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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
Assay data:1 Tested
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
Competitive binding affinity to mGluR7 (unknown origin) assessed as rightward shift in forskolin-induced cAMP production level by measuring fold change preincubated for 15 mins in the presence of LY341495 followed by forskolin stimulation and measured after 5 hrs by luminescence based steady glo assay
Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Agonist activity at human mGluR7b expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Desensitization at human mGluR7 expressed in CHO cells assessed as reduction in tool agonist response at EC80 concentration preincubated for 1 hrs followed by compound replacement with assay buffer and measured 1 hrs after tool agonist addition by CellKey impedance assay relative to control
Desensitization at human mGluR7 expressed in CHO cells assessed as reduction in tool agonist response at 10 uM preincubated for 1 hrs followed by compound replacement with assay buffer and measured 1 hrs after tool agonist addition by CellKey impedance assay relative to control
Agonist activity at human mGluR7 expressed in CHO cells assessed as change in extracellular impedance incubated for 40 mins by CellKey impedance assay
Assay data:3 Active, 3 Tested
Agonist activity at mouse mGluR7 expressed in CHO cells expressing CRE-Luc reporter gene assessed as reduction in forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin stimulation and measured after 5 hrs by luminescence based Steady glo assay
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