Reaction Details Report a problem with these data
Target
Tyrosine-protein kinase Lck
Ligand
BDBM14949
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
0.2±n/a nM
Citation
 DiMauro, EF; Newcomb, J; Nunes, JJ; Bemis, JE; Boucher, C; Chai, L; Chaffee, SC; Deak, HL; Epstein, LF; Faust, T; Gallant, P; Gore, A; Gu, Y; Henkle, B; Hsieh, F; Huang, X; Kim, JL; Lee, JH; Martin, MW; McGowan, DC; Metz, D; Mohn, D; Morgenstern, KA; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, PE; Schneider, S; Tomlinson, SA; Tudor, YY; Turci, SM; Welcher, AA; Zhao, H; Zhu, L; Zhu, X Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. J Med Chem 51:1681-94 (2008) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Lck
Synonyms:
2.7.10.2 | LCK | LCK_HUMAN | LSK | Leukocyte C-terminal Src kinase | Lymphocyte cell-specific protein-tyrosine kinase | Lymphocyte-specific protein tyrosine kinase | P56-LCK | Protein YT16 | Proto-oncogene Lck | Proto-oncogene tyrosine-protein kinase LCK | Src/Lck kinase | T cell-specific protein-tyrosine kinase
Type:
n/a
Mol. Mass.:
57987.83
Organism:
Homo sapiens (Human)
Description:
P06239
Residue:
509
Sequence:
MGCGCSSHPEDDWMENIDVCENCHYPIVPLDGKGTLLIRNGSEVRDPLVTYEGSNPPASPLQDNLVIALHSYEPSHDGDLGFEKGEQLRILEQSGEWWKAQSLTTGQEGFIPFNFVAKANSLEPEPWFFKNLSRKDAERQLLAPGNTHGSFLIRESESTAGSFSLSVRDFDQNQGEVVKHYKIRNLDNGGFYISPRITFPGLHELVRHYTNASDGLCTRLSRPCQTQKPQKPWWEDEWEVPRETLKLVERLGAGQFGEVWMGYYNGHTKVAVKSLKQGSMSPDAFLAEANLMKQLQHQRLVRLYAVVTQEPIYIITEYMENGSLVDFLKTPSGIKLTINKLLDMAAQIAEGMAFIEERNYIHRDLRAANILVSDTLSCKIADFGLARLIEDNEYTAREGAKFPIKWTAPEAINYGTFTIKSDVWSFGILLTEIVTHGRIPYPGMTNPEVIQNLERGYRMVRPDNCPEELYQLMRLCWKERPEDRPTFDYLRSVLEDFFTATEGQYQPQP
  
Inhibitor
Name:
BDBM14949
Synonyms:
2-aminoquinazoline 5 | 3-(2-aminoquinazolin-6-yl)-4-methyl-N-[3-(trifluoromethyl)phenyl]benzamide | CHEMBL385937 | JMC511681 Compound 34
Type:
Small organic molecule
Emp. Form.:
C23H17F3N4O
Mol. Mass.:
422.4025
SMILES:
Cc1ccc(cc1-c1ccc2nc(N)ncc2c1)C(=O)Nc1cccc(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated gastrin substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2100.22
Organism:
n/a
Description:
n/a
Residue:
17
Sequence:
ITINYLEEEEAYGWLDF