Reaction Details |
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Target | Epidermal growth factor receptor [T790M,L858R] |
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Ligand | BDBM149404 |
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Substrate/Competitor | n/a |
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Meas. Tech. | EGFR in vitro assay |
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Kd | 1.40±n/a nM |
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Citation | Zhang, D Substituted pyrimidines useful as EGFR-T790M kinase inhibitors US Patent US10167264 Publication Date 1/1/2019 |
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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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BDBM149404 |
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n/a |
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Name | BDBM149404 |
Synonyms: | AVL-301 | CHEMBL3545308 | CNX-419 | CO-1686 | Rociletinib | Tube721 | US10167264, Compound CO-1686 | US10300058, CO-1686 | US10434101, Compound I-4 | US11096942, Compound I-4 | US8975249, I-4 | US9783524, CO-1686 |
Type | Small organic molecule |
Emp. Form. | C27H28F3N7O3 |
Mol. Mass. | 555.5515 |
SMILES | COc1cc(ccc1Nc1ncc(c(Nc2cccc(NC(=O)C=C)c2)n1)C(F)(F)F)N1CCN(CC1)C(C)=O |
Structure |
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