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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]