| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID412997 | Increase in transcriptional activity of RXRalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID413007 | Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1191334 | Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay relative to Wy-14,643 | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID440653 | Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay relative to Wy-14643 | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1561627 | Inhibition of CDK5 (unknown origin) assessed as reduction in histone H1 phosphorylation | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID413005 | Increase in transcriptional activity of HNF-4alpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561644 | Binding affinity to low affinity alternative site of GW9662 bound N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS at 0.1 to 10 uM by SPR assay | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID412999 | Increase in transcriptional activity of human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561626 | Inhibition of N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in S245 phosphorylation level at 10 uM incubated for 60 mins by ELISA | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID413010 | Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay relative to Wy 14,643 | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561632 | Binding affinity to N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS by SPR analysis | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID240267 | Effective concentration against human PPARalpha expressed in HepG2 cells | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID413004 | Increase in transcriptional activity of ROR ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID440656 | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay relative to rosiglitazone | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1400346 | Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. |
| AID1400347 | Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay relative to rosiglitazone | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. |
| AID413006 | Increase in transcriptional activity of Nurr1 ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561635 | Inhibition of N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as S245 phosphorylation level at 10 uM by phospho gel stain method relative to control | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID440657 | Inhibition of CIC1 in Wistar rat extensor digitorum longus muscle assessed as decrease in resting chloride channel conductance at 5 uM by electrophysiology method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1561633 | Stabilization of N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS by CD spectroscopy | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1400344 | Transactivation of GAL4-tagged human PPARalpha LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. |
| AID413003 | Increase in transcriptional activity of FXR ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID413011 | Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1191344 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in CD36 gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID1561631 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS by SPR analysis | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1561638 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at H3 region (277 to 286 residues) by hydrogen/deuterium exchange/mass spectrom | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID744325 | Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists. |
| AID1561637 | Inhibition of N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as guanidine concentration to achieve 50% of folded protein incubated for 2 hrs by CD spectroscopy (Rvb = | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID413002 | Increase in transcriptional activity of LXRbeta ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID744324 | Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Molecular determinants for nuclear receptors selectivity: chemometric analysis, dockings and site-directed mutagenesis of dual peroxisome proliferator-activated receptors α/γ agonists. |
| AID243394 | Efficacy against murine PPARalpha relative to Wy-14,643 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID1561642 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at external beta1 strand of beta sheet by hydrogen/deuterium exchange/mass spec | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID412998 | Increase in transcriptional activity of human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1191347 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in FABP1 gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID413009 | Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561641 | Binding affinity to N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at H12 region by hydrogen/deuterium exchange/mass spectrometry | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID440659 | Inhibition of resting potassium conductance in Wistar rat extensor digitorum longus muscle by electrophysiology method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1191345 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in ANGPTL4 gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID1561645 | Binding affinity to low affinity alternative site of GW9662 bound N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS at 100 uM by SPR assay | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID722385 | Binding affinity to PPARgamma-LBD site A (unknown origin) at 500 uM | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression. |
| AID240162 | Effective concentration against murine PPARalpha in transactivation assay | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID1561628 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as induction of M348 cross-peak shift at 1 mol equiv by 2D 1H-15N HSQC NMR analysis | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID413008 | Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay relative to rosiglitazone | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID240268 | Effective concentration against human PPARgamma expressed in HepG2 cells | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID413001 | Increase in transcriptional activity of LXRalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1400345 | Transactivation of GAL4-tagged human PPARalpha LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay relative to Wy-14,643 | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Identification of the First PPARα/γ Dual Agonist Able To Bind to Canonical and Alternative Sites of PPARγ and To Inhibit Its Cdk5-Mediated Phosphorylation. |
| AID1191343 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in CPT1A gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID413274 | Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay relative to Wy 14,643 | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID243395 | Efficacy against human PPARalpha expressed in HepG2 cells relative to Wy-14,643 | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID440652 | Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1191348 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in HMGCS2 gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID1561640 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at H12 region by hydrogen/deuterium exchange/mass spectrometry | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1561630 | Binding affinity to N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as induction of M348 cross-peak shift at 0.1 to 1 mol equiv by 2D 1H-15N HSQC NMR analysis | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID722391 | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay relative to rosiglitazone | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression. |
| AID440654 | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID722392 | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression. |
| AID412996 | Increase in transcriptional activity of RARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561629 | Binding affinity to N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as induction of M348 cross-peak shift at 0.1 to 1 mol equiv by 2D 1H-15N HSQC NMR analysis | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1191335 | Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID722393 | Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay relative to WY-14643 | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression. |
| AID722394 | Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
| New 2-(aryloxy)-3-phenylpropanoic acids as peroxisome proliferator-activated receptor α/γ dual agonists able to upregulate mitochondrial carnitine shuttle system gene expression. |
| AID243396 | Efficacy against human PPARgamma expressed in HepG2 cells relative to rosiglitazone | 2005 | Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
| Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity. |
| AID1561636 | Stabilization of N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as guanidine concentration to achieve 50% of folded protein incubated for 2 hrs by CD spectroscopy (Rvb = 1.69 uM) | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID440655 | Inhibition of CIC1 in Wistar rat extensor digitorum longus muscle assessed as decrease in resting chloride channel conductance at 100 uM by electrophysiology method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
| New 2-aryloxy-3-phenyl-propanoic acids as peroxisome proliferator-activated receptors alpha/gamma dual agonists with improved potency and reduced adverse effects on skeletal muscle function. |
| AID1561625 | Inhibition of N-terminal His-tagged human PPARgamma LBD (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as S245 phosphorylation level at 10 uM by phospho gel stain method relative to control | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1561634 | Stabilization of N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS by CD spectroscopy | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1191346 | Agonist activity at PPARalpha/PPARgamma in human HepaR cells assessed as increase in FABP4 gene expression at 10 uM incubated for 1 day by quantitative PCR method relative to untreated control | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID413000 | Increase in transcriptional activity of human PPARbeta/delta ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561639 | Binding affinity to N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at H3 region (277 to 286 residues) by hydrogen/deuterium exchange/ | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1191336 | Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay relative to rosiglitazone | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID412995 | Increase in transcriptional activity of TRalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| AID1561643 | Binding affinity to N-terminal His-tagged human PPARgamma LBD I281A mutant (207 to 474 residues) expressed in Escherichia coli Rosetta (DE3) pLysS assessed as reduction in deuterium uptake at external beta1 strand of beta sheet by hydrogen/deuterium excha | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
| Insights into PPARγ Phosphorylation and Its Inhibition Mechanism. |
| AID1191333 | Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Design, synthesis and biological evaluation of a class of bioisosteric oximes of the novel dual peroxisome proliferator-activated receptor α/γ ligand LT175. |
| AID1798922 | Cell-Based Transcription Assay from Article 10.1021/jm800733h: \\Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket coul | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
| Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |