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 119 hits for monomerid = 5445
Affinity DataKi: 3nMAssay Description:Inhibition of EGFR (unknown origin)More data for this Ligand-Target Pair
3D Structure (crystal)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
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: 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
TargetEpidermal growth factor receptor [G719C](Homo sapiens (Human))
Ambit Biosciences
Curated by PubChem BioAssay
Ambit Biosciences
Curated by PubChem BioAssay
Affinity DataKd: 0.920nMpH: 7.4 T: 2°CAssay 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
Affinity DataKd: 8.60nMAssay 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
TargetEpidermal growth factor receptor [1-999,L858R](Homo sapiens (Human))
Ambit Biosciences
Curated by PubChem BioAssay
Ambit Biosciences
Curated by PubChem BioAssay
Affinity DataKd: 2.80E+3nMAssay 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
Affinity DataKd: 4.20nMAssay 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
Affinity DataKd: 2.40nMAssay 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
Affinity DataKd: 2.10nMAssay 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
Affinity DataKd: 2.20nMAssay 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
Affinity DataKd: 3.90nMAssay 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
Affinity DataKd: 3.5nMAssay 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
Affinity DataKd: 1.20nMAssay 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
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: 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 DataKd: 2.20nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.10nMAssay Description:Binding constant for EGFR(G719S) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 1.20nMAssay Description:Binding constant for EGFR(L861Q) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 8.60nMAssay Description:Binding constant for EGFR(E746-A750del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.40nMAssay Description:Binding constant for EGFR kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for EGFR(L858R,T790M) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.80nMAssay Description:Binding constant for EGFR(L858R) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.90nMAssay Description:Binding constant for EGFR(L747-S752del, P753S) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 0.920nMAssay Description:Binding constant for EGFR(G719C) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.5nMAssay Description:Binding constant for EGFR(L747-T751del,Sins) kinase domainMore 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 DataKd: 4.20nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.5nMAssay Description:Binding constant for EGFR(L747-T751del,Sins) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 4.20nMAssay Description:Binding constant for EGFR(S752-I759del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.80nMAssay Description:Binding constant for EGFR(L858R) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 0.920nMAssay Description:Binding constant for EGFR(G719C) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.40nMAssay Description:Binding constant for EGFR kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.10nMAssay Description:Binding constant for EGFR(G719S) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 8.60nMAssay Description:Binding constant for EGFR(E746-A750del) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 2.20nMAssay Description:Binding constant for EGFR(L747-E749del, A750P) kinase domainMore data for this Ligand-Target Pair
Affinity DataKd: 3.90nMAssay Description:Binding constant for EGFR(L747-S752del, P753S) kinase domainMore 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
Affinity DataIC50: 10nMAssay Description:Inhibitory activity against metabotropic glutamate receptor 5 (mGluR5)More 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
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: 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 DataKd: 5.5nMAssay Description:Average Binding Constant for EGFR; NA=Not Active at 10 uMMore data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:Inhibition of human recombinant EGFRMore 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: 140nMAssay Description:Inhibition of EGFR in human A431 cells by HTRF assayMore data for this Ligand-Target Pair