Selectivity data for probe PF-04418948 and control PF-04475866
Jump to control PDSP data
PF-04418948
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| M3 | CHRM3 | 19.22 | ||
| Sigma 1 | SIGMAR1 | 21.07 | ||
| DAT | SLC6A3 | -14.46 | ||
| M2 | CHRM2 | 16.71 | ||
| SERT | SLC6A4 | -6.83 | ||
| 5-HT1A | HTR1A | -22.74 | ||
| GABAA/BZP | 18.70 | |||
| D3 | DRD3 | 32.96 | ||
| D4 | DRD4 | 8.76 | ||
| D5 | DRD5 | -2.51 | ||
| GABAA | -1.97 | |||
| H1 | HRH1 | -11.53 | ||
| H2 | HRH2 | 3.00 | ||
| KOR | OPRK1 | 16.41 | ||
| MOR | OPRM1 | 1.07 | ||
| 5-HT1B | HTR1B | -11.25 | ||
| 5-HT1D | HTR1D | -24.02 | ||
| 5-HT1E | HTR1E | 10.97 | ||
| 5-HT6 | HTR6 | -6.47 | ||
| 5-HT7A | HTR7 | -9.26 | ||
| Beta2 | ADRB2 | -17.45 | ||
| D1 | DRD1 | -26.64 | ||
| D2 | DRD2 | -23.45 | ||
| DOR | OPRD1 | 5.07 | ||
| H3 | HRH3 | -15.34 | ||
| M1 | CHRM1 | -0.03 | ||
| M5 | CHRM5 | -7.44 | ||
| Beta1 | ADRB1 | -12.18 | ||
| Beta3 | ADRB3 | -19.86 | ||
| H4 | HRH4 | -17.71 | ||
| 5-HT2A | HTR2A | 6.25 | ||
| 5-HT2B | HTR2B | -0.11 | ||
| 5-HT2C | HTR2C | 12.35 | ||
| 5-HT3 | HTR3A | 0.08 | ||
| 5-HT5A | HTR5A | -8.97 | ||
| Alpha1A | ADRA1A | 2.52 | ||
| Alpha1B | ADRA1B | -11.36 | ||
| Alpha1D | ADRA1D | -3.76 | ||
| Alpha2A | ADRA2A | 21.80 | ||
| Alpha2B | ADRA2B | 9.24 | ||
| Alpha2C | ADRA2C | 9.72 | ||
| M4 | CHRM4 | -18.57 | ||
| NET | SLC6A2 | 11.01 | ||
| Sigma 2 | TMEM97 | -1.29 | ||
| GABA/PBR | -30.46 |
PF-04475866
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| GABA/PBR | 16.30 | |||
| Beta1 | ADRB1 | -6.66 | ||
| Beta3 | ADRB3 | -13.27 | ||
| H4 | HRH4 | -26.19 | > 10000.00 | < 5.00 |
| 5-HT1B | HTR1B | -16.87 | ||
| 5-HT1D | HTR1D | -24.94 | ||
| 5-HT1E | HTR1E | 12.21 | ||
| 5-HT6 | HTR6 | -2.64 | ||
| 5-HT7A | HTR7 | -12.04 | ||
| Beta2 | ADRB2 | -14.97 | ||
| D1 | DRD1 | -52.32 | > 10000.00 | < 5.00 |
| D2 | DRD2 | -29.44 | ||
| DOR | OPRD1 | -5.22 | ||
| H3 | HRH3 | -19.98 | ||
| M1 | CHRM1 | -0.69 | ||
| M5 | CHRM5 | -0.33 | ||
| 5-HT1A | HTR1A | -18.08 | ||
| GABAA/BZP | -5.33 | |||
| D3 | DRD3 | 3.89 | ||
| D4 | DRD4 | -7.87 | ||
| D5 | DRD5 | 2.20 | ||
| GABAA | -8.88 | |||
| H1 | HRH1 | -4.38 | ||
| H2 | HRH2 | 15.69 | ||
| KOR | OPRK1 | -9.45 | ||
| MOR | OPRM1 | -11.90 | ||
| 5-HT2A | HTR2A | -2.23 | ||
| 5-HT2B | HTR2B | -2.50 | ||
| 5-HT2C | HTR2C | 30.19 | ||
| 5-HT3 | HTR3A | 16.59 | ||
| 5-HT5A | HTR5A | -14.33 | ||
| Alpha1A | ADRA1A | -4.09 | ||
| Alpha1B | ADRA1B | -14.57 | ||
| Alpha1D | ADRA1D | 5.00 | ||
| Alpha2A | ADRA2A | 14.22 | ||
| Alpha2B | ADRA2B | 12.13 | ||
| Alpha2C | ADRA2C | 11.28 | ||
| M4 | CHRM4 | -15.97 | ||
| NET | SLC6A2 | 16.75 | ||
| Sigma 2 | TMEM97 | -12.24 | ||
| DAT | SLC6A3 | 6.07 | ||
| M2 | CHRM2 | 26.66 | ||
| SERT | SLC6A4 | -6.29 | ||
| Sigma 1 | SIGMAR1 | 20.31 | ||
| M3 | CHRM3 | 27.93 |
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-04418948
| HGNC target name | DiscoverX gene symbol of kinase | % Control | Compound Concentration [nM] | Kd [nM] | AAK1 | AAK1 | 100.0 | 1000 | ABL1 | ABL1-phosphorylated | 100.0 | 1000 | ABL2 | ABL2 | 100.0 | 1000 | ACVR1 | ACVR1 | 100.0 | 1000 | ACVR1B | ACVR1B | 78.0 | 1000 | ACVR2A | ACVR2A | 100.0 | 1000 | ACVR2B | ACVR2B | 100.0 | 1000 | ACVRL1 | ACVRL1 | 93.0 | 1000 | COQ8A | ADCK3 | 100.0 | 1000 | COQ8B | ADCK4 | 100.0 | 1000 | AKT1 | AKT1 | 100.0 | 1000 | AKT2 | AKT2 | 100.0 | 1000 | AKT3 | AKT3 | 88.0 | 1000 | ALK | ALK(L1196M) | 100.0 | 1000 | PRKAA1 | AMPK-alpha1 | 100.0 | 1000 | PRKAA2 | AMPK-alpha2 | 28.0 | 1000 | ANKK1 | ANKK1 | 86.0 | 1000 | NUAK1 | ARK5 | 94.0 | 1000 | MAP3K5 | ASK1 | 98.0 | 1000 | MAP3K6 | ASK2 | 95.0 | 1000 | AURKA | AURKA | 100.0 | 1000 | AURKB | AURKB | 100.0 | 1000 | AURKC | AURKC | 98.0 | 1000 | AXL | AXL | 100.0 | 1000 | BMP2K | BIKE | 100.0 | 1000 | BLK | BLK | 93.0 | 1000 | BMPR1A | BMPR1A | 88.0 | 1000 | BMPR1B | BMPR1B | 95.0 | 1000 | BMPR2 | BMPR2 | 87.0 | 1000 | BMX | BMX | 87.0 | 1000 | BRAF | BRAF(V600E) | 100.0 | 1000 | PTK6 | BRK | 99.0 | 1000 | BRSK1 | BRSK1 | 85.0 | 1000 | BRSK2 | BRSK2 | 100.0 | 1000 | BTK | BTK | 84.0 | 1000 | BUB1 | BUB1 | 100.0 | 1000 | CAMK1 | CAMK1 | 100.0 | 1000 | PNCK | CAMK1B | 100.0 | 1000 | CAMK1D | CAMK1D | 100.0 | 1000 | CAMK1G | CAMK1G | 100.0 | 1000 | CAMK2A | CAMK2A | 100.0 | 1000 | CAMK2B | CAMK2B | 100.0 | 1000 | CAMK2D | CAMK2D | 100.0 | 1000 | CAMK2G | CAMK2G | 100.0 | 1000 | CAMK4 | CAMK4 | 88.0 | 1000 | CAMKK1 | CAMKK1 | 91.0 | 1000 | CAMKK2 | CAMKK2 | 94.0 | 1000 | CASK | CASK | 91.0 | 1000 | CDK11B | CDC2L1 | 100.0 | 1000 | CDK11A | CDC2L2 | 100.0 | 1000 | CDK13 | CDC2L5 | 100.0 | 1000 | CDK19 | CDK11 | 95.0 | 1000 | CDK2 | CDK2 | 91.0 | 1000 | CDK3 | CDK3 | 83.0 | 1000 | CDK4 | CDK4-cyclinD3 | 100.0 | 1000 | CDK5 | CDK5 | 100.0 | 1000 | CDK7 | CDK7 | 100.0 | 1000 | CDK8 | CDK8 | 94.0 | 1000 | CDK9 | CDK9 | 100.0 | 1000 | CDKL1 | CDKL1 | 100.0 | 1000 | CDKL2 | CDKL2 | 89.0 | 1000 | CDKL3 | CDKL3 | 89.0 | 1000 | CDKL5 | CDKL5 | 97.0 | 1000 | CHEK1 | CHEK1 | 87.0 | 1000 | CHEK2 | CHEK2 | 93.0 | 1000 | CIT | CIT | 100.0 | 1000 | CLK1 | CLK1 | 79.0 | 1000 | CLK2 | CLK2 | 100.0 | 1000 | CLK3 | CLK3 | 99.0 | 1000 | CLK4 | CLK4 | 100.0 | 1000 | CSF1R | CSF1R-autoinhibited | 75.0 | 1000 | CSK | CSK | 100.0 | 1000 | CSNK1A1 | CSNK1A1 | 100.0 | 1000 | CSNK1A1L | CSNK1A1L | 100.0 | 1000 | CSNK1D | CSNK1D | 100.0 | 1000 | CSNK1E | CSNK1E | 94.0 | 1000 | CSNK1G1 | CSNK1G1 | 94.0 | 1000 | CSNK1G2 | CSNK1G2 | 100.0 | 1000 | CSNK1G3 | CSNK1G3 | 100.0 | 1000 | CSNK2A1 | CSNK2A1 | 100.0 | 1000 | CSNK2A2 | CSNK2A2 | 100.0 | 1000 | MATK | CTK | 100.0 | 1000 | DAPK1 | DAPK1 | 100.0 | 1000 | DAPK2 | DAPK2 | 98.0 | 1000 | DAPK3 | DAPK3 | 100.0 | 1000 | DCLK1 | DCAMKL1 | 100.0 | 1000 | DCLK2 | DCAMKL2 | 100.0 | 1000 | DCLK3 | DCAMKL3 | 98.0 | 1000 | DDR1 | DDR1 | 100.0 | 1000 | DDR2 | DDR2 | 100.0 | 1000 | MAP3K12 | DLK | 97.0 | 1000 | DMPK | DMPK | 76.0 | 1000 | CDC42BPG | DMPK2 | 91.0 | 1000 | STK17A | DRAK1 | 81.0 | 1000 | STK17B | DRAK2 | 100.0 | 1000 | DYRK1A | DYRK1A | 100.0 | 1000 | DYRK1B | DYRK1B | 100.0 | 1000 | DYRK2 | DYRK2 | 84.0 | 1000 | EGFR | EGFR(T790M) | 100.0 | 1000 | EIF2AK1 | EIF2AK1 | 94.0 | 1000 | EPHA1 | EPHA1 | 83.0 | 1000 | EPHA2 | EPHA2 | 100.0 | 1000 | EPHA3 | EPHA3 | 92.0 | 1000 | EPHA4 | EPHA4 | 100.0 | 1000 | EPHA5 | EPHA5 | 78.0 | 1000 | EPHA6 | EPHA6 | 100.0 | 1000 | EPHA7 | EPHA7 | 100.0 | 1000 | EPHA8 | EPHA8 | 100.0 | 1000 | EPHB1 | EPHB1 | 100.0 | 1000 | EPHB2 | EPHB2 | 100.0 | 1000 | EPHB3 | EPHB3 | 99.0 | 1000 | EPHB4 | EPHB4 | 95.0 | 1000 | EPHB6 | EPHB6 | 100.0 | 1000 | ERBB2 | ERBB2 | 100.0 | 1000 | ERBB3 | ERBB3 | 89.0 | 1000 | ERBB4 | ERBB4 | 100.0 | 1000 | MAPK3 | ERK1 | 100.0 | 1000 | MAPK1 | ERK2 | 97.0 | 1000 | MAPK6 | ERK3 | 88.0 | 1000 | MAPK4 | ERK4 | 100.0 | 1000 | MAPK7 | ERK5 | 100.0 | 1000 | MAPK15 | ERK8 | 74.0 | 1000 | ERN1 | ERN1 | 80.0 | 1000 | PTK2 | FAK | 100.0 | 1000 | FER | FER | 74.0 | 1000 | FES | FES | 100.0 | 1000 | FGFR1 | FGFR1 | 100.0 | 1000 | FGFR2 | FGFR2 | 100.0 | 1000 | FGFR3 | FGFR3(G697C) | 88.0 | 1000 | FGFR4 | FGFR4 | 100.0 | 1000 | FGR | FGR | 96.0 | 1000 | FLT1 | FLT1 | 100.0 | 1000 | FLT3 | FLT3-autoinhibited | 96.0 | 1000 | FLT4 | FLT4 | 75.0 | 1000 | FRK | FRK | 100.0 | 1000 | FYN | FYN | 100.0 | 1000 | GAK | GAK | 88.0 | 1000 | EIF2AK4 | GCN2(Kin.Dom.2,S808G) | 100.0 | 1000 | GRK1 | GRK1 | 100.0 | 1000 | GRK2 | GRK2 | 72.0 | 1000 | GRK3 | GRK3 | 67.0 | 1000 | GRK4 | GRK4 | 100.0 | 1000 | GRK7 | GRK7 | 93.0 | 1000 | GSK3A | GSK3A | 96.0 | 1000 | GSK3B | GSK3B | 100.0 | 1000 | HASPIN | HASPIN | 100.0 | 1000 | HCK | HCK | 100.0 | 1000 | HIPK1 | HIPK1 | 100.0 | 1000 | HIPK2 | HIPK2 | 78.0 | 1000 | HIPK3 | HIPK3 | 100.0 | 1000 | HIPK4 | HIPK4 | 100.0 | 1000 | MAP4K1 | HPK1 | 95.0 | 1000 | HUNK | HUNK | 100.0 | 1000 | CILK1 | ICK | 78.0 | 1000 | IGF1R | IGF1R | 100.0 | 1000 | CHUK | IKK-alpha | 100.0 | 1000 | IKBKB | IKK-beta | 100.0 | 1000 | IKBKE | IKK-epsilon | 95.0 | 1000 | INSR | INSR | 93.0 | 1000 | INSRR | INSRR | 67.0 | 1000 | IRAK1 | IRAK1 | 100.0 | 1000 | IRAK3 | IRAK3 | 100.0 | 1000 | IRAK4 | IRAK4 | 87.0 | 1000 | ITK | ITK | 100.0 | 1000 | JAK1 | JAK1(JH2domain-pseudokinase) | 96.0 | 1000 | JAK2 | JAK2(JH1domain-catalytic) | 89.0 | 1000 | JAK3 | JAK3(JH1domain-catalytic) | 100.0 | 1000 | MAPK8 | JNK1 | 76.0 | 1000 | MAPK9 | JNK2 | 100.0 | 1000 | MAPK10 | JNK3 | 85.0 | 1000 | KIT | KIT-autoinhibited | 100.0 | 1000 | LATS1 | LATS1 | 87.0 | 1000 | LATS2 | LATS2 | 90.0 | 1000 | LCK | LCK | 80.0 | 1000 | LIMK1 | LIMK1 | 100.0 | 1000 | LIMK2 | LIMK2 | 90.0 | 1000 | STK11 | LKB1 | 100.0 | 1000 | STK10 | LOK | 100.0 | 1000 | LRRK2 | LRRK2(G2019S) | 84.0 | 1000 | LTK | LTK | 100.0 | 1000 | LYN | LYN | 85.0 | 1000 | MAP3K13 | LZK | 100.0 | 1000 | MAK | MAK | 100.0 | 1000 | MAP3K1 | MAP3K1 | 100.0 | 1000 | MAP3K15 | MAP3K15 | 94.0 | 1000 | MAP3K2 | MAP3K2 | 96.0 | 1000 | MAP3K3 | MAP3K3 | 97.0 | 1000 | MAP3K4 | MAP3K4 | 65.0 | 1000 | MAP4K2 | MAP4K2 | 100.0 | 1000 | MAP4K3 | MAP4K3 | 100.0 | 1000 | MAP4K4 | MAP4K4 | 100.0 | 1000 | MAP4K5 | MAP4K5 | 86.0 | 1000 | MAPKAPK2 | MAPKAPK2 | 100.0 | 1000 | MAPKAPK5 | MAPKAPK5 | 76.0 | 1000 | MARK1 | MARK1 | 100.0 | 1000 | MARK2 | MARK2 | 91.0 | 1000 | MARK3 | MARK3 | 94.0 | 1000 | MARK4 | MARK4 | 100.0 | 1000 | MAST1 | MAST1 | 100.0 | 1000 | MAP2K1 | MEK1 | 100.0 | 1000 | MAP2K2 | MEK2 | 100.0 | 1000 | MAP2K3 | MEK3 | 95.0 | 1000 | MAP2K4 | MEK4 | 90.0 | 1000 | MAP2K5 | MEK5 | 93.0 | 1000 | MAP2K6 | MEK6 | 100.0 | 1000 | MELK | MELK | 86.0 | 1000 | MERTK | MERTK | 80.0 | 1000 | MET | MET(Y1235D) | 91.0 | 1000 | MINK1 | MINK | 100.0 | 1000 | MAP2K7 | MKK7 | 79.0 | 1000 | MKNK1 | MKNK1 | 93.0 | 1000 | MKNK2 | MKNK2 | 96.0 | 1000 | MYLK3 | MLCK | 100.0 | 1000 | MAP3K9 | MLK1 | 100.0 | 1000 | MAP3K10 | MLK2 | 100.0 | 1000 | MAP3K11 | MLK3 | 79.0 | 1000 | CDC42BPA | MRCKA | 100.0 | 1000 | CDC42BPB | MRCKB | 100.0 | 1000 | STK4 | MST1 | 100.0 | 1000 | MST1R | MST1R | 100.0 | 1000 | STK3 | MST2 | 100.0 | 1000 | STK24 | MST3 | 85.0 | 1000 | STK26 | MST4 | 100.0 | 1000 | MTOR | MTOR | 100.0 | 1000 | MUSK | MUSK | 72.0 | 1000 | MYLK | MYLK | 84.0 | 1000 | MYLK2 | MYLK2 | 100.0 | 1000 | MYLK4 | MYLK4 | 100.0 | 1000 | MYO3A | MYO3A | 100.0 | 1000 | MYO3B | MYO3B | 71.0 | 1000 | STK38 | NDR1 | 98.0 | 1000 | STK38L | NDR2 | 86.0 | 1000 | NEK1 | NEK1 | 100.0 | 1000 | NEK10 | NEK10 | 100.0 | 1000 | NEK11 | NEK11 | 93.0 | 1000 | NEK2 | NEK2 | 100.0 | 1000 | NEK3 | NEK3 | 100.0 | 1000 | NEK4 | NEK4 | 94.0 | 1000 | NEK5 | NEK5 | 100.0 | 1000 | NEK6 | NEK6 | 100.0 | 1000 | NEK7 | NEK7 | 100.0 | 1000 | NEK9 | NEK9 | 100.0 | 1000 | MAP3K14 | NIK | 82.0 | 1000 | NIM1K | NIM1 | 100.0 | 1000 | NLK | NLK | 94.0 | 1000 | OXSR1 | OSR1 | 100.0 | 1000 | MAPK14 | p38-alpha | 100.0 | 1000 | MAPK11 | p38-beta | 78.0 | 1000 | MAPK13 | p38-delta | 100.0 | 1000 | MAPK12 | p38-gamma | 100.0 | 1000 | PAK1 | PAK1 | 87.0 | 1000 | PAK2 | PAK2 | 83.0 | 1000 | PAK3 | PAK3 | 94.0 | 1000 | PAK4 | PAK4 | 94.0 | 1000 | PAK6 | PAK6 | 100.0 | 1000 | PAK5 | PAK7 | 100.0 | 1000 | CDK16 | PCTK1 | 100.0 | 1000 | CDK17 | PCTK2 | 100.0 | 1000 | CDK18 | PCTK3 | 98.0 | 1000 | PDGFRA | PDGFRA | 100.0 | 1000 | PDGFRB | PDGFRB | 100.0 | 1000 | PDPK1 | PDPK1 | 100.0 | 1000 | CDPK1 | PFCDPK1(P.falciparum) | 100.0 | 1000 | PK5 | PFPK5(P.falciparum) | 97.0 | 1000 | CDK15 | PFTAIRE2 | 100.0 | 1000 | CDK14 | PFTK1 | 100.0 | 1000 | PHKG1 | PHKG1 | 100.0 | 1000 | PHKG2 | PHKG2 | 100.0 | 1000 | PIK3C2B | PIK3C2B | 100.0 | 1000 | PIK3C2G | PIK3C2G | 100.0 | 1000 | PIK3CA | PIK3CA(Q546K) | 42.0 | 1000 | PIK3CB | PIK3CB | 100.0 | 1000 | PIK3CD | PIK3CD | 100.0 | 1000 | PIK3CG | PIK3CG | 100.0 | 1000 | PI4KB | PIK4CB | 100.0 | 1000 | PIKFYVE | PIKFYVE | 91.0 | 1000 | PIM1 | PIM1 | 96.0 | 1000 | PIM2 | PIM2 | 100.0 | 1000 | PIM3 | PIM3 | 98.0 | 1000 | PIP5K1A | PIP5K1A | 100.0 | 1000 | PIP5K1C | PIP5K1C | 84.0 | 1000 | PIP4K2B | PIP5K2B | 74.0 | 1000 | PIP4K2C | PIP5K2C | 100.0 | 1000 | PRKACA | PKAC-alpha | 100.0 | 1000 | PRKACB | PKAC-beta | 100.0 | 1000 | PKMYT1 | PKMYT1 | 100.0 | 1000 | PKN1 | PKN1 | 100.0 | 1000 | PKN2 | PKN2 | 100.0 | 1000 | PKNB | PKNB(M.tuberculosis) | 88.0 | 1000 | PLK1 | PLK1 | 100.0 | 1000 | PLK2 | PLK2 | 100.0 | 1000 | PLK3 | PLK3 | 95.0 | 1000 | PLK4 | PLK4 | 82.0 | 1000 | PRKCD | PRKCD | 100.0 | 1000 | PRKCE | PRKCE | 100.0 | 1000 | PRKCH | PRKCH | 100.0 | 1000 | PRKCI | PRKCI | 100.0 | 1000 | PRKCQ | PRKCQ | 100.0 | 1000 | PRKD1 | PRKD1 | 96.0 | 1000 | PRKD2 | PRKD2 | 93.0 | 1000 | PRKD3 | PRKD3 | 91.0 | 1000 | PRKG1 | PRKG1 | 100.0 | 1000 | PRKG2 | PRKG2 | 85.0 | 1000 | EIF2AK2 | PRKR | 100.0 | 1000 | PRKX | PRKX | 90.0 | 1000 | PRPF4B | PRP4 | 100.0 | 1000 | PTK2B | PYK2 | 100.0 | 1000 | SIK3 | QSK | 72.0 | 1000 | RAF1 | RAF1 | 100.0 | 1000 | RET | RET(V804M) | 94.0 | 1000 | RIOK1 | RIOK1 | 100.0 | 1000 | RIOK2 | RIOK2 | 100.0 | 1000 | RIOK3 | RIOK3 | 97.0 | 1000 | RIPK1 | RIPK1 | 100.0 | 1000 | RIPK2 | RIPK2 | 100.0 | 1000 | RIPK4 | RIPK4 | 66.0 | 1000 | DSTYK | RIPK5 | 100.0 | 1000 | ROCK1 | ROCK1 | 100.0 | 1000 | ROCK2 | ROCK2 | 100.0 | 1000 | ROS1 | ROS1 | 81.0 | 1000 | RPS6KA4 | RPS6KA4(Kin.Dom.2-C-terminal) | 85.0 | 1000 | RPS6KA5 | RPS6KA5(Kin.Dom.2-C-terminal) | 96.0 | 1000 | RPS6KA1 | RSK1(Kin.Dom.2-C-terminal) | 100.0 | 1000 | RPS6KA3 | RSK2(Kin.Dom.2-C-terminal) | 85.0 | 1000 | RPS6KA2 | RSK3(Kin.Dom.2-C-terminal) | 100.0 | 1000 | RPS6KA6 | RSK4(Kin.Dom.2-C-terminal) | 78.0 | 1000 | RPS6KB1 | S6K1 | 100.0 | 1000 | SBK1 | SBK1 | 100.0 | 1000 | SGK1 | SGK | 81.0 | 1000 | SBK3 | SgK110 | 100.0 | 1000 | SGK2 | SGK2 | 87.0 | 1000 | SGK3 | SGK3 | 100.0 | 1000 | SIK1 | SIK | 97.0 | 1000 | SIK2 | SIK2 | 100.0 | 1000 | SLK | SLK | 85.0 | 1000 | NUAK2 | SNARK | 92.0 | 1000 | SNRK | SNRK | 100.0 | 1000 | SRC | SRC | 100.0 | 1000 | SRMS | SRMS | 100.0 | 1000 | SRPK1 | SRPK1 | 72.0 | 1000 | SRPK2 | SRPK2 | 84.0 | 1000 | SRPK3 | SRPK3 | 100.0 | 1000 | STK16 | STK16 | 88.0 | 1000 | STK33 | STK33 | 98.0 | 1000 | STK35 | STK35 | 100.0 | 1000 | STK36 | STK36 | 89.0 | 1000 | STK39 | STK39 | 55.0 | 1000 | SYK | SYK | 64.0 | 1000 | MAP3K7 | TAK1 | 96.0 | 1000 | TAOK1 | TAOK1 | 100.0 | 1000 | TAOK2 | TAOK2 | 100.0 | 1000 | TAOK3 | TAOK3 | 35.0 | 1000 | TBK1 | TBK1 | 100.0 | 1000 | TEC | TEC | 100.0 | 1000 | TESK1 | TESK1 | 98.0 | 1000 | TGFBR1 | TGFBR1 | 100.0 | 1000 | TGFBR2 | TGFBR2 | 100.0 | 1000 | TIE1 | TIE1 | 100.0 | 1000 | TEK | TIE2 | 100.0 | 1000 | TLK1 | TLK1 | 87.0 | 1000 | TLK2 | TLK2 | 100.0 | 1000 | TNIK | TNIK | 61.0 | 1000 | TNK1 | TNK1 | 100.0 | 1000 | TNK2 | TNK2 | 100.0 | 1000 | TNNI3K | TNNI3K | 100.0 | 1000 | NTRK1 | TRKA | 71.0 | 1000 | NTRK2 | TRKB | 100.0 | 1000 | NTRK3 | TRKC | 98.0 | 1000 | TRPM6 | TRPM6 | 98.0 | 1000 | TSSK1B | TSSK1B | 100.0 | 1000 | TSSK3 | TSSK3 | 82.0 | 1000 | TTK | TTK | 100.0 | 1000 | TXK | TXK | 100.0 | 1000 | TYK2 | TYK2(JH2domain-pseudokinase) | 100.0 | 1000 | TYRO3 | TYRO3 | 100.0 | 1000 | ULK1 | ULK1 | 92.0 | 1000 | ULK2 | ULK2 | 89.0 | 1000 | ULK3 | ULK3 | 86.0 | 1000 | KDR | VEGFR2 | 100.0 | 1000 | PIK3C3 | VPS34 | 100.0 | 1000 | VRK2 | VRK2 | 100.0 | 1000 | WEE1 | WEE1 | 100.0 | 1000 | WEE2 | WEE2 | 100.0 | 1000 | WNK1 | WNK1 | 84.0 | 1000 | WNK2 | WNK2 | 84.0 | 1000 | WNK3 | WNK3 | 93.0 | 1000 | WNK4 | WNK4 | 79.0 | 1000 | STK32A | YANK1 | 97.0 | 1000 | STK32B | YANK2 | 100.0 | 1000 | STK32C | YANK3 | 100.0 | 1000 | YES1 | YES | 100.0 | 1000 | STK25 | YSK1 | 100.0 | 1000 | MAP3K19 | YSK4 | 82.0 | 1000 | MAP3K20 | ZAK | 100.0 | 1000 | ZAP70 | ZAP70 | 99.0 | 1000 |
|---|
PF-04418948
Ligand profiling has been performed at 10 µM probe concentration with IC50 and Ki follow up for specific targets.
