Target

Ligand

Substrate

Meas. Tech.

Kinase Inhibition Assay

pH

7.4±n/a

Temperature

295.15±n/a K

Citation

 Rewcastle, GW; Bridges, AJ; Fry, DW; Rubin, JR; Denny, WA Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor. J Med Chem 40:1820-6 (1997) [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

Blast this sequence in BindingDB or PDB

  
Blast E-value cutoff:

Name:

BDBM3685

Synonyms:

4-[(3-Bromophenyl)amino]-6-(dimethylamino)pyrimido-[5,4-d]pyrimidine | 4-anilinopyrimido[5,4-d]pyrimidine deriv. 5d | 8-N-(3-bromophenyl)-2-N,2-N-dimethyl-[1,3]diazino[5,4-d]pyrimidine-2,8-diamine

Type:

Small organic molecule

Emp. Form.:

C14H13BrN6

Mol. Mass.:

345.197

SMILES:

CN(C)c1ncc2ncnc(Nc3cccc(Br)c3)c2n1

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