Target
Tyrosine-protein kinase Lck [245-498]
Ligand
BDBM14948
Substrate
Gastrin Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
IC50
<1±n/a nM
Citation
 Cee, VJAlbrecht, BKGeuns-Meyer, SHughes, PBellon, SBready, JCaenepeel, SChaffee, SCCoxon, AEmery, MFretland, JGallant, PGu, YHodous, BLHoffman, DJohnson, REKendall, RKim, JLLong, AMMcGowan, DMorrison, MOlivieri, PRPatel, VFPolverino, APowers, DRose, PWang, LZhao, 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:
BDBM14948
Synonyms:
4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyridin-2-yloxy)-N-(3-(trifluoromethyl)phenyl)benzamide | 4-methyl-3-({3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl}oxy)-N-[3-(trifluoromethyl)phenyl]benzamide | pyridinyl pyrimidine 15 | pyridylpyrimidine ether 4
Type:
Small organic molecule
Emp. Form.:
C25H20F3N5O2
Mol. Mass.:
479.4538
SMILES:
CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)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