Target
Epidermal growth factor receptor [668-1210,T790M,L858R]
Ligand
BDBM287618
Substrate
n/a
Meas. Tech.
ssay of Inhibitory Activity on Wild Type EGFR and Mutant EGFR Kinase
Temperature
298.15±n/a K
IC50
5.00±n/a nM
Comments
extracted
Citation
 Jin, YBu, PHe, QLan, JZhou, FZhang, LHe, X Azabicyclo derivatives, process for preparation thereof and medical use thereof US Patent  US10085983 Publication Date 10/2/2018 
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:
BDBM287618
Synonyms:
N-(2-(4-(dimethylamino)piperidin-1-yl)-4-methoxy-5-(7-(quinolin-3-yl)pyrrolo[1,2-f][1,2,4]triazin-2-ylamino)phenyl)acrylamide | US10085983, Compound J-13
Type:
Small organic molecule
Emp. Form.:
C32H34N8O2
Mol. Mass.:
562.6648
SMILES:
COc1cc(N2CCC(CC2)N(C)C)c(NC(=O)C=C)cc1Nc1ncc2ccc(-c3cnc4ccccc4c3)n2n1
Structure:
Search PDB for entries with ligand similarity: