Pan-Assay Interference Compounds (PAINS): Warning Signs in Biochemical-Pharmacological Evaluations
نویسندگان
چکیده
منابع مشابه
Seven Year Itch: Pan-Assay Interference Compounds (PAINS) in 2017—Utility and Limitations
Pan-Assay Interference Compounds (PAINS) are very familiar to medicinal chemists who have spent time fruitlessly trying to optimize these nonprogressible compounds. Electronic filters formulated to recognize PAINS can process hundreds and thousands of compounds in seconds and are in widespread current use to identify PAINS in order to exclude them from further analysis. However, this practice i...
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The use of substructural alerts to identify Pan-Assay INterference compoundS (PAINS) has become a common component of the triage process in biological screening campaigns. These alerts, however, were originally derived from a proprietary library tested in just six assays measuring protein-protein interaction (PPI) inhibition using the AlphaScreen detection technology only; moreover, 68% (328 ou...
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Significant resources in early drug discovery are spent unknowingly pursuing artifacts and promiscuous bioactive compounds, while understanding the chemical basis for these adverse behaviors often goes unexplored in pursuit of lead compounds. Nearly all the hits from our recent sulfhydryl-scavenging high-throughput screen (HTS) targeting the histone acetyltransferase Rtt109 were such compounds....
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ژورنال
عنوان ژورنال: Biochemistry & Pharmacology: Open Access
سال: 2015
ISSN: 2167-0501
DOI: 10.4172/2167-0501.1000e173