VEGF receptor 2 kinase inhibitor I [Ligand Id: 6053] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL86943
  • ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Mouse [ChEMBL: CHEMBL3516] [GtoPdb: 1812] [UniProtKB: P35969]
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  • kinase insert domain receptor in Mouse [GtoPdb: 1813] [UniProtKB: P35918]
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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 Inhibition of ALK by ELISA-based kinase assay B 5.27 pIC50 5400 nM IC50 Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Epidermal growth factor receptor (EGF RTK). B 4 pIC50 >100000 nM IC50 J Med Chem (1998) 41: 2588-2603 [PMID:9651163]
ChEMBL Inhibition of EGF B 4 pIC50 >100000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 B 5.3 pIC50 5000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Insulin-like growth factor I receptor B 4 pIC50 >100000 nM IC50 J Med Chem (1998) 41: 2588-2603 [PMID:9651163]
platelet derived growth factor receptor beta/platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095189] [GtoPdb: 18041803] [UniProtKB: P09619P16234]
ChEMBL Inhibition of PDGF B 4 pIC50 >100000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 Test concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Platelet-derived growth factor receptor beta (PDGF RTK). B 4 pIC50 >100000 nM IC50 J Med Chem (1998) 41: 2588-2603 [PMID:9651163]
ChEMBL Inhibition of bPDGFR in human PAC1 cells B 5.4 pIC50 4000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Her-2 receptor tyrosine kinase (HER-2 RTK) B 4 pIC50 >100000 nM IC50 J Med Chem (1998) 41: 2588-2603 [PMID:9651163]
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 by ELISA-based kinase assay B 4.72 pIC50 19000 nM IC50 Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004]
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 by ELISA-based kinase assay B 5.37 pIC50 4300 nM IC50 Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells B 6.12 pIC50 760 nM IC50 Bioorg Med Chem (2010) 18: 1482-1496 [PMID:20117004]
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 Concentration required to achieve 50% inhibition of tyrosine phosphorylation on murine VEGF receptor (FLK-1 RTK). B 7.15 pIC50 70 nM IC50 J Med Chem (1998) 41: 2588-2603 [PMID:9651163]
kinase insert domain receptor in Mouse [GtoPdb: 1813] [UniProtKB: P35918]
GtoPdb - - 7.15 pIC50 70 nM IC50 J Med Chem (1998) 41: 2588-603 [PMID:9651163]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]