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Selectivity interaction (Lead profiling screen (Eurofins, GPCRs, ion channels, kinases and transporters)) EUB0000309b P2RX1
Assay data:1 Tested
SummaryRelated BioAssays by Target
Inhibition of P2X1 receptor (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Antagonist activity at human P2X1R 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
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human P2X1R 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 Active, 1 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human P2X1R transfected in CHO-K1 cells at 30 uM preincubated for 30 mins followed by alpha,beta-meATP addition by luminescence based assay relative to control
Assay data:20 Tested
Antagonist activity at human P2X1R transfected in CHO-K1 cells preincubated for 30 mins followed by alpha,beta-meATP addition by luminescence based assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human P2X1R 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 P2X1 receptor (unknown origin)
Antagonist activity at human P2X1 receptor expressed in rat C6-BU-1 cells
Antagonist activity at P2X1 receptor in human platelet assessed as inhibition of thrombin-induced platelet aggregation at 10 '-5 to 10'-6 mol/L pretreated with compound and LPS/BzATP for 10 mins followed by thrombin addition and measured for 8 mins by aggregometry analysis
Assay data:8 Tested
Antagonist activity P2X1 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation pre-incubated for 30 mins before ADP stimulation by aggregometry relative to control
Assay data:5 Tested
Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of TRAP6-induced platelet aggregation pre-incubated for 30 mins before TRAP6 stimulation by aggregometry relative to control
Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of collagen-induced platelet aggregation pre-incubated for 30 mins before collagen stimulation by aggregometry relative to control
Assay data:2 Tested
Antagonist activity P2X1 receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation pre-incubated for 30 mins before ADP stimulation by aggregometry
Assay data:2 Active, 7 Tested
Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of TRAP6-induced platelet aggregation pre-incubated for 30 mins before TRAP6 stimulation by aggregometry
Assay data:3 Active, 7 Tested
Antagonist activity P2X1 receptor in Apyrase pre-treated human platelets assessed as inhibition of collagen-induced platelet aggregation pre-incubated for 30 mins before collagen stimulation by aggregometry
Assay data:5 Active, 1 Activity ≤ 1 µM, 7 Tested
Negative allosteric modulator activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of maximal response for ATP-induced calcium influx at 100 to 500 nM pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control
Assay data:2 Active, 2 Tested
Antagonist activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx at 100 uM pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control
Antagonist activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control
Assay data:47 Active, 29 Activity ≤ 1 µM, 65 Tested
Antagonist activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx at 1 uM pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control
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