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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 mGluR1 receptor (unknown origin) assessed as effect on intracellular calcium flux measured after 5 min by Fluo-4AM dye based FLIPR analysis
Binding affinity to mGluR5 (unknown origin) by FLIPR assay
Binding affinity to mGluR1 (unknown origin) by FLIPR 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 mGluR1 (unknown origin) at 1 to 10 uM by Galphaqi5 calcium flux assay
Antagonist activity at mGluR1alpha (unknown origin)
Assay data:3 Tested
Positive allosteric modulation of mGluR5 (unknown origin)
Positive allosteric modulation of mGluR1 (unknown origin)
Positive allosteric modulation of human mGluR5
Positive allosteric modulation of human mGluR1
Radioligand Binding Assay from US Patent US11584732: "Methods of treatment using 4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators"
Assay data:22 Active, 4 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Agonist activity at mGlu5 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 mGlu1 receptor (unknown origin) expressed in human Flp-In-T-REx-293 cells by luciferase based GloSensor cAMP Assay
Displacement of [3H]quisqualate from mGluR5 (unknown origin) at 10 uM relative to control
Displacement of [3H]quisqualate from mGluR1 (unknown origin) at 10 uM relative to control
Fold Shift of Agonist Curve Determination from US Patent US11440922: "Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors"
Assay data:16 Active, 16 Activity ≤ 1 µM, 16 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Calcium Fluorescence Measurements from US Patent US11440922: "Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors"
Assay data:10 Active, 10 Activity ≤ 1 µM, 10 Tested
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