lucitanib [Ligand Id: 7649] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2220486 (S 80881, CO-3810, E-3810, Al-3810, Lucitanib, S-80881, AL-3810)
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • fibroblast growth factor receptor 2/Fibroblast growth factor receptor 2 in Human [ChEMBL: CHEMBL4142] [GtoPdb: 1809] [UniProtKB: P21802]
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  • fibroblast growth factor receptor 3/Fibroblast growth factor receptor 3 in Human [ChEMBL: CHEMBL2742] [GtoPdb: 1810] [UniProtKB: P22607]
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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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  • platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
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  • platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
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  • KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
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  • ret proto-oncogene in Human [GtoPdb: 2185] [UniProtKB: P07949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 7.76 pIC50 17.5 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of FGFR1 (unknown origin) B 7.76 pIC50 17.5 nM IC50 Eur J Med Chem (2018) 154: 9-28 [PMID:29775937]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
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 7.08 pIC50 82.5 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of FGFR2 (unknown origin) B 7.08 pIC50 82.5 nM IC50 Eur J Med Chem (2018) 154: 9-28 [PMID:29775937]
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 6.62 pIC50 237.5 nM IC50 Eur J Med Chem (2018) 154: 9-28 [PMID:29775937]
fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948]
GtoPdb - - 7.92 pIC50 12 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
ChEMBL Inhibition of VEGFR1 (unknown origin) B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of VEGFR1 (unknown origin) B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2018) 154: 9-28 [PMID:29775937]
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 7.6 pIC50 25 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2018) 154: 9-28 [PMID:29775937]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
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 8 pIC50 10 nM IC50 Eur J Med Chem (2017) 126: 476-490 [PMID:27914362]
platelet derived growth factor receptor alpha in Human [GtoPdb: 1803] [UniProtKB: P16234]
GtoPdb - - 7.89 pIC50 13 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb - - 8.1 pIC50 8 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
GtoPdb - - 6.28 pIC50 527 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]
ret proto-oncogene in Human [GtoPdb: 2185] [UniProtKB: P07949]
GtoPdb - - 6.7 pIC50 200 nM IC50 J Cell Mol Med (2012) 16: 2321-30 [PMID:22304225]

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]