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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM6088
Substrate
Biotinylated peptide substrate
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
7.2±0.07 nM
Citation
 Boschelli, DH; Wu, B; Barrios Sosa, AC; Durutlic, H; Chen, JJ; Wang, Y; Golas, JM; Lucas, J; Boschelli, F Synthesis and Src kinase inhibitory activity of 2-phenyl- and 2-thienyl-7-phenylaminothieno[3,2-b]pyridine-6-carbonitriles. J Med Chem 48:3891-902 (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:
BDBM6088
Synonyms:
7-[(2,4-Dichloro-5-methoxyphenyl)amino]-2-{5-[(4-methylpiperazin-1-yl)methyl]thien-3-yl}thieno[3,2-b]pyridine-6-carbonitrile | 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-{5-[(4-methylpiperazin-1-yl)methyl]thiophen-3-yl}thieno[3,2-b]pyridine-6-carbonitrile | 7-phenylaminothieno[3,2-b]pyridine-6-carbonitrile 34 | thieno[3,2-b]-pyridine-6-carbonitrile 2a
Type:
Small organic molecule
Emp. Form.:
C25H23Cl2N5OS2
Mol. Mass.:
544.519
SMILES:
COc1cc(Nc2c(cnc3cc(sc23)-c2csc(CN3CCN(C)CC3)c2)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