BDBM3032 CHEMBL1204168::CHEMBL29197::N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine::PD153035::US11001595, Compound PD153035::US11111252, Compound PD153035::US9422297, PD153035
SMILES COc1cc2ncnc(Nc3cccc(Br)c3)c2cc1OC
InChI Key InChIKey=LSPANGZZENHZNJ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 65 hits for monomerid = 3032
Affinity DataIC50: 2.60nMAssay Description:Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:Inhibition of human EGFR kinase activityMore data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of EGFR in human A431 cells by phosphotyrosine cell-based ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0250nMAssay Description:Inhibition of EGFRMore data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10...More data for this Ligand-Target Pair
Affinity DataIC50: 200nMAssay Description:Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation m...More data for this Ligand-Target Pair
Affinity DataIC50: 70.8nMAssay Description:Inhibition autophosphorylation of EGFR in human DiFi cells after 2 hrs by ELISAMore data for this Ligand-Target Pair
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Human)
University of Bonn
Curated by ChEMBL
University of Bonn
Curated by ChEMBL
Affinity DataIC50: 1.73E+3nMAssay Description:Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to...More data for this Ligand-Target Pair
TargetBroad substrate specificity ATP-binding cassette transporter ABCG2(Human)
University of Bonn
Curated by ChEMBL
University of Bonn
Curated by ChEMBL
Affinity DataIC50: 2.32E+3nMAssay Description:Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up ...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of EGFR expressed in human A431 cellsMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Affinity DataIC50: 143nMAssay Description:Inhibition of human ErbB2 tyrosine kinase phosphorylation expressed in mouse BaF3 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 0.660nMAssay Description:Displacement of [125I]4-(3-iodoanilino)-6,7-dimethoxyquinazoline from EGFR tyrosine kinase in human A431 cell membranesMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-4(Human)
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Affinity DataIC50: 49nMAssay Description:Inhibition of human ErbB4 tyrosine kinase phosphorylation expressed in human CEM/4 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 100nMAssay Description:Inhibition of human EGFR in presence of 1 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 2.60nMAssay Description:Inhibition of human EGFR in presence of 1 uM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 1.49E+3nMAssay Description:Inhibition of human VEGFR2 in presence of 1 uM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human VEGFR2 in presence of 1 mM ATPMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0290nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0950nMAssay Description:Inhibition of recombinant human EGFR using Ulight-CAGAGAIETDKEYYTVKD as substrate measured after 15 mins by LANCE assayMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Human)
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Lawrence Berkeley National Laboratory
Curated by ChEMBL
Affinity DataIC50: 5.40E+3nMAssay Description:Inhibition of recombinant human HER2 expressed in insect cells using biotinyl-betaAbetaAbetaAAEEEEYFELVAKKK as substrate after 30 mins by HTRF methodMore data for this Ligand-Target Pair
Affinity DataIC50: 15nMAssay Description:Inhibition of EGFR in human A431 cells assessed as reduction in EGF-stimulated EGFR autophosphorylation preincuabted for 90 mins followed by EGF-stim...More data for this Ligand-Target Pair
Affinity DataIC50: 260nMAssay Description:Inhibition of tracer 5 binding to human N-terminal nano luciferase-fused GAK expressed in HEK293 cells measured after 2 hrs by nanoBRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 680nMAssay Description:Inhibition of EGFR in human MDA-MB-468 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter methodMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0290nMAssay Description:Inhibition of EGFR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 220nMAssay Description:Inhibition of EGFR in human A431 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter methodMore data for this Ligand-Target Pair
Affinity DataIC50: 300nMAssay Description:Inhibition of EGFR in human DIFI cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter methodMore data for this Ligand-Target Pair
Affinity DataIC50: 400nMAssay Description:Inhibition of EGFR in human DU145 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter methodMore data for this Ligand-Target Pair
Affinity DataIC50: 950nMAssay Description:Inhibition of EGFR in human ME180 cells assessed as reduction in cell proliferation incubated for 72 hrs by Coulter counter methodMore data for this Ligand-Target Pair
Affinity DataIC50: 25nMAssay Description:Inhibition of human A431 cell-derived EGFR using Lys-His-Lys-LysLeu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val as substrate measured after 10 mins in pre...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Table 9: Compounds 1 and 2, Section D., (see FIG. 4, bottom row, far right column) each inhibit VEGFR-2 and PDGFR-β for antiangiogenic effects a...More data for this Ligand-Target Pair
Affinity DataKd: 29nMAssay Description:Binding affinity to GAK (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.0290nMAssay 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
TargetTyrosine-protein kinase transforming protein Abl(Abelson murine leukemia virus)
Novartis Pharmaceuticals
Novartis Pharmaceuticals
Affinity DataIC50: 30nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 1.40E+3nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+5nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 70nMAssay Description:The EGF-R kinase autophosphorylation activity was measured by DELFIA/time-resolved fluorometry with excitation at 340 nm and emission at 615 nm. Po...More data for this Ligand-Target Pair
Affinity DataIC50: 16nMpH: 7.6 T: 2°CAssay Description:The activity of EGFR, preactivated with EGF, is measured by its ability to transfer terminal phosphate from [gamma-32P]ATP to poly(GAT) substrate.More data for this Ligand-Target Pair
Affinity DataIC50: 200nMpH: 7.4 T: 2°CAssay Description:Cells used were tumor cell lines naturally expressing high levels of tyrosine kinases. Expression levels at the RNA level were derived from the NCI D...More data for this Ligand-Target Pair
Affinity DataIC50: 230nMAssay Description:Inhibition of various kinase enzyme.More data for this Ligand-Target Pair
Affinity DataIC50: 4nMAssay Description:In vitro inhibitory activity against epidermal growth factor receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 2.50E+5nMAssay Description:Inhibition of Cyclin-dependent kinase 2More data for this Ligand-Target Pair
Affinity DataKd: 8.10E+3nMAssay Description:Equilibrium binding constant for EPH receptor B2More data for this Ligand-Target Pair
Affinity DataIC50: 1.02E+4nMAssay Description:Inhibition of EPH receptor B2 using ELISAMore data for this Ligand-Target Pair
Affinity DataIC50: 28nMAssay Description:Inhibition of EGFR tyrosine kinase activityMore data for this Ligand-Target Pair
Affinity DataIC50: 0.0250nMAssay Description:Inhibition of EGFRMore data for this Ligand-Target Pair
Affinity DataIC50: 6nMAssay Description:IC50 is the inhibitor concentration which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-32P] labe...More data for this Ligand-Target Pair
Affinity DataIC50: 200nMAssay Description:Inhibition of EGFR expressed in human tumor cellsMore data for this Ligand-Target Pair