compound 8i [PMID: 22765894] [Ligand Id: 9905] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2087167
  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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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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  • 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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  • fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
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  • fms related receptor tyrosine kinase 4 in Human [GtoPdb: 1814] [UniProtKB: P35916]
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  • MET proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1815] [UniProtKB: P08581]
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  • macrophage stimulating 1 receptor in Human [GtoPdb: 1816] [UniProtKB: Q04912]
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  • AXL receptor tyrosine kinase in Human [GtoPdb: 1835] [UniProtKB: P30530]
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  • TEK receptor tyrosine kinase in Human [GtoPdb: 1842] [UniProtKB: Q02763]
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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 in human SK-N-MC cells assessed as inhibition of FGF-induced ERK phosphorylation incubated for 1 hr prior to VEGF-stimulation measured after 30 mins by ELISA B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
GtoPdb - - 8.21 pIC50 6.2 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
ChEMBL Inhibition of N-terminal GST-tagged FGFR1 using poly(Glu,Tyr) as substrate after 30 mins by alphascreen assay B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
GtoPdb - - 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894]
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 N-terminal GST-tagged PDGFRalpha after 2 hrs by luciferase-luciferin coupled chemiluminescence assay B 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
GtoPdb - - 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894]
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 - - 7.54 pIC50 29 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
ChEMBL Inhibition of N-terminal GST-tagged Flt1 using poly(Glu,Tyr) as substrate after 60 mins by alphascreen assay B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
GtoPdb - - 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894]
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 KDR in human HUVEC cells assessed as inhibition of VEGF-induced ERK phosphorylation incubated for 1 hr prior to VEGF-stimulation measured after 5 mins by ELISA B 8.22 pIC50 6 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
ChEMBL Inhibition of N-terminal GST-tagged KDR after 4 hrs by luciferase-luciferin coupled chemiluminescence assay B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4979-4985 [PMID:22765894]
GtoPdb - - 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2012) 22: 4979-85 [PMID:22765894]
GtoPdb - - 8.59 pIC50 2.6 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
platelet derived growth factor receptor beta in Human [GtoPdb: 1804] [UniProtKB: P09619]
GtoPdb - - 8.82 pIC50 1.5 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
GtoPdb - - 7.86 pIC50 13.8 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb - - 9.1 pIC50 0.8 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
fms related receptor tyrosine kinase 4 in Human [GtoPdb: 1814] [UniProtKB: P35916]
GtoPdb - - 8.52 pIC50 3 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
MET proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1815] [UniProtKB: P08581]
GtoPdb - - 6.33 pIC50 463 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
macrophage stimulating 1 receptor in Human [GtoPdb: 1816] [UniProtKB: Q04912]
GtoPdb - - 6.91 pIC50 124 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
AXL receptor tyrosine kinase in Human [GtoPdb: 1835] [UniProtKB: P30530]
GtoPdb - - 8.34 pIC50 4.6 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]
TEK receptor tyrosine kinase in Human [GtoPdb: 1842] [UniProtKB: Q02763]
GtoPdb - - 6.57 pIC50 270 nM IC50 Cancer Res (2011) 71: 4758-68 [PMID:21613405]

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]