Warning: The NCBI web site requires JavaScript to function. more...
An official website of the United States government
The .gov means it's official. Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you're on a federal government site.
The site is secure. The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.
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
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at mGluR5 (unknown origin) at 1 to 10 uM by Galphaqi5 calcium flux assay
Positive allosteric modulation of mGluR5 (unknown origin)
Positive allosteric modulation of human mGluR5
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
Displacement of [3H]quisqualate from mGluR5 (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"
Calcium Influx Assay Based on Fluorescence from US Patent US11046702: "Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same"
Assay data:198 Active, 198 Activity ≤ 1 µM, 198 Tested
In Vitro Activity Test for mGluR5 from US Patent US10618900: "5-aromatic alkynyl substituted benzamide compound and preparation method, pharmaceutical composition, and use thereof"
Assay data:4 Active, 27 Tested
SummaryCompounds, ActiveRelated BioAssays by Target
In Vitro GIRK Thallium Flux (60 minute) Assay from US Patent US10597367: "Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof"
Assay data:132 Active, 79 Activity ≤ 1 µM, 182 Tested
In Vitro GIRK Thallium Flux (2.5 minute) Assay from US Patent US10597367: "Metabotropic glutamate receptor negative allosteric modulators (NAMs) and uses thereof"
Assay data:115 Active, 43 Activity ≤ 1 µM, 171 Tested
[3H]-M-MPEP Radioligand Binding Assay from US Patent US10584111: "4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators"
mGlu5 Ca2+ Flux Assay from US Patent US10399948: "Negative allosteric modulators of metabotropic glutamate receptor 3"
Assay data:16 Active, 4 Activity ≤ 1 µM, 23 Tested
Binding Assay from US Patent US9359301: "Ethynyl derivatives"
Filters: Manage Filters
Your browsing activity is empty.
Activity recording is turned off.
Turn recording back on