Assay ID | Title | Year | Journal | Article |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID237802 | Plasma level after 1 hr following 10 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. |
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. |
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. |
AID256424 | Brain penetration measured by compound levels in brain at a dose of 10 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. |
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. |
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. |
AID237974 | Brain level after 1 hr following 10 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. |
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. |
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. |
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. |
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. |
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. |
AID1063759 | Agonist activity at human alpha4beta2alpha5 nACHR expressed in HEK-tsA201 cells by fluorometric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
| Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors. |
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. |
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. |
AID247031 | Blockage of fear-conditioning in rats determined in the fear-potentiated startle (FPS) model of anxiety administered perorally 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. |
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. |
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. |
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. |
AID256441 | Brain penetration measured by compound levels in plasma at a dose of 10 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. |
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. |
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. |
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. |
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. |
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. |
AID246866 | In vivo receptor occupancy was determined in rats administered perorally after 30 min | 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. |
AID1063766 | Positive allosteric modulation of human alpha4beta2alpha5 nACHR expressed in HEK-tsA201 cells assessed as potentiation of nicotine-induced current at 1 uM preincubated for 15 mins followed by nicotine-treatment by fluorometric analysis | 2014 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2
| Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors. |
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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |