Reaction Details |
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Target | Receptor tyrosine-protein kinase erbB-2 |
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Ligand | BDBM50208401 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_456854 (CHEMBL923200) |
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IC50 | 27±n/a nM |
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Citation | Mastalerz, H; Chang, M; Chen, P; Fink, BE; Gavai, A; Han, WC; Johnson, W; Langley, D; Lee, FY; Leavitt, K; Marathe, P; Norris, D; Oppenheimer, S; Sleczka, B; Tarrant, J; Tokarski, JS; Vite, GD; Vyas, DM; Wong, H; Wong, TW; Zhang, H; Zhang, G 5-((4-Aminopiperidin-1-yl)methyl)pyrrolotriazine dual inhibitors of EGFR and HER2 protein tyrosine kinases. Bioorg Med Chem Lett17:4947-54 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Receptor tyrosine-protein kinase erbB-2 |
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Name: | Receptor tyrosine-protein kinase erbB-2 |
Synonyms: | 2.7.10.1 | C-erbB-2 | CD_antigen=CD340 | ERBB2 | ERBB2_HUMAN | ErbB-2/ErbB-3 heterodimer | FASN/HER2 | HER-2 Substrate | HER2 | MLN 19 | MLN19 | Metastatic lymph node gene 19 protein | NEU | NGL | Proto-oncogene Neu | Proto-oncogene c-ErbB-2 | Tyrosine kinase-type cell surface receptor HER2 | p185erbB2 |
Type: | n/a |
Mol. Mass.: | 137894.47 |
Organism: | Homo sapiens (Human) |
Description: | P04626 |
Residue: | 1255 |
Sequence: | MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNL
ELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNG
DPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLA
LTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQC
AAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACP
YNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSAN
IQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLP
DLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTV
PWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQEC
VEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARC
PSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVG
ILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETEL
RKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSP
YVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVR
LVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFT
HQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWM
IDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDA
EEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEG
AGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYV
NQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQ
GGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
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BDBM50208401 |
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n/a |
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Name | BDBM50208401 |
Synonyms: | 5-((1,4-diazepan-1-yl)methyl)-N-(1-(3-fluorobenzyl)-1H-indazol-5-yl)pyrrolo[1,2-f][1,2,4]triazin-4-amine | CHEMBL392273 |
Type | Small organic molecule |
Emp. Form. | C26H27FN8 |
Mol. Mass. | 470.5446 |
SMILES | Fc1cccc(Cn2ncc3cc(Nc4ncnn5ccc(CN6CCCNCC6)c45)ccc23)c1 |
Structure |
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