Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor [696-1210,T790M]
Ligand
BDBM4583
Substrate
Tyr 04 Substrate Peptide
Meas. Tech.
EGFR IC50 Determination
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
3±n/a nM
Citation
 Michalczyk, A; Klüter, S; Rode, HB; Simard, JR; Grütter, C; Rabiller, M; Rauh, D Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. Bioorg Med Chem 16:3482-8 (2008) [PubMed]  Article 
Target
Name:
Epidermal growth factor receptor [696-1210,T790M]
Synonyms:
EGF-R Tyrosine Kinase Mutant (T790M) | EGFR | EGFR_HUMAN | ERBB | ERBB1 | HER1 | Receptor tyrosine-protein kinase ErbB-1
Type:
Cytoplasmic region
Mol. Mass.:
57805.41
Organism:
Homo sapiens (Human)
Description:
EGFR-T790M was purchased from Upstate.
Residue:
515
Sequence:
GEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM4583
Synonyms:
(2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide | 4-anilinoquinazoline deriv. 16a | BMC163482 Compound 2 | CHEMBL94061
Type:
Small organic molecule
Emp. Form.:
C20H20BrN5O
Mol. Mass.:
426.31
SMILES:
CN(C)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Tyr 04 Substrate Peptide
Synonyms:
n/a
Type:
FRET-peptide substrate
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA