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Agonist activity at mGlu3 receptor (unknown origin) expressed in human Flp-In-T-REx-293 cells by luciferase based GloSensor cAMP Assay
Assay data:1 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
GTPγS binding test from US Patent US10689327: "Prodrug amino acid derivative"
Assay data:15 Active, 15 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Binding affinity to mGlu3 (unknown origin)
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Selectivity ratio of EC50 for antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 to Ki for displacement of [3H]-LY459477 from human recombinant mGlu3 stably expressed in golden hamster AV12 cells co-expressing rat EAAT1
Assay data:4 Tested
Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method
Assay data:17 Active, 17 Activity ≤ 1 µM, 17 Tested
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay relative to glutamate
Assay data:16 Tested
Agonist activity at mGlu3 (unknown origin)
Assay data:3 Active, 3 Activity ≤ 1 µM, 3 Tested
Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay
Assay data:18 Active, 15 Activity ≤ 1 µM, 18 Tested
Antagonist activity at human mGlu3 receptor expressed in CHO cell membranes in presence of glutamate by GTPgammaS binding assay
Assay data:2 Tested
Agonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay relative to control
Agonist activity at human mGlu3 receptor expressed in CHO cell membranes by GTPgammaS binding assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 2 Tested
Positive allosteric modulation of mGluR3 (unknown origin) at 10 uM in presence of glutamate by calcium mobilization assay
Positive allosteric modulation of mGluR3 (unknown origin) by calcium mobilization assay
Negative allosteric modulation of mGlu3 receptor (unknown origin)
Positive allosteric modulation of mGlu3 receptor (unknown origin)
Antagonist activity at mGluR3 (unknown origin) by FLIPR assay
Inhibition of human mGluR3 by FLIPR assay
Assay data:1 Active, 12 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of mGluR3 (unknown origin)
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