cabozantinib [Ligand Id: 5887] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2105717 (Cabozantinib, XL-184 FREE BASE, XL184, BMS-907351, BMS-907351 FREE BASE, Cabometyx, XL-184, Cometriq)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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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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  • macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
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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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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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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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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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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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  • TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
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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
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 5.51 pIC50 3110 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of EGFR (unknown origin) by HTRF method B 6.65 pIC50 225 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of c-MET (unknown origin) using FAM-labelled peptide as substrate measured after 10 mins by mobility shift assay B 7.72 pIC50 19 nM IC50 Bioorg Med Chem (2019) 27: 2127-2139 [PMID:30940564]
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 FLT2 (unknown origin) B 7.95 pIC50 11.3 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
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 c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs B 5.72 pIC50 1900 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of human recombinant His-tagged cMET expressed in baculovirus expression system reduction in phosphorylation using tyrosine 6 peptide as substrate after 60 mins FRET based Z'-LYTE assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2019) 29: 1565-1571 [PMID:31078412]
ChEMBL Inhibition of c-Met (unknown origin) B 7.68 pIC50 21 nM IC50 Eur. J. Med. Chem. (2014) 83: 581-593 [PMID:24996144]
ChEMBL Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay B 7.7 pIC50 19.86 nM IC50 Eur J Med Chem (2018) 158: 814-831 [PMID:30248654]
ChEMBL Inhibition of c-Met (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of recombinant MET kinase domain (unknown origin) B 8.1 pIC50 8 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3351-3355 [PMID:24951334]
ChEMBL Inhibition of recombinant c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA B 8.14 pIC50 7.2 nM IC50 Bioorg Med Chem (2017) 25: 6674-6679 [PMID:29146452]
ChEMBL Inhibition of purified recombinant c-MET (unknown origin) using poly (Glu, Tyr) substrate after 60 mins by ELISA B 8.43 pIC50 3.7 nM IC50 Bioorg. Med. Chem. (2015) 23: 564-578 [PMID:25537530]
ChEMBL Inhibition of c-MET (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA B 8.44 pIC50 3.6 nM IC50 Eur J Med Chem (2018) 158: 814-831 [PMID:30248654]
ChEMBL Inhibition of recombinant c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate incubated for 60 mins by ELISA B 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. (2016) 24: 3353-3358 [PMID:27068889]
ChEMBL Inhibition of recombinant c-MET (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 45 mins by ELISA B 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of recombinant human full length c-MET using poly (Glu, Tyr) as substrate by alpha screen assay B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of full length recombinant human GST or His-tagged c-Met using poly (Glu, Tyr) as substrate by luciferase coupled chemiluminescence assay B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. (2016) 24: 3353-3358 [PMID:27068889]
ChEMBL Inhibition of MET (unknown origin) B 8.89 pIC50 1.3 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of c-MET (unknown origin) B 8.89 pIC50 1.3 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of human c-Met using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assay B 8.89 pIC50 1.3 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of c-MET (unknown origin) B 8.89 pIC50 1.3 nM IC50 Eur J Med Chem (2018) 158: 814-831 [PMID:30248654]
GtoPdb - - 8.9 pIC50 1.3 nM IC50 Mol Cancer Ther (2011) 10: 2298-308 [PMID:21926191]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of IGF1R (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
macrophage stimulating 1 receptor/Macrophage-stimulating protein receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2689] [GtoPdb: 1816] [UniProtKB: Q04912]
ChEMBL Inhibition of Ron (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 7.16 pIC50 69 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
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 PDGFRalpha (unknown origin) by HTRF method B 5 pIC50 >10000 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Further kinetic evaluation of compounds supplied by Sanofi against AuroraA within a BIAcore3000 instrument B 5.47 pKd 3363.13 nM Kd K4DD drug target binding kinetics data
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 KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs B 4.38 pIC50 42000 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of c-Kit (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 7.28 pIC50 53 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of KIT (unknown origin) by HTRF method B 8.18 pIC50 6.6 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of KIT (unknown origin) B 8.34 pIC50 4.6 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of human KIT using poly(Glu, Tyr) as substrate by AlphaScreen assay B 8.34 pIC50 4.6 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of recombinant human full length KIT using poly (Glu, Tyr) as substrate by alpha screen assay B 8.34 pIC50 4.6 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of c-Kit (unknown origin) B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3351-3355 [PMID:24951334]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs B 5.12 pIC50 7500 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of FLT3 (unknown origin) using peptide as substrate preincubated with enzyme for 10 mins followed by substrate addition further incubated for 1 hr by mobility shift assay B 6.38 pIC50 418 nM IC50 Bioorg Med Chem Lett (2019) 29: 126630-126630 [PMID:31466809]
ChEMBL Inhibition of FLT3 (unknown origin) by HTRF method B 7.6 pIC50 25 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of human FLT3 using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assay B 7.95 pIC50 11.3 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of recombinant human full length FLT3 using poly (Glu, Tyr) as substrate by alpha screen assay B 7.95 pIC50 11.3 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of FLT3 (unknown origin) B 8.22 pIC50 6 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of recombinant N-Terminal GST-tagged human RET V804M mutant (658 to end residues) incubated for 15 mins followed by substrate addition and measured after 30 mins by TR-FRET assay B 5.82 pIC50 1500 nM IC50 ACS Med Chem Lett (2020) 11: 497-505 [PMID:32292556]
ChEMBL Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA B 6.09 pIC50 811 nM IC50 Eur. J. Med. Chem. (2016) 118: 244-249 [PMID:27131066]
ChEMBL Inhibition of human RET cytoplasmic domain (658 to 1114 residues) expressed in baculovirus system preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay B 6.19 pIC50 650 nM IC50 Eur. J. Med. Chem. (2016) 112: 20-32 [PMID:26874741]
ChEMBL Inhibition of human Ret V804M mutant by radiometric assay in presence of [gamma-33P]-ATP B 6.45 pIC50 358 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
ChEMBL Inhibition of human Ret V804L mutant by radiometric assay in presence of [gamma-33P]-ATP B 6.64 pIC50 230 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
ChEMBL Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay B 6.74 pIC50 180 nM IC50 ACS Med Chem Lett (2020) 11: 497-505 [PMID:32292556]
ChEMBL Inhibition of RET (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 7.43 pIC50 37 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of human Ret M918T mutant by radiometric assay in presence of [gamma-33P]-ATP B 7.74 pIC50 18 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
ChEMBL Inhibition of RET (unknown origin) B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3351-3355 [PMID:24951334]
ChEMBL Inhibition of human Ret G691S mutant by radiometric assay in presence of [gamma-33P]-ATP B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
GtoPdb In a biochemical assay. - 7.96 pIC50 11 nM IC50 Cancer Discov (2018) 8: 836-849 [PMID:29657135]
ChEMBL Inhibition of RET (unknown origin) by HTRF method B 8 pIC50 10.1 nM IC50 Bioorg Med Chem (2017) 25: 3195-3205 [PMID:28412159]
ChEMBL Inhibition of human Ret Y791F mutant by radiometric assay in presence of [gamma-33P]-ATP B 8.15 pIC50 7 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
ChEMBL Inhibition of recombinant human full length RET using poly (Glu, Tyr) as substrate by alpha screen assay B 8.28 pIC50 5.2 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of human RET using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assay B 8.28 pIC50 5.2 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of human Ret S891A mutant by radiometric assay in presence of [gamma-33P]-ATP B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2016) 59: 358-373 [PMID:26652860]
