Reaction Details |
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Target | Epidermal growth factor receptor [671-1210,L858R] |
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Ligand | BDBM27961 |
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Substrate/Competitor | Biotinylated EGFR Peptide Substrate |
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Meas. Tech. | In Vitro Kinase Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 270±n/a nM |
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Citation | Hubbard, RD; Bamaung, NY; Fidanze, SD; Erickson, SA; Palazzo, F; Wilsbacher, JL; Zhang, Q; Tucker, LA; Hu, X; Kovar, P; Osterling, DJ; Johnson, EF; Bouska, J; Wang, J; Davidsen, SK; Bell, RL; Sheppard, GS Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases. Bioorg Med Chem Lett19:1718-21 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Epidermal growth factor receptor [671-1210,L858R] |
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Name: | Epidermal growth factor receptor [671-1210,L858R] |
Synonyms: | EGF-R Tyrosine Kinase Mutant (L858R) | EGFR | EGFR_HUMAN | ERBB | ERBB1 | HER1 | Receptor tyrosine-protein kinase ErbB-1 |
Type: | Intracellular domain |
Mol. Mass.: | 60902.51 |
Organism: | Homo sapiens (Human) |
Description: | EGFR kinase construct (L858R) was used in enzyme assays. |
Residue: | 540 |
Sequence: | RHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGL
WIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIT
QLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQH
VKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTF
GSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSK
MARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTS
RTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVP
EYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNST
FDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
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BDBM27961 |
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Biotinylated EGFR Peptide Substrate |
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Name: | Biotinylated EGFR Peptide Substrate |
Synonyms: | n/a |
Type: | Peptide |
Mol. Mass.: | 3934.43 |
Organism: | n/a |
Description: | n/a |
Residue: | 34 |
Sequence: | biotin-(aminohexanoic acid)-EEEEYFELVAKKK-CONH2
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