null
SMILES COc1cc(ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F)N1CCN(CC1)C(C)=O
InChI Key InChIKey=HUFOZJXAKZVRNJ-UHFFFAOYSA-N
PDB links: 2 PDB IDs match this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 64 hits for monomerid = 149404
Affinity DataKi: 74nMAssay Description:Reversible inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus...More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataKi: 303nMAssay Description:Binding affinity to recombinant human GST-tagged EGFR (668 to 1210 residues) cytoplasmic domain expressed in baculovirus expression systemMore data for this Ligand-Target Pair
Affinity DataIC50: 1nMpH: 7.5Assay Description:Briefly, 10x stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13xATP (AS001A) and ap...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-...More data for this Ligand-Target Pair
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 46nMAssay Description:Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 79nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 65nMAssay Description:Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 62nMAssay Description:Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 187nMAssay Description:Inhibition of EGFR Del ex19 mutant phosphorylation in human HCC827 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 211nMAssay Description:Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 4.33E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human H1299 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysisMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 460nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovir...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataKd: 1.40nMAssay Description:Kinase-tagged T7 phage strains were prepared in an E. coli host derived from the BL21 strain. E. coli were grown to log-phase and infected with T7 ph...More data for this Ligand-Target Pair
Affinity DataIC50: 344nMAssay Description:Inhibition of N-terminal 6His/TEV protease cleavage site-tagged wild type human EGFR using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 145nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514) 1. 2.5 uL-4x Test Compound or 100 nL 100x plus 2.4...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 108nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL—4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 16.6nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL—4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
Affinity DataIC50: 13.7nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL—4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
Affinity DataIC50: 101nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL—4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
Affinity DataIC50: 1.70nMAssay Description:Neuronal sodium channel blocking activity by [14C]guanidinium flux assayMore data for this Ligand-Target Pair
Affinity DataEC50: 1.66E+3nMAssay Description:Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 272nMAssay Description:Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system using Poly(Glu,Tyr)4:1 as substrate...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system using Poly(Glu,Tyr)4:1 as substr...More data for this Ligand-Target Pair
Affinity DataIC50: 145nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 2.10nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
Affinity DataIC50: 180nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 1.30nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
Affinity DataIC50: 180nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 1.30nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
Affinity DataIC50: 1.53E+5nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 2.50E+3nMAssay Description:Test compounds: a part of compounds of the invention, the chemical names and preparation methods of which can be found in their preparation examples....More data for this Ligand-Target Pair
Affinity DataIC50: 460nMAssay Description:Inhibition of recombinant wild type human EGFR (695 to end residues) using Poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins follow...More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of EGFR T790M/exon 19 deletion mutant phosphorylation in human PC9-DRH cells preincubated for 2 hrs followed by EGF stimulation for 10 min...More data for this Ligand-Target Pair
Affinity DataIC50: 79nMAssay Description:Inhibition of EGFR exon 19 deletion mutant phosphorylation in human PC9 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandw...More data for this Ligand-Target Pair
Affinity DataIC50: 16nMAssay Description:Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by s...More data for this Ligand-Target Pair
Affinity DataIC50: 46nMAssay Description:Inhibition of EGFR L858R mutant phosphorylation in human H3255 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by sandwich ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60E+3nMAssay Description:Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A549 cells preincubated for 2 hrs followed by EGF stimulation for 10 mins by san...More data for this Ligand-Target Pair
Affinity DataIC50: 5.5nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [T790M,L858R](Homo sapiens (Human))
BETTA PHARMACEUTICALS CO., LTD.
US Patent
BETTA PHARMACEUTICALS CO., LTD.
US Patent
Affinity DataIC50: 1nMAssay Description:Briefly, 10× stocks of EGFR-WT (PV3872) from Invitrogen and EGFR-T790M/L858R (40350) from BPS Bioscience, San Diego, Calif., 1.13×ATP (AS001A) and ap...More data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followe...More data for this Ligand-Target Pair