Reaction Details |
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Target | Receptor tyrosine-protein kinase erbB-2 |
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Ligand | BDBM50293250 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_492486 (CHEMBL950399) |
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IC50 | 54±n/a nM |
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Citation | Hubbard, RD; Dickerson, SH; Emerson, HK; Griffin, RJ; Reno, MJ; Hornberger, KR; Rusnak, DW; Wood, ER; Uehling, DE; Waterson, AG Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines. Bioorg Med Chem Lett18:5738-40 (2009) [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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BDBM50293250 |
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n/a |
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Name | BDBM50293250 |
Synonyms: | (S)-N-(3-chloro-4-(3-fluorobenzyloxy)phenyl)-6-(pyrrolidin-2-ylethynyl)thieno[3,2-d]pyrimidin-4-amine | CHEMBL495979 |
Type | Small organic molecule |
Emp. Form. | C25H20ClFN4OS |
Mol. Mass. | 478.969 |
SMILES | Fc1cccc(COc2ccc(Nc3ncnc4cc(sc34)C#C[C@@H]3CCCN3)cc2Cl)c1 |r| |
Structure |
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