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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
SummaryRelated BioAssays by Target
Evaluation of In Vitro Biological Activity from US Patent US20240034729: "HETEROCYCLIC COMPOUND, INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF"
Assay data:163 Active, 4 Activity ≤ 1 nM, 193 Activity ≤ 1 µM, 194 Tested
Purinergic P2X Eurofins Panlabs panel
Assay data:1 Tested
Antagonist activity against human 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
Antagonist activity against mouse P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay
Antagonist activity against rat P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay
Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX7
Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX3
Assay data:1 Active, 1 Tested
Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX1
Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX4
Affinity On-target Cellular interaction (FLIPR assay (inhibition of ATP-induced calcium influx in HEK293 cells, stably transfected with human P2X4 receptor)) EUB0000548a P2RX4
Affinity On-target Cellular interaction (FLIPR assay (inhibition of ATP-induced calcium influx in HEK293 cells, stably transfected with human P2X4 receptor)) EUB0000309b P2RX4
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Affinity Phenotypic Cellular interaction (Ephys Qpatch Assay in HEK293 cells) EUB0000309b P2RX4
Antagonist activity at P2X7 receptor in human RPMI-8226 cells assessed as inhibition of ATP-induced Ca2+ influx at 10 uM by fura-2 staining based assay relative to control
Assay data:6 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at P2X7 receptor in human RPMI-8226 cells assessed as inhibition of ATP-induced Ca2+ influx by fura-2 staining based assay
Assay data:31 Active, 18 Activity ≤ 1 µM, 46 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to human P2X7R assessed as inhibition constant
Inhibition of human P2X7R
Assay data:6 Active, 1 Activity ≤ 1 nM, 6 Activity ≤ 1 µM, 6 Tested
Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as reduction in BzATP-induced activity incubated for 5 to 10 mins by EtBr staining based fluorescence assay
Assay data:5 Active, 4 Activity ≤ 1 µM, 6 Tested
Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as BzATP Emax at 0.2 uM incubated for 30 mins by Fura-2 AM staining based calcium influx assay relative to control
Antagonist activity against human P2X7R stably transfected in human 1321N1 cells assessed as BzATP Emax at 0.1 uM incubated for 30 mins by Fura-2 AM staining based calcium influx assay relative to control
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