Reaction Details |
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Target | Epidermal growth factor receptor [T790M] |
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Ligand | BDBM50029668 |
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Substrate/Competitor | n/a |
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Meas. Tech. | EGFR Exon 19 Deletion and Exon 20 T790M Concurrent Mutations |
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IC50 | <100±n/a nM |
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Citation | Huang, W; Gong, Y; Li, F; Bencivenga, NE; Dalgarno, DC; Kohlmann, A; Shakespeare, WC; Thomas, RM; Zhu, X; West, A; Youngsaye, W; Zhang, Y; Zhou, T Heteroaryl compounds for kinase inhibition US Patent US10227342 Publication Date 3/12/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Epidermal growth factor receptor [T790M] |
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Name: | Epidermal growth factor receptor [T790M] |
Synonyms: | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR) T790M | Epidermal growth factor receptor (EGFR)(T790) | Epidermal growth factor receptor (EGFR)(T790M) | Epidermal growth factor receptor (T790M) | HER1 |
Type: | Enzyme |
Mol. Mass.: | 134309.68 |
Organism: | Homo sapiens (Human) |
Description: | P00533 (T790M) |
Residue: | 1210 |
Sequence: | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
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BDBM50029668 |
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n/a |
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Name | BDBM50029668 |
Synonyms: | AZD-9291 | Osimertinib | US10085983, Compound AZD-9291 | US10227342, Example 24 | US11111233, Example AZD9291 | US20230322822, Compound AZD9291 | US9890168, Compound AZD-9291 | WO2022090481, Example osimertinib |
Type | Small organic molecule |
Emp. Form. | C28H33N7O2 |
Mol. Mass. | 499.6073 |
SMILES | COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1nccc(n1)-c1cn(C)c2ccccc12 |
Structure |
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