lu-208075 and benzarone

lu-208075 has been researched along with benzarone* in 1 studies

Other Studies

1 other study(ies) available for lu-208075 and benzarone

Article	Year
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. Bioorganic & medicinal chemistry letters, 2016, 08-15, Volume: 26, Issue:16 Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (human CYP3A4, CYP2D6 and CYP2C9) with Hep3B cells. We screened a series of drugs to explore structural motifs that may be responsible for CYP450-dependent activation caused by reactive metabolite formation, which highlighted specific liabilities regarding certain phenols and anilines. Topics: Adenosine Triphosphate; Benzbromarone; Cell Line; Cell Survival; Chromans; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Humans; Pharmaceutical Preparations; Thiazolidinediones; Troglitazone	2016

Article

Year

Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.

Bioorganic & medicinal chemistry letters, 2016, 08-15, Volume: 26, Issue:16

Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites. In order to reduce attrition due to metabolism-induced toxicity and to improve the safety of drug candidates, we developed a simple cell viability assay by combining a bioactivation system (human CYP3A4, CYP2D6 and CYP2C9) with Hep3B cells. We screened a series of drugs to explore structural motifs that may be responsible for CYP450-dependent activation caused by reactive metabolite formation, which highlighted specific liabilities regarding certain phenols and anilines.

Topics: Adenosine Triphosphate; Benzbromarone; Cell Line; Cell Survival; Chromans; Cytochrome P-450 CYP2C9; Cytochrome P-450 CYP2D6; Cytochrome P-450 CYP3A; Cytochrome P-450 Enzyme System; Humans; Pharmaceutical Preparations; Thiazolidinediones; Troglitazone

2016