Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor [T790M,L858R]
Ligand
BDBM270540
Substrate
n/a
Meas. Tech.
Kinase Assay (EGFR)(T790M)(L858R)
IC50
15.4±n/a nM
Citation
 Hu, S; Liu, X; Bai, J; Long, W Protein tyrosine kinase modulators and methods of use US Patent  US9783524 Publication Date 10/10/2017 
Target
Name:
Epidermal growth factor receptor [T790M,L858R]
Synonyms:
EGFR | EGFR (L858R, T790M) | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor (EGFR) (T790M/L858R) | Epidermal growth factor receptor (EGFR)(T790M/L858R) | Epidermal growth factor receptor (T790M)(L858R) | Epidermal growth factor receptor (T790M, L858R) | Epidermal growth factor receptor (T790M/L858R) | Epidermal growth factor receptor(L858R, T790M) | HER1
Type:
n/a
Mol. Mass.:
134353.72
Organism:
Homo sapiens (Human)
Description:
P00533[T790M,L858R]
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM270540
Synonyms:
N-(3-(5-chloro-4-(2-(2- (dimethylamino)-2-oxoacetyl) phenylamino)pyrimidin-2- ylamino)-4-methoxyphenyl) acrylamide | US10059688, Example 67 | US9783524, Example 67
Type:
Small organic molecule
Emp. Form.:
C24H23ClN6O4
Mol. Mass.:
494.93
SMILES:
COc1ccc(NC(=O)C=C)cc1Nc1ncc(Cl)c(Nc2ccccc2C(=O)C(=O)N(C)C)n1
Structure:
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