| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID472515 | Agonist activity at human LXRbeta assessed as induction of PGC1b-2 cofactor recruitment | 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. |
| 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. |
| AID472514 | Agonist activity at human LXRbeta assessed as induction of PGC-1a cofactor recruitment | 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. |
| 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. |
| AID345478 | Agonist activity at human PPARgamma 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. |
| 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. |
| AID452983 | Ratio of AUC (0 to infinity) in brain to AUC (0 to infinity) in plasma in Long Evans rat at 30 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| 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. |
| AID472517 | Agonist activity at human LXRbeta assessed as induction of PCAF cofactor recruitment | 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. |
| AID1480571 | Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators. |
| 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. |
| AID452963 | Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID1691876 | Antiproliferative activity against human U-251 cells 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. |
| AID345479 | Agonist activity at human PPARdelta 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. |
| 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. |
| AID345477 | Agonist activity at human PPARalpha 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. |
| AID452962 | Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID1691886 | Agonist activity at LXR in 2-NBD-cholesterol labelled human U87 cells overexpressing EGFR variant III assessed as induction of cholesterol efflux to ApoA1 measured after 24 hrs | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| 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. |
| AID472510 | Agonist activity at human LXRbeta assessed as induction of SRC2-1 cofactor recruitment | 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. |
| 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. |
| AID472502 | Agonist activity at human LXRalpha assessed as induction of PGC1b-2 cofactor recruitment | 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. |
| AID472496 | Agonist activity at human LXRalpha assessed as induction of SRC1-3 cofactor recruitment | 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. |
| AID452981 | AUC (0 to infinity) in Long Evans rat brain at 30 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID345484 | Displacement of radiolabeled mibolerone from human androgen receptor by filter paper 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. |
| AID472613 | Agonist activity at human LXRbeta assessed as induction of p300-1 cofactor recruitment | 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. |
| 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. |
| AID472519 | Agonist activity at human LXRbeta assessed as induction of NRP1-3 cofactor recruitment | 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. |
| 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. |
| 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. |
| AID452964 | Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay relative to T0901317 | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID345486 | Displacement of radiolabeled estradiol from human estrogen receptor alpha by scintillation proximity 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. |
| AID345481 | Displacement of radiolabeled 9-cis retinoic acid from human RXR by scintillation proximity 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. |
| AID472512 | Agonist activity at human LXRbeta assessed as induction of SRC3-2 cofactor recruitment | 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. |
| AID1691887 | Agonist activity at LXR in human U87 cells overexpressing EGFR variant III assessed as reduction in intracellular cholesterol level measured after 48 hrs | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| 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. |
| AID472520 | Agonist activity at human LXRbeta assessed as induction of NRP1-6 cofactor recruitment | 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. |
| AID472612 | Agonist activity at human LXRalpha assessed as induction of p300-1 cofactor recruitment | 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. |
| AID472503 | Agonist activity at human LXRalpha assessed as induction of CPB/p300-2 cofactor recruitment | 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. |
| 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. |
| AID472511 | Agonist activity at human LXRbeta assessed as induction of SRC2-3 cofactor recruitment | 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. |
| AID452977 | AUC (0 to infinity) in Long Evans rat plasma at 30 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID472498 | Agonist activity at human LXRalpha assessed as induction of SRC2-3 cofactor recruitment | 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. |
| AID472516 | Agonist activity at human LXRbeta assessed as induction of CPB/p300-2 cofactor recruitment | 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. |
| AID345485 | Displacement of radiolabeled progesterone from human progesterone receptor by filter paper 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. |
| AID452979 | Cmax in Long Evans rat brain at 30 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID472509 | Agonist activity at human LXRbeta assessed as induction of SRC1-3 cofactor recruitment | 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. |
| AID472505 | Agonist activity at human LXRalpha assessed as induction of NRIP1-1 cofactor recruitment | 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. |
| AID345488 | Displacement of radiolabeled triiodothyronine from human thyroid hormone receptor alpha by filter paper 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. |
| AID452965 | Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay relative to T0901317 | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID472485 | Binding affinity to PPARalpha | 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. |
| 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. |
| AID452972 | Effect on triglyceride accumulation in human HepG2 cells relative to TO901317 | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID472504 | Agonist activity at human LXRalpha assessed as induction of PCAF cofactor recruitment | 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. |
| AID452966 | Effect on ABCA1 gene expression in human differentiated THP1 cells | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID345480 | Displacement of radiolabeled TO901317 from human PXR by scintillation proximity 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. |
| AID472518 | Agonist activity at human LXRbeta assessed as induction of NRIP1-1 cofactor recruitment | 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. |
| AID472501 | Agonist activity at human LXRalpha assessed as induction of PGC-1a cofactor recruitment | 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. |
| AID472507 | Agonist activity at human LXRalpha assessed as induction of NRP1-6 cofactor recruitment | 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. |
| AID472500 | Agonist activity at human LXRalpha assessed as induction of TRAP220-1 cofactor recruitment | 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. |
| AID1691885 | Agonist activity at LXR in human U87 cells overexpressing EGFR variant III assessed as reduction in LDL uptake measured after 48 hrs by DAPI staining based fluorescence assay | 2020 | European journal of medicinal chemistry, May-15, Volume: 194 | Discovery of new LXRβ agonists as glioblastoma inhibitors. |
| 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. |
| 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. |
| AID345680 | Displacement of radiolabeled Dexamethasone from human glucocorticoid receptor by filter paper 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. |
| AID452975 | Cmax in Long Evans rat plasma at 30 mg/kg, po | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID472497 | Agonist activity at human LXRalpha assessed as induction of SRC2-1 cofactor recruitment | 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. |
| AID1691877 | Antiproliferative activity against human A 172 cells 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. |
| AID452971 | Effect on triglyceride accumulation in human HepG2 cells | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID452967 | Effect on ABCA1 gene expression in human differentiated THP1 cells relative to TO901317 | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration. |
| AID345533 | Agonist activity at human FXR ligand binding domain 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. |
| AID345487 | Displacement of radiolabeled estradiol from human estrogen receptor beta by scintillation proximity 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. |
| AID1480570 | Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay | 2017 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
| DrugBank screening revealed alitretinoin and bexarotene as liver X receptor modulators. |
| AID472508 | Agonist activity at human LXRbeta assessed as induction of SRC1-1 cofactor recruitment | 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. |
| AID345483 | Displacement of radiolabeled aldosterone from human mineralocorticoid receptor by filter paper 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. |
| AID472513 | Agonist activity at human LXRbeta assessed as induction of TRAP220-1 cofactor recruitment | 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. |
| AID472495 | Agonist activity at human LXRalpha assessed as induction of SRC1-1 cofactor recruitment | 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. |
| 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. |
| 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. |
| AID472499 | Agonist activity at human LXRalpha assessed as induction of SRC3-2 cofactor recruitment | 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. |
| AID472506 | Agonist activity at human LXRalpha assessed as induction of NRP1-3 cofactor recruitment | 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. |
| AID472484 | Tmax in C57 mouse at 10 mg/kg, po | 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. |
| AID345489 | Displacement of radiolabeled triiodothyronine from human thyroid hormone receptor beta by filter paper 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. |
| 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. |
| AID1347160 | Primary 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. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |