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TargetMER intracellular domain/EGFR extracellular domain chimera
LigandBDBM3264
Substrate/CompetitorEGF-R Substrate
Meas. Tech.Kinase Inhibition Assay
pH7.4±n/a
Temperature295.15±n/a K
IC50 27±n/a nM
Citation Bridges, AJZhou, HRCody, DRRewcastle, GWMcMichael, AShowalter, HHFry, DWKraker, AJDenny, WA Tyrosine Kinase Inhibitors. 8. An Unusually Steep Structure-Activity Relationship for Analogues of 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a Potent Inhibitor of the Epidermal Growth Factor Receptor J Med Chem39:267-76 (1996)    Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
MER intracellular domain/EGFR extracellular domain chimera
Name:MER intracellular domain/EGFR extracellular domain chimera
Synonyms:EGF Receptor Substrate | EGFR | 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) | Epidermal growth factor receptor (T790M) | 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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BDBM3264
NameBDBM3264
Synonyms:4-Anilino quinazoline deriv. 15 | CHEMBL290096 | N-(3-bromophenyl)quinazolin-4-amine
TypeSmall organic molecule
Emp. Form.C14H10BrN3
Mol. Mass.300.153
SMILESBrc1cccc(Nc2ncnc3ccccc23)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
EGF-R Substrate
Name:EGF-R Substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:4119.23
Organism:n/a
Description:The sequence is based on a portion of phospholipase C-gamma. 10 uM ATP containing 1 uCi of [gamma-32P]ATP as co-substrate.
Residue:38
Sequence:
Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr-Glu-Glu-Val