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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM6114
Substrate
Biotinylated peptide substrate
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
2.3±n/a nM
Citation
 Boschelli, DH; Wu, B; Ye, F; Wang, Y; Golas, JM; Lucas, J; Boschelli, F Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem 49:7868-76 (2006) [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:
BDBM6114
Synonyms:
3-quinolinecarbonitrile analog 2b | 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-{5-[(4-methylpiperazin-1-yl)methyl]thiophen-2-yl}quinoline-3-carbonitrile | 7-thienyl-3-quinolinecarbonitrile 16
Type:
Small organic molecule
Emp. Form.:
C27H25Cl2N5OS
Mol. Mass.:
538.491
SMILES:
COc1cc(Nc2c(cnc3cc(ccc23)-c2ccc(CN3CCN(C)CC3)s2)C#N)c(Cl)cc1Cl
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