BDBM5445 CHEMBL554::GW572016::LAPATINIB DITOSYLATE::Lapatinib::N-{3-chloro-4-[(3-fluoro-benzyl)oxy]phenyl}-6-[5-({2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine::N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)quinazolin-4-amine::Tykerb::US10507209, Compound Lapatinib::US10822334, Compound Lapatinib::US9730934, Lapatinib ditosylate::cid_208908
SMILES CS(=O)(=O)CCNCc1ccc(o1)-c1ccc2ncnc(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2c1
InChI Key InChIKey=BCFGMOOMADDAQU-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 157 hits for monomerid = 5445
Affinity DataIC50: 10nMpH: 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
3D Structure (crystal)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
Affinity DataIC50: 11nMpH: 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
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
Affinity DataIC50: 367nMpH: 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
Affinity DataIC50: 3nMpH: 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
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
Affinity DataIC50: 347nMpH: 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
Affinity DataIC50: <32nMAssay Description:Inhibition of EGF-induced EGFR phopshorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blotMore data for this Ligand-Target Pair
Affinity DataIC50: 1.70E+4nMAssay Description:Inhibition of INSR by flash plate based radioactive enzyme assayMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of Her-2 by time-resolved fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibition of EGFR phosphorylation in EGF-stimulated human A431 after 2 hrs by Western blot analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 7.90nMAssay Description:Inhibition of HER1 (unknown origin) assessed as reduction in autophosphorylation by ELISA methodMore data for this Ligand-Target Pair
TargetPlatelet-derived growth factor receptor beta(Homo sapiens (Human))
Southeast University
Curated by ChEMBL
Southeast University
Curated by ChEMBL
Affinity DataIC50: >2.00E+5nMAssay Description:Inhibition of PDGFRbeta (unknown origin) by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 2.70nMAssay Description:Inhibition of HER2 (unknown origin) assessed as reduction in autophosphorylation by ELISA methodMore data for this Ligand-Target Pair
TargetMast/stem cell growth factor receptor Kit(Homo sapiens (Human))
Ambit Biosciences
Curated by ChEMBL
Ambit Biosciences
Curated by ChEMBL
Affinity DataIC50: >2.00E+5nMAssay Description:Inhibition of c-KIT (unknown origin) by ELISA methodMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Homo sapiens (Human))
Southeast University
Curated by ChEMBL
Southeast University
Curated by ChEMBL
Affinity DataIC50: >2.00E+5nMAssay Description:Inhibition of KDR (unknown origin) by ELISA methodMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Inhibitory activity against metabotropic glutamate receptor 5 (mGluR5)More data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibitory constant against Adenosine A2A receptor using [3H]-SCH-58,261 as radio ligandMore data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of EGFR (unknown origin) after 40 mins by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.5nMAssay Description:Inhibition of EGFR (unknown origin) by Z'-LYTE assayMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily E/KQT member 1(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 2.51E+5nMAssay Description:Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using Ion...More data for this Ligand-Target Pair
TargetSodium channel protein type 5 subunit alpha(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 3.16E+6nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using I...More data for this Ligand-Target Pair
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 1.58E+7nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 1.00E+8nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platformMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 6.31E+5nMAssay Description:Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonW...More data for this Ligand-Target Pair
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Homo sapiens (Human))
University Of Oxford
Curated by ChEMBL
University Of Oxford
Curated by ChEMBL
Affinity DataIC50: 2.00E+6nMAssay Description:Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automa...More data for this Ligand-Target Pair
Affinity DataIC50: 11nMAssay Description:Inhibition of epidermal growth factor receptor kinase (unknown origin) using [33P]-ATP after 20 to 30 mins by radiometric assayMore data for this Ligand-Target Pair
Affinity DataIC50: 9nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
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
Affinity DataIC50: 280nMAssay Description:Inhibition of His-tagged EGFR cytoplasmic domain (645-1186 aa) (unknown origin) assessed as inhibition of autophosphorylation by TR-fluorometryMore data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:Inhibition of human recombinant EGFRMore data for this Ligand-Target Pair
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
Affinity DataIC50: 52nMAssay Description:Inhibition of Her1 by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 36nMAssay Description:Inhibition of Her2 by fluorescence polarization assayMore data for this Ligand-Target Pair
Affinity DataIC50: 124nMAssay Description:Inhibition of HER2 in human SKBR3 cells by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3nMAssay Description:Inhibition of HER2 by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Inhibition of EGFR in human A431 cells by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Inhibition of EGFR by HTRF assayMore data for this Ligand-Target Pair
TargetInsulin-like growth factor 1 receptor(Homo sapiens (Human))
Abbott Laboratories
Curated by ChEMBL
Abbott Laboratories
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human recombinant IGF1R expressed in Sf21 cells by time resolved fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 52nMAssay Description:Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 100nMAssay Description:Inhibition of ErbB2 by time resolved fluorescence assayMore data for this Ligand-Target Pair
Affinity DataIC50: 140nMAssay Description:Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISAMore data for this Ligand-Target Pair