BDBM50322823 (S)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide::AFATINIB::CHEMBL1173655::US10085983, Compound BIBW2992::US10196365, Afatinib::US10435400, Compound BIBW2992::US11896597, Compound Afatinib::US9388170, Afatinib::US9890168, Compound BIBW2992::WO2022090481, Example afatinib
SMILES CN(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(F)c(Cl)c3)ncnc2cc1O[C@H]1CCOC1
InChI Key InChIKey=ULXXDDBFHOBEHA-CWDCEQMOSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 125 hits for monomerid = 50322823
Affinity DataIC50: 47nMAssay Description:BT474 Cell Line: 1. 5×103 cells per well in 100 μl of medium were seeded in 96-well plate, here the medium contained 5% FBS2. 24 hours later, 10...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type EGFR domain (unknown origin) expressed in baculovirus expression system using Poly(Glu:Tyr)4:1 substrate after 60 mins by ELI...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.610nMAssay Description:Binding constant for EGFR(T790M) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 1.10nMAssay Description:Binding constant for EGFR(L858R,T790M) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.230nMAssay Description:Binding constant for EGFR(L861Q) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.200nMAssay Description:Binding constant for EGFR(L858R) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.190nMAssay Description:Binding constant for EGFR(G719S) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.25nMAssay Description:Binding constant for EGFR kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.120nMAssay Description:Binding constant for EGFR(L747-S752del, P753S) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.140nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.110nMAssay Description:Binding constant for EGFR(E746-A750del) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.120nMAssay Description:Binding constant for EGFR(L747-T751del,Sins) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.100nMAssay Description:Binding constant for EGFR(G719C) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of wild type EGFR (unknown origin) incubated for 5 mins by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.970nMAssay Description:Inhibition of wild type EGFR T790M mutant (unknown origin) incubated for 5 mins by HTRF assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of EGFR (unknown origin) by ELISA methodMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1.60nMAssay Description:Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by addition of substrate by mobility shi...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 11nMAssay Description:Inhibition of GST-tagged EGFR expressed in Escherichia coliChecked by AuthorMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.140nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [668-1210,T790M,L858R](Homo sapiens (Human))
Shanghai Haiyan Pharmaceutical Technology
US Patent
Shanghai Haiyan Pharmaceutical Technology
US Patent
Affinity DataIC50: 5nMT: 2°CAssay Description:All reagents used in the following z′-lyte assay were purchased from Invitrogen.The inhibitory activity on T790M/L858R double mutant EGFR kinas...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1nMT: 2°CAssay Description:All reagents used in the following z′-lyte assay were purchased from Invitrogen.The inhibitory activity on T790M/L858R double mutant EGFR kinas...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.190nMAssay Description:Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELIS...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.965nMAssay Description:The kinase analysis in vitro was performed using the HTRF kinEASE TK kit of Invitrogen Co., the procedure steps were carried out according to instruc...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: <1nMAssay Description:Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubat...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1.60nMAssay Description:Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate measured after 10 mins by mobility shift assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:The inhibitory activities on T790M/L858R double mutant EGFR kinase (Invitrogen, PV4879) and wild-type EGFR kinase (Invitrogen, PV3872) were determine...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:The inhibitory activities on T790M/L858R double mutant EGFR kinase (Invitrogen, PV4879) and wild-type EGFR kinase (Invitrogen, PV3872) were determine...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 3.80nMAssay Description:Inhibition of recombinant EGFR (unknown origin) T790M/L858R double mutant preincubated for 30 mins followed by poly (Glu-Tyr) biotinylated peptide su...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: <1nMAssay Description:Inhibition of recombinant wild type EGFR (696 to C-terminal residues) (unknown origin) preincubated for 30 mins followed by poly (Glu-Tyr) biotinylat...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of wild-type EGFR (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of EGFR L858R/T790M mutant (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:The inhibitory effects of compounds to be tested on double mutant EGFR kinase (EGFR T790M/L858R Kinase) (Invitrogen, PV4879) and wild-type EGFR kinas...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:The inhibitory effects of compounds to be tested on double mutant EGFR kinase (EGFR T790M/L858R Kinase) (Invitrogen, PV4879) and wild-type EGFR kinas...More data for this Ligand-Target Pair
Affinity DataIC50: 0.570nMAssay Description:Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay Description:Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 12nMAssay Description:Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibition of probe binding to EGFR L858R mutant (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assayMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataKd: 0.25nMAssay Description:Binding affinity to wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system by Kinomescan methodMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human recombinant GST-tagged EGFR using pEY as substrate incubated for 30 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human recombinant GST-tagged EGFR L858R mutant using pEY as substrate incubated for 30 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of human recombinant GST-tagged EGFR L858R/T790M mutant using pEY as substrate incubated for 30 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Inhibition of human GST-fused EGFR kinase domain expressed in baculovirus expression system measured after 30 mins by ELISAMore data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.960nMAssay Description:Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin pe...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 0.5nMAssay Description:Irreversible inhibition of wild type EGFR (unknown origin)More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 15nMAssay Description:Inhibition of C-terminal His-tagged N-terminal GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells after 30 mins...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 22nMAssay Description:Inhibition of GST-tagged human EGFR kinase domain I858R/T790M mutant (696 to 1022 residues) using EGFR L858R/T790M substrate peptide incubated for 12...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Inhibition of GST-tagged human EGFR kinase domain (696 to 1022 residues) using poly(Glu, Tyr) 4:1 substrate incubated for 60 mins by kinase-Glo plus ...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Chinese Academy Of Sciences
Curated by ChEMBL
Chinese Academy Of Sciences
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Inhibition of GST-tagged human EGFR kinase domain (696 to 1022 residues) using poly(Glu, Tyr) 4:1 substrate incubated for 60 mins by kinase-Glo plus ...More data for this Ligand-Target Pair