BDBM32368 LAPATINIB

SMILES CS(=O)(=O)CCNCc1ccc(o1)-c1ccc2ncnc(Nc3ccc(OCc4cccc(F)c4)c(Cl)c3)c2c1

InChI Key InChIKey=BCFGMOOMADDAQU-UHFFFAOYSA-N

Data  17 IC50  4 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 21 hits for monomerid = 32368   

TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 3nMAssay Description:Inhibition of domain-GST fused human wild-type EGFR expressing in Sf9 cells using pEY (4:1) and bio-pEY as substrate for 30 min in the presence of AT...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 8nMAssay Description:Inhibition of domain-GST fused human EGFR L858R mutant expressing in Sf9 cells using pEY (4:1) and bio-pEY as substrate for 30 min in the presence of...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 15nMAssay Description:Inhibition of domain-GST fused human HER2 expressing in Sf9 cells using pEY (4:1) and bio-pEY as substrate for 30 min in the presence of ATP by ELISA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 63nMAssay Description:Inhibition of EGFR L858R mutant expressing in human NCI-H3255 cells assessed as cell survival incubated for 2 weeks and measured after 6 hrs by MTS a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataEC50:  99nMAssay Description:Inhibition of HER2-phosphorylation in HER2 expressing human BT-474 cells incubated for 1 hr followed by EGF stimulation for 20 min by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataEC50:  101nMAssay Description:Inhibition of HER2-phosphorylation in HER2 expressing human NCI-N87 cells incubated for 1 hr followed by EGF stimulation for 20 min by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataEC50:  105nMAssay Description:Inhibition of EGFR-phosphorylation in EGFR expressing human A-431 cells incubated for 1 hr followed by EGF stimulation for 20 min by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataEC50:  171nMAssay Description:Inhibition of human HER2-phosphorylation in HER2 expressing mouse NIH3T3 cells incubated for 1 hr followed by EGF stimulation for 20 min by ELISA met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 534nMAssay Description:Inhibition of wild-type EGFR expressing in human NCI-H1666 cells assessed as cell survival incubated for 2 weeks and measured after 6 hrs by MTS assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 4.00E+3nMAssay Description:Inhibition of EGFR L858R/T790M double mutant expressing in human NCI-H1975 cells assessed as cell survival incubated for 2 weeks and measured after 6...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 4.00E+3nMAssay Description:Inhibition of domain-GST fused human EGFR L858R/T790M double mutant expressing in Sf9 cells using pEY (4:1) and bio-pEY as substrate for 30 min in th...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 4.76E+3nMAssay Description:Inhibition of ERB2/EGFR in Melphalan Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueou...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEpidermal growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 5.00E+3nMAssay Description:Inhibition of EGFR T790M/L858R double mutant (unknown origin) using poly(Glu-Tyr) at 4:1 ratio as substrate in presence of ATP incubated for 60 mins ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 8.62E+3nMAssay Description:Inhibition of ERB2/EGFR in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell pro...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 9.12E+3nMAssay Description:Inhibition of ERB2/EGFR in bortezomib Resistant human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 9.85E+3nMAssay Description:Inhibition of ERB2/EGFR in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of ERB2/EGFR in human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell prol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
Knight Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of ERB2/EGFR in human bortezomib-resistant ANBL6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous o...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetProto-oncogene tyrosine-protein kinase Src(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of c-SRC (249 to 536 residues) (unknown origin) using pEY (4:1) and bio-pEY as substrate for 30 min in the presence of ATP by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetHepatocyte growth factor receptor(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of domain-GST fused HGFR (unknown origin) expressing in an Sf9 infected baculovirus expression system by ELISA methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetVascular endothelial growth factor receptor 2(Human)
Dana-Farber Cancer Institute

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 32368BDBM32368(LAPATINIB)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of VEGFR-2 (978 to 1408 residues) (unknown origin) using pEY (4:1) and bio-pEY as substrate for 20 min in the presence of ATP by ELISA met...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed