Monthly Archives: July 2010

Characterisation of p38 switch pocket inhibitors


Doramapimod (BIRB-796), from Boehringer Ingelheim, was the first reported  inhibitor of p38 which did not bind to the canonical ATP site.  This opened up the prospect of allosteric inhibition of kinases as a viable approach to identifying novel drug candidates. This … Continue reading

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The Discovery of RG1678 (Gly-T1 inhibitor)


In this interesting J.Med.Chem. article workers from Roche describe the optimisation of a series of benzoylpiperazines as Gly-T1 inhibitors for the treatment of schizophrenia culminating in the discovery of RG1678, the first potent and selective Gly-T1 inhibitor to demonstrate efficacy … Continue reading

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