BDBM86734 CAS_220127-57-1::Gleevec::NSC_0
SMILES CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
InChI Key InChIKey=KTUFNOKKBVMGRW-UHFFFAOYSA-N
Data 66 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 66 hits for monomerid = 86734
Affinity DataIC50: 21nMAssay Description:Inhibition of recombinant His-tagged human CSF1R catalytic domain expressed in baculovirus expression system using TAMRA-KKKSPGEYVNIEFG as substrate ...More data for this Ligand-Target Pair
Affinity DataIC50: 75nMAssay Description:Inhibition of human N-terminal his tagged unphosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preinc...More data for this Ligand-Target Pair
Affinity DataIC50: 75nMAssay Description:Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs ...More data for this Ligand-Target Pair
Affinity DataIC50: 188nMAssay Description:Inhibition of ABL1 (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 220nMAssay Description:Inhibition of GST tagged Abl M244V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein(Mouse)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 260nMAssay Description:Inhibition of WT BCR-ABL (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by methane-thiosul...More data for this Ligand-Target Pair
Affinity DataIC50: 280nMAssay Description:Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated ...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein(Mouse)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 280nMAssay Description:Inhibition of WT BCR-ABL (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of tyrosine phosphorylation incubated for 3 hrs by imm...More data for this Ligand-Target Pair
Affinity DataIC50: 300nMAssay Description:Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP additio...More data for this Ligand-Target Pair
Affinity DataIC50: 350nMAssay Description:Inhibition of human N-terminal his tagged native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs ...More data for this Ligand-Target Pair
Affinity DataIC50: 380nMAssay Description:Inhibition of GST tagged Abl M244V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 386nMAssay Description:Inhibition of PDGFR-beta (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Human)
The First Affiliated Hospital of Zhengzhou University
Curated by ChEMBL
The First Affiliated Hospital of Zhengzhou University
Curated by ChEMBL
Affinity DataIC50: 410nMAssay Description:Inhibition of c-Kit (unknown origin)More data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Human)
The First Affiliated Hospital of Zhengzhou University
Curated by ChEMBL
The First Affiliated Hospital of Zhengzhou University
Curated by ChEMBL
Affinity DataIC50: 413nMAssay Description:Inhibition of KIT (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 440nMAssay Description:Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor alpha(Human)
Iran University of Medical Sciences
Curated by ChEMBL
Iran University of Medical Sciences
Curated by ChEMBL
Affinity DataIC50: 759nMAssay Description:Inhibition of PDGFRA exon 18 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 775nMAssay Description:Inhibition of GST tagged Abl F311L mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Inhibition of GST tagged Abl H396P mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Inhibition of GST tagged Abl F311L mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Inhibition of GST tagged Abl F317L mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 800nMAssay Description:Inhibition of GST tagged Abl V379I mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 820nMAssay Description:Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 825nMAssay Description:Inhibition of GST tagged Abl L387M mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 900nMAssay Description:Inhibition of GST tagged Abl F359V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 900nMAssay Description:Inhibition of GST tagged Abl F317L mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 950nMAssay Description:Inhibition of GST tagged Abl V379I mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of GST tagged Abl G250E mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+3nMAssay Description:Inhibition of GST tagged Abl H396R mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 1.50E+3nMAssay Description:Inhibition of GST tagged Abl L387M mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 1.65E+3nMAssay Description:Inhibition of GST tagged Abl G250E mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 1.95E+3nMAssay Description:Inhibition of GST tagged Abl H396R mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of GST tagged Abl H396P mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 2.80E+3nMAssay Description:Inhibition of GST tagged Abl E255K mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+3nMAssay Description:Inhibition of human ABL1 H396P mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured e...More data for this Ligand-Target Pair
Affinity DataIC50: 3.70E+3nMAssay Description:Inhibition of GST tagged Abl E255V mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30E+3nMAssay Description:Inhibition of GST tagged Abl Y253F mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 4.70E+3nMAssay Description:Inhibition of GST tagged Abl F359V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl Y253F mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl Y253H mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
TargetBreakpoint cluster region protein(Mouse)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of native BCR-ABL T315I mutant autophosphorylation in mouse BaF3 cells incubated for 6 hrs by immunoblot analysisMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lyn(Human)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Lyn (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP additionMore data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl E255V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Human)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Src (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP additionMore data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl Y253H mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Human)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Src (unknown origin) assessed as inhibition of phosphorylation using PTK biotinylated peptide substrate 2 as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl E255K mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl T315l mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of CrkL in mouse BaF3 cells harbouring BCR-ABL1 T315I mutant measured after 6 hrs by immunoblotting analysisMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase Lyn(Human)
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Oregon Health and Science University Cancer Institute
Curated by ChEMBL
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Lyn (unknown origin) assessed as inhibition of phosphorylation using PTK biotinylated peptide substrate 2 as substrate prein...More data for this Ligand-Target Pair
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of GST tagged Abl T315l mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair