
| Cot | MAP3K8 | Homo sapiens | 3.0 | |
| DAPK1 | DAPK1 | Homo sapiens | 5.5 | |
| DCAMKL2 | DCLK2 | Homo sapiens | 0.5 | |
| DDR1 | DDR1 | Homo sapiens | -2.0 | |
| DMPK | DMPK | Homo sapiens | 2.1 | |
| DNA_PK | PRKDC | Homo sapiens | 9.0 | |
| DRAK1 | STK17A | Homo sapiens | 11.5 | |
| DYRK1A | DYRK1A | Homo sapiens | 2.0 | |
| DYRK3 | DYRK3 | Homo sapiens | 2.0 | |
| DYRK4 | DYRK4 | Homo sapiens | -5.0 | |
| EGFR | EGFR | Homo sapiens | 6.8 | |
| EGFR(T790M,L8 58R) | EGFR | Homo sapiens | 13.0 | |
| ERK2 | MAPK1 | Homo sapiens | 0.5 | |
| EphA1 | EPHA1 | Homo sapiens | 20.8 | |
| EphA3 | EPHA3 | Homo sapiens | 4.5 | |
| EphA7 | EPHA7 | Homo sapiens | 20.0 | |
| EphA8 | EPHA8 | Homo sapiens | 13.0 | |
| EphB1 | EPHB1 | Homo sapiens | 23.0 | |
| EphB3 | EPHB3 | Homo sapiens | 0.0 | |
| ErbB2 | ERBB2 | Homo sapiens | 1.5 | |
| ErbB4 | ERBB4 | Homo sapiens | 5.0 | |
| FAK | PTK2 | Homo sapiens | 19.5 | |
| FGFR1 | FGFR1 | Homo sapiens | 5.5 | |
| FGFR3 | FGFR3 | Homo sapiens | 1.5 | |
| FGFR4 | FGFR4 | Homo sapiens | -2.0 | |
| Fes | FES | Homo sapiens | 19.0 | |
| Fgr | FGR | Homo sapiens | 53.0 | |
| Flt1 | FLT1 | Homo sapiens | -1.0 | |
| Flt3 | FLT3 | Homo sapiens | 90.8 | 177.00 |
| Flt4 | FLT4 | Homo sapiens | 13.0 | |
| Frk | FRK | Homo sapiens | 5.5 | |
| GRK2 | GRK2 | Homo sapiens | -3.0 | |
| GRK3 | GRK3 | Homo sapiens | -1.0 | |
| GRK5 | GRK5 | Homo sapiens | -2.0 | |
| GRK6 | GRK6 | Homo sapiens | 3.5 | |
| GSK3_alpha | GSK3A | Homo sapiens | 15.5 | |
| GSK3_beta | GSK3B | Homo sapiens | 7.8 | |
| HIPK1 | HIPK1 | Homo sapiens | 0.0 | |
| HIPK2 | HIPK2 | Homo sapiens | 4.5 | |
| HIPK4 | HIPK4 | Homo sapiens | 2.5 | |
| HPK1 | MAP4K1 | Homo sapiens | 13.3 | |
| Hyl | MATK | Homo sapiens | -4.0 | |
| IGF1R | IGF1R | Homo sapiens | 11.5 | |
| IKK_alpha | CHUK | Homo sapiens | 8.5 | |
| IKK_beta | IKBKB | Homo sapiens | 1.5 | |
| IKK_epsilon | IKBKE | Homo sapiens | -0.5 | |
| IRAK1 | IRAK1 | Homo sapiens | 64.3 | |
| IRAK4 | IRAK4 | Homo sapiens | 101.3 | |
| IRR | INSRR | Homo sapiens | 18.0 | |
| ITK | ITK | Homo sapiens | 21.0 | |
| InsR | INSR | Homo sapiens | 34.5 | |
| JAK1 | JAK1 | Homo sapiens | 83.5 | 282.00 |
| JAK2 | JAK2 | Homo sapiens | 80.5 | 486.00 |
| JAK3 | JAK3 | Homo sapiens | 28.0 | |
| JNK1_alpha1 | MAPK8 | Homo sapiens | -1.5 | |
| JNK2 | MAPK9 | Homo sapiens | 2.5 | |
| JNK3 | MAPK10 | Homo sapiens | 10.5 | |
| KDR | KDR | Homo sapiens | 17.0 | |
| KHS1 | MAP4K5 | Homo sapiens | 36.5 | |
