VEGF receptor tyrosine kinase inhibitor II [Ligand Id: 6056] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL101683
  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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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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  • MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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  • KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of Cyclin-dependent kinase 1 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of Epidermal growth factor receptor B 5.14 pIC50 7300 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581]
ChEMBL Inhibition of Met proto-oncogene tyrosine kinase B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of Insulin-like growth factor I receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
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 Proto-oncogene tyrosine-protein kinase Kit B 6.62 pIC50 240 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibition of c-Src tyrosine kinase B 5.15 pIC50 7000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
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 vascular endothelial growth factor receptor 1 B 6.74 pIC50 180 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
GtoPdb - - 7.82 pKi 15 nM Ki Bioorg Med Chem Lett (2007) 17: 6003-8 [PMID:17869515]
ChEMBL Inhibition of phosphorylated-Kdr after 30 mins B 7.82 pKi 15 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 6003-6008 [PMID:17869515]
ChEMBL Inhibition of Vascular endothelial growth factor receptor 2 B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 2967-2971 [PMID:12941313]
ChEMBL Inhibition of KDR by ELISA B 7.7 pIC50 20 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2939-2943 [PMID:18420406]

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]