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Target
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M,S345C]
Ligand
BDBM4567
Substrate
Tyr 02 Substrate Peptide
Meas. Tech.
Src IC50 Determination
pH
7.5±n/a
Temperature
296.15±n/a K
IC50
2810±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:
BDBM4567
Synonyms:
4-anilinoquinazoline deriv. 2 | BMC163482 Compound 1 | CHEMBL285063 | N-{4-[(3-bromophenyl)amino]quinazolin-6-yl}prop-2-enamide | US9422297, PD168393
Type:
Small organic molecule
Emp. Form.:
C17H13BrN4O
Mol. Mass.:
369.215
SMILES:
Brc1cccc(Nc2ncnc3ccc(NC(=O)C=C)cc23)c1
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