Target
Epidermal growth factor receptor [668-1210]
Ligand
BDBM238271
Substrate
n/a
Meas. Tech.
Omnia Assay
pH
7.5±n/a
IC50
5±n/a nM
Comments
extracted
Citation
 Lee, KNiu, DBaevsky, MF Mutant-selective EGFR inhibitors and uses thereof US Patent  US9409887 Publication Date 8/9/2016 
Target
Name:
Epidermal growth factor receptor [668-1210]
Synonyms:
EGF-R Tyrosine Kinase | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR) | HER1 | Receptor tyrosine-protein kinase ErbB-1
Type:
Cytoplasmic region
Mol. Mass.:
61304.06
Organism:
Homo sapiens (Human)
Description:
Wildtype EGFR was purchased from Invitrogen.
Residue:
543
Sequence:
MRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM238271
Synonyms:
US9409887, I-2
Type:
Small organic molecule
Emp. Form.:
C26H26F3N7O3
Mol. Mass.:
541.5249
SMILES:
COc1cc(NC2CN(C2)C(C)=O)ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: