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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 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 mGluR1 (unknown origin) by FLIPR assay
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
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 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 mGluR1 (unknown origin)
Positive allosteric modulation of human mGluR1
Agonist activity at mGlu1 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 mGluR1 (unknown origin) at 10 uM relative to control
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
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
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
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
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
FLIPR Calcium 5 Assay from US Patent US9260448: "Thienopyrimidinone derivatives as mGluR1 antagonists"
Assay data:11 Active, 10 Activity ≤ 1 µM, 11 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Fluorometric Imaging Plate Reader (FLIPR) Assay from US Patent US8853203: "Diazepinone derivatives"
Assay data:181 Active, 3 Activity ≤ 1 nM, 162 Activity ≤ 1 µM, 185 Tested
Metabotropic Glutamate Receptor Activity Assay from US Patent US8796295: "Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same"
Assay data:14 Active, 12 Activity ≤ 1 µM, 15 Tested
Binding Assay from US Patent US8609852: "Thiazolyl mGluR5 antagonists and methods for their use"
Assay data:102 Active, 11 Activity ≤ 1 nM, 102 Activity ≤ 1 µM, 102 Tested
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