BDBM50322535 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide::3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide::CHEMBL1171837::PONATINIB::US10464902, Ponatinib::US9255107, AP24534
SMILES Cc1ccc(cc1C#Cc2cnc3n2nccc3)C(=O)Nc4ccc(c(c4)C(F)(F)F)CN5CCN(CC5)C
InChI Key InChIKey=PHXJVRSECIGDHY-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 144 hits for monomerid = 50322535
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of FLT3-ITD mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hr...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of FLT3-ITD F691I mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Oribase Pharma
Curated by ChEMBL
Oribase Pharma
Curated by ChEMBL
Affinity DataEC50: 0.0500nMAssay Description:Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.110nMAssay Description:Binding affinity to human HCK using KVEKIGEGTYGVVYK as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.160nMAssay Description:Binding affinity to LYN (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.240nMAssay Description:Inhibition of recombinant human Lyn using peptide substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.280nMAssay Description:Binding affinity to human LCK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of FLT3 (unknown origin) by kinase hotspot assayMore data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Oribase Pharma
Curated by ChEMBL
Oribase Pharma
Curated by ChEMBL
Affinity DataEC50: 0.300nMAssay Description:Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Chinese Academy of Sciences
Curated by ChEMBL
Chinese Academy of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of recombinant RET (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL Q252H mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL Y253F mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL M351T mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL H396P mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.310nMAssay Description:Inhibition of human ABL1 assessed as residual activity using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMAssay Description:Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.360nMAssay Description:Binding affinity to human FYN using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Binding affinity to human ABL1 using EAIYAAPFAKKK as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of recombinant wild type Abl (unknown origin) in presence of [33P]-ATP by radiometric hotspot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of ABL (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of wild type human ABL using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of ABL autophosphorylationMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of Abl (unknown origin) in presence of ATP by ADP Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of recombinant human ABL using peptide substrate EAIYAAPFAKKK in presence of [33-P]ATP by kinase hotspot assayMore data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Oribase Pharma
Curated by ChEMBL
Oribase Pharma
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of BCR-ABL (unknown origin) by kinase hotspot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.580nMAssay Description:Inhibition of breakpoint cluster region-Abelson tyrosine kinase T315I mutant (unknown origin) using [gamma-33P]ATP as substrate by radiometric kinase...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of FGFR1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.700nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against a panel...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of FGFR-1 (unknown origin)More data for this Ligand-Target Pair
Affinity DataKd: 0.700nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against phospho...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of human FGFR1More data for this Ligand-Target Pair
Affinity DataIC50: 0.890nMAssay Description:Binding affinity to human YES using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Chicken)
Technical University of Dortmund
Curated by ChEMBL
Technical University of Dortmund
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of chicken wild-type cSRC (251 to 533)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) prein...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Oribase Pharma
Curated by ChEMBL
Oribase Pharma
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of Bcr-Abl T315I mutant (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Chinese Academy of Sciences
Curated by ChEMBL
Chinese Academy of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of RET (unknown origin) using poly[Glu:Tyr] (4:1) as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMT: 2°CAssay Description:Serially diluting the compound of the present invention from 1 uM initial concentration in three-fold fashion and formulating 10 concentrations (50.8...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Oribase Pharma
Curated by ChEMBL
Oribase Pharma
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assayMore data for this Ligand-Target Pair
TargetReceptor-interacting serine/threonine-protein kinase 2(Human)
Fudan University
Curated by ChEMBL
Fudan University
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant human His-tagged RIPK2 (8 to 317 residues) incubated for 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of human ABL T315I mutant using EAIYAAPFAKKK substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Inhibition of recombinant PDGFRalpha (unknown origin) in presence of [33P]-ATP by kinase hotspot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.10nMAssay Description:Binding affinity to human PDGFRalpha using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor beta(Human)
Chinese Academy of Sciences
Curated by ChEMBL
Chinese Academy of Sciences
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant PDGFRbeta (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of BCR-ABL (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition incubated for 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant FGFR1 (unknown origin) using poly (Glu, Tyr) 4:1 after 60 mins by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Binding affinity to human FRK using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Refer to Reaction Biology Corps.More data for this Ligand-Target Pair
Affinity DataIC50: 1.30nMAssay Description:Inhibition of recombinant FGFR2 (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.40nMAssay Description:Inhibition of Abl (unknown origin) incubated for 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.5nMAssay 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 DataIC50: 1.5nMAssay Description:Inhibition of recombinant human VEGFR2 using substrate poly[Glu:Tyr] (4:1) in presence of [33-P]ATP by kinase hotspot assayMore data for this Ligand-Target Pair

3D Structure (crystal)