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Activity against GLUTAMAT/R in the Eurofins Panlabs screen (BI) by Radioactive Assay
Assay data:1 Tested
SummaryRelated BioAssays by Target
Negative allosteric modulation at mGluR3 receptor (unknown origin) assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
Assay data:1 Active, 3 Tested
Negative allosteric modulation at human mGluR2 receptor stably expressed in DHFR null CHO cells co-expressing Galpha16 assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
Assay data:35 Active, 33 Activity ≤ 1 µM, 36 Tested
Binding affinity to mGluR2 (unknown origin) FLIPR assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Binding affinity to mGluR3 (unknown origin) by FLIPR assay
Binding affinity to human mGluR2 expressed in cell membrane incubated for 1 hr in presence of tritium labeled [3H]-7-((2,5-dioxopyrrolidin-1-yl)methyl)-4-(4-fluorophenyl)quinoline-2-carboxamide by competitive radioligand binding assay
Assay data:23 Active, 9 Activity ≤ 1 nM, 23 Activity ≤ 1 µM, 23 Tested
Positive allosteric modulator activity at rat mGlu2 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition by thallium flux assay
SummaryPubMed CitationRelated BioAssays by Target
Positive allosteric modulator activity at rat mGlu3 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition by thallium flux assay
Agonist activity at mGluR3 (unknown origin) at 1 to 10 uM by Galphaqi5 calcium flux assay
Agonist activity at mGluR2 (unknown origin) at 1 to 10 uM by cAMP assay
Positive allosteric modulation of mGluR3 (unknown origin)
Positive allosteric modulation of mGluR2 (unknown origin)
Positive allosteric modulation of human mGluR3
Positive allosteric modulation of human mGluR2
Antagonist activity at human mGlur2
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Assessment of mGlu2 Receptor Negative Allosteric Modulator Activity from US Patent US11633395: "Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor"
Assay data:19 Active, 19 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Positive allosteric modulator activity at mGluR2 receptor (unknown origin) assessed as glutamate-induced [35S]GTPgammaS binding
Assay data:10 Active, 10 Activity ≤ 1 µM, 10 Tested
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
Agonist activity at mGlu2 receptor (unknown origin) expressed in human Flp-In-T-REx-293 cells by luciferase based GloSensor cAMP Assay
Assay data:7 Active, 4 Activity ≤ 1 µM, 7 Tested
Positive allosteric modulation of mGlu2 receptor (unknown origin) expressed in human Flp-In-T-REx-293 cells in presence of L-glutamate by luciferase based GloSensor cAMP Assay
Assay data:6 Active, 6 Activity ≤ 1 µM, 7 Tested
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