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Target
Receptor tyrosine-protein kinase erbB-2
Ligand
BDBM28508
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Homogeneous Time Resolved Fluorescence (HTRF) Assay
IC50
2660±n/a nM
Citation
 Waterson, AG; Petrov, KG; Hornberger, KR; Hubbard, RD; Sammond, DM; Smith, SC; Dickson, HD; Caferro, TR; Hinkle, KW; Stevens, KL; Dickerson, SH; Rusnak, DW; Spehar, GM; Wood, ER; Griffin, RJ; Uehling, DE Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors. Bioorg Med Chem Lett 19:1332-6 (2009) [PubMed]  Article 
Target
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:
MELAALCRWGLLLALLPPGAASTQVCTGTDMKLRLPASPETHLDMLRHLYQGCQVVQGNLELTYLPTNASLSFLQDIQEVQGYVLIAHNQVRQVPLQRLRIVRGTQLFEDNYALAVLDNGDPLNNTTPVTGASPGGLRELQLRSLTEILKGGVLIQRNPQLCYQDTILWKDIFHKNNQLALTLIDTNRSRACHPCSPMCKGSRCWGESSEDCQSLTRTVCAGGCARCKGPLPTDCCHEQCAAGCTGPKHSDCLACLHFNHSGICELHCPALVTYNTDTFESMPNPEGRYTFGASCVTACPYNYLSTDVGSCTLVCPLHNQEVTAEDGTQRCEKCSKPCARVCYGLGMEHLREVRAVTSANIQEFAGCKKIFGSLAFLPESFDGDPASNTAPLQPEQLQVFETLEEITGYLYISAWPDSLPDLSVFQNLQVIRGRILHNGAYSLTLQGLGISWLGLRSLRELGSGLALIHHNTHLCFVHTVPWDQLFRNPHQALLHTANRPEDECVGEGLACHQLCARGHCWGPGPTQCVNCSQFLRGQECVEECRVLQGLPREYVNARHCLPCHPECQPQNGSVTCFGPEADQCVACAHYKDPPFCVARCPSGVKPDLSYMPIWKFPDEEGACQPCPINCTHSCVDLDDKGCPAEQRASPLTSIISAVVGILLVVVLGVVFGILIKRRQQKIRKYTMRRLLQETELVEPLTPSGAMPNQAQMRILKETELRKVKVLGSGAFGTVYKGIWIPDGENVKIPVAIKVLRENTSPKANKEILDEAYVMAGVGSPYVSRLLGICLTSTVQLVTQLMPYGCLLDHVRENRGRLGSQDLLNWCMQIAKGMSYLEDVRLVHRDLAARNVLVKSPNHVKITDFGLARLLDIDETEYHADGGKVPIKWMALESILRRRFTHQSDVWSYGVTVWELMTFGAKPYDGIPAREIPDLLEKGERLPQPPICTIDVYMIMVKCWMIDSECRPRFRELVSEFSRMARDPQRFVVIQNEDLGPASPLDSTFYRSLLEDDDMGDLVDAEEYLVPQQGFFCPDPAPGAGGMVHHRHRSSSTRSGGGDLTLGLEPSEEEAPRSPLAPSEGAGSDVFDGDLGMGAAKGLQSLPTHDPSPLQRYSEDPTVPLPSETDGYVAPLTCSPQPEYVNQPDVRPQPPSPREGPLPAARPAGATLERPKTLSPGKNGVVKDVFAFGGAVENPEYLTPQGGAAPQPHPPPAFSPAFDNLYYWDQDPPERGAPPSTFKGTPTAENPEYLGLDVPV
  
Inhibitor
Name:
BDBM28508
Synonyms:
(3R,5S)-5-[2-(4-{[1-(2-phenylethyl)-1H-indol-5-yl]amino}thieno[3,2-d]pyrimidin-6-yl)ethynyl]pyrrolidin-3-yl morpholine-4-carboxylate | alkynyl thienopyrimidine, 15t
Type:
Small organic molecule
Emp. Form.:
C33H32N6O3S
Mol. Mass.:
592.711
SMILES:
O=C(O[C@H]1CN[C@@H](C1)C#Cc1cc2ncnc(Nc3ccc4n(CCc5ccccc5)ccc4c3)c2s1)N1CCOCC1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3934.43
Organism:
n/a
Description:
n/a
Residue:
34
Sequence:
ITINAMINHEANICACIDEEEEYFELVAKKKCNH