Conclusion: Closest off-targets at 10 µM are LTB4 (IC50 = 9.7 µM), ML2 (IC50 = 0.53 µM) and PDE3 (IC50 = 3.5 µM).
| Target protein | HGNC name | Species | % inhibition at 10 µM | IC50 [nM] | Ki [nM] |
|---|---|---|---|---|---|
| 5-HT transporter (h) | SLC6A4 | Homo sapiens | -8.0 | ||
| 5-HT1A (h) | HTR1A | Homo sapiens | 6.0 | ||
| 5-HT1B | HTR1B | Homo sapiens | -7.0 | ||
| 5-HT1D | HTR1D | -10.0 | |||
| 5-HT2A (h) | HTR2A | 0.0 | |||
| 5-HT2A (h) (agonist site) | HTR2A | Homo sapiens | -15.0 | ||
| 5-HT2B (h) (agonist site/DOI) | HTR2B | Homo sapiens | 13.0 | ||
| 5-HT2C (h) | HTR2C | Homo sapiens | 8.0 | ||
| 5-HT2C (h) (agonist site) | HTR2C | Homo sapiens | -6.0 | ||
| 5-HT3 (h) | HTR3A | Homo sapiens | -6.0 | ||
| 5-HT4e (h) | HTR4 | Homo sapiens | -14.0 | ||
| 5-HT6 (h) | HTR6 | Homo sapiens | 0.0 | ||
| 5-HT7 (h) | HTR7 | Homo sapiens | -2.0 | ||
| A1 (h) | ADORA1 | Homo sapiens | -2.0 | ||
| A2A (h) | ADORA2A | Homo sapiens | -9.0 | ||
| A3 (h) | ADORA3 | Homo sapiens | -10.0 | ||
| Abl kinase (h) | ABL1 | Homo sapiens | 9.0 | ||
| ACE (h) | ACE | Homo sapiens | 14.0 | ||
| Acetylcholinesterase (h) | ACHE | Homo sapiens | 45.0 | ||
| alpha 1 (non- selective) | 9.0 | ||||
| alpha 2A (h) | ADRA2A | Homo sapiens | 26.0 | ||
| alpha 2B (h) | ADRA2B | Homo sapiens | 1.0 | ||
| alpha 2C (h) | ADRA2C | Homo sapiens | 4.0 | ||
| AMPA | -13.0 | ||||
| Androgen (h) (AR) | AR | Homo sapiens | 0.0 | ||
| AT1 (h) | AGTR1 | Homo sapiens | 1.0 | ||
| ATPase (Na+/K+) | Homo sapiens | 5.0 | |||
| beta 1 (h) | ADRB1 | Homo sapiens | 9.0 | ||
| beta 2 (h) | ADRB2 | Homo sapiens | -4.0 | ||
| beta 3 (h) | ADRB3 | Homo sapiens | 3.0 | ||
| Ca2+ channel (L, DHP site) | Homo sapiens | -3.0 | |||
| Ca2+ channel (L, diltiazem site) | Homo sapiens | 6.0 | |||
| Ca2+ channel (L, verapamil site) | Homo sapiens | -5.0 | |||
| Ca2+ channel (N) | Homo sapiens | -7.0 | |||
| CaMK2alpha (h) | CAMK2A | Homo sapiens | 5.0 | ||
| Carbonic anhydrase II (h) | CA2 | Homo sapiens | 9.0 | ||
| Caspase-3 (h) | CASP3 | Homo sapiens | 0.0 | ||
| CB1 (h) | CNR1 | Homo sapiens | 0.0 | ||
| CB2 (h) | CNR2 | Homo sapiens | 0.0 | ||
| CCKA (h) (CCK1) | CCKAR | Homo sapiens | 29.0 | ||
| CCKB (h) (CCK2) | CCKBR | Homo sapiens | -8.0 | ||
| Choline transporter (h) (CHT1) | SLC5A7 | Homo sapiens | 4.0 | ||
| Cl- channel | 19.0 | ||||
| COX1 (h) | PTGS1 | Homo sapiens | -25.0 | ||
| COX2 (h) | PTGS2 | Homo sapiens | 2.0 | ||
| CXCR4 (h) | CXCR4 | Homo sapiens | 4.0 | ||
| CYP2C19 inhibition | CYP2C19 | 5.0 | |||
| CYP2C9 inhibition | CYP2C9 | 41.0 | |||
| CYP2D6 inhibition | CYP2D6 | 18.0 | |||
| CYP3A4 inhibition | CYP3A4 | 17.0 | |||
| D1 (h) | DRD1 | Homo sapiens | 5.0 | ||
| D2S (h) | DRD2 | Homo sapiens | -2.0 | ||
| D2S (h) (agonist site) | DRD2 | Homo sapiens | -6.0 | ||
| D3 (h) | DRD3 | Homo sapiens | 1.0 | ||
| D4.4 (h) | DRD4 | Homo sapiens | -8.0 | ||