| Kit | KIT | Homo sapiens | 3.0 | |
| LIMK1 | LIMK1 | Homo sapiens | -4.5 | |
| LRRK2 | LRRK2 | Homo sapiens | 91.4 | 198.00 |
| LTK | LTK | Homo sapiens | 45.0 | |
| Lck | LCK | Homo sapiens | 41.3 | |
| Lyn | LYN | Homo sapiens | 55.3 | |
| MAP4K4 | MAP4K4 | Homo sapiens | 86.3 | 680.00 |
| MAPKAPK2 | MAPKAPK2 | Homo sapiens | 9.5 | |
| MAPKAPK3 | MAPKAPK3 | Homo sapiens | 6.0 | |
| MARK1 | MARK1 | Homo sapiens | -1.0 | |
| MARK3 | MARK3 | Homo sapiens | 8.5 | |
| MEK1 | MAP2K1 | Homo sapiens | 20.5 | |
| MEK3 | MAP2K3 | Homo sapiens | 12.0 | |
| MEKK2 | MAP3K2 | Homo sapiens | 3.5 | |
| MELK | MELK | Homo sapiens | 12.5 | |
| MKK6 | MAP2K6 | Homo sapiens | -5.5 | |
| MKNK1 | MKNK1 | Homo sapiens | -6.0 | |
| MKNK2 | MKNK2 | Homo sapiens | 6.5 | |
| MLK1 | MAP3K9 | Homo sapiens | 14.0 | |
| MLK2 | MAP3K10 | Homo sapiens | 7.5 | |
| MRCK_alpha | CDC42BPA | Homo sapiens | 1.5 | |
| MSK1 | RPS6KA5 | Homo sapiens | -2.0 | |
| MSSK1 | SRPK3 | Homo sapiens | 2.5 | |
| MST1 | STK4 | Homo sapiens | -1.0 | |
| MST2 | STK3 | Homo sapiens | 7.0 | |
| MST3 | STK24 | Homo sapiens | 5.5 | |
| MST4 | STK26 | Homo sapiens | 2.0 | |
| MYLK(smMLCK) | MYLK | Homo sapiens | 12.0 | |
| MYLK3(caMLCK) | MYLK3 | Homo sapiens | 4.5 | |
| Mer | MERTK | Homo sapiens | 28.0 | |
| Met | MET | Homo sapiens | -2.0 | |
| Mink1 | MINK1 | Homo sapiens | 80.5 | 879.00 |
| MuSK | MUSK | Homo sapiens | 13.0 | |
| NEK1 | NEK1 | Homo sapiens | 11.0 | |
| NEK4 | NEK4 | Homo sapiens | 10.0 | |
| NEK6 | NEK6 | Homo sapiens | 7.0 | |
| NEK9 | NEK9 | Homo sapiens | -2.5 | |
| NLK | NLK | Homo sapiens | 7.0 | |
| PAK1 | PAK1 | Homo sapiens | 9.0 | |
| PAK3 | PAK3 | Homo sapiens | 2.0 | |
| PAK4 | PAK4 | Homo sapiens | 5.0 | |
| PAK6 | PAK6 | Homo sapiens | 7.0 | |
| PASK | PASK | Homo sapiens | -6.5 | |
| PDGFR_alpha | PDGFRA | Homo sapiens | 40.5 | |
| PDK1(direct) | PDK1 | Homo sapiens | 4.5 | |
| PI3KA | PIK3CA | Homo sapiens | 21.5 | |
| PI3KG | PIK3CG | Homo sapiens | 46.5 | |
| PIM1 | PIM1 | Homo sapiens | 1.5 | |
| PKA | PRKACA | Homo sapiens | 5.0 | |
| PKC_alpha | PRKCA | Homo sapiens | 11.0 | |
| PKC_beta1 | PRKCB | Homo sapiens | 4.0 | |
| PKC_delta | PRKCD | Homo sapiens | 12.5 | |
| PKC_epsilon | PRKCE | Homo sapiens | 13.0 | |
| PKC_eta | PRKCH | Homo sapiens | 8.0 | |
| PKC_theta | PRKCQ | Homo sapiens | 1.0 | |
| PKC_zeta | PRKCZ | Homo sapiens | 6.0 | |
| PKD1 | PRDK1 | Homo sapiens | 7.5 | |
| PKG1_alpha | PRKG1 | Homo sapiens | 1.0 | |
| PLK1 | PLK1 | Homo sapiens | -2.0 | |
| PLK2 | PLK2 | Homo sapiens | -3.5 | |
| PLK3 | PLK3 | Homo sapiens | -3.0 | |
| PRAK | MAPKAPK5 | Homo sapiens | -3.5 | |
| PRK1 | PKN1 | Homo sapiens | 0.5 | |
| PRKAA1 | PRKAA1 | Homo sapiens | 5.5 | |
| PhK_gamma1 | PHKG1 | Homo sapiens | 18.5 | |
| PhK_gamma2 | PHKG2 | Homo sapiens | -3.0 | |
| PrKX | PRKX | Homo sapiens | -2.5 | |
| RAF1(Y340D,Y3 41D) | RAF1 | Homo sapiens | -1.5 | |
| RIPK2 | RIPK2 | Homo sapiens | 22.5 | |
| ROCK1 | ROCK1 | Homo sapiens | 5.0 | |
| ROCK2 | ROCK2 | Homo sapiens | 6.0 | |
| RSK1 | RPS6KA1 | Homo sapiens | 7.5 | |
| RSK2 | RPS6KA3 | Homo sapiens | 15.0 | |
| RSK3 | RPS6KA2 | Homo sapiens | 9.0 | |
| Ret | RET | Homo sapiens | 31.5 | |
| Ron | MST1R | Homo sapiens | 2.5 | |
| Ros | ROS1 | Homo sapiens | 38.5 | |
| Rse | TYRO3 | Homo sapiens | 18.0 | |
| SGK1 | SGK1 | Homo sapiens | 4.0 | |
| SGK2 | SGK2 | Homo sapiens | 5.5 | |
| SGK3 | SGK3 | Homo sapiens | -0.5 | |
| SIK2 | SIK2 | Homo sapiens | 12.0 | |
| SLK | SLK | Homo sapiens | 4.0 | |
| SPHK1 | SPHK1 | Homo sapiens | -11.0 | |
| SRPK1 | SRPK1 | Homo sapiens | 1.5 | |
| STK16 | STK16 | Homo sapiens | 15.0 | |
| STK33 | STK33 | Homo sapiens | 3.5 | |
| Src | SRC | Homo sapiens | 23.8 | |
| Srm | SRMS | Homo sapiens | 16.0 | |
| Syk | SYK | Homo sapiens | 9.0 | |
| TAK1-TAB1 |
MAP3K7 TAB1 |
Homo sapiens | 74.5 | 966.00 |
| TAO1 | TAOK1 | Homo sapiens | 2.0 | |
| TBK1 | TBK1 | Homo sapiens | 5.5 | |
| TEC | TEC | Homo sapiens | 0.5 | |
| TGFBR1 | TGFBR1 | Homo sapiens | 0.5 | |
| TNK2 | TNK2 | Homo sapiens | 37.5 | |
| TSSK1 | TSSK1B | Homo sapiens | 5.0 | |
| TTK | TTK | Homo sapiens | 13.0 | |
| TXK | TXK | Homo sapiens | 34.0 | |
| TYK2 | TYK2 | Homo sapiens | 53.5 | |
| Tie2 | TEK | Homo sapiens | 6.5 | |
| TrkA | NTRK1 | Homo sapiens | 71.0 | 313.00 |
| TrkB | NTRK2 | Homo sapiens | 86.0 | 259.00 |
| WEE1 | WEE1 | Homo sapiens | 5.5 | |
| WNK2 | WNK2 | Homo sapiens | 2.5 | |
| YSK1 | STK25 | Homo sapiens | 5.0 | |
| Yes | YES1 | Homo sapiens | 41.5 | |
| ZAK | MAP3K20 | Homo sapiens | 5.5 | |
| ZAP-70 | ZAP70 | Homo sapiens | -6.5 | |
| ZIPK | DAPK3 | Homo sapiens | 3.5 | |
| eEF_2K | EEF2K | Homo sapiens | 0.0 | |
| mTOR | MTOR | Homo sapiens | 0.0 | |
| p38_alpha(direct) | MAPK14 | Homo sapiens | 4.0 | |
| p38_beta | MAPK11 | Homo sapiens | 4.0 | |
| p38_delta | MAPK13 | Homo sapiens | 5.5 | |
| p38_gamma | MAPK12 | Homo sapiens | 0.5 | |
| p70S6K | RPS6KB1 | Homo sapiens | 1.0 |