Page last updated: 2024-12-11

azd9272

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

AZD9272: an mGluR5 antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9838729
CHEMBL ID2164550
CHEMBL ID2164551
SCHEMBL ID2027395
MeSH IDM0578549

Synonyms (26)

Synonym
3-fluoro-5-[3-(5-fluoropyridin-2-yl)-1,2,4-oxadiazol-5-yl]benzonitrile
CHEMBL2164550 ,
bdbm50395923
azd-9272
CHEMBL2164551
azd9272
gtpl6439
azd 9272
RBSPCALDSNXWEP-UHFFFAOYSA-N ,
5-(3-cyano-5-fluorophenyl)-3-(5-fluoro-pyrid-2-yl)-1,2,4-oxadiazole
SCHEMBL2027395
unii-54sq9b412i
azd 9272 [who-dd]
54SQ9B412I ,
3-fluoro-5-(3-(5-fluoropyridin-2-yl)-1,2,4-oxadiazol-5-yl)benzonitrile
3-(5-fluoropyridyl-2-yl)-5-(3-cyano-5-fluorophenyl)-1,2,4-oxadiazole
benzonitrile, 3-fluoro-5-(3-(5-fluoro-2-pyridinyl)-1,2,4-oxadiazol-5-yl)-
327056-26-8
3-fluoro-5-[3-(5-fluoro-2-pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile
azd9272, >=98% (hplc)
AKOS027470228
Q27074816
CS-0033119
HY-110254
CNA05626
EX-A7965

Research Excerpts

Overview

AZD9272 is a new chemical entity pharmacologically characterised as a noncompetitive antagonist at the metabotropic glutamate receptor subtype 5 (mGluR5)

ExcerptReferenceRelevance
"AZD9272 is a new chemical entity pharmacologically characterised as a noncompetitive antagonist at the metabotropic glutamate receptor subtype 5 (mGluR5)."( Non-linear mixed effects modelling of positron emission tomography data for simultaneous estimation of radioligand kinetics and occupancy in healthy volunteers.
Cselényi, Z; Hooker, AC; Jönsson, S; Kågedal, M; Karlsson, MO; Nyberg, S; Raboisson, P; Stenkrona, P, 2012
)
1.1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)IC50 (µMol)0.00260.00000.52627.9700AID697344
Metabotropic glutamate receptor 5Homo sapiens (human)IC50 (µMol)0.01680.00050.439410.0000AID697343; AID697601
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)33.00000.00091.901410.0000AID697602
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Processvia Protein(s)Taxonomy
desensitization of G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of DNA-templated transcriptionMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 5Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
learning or memoryMetabotropic glutamate receptor 5Homo sapiens (human)
learningMetabotropic glutamate receptor 5Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMetabotropic glutamate receptor 5Homo sapiens (human)
synapse organizationMetabotropic glutamate receptor 5Homo sapiens (human)
positive regulation of calcium-mediated signalingMetabotropic glutamate receptor 5Homo sapiens (human)
cognitionMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
cellular response to amyloid-betaMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 5Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmissionMetabotropic glutamate receptor 5Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase activator activityMetabotropic glutamate receptor 5Homo sapiens (human)
A2A adenosine receptor bindingMetabotropic glutamate receptor 5Homo sapiens (human)
identical protein bindingMetabotropic glutamate receptor 5Homo sapiens (human)
protein tyrosine kinase bindingMetabotropic glutamate receptor 5Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 5Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 5Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 5Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
dendriteMetabotropic glutamate receptor 5Homo sapiens (human)
cytoplasmMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 5Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 5Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 5Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 5Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 5Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 5Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

Assay IDTitleYearJournalArticle
AID697581Antagonist activity at mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697604Negative 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 assay2012Bioorganic & 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.
AID697598Equilibrium solubility of the compound in DMSO2012Bioorganic & 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.
AID697343Negative 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 assay2012Bioorganic & 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.
AID697585Antagonist activity at mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697597Cmax in Sprague-Dawley rat at 3 umol/kg, po2012Bioorganic & 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.
AID697577Positive allosteric modulation of mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697573Positive allosteric modulation of mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697563Tmax in Sprague-Dawley rat at 3 umol/kg, po2012Bioorganic & 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.
AID697567Plasma protein binding in Sprague-Dawley rat after 6 hrs by equilibrium dialysis method2012Bioorganic & 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.
AID697602Inhibition of human ERG by IonWorks assay2012Bioorganic & 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.
AID697589Agonist activity at mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697582Antagonist activity at mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697586Antagonist activity at mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697584Antagonist activity at mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697579Positive allosteric modulation of mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697568Ratio of drug level in brain to plasma of Sprague-Dawley rat at 3 umol/kg, po2012Bioorganic & 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.
AID697601Negative 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 challen2012Bioorganic & 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.
AID697600Intrinsic clearance in human liver microsomes2012Bioorganic & 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.
AID697587Agonist activity at mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697590Agonist activity at mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697606Negative 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 assay2012Bioorganic & 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.
AID697588Agonist activity at mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697583Antagonist activity at mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697566Oral bioavailability in Sprague-Dawley rat at 3 umol/kg2012Bioorganic & 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.
AID697562Clearance in Sprague-Dawley rat at 3 umol/kg, iv2012Bioorganic & 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.
AID697599Intrinsic clearance in rat liver microsomes2012Bioorganic & 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.
AID697564AUC in Sprague-Dawley rat at 3 umol/kg, po2012Bioorganic & 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.
AID697575Positive allosteric modulation of mGluR6 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697592Agonist activity at mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697578Positive allosteric modulation of mGluR2 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697344Negative 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 assay2012Bioorganic & 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.
AID697605Negative 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 assay2012Bioorganic & 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.
AID697594Volume of distribution at steady state in Sprague-Dawley rat at 3 umol/kg, iv2012Bioorganic & 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.
AID697593Agonist activity at mGluR1 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697574Positive allosteric modulation of mGluR7 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697560Terminal half life in Sprague-Dawley rat at 3 umol/kg, iv2012Bioorganic & 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.
AID697580Antagonist activity at mGluR8 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697576Positive allosteric modulation of mGluR4 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID697603Negative 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 assay2012Bioorganic & 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.
AID697607Noncompetitive 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 assay2012Bioorganic & 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.
AID697591Agonist activity at mGluR3 assessed as effect on intracellular Ca2+ level up to 30 uM by cell based FLIPR assay2012Bioorganic & 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.
AID1346269Human mGlu5 receptor (Metabotropic glutamate receptors)2012Bioorganic & 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]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (83.33)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.43 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (16.67%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]