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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 mGluR5 receptor (unknown origin) assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
SummaryPubMed CitationRelated 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
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Negative allosteric modulation at mGluR1 receptor (unknown origin) assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to mGluR5 (unknown origin) by FLIPR assay
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 mGluR1 (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
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
Positive allosteric modulator activity at rat mGlu5 in human HEK cells assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition by Fluo-4 AM dye based calcium mobilization assay
Agonist activity at mGluR5 (unknown origin) at 1 to 10 uM by Galphaqi5 calcium flux assay
Agonist activity at mGluR3 (unknown origin) at 1 to 10 uM by Galphaqi5 calcium flux assay
Agonist activity at mGluR1 (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
Antagonist activity at mGluR1alpha (unknown origin)
Assay data:3 Tested
Positive allosteric modulation of mGluR5 (unknown origin)
Positive allosteric modulation of mGluR3 (unknown origin)
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