Page last updated: 2024-11-13

vu0422288

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Description

VU0422288: a positive allosteric modulator of metabotropic glutamate receptor 7; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID73058507
CHEMBL ID4162576
SCHEMBL ID20166019
MeSH IDM000609042

Synonyms (21)

Synonym
bdbm50283487
chembl4162576 ,
VU0422288-4
ml 396
1630936-95-6
vu 0422288
n-[3-chloro-4-[(5-chloro-2-pyridinyl)oxy]phenyl]-2-pyridinecarboxamide
AKOS025293496
n-(3-chloro-4-((5-chloropyridin-2-yl)oxy)phenyl)picolinamide
ml396, >=98% (hplc)
n-[3-chloro-4-(5-chloropyridin-2-yl)oxyphenyl]pyridine-2-carboxamide
SCHEMBL20166019
ml-396
gtpl10239
vu0422288
n-{3-chloro-4-[(5-chloropyridin-2-yl)oxy]phenyl}pyridine-2-carboxamide
vu-0422288
NCGC00476190-02
MS-25683
HY-110190
CS-0033054
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)EC50 (µMol)0.10800.00010.23283.2000AID1492909
Metabotropic glutamate receptor 7Rattus norvegicus (Norway rat)EC50 (µMol)0.14600.14600.82301.5000AID1492913; AID1571664
Metabotropic glutamate receptor 8Rattus norvegicus (Norway rat)EC50 (µMol)0.12500.03101.18138.0000AID1492915; AID1571665
Metabotropic glutamate receptor 4Homo sapiens (human)EC50 (µMol)0.10800.00401.71939.8000AID1492909; AID1571663
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (26)

Processvia Protein(s)Taxonomy
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 4Homo sapiens (human)
neurotransmitter secretionMetabotropic glutamate receptor 4Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of neuron apoptotic processMetabotropic glutamate receptor 4Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 4Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (26)

Processvia Protein(s)Taxonomy
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
cytoplasmic vesicleMetabotropic glutamate receptor 4Homo sapiens (human)
presynapseMetabotropic glutamate receptor 4Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID1571664Agonist activity at rat mGlu7 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay2019MedChemComm, Feb-01, Volume: 10, Issue:2
Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present.
AID1571663Agonist activity at human mGlu4 expressed in CHO cells co-expressing Gqi5 (unknown origin) assessed as reduction in intracellular Ca2+ levels by Fluo-4-AM dye based fluorescence assay2019MedChemComm, Feb-01, Volume: 10, Issue:2
Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present.
AID1571665Agonist activity at rat mGlu8 receptor expressed in HEK cell co-expressing Galpha15 (unknown origin) assessed as reduction in intracellular Ca2+ mobilization by Fluo-4-AM dye based fluorescence assay2019MedChemComm, Feb-01, Volume: 10, Issue:2
Progress toward allosteric ligands of metabotropic glutamate 7 (mGlu7) receptor: 2008-present.
AID1492913Positive allosteric modulation of rat mGlu7 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Discovery of VU6005649, a CNS Penetrant mGlu
AID1492915Positive allosteric modulation of rat mGlu8 receptor expressed in HEK cells co-expressing Galphai5 assessed as increase in glutamate-induced calcium flux incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye based f2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Discovery of VU6005649, a CNS Penetrant mGlu
AID1492909Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium mobilization incubated for 142 secs followed by glutamate addition measured after 120 secs by Fluo4-AM dye b2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Discovery of VU6005649, a CNS Penetrant mGlu
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[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]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)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]