Reaction Details |
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Target | Epidermal growth factor receptor |
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Ligand | BDBM50505837 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1824357 (CHEMBL4324121) |
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IC50 | 2100±n/a nM |
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Citation | Engelhardt, H; Böse, D; Petronczki, M; Scharn, D; Bader, G; Baum, A; Bergner, A; Chong, E; Döbel, S; Egger, G; Engelhardt, C; Ettmayer, P; Fuchs, JE; Gerstberger, T; Gonnella, N; Grimm, A; Grondal, E; Haddad, N; Hopfgartner, B; Kousek, R; Krawiec, M; Kriz, M; Lamarre, L; Leung, J; Mayer, M; Patel, ND; Simov, BP; Reeves, JT; Schnitzer, R; Schrenk, A; Sharps, B; Solca, F; Stadtmüller, H; Tan, Z; Wunberg, T; Zoephel, A; McConnell, DB Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. J Med Chem62:10272-10293 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Epidermal growth factor receptor |
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Name: | Epidermal growth factor receptor |
Synonyms: | EGF Receptor Substrate | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal Growth Factor Receptor Tyrosine Kinase | Epidermal Growth Factor Receptor erbB-1 | Epidermal Growth Factor Receptor, ErbB-1 | Epidermal growth factor receptor (EGFR) | Epidermal growth factor receptor (HER1) | HER1 | Protein-Tyrosine Kinase Erbb-1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase ErbB-1 | Tyrosine-Protein Kinase ErbB-1 |
Type: | Receptor Kinase Domain |
Mol. Mass.: | 134279.59 |
Organism: | Homo sapiens (Human) |
Description: | P00533 |
Residue: | 1210 |
Sequence: | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
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BDBM50505837 |
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n/a |
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Name | BDBM50505837 |
Synonyms: | CHEMBL4591327 |
Type | Small organic molecule |
Emp. Form. | C23H21FN4O2 |
Mol. Mass. | 404.4368 |
SMILES | CC(C)(O)Cn1c2ccccc2[nH]\c1=N/C(=O)c1cc(F)cc(c1)-c1cccnc1 |
Structure |
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