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ChEMBL ligand: CHEMBL2105717 (Cabozantinib, XL-184 FREE BASE, XL184, BMS-907351, BMS-907351 FREE BASE, Cabometyx, XL-184, Cometriq) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, 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]