Target
Epidermal growth factor receptor
Ligand
BDBM3064
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
8700±n/a nM
Citation
 Klutchko, SRHamby, JMBoschelli, DHWu, ZKraker, AJAmar, AMHartl, BGShen, CKlohs, WDSteinkampf, RWDriscoll, DLNelson, JMElliott, WLRoberts, BJStoner, CLVincent, PWDykes, DJPanek, RLLu, GHMajor, TCDahring, TKHallak, HBradford, LAShowalter, HDDoherty, AM 2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity. J Med Chem 41:3276-92 (1998) [PubMed]  Article 
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:
Homo sapiens (Human)
Description:
P00533
Residue:
1210
Sequence:
MRPSGTAGAALLALLAALCPASRALEEKKVCQGTSNKLTQLGTFEDHFLSLQRMFNNCEVVLGNLEITYVQRNYDLSFLKTIQEVAGYVLIALNTVERIPLENLQIIRGNMYYENSYALAVLSNYDANKTGLKELPMRNLQEILHGAVRFSNNPALCNVESIQWRDIVSSDFLSNMSMDFQNHLGSCQKCDPSCPNGSCWGAGEENCQKLTKIICAQQCSGRCRGKSPSDCCHNQCAAGCTGPRESDCLVCRKFRDEATCKDTCPPLMLYNPTTYQMDVNPEGKYSFGATCVKKCPRNYVVTDHGSCVRACGADSYEMEEDGVRKCKKCEGPCRKVCNGIGIGEFKDSLSINATNIKHFKNCTSISGDLHILPVAFRGDSFTHTPPLDPQELDILKTVKEITGFLLIQAWPENRTDLHAFENLEIIRGRTKQHGQFSLAVVSLNITSLGLRSLKEISDGDVIISGNKNLCYANTINWKKLFGTSGQKTKIISNRGENSCKATGQVCHALCSPEGCWGPEPRDCVSCRNVSRGRECVDKCNLLEGEPREFVENSECIQCHPECLPQAMNITCTGRGPDNCIQCAHYIDGPHCVKTCPAGVMGENNTLVWKYADAGHVCHLCHPNCTYGCTGPGLEGCPTNGPKIPSIATGMVGALLLLLVVALGIGLFMRRRHIVRKRTLRRLLQERELVEPLTPSGEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGLAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQGFFSSPSTSRTPLLSSLSATSNNSTVACIDRNGLQSCPIKEDSFLQRYSSDPTGALTEDSIDDTFLPVPEYINQSVPKRPAGSVQNPVYHNQPLNPAPSRDPHYQDPHSTAVGNPEYLNTVQPTCVNSTFDSPAHWAQKGSHQISLDNPDYQQDFFPKEAKPNGIFKGSTAENAEYLRVAPQSSEFIGA
  
Inhibitor
Name:
BDBM3064
Synonyms:
2-aminopyrido[2,3-d]pyrimidin-7(8H)-one 31 | 6-(2,6-dichlorophenyl)-8-methyl-2-{[3-(4-methylpiperazin-1-yl)propyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | CHEMBL299194 | PD 166285 analog
Type:
Small organic molecule
Emp. Form.:
C22H26Cl2N6O
Mol. Mass.:
461.387
SMILES:
CN1CCN(CCCNc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)CC1 |(-10.37,-10.59,;-9.97,-9.1,;-8.49,-8.7,;-8.09,-7.22,;-9.18,-6.13,;-8.52,-4.79,;-8.92,-3.31,;-8.15,-1.97,;-8.15,-.43,;-6.82,.34,;-6.82,1.88,;-5.48,2.65,;-4.15,1.88,;-2.82,2.65,;-1.48,1.88,;-.15,2.65,;-.15,4.19,;-1.48,4.96,;1.18,4.96,;2.52,4.19,;2.52,2.65,;1.18,1.88,;1.18,.34,;-1.48,.34,;-.15,-.43,;-2.82,-.43,;-2.82,-1.97,;-4.15,.34,;-5.48,-.43,;-10.66,-6.53,;-11.06,-8.01,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly(E:Y)
Synonyms:
n/a
Type:
Random polymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
Random copolymer of glutamic acid and tyrosine (4:1). 50 uM ATP containing 0.4 uCi of [gamma-32P]ATP as co-substrate
Residue:
3
Sequence:
NA