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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM4054
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
pH
7.4±n/a
Temperature
298.15±n/a K
IC50
340±n/a nM
Citation
 Boschelli, DH; Wu, Z; Klutchko, SR; Showalter, HD; Hamby, JM; Lu, GH; Major, TC; Dahring, TK; Batley, B; Panek, RL; Keiser, J; Hartl, BG; Kraker, AJ; Klohs, WD; Roberts, BJ; Patmore, S; Elliott, WL; Steinkampf, R; Bradford, LA; Hallak, H; Doherty, AM Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors. J Med Chem 41:4365-77 (1998) [PubMed]  Article 
Target
Name:
Proto-oncogene tyrosine-protein kinase Src
Synonyms:
Calmodulin/Proto-oncogene tyrosine-protein kinase Src | Protein cereblon/Tyrosine-protein kinase SRC | Proto-oncogene c-Src | Proto-oncogene tyrosine-protein kinase Src (c-Src) | SRC | SRC1 | SRC_HUMAN | Tyrosine-protein kinase Src (SRC) | V-src sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog (avian) | c-Src | p60-Src | pp60c-src
Type:
Protein
Mol. Mass.:
59838.60
Organism:
Homo sapiens (Human)
Description:
P12931
Residue:
536
Sequence:
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM4054
Synonyms:
2-Amino-6-(2,6-dichlorophenyl)-7-oxo-7H-pyrido[2,3-d]pyrimidin-8-yl]acetic acid methyl ester | methyl 2-[2-amino-6-(2,6-dichlorophenyl)-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-8-yl]acetate | pyrido[2,3-d]pyrimidin-7-one deriv. 9
Type:
Small organic molecule
Emp. Form.:
C16H12Cl2N4O3
Mol. Mass.:
379.197
SMILES:
COC(=O)Cn1c2nc(N)ncc2cc(-c2c(Cl)cccc2Cl)c1=O |(2.35,-3.56,;1.02,-2.79,;-.32,-3.56,;-.32,-5.1,;-1.65,-2.79,;-1.65,-1.25,;-2.98,-.48,;-4.32,-1.25,;-5.65,-.48,;-6.98,-1.25,;-5.65,1.06,;-4.32,1.83,;-2.98,1.06,;-1.65,1.83,;-.32,1.06,;1.02,1.83,;1.02,3.37,;-.32,4.14,;2.35,4.14,;3.69,3.37,;3.69,1.83,;2.35,1.06,;2.35,-.48,;-.32,-.48,;1.02,-1.25,)|
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