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Antagonist activity at human glycine receptor subunit alpha-1 assessed as inhibition of glycine-induced current measured at the later state of compound application by patch-clamp assay
Assay data:5 Active, 5 Activity ≤ 1 µM, 5 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Antagonist activity at human glycine receptor subunit alpha-1 assessed as inhibition of glycine-induced current measured at the onset of compound application by patch-clamp assay
Assay data:5 Active, 2 Activity ≤ 1 µM, 5 Tested
Displacement of [3H]strychnine from human glycine receptor subunit alpha-1 expressed in HEK293 cell membranes preincubated for 30 mins followed by [3H]strychnine addition and measured after 30 mins by liquid scintillation counting method
Antagonist activity at human glycine receptor subunit alpha-1beta expressed in HEK293 cells assessed as reduction in glycine-induced currents by whole-cell patch-clamp assay
Assay data:4 Active, 2 Activity ≤ 1 µM, 4 Tested
Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced currents by whole-cell patch-clamp assay
Assay data:13 Active, 7 Activity ≤ 1 µM, 13 Tested
Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay
Assay data:22 Active, 5 Activity ≤ 1 µM, 27 Tested
Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response incubated for 30 mins by fluorescence-based FLIPR membrane potential blue assay
Assay data:22 Active, 4 Activity ≤ 1 µM, 27 Tested
Agonist activity at human TAS2R46 stably expressed in HEK293T/Galpha16-gustducin 44 cells assessed as effect on calcium flux by measuring deltaF/F0 ratio by Fluo-4-AM dye based FLIPR assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Activity at human TAS2R10 expressed in HEK-293T-Galpha16-gustducin44 cells assessed as threshold concentration of compound at which point receptor detects compounds by measuring calcium response by FLIPR assay
Assay data:4 Active, 4 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
Activity at human TAS2R10 expressed in HEK293/15 cells assessed as compound concentration showing threshold of activation on calcium response by FLIPR assay
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Activity at human TAS2R10 expressed in HEK293/15 cells assessed as effect on calcium response by FLIPR assay
Assay data:2 Active, 2 Tested
Antagonist activity at human glycine receptor subunit alpha-1beta expressed in HEK293 cells assessed as reduction in glycine-induced whole cell currents by patch-clamp technique
Assay data:2 Active, 2 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human glycine receptor subunit alpha-1 expressed in HEK293 cells assessed as reduction in glycine-induced whole cell currents by patch-clamp technique
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human glycine receptor subunit alpha-1beta expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human glycine receptor subunit alpha-1 expressed in human tsA201 cells assessed as reduction in glycine-induced response by fluorescence-based FLIPR membrane potential blue assay
Displacement of [3H]strychnine from human glycine receptor subunit alpha-1 expressed in HEK293 cell membranes
Displacement of [3H]strychnine from recombinant human glycine receptor alpha 1 expressed in HEK293 cell membranes after 30 mins by liquid scintillation counting method
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Displacement of [3H]strychnine from glycine receptor alpha 1 in rat brain synaptic membranes
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Antagonist activity at recombinant human glycine receptor alpha 1 beta expressed in HEK293 cells assessed as inhibition of glycine-induced current at -50mV holding potential by whole cell patch-clamp method
Assay data:9 Active, 8 Activity ≤ 1 µM, 9 Tested
Antagonist activity at recombinant human glycine receptor alpha 1 expressed in HEK293 cells assessed as inhibition of glycine-induced current at -50 mV holding potential by whole cell patch-clamp method
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