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Target
Epidermal growth factor receptor [L858R,T790M,C797S]
Ligand
BDBM495017
Substrate
n/a
Meas. Tech.
TR-FRET Assay for ERBB Kinases
IC50
20.0±n/a nM
Citation
 Crew, AP; Zimmermann, K; Wang, J; Crews, CM; Jaime-Figueroa, S; Burslem, G EGFR proteolysis targeting chimeric molecules and associated methods of use US Patent  US10994015 Publication Date 5/4/2021 
Target
Name:
Epidermal growth factor receptor [L858R,T790M,C797S]
Synonyms:
EGFR | EGFR (L858R, T790M, C797S) | EGFR_HUMAN | ERBB | ERBB1 | HER1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
134337.65
Organism:
Homo sapiens (Human)
Description:
P00533[L858R,T790M,C797S]
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGSLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM495017
Synonyms:
US10994015, Example 313 | US10994015, Example 314
Type:
Small organic molecule
Emp. Form.:
C46H54N14O6S
Mol. Mass.:
931.076
SMILES:
CC(C)n1nc(N2CC(CN3CCN(CC4CCN(CC4)c4ccc5C(=O)N(C6CCC(=O)NC6=O)C(=O)c5c4)CC3)C2)c2cnc(Nc3ccnc(n3)-c3cnn(c3)S(=O)(=O)C3CC3)cc12
Structure:
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