| Assay ID | Title | Year | Journal | Article |
|---|
| AID683167 | Anxiolytic activity in ip dosed Swiss Webster mouse assessed as increase in time spent in the centre region administered as single dose 15 mins prior to testing by open-field test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID246967 | Effective dose of compound was tested for mGlu5 receptor antagonistic activity in rat upon oral administration | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID683177 | Anxiolytic activity in Swiss Webster mouse assessed as increase in number of compartment transitions at 10 mg/kg, ip administered as single dose 15 mins prior to testing by light-dark box test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID1275089 | Displacement of [3H]-3-methoxy-5-(pyridin-2-ylethynyl)pyridine from mGlu5R in rat cortical membranes by liquid scintillation spectrometric analysis | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
| 7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5. |
| AID762678 | Antinociceptive activity in Sprague-Dawley rat assessed as reduction in formalin-induced nocifensive behavior at 10 mg/kg, po administered 30 mins prior to formalin-challenge | 2013 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 23, Issue:16
| A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core. |
| AID683175 | Anxiolytic activity in Swiss Webster mouse assessed as increase in time spent in the centre region at 10 mg/kg, ip administered as single dose 15 mins prior to testing by open-field test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID177694 | In vivo intraperitoneal effective dose to block fear conditioning in rats was determined by FPS (fear potentiated startle) model of anxiety | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID236053 | Bioavailability in rat (dose 10 mg/kg p.o.) | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID270777 | Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPR | 2006 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
| A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5). |
| AID738947 | Antidepressant activity in ICR mouse assessed as decrease in immobility time at 10 mg/kg, po administered 1 hr before test measured for 4 mins following training for 2 mins by forced swimming test | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators. |
| AID237073 | Half-life of compound after i.v. administration | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID19407 | Lipophilicity (Log D) was determined | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
| [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. |
| AID479059 | Inhibition of mGluR1 expressed in CHO cells at 10 uM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID259883 | Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. |
| AID107070 | In vivo intraperitoneal effective dose for affinity at the Metabotropic glutamate receptor 5 was determined by occupancy assay | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID236609 | Maximum plasma concentration of compound after p.o. administration | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID375049 | Displacement of [3H]MPEP from cloned mGluR5 expressed in HEK293T cells by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
| AID1456859 | Anxiolytic-like activity in Harlan CD1 mouse marble burying model of anxiety/OCD assessed as suppression of marble burying activity at 15 mg/kg, ip administered 15 mins prior to test measured over 30 mins relative to vehicle-control | | | |
| AID601415 | Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. |
| AID683166 | Anxiolytic activity in ip dosed Swiss Webster mouse assessed as increase in locomotor activity administered as single dose 15 mins prior to testing by open-field test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID1614057 | Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID479056 | Displacement of [3HMPEP from rat cloned mGluR5 expressed in HEK293T cells by by scintillation counting | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID1277353 | Anxiolytic activity in water deprived rat assessed as increase in number of accepted shocks at 10 mg/kg, po after 1 hr by Vogel punished drinking test | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4
| 4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate. |
| AID236049 | Bioavailability in rat (dose 2 mg/kg i.v.) | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID601416 | Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting | 2011 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 21, Issue:11
| Potent mGluR5 antagonists: pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series. |
| AID107078 | Tested for displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl) pyridine from Metabotropic glutamate receptor 5 in rat cortical membrane | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID1614063 | Inhibition of recombinant human CYP3A4 using 7-benzyloxy-trifluoromethylcoumarin as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID683163 | Displacement of [3H]MPEP from mGluR5 in Sprague-Dawley rat brain membrane after 60 mins by liquid scintillation counting | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID738966 | Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay | 2013 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 23, Issue:7
| Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators. |
| AID479063 | Inhibition of mGluR4 expressed in CHO cells at 10 uM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID1614060 | Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobilization incubated for 18 hrs and measured every 1.5 secs intervals for 60 secs by Fluo-4/AM dye-based fluore | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID267553 | Inhibition of [3H]MPEP binding to mGluR5 in rat brain membrane | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. |
| AID1236883 | Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity. |
| AID479061 | Inhibition of mGluR6 expressed in CHO cells at 10 uM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID683165 | Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID27867 | Amount in vivo in rat cerebrospinal fluid (CSF) after intraperitoneal dose of 30 mg/Kg | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID375051 | Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
