Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM4182
Substrate
Poly (GluTyr ) Substrate
Meas. Tech.
Kinase Inhibition Assay
IC50
550±n/a nM
Citation
 Thompson, AMRewcastle, GWBoushelle, SLHartl, BGKraker, AJLu, GHBatley, BLPanek, RLShowalter, HDDenny, WA Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src). J Med Chem 43:3134-47 (2000) [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:
BDBM4182
Synonyms:
1,6-naphthyridin-2(1H)-one deriv. 7o | 3-(2,6-Dichlorophenyl)-1-methyl-7-(4-pyridinylamino)-1,6-naphthyridin-2(1H)-one | 3-(2,6-dichlorophenyl)-1-methyl-7-(pyridin-4-ylamino)-1,2-dihydro-1,6-naphthyridin-2-one
Type:
Small organic molecule
Emp. Form.:
C20H14Cl2N4O
Mol. Mass.:
397.257
SMILES:
Cn1c2cc(Nc3ccncc3)ncc2cc(-c2c(Cl)cccc2Cl)c1=O |(-1.18,-3.43,;-1.18,-1.89,;-2.52,-1.12,;-3.85,-1.95,;-5.18,-1.18,;-6.52,-1.95,;-7.85,-1.18,;-7.85,.36,;-9.18,1.13,;-10.52,.36,;-10.52,-1.18,;-9.18,-1.95,;-5.18,.36,;-3.85,1.13,;-2.52,.42,;-1.18,1.19,;.15,.42,;1.48,1.19,;1.48,2.73,;.15,3.5,;2.82,3.5,;4.15,2.73,;4.15,1.19,;2.82,.42,;2.82,-1.12,;.15,-1.12,;1.48,-1.89,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly (GluTyr ) Substrate
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
5 uM ATP containing 0.2 uCi labeled [32P]ATP as co-substrate.
Residue:
3
Sequence:
NA