Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Article Details

Citation

Verhoest PR, Proulx-Lafrance C, Corman M, Chenard L, Helal CJ, Hou X, Kleiman R, Liu S, Marr E, Menniti FS, Schmidt CJ, Vanase-Frawley M, Schmidt AW, Williams RD, Nelson FR, Fonseca KR, Liras S

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

J Med Chem. 2009 Dec 24;52(24):7946-9. doi: 10.1021/jm9015334.

PubMed ID
19919087 [ View in PubMed
]
Abstract

By use of chemical enablement and prospective design, a novel series of selective, brain penetrant PDE9A inhibitors have been identified that are capable of producing in vivo elevations of brain cGMP.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9AO76083Details