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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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated 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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
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 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
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 fluorescence-based thiol-reactive (MSTI) qHTS assay for identification of artifact compounds.
Assay data:494 Active, 184 Activity ≤ 1 µM, 5098 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Depositor
Inhibition of P2Y12 in human platelet rich plasma assessed as reduction in ADP-induced platelet aggregation pre-incubated before ADP addition and measured after 10 mins by Bruker spectrophotometry
Assay data:1 Active, 1 Activity ≤ 1 µM, 26 Tested
Primary qHTS to identify gynecologic anti-cancer compounds using libraries of approved drugs and bioactive compounds
Assay data:1106 Active, 14 Activity ≤ 1 nM, 6478 Activity ≤ 1 µM, 7578 Tested
Antagonist activity at P2Y12 receptor (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Antagonist activity at P2Y12 receptor in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay
Assay data:10 Active, 5 Activity ≤ 1 µM, 12 Tested
Antagonist activity at P2Y12 receptor in rat platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay
Assay data:13 Active, 9 Activity ≤ 1 µM, 14 Tested
Cmax in rat at 10 mg/kg, po
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
Cmax in dog at 1 mg/kg, po
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Displacement of [33P]2-MeS-ADP from human recombinant P2Y12 receptor expressed in CHO cell membranes by scintillation counting method
Assay data:60 Active, 1 Activity ≤ 1 nM, 59 Activity ≤ 1 µM, 63 Tested
Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets
Assay data:14 Active, 2 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 14 Tested
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