BDBM50021574 BMS-907351::CABOZANTINIB::CHEBI:72317::Cabometyx::Cometriq::US10183928, Cabozantinib::US10202365, Compound Cabozantinib::US10227329, Compound Cabozantinib::US10273211, Compound Cabozantinib::US10464902, Cabozantinib::US10774070, Compound Cabozantinib::US11279688, Compound Cabozantinib::XL-184::cabozantinib s-malate
SMILES COc1cc2nccc(Oc3ccc(NC(=O)C4(CC4)C(=O)Nc4ccc(F)cc4)cc3)c2cc1OC
InChI Key InChIKey=ONIQOQHATWINJY-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 157 hits for monomerid = 50021574
Affinity DataKi: 0.0350nMAssay Description:Compounds 2-4 and cabozantinib were each tested for binding of c-Met, VEGFR2, TIE2 and the control compound, staurosporine. Specifically, each compou...More data for this Ligand-Target Pair
Affinity DataKd: 2.80E+3nMAssay Description:Briefly, 5 mg of a protein mixture of the four cell lines or a single cell line were incubated with compound dilution series in DMSO (3 nM, 10 nM, 30...More data for this Ligand-Target Pair
Affinity DataIC50: 9.90nMpH: 7.4 T: 2°CAssay Description:Briefly, 20 μg/mL poly (Glu,Tyr) 4:1 (Sigma) was pre-coated in 96-well plates as a substrate. A 50 μL aliquot of 10 μmol/L ATP solutio...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMpH: 7.4 T: 2°CAssay Description:Briefly, 20 μg/mL poly (Glu,Tyr) 4:1 (Sigma) was pre-coated in 96-well plates as a substrate. A 50 μL aliquot of 10 μmol/L ATP solutio...More data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Inhibition of c-Met (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant MET kinase domain (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 7nMAssay Description:Inhibition of recombinant VEGFR2 kinase domain (unknown origin)More data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of c-Kit (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 16nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.70nMAssay Description:Inhibition of purified recombinant c-MET (unknown origin) using poly (Glu, Tyr) substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 18nMAssay Description:Inhibition of human Ret M918T mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 230nMAssay Description:Inhibition of human Ret V804L mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 358nMAssay Description:Inhibition of human Ret V804M mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibition of human Ret S891A mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Inhibition of human Ret G691S mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of human Ret Y791F mutant by radiometric assay in presence of [gamma-33P]-ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0350nMAssay Description:Inhibition of human VEGFR-2 using poly(Glu, Tyr) as substrate by AlphaScreen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human c-Met using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 5.20nMAssay Description:Inhibition of human RET using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assayMore data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 4.60nMAssay Description:Inhibition of human KIT using poly(Glu, Tyr) as substrate by AlphaScreen assayMore data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Inhibition of human TIE2 using poly(Glu, Tyr) as substrate by [33P]-phosphoryl transfer assayMore data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of human FLT3 using poly(Glu, Tyr) as substrate by Luciferase-Coupled Chemiluminescence assayMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of human AXL using poly(Glu, Tyr) as substrateMore data for this Ligand-Target Pair
Affinity DataIC50: 1.90E+3nMAssay Description:Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 7.80E+3nMAssay Description:Inhibition of VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrsMore data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 7.50E+3nMAssay Description:Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrsMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrsMore data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 4.20E+4nMAssay Description:Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrsMore data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 650nMAssay Description:Inhibition of human RET cytoplasmic domain (658 to 1114 residues) expressed in baculovirus system preincubated for 15 mins followed by substrate addi...More data for this Ligand-Target Pair
TargetKinesin-1 heavy chain/Proto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
University Of Manchester
Curated by ChEMBL
University Of Manchester
Curated by ChEMBL
Affinity DataIC50: 190nMAssay Description:Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based ...More data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description: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 lumine...More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of full length recombinant human GST or His-tagged c-Met using poly (Glu, Tyr) as substrate by luciferase coupled chemiluminescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0350nMAssay Description:Inhibition of full length recombinant human GST or His-tagged VEGFR2 using poly (Glu, Tyr) as substrate by AlphaScreen assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.20nMAssay Description:Inhibition of recombinant c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant VEGFR2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 3nMAssay Description: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...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 811nMAssay Description: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 substr...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 1(Homo sapiens (Human))
St. John'S University
Curated by ChEMBL
St. John'S University
Curated by ChEMBL
Affinity DataIC50: 12nMAssay Description:Inhibition of FLT1 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 7nMAssay Description:Inhibition of AXL (unknown origin)More data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 6nMAssay Description:Inhibition of FLT3 (unknown origin)More data for this Ligand-Target Pair
TargetFibroblast growth factor receptor 1(Homo sapiens (Human))
St. John'S University
Curated by ChEMBL
St. John'S University
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of FLT2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of MET (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.0350nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 4nMAssay Description:Inhibition of RET (unknown origin)More data for this Ligand-Target Pair
TargetAngiopoietin-1 receptor(Homo sapiens (Human))
Shenyang Pharmaceutical University
Curated by ChEMBL
Shenyang Pharmaceutical University
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Inhibition of TIE-2 (unknown origin)More data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 4.60nMAssay Description:Inhibition of KIT (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Central China Normal University
Curated by ChEMBL
Central China Normal University
Curated by ChEMBL
Affinity DataIC50: 46nMAssay Description:A compound described herein can be tested in vitro for inhibition of wild-type RET and various mutant RET kinases, including e.g., RET V804L, RET V80...More data for this Ligand-Target Pair