BDBM25117 AG-013736::AXITINIB::N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide::US10464902, Axitinib::US20250129067, Compound Axitinib::US9205078, Axitinib ::US9617222, Compound A
SMILES CNC(=O)c1ccccc1Sc2ccc3c(c2)[nH]nc3/C=C/c4ccccn4
InChI Key InChIKey=RITAVMQDGBJQJZ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 489 hits for monomerid = 25117
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.0200nMAssay Description:Inhibition of VEGFR-2 (unknown origin) expressed in PAE cells assessed as reduction in VEGFA induced protein phosphorylation preincubated for 1 hr fo...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Human)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of VEGFR3 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.100nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Human)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of VEGFR3 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.180nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataKi: 0.200nMAssay 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
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of human VEGFR2More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using A...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.25nMAssay Description:Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.418nMpH: 7.5 T: 2°CAssay Description:Axitinib was tested using a Z′-LYTE Screening Protocol (Invitrogen, Carlsbad, Calif.). Axitinib was prepared in 100% DMSO, and added to the rea...More data for this Ligand-Target Pair
Affinity DataKd: 0.490nMAssay Description:Binding constant for KIT(V559D) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 0.510nMAssay Description:Binding constant for PDGFRA kinase domainMore data for this Ligand-Target Pair
Affinity DataIC50: 0.551nMpH: 7.5 T: 2°CAssay Description:Axitinib was tested with the Caliper LabChip3000 assay (Caliper Life Science, Hopkinton, Mass.), which is a mobility-shift assay (MSA) that combines ...More data for this Ligand-Target Pair
Affinity DataKd: 0.570nMAssay Description:Binding constant for PDGFRB kinase domainMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 0.910nMAssay Description:Measurement of the kinase inhibitory activity of each compound produced in Examples was conducted using the Off-chip Mobility Shift Assay. For this t...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells asses...More data for this Ligand-Target Pair
Affinity DataKd: 1.30nMAssay Description:Binding constant for AURKC kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 1.40nMAssay Description:Binding constant for KIT(V559D,T670I) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 1.5nMAssay Description:Binding constant for ABL1(T315I)-phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60nMAssay Description:Inhibition of PDGFRbeta (unknown origin) expressed in PAE cells assessed as reduction in PDGF-BB induced protein phosphorylation preincubated for 1 h...More data for this Ligand-Target Pair
Affinity DataKd: 1.70nMAssay Description:Binding constant for KIT(L576P) kinase domainMore data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of KIT (unknown origin) expressed in PAE cells assessed as reduction in SCF induced protein phosphorylation preincubated for 1 hr followed...More data for this Ligand-Target Pair
Affinity DataIC50: 2.60nMpH: 7.5 T: 2°CAssay Description:Axitinib was tested using a Z′-LYTE Screening Protocol (Invitrogen, Carlsbad, Calif.). Axitinib was prepared in 100% DMSO, and added to the rea...More data for this Ligand-Target Pair
Affinity DataKd: 3.20nMAssay Description:Binding constant for KIT kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.5nMAssay Description:Binding constant for KIT(V559D,V654A) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.60nMAssay Description:Binding constant for ABL1(T315I)-non phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.70nMAssay Description:Binding affinity to c-KIT (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 4.20nMAssay Description:Inhibition of PLK-4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 4.20nMAssay Description:Inhibition of human PLK4More data for this Ligand-Target Pair
Affinity DataKi: 4.20nMAssay Description:Kinase was assayed in 384-well polypropylene plate format. The compound was mixed with kinase and biotinylated peptide substrate and incubated. After...More data for this Ligand-Target Pair
Affinity DataIC50: 4.20nMAssay Description:Inhibition of PLK4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 4.20nMAssay Description:Inhibition of PLK4 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 3(Human)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibition of VEGFR3 (unknown origin)More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:Inhibition of VEGFR2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of VEGFR1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of c-Kit (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 5.80nMAssay Description:Binding constant for FLT1 kinase domainMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
Southwest Jiaotong University
Curated by ChEMBL
Southwest Jiaotong University
Curated by ChEMBL
Affinity DataKd: 5.90nMAssay Description:Binding constant for VEGFR2 kinase domainMore data for this Ligand-Target Pair
Affinity DataIC50: 7.78nMpH: 7.5 T: 2°CAssay Description:Axitinib was tested with the Caliper LabChip3000 assay (Caliper Life Science, Hopkinton, Mass.), which is a mobility-shift assay (MSA) that combines ...More data for this Ligand-Target Pair
Affinity DataKd: 11nMAssay Description:Binding constant for AURKB kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 13nMAssay Description:Binding affinity to c-KIT V559D/T670I double mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 16nMAssay Description:Binding constant for PLK4 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 20nMAssay Description:Binding constant for ABL1(H396P)-non phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 21nMAssay Description:Binding constant for CSF1R kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 23nMAssay Description:Binding constant for ABL1(H396P)-phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 31nMAssay Description:Binding constant for FLT3(K663Q) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 36nMAssay Description:Binding constant for ABL1(M351T)-phosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 36nMAssay Description:Binding constant for ABL1-phosphorylated kinase domainMore data for this Ligand-Target Pair

3D Structure (crystal)