| Assay ID | Title | Year | Journal | Article |
|---|
| AID239658 | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID236526 | Plasma clearance in rat | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID236197 | Plasma clearance after dosing 2 mg/kg iv and 10 mg/kg po | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID256216 | Effective dose for maximum occupancy in rat upon oral administration measured 1 hr post administration; n = 6 - 7 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID235968 | Bioavailability in rat | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID243449 | Percent occupancy of the Metabotropic glutamate receptor 5 by the [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine ligand 1 hr post-administration of 10 mg/kg compound ip | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID253565 | Oral bioavailability in rat (dose 10 mg/kg p.o.) | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID253613 | Volume of distribution in rat upon intravenous administration at a dose of 2 mg/kg; n = 2 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID253722 | Maximum concentration in rat upon oral administration at a dose of 10 mg/kg; n = 3 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID253680 | Clearance in rat upon intravenous administration at a dose of 2 mg/kg; n = 2 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID243310 | Antagonistic activity against recombinant cytochrome P450 2C9 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID236305 | Volume of distribution after dosing 2 mg/kg iv and 10 mg/kg po | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID237282 | Half life i.v. dosing at 2 mg/kg of 50% PEG400/H 20, po dosing at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID248415 | Inhibitory concentration towards human glutamate receptor 5 in calcium flux assay | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID239660 | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID236283 | Volume of distribution in rat | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID237190 | Half life after dosing 2 mg/kg iv and 10 mg/kg po | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID256423 | Brain penetration measured by compound levels in brain at a dose of 3 mg/kg upon intraperitoneal after 1 hr | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID236690 | Maximum concentration in rat when administered at 10 mg/kg perorally | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID237068 | Half life in rat | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID248796 | Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID246855 | In vivo receptor occupancy was determined in rats administered perorally after 2 hr | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID252366 | Concentration in rat brain measured at 1 hr post-administration of 10 mg/kg ip | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID248795 | Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID239659 | Binding affinity towards Metabotropic glutamate receptor was determined by displacing [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID256425 | Ratio of compound levels in brain to that of plasma level was determined | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID237385 | Plasma level after 1 hr following 10 mg/kg dose ip | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID243313 | Antagonistic activity against recombinant cytochrome P450 2C19 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID256217 | Effective dose for maximum occupancy in rat upon intraperitoneal administration measured 1 hr post administration; n = 5 - 6 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID243309 | Antagonistic activity against recombinant cytochrome P450 1A2 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID255954 | In vitro functional activity measured by changes in cytosolic [Ca2+] concentrations against rat metabotropic glutamate receptor 5 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID236391 | Area under the curve after dosing 2 mg/kg iv and 10 mg/kg po | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID239476 | Displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from glutamate 5 receptor of rat cortical membranes | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID250847 | Antagonistic activity against Metabotropic glutamate receptor 5 in [Ca2+] flux assay using glutamate (10 uM) as agonist | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID253817 | Half life in rat upon intravenous administration at a dose of 2 mg/kg; n = 2 | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID254468 | Ability to displace [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from binding to metabotropic glutamate receptor 5 in rat cortical membranes | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID243312 | Antagonistic activity against recombinant cytochrome P450 3A4 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID256440 | Brain penetration measured by compound levels in plasma at a dose of 3 mg/kg upon intraperitoneal after 1 hr | 2005 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 15, Issue:22
| 3-[Substituted]-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitriles: identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists. |
| AID246878 | In vivo receptor occupancy was determined in rats administered intraperitoneally after 1 hr | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID237973 | Brain level after 1 hr following 3 mg/kg dose administered intraperitoneally | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID243450 | Percent occupancy of the Metabotropic glutamate receptor 5 by the [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine ligand 1 hr post-administration of 10 mg/kg compound ip | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID237365 | Level in rat brain after 1 hr following 10 mg/kg dose ip | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID236512 | Plasma clearance i.v. dosing at 2 mg/kg of 50% PEG400/H 20, po dosing at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID247057 | Blockage of fear-conditioning in rats determined in the fear-potentiated startle (FPS) model of anxiety administered perorally after 1 hr; NT= Not tested | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID243311 | Antagonistic activity against recombinant cytochrome P450 2D6 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID236130 | Oral bioavailability after i.v. dosing at 2 mg/kg of 50% PEG400/H 20, po dosing at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID247024 | Effective dose against rat Metabotropic glutamate receptor 5 occupancy after ip dosing of 10 mg/kg of 50% PEG400/H 20 | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID236074 | Oral bioavailability after dosing 2 mg/kg iv and 10 mg/kg po | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID237801 | Plasma level after 1 hr following 3 mg/kg dose administered intraperitoneally | 2004 | Journal of medicinal chemistry, Sep-09, Volume: 47, Issue:19
| Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity. |
| AID236726 | Maximum concentration i.v. dosing at 2 mg/kg of 50% PEG400/H 20, po dosing at 10 mg/kg | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| 3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: a highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist. |
| AID1346254 | Rat mGlu5 receptor (Metabotropic glutamate receptors) | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2004 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22
| Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |