BDBM25117 AG-013736::AXITINIB::N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide::US10464902, Axitinib::US9205078, Axitinib ::US9617222, Compound A
SMILES CNC(=O)c1ccccc1Sc1ccc2c(\C=C\c3ccccn3)n[nH]c2c1
InChI Key InChIKey=RITAVMQDGBJQJZ-FMIVXFBMSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 478 hits for monomerid = 25117
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
3D Structure (crystal)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 PLK4 (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 DataKi: >2.00E+4nM ΔG°: >-6.34kcal/molepH: 7.5 T: 22°CAssay 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 DataKi: >2.00E+4nM ΔG°: >-6.34kcal/molepH: 7.5 T: 22°CAssay 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 DataKi: >2.00E+4nMAssay 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: >1.00E+4nMAssay Description:Inhibition of PLK3 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK2 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK1 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
Affinity DataIC50: 46nMAssay Description:Inhibition of N-terminal GST-tagged human PLK4 (1 to 391 amino acids) expressed in Escherichia coli using TMB as substrate after 30 mins by indirect ...More data for this Ligand-Target Pair
Affinity DataIC50: 470nMAssay Description:IC50 determinations for TBK1 were performed with the KinEASE-STK assay from Cisbio according to the manufacturer's instructions. A biotinylated s...More data for this Ligand-Target Pair
Affinity DataKd: 3.10E+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: 7.78nMpH: 7.5 T: 25°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 DataIC50: 0.551nMpH: 7.5 T: 25°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 DataIC50: 2.60nMpH: 7.5 T: 25°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 DataIC50: 0.418nMpH: 7.5 T: 25°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
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for INSR kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GCN2(Kin.Dom.2,S808G) 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: 2.60E+3nMAssay Description:Binding constant for ABL1(F317I)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) 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: 560nMAssay Description:Binding constant for MINK kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 20nMAssay Description:Binding constant for ABL1(H396P)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DMPK2 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MARK3 kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 290nMAssay Description:Binding constant for ABL1(Q252H)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 330nMAssay Description:Binding constant for FLT3(D835H) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 210nMAssay Description:Binding constant for FGFR3(G697C) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.40E+3nMAssay Description:Binding constant for FLT3(R834Q) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 230nMAssay Description:Binding constant for ABL1(Y253F)-phosphorylated kinase domainMore data for this Ligand-Target Pair
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: 990nMAssay Description:Binding constant for LRRK2(G2019S) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 84nMAssay Description:Binding constant for ABL1-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 270nMAssay Description:Binding constant for FLT3(D835Y) kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
TargetCalcium/calmodulin-dependent protein kinase type II subunit beta(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CAMK2B kinase domainMore data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Human)
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MYO3B kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 1.10E+3nMAssay Description:Binding constant for MET(M1250T) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 1.80E+3nMAssay Description:Binding constant for KIT(A829P) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DRAK1 kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for BRSK1 kinase domainMore data for this Ligand-Target Pair