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Target
Tyrosine-protein kinase Lck
Ligand
BDBM8796
Substrate
poly-Glu-Ala-Tyr
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
110±n/a nM
Citation
 Burchat, AF; Calderwood, DJ; Friedman, MM; Hirst, GC; Li, B; Rafferty, P; Ritter, K; Skinner, BS Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck - a selectivity insight. Bioorg Med Chem Lett 12:1687-90 (2002) [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:
BDBM8796
Synonyms:
3-(4-benzoylphenyl)-1-[4-(4-methylpiperazin-1-yl)cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidin-4-amine | Pyrazolo[3,4-d]pyrimidine 4
Type:
Small organic molecule
Emp. Form.:
C29H33N7O
Mol. Mass.:
495.6186
SMILES:
CN1CCN(CC1)[C@H]1CC[C@@H](CC1)n1nc(-c2ccc(cc2)C(=O)c2ccccc2)c2c(N)ncnc12 |r,wU:10.14,wD:7.7,(-.91,-10.51,;-1.37,-9.04,;-2.87,-8.71,;-3.34,-7.24,;-2.3,-6.11,;-.8,-6.44,;-.33,-7.91,;-2.72,-4.63,;-1.64,-3.52,;-2.06,-2.04,;-3.55,-1.66,;-4.63,-2.76,;-4.21,-4.25,;-4.03,-.2,;-3.12,1.05,;-4.03,2.3,;-3.55,3.76,;-4.69,4.8,;-4.36,6.3,;-2.89,6.77,;-1.75,5.73,;-2.08,4.23,;-2.56,8.27,;-3.7,9.31,;-1.1,8.74,;-.51,10.17,;1.01,10.37,;1.96,9.15,;1.37,7.73,;-.15,7.52,;-5.49,1.82,;-6.82,2.59,;-6.82,4.13,;-8.16,1.82,;-8.16,.28,;-6.82,-.49,;-5.49,.28,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
poly-Glu-Ala-Tyr
Synonyms:
poly-Glu-Ala-Tyr-biotin
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
It is a synthetic polymer of glutamic acid, alanine and tyrosine (poly-Glu-Ala-Tyr) that has been biotinylated.
Residue:
3
Sequence:
NA