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ER-alpha Binding Assay from US Patent US20240131013: "TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS"
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
SummaryRelated BioAssays by Target
Protac activity at VHL/ERRalpha in human MCF7 cells assessed as maximum efficacy relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Protac activity at VHL/ERRalpha in human MCF7 cells
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Invivo protac activity at ERRalpha in human MDA-MB-231 cells xenografted mouse assessed as reduction in ERRalpha level in tumor at 100 mg/kg, ip administered 3 times a day
Protac activity at VHL/ERRalpha in human MCF7 cells assessed as maximum degradation
Protac activity at VHL/ERRalpha in human MCF7 cells relative to control
Binding Assay from US Patent US11285226: "Aryl ethene derivative and pharmaceutical composition containing same as active ingredient"
Assay data:32 Active, 32 Activity ≤ 1 µM, 32 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding Assay from US Patent US10934303: "Aryl ethene derivative and pharmaceutical composition containing same as active ingredient"
Assay data:28 Active, 13 Activity ≤ 1 µM, 28 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Assay data:28 Active, 28 Activity ≤ 1 µM, 28 Tested
Radioligand Displacement Assay from Article 10.1016/j.bbrc.2008.06.050: "ERRgamma tethers strongly bisphenol A and 4-alpha-cumylphenol in an induced-fit manner."
Assay data:3 Active, 3 Activity ≤ 1 µM, 4 Tested
ERRgamma FRET Assay from Article 10.1021/jm050161j: "Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma."
Assay data:7 Active, 5 Activity ≤ 1 µM, 7 Tested
Radioligand Displacement Assay from Article 10.1016/j.bmcl.2005.11.030: "Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma."
Assay data:11 Active, 1 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
Fluorescence Energy Transfer (FRET) Measurement from Article 10.1074/jbc.M703337200: "Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism."
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Competitive Radioligand-Binding Assay from US Patent US9604931: "Nuclear receptor binding agents"
Assay data:12 Active, 1 Activity ≤ 1 nM, 12 Activity ≤ 1 µM, 12 Tested
Modulation of ERRgamma (unknown origin) expressed in MG63 cells assessed as transcriptional activity up to 7.9 uM incubated for 18 hrs by dual-Glo luciferase assay relative to control
Agonist activity at recombinant full-length human ERRalpha expressed in MG63 cells assessed as transcriptional activation incubated for 18 hrs by dual-Glo luciferase assay relative to control
Assay data:13 Tested
Agonist activity at recombinant full-length human ERRalpha expressed in MG63 cells assessed as transcriptional activation incubated for 18 hrs by dual-Glo luciferase assay
Assay data:4 Active, 13 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of FITC-RIP140 peptide binding to N-terminal His-tagged human GST-ERRalpha-LBD (290 to 519 residues) expressed in Escherichia coli incubated for 4 hrs by fluorescence polarization assay
Assay data:12 Active, 11 Activity ≤ 1 µM, 13 Tested
Inhibition of FITC-RIP140 peptide binding to N-terminal His-tagged human GST-ERRalpha-LBD (290 to 519 residues) expressed in Escherichia coli incubated for 4 hrs by fluorescence polarization assay relative to control
Assay data:12 Tested
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