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Binding affinity to recombinant human LRH1 ligand binding domain (300 to 537 residues) expressed in Escherichia coli BL21 cells assessed as destabilization of AF-H part near AFB region of receptor at 5-fold molar excess to protein concentration incubated overnight at 4 degC by HDX mass spectrometry
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Binding affinity to recombinant human LRH1 ligand binding domain (300 to 537 residues) expressed in Escherichia coli BL21 cells assessed as stabilization of helix 4 near AFS region of receptor at 5-fold molar excess to protein concentration incubated overnight at 4 degC by HDX mass spectrometry
Agonist activity at human full length LRH1 transfected in human HeLa cells assessed as relative efficacy incubated for 24 hrs by renilla luciferase reporter gene assay relative to RJW100
Assay data:15 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at recombinant human LRH1 ligand binding domain (300 to 537 residues) expressed in Escherichia coli BL21 cells assessed as increase in fluorescein-labeled Tif2 peptide coactivator recruitment by fluorescence polarization assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Activation of human full length LRH1 H390A mutant transfected in human HeLa cells at 10 uM incubated for 24 hrs by renilla luciferase reporter gene assay
Assay data:1 Active, 2 Tested
Activation of human full length LRH1 M345L mutant transfected in human HeLa cells at 10 uM incubated for 24 hrs by renilla luciferase reporter gene assay
Agonist activity at recombinant full length SF1 (unknown origin) transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay
Assay data:3 Active, 4 Tested
Binding affinity to recombinant human LRH1 ligand binding domain (300 to 537 residues) expressed in Escherichia coli BL21 cells assessed as receptor stabilization by measuring change in melting temperature at saturating concentration incubated for overnight at 4 degC by differential scanning fluorimetry relative to RJW100
Assay data:6 Tested
Agonist activity at human full length LRH1 transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay
Assay data:15 Active, 9 Activity ≤ 1 µM, 32 Tested
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