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

Data  8 KI  25 IC50  445 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 478 hits for monomerid = 25117   

TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Ontogenesis

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails US Patent
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi:  4.20nMAssay Description:Inhibition of PLK-4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi:  4.20nMAssay Description:Inhibition of PLK4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi:  4.20nMAssay Description:Inhibition of human PLK4More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK2(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi: >2.00E+4nM ΔG°: >-6.34kcal/molepH: 7.5 T: 2°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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKi: >2.00E+4nM ΔG°: >-6.34kcal/molepH: 7.5 T: 2°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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK3(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK3(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK3 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK2(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK2 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK1(Homo sapiens (Human))
Abbott Laboratories

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PLK1 (unknown origin) by FRET-based homogeneous assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase PLK4(Homo sapiens (Human))
Zhengzhou University

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase TBK1(Homo sapiens (Human))
Technical University Of Dortmund

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails ArticlePubMed
TargetFerrochelatase, mitochondrial [R115L](Homo sapiens (Human))
Technical University Of Munich

LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails US Patent
TargetTyrosine-protein kinase ABL1 [T315I](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails US Patent
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails US Patent
TargetTyrosine-protein kinase ABL1 [T315I](Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
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
In DepthDetails US Patent
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047L) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetInsulin receptor(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for INSR kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargeteIF-2-alpha kinase GCN2(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GCN2(Kin.Dom.2,S808G) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  31nMAssay Description:Binding constant for FLT3(K663Q) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  2.60E+3nMAssay Description:Binding constant for ABL1(F317I)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  36nMAssay Description:Binding constant for ABL1(M351T)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMisshapen-like kinase 1(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  560nMAssay Description:Binding constant for MINK kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(H1047Y) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  20nMAssay Description:Binding constant for ABL1(H396P)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase MRCK gamma(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DMPK2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMAP/microtubule affinity-regulating kinase 3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MARK3 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  290nMAssay Description:Binding constant for ABL1(Q252H)-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  330nMAssay Description:Binding constant for FLT3(D835H) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetFibroblast growth factor receptor 3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  210nMAssay Description:Binding constant for FGFR3(G697C) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  2.40E+3nMAssay Description:Binding constant for FLT3(R834Q) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  230nMAssay Description:Binding constant for ABL1(Y253F)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetLeucine-rich repeat serine/threonine-protein kinase 2(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  990nMAssay Description:Binding constant for LRRK2(G2019S) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Pfizer

US Patent
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  84nMAssay Description:Binding constant for ABL1-nonphosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  270nMAssay Description:Binding constant for FLT3(D835Y) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(I800L) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCalcium/calmodulin-dependent protein kinase type II subunit beta(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for CAMK2B kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(Q546K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMyosin-IIIb(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for MYO3B kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  1.10E+3nMAssay Description:Binding constant for MET(M1250T) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd:  1.80E+3nMAssay Description:Binding constant for KIT(A829P) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase 17A(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DRAK1 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase BRSK1(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM25117(AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyri...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for BRSK1 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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