Compounds > vu0409106
Page last updated: 2024-11-13

vu0409106

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Description

VU0409106: a metabotropic glutamate receptor 5 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID50990953
CHEMBL ID2440659
SCHEMBL ID1487938
MeSH IDM0580413

Synonyms (19)

Synonym
3-fluoro-n-(4-methylthiazol-2-yl)-5-(pyrimidin-5-yloxy)benzamide
AXVLPJHYYFHCHK-UHFFFAOYSA-N ,
bdbm50442525
chembl2440659 ,
us8796295, table 2: compound: 1
SCHEMBL1487938
3-fluoro-n-(4-methyl-2-thiazolyl)-5-(5-pyrimidinyloxy)benzamide
vu 0409106
1276617-62-9
HY-110180
AKOS027470171
3-fluoro-n-(4-methyl-thiazol-2-yl)-5-(pyrimidin-5-yloxy)-benzamide
vu0409106
3-fluoro-n-(4-methyl-1,3-thiazol-2-yl)-5-pyrimidin-5-yloxybenzamide
vu-0409106
unii-j65udu5wea
benzamide, 3-fluoro-n-(4-methyl-2-thiazolyl)-5-(5-pyrimidinyloxy)-
j65udu5wea ,
CS-0033044

Research Excerpts

Overview

VU0409106 is a potent and selective negative allosteric modulator of mGlu5. It demonstrates good CNS exposure following intraperitoneal dosing in mice.

ExcerptReferenceRelevance
"VU0409106 is a potent and selective negative allosteric modulator of mGlu5 that binds at the known allosteric binding site and demonstrates good CNS exposure following intraperitoneal dosing in mice."( Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bates, BS; Blobaum, AL; Byers, FW; Conn, PJ; Daniels, JS; Emmitte, KA; Felts, AS; Jones, CK; Lindsley, CW; Manka, JT; Morrison, RD; Niswender, CM; Rodriguez, AL; Venable, DF, 2013)		1.48

Dosage Studied

ExcerptRelevanceReference
" VU0409106 is a potent and selective negative allosteric modulator of mGlu5 that binds at the known allosteric binding site and demonstrates good CNS exposure following intraperitoneal dosing in mice."( Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
Bates, BS; Blobaum, AL; Byers, FW; Conn, PJ; Daniels, JS; Emmitte, KA; Felts, AS; Jones, CK; Lindsley, CW; Manka, JT; Morrison, RD; Niswender, CM; Rodriguez, AL; Venable, DF, 2013)		1.67
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)IC50 (µMol)0.02400.00000.52627.9700AID1456779; AID779916
Metabotropic glutamate receptor 5Homo sapiens (human)IC50 (µMol)0.03750.00050.439410.0000AID1213780; AID779896
Metabotropic glutamate receptor 5Homo sapiens (human)Ki0.00680.00050.54638.2000AID779904
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (20)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (132)

Assay IDTitleYearJournalArticle
AID779904Displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from mGlu5 receptor allosteric binding site (unknown origin)2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779871Displacement of [3H]-Flunitrazepam from central-type GABAA receptor flunitrazepam binding site in cerebellum-less rat brain homogenate at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213783Inhibition of group 3 mGluR (unknown origin)2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779870Displacement of [3H]-Muscimol from central-type GABAA receptor muscimol binding site in cerebellum-less rat brain homogenate at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779894Displacement of [3H]-CGS-21680 from human recombinant adenosine A2A receptor expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779912Fraction unbound in mouse brain homogenates after 1 hr by equilibrium dialysis technique2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213775Drug metabolism in human cryopreserved hepatocytes assessed as 3-fluoro-N-(4-methylthiazol-2-yl)-5-(6-oxo-1,6-dihydropyrimidin-5-yloxy)benzamide at 25 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213757Drug metabolism in human cryopreserved hepatocytes assessed as hydroxylated thiazole metabolite formation at 25 uM by LC-MS/MS analysis in presence of 1-ABT pan-450 inactivator2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213788Effective half life in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779840Displacement of [35S]-ATP-alpha-S from purinergic P2Y receptor in rat brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779866Displacement of [3H]-CGP-39653 from NMDA receptor agonist binding site in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213774Drug metabolism in human hepatic S9 fraction assessed as 3-fluoro-N-(4-methylthiazol-2-yl)-5-(6-oxo-1,6-dihydropyrimidin-5-yloxy)benzamide at 1 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779891Displacement of [3H]-Prazosin from adrenergic alpha1A receptor in rat submaxillary gland at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779826Anxiolytic activity in Harlan CD-1 mouse assessed as inhibition of marble burying behavior at >= 3 mg/kg, ip2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779868Displacement of [3H]-CGP-54626 from human recombinant GABAB1A receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779896Allosteric modulation of human mGlu5 receptor expressed in HEK cells assessed as effect on glutamate-induced calcium mobilization2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779864Displacement of [3H]-MDL 105,519 from NMDA receptor glycine binding site in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779854Displacement of [3H]-N-Methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779888Displacement of [3H]-CGP-12177 from human recombinant adrenergic beta2 receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779852Displacement of [125I]-Peptide YY from neuropeptide Y Y1 receptor in human SK-N-MC cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779873Displacement of [125I]-Endothelin-1 from human recombinant ETB receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213772Drug metabolism in Sprague-Dawley rat hepatic S9 fraction assessed as 3-fluoro-N-(4-methylthiazol-2-yl)-5-(6-oxo-1,6-dihydropyrimidin-5-yloxy)benzamide at 25 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779903Allosteric modulation of rat mGlu1 receptor expressed in HEK293 cells assessed as effect on glutamate-induced calcium mobilization at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779901Allosteric modulation of rat mGlu3 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on glutamate-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779898Allosteric modulation of rat mGlu7 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on L-AP4-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213787Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213780Inhibition of mGluR5 (unknown origin)2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1456878Plasma clearance in cynomolgus monkey at 0.2 mg/kg, iv up to 24 hrs by LC/MS/MS analysis
AID779874Displacement of [125I]-EGF from epidermal growth factor receptor in human A431 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779895Displacement of [125I]-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1456779Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate induced-calcium mobilization preincubated for 2.3 mins followed by glutamate addition measured after 1.9 mins by Fluo-4 AM dye based fluore
AID1213777Drug metabolism in cynomolgus monkey hepatic S9 fraction assessed as 3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yloxy)-5-fluoro-N-(thiazol-2-yl)benzamide at 1 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779865Displacement of [3H]-TCP from NMDA receptor phencyclidine binding site in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213756Drug metabolism in Sprague-Dawley rat cryopreserved hepatocytes assessed as hydroxylated pyrimidine metabolite formation at 25 uM by LC-MS/MS analysis in presence of 1-ABT pan-450 inactivator2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779832Displacement of [125I]-Triiodothyronine from thyroid hormone receptor in rat liver at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779855Displacement of [3H]-N-Methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213763Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779862Displacement of [3H]-N(-)-alpha-Methylhistamine from human recombinant histamine H3 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779860Displacement of [3H]-Idazoxan from central-type imidazoline I2 receptor in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1456802Oral bioavailability in Sprague-Dawley rat at 10 mg/kg, administered via nasogastric gavage up to 24 hrs by LC/MS/MS analysis
AID1213755Drug metabolism in Sprague-Dawley rat cryopreserved hepatocytes assessed as hydroxylated thiazole metabolite formation at 25 uM by LC-MS/MS analysis in presence of 1-ABT pan-450 inactivator2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213734Retention time in Sprague-Dawley rat plasma treated with 56.6 mg/kg, ip VU0409106 single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779914Inhibition of CYP3A4 in human liver microsomes in presence of NADPH2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779889Displacement of [3H]-Prazosin from human recombinant adrenergic alpha1D receptor expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779877Displacement of [3H]-Spiperone from human recombinant dopamine D4.2 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779880Displacement of [3H]-SR141716A from human recombinant CB1 receptor expressed in rat Chem-1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779905Ratio of drug level in brain to plasma in CD-1 mouse at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779837Displacement of [3H]-Lysergic acid diethylamide from human recombinant 5-HT2B receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779900Allosteric modulation of rat mGlu4 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on glutamate-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779892Displacement of [3H]-Rauwolscine from human recombinant adrenergic alpha2A receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779850Displacement of [125I]-alpha-Bungarotoxin from nicotinic acetylcholine alpha1 receptor bungarotoxin binding site in human RD cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779883Displacement of [3H]-Diltiazem from L-Type calcium channel benzothiazepine binding site in rat brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779884Displacement of [3H]-(Des-Arg10)-Kallidin from bradykinin B1 receptor in human IMR90 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213778Drug metabolism in human hepatic S9 fraction assessed as 3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yloxy)-5-fluoro-N-(thiazol-2-yl)benzamide at 1 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213773Drug metabolism in cynomolgus monkey hepatic S9 fraction assessed as 3-fluoro-N-(4-methylthiazol-2-yl)-5-(6-oxo-1,6-dihydropyrimidin-5-yloxy)benzamide at 1 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213776Drug metabolism in Sprague-Dawley rat hepatic S9 fraction assessed as 3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yloxy)-5-fluoro-N-(thiazol-2-yl)benzamide at 25 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779879Displacement of [3H]-Spiperone from human recombinant dopamine D3 receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1456789Plasma clearance in Sprague-Dawley rat at 1 mg/kg, iv up to 24 hrs post dose by LC/MS/MS Analysis
AID779848Displacement of [3H]-Diprenorphine from human recombinant kappa receptor expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779887Displacement of [125I]-Cyanopindolol from human recombinant adrenergic beta1 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779845Displacement of [3H]-PAF from platelet activating factor receptor in human platelets at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779849Displacement of [3H]-Naltrindole from human recombinant delta opioid receptor expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779846Displacement of [3H]-PDBu from phorbol ester receptor in mouse brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213758Drug metabolism in human cryopreserved hepatocytes assessed as hydroxylated pyrimidine metabolite formation at 25 uM by LC-MS/MS analysis in presence of 1-ABT pan-450 inactivator2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779886Displacement of [3H]-Methyltrienolone from androgen receptor in human LNCAP cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779909Tmax in CD-1 mouse brain at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779893Displacement of [3H]-DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779856Displacement of [3H]-N-Methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779915Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization at 30 uM preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds relative to glu2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779899Allosteric modulation of rat mGlu6 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on glutamate-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213760Intrinsic clearance in Sprague-Dawley rat hepatic S9 fraction at 1 uM in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779885Displacement of [3H]-Bradykinin from human recombinant bradykinin B2 receptor expressed in rat Chem-1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779841Displacement of [3H]-alpha,beta-Methylene-ATP from purinergic P2x receptor in rabbit urinary bladder at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1456780Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate induced-calcium mobilization at 30 uM preincubated for 2.3 mins followed by glutamate addition measured after 1.9 mins by Fluo-4 AM dye bas
AID1213770Intrinsic clearance in human hepatic cytosol at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779916Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779844Displacement of [3H]-Glyburide from ATP-sensitive potassium channel in hamster pancreatic HIT-T15 beta cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779839Displacement of [3H]-Rolipram from rolipram binding site in rat brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779917Fraction unbound in mouse brain homogenates by equilibrium dialysis technique2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779908Cmax in CD-1 mouse brain at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1456786Inhibition of CYP1A2 in human liver microsomes using tacrine as substrate preincubated for 5 mins followed by NADPH addition measured after 8 mins by LC/MS/MS analysis
AID779872Displacement of [3H]-Estradiol from human recombinant ERalpha receptor expressed in insect Sf9 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213779Drug metabolism in human cryopreserved hepatocytes assessed as 3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yloxy)-5-fluoro-N-(thiazol-2-yl)benzamide at 25 uM by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779910Cmax in CD-1 mouse plasma at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779830Displacement of [3H]-GABA from GABA transporter in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213761Intrinsic clearance in Sprague-Dawley rat hepatic cytosol at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213759Intrinsic clearance in Sprague-Dawley rat hepatic S9 fraction at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779858Displacement of [3H]-LTD4 from human recombinant leukotriene cysteinyl CysLT1 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779836Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779847Displacement of [3H]-Diprenorphine from human recombinant mu opioid receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779907AUC in CD-1 mouse plasma at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779913Fraction unbound in mouse brain homogenates after 15 mins by equilibrium dialysis technique2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213751Drug metabolism in Sprague-Dawley rat plasma assessed as hydroxylated thiazole metabolite formation at 56.6 mg/kg, ip single dose by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779853Displacement of [125I]-Peptide YY from neuropeptide Y Y2 receptor in human KAN-TS cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779838Displacement of [3H]-GR-65630 from human recombinant 5-HT3 receptor expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779881Displacement of [125I]-Omega-Conotoxin GVIA from from N-type calcium channel in rat frontal brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779834Displacement of [3H]-Batrachotoxin from sodium channel site 2 in rat brain at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779833Displacement of [3H]-Substance P from human recombinant tachykinin NK1 receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213771Intrinsic clearance in human cryopreserved hepatocytes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779861Displacement of [3H]-Pyrilamine from human recombinant histamine H1 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213769Intrinsic clearance in human hepatic S9 fraction at 1 uM in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779843Displacement of [3H]-Astemizole from human recombinant ERG expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213762Intrinsic clearance in Sprague-Dawley rat cryopreserved hepatocytes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213764Intrinsic clearance in cynomolgus monkey hepatic S9 fraction at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779890Displacement of [3H]-Prazosin from adrenergic alpha1B receptor in rat liver at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779911Tmax in CD-1 mouse plasma at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779875Displacement of [125I]-Endothelin-1 from human recombinant ETA receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779827Anxiolytic activity in ip dosed Harlan CD-1 mouse assessed as inhibition of marble burying behavior2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779863Displacement of [125I]-Aminopotentidine from human recombinant histamine H2 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779882Displacement of [3H]-Nitrendipine from from L-type calcium channel dihydropyridine binding site in rat cerebral cortex at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779878Displacement of [3H]-Spiperone from human recombinant dopamine D2S receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213767Plasma clearance in cynomolgus monkey at 1 mg/kg, iv administered as single dose2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779842Displacement of [3H]-PGE2 from human recombinant prostanoid EP4 receptor expressed in rat Chem-1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779906AUC in CD-1 mouse brain at 10 mg/kg, ip by LC-MS/MS analysis2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779869Displacement of [3H]-Dexamethasone from human recombinant glucocorticoid receptor at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213781Inhibition of group 1 mGluR (unknown origin)2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213766Intrinsic clearance in cynomolgus monkey cryopreserved hepatocytes at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779851Displacement of [125I] Epibatidine from nicotinic acetylcholine receptor in human IMR32 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779829Displacement of [125I]-RTI-55 from human recombinant NET expressed in MDCK cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779867Displacement of [3H]-Kainic acid from kainate receptor in cerebellum-less rat brain homogenate at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779835Displacement of [3H]-Haloperidol from sigma1 receptor in human Jurkat cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779859Displacement of [125I]-Interleukin-1beta from IL-1 receptor in mouse 3T3-SWISS cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779902Allosteric modulation of rat mGlu2 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on glutamate-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213782Inhibition of group 2 mGluR (unknown origin)2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID1213752Drug metabolism in Sprague-Dawley rat plasma assessed as hydroxylated pyrimidine metabolite formation at 56.6 mg/kg, ip single dose by LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779876Displacement of [3H]-SCH-23390 from human recombinant dopamine D1 receptor expressed in CHO cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213765Intrinsic clearance in cynomolgus monkey hepatic S9 fraction at 1 uM in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779897Allosteric modulation of rat mGlu8 receptor expressed in HEK293 cells coexpressing G protein-activated inward rectifier potassium channel assessed as effect on glutamate-induced thallium flux at 10 uM2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779828Displacement of [3H]-Paroxetine from human recombinant SERT expressed in HEK293 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID779857Displacement of [125I]-2-Iodomelatonin from human recombinant MT1 receptor expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
AID1213768Intrinsic clearance in human hepatic S9 fraction at 1 uM2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
AID779831Displacement of [125I]-RTI-55 from human recombinant DAT expressed in CHO-K1 cells at 10 uM relative to control2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

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 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
niacinamide
nicotinamide : A pyridinecarboxamide that is pyridine in which the hydrogen at position 3 is replaced by a carboxamide group.		2.1110pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor
1-aminobenzotriazole
[no description available]		2.1310
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		2.1110primary amine
thiazoles
[no description available]		3.01401,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
raloxifene hydrochloride
Raloxifene Hydrochloride: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.. raloxifene hydrochloride : A hydrochloride salt resulting from the reaction of equimolar amounts of raloxifene and hydrogen chloride.		2.0710hydrochloridebone density conservation agent;
estrogen antagonist;
estrogen receptor modulator
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.		2.13101,2,3-triazole
vu0092273
VU0092273: mGlu(5) positive allosteric modulator		2.1110
piperidines
Piperidines: A family of hexahydropyridines.		2.1110
n-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide
N-cyclobutyl-6-((3-fluorophenyl)ethynyl)nicotinamide: an mGlu5 agonist; structure in first source		2.1110
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		2.0710nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
ConditionIndicatedRelationship StrengthStudiesTrials
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		07.0810