Structure-based design of a potent, selective, and brain penetrating PDE2 inhibitor with demonstrated target engagement

ACS Medicinal Chemistry Letters

Volumn 5, Issue 9, 2014, Pages 1049-1053

  Buijnsters, Peter ^a   De Angelis, Meri ^a   Langlois, Xavier ^a   Rombouts, Frederik J R ^a   Sanderson, Wendy ^a   Tresadern, Gary ^a   Ritchie, Alison ^b   Trabanco, Andrés A ^a   Vanhoof, Greet ^a   Roosbroeck, Yves Van ^a   Andrés, José Ignacio ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^b BioFocus DPI   (United Kingdom)

Author keywords

PDE2 inhibitor; phosphodiesterase 2; target engagement; 1,2,4 triazolo 4,3 a quinoxalines

Indexed keywords

CYCLIC GMP; PHOSPHODIESTERASE; PHOSPHODIESTERASE 10; PHOSPHODIESTERASE 11; PHOSPHODIESTERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BRAIN; BRAIN REGION; DRUG CLEARANCE; DRUG HALF LIFE; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; X RAY CRYSTALLOGRAPHY;

EID: 84907529646     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml500262u     Document Type: Article

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