Page last updated: 2024-12-11

azd9272

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Description

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

Cross-References

ID Source	ID
PubMed CID	9838729
CHEMBL ID	2164550
CHEMBL ID	2164551
SCHEMBL ID	2027395
MeSH ID	M0578549

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)

Excerpt	Reference	Relevance
"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

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Metabotropic glutamate receptor 5	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0026	0.0000	0.5262	7.9700	AID697344
Metabotropic glutamate receptor 5	Homo sapiens (human)	IC50 (µMol)	0.0168	0.0005	0.4394	10.0000	AID697343; AID697601
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	33.0000	0.0009	1.9014	10.0000	AID697602
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (42)

Process	via Protein(s)	Taxonomy
desensitization of G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of DNA-templated transcription	Metabotropic glutamate receptor 5	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathway	Metabotropic glutamate receptor 5	Homo sapiens (human)
chemical synaptic transmission	Metabotropic glutamate receptor 5	Homo sapiens (human)
learning or memory	Metabotropic glutamate receptor 5	Homo sapiens (human)
learning	Metabotropic glutamate receptor 5	Homo sapiens (human)
locomotory behavior	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of MAPK cascade	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticity	Metabotropic glutamate receptor 5	Homo sapiens (human)
synapse organization	Metabotropic glutamate receptor 5	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Metabotropic glutamate receptor 5	Homo sapiens (human)
cognition	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of postsynaptic membrane potential	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentration	Metabotropic glutamate receptor 5	Homo sapiens (human)
cellular response to amyloid-beta	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of synaptic transmission, glutamatergic	Metabotropic glutamate receptor 5	Homo sapiens (human)
trans-synaptic signaling by endocannabinoid, modulating synaptic transmission	Metabotropic glutamate receptor 5	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

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

Ceullar Components (13)

Process	via Protein(s)	Taxonomy
dendrite	Metabotropic glutamate receptor 5	Homo sapiens (human)
cytoplasm	Metabotropic glutamate receptor 5	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
dendritic spine	Metabotropic glutamate receptor 5	Homo sapiens (human)
dendritic shaft	Metabotropic glutamate receptor 5	Homo sapiens (human)
astrocyte projection	Metabotropic glutamate receptor 5	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Metabotropic glutamate receptor 5	Homo sapiens (human)
glutamatergic synapse	Metabotropic glutamate receptor 5	Homo sapiens (human)
postsynaptic density membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
plasma membrane	Metabotropic glutamate receptor 5	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (43)

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]

Research

Studies (6)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	5 (83.33)	24.3611
2020's	1 (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.

Metric	This Compound (vs All)
Research Demand Index	12.43 (24.57)
Research Supply Index	2.08 (2.92)
Research Growth Index	4.51 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.43)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (16.67%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	2.1	1	0	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
thiazoles [no description available]	2.1	1	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
dronabinol Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.. Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy.	2.1	1	0	benzochromene; diterpenoid; phytocannabinoid; polyketide	cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic
palladium Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.	7.08	1	0	metal allergen; nickel group element atom; platinum group metal atom
selegiline Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.	2.25	1	0	selegiline; terminal acetylenic compound	geroprotector
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.1	1	0	1,2,3-triazole
6-methyl-2-(phenylethynyl)pyridine 6-methyl-2-(phenylethynyl)pyridine: an mGlu5 antagonist. 2-methyl-6-(phenylethynyl)pyridine : A methylpyridine that coinsists of 2-methylp[yridine bearing an additional phenylethynyl group at position 6. Potent and highly selective non-competitive antagonist at the mGlu5 receptor subtype (IC50 = 36 nM) and a positive allosteric modulator at mGlu4 receptors. Centrally active following systemic administration in vivo. Reverses mechanical hyperalgesia in the inflamed rat hind paw.	2.07	1	0	acetylenic compound; methylpyridines	anxiolytic drug; metabotropic glutamate receptor antagonist
oxadiazoles Oxadiazoles: Compounds containing five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom which exist in various regioisomeric forms.	4.73	6	1
azd2066 [no description available]	7.1	1	0
fenobam fenobam: in USAN fenobam refers to monohydrate	7.25	1	0	ureas

Condition	Relationship Strength	Studies	Trials
Psychoses, Drug [description not available]	2.25	1	0
Allodynia [description not available]	3.47	1	1
Ache [description not available]	3.47	1	1
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	3.47	1	1

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