null
SMILES Brc1cccc(Nc2ncnc3ccc(NC(=O)C=C)cc23)c1
InChI Key InChIKey=HTUBKQUPEREOGA-UHFFFAOYSA-N
PDB links: 4 PDB IDs match this monomer. 2 PDB IDs contain inhibitors having a similarity of 90% to this monomer.
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 40 hits for monomerid = 4567
Affinity DataIC50: 2nMpH: 7.4 T: 2°CAssay 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
3D Structure (crystal)Affinity DataIC50: 3.90nMAssay Description:Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured at 1 hr by Western blot...More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMpH: 7.4 T: 2°CAssay Description:Enzyme assays for IC50 determinations were performed in 96-well filter plates. IC50 is the inhibitor concentration which inhibits 50% of kinase activ...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [668-1210](Homo sapiens (Human))
Chemical Genomics Centre of the Max Planck Society
Chemical Genomics Centre of the Max Planck Society
Affinity DataIC50: 0.0800nMpH: 7.5 T: 2°CAssay Description:The kinase reaction for EGFR consisted of BSA-supplemented kinase buffer, kinase, peptide, and ATP. For IC50 determinations, 10 different concentrati...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor [696-1210,T790M](Homo sapiens (Human))
Chemical Genomics Centre of the Max Planck Society
Chemical Genomics Centre of the Max Planck Society
Affinity DataIC50: 1.20nMpH: 7.5 T: 2°CAssay Description:The kinase reaction for EGFR consisted of BSA-supplemented kinase buffer, kinase, peptide, and ATP. For IC50 determinations, 10 different concentrati...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src [251-533,S345C](Gallus gallus (Chicken))
Chemical Genomics Centre of the Max Planck Society
Chemical Genomics Centre of the Max Planck Society
Affinity DataIC50: 340nMpH: 7.5 T: 2°CAssay Description:IC50 values were determined with the Z lyte assay system (Invitrogen). The reactions were performed in 384-well small volume plates from Greiner (#7...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src [251-533,T338M,S345C](Gallus gallus (Chicken))
Chemical Genomics Centre of the Max Planck Society
Chemical Genomics Centre of the Max Planck Society
Affinity DataIC50: 2.81E+3nMpH: 7.5 T: 2°CAssay Description:IC50 values were determined with the Z lyte assay system (Invitrogen). The reactions were performed in 384-well small volume plates from Greiner (#7...More data for this Ligand-Target Pair
Affinity DataIC50: 130nMAssay Description:Inhibition of various kinase enzyme.More data for this Ligand-Target Pair
Affinity DataIC50: 521nMAssay Description:Inhibition of various kinase enzyme.More data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of phosphorylation of glutamic acid/tyrosine random copolymer by isolated epidermal growth factor receptor (EGFR)More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMAssay Description:Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cellsMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
University of Auckland
Curated by ChEMBL
University of Auckland
Curated by ChEMBL
Affinity DataIC50: 5.70nMAssay Description:Inhibition of heregulin-stimulated autophosphorylation of ERBB2 receptor kinase in MDA-MB-453 cells.More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
University of Auckland
Curated by ChEMBL
University of Auckland
Curated by ChEMBL
Affinity DataIC50: 5.70nMAssay Description:Inhibition of autophosphorylation of ERBB2 receptor kinase in MDA-MB 453 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 2.70nMAssay Description:Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblottingMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Inhibition of phosphorylation of a polyglutamic acid/tyrosine random copolymer by EGFR enzyme prepared from human A431 carcinoma cell vesicles by imm...More data for this Ligand-Target Pair
Affinity DataIC50: 36nMAssay Description:Inhibition of EGFR tyrosine kinase activityMore data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
University of Auckland
Curated by ChEMBL
University of Auckland
Curated by ChEMBL
Affinity DataIC50: 24nMAssay Description:Inhibition of HER2 (unknown origin)More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-4(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 12nMAssay Description:Inhibition of HER4 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 3.14E+3nMAssay Description:Inhibition of JAK3 (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 5.47E+3nMAssay Description:Inhibition of Blk (unknown origin)More data for this Ligand-Target Pair
TargetSerine/threonine-protein kinase STK11(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of Lkb1 (unknown origin)More data for this Ligand-Target Pair
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of Bmx (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 5.83E+3nMAssay Description:Inhibition of Btk (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase ITK/TSK(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of Itk (unknown origin)More data for this Ligand-Target Pair
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of JAK3 (unknown origin) expressed in mouse BAF3 cells assessed as cytotoxicityMore data for this Ligand-Target Pair
TargetTyrosine-protein kinase Blk(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of Blk (unknown origin) expressed in mouse BAF3 cells assessed as cytotoxicityMore data for this Ligand-Target Pair
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 303nMAssay Description:Inhibition of Bmx (unknown origin) expressed in mouse BAF3 cells assessed as cytotoxicityMore data for this Ligand-Target Pair
TargetCytoplasmic tyrosine-protein kinase BMX(Homo sapiens (Human))
The Scripps Research Institute
Curated by ChEMBL
The Scripps Research Institute
Curated by ChEMBL
Affinity DataIC50: 324nMAssay Description:Inhibition of wild type Bmx (unknown origin) expressed in mouse BAF3 cells assessed as cytotoxicityMore data for this Ligand-Target Pair
Affinity DataIC50: 36nMAssay Description:Inhibition of EGFR-TK in human A431 cell lysate assessed as reduction in EGF stimulated kinase activity after 60 mins using biotinylated peptide subs...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of human recombinant EGFRMore data for this Ligand-Target Pair
Affinity DataIC50: 1.69nMAssay Description:Inhibition of human recombinant EGFR expressed in insect cells by time-resolved fluorometryMore data for this Ligand-Target Pair
Affinity DataIC50: 152nMAssay Description:Inhibition of EGFR autophosphorylation in human A431 cells after 8 hrs by western blotMore data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Inhibition of EGFR autophosphorylation in human A431 cells after 1 hr by western blotMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Homo sapiens (Human))
University of California
Curated by ChEMBL
University of California
Curated by ChEMBL
Affinity DataIC50: 2.70E+4nMAssay Description:Inhibition of c-src in by radioactive phosphotransfer assayMore data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+5nMAssay Description:Inhibition of Fyn expressed in Escherichia coli C43 by radioactive phosphotransfer assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of autophosphorylation of cytoplasmic domain of epidermal growth factor receptorMore data for this Ligand-Target Pair
Affinity DataIC50: 0.700nMAssay Description:Irreversible inhibition of EGFRMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase Src(Gallus gallus (Chicken))
Covalution Pharma BV
Curated by ChEMBL
Covalution Pharma BV
Curated by ChEMBL
Affinity DataIC50: 2.70E+4nMAssay Description:Inhibition of chicken c-SrcMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Inhibition of wild type EGFR autophosphorylation in human A549 cells incubated for 1 hr followed by compound washout measured after 8 hrs by Western ...More data for this Ligand-Target Pair
TargetReceptor tyrosine-protein kinase erbB-2(Homo sapiens (Human))
University of Auckland
Curated by ChEMBL
University of Auckland
Curated by ChEMBL
Affinity DataIC50: 114nMAssay Description:The HER-2 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