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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM6539
Substrate
Biotinylated peptide substrate
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
11±n/a nM
Citation
 Barrios Sosa, AC; Boschelli, DH; Wu, B; Wang, Y; Golas, JM Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor. Bioorg Med Chem Lett 15:1743-7 (2005) [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:
BDBM6539
Synonyms:
4-[(E)-2-{3-cyano-6-methoxy-4-[(3,4,5-trimethoxyphenyl)amino]quinolin-7-yl}ethenyl]-1-oxidopyridin-1-ium | ethenyl-4-phenylamino-3-quinolinecarbonitrile 20c
Type:
Small organic molecule
Emp. Form.:
C27H24N4O5
Mol. Mass.:
484.5033
SMILES:
COc1cc2c(Nc3cc(OC)c(OC)c(OC)c3)c(cnc2cc1\C=C\c1cc[n+]([O-])cc1)C#N
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated peptide substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2353.23
Organism:
n/a
Description:
Biotinylated peptide corresponding to residues 6 to 20 of Cdk1. 100 uM ATP as co-substrate.
Residue:
21
Sequence:
ITINKVEKIGEGTYGVVYKCH