Literature DB >> 24900218

Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

Wesley P Blackaby1, Richard T Lewis1, Joanne L Thomson1, Andrew S R Jennings1, Simon C Goodacre1, Leslie J Street1, Angus M MacLeod1, Andrew Pike1, Suzanne Wood1, Steve Thomas1, Terry A Brown1, Alison Smith1, Gopalan Pillai1, Sarah Almond1, Martin R Guscott1, H Donald Burns2, Waisi Eng2, Christine Ryan2, Jacquelynn Cook2, Terence G Hamill2.   

Abstract

Amalgamation of the structure-activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy of GlyT1 transporters in rhesus monkey as determined by displacement of a PET tracer ligand.

Entities:  

Keywords:  DCCCyB; GlyT1; Inhibitor; PET tracer ligand; structure−activity relationship

Year:  2010        PMID： 24900218      PMCID： PMC4007840          DOI： 10.1021/ml1001085

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


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9.  Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.

Authors:  Joanne L Thomson; Wesley P Blackaby; Andrew S R Jennings; Simon C Goodacre; Andrew Pike; Steve Thomas; Terry A Brown; Alison Smith; Gopalan Pillai; Leslie J Street; Richard T Lewis
Journal:  Bioorg Med Chem Lett       Date:  2009-02-28       Impact factor: 2.823

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