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Target
Tyrosine-protein kinase Lck [245-498]
Ligand
BDBM14958
Substrate
Gastrin Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
210±n/a nM
Citation
 Cee, VJ; Albrecht, BK; Geuns-Meyer, S; Hughes, P; Bellon, S; Bready, J; Caenepeel, S; Chaffee, SC; Coxon, A; Emery, M; Fretland, J; Gallant, P; Gu, Y; Hodous, BL; Hoffman, D; Johnson, RE; Kendall, R; Kim, JL; Long, AM; McGowan, D; Morrison, M; Olivieri, PR; Patel, VF; Polverino, A; Powers, D; Rose, P; Wang, L; Zhao, H Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase. J Med Chem 50:627-40 (2007) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Lck [245-498]
Synonyms:
LCK | LCK_HUMAN | LSK | Lymphocyte cell-specific protein-tyrosine kinase | Proto-oncogene tyrosine-protein kinase LCK | T cell-specific protein-tyrosine kinase | p56-LCK
Type:
Kinase domain
Mol. Mass.:
29166.29
Organism:
Homo sapiens (Human)
Description:
Recombinant kinase domain (amino acid 245 to 498) fused with GST tag.
Residue:
254
Sequence:
LKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFF
  
Inhibitor
Name:
BDBM14958
Synonyms:
5-[(2-aminopyrimidin-5-yl)ethynyl]-2-fluoro-N-[2-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]benzamide | 5-[2-(2-aminopyrimidin-5-yl)ethynyl]-2-fluoro-N-[2-(4-methylpiperazin-1-yl)-5-(trifluoromethyl)phenyl]benzamide | alkynylpyrimidine amide 6i
Type:
Small organic molecule
Emp. Form.:
C25H22F4N6O
Mol. Mass.:
498.4754
SMILES:
CN1CCN(CC1)c1ccc(cc1NC(=O)c1cc(ccc1F)C#Cc1cnc(N)nc1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Gastrin Peptide Substrate
Synonyms:
Biotinylated gastrin peptide substrate | biotinylated gastrin substrate | gastrin substrate
Type:
Peptide
Mol. Mass.:
1823.88
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINEEEEAYGWLDF