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Target
Tyrosine-protein kinase Lck [245-498]
Ligand
BDBM14967
Substrate
Gastrin Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
<1±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:
BDBM14967
Synonyms:
3-(2-(3H-Imidazo[4,5-b]pyridin-6-yl)ethynyl)-4-methyl-N-(3-(trifluoromethyl)phenyl)benzamide | 3-(2-{3H-imidazo[4,5-b]pyridin-6-yl}ethynyl)-4-methyl-N-[3-(trifluoromethyl)phenyl]benzamide | heterocyclic akynyl amide 13b
Type:
Small organic molecule
Emp. Form.:
C23H15F3N4O
Mol. Mass.:
420.3866
SMILES:
Cc1ccc(cc1C#Cc1cnc2nc[nH]c2c1)C(=O)Nc1cccc(c1)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