Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor
Ligand
BDBM5456
Substrate
EGFR Substrate Peptide
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
11±n/a nM
Citation
 Gaul, MD; Guo, Y; Affleck, K; Cockerill, GS; Gilmer, TM; Griffin, RJ; Guntrip, S; Keith, BR; Knight, WB; Mullin, RJ; Murray, DM; Rusnak, DW; Smith, K; Tadepalli, S; Wood, ER; Lackey, K Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines. Bioorg Med Chem Lett 13:637-40 (2003) [PubMed]  Article 
Target
Name:
Epidermal growth factor receptor
Synonyms:
EGF Receptor Substrate | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal Growth Factor Receptor Tyrosine Kinase | Epidermal Growth Factor Receptor erbB-1 | Epidermal Growth Factor Receptor, ErbB-1 | Epidermal growth factor receptor (EGFR) | Epidermal growth factor receptor (HER1) | HER1 | Protein-Tyrosine Kinase Erbb-1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase ErbB-1 | Tyrosine-Protein Kinase ErbB-1
Type:
Receptor Kinase Domain
Mol. Mass.:
134279.59
Organism:
Homo sapiens (Human)
Description:
P00533
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM5456
Synonyms:
6-alkoxy-4-anilinoquinazoline 8b | N-(3-ethynylphenyl)-6-{4-[(2-methanesulfonylethyl)amino]butoxy}quinazolin-4-amine
Type:
Small organic molecule
Emp. Form.:
C23H26N4O3S
Mol. Mass.:
438.543
SMILES:
CS(=O)(=O)CCNCCCCOc1ccc2ncnc(Nc3cccc(c3)C#C)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
EGFR Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3934.43
Organism:
n/a
Description:
10 uM ATP as co-substrate.
Residue:
34
Sequence:
ITINAMINHEANICACIDEEEEYFELVAKKKCNH