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Target
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M]
Ligand
BDBM31827
Substrate
biotinylated poly-Glu-Tyr
Meas. Tech.
Kinetics Assay for IC50 Determination
pH
7±n/a
Temperature
296.15±n/a K
IC50
101±4 nM
Citation
 Getlik, M; Grütter, C; Simard, JR; Klüter, S; Rabiller, M; Rode, HB; Robubi, A; Rauh, D Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc. J Med Chem 52:3915-26 (2009) [PubMed]  Article 
Target
Name:
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M]
Synonyms:
Proto-oncogene tyrosine-protein kinase Src | SRC | SRC_CHICK | Src Mutant (T338M)
Type:
Tyr protein kinase
Mol. Mass.:
32390.51
Organism:
Gallus gallus (Chicken)
Description:
Mutation of T338M was introduced by site-directed mutagenesis and confirmed by sequence analysis.
Residue:
283
Sequence:
QTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVMEYMSKGSLLDFLKGEMGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKDPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM31827
Synonyms:
quinazoline-pyrazolourea hybrid compound, 3a
Type:
Small organic molecule
Emp. Form.:
C29H28N8O3
Mol. Mass.:
536.5844
SMILES:
Cc1cccc(c1)-n1nc(cc1NC(=O)Nc1ccc(Nc2ncnc3ccc(cc23)[N+]([O-])=O)cc1)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated poly-Glu-Tyr
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA