Target
Tyrosine-protein kinase Lck
Ligand
BDBM17717
Substrate
biotinylated gastrin substrate
Meas. Tech.
HTRF Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
22±n/a nM
Citation
 Martin, MWNewcomb, JNunes, JJBemis, JEMcGowan, DCWhite, RDBuchanan, JLDiMauro, EFBoucher, CFaust, THsieh, FHuang, XLee, JHSchneider, STurci, SMZhu, X Discovery of novel 2,3-diarylfuro[2,3-b]pyridin-4-amines as potent and selective inhibitors of Lck: synthesis, SAR, and pharmacokinetic properties. Bioorg Med Chem Lett 17:2299-304 (2007) [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:
BDBM17717
Synonyms:
2,3-Diarylfuro[2,3-b]pyridine-4-amine, 13 | 2-{4-[2-(morpholin-4-yl)ethoxy]phenyl}-3-phenyl-N-[2-(piperazin-1-yl)ethyl]furo[2,3-b]pyridin-4-amine
Type:
Small organic molecule
Emp. Form.:
C31H37N5O3
Mol. Mass.:
527.6572
SMILES:
C(CN1CCNCC1)Nc1ccnc2oc(c(-c3ccccc3)c12)-c1ccc(OCCN2CCOCC2)cc1
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