| AID107056 | Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as antagonist | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID28623 | Amount in vivo in rat plasma after intraperitoneal dose of 3 mg/Kg | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID479060 | Inhibition of mGluR2 expressed in CHO cells at 10 uM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID375052 | Antagonist activity at cloned mGluR5 expressed in CHO cells co-transfected with chimeric G protein Gqi9 assessed as inhibition of glutamate-induced intracellular inositol phosphate accumulation at 10 uM by phosphoinositide hydrolysis assay | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
| AID375054 | Antagonist activity at cloned mGluR6 expressed in CHO cells co-transfected with chimeric G protein Gqi9 assessed as inhibition of glutamate-induced intracellular inositol phosphate accumulation at 10 uM by phosphoinositide hydrolysis assay | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
| AID1614068 | Competitive inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 20 mins by LC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID143914 | Tested for in vitro antagonistic activity against recombinant human N-methyl-D-aspartate glutamate receptor 2B | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID267556 | Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
| Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists. |
| AID683168 | Anxiolytic activity in ip dosed Swiss Webster mouse assessed as increase in time spent in light compartment administered as single dose 15 mins prior to testing by light-dark box test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID239004 | Displacement by compound of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID1236882 | Displacement of [3H]MPEP from mGluR5 receptor in Sprague-Dawley rat forebrain membrane after 60 mins by liquid scintillation spectrometry | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity. |
| AID375053 | Antagonist activity at cloned mGluR1 expressed in CHO cells co-transfected with chimeric G protein Gqi9 assessed as inhibition of glutamate-induced intracellular inositol phosphate accumulation at 10 uM by phosphoinositide hydrolysis assay | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists. |
| AID1614058 | Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID236531 | Plasma clearance of compound upon p.o. administration at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID479055 | Displacement of [3H]MK801 from NMDA receptor in rat brain homogenate at 10 uM by scintillation counting | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID27570 | LogD value was determined | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID683169 | Anxiolytic activity in ip dosed Swiss Webster mouse assessed as increase in number of compartment transitions administered as single dose 15 mins prior to testing by light-dark box test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID259886 | Ability to prevent reinstatement of cocaine-seeking behavior by environmental stimuli associated with cocaine availability in Wistar rat | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
| Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. |
| AID221492 | In vitro functional potency using an automated assay employing LtK-cells stably expressing human recombinant mGlu5 receptor by measuring changes in cytosolic [Ca2+] concentration | 2003 | Bioorganic & medicinal chemistry letters, Feb-10, Volume: 13, Issue:3
| [3H]-methoxymethyl-MTEP and [3H]-methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor. |
| AID126363 | Tested for in vitro antagonistic activity against Monoamine oxidase A | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID479062 | Inhibition of mGluR8 expressed in CHO cells at 10 uM | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
| Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5. |
| AID1236884 | Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity. |
| AID1614062 | Inhibition of recombinant human CYP2D6 using 3-[2-(N,N-diethylamino)ethyl]-7-methoxy-4-methylcoumarin as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5. |
| AID683176 | Anxiolytic activity in Swiss Webster mouse assessed as increase in time spent in light compartment at 10 mg/kg, ip administered as single dose 15 mins prior to testing by light-dark box test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID23661 | Amount in vivo in rat brain after intraperitoneal dose of 3 mg/Kg | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID246966 | Effective dose of compound was tested for mGlu5 receptor antagonistic activity in rat upon i.p. administration | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID1236885 | Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity. |
| AID236902 | logD value was determined | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID242195 | In vitro potency against human recombinant mGlu5 receptor was determined by [Ca2+] flux assay using glutamate as agonist | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID236529 | Plasma clearance of compound upon i.v. administration at 2 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
| 5-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-2,3'-bipyridine: a highly potent, orally active metabotropic glutamate subtype 5 (mGlu5) receptor antagonist with anxiolytic activity. |
| AID108662 | Tested for in vitro antagonistic activity against Metabotropic glutamate receptor 1 | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]-pyridine: a potent and highly selective metabotropic glutamate subtype 5 receptor antagonist with anxiolytic activity. |
| AID242780 | Inhibitory concentration against human recombinant metabotropic glutamate receptor 5 (mGlu5) in Ltk cells determined using fluorescence detection method | 2005 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
| Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists. |
| AID683174 | Anxiolytic activity in Swiss Webster mouse assessed as increase in locomotor activity at 10 mg/kg, ip administered as single dose 15 mins prior to testing by open-field test | 2012 | ACS medicinal chemistry letters, Jul-12, Volume: 3, Issue:7
| Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation. |
| AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2002 | The European journal of neuroscience, Dec, Volume: 16, Issue:11
| Reduced stress-induced hyperthermia in mGluR5 knockout mice. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |