Affinity DataIC50: 0.0600nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.0600nMAssay Description:Inhibition of HER2 (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0900nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataKi: 0.100nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.100nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
Affinity DataKi: 0.110nMAssay Description:Reversible binding affinity to human EGFR L858R/ T790M double mutant expressed in baculovirus by fluorometric analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 0.140nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.140nMAssay Description:Inhibition of HER2 (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.150nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.150nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2 [V777L](Homo sapiens (Human))
Shanghai Pharmaceuticals Holding
Curated by ChEMBL
Shanghai Pharmaceuticals Holding
Curated by ChEMBL
Affinity DataIC50: 0.160nMAssay Description:Inhibition of HER2 V777L mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
Affinity DataIC50: 0.160nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.180nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.190nMAssay Description:Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated fo...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR exon19 deletion mutant (unknown origin) by HTRF assay in presence of Km of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) by HTRF assay in presence of Km of ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.200nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.280nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.290nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Inhibition of EGFR T790M/del746 to 750 mutant (unknown origin) by high-throughput biochemical screeningMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2 [1-775,'YVMA',776-1255](Human)
Korea Reserarch Institute of Chemical Technology
US Patent
Korea Reserarch Institute of Chemical Technology
US Patent
Affinity DataIC50: 0.300nMAssay Description:The activity of the compounds of the present invention against HER mutant enzymes was measured using the HTRF system purchased by Cisbio as follows. ...More data for this Ligand-Target Pair
Ligand InfoSimilars
Affinity DataIC50: 0.300nMAssay Description:Inhibition of HER-2 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.310nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
Affinity DataIC50: 0.310nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.340nMAssay Description:An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four dif...More data for this Ligand-Target Pair
Affinity DataIC50: 0.350nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
Affinity DataIC50: 0.350nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.380nMAssay Description:Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition for...More data for this Ligand-Target Pair
Affinity DataKi: 0.400nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.420nMAssay Description:Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 m...More data for this Ligand-Target Pair
Affinity DataIC50: 0.420nMAssay Description:Inhibition of HER2 D769H mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
Affinity DataIC50: 0.430nMAssay Description:Inhibition of HER2 D769Y mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore data for this Ligand-Target Pair
Affinity DataIC50: 0.430nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of HER2 (unknown origin) assessed as reduction in autophosphorylation by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of HER stimulated human erbB autophosphorylation in MDA-MB-453 cellsMore data for this Ligand-Target Pair
Affinity DataKi: <0.5nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: <0.5nMAssay Description:Inhibition of EGFR deletion (746 to 750 residues) mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.5nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of erbB2 fusion protein expressed in baculovirus by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.550nMAssay Description:PBD compounds and conjugates thereof were evaluated for their antiproliferation properties in tumor cell lines in vitro using CellTiter-Glo (Promega ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.560nMAssay Description:An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four dif...More data for this Ligand-Target Pair
Affinity DataIC50: 0.560nMAssay Description:Inhibition of HER2 R896C mutant (unknown origin) incubated for 120 mins in presence of 33P-ATP by P81 ion exchange cellulose chromatographyMore 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




3D Structure (crystal)




























