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Compound was evaluated for inhibition of rat Slc18a2 in an ex vivo assay measured by radioactivity method
Assay data:39 Active, 1 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 82 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Methods for Determining VMAT2 Inhibitory Activity of a Compound from US Patent US11718618: "Substituted pyrido[2,1-a]isoquinolines as VMAT2 inhibitors"
Assay data:98 Active, 10 Activity ≤ 1 nM, 98 Activity ≤ 1 µM, 106 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (Radioligand binding assay (MDS Pharma Service)) EUB0000296b SLC18A2
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Selectivity interaction (Enzyme and Receptor panel (MSD Pharma/Taiwan)) EUB0000750a SLC18A2
Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells (PubChem AID: 1794817)
Assay data:3 Active, 2 Activity ≤ 1 µM, 3 Tested
Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells (PubChem AID: 1794818)
Assay data:2 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of vesicular monoamine transporter 2 (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of rat VMAT2 transfected in HEK cells using FFN206 as fluorescent substrate preincubated for 1 hr followed by substrate addition and measured after 30 mins by fluorescence plate reader assay
Assay data:12 Active, 7 Activity ≤ 1 µM, 12 Tested
Determining human Vmat2 Inhibitory Activity of a Compound from US Patent US11053242: "[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11BH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto"
Assay data:133 Active, 154 Activity ≤ 1 µM, 154 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Determining Vmat2 Inhibitory Activity of a Compound from US Patent US11053242: "[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11BH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto"
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibitory Activity Assay from US Patent US11040970: "VMAT2 inhibitor compounds and compositions thereof"
Assay data:41 Active, 42 Activity ≤ 1 µM, 42 Tested
[3H]TBZOH Binding Assay from Article 10.1074/jbc.M113.502971: "Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
[3H]Serotonin Uptake Assay from Article 10.1074/jbc.M113.502971: "Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine."
FFN206 based assay for SLC18A1 using HEK-293 SLC18A1 OE cells
FFN206 based assay for SLC18A2 using HEK-293 SLC18A2 OE cells
Transporter, Monoamine Eurofins-Panlabs radioligand binding assay
Assay data:2 Tested
SummaryRelated BioAssays by Target
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method
Assay data:9 Active, 9 Activity ≤ 1 µM, 12 Tested
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome at 0.1 uM incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method relative to control
Assay data:10 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome at 1 uM incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method relative to control
Inhibition of [3H]DTBZ binding to VMAT2 in rat brain incubated for 30 mins by liquid scintillation spectrometry analysis
Assay data:17 Active, 24 Activity ≤ 1 µM, 24 Tested
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