PF-543 [Ligand Id: 6623] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3134157
  • EPH receptor A2/Ephrin type-A receptor 2 in Human [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
Created with Highcharts 10.3.3ValuesChart context menuEphrin type-A receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
Created with Highcharts 10.3.3ValuesChart context menuEphrin type-B receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
Created with Highcharts 10.3.3ValuesChart context menuEpidermal growth factor receptor erbB1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
Created with Highcharts 10.3.3ValuesChart context menuFibroblast growth factor receptor 4pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
Created with Highcharts 10.3.3ValuesChart context menuInsulin-like growth factor I receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuInsulin receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
Created with Highcharts 10.3.3ValuesChart context menuMacrophage colony stimulating factor receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
Created with Highcharts 10.3.3ValuesChart context menuPlatelet-derived growth factor receptor alphapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
Created with Highcharts 10.3.3ValuesChart context menuPlatelet-derived growth factor receptor betapKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
Created with Highcharts 10.3.3ValuesChart context menuReceptor protein-tyrosine kinase erbB-2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
Created with Highcharts 10.3.3ValuesChart context menuReceptor protein-tyrosine kinase erbB-4pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • sphingosine kinase 1/Sphingosine kinase 1 in Human [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
  • sphingosine kinase 1/Sphingosine kinase 1 in Mouse [ChEMBL: CHEMBL2401605] [GtoPdb: 2204] [UniProtKB: Q8CI15]
Created with Highcharts 10.3.3ValuesChart context menuSphingosine kinase 1pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 Mouse0246810Highcharts.com
  • sphingosine kinase 2/Sphingosine kinase 2 in Human [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
Created with Highcharts 10.3.3ValuesChart context menuSphingosine kinase 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine kinase non-receptor protein 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase ABLpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase BTKpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor FLT3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase receptor RETpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
Created with Highcharts 10.3.3ValuesChart context menuTyrosine-protein kinase SRCpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
Created with Highcharts 10.3.3ValuesChart context menuVascular endothelial growth factor receptor 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
Created with Highcharts 10.3.3ValuesChart context menuVascular endothelial growth factor receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
Created with Highcharts 10.3.3ValuesChart context menuVascular endothelial growth factor receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
EPH receptor A2/Ephrin type-A receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2068] [GtoPdb: 1822] [UniProtKB: P29317]
ChEMBL Inhibition of EPHA2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Inhibition of EPHB2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
ChEMBL Inhibition of FGFR1 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
ChEMBL Inhibition of FGFR2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Inhibition of FGFR3 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Inhibition of FGFR4 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of IGF1R (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Inhibition of Insulin receptor (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Inhibition of CSF1R (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
ChEMBL Inhibition of PDGFRalpha (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibition of PDGFRbeta (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
ChEMBL Inhibition of ERBB2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
ChEMBL Inhibition of ERBB4 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
sphingosine kinase 1/Sphingosine kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4394] [GtoPdb: 2204] [UniProtKB: Q9NYA1]
ChEMBL Binding affinity to SK1 (unknown origin) assessed as inhibition of sphingosine phosphorylation B 8.3 pKd 5 nM Kd J Med Chem (2018) 61: 9811-9840 [PMID:29969256]
ChEMBL Inhibition of His6 tagged human SphK1 expressed in Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins prior substrate addition by Caliper assay B 8.37 pKi 4.3 nM Ki ACS Med Chem Lett (2014) 5: 1329-1333 [PMID:25516793]
ChEMBL Inhibition of SK1 (unknown origin) B 8.4 pKi 4 nM Ki J Med Chem (2016) 59: 965-984 [PMID:26780304]
GtoPdb - - 8.44 pKi 3.6 nM Ki Biochem J (2012) 444: 79-88 [PMID:22397330]
ChEMBL Inhibition of recombinant human C-terminal His-tagged SPHK1 expressed in fall armyworm sf21 cells using sphingosine as substrate after 1 hr by FITC-based caliper assay B 8.44 pKi 3.6 nM Ki J Med Chem (2017) 60: 3933-3957 [PMID:28406646]
ChEMBL Inhibition of human C-terminal His6-tagged SphK1 expressed in baculovirus infected Sf21 insect cells B 8.44 pKi 3.6 nM Ki Eur J Med Chem (2017) 139: 461-481 [PMID:28822281]
ChEMBL Inhibition of recombinant human SphK1 expressed in baculovirus infected Sf9 cells assessed as decrease in [33P]SIP production using D-erythro-sphingosine as substrate in presence of [gamma33P]-ATP by scintillation counting method B 8.44 pKi 3.6 nM Ki Bioorg Med Chem (2021) 30: 115941-115941 [PMID:33385956]
ChEMBL Competitive inhibition of recombinant human C-terminal His-tagged SphK1 expressed in baculovirus infected Sf21 cells using varying concentrations of FITC-sphingosine as substrate incubated for 30 mins by LC-MS/MS analysis B 8.44 pKi 3.6 nM Ki Eur J Med Chem (2020) 206: 112713-112713 [PMID:32919113]
ChEMBL Competitive-inhibition of recombinant human C-terminal His6-tagged Sphk1 expressed in baculovirus infected Sf21 insect cells using varying levels of sphingosine as substrate measured after 30 mins by LC-MS analysis B 8.44 pKi 3.6 nM Ki Eur J Med Chem (2021) 212: 113121-113121 [PMID:33445156]
ChEMBL Inhibition of human recombinant SphK1 expressed in Sf9 cells assessed as radiolabeled products using 5 uM sphingosine and 10 uM gamma[32P]ATP by liquid scintillation counting B 8.44 pKi 3.6 nM Ki J Med Chem (2015) 58: 1879-1899 [PMID:25643074]
ChEMBL Inhibition of recombinant His-tagged human SK1 assessed as production of [32P]-S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP B 6.41 pIC50 387 nM IC50 J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of SphK1 (unknown origin) using D-Sph as substrate incubated for 40 mins by ADP-Glo Plus luminescence kinase assay B 6.97 pIC50 107 nM IC50 Bioorg Med Chem (2023) 93: 117441-117441 [PMID:37586181]
ChEMBL Inhibition of SphK1 (unknown origin) B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967]
ChEMBL Inhibition of recombinant SK1 (unknown origin) using sphingosine and [gamma-32P]ATP as substrate after 30 mins B 7.55 pIC50 28 nM IC50 Medchemcomm (2013) 4: 1394-1399 [PMID:24396570]
ChEMBL Inhibition of SK1 (unknown origin) using 5 uM of sphingosine as substrate B 7.55 pIC50 28 nM IC50 J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of GFP-tagged SK1 (unknown origin) expressed in HEK293 cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis B 7.55 pIC50 28 nM IC50 J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL Inhibition of SPHK1 in human whole-blood using C17-sphingosine as substrate assessed as reduction in C17-S1P production preincubated for 30 mins followed by substrate addition measured after 10 mins by MS analysis B 7.7 pIC50 20 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL Inhibition of C-terminal His6-tagged human SPHK1 expressed in baculovirus infected Sf21 insect cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper mobility shift assay B 8.44 pIC50 3.6 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ChEMBL Inhibition of SK1 (unknown origin) using 3 uM of sphingosine as substrate B 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of recombinant human C-terminus His-tagged SphK1 expressed in baculovirus infected Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper fluorescent assay B 8.57 pIC50 2.7 nM IC50 Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547]
ChEMBL Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in S1P formation using sphingosine as substrate after 1 hr by FITC-based caliper assay B 8.57 pIC50 2.7 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL Inhibition of recombinant C-terminal His6-tagged human SphK1 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay B 8.57 pIC50 2.7 nM IC50 Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190]
GtoPdb - - 8.57 pIC50 2.7 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL Inhibition of SPHK1 (unknown origin) using sphingosine-fluorescein as substrate incubated for 1 hr in presence of ATP by mobility shift assay B 8.59 pIC50 2.6 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ChEMBL Inhibition of human C-terminal His6-tagged SPHK1 expressed in fall armyworm sf9 cells assessed as reduction in ADP formation using sphingosine as substrate preincubated for 15 mins followed by substrate addition after 1 hr by transcreener-based fluorescence polarization assay B 8.7 pIC50 2 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
GtoPdb - - 8.7 pIC50 2 nM IC50 Biochem J (2012) 444: 79-88 [PMID:22397330]
ChEMBL Inhibition of SPHK1 in human MDA1483 cells using C17-sphingosine as substrate assessed as reduction in C17-S1P formation preincubated for 30 mins with substrate measured after 15 mins by LC-MS analysis B 9.1 pIC50 0.8 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
sphingosine kinase 1/Sphingosine kinase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2401605] [GtoPdb: 2204] [UniProtKB: Q8CI15]
ChEMBL Inhibition of SphK1 in mouse erythrocytes using sphingosine as substrate by luminescence assay B 8.44 pKi 3.6 nM Ki ACS Med Chem Lett (2016) 7: 229-234 [PMID:26985306]
sphingosine kinase 2/Sphingosine kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3023] [GtoPdb: 2205] [UniProtKB: Q9NRA0]
ChEMBL Inhibition of SK2 (unknown origin) B 8.44 pKi 3.6 nM Ki J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL Inhibition of recombinant human SK2 assessed as production of [32P] S1P using 10 uM sphingosine as substrate by TLC method in presence of 100 uM [gamma32P]-ATP relative to control B 4.77 pIC50 17000 nM IC50 J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of SK2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 965-984 [PMID:26780304]
ChEMBL Inhibition of SPHK2 (unknown origin) using sphingosine-fluorescein as substrate incubated for 1 hr in presence of ATP by mobility shift assay B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ChEMBL Inhibition of SphK2 (unknown origin) B 5.27 pIC50 5400 nM IC50 Bioorg Med Chem Lett (2021) 34: 127754-127754 [PMID:33347967]
ChEMBL Inhibition of recombinant human full-length N-terminal His-tagged SK2 expressed in baculovirus infected Sf9 insect cells using Sph as substrate measured after 30 mins in presence of [gamma32P]ATP by Cerenkov counting analysis B 5.3 pIC50 >5000 nM IC50 J Med Chem (2019) 62: 3658-3676 [PMID:30889352]
ChEMBL Inhibition of SPHK2 (unknown origin) B 5.3 pIC50 >5000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ChEMBL Inhibition of SphK2 (unknown origin) using NBD-Sph as substrate by fluorescent plate reader analysis B 6.32 pIC50 480 nM IC50 Bioorg Med Chem (2023) 93: 117441-117441 [PMID:37586181]
ChEMBL Inhibition of human recombinant C-terminal His6 tagged SphK2 expressed in baculovirus infected sf21 cells using FITC-sphingosine as substrate after 1 hr in presence of ATP by microfluidic capillary electrophoresis mobility shift assay B 6.44 pIC50 360 nM IC50 Bioorg Med Chem (2017) 25: 3046-3052 [PMID:28408190]
ChEMBL Inhibition of SPHK2 (unknown origin) by FITC-based caliper assay B 6.45 pIC50 356 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
ChEMBL Inhibition of recombinant human C-terminus His-tagged SphK2 expressed in baculovirus infected Sf21 cells using FITC-sphingosine as substrate preincubated for 90 mins followed by substrate addition in presence of ATP by caliper fluorescent assay B 6.45 pIC50 356 nM IC50 Eur J Med Chem (2021) 213: 113164-113164 [PMID:33454547]
GtoPdb - - 6.45 pIC50 356 nM IC50 J Med Chem (2017) 60: 2562-2572 [PMID:28231433]
tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912]
ChEMBL Inhibition of ACK1 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of ABL (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of BTK (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of RET (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of SRC (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
ChEMBL Inhibition of VEGFR1 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
ChEMBL Inhibition of VEGFR3 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2022) 65: 7697-7716 [PMID:35439002]

ChEMBL data shown on this page come from version 35:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]