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Selectivity interaction (GPCR panel (PDSP screen)) EUB0001079a HTR6
Assay data:1 Tested
SummaryRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000276b HTR6
Activity against 5HT6/H in the Eurofins SafetyScreen44 (BI) by Others (Old_Cerep_3)
PDSP Primary Binding target: HTR6 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintilation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter.
Assay data:25 Active, 175 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
PDSP Secondary Binding target: HTR6 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
Assay data:25 Active, 17 Activity ≤ 1 µM, 27 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Antagonist activity at 5-HT6 receptor (unknown origin) assessed as equilibrium binding constant
Assay data:15 Active, 9 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]-LSD from 5-HT6 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay
Assay data:22 Active, 1 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
Binding affinity to 5-HT6 (unknown origin) at 10 uM
SummaryPubMed CitationRelated BioAssays by Target
Inverse agonist activity at human 5HT-6 receptor at Cdk5 signaling expressed in human NG108-15 cells assessed as reduction in neurite growth at 1 uM measured after 24 hrs by microscopic analysis
Assay data:2 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inverse agonist activity at human 5HT-6 receptor expressed in human NG108-15 cells assessed as inhibition of constitutive activity of receptor at Gs signaling by measuring basal cAMP level by CAMYEL probe based BRET analysis
Assay data:1 Active, 1 Tested
Neutral antagonist activity at human 5HT-6 receptor expressed in human NG108-15 cells assessed as constitutive activity of receptor at Gs signaling by measuring basal cAMP level by CAMYEL probe based BRET analysis
Antagonist activity at human 5HT-6 receptor expressed in human 1321N1 cells assessed as increases in 5-CT induced cyclic-AMP production by measuring equilibrium binding constant incubated for 30 mins by Lance cAMP assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Displacement of [3H]-LSD from human 5HT-6 receptor expressed in HEK293 cell membranes assessed as inhibition constant measured after 1 hr by microplate reader analysis
Assay data:25 Active, 21 Activity ≤ 1 µM, 25 Tested
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells assessed as inhibition constant incubated for 120 mins by spectrophotometric analysis
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells incubated for 120 mins by spectrophotometric analysis
Displacement of [3H] LSD from human recombinant 5-HT6 receptor expressed in human HeLa cells at 10 uM incubated for 120 mins by spectrophotometric analysis relative to control
Assay data:2 Tested
Inhibition of [3H]LSD from binding to 5-HT6 receptor (unknown origin) at 10 uM relative to control
Inhibition of human 5-HT6 receptor assessed as inhibition constant by microbeta scintillation counting method
Inhibition of human 5-HT6 receptor at 10 uM by microbeta scintillation counting method relative to control
Assay data:8 Tested
Antagonist activity at human 5-HT6 receptor expressed in CHO-K1 cells coexpressing Galpha16 and mitochondrially targeted aequorin assessed as equilibrium binding constant preincubated for 30 mins followed by agonist addition and further incubated for 16 hrs without light by luminescence based assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
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