Assay ID | Title | Year | Journal | Article |
AID719494 | Selectivity ratio of EC50 for human mGlu5 receptor expressed in HEK293 cells to EC50 for rat mGlu5 receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
| Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. |
AID1325983 | Selectivity ratio of EC50 for mGlu5 receptor CPPHA allosteric binding site mutant (unknown origin) expressed in HEK cells to EC50 for mGlu5 receptor (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Development of 1 |
AID305982 | Activity at human mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay relative to glutamate | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. |
AID1325979 | Displacement of [3H]-MethoxyPEPy from mGlu5 receptor in primary rat astrocytes after 8 hrs by micro beta scintillation counting analysis | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Development of 1 |
AID420119 | Activity at human mGluR5 transiently transfected in BHK cells assessed as decrease in maximum response of L-glutamate for calcium flux at 1500 nM by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
| Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. |
AID1325977 | Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Development of 1 |
AID420104 | Activity at human mGluR5 transiently transfected in BHK cells assessed as decrease in maximum response of L-glutamate for calcium flux at 15 nM by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
| Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. |
AID240173 | Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. |
AID1325981 | Selectivity ratio of EC50 for mGlu5 receptor MPEP allosteric binding site mutant (unknown origin) expressed in HEK cells to EC50 for mGlu5 receptor (unknown origin) | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Development of 1 |
AID305983 | Activity at rat mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. |
AID773852 | Positive allosteric modulation of human mGluR5 | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide |
AID343891 | Induction of rat mGluR5 activation expressed in HEK293A cells assessed as maximal response in presence of glutamate | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold. |
AID252325 | Fold potentiation in CHO cells overexpressing human metabotropic glutamate receptor 5 | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo. |
AID305981 | Activity at human mGluR5 expressed in CHO cells assessed as potentiation of glutamate response by FLIPR assay | 2007 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 17, Issue:5
| Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA. |
AID420103 | Activity at human mGluR5 transiently transfected in BHK cells assessed as decrease in maximum response of L-glutamate for calcium flux at 150 nM by FLIPR assay | 2009 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12
| Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. |
AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2004 | The Journal of pharmacology and experimental therapeutics, May, Volume: 309, Issue:2
| A novel selective allosteric modulator potentiates the activity of native metabotropic glutamate receptor subtype 5 in rat forebrain. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |