| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Epidermal growth factor receptor |
|---|
| Ligand | BDBM50131842 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1526584 (CHEMBL3635803) |
|---|
| IC50 | 521±n/a nM |
|---|
| Citation |  Wurz, RP; Pettus, LH; Ashton, K; Brown, J; Chen, JJ; Herberich, B; Hong, FT; Hu-Harrington, E; Nguyen, T; St Jean, DJ; Tadesse, S; Bauer, D; Kubryk, M; Zhan, J; Cooke, K; Mitchell, P; Andrews, KL; Hsieh, F; Hickman, D; Kalyanaraman, N; Wu, T; Reid, DL; Lobenhofer, EK; Andrews, DA; Everds, N; Guzman, R; Parsons, AT; Hedley, SJ; Tedrow, J; Thiel, OR; Potter, M; Radinsky, R; Beltran, PJ; Tasker, AS Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett6:987-92 (2015) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Epidermal growth factor receptor |
|---|
| 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: | MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEV
VLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALA
VLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDF
QNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGC
TGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYV
VTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFK
NCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAF
ENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKL
FGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCN
LLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVM
GENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVV
ALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGS
GAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGI
CLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAA
RNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSY
GVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPK
FRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQ
QGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTED
SIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLN
TVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRV
APQSSEFIGA
|
|
|
|---|
| BDBM50131842 |
|---|
| n/a |
|---|
| Name | BDBM50131842 |
|---|
| Synonyms: | CHEMBL3633151 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C29H33N7O3 |
|---|
| Mol. Mass. | 527.6174 |
|---|
| SMILES | COc1cc(ccc1Nc1ncc2c(C)cc(=O)n(-c3cccc(NC(=O)C=C)c3)c2n1)N(C)CCN(C)C |
|---|
| Structure | 
|
|---|
Search and Browse
