Tag Archives: Roche

TAK-733 & CH4987655 (Allosteric MEK Inhibitors)


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

Posted in Clinical Candidates, Enzyme Inhibitors, Kinase Inhibitors, Kinases | Tagged , , , , , , , , , , , , , , , , , , , , , | Leave a comment

Halogen Bonding


Investigators at Roche recently published a communication describing a systematic study of halogen bonding effects in protein-ligand complexes of human Cathepsin L (hCatL).  They found that an inhibitor incorporating a 4-chlorophenyl moiety enhanced binding affinity by a factor of 13, … Continue reading

Posted in Computational Methods, Enzyme Inhibitors, Med Chem Strategy | Tagged , , , | 12 Comments

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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