Reaction Details Report a problem with these data
Target
Epidermal growth factor receptor
Ligand
BDBM270571
Substrate
n/a
Meas. Tech.
High Throughput EGFR Biochemical Assay
IC50
11.0±n/a nM
Citation
Balan, G; Chou, C; Kim, M; Kirschberg, TA; Link, JO; Phillips, G; Saito, RD; Squires, NH; Taylor, JG; Watkins, WJ; Wright, NE Cot modulators and methods of use thereof US Patent US10577352 Publication Date 3/3/2020
More Info.:
Target
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:
Human
Description:
P00533
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
Inhibitor
Name:
BDBM270571
Synonyms:
(S)-N6-((1- cyclopropyl-1H- 1,2,3-triazol-4-yl)(4- fluorophenyl)methyl- d)-N4-((4- methyltetrahydro- 2H-pyran-4- yl)methyl)quinazoline- 4,6-diamine | US10059695, I-3 | US10577352, Compound I-3
Type:
Small organic molecule
Emp. Form.:
C27H30FN7O
Mol. Mass.:
487.5718
SMILES:
CC1(CNc2ncnc3ccc(NC(c4cn(nn4)C4CC4)c4ccc(F)cc4)cc23)CCOCC1