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Target
Epidermal growth factor receptor [671-1210,L858R]
Ligand
BDBM27963
Substrate
Biotinylated EGFR Peptide Substrate
Meas. Tech.
In Vitro Kinase Inhibition Assay
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
65±n/a nM
Citation
 Hubbard, RD; Bamaung, NY; Fidanze, SD; Erickson, SA; Palazzo, F; Wilsbacher, JL; Zhang, Q; Tucker, LA; Hu, X; Kovar, P; Osterling, DJ; Johnson, EF; Bouska, J; Wang, J; Davidsen, SK; Bell, RL; Sheppard, GS Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases. Bioorg Med Chem Lett 19:1718-21 (2009) [PubMed]  Article 
Target
Name:
Epidermal growth factor receptor [671-1210,L858R]
Synonyms:
EGF-R Tyrosine Kinase Mutant (L858R) | EGFR | EGFR_HUMAN | ERBB | ERBB1 | HER1 | Receptor tyrosine-protein kinase ErbB-1
Type:
Intracellular domain
Mol. Mass.:
60902.51
Organism:
Homo sapiens (Human)
Description:
EGFR kinase construct (L858R) was used in enzyme assays.
Residue:
540
Sequence:
RHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM27963
Synonyms:
3-(2-(2-chlorobenzyl)-1H-benzo[d]imidazol-5-yl)-1-((1r,4r)-4-morpholinocyclohexyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine | 3-(2-(2-chlorobenzyl)-1H-benzo[d]imidazol-6-yl)-1-((trans)-4-morpholinocyclohexyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine | 3-{2-[(2-chlorophenyl)methyl]-1H-1,3-benzodiazol-6-yl}-1-[4-(morpholin-4-yl)cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine | CHEMBL251732 | substituted benzimidazole, 8
Type:
Small organic molecule
Emp. Form.:
C29H31ClN8O
Mol. Mass.:
543.062
SMILES:
Nc1ncnc2n(nc(-c3ccc4nc(Cc5ccccc5Cl)[nH]c4c3)c12)[C@H]1CC[C@@H](CC1)N1CCOCC1 |r,wU:30.38,wD:27.31,(-3.15,6.99,;-3.15,5.45,;-4.48,4.68,;-4.48,3.14,;-3.15,2.37,;-1.82,3.14,;-.35,2.66,;.55,3.91,;-.35,5.15,;.12,6.62,;-.85,7.81,;-.31,9.25,;1.21,9.5,;2.04,10.8,;3.53,10.41,;4.72,11.39,;6.16,10.84,;6.16,9.3,;7.49,8.53,;8.83,9.3,;8.83,10.84,;7.49,11.61,;7.49,13.15,;3.62,8.87,;2.19,8.31,;1.64,6.87,;-1.82,4.68,;.42,1.33,;-.41,.03,;.29,-1.34,;1.83,-1.41,;2.66,-.11,;1.96,1.26,;2.6,-2.74,;1.94,-4.13,;2.81,-5.4,;4.35,-5.28,;5.01,-3.89,;4.14,-2.62,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated EGFR Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
3934.43
Organism:
n/a
Description:
n/a
Residue:
34
Sequence:
ITINAMINHEANICACIDEEEEYFELVAKKKCNH