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Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2010 ; 1 (7): 350-4 Nephropedia Template TP
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Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1 #MMPMID24900218
Blackaby WP; Lewis RT; Thomson JL; Jennings AS; Goodacre SC; Street LJ; MacLeod AM; Pike A; Wood S; Thomas S; Brown TA; Smith A; Pillai G; Almond S; Guscott MR; Burns HD; Eng W; Ryan C; Cook J; Hamill TG
ACS Med Chem Lett 2010[Oct]; 1 (7): 350-4 PMID24900218show ga
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.