| Assay ID | Title | Year | Journal | Article |
|---|
| AID1576282 | Antagonist activity at human FXR T396E mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence after 18 hrs in presence of 1 uM FXR agonist, UPF930 by luciferase based reporter gene transacti | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576277 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for UPF930-induced biotinylated SRC-1 recruitment at 50 uM after 30 mins in presence of FXR agonist, UPF930 by Alpha Screen assay (Rvb = 0.14 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1656914 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced COX2 protein level at 6.25 to 12.5 microM by Western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID1350192 | Antiadipogenic activity in mouse 3T3L1 cells assessed as inhibition of CDCA-induced intracellular lipid droplets after 6 days by Oil Red O staining based assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
| Nonacidic Chemotype Possessing |
| AID1576253 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Akr1c13 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576236 | Agonist activity at VDR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID376807 | Antibacterial activity against Corynebacterium diphtheriae | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Microbial transformations of hypolipemic E-guggulsterone. |
| AID1576227 | Antagonist activity at PPARdelta (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1656916 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced TNFalpha level preincubated for 2 hrs followed by LPS addition and measured after 18 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID1576250 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Plaur gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576286 | Antagonist activity at human FXR T396E mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 1 uM FXR agonist, UPF930 by luciferase based reporter gene | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576248 | Agonist activity at PR (unknown origin) by Alpha Screen assay relative to progesterone | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576238 | Agonist activity at ER (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576234 | Agonist activity at RXRalpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576220 | Agonist activity at LXR beta (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1656913 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced iNOS protein level at 6.25 to 12.5 microM by Western blot analysis | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID254767 | Inhibitory concentration against Estrogen receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576233 | Antagonist activity at RAR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576280 | Antagonist activity at human FXR T396E mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene transactiv | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576228 | Agonist activity at PPARgamma (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID568578 | Cytotoxicity against african green monkey CV1 cells by MTT assay | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1
| Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus. |
| AID1576222 | Agonist activity at MR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1656915 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced IL6 level preincubated for 2 hrs followed by LPS addition and measured after 18 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID1576239 | Antagonist activity at ER (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID568576 | Antagonist activity at human FXR expressed in CV-1 cells assessed as inhibition of CDCA-induced transactivation after 24 hrs by luciferase reporter gene assay | 2011 | Journal of natural products, Jan-28, Volume: 74, Issue:1
| Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus. |
| AID1888806 | Preferential cytotoxic activity against human PANC-1 cells in nutrient-deprived medium | 2022 | Bioorganic & medicinal chemistry, 01-15, Volume: 54 | Structure-activity relationship and mechanistic study on guggulsterone derivatives; Discovery of new anti-pancreatic cancer candidate. |
| AID1576264 | Effect on Akr1c13 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254827 | Inhibitory concentration against Mineralocorticoid receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1350191 | Antiadipogenic activity in mouse 3T3L1 cells assessed as reduction in intracellular lipid droplets at 10 uM after 6 days by Oil Red O staining based assay | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
| Nonacidic Chemotype Possessing |
| AID1576240 | Agonist activity at GR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576252 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Slc48a1 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576279 | Antagonist activity at human wild type FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene transactivati | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576225 | Antagonist activity at PPARalpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576232 | Agonist activity at RAR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID376805 | Antibacterial activity against Pseudomonas aeruginosa | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Microbial transformations of hypolipemic E-guggulsterone. |
| AID1576270 | Effect on Ccl20 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576258 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Cd38 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID311801 | Cytotoxicity against monkey CV1 cells after 24 hrs by MTT assay | 2007 | Journal of natural products, Nov, Volume: 70, Issue:11
| Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity. |
| AID254310 | Inhibitory concentration against Estrogen receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576276 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for UPF930-induced biotinylated SRC-1 recruitment at 10 uM after 30 mins in presence of FXR agonist, UPF930 by Alpha Screen assay (Rvb = 0.14 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576216 | Agonist activity at GST-tagged FXR-LBD (unknown origin) assessed as biotinylated SRC-1 recruitment after 30 mins by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576260 | Effect on Hspb8 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing based data analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576245 | Antagonist activity at TR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576272 | Antagonist activity at human FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 1 uM FXR agonist, UPF-930 by luciferase based reporter gene transactivat | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576271 | Antagonist activity at human FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene transactivatio | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576288 | Antagonist activity at human FXR S355F mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene t | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254320 | Inhibitory concentration against Farnesoid X receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1656912 | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 1 hr followed by LPS addition and measured after 24 hrs | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID1667025 | Cytotoxicity against human PANC1 cells incubated in normal DMEM medium | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
| Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells. |
