Reaction Details
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Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM3452
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
12±n/a nM
Citation
Schroeder, MC; Hamby, JM; Connolly, CJ; Grohar, PJ; Winters, RT; Barvian, MR; Moore, CW; Boushelle, SL; Crean, SM; Kraker, AJ; Driscoll, DL; Vincent, PW; Elliott, WL; Lu, GH; Batley, BL; Dahring, TK; Major, TC; Panek, RL; Doherty, AM; Showalter, HD Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. J Med Chem 44:1915-26 (2001) [PubMed] Article More Info.:
Target
Name:
Proto-oncogene tyrosine-protein kinase Src
Synonyms:
Protein cereblon/Tyrosine-protein kinase SRC | Calmodulin/Proto-oncogene tyrosine-protein kinase Src | Proto-oncogene c-Src | Proto-oncogene tyrosine-protein kinase Src (c-Src) | Tyrosine-protein kinase Src (SRC) | V-src sarcoma (Schmidt-Ruppin A-2) viral oncogene homolog (avian) | c-Src | p60-Src | pp60c-src | SRC_HUMAN | SRC | SRC1
Type:
Protein
Mol. Mass.:
59838.60
Organism:
Human
Description:
P12931
Residue:
536
Sequence:
MGSNKSKPKDASQRRRSLEPAENVHGAGGGAFPASQTPSKPASADGHRGPSAAFAPAAAEPKLFGGFNSSDTVTSPQRAGPLAGGVTTFVALYDYESRTETDLSFKKGERLQIVNNTEGDWWLAHSLSTGQTGYIPSNYVAPSDSIQAEEWYFGKITRRESERLLLNAENPRGTFLVRESETTKGAYCLSVSDFDNAKGLNVKHYKIRKLDSGGFYITSRTQFNSLQQLVAYYSKHADGLCHRLTTVCPTSKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVTEYMSKGSLLDFLKGETGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKEPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
Inhibitor
Name:
BDBM3452
Synonyms:
1-cyclohexyl-3-[6-(2,6-dichlorophenyl)-2-{[4-(diethylamino)butyl]amino}pyrido[2,3-d]pyrimidin-7-yl]urea | 6-arylpyrido[2,3-d]pyrimidine deriv. 34
Type:
Small organic molecule
Emp. Form.:
C28H37Cl2N7O
Mol. Mass.:
557.24
SMILES:
CCN(CC)CCCCNc1ncc2cc(-c3c(Cl)cccc3Cl)c(NC(=O)NC3CCCCC3)nc2n1
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
