BDBM50185140 AP-26113::Brigatinib::US11248003, Example Brigatinib::US20230322822, Compound Brigatinib
SMILES COc1cc(ccc1Nc1ncc(Cl)c(Nc2ccccc2P(C)(C)=O)n1)N1CCC(CC1)N1CCN(C)CC1
InChI Key InChIKey=AILRADAXUVEEIR-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 60 hits for monomerid = 50185140
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
Ariad Pharmaceuticals
Curated by ChEMBL
Ariad Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human FLT3 using EAIYAAPFAKKK as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 8nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in Bac-to-Bac baculovirus expression system measured after 2 hrs by ELI...More data for this Ligand-Target Pair
Affinity DataIC50: 196nMAssay Description:Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Ariad Pharmaceuticals
Curated by ChEMBL
Ariad Pharmaceuticals
Curated by ChEMBL
Affinity DataIC50: 25nMAssay Description:Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 0.370nMAssay Description:Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hrMore data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant using poly (Glu,Tyr)...More data for this Ligand-Target Pair
Affinity DataIC50: 51nMAssay Description:Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 77nMAssay Description:Inhibition of wild-type EGFR (unknown origin) using Poly(Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of human C-terminal His-tagged and N-terminal GST-tagged EGFR L858R/T790M/C797S triple mutant ( 668 to 1210 amino acids) expressed in bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Bac...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Bac...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 1nMAssay Description:Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Bacu...More data for this Ligand-Target Pair
Affinity DataIC50: 48nMAssay Description:Inhibition of wild type EGFR (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 2.5nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.5nMAssay Description:Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Homo sapiens (Human))
Jinan University
Curated by ChEMBL
Jinan University
Curated by ChEMBL
Affinity DataIC50: 41nMAssay Description:Inhibition of EML4/ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as antiproliferative activity after 72 hrs by CellTiter...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor/Echinoderm microtubule-associated protein-like 4(Homo sapiens (Human))
Jinan University
Curated by ChEMBL
Jinan University
Curated by ChEMBL
Affinity DataIC50: 184nMAssay Description:Inhibition of EML4/ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as antiproliferative activity after 72 hrs by CellTiter...More data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of human ALK G1202R mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human ALK L1196M mutant using poly[Glu:Tyr] (4:1) as substrate in presence of [gamma-33P]-ATP assay by radiometric HotSpot assayMore data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR...More data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme...More data for this Ligand-Target Pair
Affinity DataIC50: 261nMAssay Description:Inhibition of wild type EGFR (unknown origin) measured by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.20nMAssay Description:Binding affinity to ALK (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.10nMAssay Description:Binding affinity to ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Inhibition of Wild type EGFR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 203nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as protein phosphorylation measured after 2 hrs by...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [1-18,20-1210,T790M,C797S](Homo sapiens (Human))
Oncobix
US Patent
Oncobix
US Patent
Affinity DataIC50: 2nMAssay Description:The inhibitory activity on a C797S-containing epidermal growth factor receptor (EGFR) kinase and an MET kinase was measured for compound 1 obtained i...More data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:The inhibitory activity on a C797S-containing epidermal growth factor receptor (EGFR) kinase and an MET kinase was measured for compound 1 obtained i...More data for this Ligand-Target Pair
Affinity DataIC50: 0.820nMAssay Description:Inhibition of EGFR del18/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.40nMAssay Description:Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 53nMAssay Description:Inhibition of wild type EGFR (unknown origin) using TK as substrate incubated for 120 mins in the presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 75nMAssay Description:Inhibition of wild type EGFR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 28nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of EGFR del19 mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of EGFR del19/T790M mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 4.90nMAssay Description:Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 3.90nMAssay Description:Inhibition of EGFR del19/T790M/C797S mutant (unknown origin)More data for this Ligand-Target Pair
TargetNUAK family SNF1-like kinase 1(Homo sapiens (Human))
University Of Science And Technology (Ust)
Curated by ChEMBL
University Of Science And Technology (Ust)
Curated by ChEMBL
Affinity DataIC50: 47nMAssay Description:Inhibition of NUAK1 (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [1-18,20-1210,T790M](Homo sapiens (Human))
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Affinity DataIC50: 164nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [1-18,20-1210,C797S](Homo sapiens (Human))
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Affinity DataIC50: 178nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Affinity DataIC50: 148nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [L858R,C797S](Homo sapiens (Human))
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Affinity DataIC50: 548nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [L858R,T790M,C797S](Homo sapiens (Human))
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Chengdu Di''Ao Jiuhong Pharmaceutical Factory
US Patent
Affinity DataIC50: 752nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [1-18,20-1210,T790M,C797S](Homo sapiens (Human))
Oncobix
US Patent
Oncobix
US Patent
Affinity DataIC50: 194nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair
Affinity DataIC50: 1.70E+3nMAssay Description:To assess the effect of compounds on the activity of wild-type and mutant EGFR kinases, kinase activity was tested by measuring ATP consumption in an...More data for this Ligand-Target Pair