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

Data  3 KI  158 IC50  780 Kd  2 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 5445   

TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataIC50: 7.60nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2019
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataKd:  54nMAssay Description:Binding constant for ERBB4 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataKd:  54nMAssay Description:Inhibition of recombinant human wild type partial length HER4 (690 to 994 residues) expressed in bacterial expression system by competitive binding a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataIC50: 190nMAssay Description:Inhibition of ErbB4 in human T47D cells assessed as suppression of neuregulin 1-induced autophosphorylation incubated for 90 mins by sandwich ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2022
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataIC50: 250nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2020
Entry Details
US Patent

TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
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
In Depth
Date in BDB:
9/10/2012
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
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
In Depth
Date in BDB:
4/5/2009
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataIC50: 387nMAssay Description:Inhibition of HER4 (unknown origin) in presence of radiolabelled gammaATP by radioisotope filter binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Xuanzhu Pharma

US Patent
LigandPNGBDBM5445(N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of HER4 preincubated for 10 mins followed by incubation for 30 mins by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMed