GNF-5837 [Ligand Id: 8071] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL2037226
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Mouse [ChEMBL: CHEMBL5771] [GtoPdb: 1839] [UniProtKB: P97793]
There should be some charts here, you may need to enable JavaScript!
  • BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Mouse [ChEMBL: CHEMBL2034793] [GtoPdb: 1942] [UniProtKB: P97504]
There should be some charts here, you may need to enable JavaScript!
  • EPH receptor A3/Ephrin type-A receptor 3 in Human [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
  • EPH receptor A3/Ephrin type-A receptor 3 in Mouse [ChEMBL: CHEMBL2034794] [GtoPdb: 1823] [UniProtKB: P29319]
There should be some charts here, you may need to enable JavaScript!
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
  • EPH receptor B2/Ephrin type-B receptor 2 in Mouse [ChEMBL: CHEMBL5961] [GtoPdb: 1831] [UniProtKB: P54763]
There should be some charts here, you may need to enable JavaScript!
  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Mouse [ChEMBL: CHEMBL4066] [GtoPdb: 1810] [UniProtKB: Q61851]
There should be some charts here, you may need to enable JavaScript!
  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
  • fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Mouse [ChEMBL: CHEMBL3839] [GtoPdb: 1811] [UniProtKB: Q03142]
There should be some charts here, you may need to enable JavaScript!
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Mouse [ChEMBL: CHEMBL5585] [GtoPdb: 1815] [UniProtKB: P16056]
There should be some charts here, you may need to enable JavaScript!
  • Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Mouse [ChEMBL: CHEMBL5381] [GtoPdb: 1801] [UniProtKB: Q60751]
There should be some charts here, you may need to enable JavaScript!
  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
There should be some charts here, you may need to enable JavaScript!
  • colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
There should be some charts here, you may need to enable JavaScript!
  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Mouse [ChEMBL: CHEMBL1795170] [GtoPdb: 1816] [UniProtKB: Q62190]
There should be some charts here, you may need to enable JavaScript!
  • KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Mouse [ChEMBL: CHEMBL2034798] [GtoPdb: 1805] [UniProtKB: P05532]
There should be some charts here, you may need to enable JavaScript!
  • mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Mouse [ChEMBL: CHEMBL2034797] [GtoPdb: 1497] [UniProtKB: Q9WTU6]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
There should be some charts here, you may need to enable JavaScript!
  • neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
There should be some charts here, you may need to enable JavaScript!
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
There should be some charts here, you may need to enable JavaScript!
  • ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Mouse [ChEMBL: CHEMBL2034799] [GtoPdb: 2185] [UniProtKB: P35546]
There should be some charts here, you may need to enable JavaScript!
  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
  • c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Mouse [ChEMBL: CHEMBL2034802] [GtoPdb: 1840] [UniProtKB: Q78DX7]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Mouse [ChEMBL: CHEMBL2034796] [GtoPdb: 1807] [UniProtKB: Q00342]
There should be some charts here, you may need to enable JavaScript!
  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
There should be some charts here, you may need to enable JavaScript!
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
There should be some charts here, you may need to enable JavaScript!
  • BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
There should be some charts here, you may need to enable JavaScript!
  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
  • FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Mouse [ChEMBL: CHEMBL2034795] [GtoPdb: 2024] [UniProtKB: P14234]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
There should be some charts here, you may need to enable JavaScript!
  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Mouse [ChEMBL: CHEMBL2258] [GtoPdb: 2060] [UniProtKB: P25911]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
There should be some charts here, you may need to enable JavaScript!
  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
There should be some charts here, you may need to enable JavaScript!
  • tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Human [ChEMBL: CHEMBL5274] [GtoPdb: 1841] [UniProtKB: P35590]
  • tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Mouse [ChEMBL: CHEMBL2034800] [GtoPdb: 1841] [UniProtKB: Q06806]
There should be some charts here, you may need to enable JavaScript!
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
There should be some charts here, you may need to enable JavaScript!
  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
  • zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Mouse [ChEMBL: CHEMBL2034801] [GtoPdb: 2285] [UniProtKB: P43404]
There should be some charts here, you may need to enable JavaScript!
  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Mouse [ChEMBL: CHEMBL3516] [GtoPdb: 1812] [UniProtKB: P35969]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b ALK B 5.17 pIC50 6800 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b ALK B 5.47 pIC50 3400 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5771] [GtoPdb: 1839] [UniProtKB: P97793]
ChEMBL Inhibition of Tel-fused ALK in mouse BA/F3 cells B 5.47 pIC50 3400 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034793] [GtoPdb: 1942] [UniProtKB: P97504]
ChEMBL Inhibition of Tel-fused BMX in mouse BA/F3 cells B 5.17 pIC50 6700 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
EPH receptor A3/Ephrin type-A receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4954] [GtoPdb: 1823] [UniProtKB: P29320]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b EPHA3 B 5.23 pIC50 5900 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
EPH receptor A3/Ephrin type-A receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034794] [GtoPdb: 1823] [UniProtKB: P29319]
ChEMBL Inhibition of Tel-fused EPHA3 in mouse BA/F3 cells B 5.23 pIC50 5900 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b EPHB2 B 5.24 pIC50 5800 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
EPH receptor B2/Ephrin type-B receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5961] [GtoPdb: 1831] [UniProtKB: P54763]
ChEMBL Inhibition of Tel-fused EPHB2 in mouse BA/F3 cells B 5.24 pIC50 5800 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b FGFR3 B 5.03 pIC50 9300 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4066] [GtoPdb: 1810] [UniProtKB: Q61851]
ChEMBL Inhibition of Tel-fused FGFR3 in mouse BA/F3 cells B 5.03 pIC50 9300 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3973] [GtoPdb: 1811] [UniProtKB: P22455]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b FGFR4 B 5.15 pIC50 7000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
fibroblast growth factor receptor 4/Fibroblast growth factor receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3839] [GtoPdb: 1811] [UniProtKB: Q03142]
ChEMBL Inhibition of Tel-fused FGFR4 in mouse BA/F3 cells B 5.15 pIC50 7000 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b MET B 5.24 pIC50 5800 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5585] [GtoPdb: 1815] [UniProtKB: P16056]
ChEMBL Inhibition of Tel-fused MET in mouse BA/F3 cells B 5.24 pIC50 5800 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
Insulin-like growth factor I receptor/Insulin-like growth factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5381] [GtoPdb: 1801] [UniProtKB: Q60751]
ChEMBL Inhibition of Tel-fused IGF1R in mouse BA/F3 cells B 5.12 pIC50 7600 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b IGF1R B 5.12 pIC50 7600 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b INSR B 5.1 pIC50 8000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
Insulin receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3187] [GtoPdb: 1800] [UniProtKB: P15208]
ChEMBL Inhibition of Tel-fused INSR in mouse BA/F3 cells B 5.1 pIC50 8000 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581]
ChEMBL Inhibition of Tel-fused FMS in mouse BA/F3 cells B 5.4 pIC50 4000 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b CSF1R B 5.4 pIC50 4000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b MST1R B 5.33 pIC50 4700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795170] [GtoPdb: 1816] [UniProtKB: Q62190]
ChEMBL Inhibition of Tel-fused RON in mouse BA/F3 cells B 5.33 pIC50 4700 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
KIT proto-oncogene, receptor tyrosine kinase/Mast/stem cell growth factor receptor Kit in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034798] [GtoPdb: 1805] [UniProtKB: P05532]
ChEMBL Inhibition of Tel-fused KIT in mouse BA/F3 cells B 6.04 pIC50 910 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
mitogen-activated protein kinase 9/Mitogen-activated protein kinase 9 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034797] [GtoPdb: 1497] [UniProtKB: Q9WTU6]
ChEMBL Inhibition of Tel-fused JNK2 in mouse BA/F3 cells B 5.54 pIC50 2900 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629]
ChEMBL Inhibition of N-terminal GST-tagged human recombinant TRKA G595R mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2023) 253: 115291-115291 [PMID:37030091]
ChEMBL Inhibition of N-terminal GST-tagged human recombinant TRKA G667C mutant (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by HTRF assay B 7.35 pIC50 45 nM IC50 Eur J Med Chem (2023) 253: 115291-115291 [PMID:37030091]
ChEMBL Affinity On-target Cellular interaction: (Proliferation assay (in Ba/F3 cells expressing activated NTRK1, Tel-TRK or Tel-KDR fusions)) EUB0000136b NTRK1 B 7.96 pIC50 11 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
GtoPdb - - 7.96 pIC50 11 nM IC50 ACS Med Chem Lett (2012) 3: 140-5 [PMID:24900443]
ChEMBL Inhibition of TRKA by HTRF assay B 8.1 pIC50 8 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
ChEMBL Affinity Biochemical interaction: (HTRF assay) EUB0000136b NTRK1 B 8.1 pIC50 8 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
