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Activation of human mineralocorticoid receptor transfected in HEK293T cells at 10 nM incubated for 16 hrs by luciferase based analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Activation of human mineralocorticoid receptor transfected in HEK293T cells incubated for 16 hrs by luciferase based analysis
Assay data:1 Active, 2 Tested
Agonist activity at human MR expressed in CHO-K1 cells by PathHunter assay
Assay data:1 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human MR expressed in CHO-K1 cells assessed as maximum relative efficacy at 100 uM by PathHunter assay relative to aldosterone
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human wild-type mineralocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of aldosterone-induced transcriptional activity incubated for 24 hrs in presence of 1 nM aldosterone by Steady-Glo reagent based reporter gene assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human wild-type mineralocorticoid receptor expressed in CHO-K1 cells assessed as inhibition of aldosterone-induced transcriptional activity incubated for 24 hrs in presence of 1 nM aldosterone by Steady-Glo reagent based reporter gene assay relative to control
Assay data:3 Tested
Displacement of [3H]-aldosterone from recombinant human mineralocorticoid receptor expressed in baculovirus infected insect cells incubated overnight by liquid scintillation counting analysis
Assay data:16 Active, 13 Activity ≤ 1 µM, 16 Tested
Displacement of [3H]-aldosterone from rat mineralocorticoid receptor incubated overnight by liquid scintillation counting analysis
Assay data:18 Active, 10 Activity ≤ 1 µM, 23 Tested
Agonist activity at mineralocorticoid receptor (unknown origin) expressed in HEK293T cells co-transfected with pGL4.36[luc2P MMTV Hygro]/Renilla at 10 to 25 uM incubated for 16 hrs by luciferase reporter gene assay
Antagonist activity at mineralocorticoid receptor (unknown origin) transfected in PC-3 cells assessed as inhibition of aldosterone-stimulated transcriptional activity after 3 days by dual luciferase reporter assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 4 Tested
Agonist activity at mineralocorticoid receptor in human PC-3 cells by dual-Glo luciferase assay
Assay data:2 Tested
Antagonist activity at mineralocorticoid receptor in human PC-3 cells assessed as reduction in aldosterone-induced luciferase activity at 10 uM by dual-Glo luciferase assay
Binding Assay from US Patent US9394291: "Benzoxazinone amides as mineralocorticoid receptor modulators"
Assay data:5 Active, 3 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Assay data:10 Active, 8 Activity ≤ 1 µM, 10 Tested
Receptor Binding Assay from US Patent US9034856: "17-(1′propenyl)-17-3′-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative"
Assay data:12 Active, 12 Activity ≤ 1 µM, 12 Tested
Competitive Molecular Binding Assay from US Patent US8722709: "Mineralocorticoid receptor antagonists"
Assay data:55 Active, 41 Activity ≤ 1 µM, 57 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
scintillation proximity assay (SPA) from US Patent US10017502: "Benzoxazinone amides as mineralocorticoid receptor modulators"
Assay data:16 Active, 11 Activity ≤ 1 µM, 18 Tested
Competitive Receptor Binding Assay from Article 10.1021/jm050205o: "Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators."
Assay data:7 Active, 2 Activity ≤ 1 nM, 7 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Fluorescence Polarization Competitive Binding Assay. from Article 10.1016/j.bmcl.2007.07.021: "Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists."
Assay data:24 Active, 23 Activity ≤ 1 µM, 28 Tested
Competitive Ligand Binding Assay, GR-Mediated Agonist Activity Assay, and IL-6 Repression Assay from Article 10.1021/jm070370z: "Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma."
Assay data:8 Active, 3 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
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