Reaction Details |
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Target | Epidermal growth factor receptor [T790M,L858R] |
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Ligand | BDBM195880 |
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Substrate/Competitor | n/a |
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Meas. Tech. | EGFR kinase assay |
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Temperature | 298.15±n/a K |
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IC50 | 4.39±n/a nM |
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Comments | extracted |
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Citation | Li, H; Xu, Y; Zhao, Z; Liu, X; Zhou, W; Bai, F; Xue, M; Zhang, L; Zhang, Y Pteridine ketone derivative and applications thereof as EGFR, BLK, and FLT3 inhibitor US Patent US9670213 Publication Date 6/6/2017 |
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More Info.: | Get all data from this article, Assay Method |
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Epidermal growth factor receptor [T790M,L858R] |
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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: | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
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BDBM195880 |
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n/a |
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Name | BDBM195880 |
Synonyms: | US9670213, Compound 025 4-(8-(3-acrylamidephenyl)-7-oxo-7,8-dihydropteridinyl-2-amino)benzamide |
Type | Small organic molecule |
Emp. Form. | C22H17N7O3 |
Mol. Mass. | 427.4155 |
SMILES | NC(=O)c1ccc(Nc2ncc3ncc(=O)n(-c4cccc(NC(=O)C=C)c4)c3n2)cc1 |
Structure |
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