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Target
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M,S345C]
Ligand
BDBM4583
Substrate
Tyr 02 Substrate Peptide
Meas. Tech.
Src IC50 Determination
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
5710±n/a nM
Citation
 Michalczyk, A; Klüter, S; Rode, HB; Simard, JR; Grütter, C; Rabiller, M; Rauh, D Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR. Bioorg Med Chem 16:3482-8 (2008) [PubMed]  Article 
Target
Name:
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M,S345C]
Synonyms:
Proto-oncogene tyrosine-protein kinase Src | SRC | SRC_CHICK | Src Mutant (S345C/T338M) | cSRC-DM
Type:
Tyr protein kinase
Mol. Mass.:
32732.47
Organism:
Gallus gallus (Chicken)
Description:
Mutations of T338 to methionine and S345 to cysteine were introduced by site-directed mutagenesis and confirmed by sequence analysis.
Residue:
286
Sequence:
GHMQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVMEYMSKGCLLDFLKGEMGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKDPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM4583
Synonyms:
(2E)-N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide | 4-anilinoquinazoline deriv. 16a | BMC163482 Compound 2 | CHEMBL94061
Type:
Small organic molecule
Emp. Form.:
C20H20BrN5O
Mol. Mass.:
426.31
SMILES:
CN(C)C\C=C\C(=O)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Tyr 02 Substrate Peptide
Synonyms:
n/a
Type:
FRET-peptide substrate
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA