BDBM149404 AVL-301::CHEMBL3545308::CNX-419::CO-1686::Rociletinib::Tube721::US10167264, Compound CO-1686::US10300058, CO-1686::US10434101, Compound I-4::US11096942, Compound I-4::US8975249, I-4::US9783524, CO-1686
SMILES CC(=O)N1CCN(CC1)c2ccc(c(c2)OC)Nc3ncc(c(n3)Nc4cccc(c4)NC(=O)C=C)C(F)(F)F
InChI Key InChIKey=HUFOZJXAKZVRNJ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 64 hits for monomerid = 149404
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: 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: 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: 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: 1.30nMAssay 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 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: 1.70nMAssay Description:Inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression...More data for this Ligand-Target Pair
Affinity DataIC50: 1.80nMAssay Description:Inhibition of recombinant human EGFR T790M/L858R mutant expressed in baculovirus insect cell expression system in presence of ATP preincubated 5 mins...More 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: 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: 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: 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: 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
Affinity DataIC50: 4.20nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin) incubated for 35 mins by HTRF KinEASE-TK assayMore 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
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
Affinity DataIC50: 5.5nMpH: 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: 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: 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: 13.7nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL4× Test Compound or 100 nL 100×...More 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: 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: 16.6nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Inhibition of N-terminal GST tagged human recombinant EGFR L858R/T790M mutant (695 to end amino acids) expressed in baculovirus infected Sf9 insect c...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: 20nMAssay Description:Inhibition of EGFR L858R/T790M (unknown origin) incubated for 60 mins in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Inhibition of EGFR (unknown origin) incubated for 60 mins in presence of ATP by ADP-Glo kinase assayMore 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: 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: 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: 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 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
Affinity DataIC50: 76nMAssay Description:Inhibition of wild type EGFR (unknown origin) in presence of ATP preincubated 5 mins measured for 30 mins by detection reagent based HTRF analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 77nMAssay Description:Inhibition of wild type EGFR (unknown origin) incubated for 10 mins by HTRF KinEASE-TK assayMore 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: 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: 101nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL4× Test Compound or 100 nL 100×...More data for this Ligand-Target Pair
Affinity DataIC50: 108nMAssay Description:Kinase Assay Protocol:Bar-coded Corning, low volume NBS, black 384-well plate (Corning Cat. #4514)1. 2.5 μL4× Test Compound or 100 nL 100×...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
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
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
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
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: 262nMAssay Description:Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA methodMore 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 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

3D Structure (crystal)