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Inhibition Assay from US Patent US8859534: "2-carboxamide-7-piperazinyl-benzofuran derivatives"
Assay data:53 Active, 30 Activity ≤ 1 nM, 53 Activity ≤ 1 µM, 53 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Cytotoxicity against CHO cells assessed as cell growth inhibition incubated for 48 hrs by AlamarBlue assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Cytotoxicity against CHO cells assessed as cell growth inhibition by MTT assay
Assay data:1 Tested
SummaryPubMed Citation
Drug localization in plasma membrane of chinese hamster CHO cells expressing YFP-tagged H1R at 1 to 25 nM incubated for 30 min by confocal microscopy
Drug uptake in chinese hamster CHO cells expressing YFP-tagged H1R assessed as intracellular uptake at 1 to 25 nM preincubated for 30 min with mepyramine followed by compound addition and measured after 30 min by confocal microscopy analysis
Drug localization in plasma membrane of chinese hamster CHO cells expressing YFP-tagged H1R at 1 to 25 nM preincubated for 30 min with mepyramine followed by compound addition and measured after 30 min by confocal microscopy analysis
Drug uptake in chinese hamster CHO cells expressing YFP-tagged H1R assessed as intracellular uptake at 1 to 25 nM incubated for 30 min by confocal microscopy
Induction of degradation of endogenous HMGCR in CHO-7 cells assessed as decrease in protein level incubated for 16 hrs in sterol-depleted medium by immunoblot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Growth inhibition of CHO-7 cells at 0.3 to 10 uM cultured for 7 days in sterol depleted medium in the presence of cholesterol and measured on day 8 by crystal violet staining based microscopic analysis
Growth inhibition of CHO-7 cells at 0.3 to 10 uM cultured for 7 days in sterol depleted medium in the absence of cholesterol and measured on day 8 by crystal violet staining based microscopic analysis
Induction of degradation of wild type HMGCR in CHO-K1 cells by immunoblot analysis
Induction of degradation of HMGCR in CHO-K1 cells at 1 to 10 uM incubated for 8 hrs in presence of proteosome inhibitor MG-132 by immunoblot analysis
Downregulation of lovastatin-induced HMGCR expression in CHO-K1 cells incubated for 16 hrs by immunoblot analysis
Downregulation of HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 10 uM incubated for 16 hrs by immunoblot analysis (Rvb = 1.0 No_unit)
Downregulation of lovastatin-induced HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 10 uM incubated for 16 hrs by immunoblot analysis (Rvb = 15.2 No_unit)
Downregulation of lovastatin-induced HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 3 uM incubated for 16 hrs by immunoblot analysis (Rvb = 15.2 No_unit)
Downregulation of lovastatin-induced HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 1 uM incubated for 16 hrs by immunoblot analysis (Rvb = 15.2 No_unit)
Induction of degradation of hamster HMGCR (TM1-8)-GFP (1 to 346 residues) transfected in CHO-7 cells incubated for 16 hrs in sterol-depleted medium by fluorescence based microplate reader assay
Assay data:39 Active, 21 Activity ≤ 1 µM, 43 Tested
Downregulation of HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 1 uM incubated for 16 hrs by immunoblot analysis (Rvb = 1.0 No_unit)
Downregulation of HMGCR expression in CHO-K1 cells assessed as fold change in HMGCR expression at 3 uM incubated for 16 hrs by immunoblot analysis (Rvb = 1.0 No_unit)
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