ChEMBL Inhibition of RET (unknown origin) B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2015) 58: 3672-3681 [PMID:25625428]
ChEMBL Inhibition of RET (unknown origin) B 8.4 pIC50 4 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA B 8.52 pIC50 3 nM IC50 Eur. J. Med. Chem. (2016) 118: 244-249 [PMID:27131066]
ChEMBL Inhibition of Ret (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA B 8.62 pIC50 2.4 nM IC50 Eur J Med Chem (2017) 135: 370-381 [PMID:28460311]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs B 5.3 pIC50 5000 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of AXL (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 8.02 pIC50 9.5 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of human AXL using poly(Glu, Tyr) as substrate B 8.15 pIC50 7 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of AXL (unknown origin) B 8.15 pIC50 7 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of recombinant human full length AXL using poly (Glu, Tyr) as substrate by alpha screen assay B 8.15 pIC50 7 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of AXL (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA B 8.47 pIC50 3.4 nM IC50 Eur J Med Chem (2017) 135: 370-381 [PMID:28460311]
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 Src (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 6.75 pIC50 178 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763]
ChEMBL Inhibition of human TIE2 using poly(Glu, Tyr) as substrate by [33P]-phosphoryl transfer assay B 7.84 pIC50 14.3 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of TIE-2 (unknown origin) B 7.84 pIC50 14.3 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of recombinant human full length TIE2 using poly (Glu, Tyr) as substrate by alpha screen assay B 7.84 pIC50 14.3 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
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 FLT1 (unknown origin) B 7.92 pIC50 12 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
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 VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrs B 5.11 pIC50 7800 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay B 7.8 pIC50 16 nM IC50 Eur. J. Med. Chem. (2016) 112: 20-32 [PMID:26874741]
ChEMBL Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay B 7.85 pIC50 14 nM IC50 Eur. J. Med. Chem. (2016) 112: 20-32 [PMID:26874741]
ChEMBL Inhibition of recombinant VEGFR2 kinase domain (unknown origin) B 8.15 pIC50 7 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3351-3355 [PMID:24951334]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 8.15 pIC50 7 nM IC50 Eur. J. Med. Chem. (2014) 83: 581-593 [PMID:24996144]
ChEMBL Inhibition of recombinant VEGFR2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA B 8.4 pIC50 4 nM IC50 Bioorg Med Chem (2017) 25: 6674-6679 [PMID:29146452]
ChEMBL Inhibition of VEGFR2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA B 8.48 pIC50 3.3 nM IC50 Eur J Med Chem (2018) 158: 814-831 [PMID:30248654]
ChEMBL Inhibition of recombinant VEGFR2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate incubated for 60 mins by ELISA B 8.52 pIC50 3 nM IC50 Bioorg. Med. Chem. (2016) 24: 3353-3358 [PMID:27068889]
ChEMBL Inhibition of KDR (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA B 9.32 pIC50 0.48 nM IC50 Eur J Med Chem (2018) 146: 368-380 [PMID:29407963]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 10.46 pIC50 0.04 nM IC50 Eur J Med Chem (2019) 179: 916-935 [PMID:31306818]
ChEMBL Inhibition of human VEGFR-2 using poly(Glu, Tyr) as substrate by AlphaScreen assay B 10.46 pIC50 0.04 nM IC50 Eur. J. Med. Chem. (2016) 108: 495-504 [PMID:26717201]
ChEMBL Inhibition of full length recombinant human GST or His-tagged VEGFR2 using poly (Glu, Tyr) as substrate by AlphaScreen assay B 10.46 pIC50 0.04 nM IC50 Bioorg. Med. Chem. (2016) 24: 3353-3358 [PMID:27068889]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 10.46 pIC50 0.04 nM IC50 J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL Inhibition of VEGFR2 phosphorylation (unknown origin) B 10.46 pIC50 0.04 nM IC50 Bioorg Med Chem Lett (2017) 27: 3231-3237 [PMID:28651979]
ChEMBL Inhibition of recombinant human full length VEGFR2 using poly (Glu, Tyr) as substrate by alpha screen assay B 10.46 pIC50 0.04 nM IC50 Eur J Med Chem (2017) 138: 942-951 [PMID:28755635]
ChEMBL Inhibition of VEGFR2 (unknown origin) B 10.46 pIC50 0.04 nM IC50 Eur J Med Chem (2018) 158: 814-831 [PMID:30248654]
GtoPdb - - 10.46 pIC50 0.04 nM IC50 Mol Cancer Ther (2011) 10: 2298-308 [PMID:21926191]
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 8.22 pIC50 6 nM IC50 Eur J Med Chem (2019) 179: 916-935 [PMID:31306818]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]