Target
Tyrosine-protein kinase Lck
Ligand
BDBM17738
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
1±n/a nM
Citation
 Martin, MWNewcomb, JNunes, JJMcGowan, DCArmistead, DMBoucher, CBuchanan, JLBuckner, WChai, LElbaum, DEpstein, LFFaust, TFlynn, SGallant, PGore, AGu, YHsieh, FHuang, XLee, JHMetz, DMiddleton, SMohn, DMorgenstern, KMorrison, MJNovak, PMOliveira-dos-Santos, APowers, DRose, PSchneider, SSell, STudor, YTurci, SMWelcher, AAWhite, RDZack, DZhao, HZhu, LZhu, XGhiron, CAmouzegh, PErmann, MJenkins, JJohnston, DNapier, SPower, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem 49:4981-91 (2006) [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:
BDBM17738
Synonyms:
2,6-dimethylphenyl N-(2,4-dimethoxyphenyl)-N-[2-({4-[3-(dimethylamino)propoxy]phenyl}amino)pyrimidin-4-yl]carbamate | 2-aminopyrimidine carbamate, 37
Type:
Small organic molecule
Emp. Form.:
C32H37N5O5
Mol. Mass.:
571.6667
SMILES:
COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3ccc(OCCCN(C)C)cc3)n2)c(OC)c1
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