Reaction Details |
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Target | Epidermal growth factor receptor [1-18,20-745,747-749,751-1210] |
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Ligand | BDBM495012 |
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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 | 53.0±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 [1-18,20-745,747-749,751-1210] |
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Name: | Epidermal growth factor receptor [1-18,20-745,747-749,751-1210] |
Synonyms: | EGFR | EGFR Delta 19/746/750 | EGFR_HUMAN | ERBB | ERBB1 | HER1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 133977.26 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 1207 |
Sequence: | MRPSGTAGAALLALLAALPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVV
LGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAV
LSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQ
NHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCT
GPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVV
TDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKN
CTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFE
NLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLF
GTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNL
LEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMG
ENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVA
LGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSG
AFGTVYKGLWIPEGEKVKIPVAIKLRETSPKANKEILDEAYVMASVDNPHVCRLLGICLT
STVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNV
LVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVT
VWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRE
LIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGF
FSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSID
DTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQ
PTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQ
SSEFIGA
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BDBM495012 |
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n/a |
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Name | BDBM495012 |
Synonyms: | US10994015, Example 308 |
Type | Small organic molecule |
Emp. Form. | C53H70N14O8S2 |
Mol. Mass. | 1095.342 |
SMILES | CC(C)n1nc(N2CC(CNCCCOCCOCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)C2)c2cnc(Nc3ccnc(n3)-c3cnn(c3)S(=O)(=O)C3CC3)cc12 |r| |
Structure |
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