| Assay ID | Title | Year | Journal | Article |
|---|
| AID1797957 | Cell-Free Ligand Sensing Assay (LiSA)-LXRbeta-SRC1 Assay from Article 10.1021/jm050532w: \\Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.\\ | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID1797953 | Scintillation Proximity Assay from Article 10.1021/jm070453f: \\N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.\\ | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID1797956 | Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay from Article 10.1021/jm050532w: \\Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.\\ | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID1798783 | Fluorescence Resonance Energy Transfer (FRET) Ligand Sensing Assay (LiSA) from Article 10.1016/j.bmcl.2009.01.004: \\Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.\\ | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. |
| AID1798629 | LXR Binding Assay and hLXR Reporter Assay from Article 10.1021/jm800799q: \\Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis\\ | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1797958 | Cell-Free Ligand Sensing Assay (LiSA)-LXRalpha-SRC1 Assay from Article 10.1021/jm0255116: \\Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.\\ | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID1798792 | HTRF Cofactor Peptide Recruitment Assay from Article 10.1016/j.bmcl.2007.06.017: \\2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.\\ | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID1797932 | LXR Binding Assay from Article 10.1021/jm0609566: \\Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.\\ | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID1797933 | LXR Binding Assay and hLXR beta Reporter Assay from Article 10.1021/jm0609566: \\Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis.\\ | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID1797952 | Fluorescence-Resonance Energy Transfer Assay from Article 10.1021/jm070453f: \\N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta.\\ | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID1803987 | SARS-CoV-2 CPE assay from Article 10.1101/2020.07.17.207019: \\Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.\\ | 2020 | bioRxiv : the preprint server for biology, Aug-11 | Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening. |
| AID1803986 | 3CLpro enzyme assay from Article 10.1101/2020.07.17.207019: \\Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.\\ | 2020 | bioRxiv : the preprint server for biology, Aug-11 | Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening. |
| AID1805801 | Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\ | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Perspectives on SARS-CoV-2 Main Protease Inhibitors. |
| AID1798364 | alpha-Glucosidase Inhibition Assay from Article 10.1016/j.bmc.2008.02.078: \\Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.\\ | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1192871 | Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID1752676 | Antischistosomal activity against Schistosoma mansoni Liberian NTS incubated for 72 hrs by microscopic method | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here? |
| AID472565 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scd1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID299788 | Agonist activity at human LXRalpha receptor after 1 hr by HTRF cofactor recruitment assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID472594 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as cyp7a1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID418427 | Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. |
| AID266386 | Normalized AUC in mouse at 0.5 mg/kg, iv or 20 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID391702 | Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production by ELISA relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID472540 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of SREBP-1c expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345491 | Effect on ABCA1 gene expression in human differentiated THP1 cells relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1652184 | Binding affinity to LXRalpha (unknown origin) by surface plasmon resonance assay | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4
| Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus |
| AID472563 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pltp gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID28226 | Oral bioavailability after administration of a dose of 10 mg/kg | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID1565982 | Lipid lowering activity in human HepG2 cells assessed as decrease in OA-induced TG accumulation at 10 uM incubated for 24 hrs | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID472593 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoe gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID273409 | Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay relative to TO901317 | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID266385 | Half life in mouse at 0.5 mg/kg, iv or 20 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID472583 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pltp gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID239783 | Relative efficacy in human ATP binding cassette transporter A1 (ABCA1) transcriptional activation assay compared to GW-3965 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID472536 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG8 expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID307303 | Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID472538 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of SREBP-1c expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266396 | Increase of total cholesterol level in C57BL/6 mouse at 1 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID474688 | Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID1691895 | Antitumor activity against human U87 cells overexpressing EGFR variant III xenografted in Balb/c nu/nu mouse assessed as reduction in tumor size at 40 mg/kg/day, ig for 15 days by caliper method | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID331151 | Induction of LXRalpha gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID472582 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pcsk9 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266389 | Increase of HDL level in C57BL/6 mouse at 30 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID472561 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Irp1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID307302 | Agonist activity at LXRalpha LBD by HTRF cofactor peptide recruitment assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID472541 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCA1 expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345472 | Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID331155 | Induction of SREBP1c gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID328049 | Agonist activity at LXR | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. |
| AID472527 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as reduction in total plasma cholesterol | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472568 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472606 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as srebf1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID30959 | the half-life (t1/2) in mice after a dose of 10 mg/kg | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID1304660 | Binding to human LXRbeta | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist. |
| AID1565970 | Agonist activity at rat LXRbeta transfected in HEK293T cells at 10 uM incubated for 20 hrs by luciferase reporter gene assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID101836 | Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID391725 | Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID101842 | Relative efficacy compared to 24(S),25-epoxy cholesterol in LXR alpha-Gal4 receptor gene assay | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID240219 | Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor) | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID1565979 | Agonist activity at LXR in C57BL/6 mouse PBMC assessed as increase in sREBP-1c mRNA expression at 10 uM incubated for 48 hrs by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID437774 | Increase in ABCA1 gene expression in human primary macrophages at 100 nM relative to control | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID472574 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as cyp7a1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266397 | Increase of total cholesterol level in C57BL/6 mouse at 10 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID331163 | Induction of TBP gene expression in human THP1 cells at 10 uM using by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID331160 | Induction of Cox2 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID392873 | Increase in ABCA1 expression in orally dosed C57BL/6J mouse macrophages compound administered twice daily by cholesterol efflux assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. |
| AID418425 | Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. |
| AID472598 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Lipc gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID297207 | Increase in ABCA1 gene expression in THP1 cells at 1 uM relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID1565973 | Selectivity index, ratio of compound effect for agonist activity at human LXRalpha to compound effect for agonist activity at rat LXRbeta | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID345495 | Effect on SREBP1c gene expression in human HepG2 cells relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID768601 | Agonist activity at LXRbeta in mouse RAW264.7 cells assessed as induction of ABCA1 promoter activation at 1 uM after 24 hrs by Dual-Glo luciferase reporter gene assay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID288024 | Reduction of aortic arch lesion in C57BL/6 ApoE knockout mouse at 10 mg/kg, po for 12 weeks | 2007 | Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
| Further modification on phenyl acetic acid based quinolines as liver X receptor modulators. |
| AID472571 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as adfp gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472576 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoc1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472592 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apo5 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472556 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoc1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472604 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scab1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID307306 | Ratio of induction of SREBP1c gene expression in THP1 cells at 10 uM to control | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID1565989 | Agonist activity at LXR in mouse 3T3L1 preadipocytes assessed as increase in ABCA1 mRNA expression at 10 uM by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID297217 | Activity at human LXRalpha by Gal4 transactivation assay | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID472549 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg5 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID331152 | Induction of ABCA1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID418426 | Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. |
| AID472589 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg5 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID437600 | Agonist activity at human LXRbeta assessed as association of SRC1 to LXRbeta ligand binding domain by FRET based cell-free ligand sensing assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID472548 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID391724 | Inhibition of LPS-stimulated nuclear co-repressor release from iNOS promoter in mouse RAW264.7 cells at 1 uM by RT-PCR | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID345492 | Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID241121 | Inhibition of human GSK3-beta; NT=Not tested | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID331162 | Induction of B2M gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID474684 | Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID239785 | Relative efficacy for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha compared to GW-3965 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID472529 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCA1 expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472535 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG8 expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345475 | Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID768597 | Agonist activity at human LXRbeta transfected in HEK293 cells at 0.1 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID472558 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Lipc gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472545 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCG1 expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472534 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG5 expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID768588 | Agonist activity at LXRbeta in mouse BV2 cells assessed as degradation of intracellular soluble amyloid beta42 at 1 uM preincubated for 18 hrs followed by soluble amyloid beta42 addition measured after 24 hrs by ELISA relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID345493 | Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1881845 | Protac activity at VHL/LXR (unknown origin) by TR-FRET assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives. |
| AID391730 | Induction of LXRbeta SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID437773 | Increase in ABCA1 gene expression in human primary macrophages at 30 nM relative to control | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID297219 | Activity at human LXRalpha by Gal4 transactivation assay relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID768599 | Agonist activity at human LXRalpha transfected in HEK293 cells at 0.1 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID768571 | Induction of cytoplasmic lipid accumulation in human HepG2 cells at 1 uM after 4 days by oil red O staining-based light microscopic analysis | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID1565984 | Agonist activity at LXR in human HepG2 cells assessed as increase in ABCA1 mRNA expression at 10 uM incubated for 24 hrs by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID297206 | Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID345476 | Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID345473 | Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID472603 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pltp gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID307307 | Induction of cholesterol efflux in THP1 cells after 18 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID1192874 | Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells assessed as maximal efficacy at 10 uM after 24 hrs by luciferase reporter gene assay relative to T0901317 luminescence intensity | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID345497 | Effect on triglyceride accumulation in human HepG2 cells relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID299794 | Induction of cholesterol efflux in THP1 cells at 10 uM relative to control | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID345506 | Effect on triglyceride level in LDL receptor knockout C57BL/6 mouse plasma at 10 mg/kg administered with Western diet after 8 weeks | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID331154 | Induction of APOE gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID1691870 | Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID266416 | Increase of triglyceride level in C57BL/6 mouse liver at 30 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID472550 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg8 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID474686 | Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID345505 | Decrease in total cholesterol level in LDL receptor knockout C57BL/6 mouse plasma at 10 mg/kg administered with Western diet after 8 weeks | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID299793 | Induction of cholesterol efflux in THP1 cells | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID472546 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCG1 expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472572 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apo5 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID297204 | Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID472596 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoc1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472537 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG8 expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1665619 | AUC (0.5 to 6 hrs) in C57BL/6 mouse serum at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID297203 | Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID345471 | Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID472551 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as adfp gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID307309 | Ratio of induction of cholesterol efflux in THP1 cells at 10 uM to control after 18 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID472532 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG5 expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID297218 | Activity at human LXRbeta by Gal4 transactivation assay | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID472585 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scd1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472543 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCA1 expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266407 | Increase of triglyceride level in C57BL/6 mouse plasma at 30 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID472554 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as cyp7a1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1665630 | Brain to serum concentration ratio, Kp of the compound in C57BL/6 mouse at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID297211 | Induction on FAS gene expression in human primary hepatocytes at 1 uM | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID1192877 | Ratio of induction of ABCA1 mRNA expression to SREBP-1c mRNA expression in human HepG2 cells at 5 uM | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID1192876 | Induction of SREBP-1c mRNA expression in human HepG2 cells at 5 uM relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID474683 | Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID472587 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abca1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472601 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Irp1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1562693 | Agonist activity at recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as peptide D22 recruitment fluorescence polarization binding assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay. |
| AID474685 | Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID391703 | Lipogenic activity against human HuH7 cells assessed as triglyceride accumulation at 10 uM after 4 days relative to N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-(2,2,2-trifluoroethyl)benzenesulfonamide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID437786 | Binding affinity to PXR by scintillation proximity binding assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID768596 | Agonist activity at human LXRbeta transfected in HEK293 cells at 1 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID299787 | Agonist activity at human LXRbeta receptor after 1 hr by HTRF cofactor recruitment assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID391723 | Reduction of LPS-stimulated iNOS gene expression in mouse RAW264.7 cells expressing LXRalpha at 1 uM by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID266384 | Volume of distribution in mouse at 0.5 mg/kg, iv or 20 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID1565969 | Agonist activity at human LXRalpha transfected in HEK293T cells at 10 uM incubated for 20 hrs by luciferase reporter gene assay relative to control | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID1565978 | Agonist activity at LXR in C57BL/6 mouse PBMC assessed as increase in ABCA1 mRNA expression at 10 uM incubated for 48 hrs by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID472602 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pcsk9 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1565980 | Agonist activity at LXR in mouse RAW264.7 cells assessed as increase in sREBP-1c mRNA expression at 10 uM incubated for 48 hrs by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID297208 | Increase in ABCA1 gene expression in THP1 cells at 10 uM relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID768572 | Induction of intracellular triglyceride accumulation in human HepG2 cells at 10 uM after 4 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID437779 | Increase in ABCG1 gene expression in human primary macrophages | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID1466797 | Chaperone activity at FLAG/GFP-tagged NPC1 I1061T mutant (unknown origin) expressed in HEK293 cells assessed as increase in localization of protein mutant in late endosomes at 30 uM after 24 hrs by Hoechst 33342 staining based fluorescence microscopic ana | 2017 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
| Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein. |
| AID288025 | Increase in plasma triglyceride level in C57BL/6 ApoE knockout mouse at 10 mg/kg, po for 12 weeks | 2007 | Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
| Further modification on phenyl acetic acid based quinolines as liver X receptor modulators. |
| AID299791 | Induction of ABCA1 gene expression in THP1 cells at 10 uM relative to control | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID472542 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCA1 expression at 0.6 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID437771 | Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID472560 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as IPl gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1233301 | Agonist activity at LXRalpha (unknown origin) relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
| Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists. |
| AID266406 | Increase of triglyceride level in C57BL/6 mouse plasma at 10 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID392870 | Agonist activity at LXRalpha by FRET assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. |
| AID1304658 | Agonist activity at human LXRalpha by Gal4 assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist. |
| AID391716 | Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced srebp1c mRNA expression in human HepG2 cells at 500 nM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID28064 | Cmax in mice after 10 mg/kg oral dose | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID307305 | Ratio of induction of ABCA1 gene expression in THP1 cells at 10 uM to control | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID297205 | Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID437598 | Agonist activity at human LXRalpha assessed as association of SRC1 to LXRalpha ligand binding domain by FRET based cell-free ligand sensing assay | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID472586 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as srebf1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1691873 | Selectivity index, ratio of EC50 for agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells to EC50 for agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID1692276 | Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay | 2020 | Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
| Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis. |
| AID299789 | Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID307308 | Ratio of induction of lipogenesis in HepG2 cells at 10 uM to control after 24 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID472599 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as lipg gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266415 | Increase of triglyceride level in C57BL/6 mouse liver at 10 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID391722 | Reduction of LPS-stimulated iNOS gene expression in LXRalpha and LXRbeta deficient mouse RAW264.7 cells at 1 uM by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID437775 | Increase in ABCG1 gene expression in human primary macrophages at 30 nM relative to control | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID345511 | Upregulation of ABCA1 gene expression in LDL receptor knockout C57BL/6 mouse duodenum at 10 mg/kg administered with Western diet | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID391719 | Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced fas mRNA expression in human HepG2 cells at 500 nM | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID331157 | Induction of SCD1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID1565985 | Agonist activity at LXR in human HepG2 cells assessed as increase in sREBP-1c mRNA expression at 10 uM incubated for 24 hrs by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID472578 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Lipc gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472595 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Fasn gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472569 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg5 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472580 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as IPl gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1665608 | AUC (0.5 to 6 hrs) in C57BL/6 mouse brain at 9.14 umol/kg, ip by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators. |
| AID472526 | Plasma concentration in high fat/high cholesterol fed LDLR-deficient mouse administered with diet for 8 weeks measured after 3 hrs of last dose | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472597 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as ldlr gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID299792 | Induction of SREBP1c gene expression in HepG2 cells at 10 uM relative to control | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID472555 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Fasn gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472566 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as srebf1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1233303 | Agonist activity at LXRbeta (unknown origin) relative to control | 2015 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
| Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists. |
| AID437776 | Increase in ABCG1 gene expression in human primary macrophages at 100 nM relative to control | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID240246 | Effective concentration in human ATP binding cassette transporter A1 (ABCA1) transcriptional activation assay | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID297220 | Activity at human LXRbeta by Gal4 transactivation assay relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID472528 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as reduction in plasma triglyceride level | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1192872 | Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells assessed as maximal efficacy at 10 uM after 24 hrs by luciferase reporter gene assay relative to T0901317 luminescence intensity | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID472590 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg8 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID299790 | Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965 | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID472533 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCG5 expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266387 | Increase of HDL level in C57BL/6 mouse at 1 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID472579 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as lipg gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID331156 | Induction of FASN gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID1691872 | Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay relative to GW3965 | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID240223 | Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha (Liver X receptor) | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID472564 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scab1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID331161 | Induction of ACTB gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID345490 | Effect on ABCA1 gene expression in human differentiated THP1 cells | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1752680 | Antischistosomal activity against Schistosoma mansoni infected in NMRI mouse assessed as worm burden reduction at 200 mg/kg, po administered as single dose measured after 16 to 18 days | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here? |
| AID273431 | Reduction of atherosclerotic lesion of thoracic aorta in LDLr knockout C57BL/6 mouse at 10 mg/kg/day, po after 8 weeks relative to control | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID418705 | Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides. |
| AID472539 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of SREBP-1c expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1233302 | Agonist activity at LXRbeta (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
| Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists. |
| AID1562690 | Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay. |
| AID101843 | Relative efficacy compared to 24(S),25-epoxy cholesterol in Liver X receptor-alpha ligand-sensing assay | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID437778 | Increase in ABCA1 gene expression in human primary macrophages | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID266383 | Clearance in mouse at 0.5 mg/kg, iv or 20 mg/kg, po | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID1691874 | Displacement of hyodeoxycholicacid-based fluorescent tracer from recombinant human LXRbeta LBD (215 to 461 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins under shaking condition and measured after 30 mins by fluorescence polar | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID345496 | Effect on triglyceride accumulation in human HepG2 cells | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1192873 | Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID273407 | Displacement of [3H]T-0901317 from human LXR beta receptor | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID299795 | Induction of Lipogenesis in HepG2 cells at 10 uM relative to control | 2007 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 17, Issue:16
| 2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists. |
| AID391726 | Induction of LXRalpha SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID1691875 | Antiproliferative activity against human U87 cells overexpressing EGFR variant III measured after 7 days by CCK8 assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID266414 | Increase of triglyceride level in C57BL/6 mouse liver at 1 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID307304 | Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
| Discovery and structure-activity relationship studies of indole derivatives as liver X receptor (LXR) agonists. |
| AID472547 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abca1 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID266398 | Increase of total cholesterol level in C57BL/6 mouse at 30 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID273408 | Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID239784 | Relative efficacy in Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta compared to GW-3965 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure. |
| AID297202 | Displacement of [3H]T-0901317 from GAL-linked human LXRbeta expressed in THP1 cells at 20 uM by SPA relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID297201 | Displacement of [3H]T-0901317 from GAL-linked human LXRalpha expressed in THP1 cells at 20 uM by SPA relative to GW-3965 | 2007 | Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
| N-Acylthiadiazolines, a new class of liver X receptor agonists with selectivity for LXRbeta. |
| AID472575 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Fasn gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345474 | Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO901317 | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID472553 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoe gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID392871 | Agonist activity at LXRbeta by FRET assay | 2009 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
| Synthesis and SAR of potent LXR agonists containing an indole pharmacophore. |
| AID391701 | Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID472557 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as ldlr gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID437777 | Increase in SREBP1 gene expression in human primary macrophages at 100 nM relative to control | 2009 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
| The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. |
| AID331158 | Induction of HDS11B1 gene expression in human THP1 cells at 10 uM using Array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID1565990 | Agonist activity at LXR in mouse 3T3L1 preadipocytes assessed as increase in sREBP-1c mRNA expression at 10 uM by qPCR analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID472600 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as IPl gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472562 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as pcsk9 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID391700 | Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID472577 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as ldlr gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1304659 | Binding affinity to human LXRalpha | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist. |
| AID1691871 | Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay relative to GW3965 | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID474687 | Cytotoxicity against african green monkey CV1 cells | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Discovery of tertiary sulfonamides as potent liver X receptor antagonists. |
| AID273406 | Displacement of [3H]T-0901317 from human LXR alpha receptor | 2006 | Journal of medicinal chemistry, Oct-19, Volume: 49, Issue:21
| Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. |
| AID472531 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCA1 expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472567 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abca1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472605 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scd1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345494 | Effect on SREBP1c gene expression in human HepG2 cells | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID472552 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apo5 gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1691897 | Effect on serum triglyceride level in Balb/c nu/nu mouse xenografted with human U87 cells overexpressing EGFR variant III at 50 mg/kg/day, ip for 15 days | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID1192875 | Induction of ABCA1 mRNA expression in human HepG2 cells at 5 uM relative to control | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
| Design and discovery of 2-oxochromene derivatives as liver X receptor β-selective agonists. |
| AID472573 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as apoe gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472591 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as adfp gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID768573 | Induction of intracellular triglyceride accumulation in human HepG2 cells at 1 uM after 4 days relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID472530 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse duodenum assessed as induction of ABCA1 expression at 3 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID331150 | Induction of NR1H2 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID331159 | Induction of IL6 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID1812739 | Binding affinity to full-length human LXRalpha by surface plasmon resonance assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| LXR-Mediated Regulation of Marine-Derived Piericidins Aggravates High-Cholesterol Diet-Induced Cholesterol Metabolism Disorder in Mice. |
| AID768598 | Agonist activity at human LXRalpha transfected in HEK293 cells at 1 uM after 24 hrs by luciferase reporter gene assay relative to vehicle-treated control | 2013 | Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
| Synthesis and identification of new flavonoids targeting liver X receptor β involved pathway as potential facilitators of Aβ clearance with reduced lipid accumulation. |
| AID345513 | Increase in CYP7A1 gene expression in LDL receptor knockout C57BL/6 mouse liver at 10 mg/kg administered with Western diet | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID472588 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg1 gene regulation at 10 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID345507 | Reduction in atherosclerotic lesion size in LDL receptor knockout C57BL/6 mouse thoracic aorta at 10 mg/kg administered with Western diet after 8 weeks by oil Red-O staining | 2008 | Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
| Indazole-based liver X receptor (LXR) modulators with maintained atherosclerotic lesion reduction activity but diminished stimulation of hepatic triglyceride synthesis. |
| AID1752700 | Antischistosomal activity against Schistosoma mansoni incubated for 72 hrs by inverted microscopic method | 2020 | RSC medicinal chemistry, Apr-01, Volume: 11, Issue:4
| Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here? |
| AID266405 | Increase of triglyceride level in C57BL/6 mouse plasma at 1 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID328046 | Inhibition of Saccharomyces sp. alpha-glucosidase | 2008 | Bioorganic & medicinal chemistry, Apr-15, Volume: 16, Issue:8
| Co-existence of alpha-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development. |
| AID472570 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as abcg8 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID288023 | Reduction in aortic arch lesion area in C57BL/6 ApoE knockout mouse at 10 mg/kg, po for 12 weeks | 2007 | Bioorganic & medicinal chemistry, May-15, Volume: 15, Issue:10
| Further modification on phenyl acetic acid based quinolines as liver X receptor modulators. |
| AID331153 | Induction of ABCG1 gene expression in human THP1 cells at 10 uM by array plate mRNA assay | 2008 | Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
| Combination of virtual screening and high throughput gene profiling for identification of novel liver X receptor modulators. |
| AID472581 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as Irp1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID101837 | Effective concentration in LXR alpha-Gal4 receptor gene assay | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID391731 | Induction of LXRalpha SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID1565983 | Effect on TG accumulation in human HepG2 cells at 10 uM incubated for 24 hrs | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Discovery of tissue selective liver X receptor agonists for the treatment of atherosclerosis without causing hepatic lipogenesis. |
| AID472559 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as lipg gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472584 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as scab1 gene regulation at 3 mg/kg administered with diet for 7 days by Experion chip analysis | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID472544 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse macrophages assessed as induction of ABCG1 expression at 10 mg/kg administered with diet for 8 weeks | 2010 | Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
| Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist. |
| AID1691869 | Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| AID391699 | Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRalpha ligand binding domain | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. |
| AID1304657 | Agonist activity at human LXRbeta by Gal4 assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist. |
| AID1233300 | Agonist activity at LXRalpha (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 25, Issue:13
| Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists. |
| AID266388 | Increase of HDL level in C57BL/6 mouse at 10 mg/kg qd after 8 days relative to control | 2006 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
| SAR studies: designing potent and selective LXR agonists. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347164 | 384 well plate NINDS Rhodamine confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
| Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347149 | Furin counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347167 | Vero cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347168 | HepG2 cells viability qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347156 | DAPI mCherry counterscreen qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347153 | Confirmatory screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347171 | Orthogonal mCherry assay for qRT-PCR qHTS of selected Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347152 | Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347158 | ZIKV-mCherry secondary qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347172 | Secondary qRT-PCR qHTS assay for selected Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347163 | 384 well plate NINDS AMC confirmatory qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347161 | Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346993 | Human Liver X receptor-beta (1H. Liver X receptor-like receptors) | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| AID1346755 | Human Liver X receptor-alpha (1H. Liver X receptor-like receptors) | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10
| Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |