Target
Epidermal growth factor receptor [696-1022,T790M]
Ligand
BDBM5447
Substrate
BDBM10852
Meas. Tech.
Fluorescence Binding Assay
pH
7.4000±n/a
Temperature
295.1500±n/a K
Kd
4.6±.1 nM
Citation
 Yun, CHMengwasser, KEToms, AVWoo, MSGreulich, HWong, KKMeyerson, MEck, MJ The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A 105:2070-5 (2008) [PubMed]  Article 
Target
Name:
Epidermal growth factor receptor [696-1022,T790M]
Synonyms:
EGFR_HUMAN | EGFR | ERBB | ERBB1 | HER1 | EGF-R Tyrosine Kinase Mutant (T790M)
Type:
Tyrosine-protein kinase
Mol. Mass.:
37282.81
Organism:
Human
Description:
P00533[696-1022,T790M]
Residue:
327
Sequence:
GEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQG
  
Inhibitor
Name:
BDBM5447
Synonyms:
ZD1839 | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine | N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine | cid_123631 | CHEMBL939 | GEFITINIB | Iressa | US9416123, Gefitinib | US10106508, Gefitinib | US9730934, Gefitinib | US9783524, Gefitinib | US10507209, Compound Gefitinib | WO2022090481, Example gefitinib
Type:
Small organic molecule
Emp. Form.:
C22H24ClFN4O3
Mol. Mass.:
446.15
SMILES:
COc1cc2c(cc1OCCCN3CCOCC3)c(ncn2)Nc4ccc(c(c4)Cl)F
Structure:
Search PDB for entries with ligand similarity:
Substrate