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Antagonist activity at human recombinant LRH-1 LBD (91 to 541 residues)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of full length LRH1 in HEK293T cells at 10 uM incubated for 20 hrs by luciferase reporter assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of full length LRH1 in HEK293T cells at 550 nM incubated for 20 hrs by luciferase reporter assay relative to control
Inhibition of full length LRH1 transfected in HEK293T cells incubated for 20 hrs by luciferase reporter assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human full length LRH1 transfected in human HepG2 cells assessed as fold increase in expression of CYP24A1 at 10 uM incubated for 16 hrs by RT-qPCR analysis
Assay data:2 Tested
Agonist activity at human full length LRH1 transfected in human HeLa cells
Assay data:1 Active, 2 Tested
Agonist activity at human full length LRH1 transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay relative to control
Binding affinity to human LRH-1
Antagonist activity at human LRH-1
Assay data:2 Active, 2 Tested
Inhibition of Wnt in human HEK293 cells assessed as reduction in STF expression at 1 to 3 uM by Western blot analysis
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inverse agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with PGC-1 assessed as downregulation of PGC-1 expression at 5 to 500 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with PGC-1 assessed as effect on PGC-1 expression at 0.1 to 10 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Inverse agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with SRC3 assessed as downregulation of SRC3 expression at 0.1 to 10 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Inverse agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with p300 assessed as downregulation of p300 expression at 0.1 to 10 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with PGC-1 assessed as effect on PGC-1 expression at 5 to 500 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Inverse agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with PGC-1 assessed as downregulation of PGC-1 expression incubated for 24 hrs by DualGlo luciferase reporter assay
Agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with NCOR1 assessed as minimal effect of NCOR1 at 5 to 500 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Agonist activity to full length LRH-1 (unknown origin) transfected in human HeLa cells co-transfected with NCOR1 assessed as minimal effect of NCOR1 at 0.1 to 10 uM incubated for 24 hrs by DualGlo luciferase reporter assay
Binding affinity to N-terminal 6-His tagged human LRH-1 LBD (299 to 541 residues) expressed in Escherichia coli BL21-(DE3) assessed as dissociation constant of SHP using FAM-labeled +H3N-QGAASRPAILYALLSSSLK-CO2- peptide as substrate incubated overnight followed by substrate addition incubated for overnight by fluorescence polarization assay (Rvb = 1200 nM)
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Binding affinity to N-terminal 6-His tagged human LRH-1 LBD (299 to 541 residues) expressed in Escherichia coli BL21-(DE3) assessed as dissociation constant of PGC-1alpha using FAM-labeled +H3N-EAEEPSLLKKLLLAPANTQ-CO2- peptide as substrate incubated overnight followed by substrate addition incubated for overnight by fluorescence polarization assay (Rvb = 1300 nM)
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