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Target
Proto-oncogene tyrosine-protein kinase Src
Ligand
BDBM6542
Substrate
Biotinylated peptide substrate
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
1000±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
More Info.:
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:
BDBM6542
Synonyms:
3-quinolinecarbonitrile deriv. 7a | 4-{[(3,5-dichlorophenyl)methyl]amino}-7-[(E)-2-(pyridin-4-yl)ethenyl]quinoline-3-carbonitrile
Type:
Small organic molecule
Emp. Form.:
C24H16Cl2N4
Mol. Mass.:
431.317
SMILES:
Clc1cc(Cl)cc(CNc2c(cnc3cc(\C=C\c4ccncc4)ccc23)C#N)c1
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