Target
Epidermal growth factor receptor [668-1210,T790M,L858R]
Ligand
BDBM238273
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,T790M,L858R]
Synonyms:
EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR)(T790M/L858R) | HER1
Type:
Enzyme
Mol. Mass.:
61378.18
Organism:
Homo sapiens (Human)
Description:
a.a: 668-1210
Residue:
543
Sequence:
MRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM238273
Synonyms:
US9409887, I-4
Type:
Small organic molecule
Emp. Form.:
C23H25ClN6O2
Mol. Mass.:
452.937
SMILES:
COc1cc(NC(C)C)ccc1Nc1ncc(Cl)c(Nc2cccc(NC(=O)C=C)c2)n1
Structure:
Search PDB for entries with ligand similarity: