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Found 47 Enz. Inhib. hit(s) with Target = 'Receptor tyrosine-protein kinase erbB-2' and Ligand = 'BDBM5445'
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  2.70nMAssay Description:Inhibition of HER2 (unknown origin) assessed as reduction in autophosphorylation by ELISA methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  2.80nMAssay Description:Inhibition of C-terminal His6-tagged HER2 (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated fo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  3nMAssay Description:Inhibition of HER2 by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  4nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of HER2 by flash plate based radioactive enzyme assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  7.60nMMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of ErbB2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibitory constant against Adenosine A2A receptor using [3H]-SCH-58,261 as radio ligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of Her-2 by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMpH: 7.5 T: 2°CAssay Description:Enzymatic reactions were initiated by adding kinase to the reaction mixture containing ATP, [gamma-33P] ATP, peptide substrate and test inhibitor com...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMpH: 7.5 T: 2°CAssay Description:Assays were performed in 96-well microtiter plates in reaction buffer containing biotinylated substrate, ATP/[gamma-33P]ATP, and purified kinase in t...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of HER2 by homogeneous time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of Her-2 by time-resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9nMAssay Description:Inhibition of ErbB2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.20nMAssay Description:Inhibition of HER2 (unknown origin) expressed in baculovirus infected insect cells after 20 mins in presence of ATP by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.20nMAssay Description:Inhibition of HER2 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.20nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.80nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.80nMAssay Description:Antagonist potency against adenosine A2A receptor of Sprague-Dawley rat aortic smooth muscleMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  9.80nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10nMAssay Description:Inhibition of HER-2 (unknown origin) using poly-(Glu4-Tyr) as substrate after 1 hr by ELISA-based spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10nMAssay Description:Inhibition of HER2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10nMAssay Description:Inhibition of erbB2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10nMAssay Description:Inhibition of ErbB2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  10.3nMAssay Description:Inhibition of human ErbB2 preincubated for 2 hrs prior addition of ATP by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  13nMAssay Description:Inhibition of HER2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 40 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  13nMpH: 7.5Assay Description:The EGFR, HER2 and HER4 kinase assay were performed using radiolabeled [gamma-32P] ATP from GE Healthcare. More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  17nMAssay Description:Inhibition of His-tagged human HER2 (676 to 1255 residues) expressed in baculovirus after 1 hr by Z-lyte assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  23.1nMAssay Description:HER2: The compounds' inhibition of target modulation were determined as follows: BT474 cells were sorted in 96 well plates (20000 cells/well) wit...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  24nMAssay Description:Inhibition of HER2 (unknown origin) assessed as remaining ATP level measured after 15 mins by luminescence analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  29nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  33nMAssay Description:Inhibition of wild type human N-terminal His-tagged HER2 cytoplasmic domain (676 to 1255 residues) expressed in baculovirus expression system after 1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  36nMAssay Description:Inhibition of Her2 by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  36.3nMAssay Description:Inhibition of HER2 preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  42nMAssay Description:Inhibition of HER2 (unknown origin) by ADP-Glo assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  60nMAssay Description:Inhibition of His-tagged human recombinant Her2 (676 to 1255 residues) expressed in baculovirus by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  60nMAssay Description:Inhibition of Erbb2 using poly(Glu,Tyr)4:1 as substrate and [gamma33P]ATP after 60 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  96nMAssay Description:Inhibition of HER2 (unknown origin) in presence of substrate incubated for 30 mins by ADP-Glo assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  100nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  124nMAssay Description:Inhibition of HER2 in human SKBR3 cells by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  140nMAssay Description:Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataIC50:  540nMAssay Description:Inhibition of His-tagged human HER-2 cytoplasmic domain (676-1245 aa) (unknown origin) assessed as inhibition of autophosphorylation by TR-fluorometr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataKd:  7nMAssay Description:Binding constant for ERBB2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataKd:  7nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In DepthDetails PCBioAssay
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataKd:  7nMAssay Description:Binding constant for ERBB2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
Southeast University

Curated by ChEMBL
LigandPNGBDBM5445(CHEMBL554 | GW572016 | LAPATINIB DITOSYLATE | Lapa...)
Affinity DataKd:  11nMAssay Description:Average Binding Constant for ERBB2; NA=Not Active at 10 uMMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed