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MT1/MT2 Receptor Binding Assay from US Patent US11980598: "N-(2-(substituted-naphth-1-yl)ethyl) substituted amide compound, preparation and uses thereof"
Assay data:3 Active, 3 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Agonist activity at human melatonin MT2 receptor stably expressing in human HEK293 cells
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells
Agonist activity at human MT2R stably expressed in HEK293 cells at 1 mM by FlexStation3 Bench-top MultiMode Microplate Reader relative to control
Assay data:1 Tested
Agonist activity at human MT1R stably expressed in HEK293 cells at 1 mM by FlexStation3 Bench-top MultiMode Microplate Reader relative to control
Agonist activity at human MT2R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
Agonist activity at human MT1R stably expressed in HEK293 cells by FlexStation3 Bench-top MultiMode Microplate Reader
Selectivity interaction (CEREP panel (Eurofins, radioligand binding assay, enzymes, GPCRS, transporters, and ion channels)) EUB0000308b MTNR1A
SummaryRelated BioAssays by Target
Selectivity interaction (CEREP Wide Ligand screening panel (ion channels, receptors, enzymes)) EUB0000304b MTNR1B
Selectivity interaction (CEREP panel (receptors, ion channels)) EUB0000222b MTNR1A
Binding affinity to human melatonin MT1 assessed as inhibition constant
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor stably expressing in human HEK293 cell membranes upto 1 uM in presence of light-activated compounds by radioligand based competition binding assay
Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor stably expressing in human HEK293 cell membranes upto 1 uM under dark condition by radioligand based competition binding assay
Agonist activity at human melatonin MT2 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring maximal efficacy after 30 mins under dark condition by cAMP assay relative to control
Agonist activity at human melatonin MT2 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
Assay data:3 Active, 2 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 4 Tested
Agonist activity at human melatonin MT2 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
Assay data:4 Active, 1 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 5 Tested
Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor stably expressing in human HEK293 cell membranes upto 1 uM under dark condition by radioligand based competition binding assay
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring maximal efficacy after 30 mins under dark condition by cAMP assay relative to control
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins in presence of light-activated compounds by cAMP assay
Assay data:3 Active, 3 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 4 Tested
Agonist activity at human melatonin MT1 receptor stably expressing in human HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins under dark condition by cAMP assay
Assay data:4 Active, 2 Activity ≤ 1 nM, 4 Activity ≤ 1 µM, 5 Tested
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