Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM6084
Substrate
Biotinylated peptide substrate
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
pH
7.5±n/a
Temperature
310.15±n/a K
IC50
50±2 nM
Citation
 Boschelli, DHWu, BBarrios Sosa, ACDurutlic, HYe, FRaifeld, YGolas, JMBoschelli, F Identification of 7-phenylaminothieno- [3,2-b]pyridine-6-carbonitriles as a new class of Src kinase inhibitors. J Med Chem 47:6666-8 (2004) [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:
BDBM6084
Synonyms:
7-[(2,4-dichlorophenyl)amino]-2-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}thieno[3,2-b]pyridine-6-carbonitrile | 7-phenylaminothieno[3,2-b]pyridine-6-carbonitrile 4 | thieno[3,2-b]pyridine-6-carbonitrile 37
Type:
Small organic molecule
Emp. Form.:
C26H23Cl2N5S
Mol. Mass.:
508.465
SMILES:
CN1CCN(Cc2ccc(cc2)-c2cc3ncc(C#N)c(Nc4ccc(Cl)cc4Cl)c3s2)CC1
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