tivozanib [Ligand Id: 6058] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1289494 (ASP-4130, KIL8951, Kil-8951, Fotivda, Krn-951, KRN-951, AV-951, Tivozanib)
  • EPH receptor B2/Ephrin type-B receptor 2 in Human [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
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  • platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234]
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  • fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
EPH receptor B2/Ephrin type-B receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3290] [GtoPdb: 1831] [UniProtKB: P29323]
ChEMBL Inhibition of recombinant EphB2 (unknown origin) by cell-free assay B 7.76 pIC50 17.5 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2425-2428 [PMID:25908516]
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 recombinant PDGFRalpha (unknown origin) by cell-free assay B 8.65 pIC50 2.26 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2425-2428 [PMID:25908516]
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 recombinant VEGFR1 (unknown origin) by cell-free assay B 8.2 pIC50 6.26 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2425-2428 [PMID:25908516]
ChEMBL Inhibition of VEGFR1 B 9.68 pIC50 0.21 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
GtoPdb - - 9.68 pIC50 0.21 nM IC50 J Med Chem (2012) 55: 10797-822 [PMID:23098265]
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 6.47 pIC50 340 nM IC50 Eur. J. Med. Chem. (2014) 76: 193-244 [PMID:24583357]
ChEMBL Inhibition of recombinant VEGFR2 (unknown origin) by cell-free assay B 8.67 pIC50 2.14 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2425-2428 [PMID:25908516]
ChEMBL Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay B 9.8 pIC50 0.16 nM IC50 Eur. J. Med. Chem. (2010) 45: 5420-5427 [PMID:20869793]
ChEMBL Inhibition of VEGFR2 B 9.8 pIC50 0.16 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
GtoPdb - - 9.8 pIC50 0.16 nM IC50 J Med Chem (2012) 55: 10797-822 [PMID:23098265]
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 recombinant VEGFR3 (unknown origin) by cell-free assay B 8.51 pIC50 3.11 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2425-2428 [PMID:25908516]
ChEMBL Inhibition of VEGFR3 B 9.62 pIC50 0.24 nM IC50 J. Med. Chem. (2012) 55: 10797-10822 [PMID:23098265]
GtoPdb - - 9.62 pIC50 0.24 nM IC50 J Med Chem (2012) 55: 10797-822 [PMID:23098265]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]