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GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183
Assay data:52 Active, 3 Activity ≤ 1 µM, 54 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3
Assay data:26 Active, 42 Tested
SummaryCompounds, Active
PDSP Primary Binding target: TMEM97 - 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:76 Active, 175 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
PDSP Primary Binding target: SLC6A3 - 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:43 Active, 174 Tested
PDSP Secondary Binding target: TMEM97 - 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:74 Active, 45 Activity ≤ 1 µM, 74 Tested
PDSP Secondary Binding target: SLC6A3 - 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:37 Active, 17 Activity ≤ 1 µM, 39 Tested
Antagonist activity at human P2Y12R expressed in HEK293 cells assessed as inhibition of MeSADP-induced cAMP production preincubated for 0.5 hrs followed by MeSADP stimulation by cAMP-glo analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human TBXA2R in an in vitro cell-based assay measured by fluorescence spectroscopy
Assay data:34 Active, 15 Activity ≤ 1 µM, 906 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity towards human SLC6A3 in an in vitro assay with cellular components measured by scintillation counting
Assay data:128 Active, 38 Activity ≤ 1 µM, 927 Tested
Binding affinity towards human SLC29A1 in an in vitro assay with cellular components measured by scintillation proximity assay
Assay data:20 Active, 4 Activity ≤ 1 µM, 1115 Tested
Binding affinity towards human PGR in an in vitro assay with cellular components measured by scintillation counting
Assay data:87 Active, 51 Activity ≤ 1 µM, 927 Tested
Antagonist activity human CHRM1 in an in vitro cell-based assay measured by fluorescence spectroscopy
Assay data:120 Active, 64 Activity ≤ 1 µM, 812 Tested
Binding affinity towards human ADORA3 (agonistic activity) in an in vitro assay with cellular components measured by scintillation counting
Assay data:92 Active, 18 Activity ≤ 1 µM, 754 Tested
Antagonist activity at human P2Y13R expressed in HEK293 cells assessed as inhibition of 2MeSADP-induced cAMP production preincubated for 0.5 hrs followed by 2MeSADP stimulation by cAMP-glo assay
Inhibition of P2Y12 receptor in human platelet assessed as reduction in ADP-induced VASP phosphorylation by flow cytometry
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antiplatelet activity against ADP-induced human platelet in platelet rich plasma assessed as inhibition of platelet aggregation preincubated for 2 mins followed by ADP stimulation and measured for 5 mins by aggregometry
Assay data:13 Active, 9 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of P2Y12 (unknown origin)
Assay data:5 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 5 Tested
Primary Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:968 Active, 24930 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Confirmatory Screen for Target Class Profiling of Small Molecule Inhibitors of Methyltransferases
Assay data:902 Active, 1111 Tested
Inhibition of TRAP6-induced platelet aggregation in human platelet preincubated for 5 mins followed by TRAP6-stimulation and measured after 6 mins by lumi-aggregometric method
Assay data:1 Active, 12 Tested
SummaryCompounds, ActivePubMed Citation
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