The on target in vitro pharmacology

2019-07-15

The on target in vitro pharmacology of 18 was then further explored, first in respect of murine CRTh2 receptor activity (Table 5), where similar levels of activity were found in both a binding and functional assay compared with the human orthologue, consistent with our earlier observations in the sulfonamide series.

Hymenialdisine the most potent inhibitor of parasite TgCK

2019-07-13

Hymenialdisine, the most potent inhibitor of parasite TgCK1 enzymes in vitro has no whole cell anti-parasitic activity (Table 2). Like purvalanol B however, this TNP-470 also displays poor activity against target enzymes in cultured cells. For example, in vitro IC50 values for inhibition of CDK5/cyclin and GSk3-β are in the 10–30nM range, but 50μM levels were required to detect the effects on CDK5/p35 and GSK-3 kinase inhibition in rat cortical neurons [39].

Hello world!

2018-07-29