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Human P2X7 Channel Calcium-Influx Assay from US Patent US20240034737: "Heterocyclic Derivatives as P2X7 Receptor Antagonists"
Assay data:103 Active, 103 Activity ≤ 1 µM, 103 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Antagonist activity against mouse P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Displacement of [3H]-A-804598 from mouse P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis
Assay data:12 Active, 1 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 13 Tested
Antagonist activity at mouse P2X7R expressed in mouse CT26 cells assessed as reduction in ethidium bromide uptake by cells at 100 uM in presence of BzATP
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at mouse P2X7R expressed in mouse MC38 cells assessed as reduction in ethidium bromide uptake by cells at 100 uM in presence of BzATP
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
P2X7 FLIPR Assay from US Patent US10053463: "Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators"
Assay data:123 Active, 18 Activity ≤ 1 nM, 109 Activity ≤ 1 µM, 125 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
P2X7 Radioligand Binding from US Patent US10053463: "Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators"
Assay data:99 Active, 3 Activity ≤ 1 nM, 98 Activity ≤ 1 µM, 99 Tested
P2X7 FLIPR Assay from US Patent US10053462: "P2X7 modulators"
Assay data:55 Active, 51 Activity ≤ 1 µM, 56 Tested
P2X7 Radioligand Binding Assay from US Patent US10053462: "P2X7 modulators"
Assay data:51 Active, 51 Activity ≤ 1 µM, 51 Tested
Antagonist activity at P2X7R in mouse N2a cells assessed as reduction in ATP-induced EtBr uptake by cells at 0.1 to 10 uM incubated for 1 hr by fluorescence based assay
Antagonist activity at P2X7R in mouse N2a cells assessed as reduction in ATP-induced calcium influx at 5 uM incubated for 1 hr by Fluo-3AM dye based laser scanning microscopy
Antagonist activity at P2X7R in mouse N2a cells assessed as reduction in ATP-induced calcium influx at 50 uM incubated for 1 hr by Fura-2AM dye based spectrofluorometry
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced NO production at 0.1 to 10 uM incubated for 1 hr by using DAF-FM probe based fluorescence assay
Assay data:1 Tested
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced NO production by measuring NO level at 1 uM incubated for 1 hr by using DAF-FM probe based fluorescence assay relative to control
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced NO production by measuring NO level at 10 uM incubated for 1 hr by using DAF-FM probe based fluorescence assay relative to control
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced NO production at 50 uM incubated for 1 hr by using DAF-FM probe based fluorescence assay
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced NO production at 10 uM incubated for 1 hr by using DAF-FM probe based fluorescence assay
Antagonist activity at P2X7R in mouse N2a cells assessed as inhibition of ATP-induced ROS production at 1 uM incubated for 1 hr by using H2DCF-DA probe based fluorescence assay relative to control
Antagonist activity at P2X7R in mouse N2a cells assessed as cytoprotective activity against ATP-induced cell death by measuring increase in cell viability at 0.1 to 5 uM incubated for 1 hr followed by ATP addition and measured after 48 hrs by MTT assay
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