Affinity DataIC50: 8.90nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
3D Structure (crystal)
Affinity DataIC50: 9nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 9.10nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 9.20nMAssay Description:Antagonist activity at full length human FXR expressed in HeLa cells co-expressing BSEP-pGL3/pSG5-hRXR assessed as inhibition of GW4064-induced recep...More data for this Ligand-Target Pair
Affinity DataIC50: 9.30nMAssay Description:Antagonist activity at human FXR expressed in Huh7 cells assessed as inhibition of CDCA-induced FXR response element driven luciferase activity after...More data for this Ligand-Target Pair
Affinity DataIC50: 9.60nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 10nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 13.5nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 17nMAssay Description:Agonist activity at FXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 18nMAssay Description:Antagonist activity at human FXR expressed in Huh7 cells assessed as inhibition of CDCA-induced FXR response element driven luciferase activity after...More data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:The human FXRalpha LBD was expressed in E. coli strain BL21(DE3) as an N-terminally GST tagged fusion protein. The DNA encoding the FXR ligand bindin...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Agonist activity at FXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 20.5nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 21nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 21nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 22.5nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 23.5nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 24nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 24.4nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 27nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 27nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 28.3nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:The human FXRalpha LBD was expressed in E. coli strain BL21(DE3) as an N-terminally GST tagged fusion protein. The DNA encoding the FXR ligand bindin...More data for this Ligand-Target Pair
Affinity DataIC50: 31nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 33nMAssay Description:Antagonist activity at recombinant GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced Fluorecein-SRC2-2 coactivator peptide...More data for this Ligand-Target Pair
Affinity DataIC50: 35nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 35nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 35nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 35nMAssay Description:Antagonist activity at recombinant GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced Fluorecein-SRC2-2 coactivator peptide...More data for this Ligand-Target Pair
Affinity DataIC50: 35.7nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 37nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 38nMAssay Description:Antagonist activity at GST-tagged FXR LBD (unknown origin) assessed as inhibition of GW4064-induced fluorecein-labeled SRC2-2 coactivator recruitment...More data for this Ligand-Target Pair
Affinity DataIC50: 39nMpH: 7.4Assay Description:The assay buffer contained 50 mM HEPES (pH 7.4), 10 mM NaCl, 5 mM MgCl2 and 0.01% CHAPS. The reactions were incubated for 30 min in the presence of [...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 41nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataIC50: 41nMAssay Description:Antagonist activity at human FXR expressed in Huh7 cells assessed as inhibition of CDCA-induced FXR response element driven luciferase activity after...More data for this Ligand-Target Pair
