Reaction Details |
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Target | Epidermal growth factor receptor |
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Ligand | BDBM50328256 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_665430 (CHEMBL1261159) |
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IC50 | 10900±n/a nM |
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Citation | Liu, JJ; Daniewski, I; Ding, Q; Higgins, B; Ju, G; Kolinsky, K; Konzelmann, F; Lukacs, C; Pizzolato, G; Rossman, P; Swain, A; Thakkar, K; Wei, CC; Miklowski, D; Yang, H; Yin, X; Wovkulich, PM Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors. Bioorg Med Chem Lett20:5984-7 (2010) [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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BDBM50328256 |
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n/a |
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Name | BDBM50328256 |
Synonyms: | 5-(2-fluorophenyl)-2,10-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine-7-carbonitrile | CHEMBL1257795 |
Type | Small organic molecule |
Emp. Form. | C17H10FN5 |
Mol. Mass. | 303.2932 |
SMILES | Fc1ccccc1C1=Nc2cn[nH]c2Nc2ccc(cc12)C#N |t:8| |
Structure |
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