|
KKB Hot Article: Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. |
 |
 |
 |
|
Written by KKB
|
|
Tuesday, 20 April 2010 19:33 |
| Citation: Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II. |
Authors: A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src-family kinases (SFKs). These type II inhibitors were optimized using a cellular Lck-dependent proliferation assay and are capable of inhibiting Lck at single-digit nanomolar concentrations. This scaffold is likely to serve a valuable template for developing potent inhibitors of a number of SFKs
|
| PubMed PMID: 19854052 |
Abstract: A series of 4-amino-6-benzimidazole-pyrimidines was designed to target lymphocyte-specific tyrosine kinase (Lck), a member of the Src-family kinases (SFKs). These type II inhibitors were optimized using a cellular Lck-dependent proliferation assay and are capable of inhibiting Lck at single-digit nanomolar concentrations. This scaffold is likely to serve a valuable template for developing potent inhibitors of a number of SFKs
|
Targets: HCK, INSR, KDR, LCK, LYN, SRC
Number of SAR data points: 363
Number of Targets: 6
|
|
|
Last Updated on Saturday, 20 August 2011 00:07 |
KinaseData.com RSS Feed