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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 mGluR8 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 mGluR6 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 mGluR4 receptor (unknown origin) assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
Binding affinity to mGluR8 (unknown origin) by FLIPR assay
Binding affinity to mGluR6 (unknown origin) by FLIPR assay
Assay data:1 Active, 1 Tested
Binding affinity to mGluR4 (unknown origin) by FLIPR assay
Intracellular Ca2+ Mobilization Assay (FLIPR) from US Patent US12065399: "Arylsulfonamide derivatives"
Assay data:52 Active, 12 Activity ≤ 1 µM, 59 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
In Vitro Testing of mGluR4 Potency from US Patent US20240182453: "NOVEL SUBSTITUTED PYRAZINE-CARBOXAMIDE DERIVATIVES"
Assay data:175 Active, 5 Activity ≤ 1 nM, 171 Activity ≤ 1 µM, 176 Tested
In Vitro Activity Assay from US Patent US20240174652: "NOVEL DIOXANE DERIVATIVES"
Assay data:14 Active, 10 Activity ≤ 1 µM, 15 Tested
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Positive allosteric modulator activity at human mGlu4 in Chinese hamster CHO cells co-expressing Gqi5 assessed as maximum increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by Fluo-4 AM dye based calcium mobilization assay
SummaryPubMed CitationRelated BioAssays by Target
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
Positive allosteric modulator activity at rat mGlu4 in human HEK cells co-expressing GRIK assessed as maximum increase in by thallium flux preincubated for 2.5 mins followed by gluatamate addition and measured for 2 mins by thallium flux assay
Positive allosteric modulator activity at human mGlu6 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 mGlu7 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 mGlu8 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 modulation of mGluR7 (unknown origin) assessed as change in forskolin-induced cAMP production by measuring fold change in EC50 shift preincubated with compound for 15 mins in the presence of LY341495 followed by forskolin stimulation and measured after 5 hrs by luminescence based steady glo assay
Positive allosteric modulation of mGluR7 (unknown origin) assessed as change in forskolin-induced cAMP production by measuring reduction in maximum response preincubated with compound for 15 mins in the presence of LY341495 followed by forskolin stimulation and measured after 5 hrs by luminescence based steady glo assay
Allosteric agonist activity at mGluR7 (unknown origin) assessed as reduction in forskolin-induced cAMP production by measuring fold change in EC50 preincubated for 15 mins in the presence of LY341495 followed by forskolin stimulation and measured after 5 hrs by luminescence based steady glo assay
Assay data:2 Tested
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