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Radioligand Binding Assay from US Patent US11642336: "5-HT2A agonists for use in treatment of depression"
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR5A
Assay data:1 Active, 1 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000705a HTR5A
Binding affinity to 5-HT5A receptor (unknown origin) at 10000 nM by radioligand displacement assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of serotonin 5-HT5A receptor (unknown origin) at 10 uM relative to control
Binding affinity to 5HT5A receptor (unknown origin) assessed as inhibition constant
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to 5-HT5A receptor (unknown origin) assessed as inhibition constant
Assay data:5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
5-HT5A (h) (5-ht5a) CEREP panel
SummaryRelated BioAssays by Target
Displacement of [3H]-5-CT from human 5-HT5A receptor incubated for 2 hr by radioligand binding assay
Assay data:3 Active, 3 Activity ≤ 1 µM, 7 Tested
Displacement of [3H]-5-CT from human 5-HT5A receptor at 1 uM incubated for 2 hr by radioligand binding assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Displacement of [3H]-5-CT from human 5-HT5A receptor at 32 uM incubated for 2 hr by radioligand binding assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
Antagonist activity at human 5-HT5AR assessed as stimulation of [35S]GTPgammaS binding at 100 uM incubated for 3 to 5 hrs
Assay data:6 Active, 6 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human 5-HT5AR assessed as inhibition of beta-arrestin 2 recruitment by measuring reduction in RLuc8-based luminescence incubated for 20 to 30 mins in absence of agonist by luminescence based analysis
Binding affinity to human 5-HT5AR
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment by measuring maximal efficacy at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay relative to control
Assay data:2 Tested
Agonist activity at human 5-HT5A receptor transfected in HTLA cells assessed as increase in beta-arrestin 2 recruitment at 10 uM incubated for 18 to 20 hrs by bright-Glo reagent based Tango assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Displacement of [3H]-5-CT from human 5-HT5A receptor at 100 uM incubated for 2 hr by radioligand binding assay
Binding affinity to 5-HT5AR (unknown origin)
Assay data:15 Active, 11 Activity ≤ 1 µM, 16 Tested
Binding Assay or Functional Activity Assay from US Patent US9481688: "(Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists"
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Binding Assay from US Patent US8962612: "Tetrahydroisoquinoline derivative"
Assay data:20 Active, 5 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 20 Tested
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