neurotrophic receptor tyrosine kinase 2/Neurotrophic tyrosine kinase receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4898] [GtoPdb: 1818] [UniProtKB: Q16620]
ChEMBL Inhibition of TRKB by HTRF assay B 7.92 pIC50 12 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
ChEMBL Affinity Biochemical interaction: (Caliper microfluidic assay) EUB0000136b NTRK2 B 7.92 pIC50 12 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity On-target Cellular interaction: (Proliferation assay (in Ba/F3 cells expressing activated NTRK2, Tel-TRK or Tel-KDR fusions)) EUB0000136b NTRK2 B 8.05 pIC50 9 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
GtoPdb - - 8.05 pIC50 9 nM IC50 ACS Med Chem Lett (2012) 3: 140-5 [PMID:24900443]
neurotrophic receptor tyrosine kinase 3/NT-3 growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5608] [GtoPdb: 1819] [UniProtKB: Q16288]
GtoPdb - - 8.15 pIC50 7 nM IC50 ACS Med Chem Lett (2012) 3: 140-5 [PMID:24900443]
ChEMBL Affinity On-target Cellular interaction: (Proliferation assay (in Ba/F3 cells expressing activated NTRK3, Tel-TRK or Tel-KDR fusions)) EUB0000136b NTRK3 B 8.15 pIC50 7 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
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 Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b PDGFRB B 6.06 pIC50 870 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2749] [GtoPdb: 1804] [UniProtKB: P05622]
ChEMBL Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells B 6.06 pIC50 870 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
ret proto-oncogene/Proto-oncogene tyrosine-protein kinase receptor Ret in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034799] [GtoPdb: 2185] [UniProtKB: P35546]
ChEMBL Inhibition of Tel-fused RET in mouse BA/F3 cells B 5.28 pIC50 5300 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5568] [GtoPdb: 1840] [UniProtKB: P08922]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b ROS1 B 5.22 pIC50 6000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
c-ros oncogene 1, receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase ROS in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034802] [GtoPdb: 1840] [UniProtKB: Q78DX7]
ChEMBL Inhibition of Tel-fused ROS in mouse BA/F3 cells B 5.22 pIC50 6000 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034796] [GtoPdb: 1807] [UniProtKB: Q00342]
ChEMBL Inhibition of Tel-fused FLT3 in mouse BA/F3 cells B 5.29 pIC50 5100 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
ChEMBL Inhibition of c-Kit in human Mo7e cells B 6 pIC50 1000 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b KIT B 6.04 pIC50 910 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
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 Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b ABL1 B 5.09 pIC50 8200 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b BMX B 5.17 pIC50 6700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b FGR B 5.44 pIC50 3600 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fgr in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034795] [GtoPdb: 2024] [UniProtKB: P14234]
ChEMBL Inhibition of Tel-fused FGR in mouse BA/F3 cells B 5.44 pIC50 3600 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b JAK2 B 5.54 pIC50 2900 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b LYN B 5.14 pIC50 7300 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2258] [GtoPdb: 2060] [UniProtKB: P25911]
ChEMBL Inhibition of Tel-fused LYN in mouse BA/F3 cells B 5.14 pIC50 7300 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b FLT3 B 5.29 pIC50 5100 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b RET B 5.28 pIC50 5300 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5274] [GtoPdb: 1841] [UniProtKB: P35590]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b TIE1 B 5.24 pIC50 5700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
tyrosine kinase with immunoglobulin like and EGF like domains 1/Tyrosine-protein kinase receptor Tie-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034800] [GtoPdb: 1841] [UniProtKB: Q06806]
ChEMBL Inhibition of Tel-fused TIE1 in mouse BA/F3 cells B 5.24 pIC50 5700 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b SRC B 5.14 pIC50 7300 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
ChEMBL Inhibition of Tel-fused SRC in mouse BA/F3 cells B 5.14 pIC50 7300 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403]
ChEMBL Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b ZAP70 B 5.33 pIC50 4700 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034801] [GtoPdb: 2285] [UniProtKB: P43404]
ChEMBL Inhibition of Tel-fused ZAP70 in mouse BA/F3 cells B 5.33 pIC50 4700 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]
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 Selectivity interaction (Cellular Kinase Panel (Ba/F3 cells fused with a Tel dimerization partner)) EUB0000136b FLT1 B 5.36 pIC50 4400 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3516] [GtoPdb: 1812] [UniProtKB: P35969]
ChEMBL Inhibition of Tel-fused FLT1 in mouse BA/F3 cells B 5.36 pIC50 4400 nM IC50 ACS Med Chem Lett (2012) 3: 140-145 [PMID:24900443]

ChEMBL data shown on this page come from version 34:

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]