Target
Epidermal growth factor receptor [1-18,20-1210,T790M,C797S]
Ligand
BDBM547877
Substrate
n/a
Meas. Tech.
Ba/F3 cell model generation and proliferation assays
IC50
0.60±n/a nM
Citation
 Harald, EMark, PJuergen, RUlrich, RHeinz, SDirk, STobias, W SUBSTITUTED 1H-PYRAZOLO[4,3-C]PYRIDINES AND DERIVATIVES AS EGFR INHIBITORS WIPO 0:0 (2022) [PubMed] 
Target
Name:
Epidermal growth factor receptor [1-18,20-1210,T790M,C797S]
Synonyms:
EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR)(del19/T790M/C797S) | HER1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
134190.47
Organism:
Homo sapiens (Human)
Description:
P00533[1-18,20-1210,T790M,C797S]
Residue:
1209
Sequence:
MRPSGTAGAALLALLAALPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGSLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM547877
Synonyms:
WO2022090481, Example I-096
Type:
Small organic molecule
Emp. Form.:
C33H38N8O3
Mol. Mass.:
594.7066
SMILES:
COc1ccncc1-c1cc2n(ncc2c(C)n1)-c1cc2n(C)c(C(=O)N3CCN(CC3)C3COC3)c(C)c2c(n1)C(C)C
Structure:
Search PDB for entries with ligand similarity: