Page last updated: 2024-11-10

vu0155094

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Description

VU0155094: 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 CID4043841
CHEMBL ID1585091
MeSH IDM000609040

Synonyms (26)

Synonym
MLS000418059
smr000264819
VU0155094-5
ml397
methyl 4-[3-[2-(4-acetamidophenyl)sulfanylacetyl]-2,5-dimethylpyrrol-1-yl]benzoate
VU0155094-4
bdbm50283491
chembl1585091 ,
HMS2553G20
AB00550680-02
methyl 4-(3-(2-((4-acetamidophenyl)thio)acetyl)-2,5-dimethyl-1h-pyrrol-1-yl)benzoate
Z25065658
731006-86-3
AKOS033931412
EX-A4984
vu 0155094
ml-397
vu0155094
vu-0155094
ml 397
gtpl10238
methyl 4-(3-(2-((4-acetamidophenyl)thio)acetyl)-2,5-dimethyl-1h-pyrrol-1-yl) benzoate
vu0155094(ml-397)
CS-0083543
HY-121848
methyl 4-(3-{2-[(4-acetamidophenyl)sulfanyl]acetyl}-2,5-dimethyl-1h-pyrrol-1-yl)benzoate
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (30)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency54.45630.044717.8581100.0000AID485294; AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency28.18380.631035.7641100.0000AID504339
Chain A, CruzipainTrypanosoma cruziPotency39.81070.002014.677939.8107AID1476
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
ATAD5 protein, partialHomo sapiens (human)Potency16.36010.004110.890331.5287AID504467
TDP1 proteinHomo sapiens (human)Potency26.10110.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency31.62280.180013.557439.8107AID1460
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency31.62280.707912.194339.8107AID720542
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.11870.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency35.48130.036619.637650.1187AID1466; AID2242
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency25.11893.548119.542744.6684AID743266
mitogen-activated protein kinase 1Homo sapiens (human)Potency28.18380.039816.784239.8107AID1454
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency13.37140.168316.404067.0158AID720504
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency22.38720.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency29.09290.004611.374133.4983AID624296
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency35.48133.548118.039535.4813AID1466
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Potency35.48133.548118.039535.4813AID1466
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
metabotropic glutamate receptor 7 [Homo sapiens]Homo sapiens (human)EC50 (µMol)15.36671.500015.366728.4000AID743384; AID743385; AID743386
Glutamate receptor, metabotropic 4Homo sapiens (human)EC50 (µMol)3.10330.23901.63483.4300AID743393; AID743423; AID743466
glutamate receptor, metabotropic 6Homo sapiens (human)EC50 (µMol)0.39000.39000.39000.3900AID743421
Cytochrome P450 3A4Homo sapiens (human)EC50 (µMol)3.20000.00010.23283.2000AID1492909
Metabotropic glutamate receptor 7Rattus norvegicus (Norway rat)EC50 (µMol)1.50000.14600.82301.5000AID1492913; AID1571664
Metabotropic glutamate receptor 8Rattus norvegicus (Norway rat)EC50 (µMol)0.91500.03101.18138.0000AID1492915; AID1571665
Metabotropic glutamate receptor 4Homo sapiens (human)EC50 (µMol)3.31500.00401.71939.8000AID1492909; 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 (19)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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
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.
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
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (12.50)29.6817
2010's6 (75.00)24.3611
2020's1 (12.50)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 (12.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]