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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
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
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
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
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
Assay data:2 Tested
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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)
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 SRC3 using FAM-labeled +H3N-KKENNALLRYLLDRDDPSD-CO2- peptide as substrate incubated overnight followed by substrate addition incubated for overnight by fluorescence polarization assay (Rvb = 7 microM)
Assay data:3 Active, 3 Tested
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of Gm2a mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of N-sdhl mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of S-qle mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of A-caca mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of P-csk9 mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of L-dlr mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of H-mgcr mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of A-cly mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
Agonist activity at LRH-1 in human HepG2 cells assessed as downregulation of Ttc39c mRNA expression at 10 uM incubated for 24 hrs by RT-qPCR based RNA-seq analysis
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