Category Archives: Kinase Inhibitors

Discovery of PF-04691502 (PI3K/mTOR dual inhibitor)

Posted on March 17, 2011 by mcb

Rapamycin and it’s analogues (or rapalogues e.g. CCI-779) modulate the phosphatidylinositol 3-kinase (PI3K) signalling cascade by binding to an allosteric site on the mTORC1 complex (Mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, forms two functional complexes, … Continue reading →

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TAK-733 & CH4987655 (Allosteric MEK Inhibitors)

Posted on February 4, 2011 by mcb

The mitogen-activated protein kinase (MAPK) signalling cascade is one of the key pathways regulating cell proliferation and differentiation and aberrant activation of this pathway is implicated in a number of cancers. Targeting components of the cascade thus has the potential … Continue reading →

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Improved PK profile through fluorine and deuterium incorporation

Posted on December 15, 2010 by mcb

Compound (1) was identified by scientists at Merck as a potent Aurora kinase inhibitor with the potential to be useful in the treatment of various cancers.  In this paper the authors reveal that the basic amine which is key to good … Continue reading →

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Characterisation of p38 switch pocket inhibitors

Posted on July 23, 2010 by mcb

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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