Assay ID | Title | Year | Journal | Article |
AID697581 | Antagonist activity at mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697604 | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of ATP-induced intracellular Ca2+ level at 10 uM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697598 | Equilibrium solubility of the compound in DMSO | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697343 | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697585 | Antagonist activity at mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697597 | Cmax in Sprague-Dawley rat at 3 umol/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697577 | Positive allosteric modulation of mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697573 | Positive allosteric modulation of mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697563 | Tmax in Sprague-Dawley rat at 3 umol/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697567 | Plasma protein binding in Sprague-Dawley rat after 6 hrs by equilibrium dialysis method | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697602 | Inhibition of human ERG by IonWorks assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697589 | Agonist activity at mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697582 | Antagonist activity at mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697586 | Antagonist activity at mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697584 | Antagonist activity at mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697579 | Positive allosteric modulation of mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697568 | Ratio of drug level in brain to plasma of Sprague-Dawley rat at 3 umol/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697601 | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challen | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697600 | Intrinsic clearance in human liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697587 | Agonist activity at mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697590 | Agonist activity at mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697606 | Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level at 0.001 to 3 uM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697588 | Agonist activity at mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697583 | Antagonist activity at mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697566 | Oral bioavailability in Sprague-Dawley rat at 3 umol/kg | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697562 | Clearance in Sprague-Dawley rat at 3 umol/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697599 | Intrinsic clearance in rat liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697564 | AUC in Sprague-Dawley rat at 3 umol/kg, po | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697575 | Positive allosteric modulation of mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697592 | Agonist activity at mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697578 | Positive allosteric modulation of mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697344 | Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697605 | Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level at 0.001 to 3 uM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697594 | Volume of distribution at steady state in Sprague-Dawley rat at 3 umol/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697593 | Agonist activity at mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697574 | Positive allosteric modulation of mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697560 | Terminal half life in Sprague-Dawley rat at 3 umol/kg, iv | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697580 | Antagonist activity at mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697576 | Positive allosteric modulation of mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697603 | Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of ATP-induced intracellular Ca2+ level at 10 uM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697607 | Noncompetitive inhibition of human mGluR5 expressed in HEK cells assessed as inhibition of DHPG-induced intracellular Ca2+ level at 10 to 300 nM after 30 mins by FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID697591 | Agonist activity at mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2012 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
| Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |