| Reaction Details |
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 | Report a problem with these data |
| Target | Epidermal growth factor receptor [L858R,T790M,C797S] |
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| Ligand | BDBM494991 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | TR-FRET Assay for ERBB Kinases |
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| IC50 | 16.0±n/a nM |
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| 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 |
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| More Info.: | Get all data from this article, Assay Method |
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| Epidermal growth factor receptor [L858R,T790M,C797S] |
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| Name: | Epidermal growth factor receptor [L858R,T790M,C797S] |
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| Synonyms: | EGFR | EGFR (L858R, T790M, C797S) | EGFR_HUMAN | ERBB | ERBB1 | HER1 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 134337.65 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P00533[L858R,T790M,C797S] |
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| Residue: | 1210 |
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| Sequence: | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLIMQLMPFGSLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
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| BDBM494991 |
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| n/a |
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| Name | BDBM494991 |
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| Synonyms: | US10994015, Example 287 |
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| Type | Small organic molecule |
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| Emp. Form. | C40H49N11O6 |
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| Mol. Mass. | 779.8872 |
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| SMILES | COC1CCN(CC1)c1nccc(Nc2cc3n(c(COCCN4CCN(CC4)c4ccc5C(=O)N(C6CCC(=O)NC6=O)C(=O)c5c4)nc3cn2)C(C)(C)C)n1 |
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| Structure | 
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