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Target
Epidermal growth factor receptor [668-1210,T790M,L858R]
Ligand
BDBM50029668
Substrate
n/a
Meas. Tech.
ssay of Inhibitory Activity on Wild Type EGFR and Mutant EGFR Kinase
Temperature
298.15±n/a K
IC50
2.00±n/a nM
Comments
extracted
Citation
 Jin, Y; Bu, P; He, Q; Lan, J; Zhou, F; Zhang, L; He, 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:
BDBM50029668
Synonyms:
AZD-9291 | Osimertinib | US10085983, Compound AZD-9291 | US10227342, Example 24 | US11111233, Example AZD9291 | US11896597, Compound AZD9291 | US20230322822, Compound AZD9291 | US9890168, Compound AZD-9291 | WO2022090481, Example osimertinib
Type:
Small organic molecule
Emp. Form.:
C28H33N7O2
Mol. Mass.:
499.6073
SMILES:
COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12
Structure:
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