| AID1576249 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Hspb8 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254309 | Inhibitory concentration against Androgen receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576268 | Effect on Frat2 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576241 | Antagonist activity at GR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254324 | Inhibitory concentration against Progesterone receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576257 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Frat2 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576247 | Agonist activity at PXR (unknown origin) by Alpha Screen assay relative to SR12183 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576274 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for OCA-induced biotinylated SRC-1 recruitment at 50 uM after 30 mins in presence of FXR agonist, OCA by Alpha Screen assay (Rvb = 0.2 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576283 | Antagonist activity at human wild type FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene tran | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576261 | Effect on Plaur gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576231 | Antagonist activity at PXR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576242 | Agonist activity at PR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576226 | Agonist activity at PPARdelta (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576254 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Cxcl3 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576230 | Agonist activity at PXR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576284 | Antagonist activity at human FXR T396E mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene t | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576278 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for UPF930-induced biotinylated SRC-1 recruitment at 100 uM after 30 mins in presence of FXR agonist, UPF930 by Alpha Screen assay (Rvb = 0.14 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576246 | Agonist activity at LXRbeta (unknown origin) by Alpha Screen assay relative to T091317 | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254776 | Inhibitory concentration against Pregnane X receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1304570 | Antagonist activity at human FXR expressed in HEK293 cells assessed as inhibition of GW4064-induced transactivation after 24 hrs by luciferase reporter gene assay | 2016 | Journal of natural products, Mar-25, Volume: 79, Issue:3
| The Halicylindramides, Farnesoid X Receptor Antagonizing Depsipeptides from a Petrosia sp. Marine Sponge Collected in Korea. |
| AID1576263 | Effect on Slc48a1 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254336 | Inhibitory concentration against Mineralocorticoid receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID254323 | Inhibitory concentration against Glucocorticoid receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1656910 | Cytotoxicity against mouse RAW264 cells assessed as reduction in cell viability at 25 uM incubated for 24 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
| Synthesis and inhibitory effect of cis-guggulsterone on lipopolysaccharide-induced production of nitric oxide in macrophages. |
| AID254908 | Inhibitory concentration against Farnesoid X receptor; range from 50-100000 | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576223 | Antagonist activity at MR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576259 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Ccl20 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576285 | Antagonist activity at human wild type FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 1 uM FXR agonist, UPF-930 by luciferase based reporter gene tr | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576219 | Antagonist activity at LXR alpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576251 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Lpin2 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576237 | Antagonist activity at VDR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID311800 | Antagonist activity at human FXR expressed in monkey CV1 cells after 24 hrs by ecdysone receptor response element-driven luciferase reporter assay | 2007 | Journal of natural products, Nov, Volume: 70, Issue:11
| Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity. |
| AID1576265 | Effect on Cxcl3 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576262 | Effect on Lpin2 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254785 | Inhibitory concentration against Glucocorticoid receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576287 | Antagonist activity at human FXR S355E mutant expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence at 10 uM after 18 hrs in presence of 0.5 uM FXR agonist, OCR by luciferase based reporter gene t | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID376804 | Antibacterial activity against Shigella boydii | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Microbial transformations of hypolipemic E-guggulsterone. |
| AID1576229 | Antagonist activity at PPARgamma (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576267 | Effect on Rab27a gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576224 | Agonist activity at PPARalpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576269 | Effect on Cd38 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576281 | Antagonist activity at human wild type FXR expressed in HEK293T cells co-transfected with reporter vector harboring human FXR-IR1 response element sequence after 18 hrs in presence of 1 uM FXR agonist, UPF-930 by luciferase based reporter gene transactiva | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID376803 | Cytotoxicity against human NCI-H226 cells | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Microbial transformations of hypolipemic E-guggulsterone. |
| AID1576273 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for OCA-induced biotinylated SRC-1 recruitment at 10 uM after 30 mins in presence of FXR agonist, OCA by Alpha Screen assay (Rvb = 0.2 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576256 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Rab27a gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1667024 | Anti-austerity activity against human PANC1 cells assessed as cell killing incubated in nutrient deprived medium | 2020 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
| Synthesis of guggulsterone derivatives as potential anti-austerity agents against PANC-1 human pancreatic cancer cells. |
| AID1576235 | Antagonist activity at RXRalpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254766 | Inhibitory concentration against Androgen receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576266 | Effect on Rnf152 gene expression in FXR knockout mouse liver organoids assessed as log(2) fold change in expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576217 | Antagonist activity at GST-tagged FXR-LBD (unknown origin) assessed as inhibition of CDCA-induced biotinylated SRC-1 recruitment after 30 mins in presence of CDCA by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID254788 | Inhibitory concentration against Progesterone receptor | 2005 | Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
| Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
| AID1576218 | Agonist activity at LXR alpha (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576244 | Agonist activity at TR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576275 | Noncompetitive antagonist activity at GST-tagged human FXR-LBD domain assessed as EC50 for OCA-induced biotinylated SRC-1 recruitment at 100 uM after 30 mins in presence of FXR agonist, OCA by Alpha Screen assay (Rvb = 0.2 uM) | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576243 | Antagonist activity at PR (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576255 | Allosteric modulation of FXR in wild type mouse liver organoids assessed as log(2) fold change in Rnf152 gene expression at 50 uM after 8 hrs by Heat map RNA sequencing data based analysis relative to control | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID1576221 | Antagonist activity at LXR beta (unknown origin) by Alpha Screen assay | 2019 | MedChemComm, Aug-01, Volume: 10, Issue:8
| Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool. |
| AID376806 | Antibacterial activity against Escherichia coli | 1998 | Journal of natural products, Apr, Volume: 61, Issue:4
| Microbial transformations of hypolipemic E-guggulsterone. |
| AID1346734 | Mouse Farnesoid X receptor (1H. Liver X receptor-like receptors) | 2002 | Science (New York, N.Y.), May-31, Volume: 296, Issue:5573
| A natural product that lowers cholesterol as an antagonist ligand for FXR. |
| AID1346766 | Human Farnesoid X receptor (1H. Liver X receptor-like receptors) | 2002 | Molecular endocrinology (Baltimore, Md.), Jul, Volume: 16, Issue:7
| The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |