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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
SummaryRelated BioAssays by Target
Purinergic P2X Eurofins Panlabs panel
Assay data:1 Tested
Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX3
Assay data:1 Active, 1 Tested
Inhibition of P2X3 receptor (unknown origin)
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human P2X2R/P2X3R expressing CHO cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed by compound addition and further incubated for 30 mins in presence of ATP by multimode plate reader analysis
Assay data:3 Tested
Antagonist activity at human P2X3R expressing CHO cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed by compound addition and further incubated for 30 mins in presence of ATP by multimode plate reader analysis
Agonist activity at human P2X2R/P2X3R expressing CHO cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed by compound addition and further incubated for 30 mins in presence of ATP by multimode plate reader analysis
Assay data:10 Active, 7 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human P2X3R expressing CHO cells assessed as reduction in intracellular Ca2+ influx pretreated with Fluo-4 for 1 hr followed by compound addition and further incubated for 30 mins in presence of ATP by multimode plate reader analysis
Assay data:6 Active, 3 Activity ≤ 1 µM, 16 Tested
Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reduction in alphabeta-MeATP-induced intracellular Ca2+ influx pretreated with compound followed by alphabeta-MeATP addition and measured by Fluo-4 dye fluorescence analysis
Assay data:12 Active, 5 Activity ≤ 1 µM, 21 Tested
Non-competitive antagonist activity at human P22X3 receptor assessed as right shift in alphabetameATP-induced calcium influx by measuring maximum efficacy of agonist at 200 nM relative to control
Assay data:2 Tested
Antagonist activity at human P2X2R/P2X3R by cell based assay
Assay data:3 Active, 3 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human P2X3 receptor at 2 uM by cell based assay relative to control
Assay data:8 Tested
Antagonist activity at human P2X3 receptor by cell based assay
Assay data:11 Active, 8 Activity ≤ 1 µM, 18 Tested
Antagonist activity at human P2X3R transfected in CHO-K1 cells at 30 uM preincubated for 30 mins followed by alpha,beta-meATP addition by fluorescence based assay relative to control
Assay data:20 Tested
Antagonist activity at human P2X3R transfected in CHO-K1 cells preincubated for 30 mins followed by alpha,beta-meATP addition by fluorescence based assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human P2X2/3R transfected in CHO-K1 cells at 30 uM preincubated for 30 mins followed by alpha,beta-meATP addition by fluorescence based assay relative to control
Antagonist activity at human P2X2/3R transfected in CHO-K1 cells preincubated for 30 mins followed by alpha,beta-meATP addition by fluorescence based assay
Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reduction in intracellular Ca2+ influx at 10 uM pretreated with Fluo-4 for 1 hr followed by compound addition and further incubated for 30 mins in presence of ATP by multimode plate reader analysis relative to control
Assay data:4 Tested
Antagonist activity at rat P2X3 receptor
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
Antagonist activity at P2X3 receptor (unknown origin)
Assay data:38 Active, 37 Activity ≤ 1 µM, 38 Tested
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