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Positive allosteric modulator activity at rat mGlu1 in human HEK cells assessed assessed as increase in calcium flux preincubated for 2.5 mins followed by gluatamate addition by Fluo-4 AM dye based calcium mobilization assay
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
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
Radioligand Binding Assay at Cloned Human mGluR5 Receptor Subtype from US Patent US11440922: "Heterocyclylmethylidene derivatives and their use as modulators of mGluR5 receptors"
Assay data:29 Active, 3 Activity ≤ 1 nM, 29 Activity ≤ 1 µM, 29 Tested
New CNS Specificity Data for AK3-238 (FA44) and AK3-99B (FA26) from US Patent US11173137: "Compositions and methods to modulate chloride ion channel activity"
Assay data:2 Active, 2 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
MPEP Binding Assay from US Patent US11059766: "Ethynyl derivatives"
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Intracellular Ca2+ Mobilization Assay from US Patent US11059766: "Ethynyl derivatives"
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