Target

Ligand

Substrate

Meas. Tech.

Kinase Inhibition Assay

pH

7.4±n/a

Temperature

295.15±n/a K

Citation

 Showalter, HD; Bridges, AJ; Zhou, H; Sercel, AD; McMichael, A; Fry, DW Tyrosine kinase inhibitors. 16. 6,5,6-tricyclic benzothieno[3, 2-d]pyrimidines and pyrimido[5,4-b-] and -[4,5-b]indoles as potent inhibitors of the epidermal growth factor receptor tyrosine kinase. J Med Chem 42:5464-74 (1999) [PubMed]  Article Copy BDB DOI

More Info.:

Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method

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:

MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA

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Blast E-value cutoff:

Name:

BDBM3603

Synonyms:

4-N-(3-bromophenyl)-6-N-methylpyrido[3,4-d]pyrimidine-4,6-diamine | 4-[(3-bromophenyl)amino]-6-(methylamino)pyrido[3,4-d]pyrimidine | CHEMBL53753 | PD158780

Type:

Small organic molecule

Emp. Form.:

C14H12BrN5

Mol. Mass.:

330.183

SMILES:

CNc1cc2c(Nc3cccc(Br)c3)ncnc2cn1

Structure:

Search PDB for entries with ligand similarity:

Similarity to this molecule at least:

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:

LYSHISLYSLYSLEALAGLGLYSERALATYRGLGLVAL