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    Bioorg Med Chem Lett. 2008 Jan 1;18(1):350-4. Epub 2007 Oct 24.

    Uncovering false positives on a virtual screening search for cruzain inhibitors.

    Source

    Departamento de Química Fundamental, Instituto de Química, Universidade de São Paulo, C.P. 26077, 05513-970 São Paulo, SP, Brazil.

    Abstract

    Some unexpected promiscuous inhibitors were observed in a virtual screening protocol applied to select cruzain inhibitors from the ZINC database. Physical-chemical and pharmacophore model filters were used to reduce the database size. The selected compounds were docked into the cruzain active site. Six hit compounds were tested as inhibitors. Although the compounds were designed to be nucleophilically attacked by the catalytic cysteine of cruzain, three of them showed typical promiscuous behavior, revealing that false positives are a prevalent concern in VS programs.

    PMID:
    17981033
    [PubMed - indexed for MEDLINE]

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