Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor [L858R,T790M,C797S]
Ligand
BDBM494934
Substrate
n/a
Meas. Tech.
TR-FRET Assay for ERBB Kinases
IC50
36.0±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:
BDBM494934
Synonyms:
2-(2,6-dioxopiperidin-3-yl)-5-(2-(4-(2-((1-isopropyl-6-((2-(4-methoxypiperidin-1-yl)pyrimidin-4-yl)amino)-1H-imidazo[4,5-c]pyridin-2-yl)methoxy)ethyl)piperazin-1-yl)ethoxy)isoindoline-1,3-dione | US10994015, Example 76
Type:
Small organic molecule
Emp. Form.:
C41H51N11O7
Mol. Mass.:
809.9131
SMILES:
COC1CCN(CC1)c1nccc(Nc2cc3n(C(C)C)c(COCCN4CCN(CCOc5ccc6C(=O)N(C7CCC(=O)NC7=O)C(=O)c6c5)CC4)nc3cn2)n1
Structure:
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