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Antagonist activity at human ADRA2A in an in vitro cell-based assay measured by fluorescent imaging plate reader
Assay data:80 Active, 18 Activity ≤ 1 µM, 1172 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Human gonadotropin-releasing hormone receptor (GnRHR) small molecule agonists, calcium flux assay in GnRHR-HEK293 cells: Summary
Assay data:109 Active, 9667 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Same Project
HTRF Coactivator Recruitment Assay from Article 10.1073/pnas.0710981105: "Identification of a potent synthetic FXR agonist with an unexpected mode of binding and activation."
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
TGR5 Activity Assay from Article 10.1021/jm070633p: "Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5."
Assay data:6 Active, 3 Activity ≤ 1 µM, 9 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Agonist activity at glutathione transferase-tagged human FXR-LBD using biotinylated Src-1 peptide incubated for 30 mins by recruitment coactivator assay
Assay data:8 Active, 4 Activity ≤ 1 µM, 10 Tested
Agonist activity at FXR in human HepG2 cells assessed as increase in BSEP mRNA expression at 30 uM incubated for 8 hrs by qRT-PCR analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at FXR in human HepG2 cells assessed as increase in SHP mRNA expression at 30 uM incubated for 8 hrs by qRT-PCR analysis
Cytochrome P450 Family 1 Subfamily A Member 2 (CYP1A2) small molecule antagonists: luciferase reporter qHTS assay
Assay data:2934 Active, 132 Activity ≤ 1 µM, 9667 Tested
Cytochrome P450 Family 2 Subfamily C Member 9 (CYP2C9) small molecule antagonists: luciferase reporter qHTS assay
Assay data:2931 Active, 3 Activity ≤ 1 nM, 133 Activity ≤ 1 µM, 9667 Tested
Cytochrome P450 Family 2 Subfamily C Member 19 (CYP2C19) small molecule antagonists: luciferase reporter qHTS assay
Assay data:3508 Active, 4 Activity ≤ 1 nM, 319 Activity ≤ 1 µM, 9667 Tested
Cytochrome P450 Family 2 Subfamily D Member 6 (CYP2D6) small molecule antagonists: luciferase reporter qHTS assay
Assay data:2225 Active, 268 Activity ≤ 1 µM, 9667 Tested
Agonist activity at GST-tagged FXR-LBD (unknown origin) assessed as biotinylated SRC-1 recruitment after 30 mins by Alpha Screen assay
Assay data:1 Active, 2 Tested
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as reduction in NTCP protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as reduction in CYP8B1 protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as reduction in CYP7A1 protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in SULT2A1 protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in MRP2 protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in BSEP protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Agonist activity at FXR in guggulsterone-treated human LO2 cells assessed as increase in SHP1 protein expression at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
Increase in FXR protein expression in guggulsterone-treated human LO2 cells at 80 uM treated with FXR antagonist, guggulsterone for 24 hrs followed by incubation with compound for 24 hrs by western blot analysis
SummaryCompounds, ActivePubMed Citation
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