Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor [1-18,20-745,747-749,751-1210,T790M]
Ligand
BDBM495016
Substrate
n/a
Meas. Tech.
TR-FRET Assay for ERBB Kinases
IC50
4.90±n/a nM
Citation
 Crew, AP; Zimmermann, K; Wang, J; Crews, CM; Jaime-Figueroa, S; Burslem, G EGFR proteolysis targeting chimeric molecules and associated methods of use US Patent  US10994015 Publication Date 5/4/2021 
Target
Name:
Epidermal growth factor receptor [1-18,20-745,747-749,751-1210,T790M]
Synonyms:
EGFR | EGFR Delta 19/746/750 T790M | EGFR_HUMAN | ERBB | ERBB1 | HER1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
134007.35
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
1207
Sequence:
MRPSGTAGAALLALLAALPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKLRETSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLIMQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM495016
Synonyms:
US10994015, Example 312
Type:
Small organic molecule
Emp. Form.:
C42H47N13O6S
Mol. Mass.:
861.971
SMILES:
CC(C)n1nc(N2CCN(CC3CCN(CC3)c3ccc4C(=O)N(C5CCC(=O)NC5=O)C(=O)c4c3)CC2)c2cnc(Nc3ccnc(n3)-c3cnn(c3)S(=O)(=O)C3CC3)cc12
Structure:
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