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Target
Proto-oncogene tyrosine-protein kinase Src [251-533,T338M]
Ligand
BDBM13216
Substrate
biotinylated poly-Glu-Tyr
Meas. Tech.
Kinetics Assay for IC50 Determination
pH
7.0000±n/a
Temperature
296.1500±n/a K
IC50
480±400 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:
SRC_CHICK | SRC | Proto-oncogene tyrosine-protein kinase Src | Src Mutant (T338M)
Type:
Tyr protein kinase
Mol. Mass.:
32390.51
Organism:
Chicken
Description:
Mutation of T338M was introduced by site-directed mutagenesis and confirmed by sequence analysis.
Residue:
283
Sequence:
QTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTTRVAIKTLKPGTMSPEAFLQEAQVMKKLRHEKLVQLYAVVSEEPIYIVMEYMSKGSLLDFLKGEMGKYLRLPQLVDMAAQIASGMAYVERMNYVHRDLRAANILVGENLVCKVADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELTTKGRVPYPGMVNREVLDQVERGYRMPCPPECPESLHDLMCQCWRKDPEERPTFEYLQAFLEDYFTSTEPQYQPGENL
  
Inhibitor
Name:
BDBM13216
Synonyms:
N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide | cid_3062316 | N-(2-chloro-6-methylphenyl)-2-({6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4-yl}amino)-1,3-thiazole-5-carboxamide | CHEMBL1421 | DASATINIB | BMS-354825 | US10294227, Code Dasatinib | med.21724, Compound Dasatinib | US20230348453, Compound A8
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
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