| Reaction Details |
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 | Report a problem with these data |
| Target | Epidermal growth factor receptor |
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| Ligand | BDBM50191488 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1613063 (CHEMBL3854863) |
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| IC50 | 14±n/a nM |
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| Citation |  Smaill, JB; Gonzales, AJ; Spicer, JA; Lee, H; Reed, JE; Sexton, K; Althaus, IW; Zhu, T; Black, SL; Blaser, A; Denny, WA; Ellis, PA; Fakhoury, S; Harvey, PJ; Hook, K; McCarthy, FO; Palmer, BD; Rivault, F; Schlosser, K; Ellis, T; Thompson, AM; Trachet, E; Winters, RT; Tecle, H; Bridges, A Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. J Med Chem59:8103-24 (2016) [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 |
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| 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 |
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| Type: | Receptor Kinase Domain |
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| Mol. Mass.: | 134279.59 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P00533 |
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| Residue: | 1210 |
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| 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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| BDBM50191488 |
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| n/a |
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| Name | BDBM50191488 |
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| Synonyms: | CHEMBL3930506 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H22ClFN6O |
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| Mol. Mass. | 440.901 |
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| SMILES | Fc1ccc(Nc2ncnc3cnc(NC(=O)\C=C\CN4CCCCC4)cc23)cc1Cl |
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| Structure | 
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