| DA transporter (h) | SLC6A3 | Homo sapiens | 11.0 | ||
| delta 2 (h) (DOP) | OPRD1 | Homo sapiens | 0.0 | ||
| ETA (h) | EDNRA | Homo sapiens | 3.0 | ||
| ETB (h) | EDNRB | Homo sapiens | -1.0 | ||
| FLT-1 kinase (h) (VEGFR1) | FLT1 | Homo sapiens | 9.0 | ||
| GABAA BZD (central) | 10.0 | ||||
| GABA transporter | SLC6A1 | 14.0 | |||
| GABAA | 16.0 | ||||
| GABAB (1b) (h) | GABBR1 | Homo sapiens | -21.0 | ||
| Ghrelin (h) (GHS) | GHRL | Homo sapiens | -6.0 | ||
| GR (h) | NR3C1 | Homo sapiens | -1.0 | ||
| Glycine (strychnine-insensitive) | 11.0 | ||||
| H1 (h) | HRH1 | Homo sapiens | 0.0 | ||
| H2 (h) | HRH2 | Homo sapiens | 3.0 | ||
| H3 (h) | HRH3 | Homo sapiens | 10.0 | ||
| H4 (h) | HRH4 | Homo sapiens | -4.0 | ||
| I1 | GNAI1 | -14.0 | |||
| Kainate | GRIK2 | -15.0 | |||
| kappa (KOP) | OPRK1 | Homo sapiens | 46.0 | ||
| LTB4 (h) (BLT1) | LTB4R | Homo sapiens | 51.0 | 9700.00 | 4800.00 |
| LTD4 (h) (CysLT1) | CYSLTR1 | Homo sapiens | 2.0 | ||
| Lyn kinase (h) | LYN | Homo sapiens | 2.0 | ||
| M1 (h) | CHRM1 | Homo sapiens | 9.0 | ||
| M2 (h) | CHRM2 | Homo sapiens | 1.0 | ||
| M3 (h) | CHRM3 | Homo sapiens | 1.0 | ||
| M4 (h) | CHRM4 | Homo sapiens | 0.0 | ||
| M5 (h) | CHRM5 | Homo sapiens | 1.0 | ||
| MAO-A | MAOA | 3.0 | |||
| MC1 | MC1R | 6.0 | |||
| MC3 (h) | MC3R | Homo sapiens | -11.0 | ||
| MC4 (h) | MC4R | Homo sapiens | 8.0 | ||
| MCH1 (h) | MCHR1 | Homo sapiens | -13.0 | ||
| ML1 | MCOLN1 | -3.0 | |||
| ML2 (MT3) | NQO2 | 93.0 | 530.00 | 520.00 | |
| MMP-9 (h) | MMP9 | Homo sapiens | 10.0 | ||
| Motilin (h) | MLNR | Homo sapiens | -5.0 | ||
| mu (h) (MOP) (agonist site) | OPRM1 | Homo sapiens | -7.0 | ||
| N (muscle-type) (h) | CHRNA4 | Homo sapiens | -10.0 | ||
| N (neuronal) (alpha -BGTX-insensitive) (alpha 4 beta 2) | CHRNA1 | -10.0 | |||
| Na+ channel (site 2) | 9.0 | ||||
| NE transporter (h) | SLC6A2 | Homo sapiens | -2.0 | ||
| NK1 (h) | TACR1 | Homo sapiens | 3.0 | ||
| NK2 (h) | TACR2 | Homo sapiens | 0.0 | ||
| NMDA | 1.0 | ||||
| p38 alpha kinase (h) | MAPK14 | Homo sapiens | -1.0 | ||
| PCP | PRCP | -6.0 | |||
| PDE11 (h) | PDE11A | Homo sapiens | 14.0 | ||
| PDE2 (h) | PDE2A | Homo sapiens | 5.0 | ||
| PDE3 (h) | Homo sapiens | 78.0 | 3500.00 | ||
| PDE4 (h) | Homo sapiens | 8.0 | |||
| PDE5 (h) | PDE5A | Homo sapiens | 6.0 | ||
| PDE6 | 3.0 | ||||
| PPAR gamma (h) | PPARG | Homo sapiens | 14.0 | ||
| Rolipram | 3.0 | ||||
| sigma (non-selective) | 0.0 | ||||
| SK+Ca channel | -1.0 | ||||
| sst4 (h) | SSTR4 | Homo sapiens | 0.0 | ||
| TH | TH | -10.0 | |||
| TNF-alpha (h) | TNF | Homo sapiens | -1.0 | ||
| TXA2/P GH2 (h)(TP) | TBXA2R | Homo sapiens | 0.0 | ||
| UT1 (h) | SLC14A1 | Homo sapiens | 14.0 | ||
| V1a (h) | AVPR1A | Homo sapiens | -3.0 | ||
| V2 (h) | AVPR2 | Homo sapiens | -1.0 | ||
| VIP1 (h) (VPAC1) | VIPR1 | Homo sapiens | -13.0 | ||
| Y1 (h) | NPY1R | Homo sapiens | 1.0 | ||
| ZAP70 kinase (h) | ZAP70 | Homo sapiens | 9.0 |