Target
Epidermal growth factor receptor [T790M,L858R]
Ligand
BDBM149405
Substrate
n/a
Meas. Tech.
Omnia Assay Protocol for Potency Assessment Against EGFR (WT) and EGFR (T790M/L858R) Active Enzymes
IC50
5.50±n/a nM
Citation
 Lee, KNiu, DPetter, RCBaevsky, MFSingh, J Heterocyclic compounds and uses thereof US Patent  US10434101 Publication Date 10/8/2019 
Target
Name:
Epidermal growth factor receptor [T790M,L858R]
Synonyms:
EGFR | EGFR (L858R, T790M) | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR) (T790M/L858R) | Epidermal growth factor receptor (EGFR)(T790M/L858R) | Epidermal growth factor receptor (T790M)(L858R) | Epidermal growth factor receptor (T790M, L858R) | Epidermal growth factor receptor (T790M/L858R) | Epidermal growth factor receptor(L858R, T790M) | HER1
Type:
n/a
Mol. Mass.:
134353.72
Organism:
Homo sapiens (Human)
Description:
P00533[T790M,L858R]
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM149405
Synonyms:
US10434101, Compound I-5 | US11096942, Compound I-5 | US8975249, I-15 | US8975249, I-5
Type:
Small organic molecule
Emp. Form.:
C24H24ClN5O4
Mol. Mass.:
481.931
SMILES:
COc1cc(ccc1Nc1ncc(Cl)c(Oc2cccc(NC(=O)C=C)c2)n1)N1CCOCC1
Structure:
Search PDB for entries with ligand similarity: