Page last updated: 2024-11-10

sib 1893

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Description

SIB 1893: a selective mGluR5 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5311432
CHEMBL ID88612
CHEBI ID93178
MeSH IDM0332161

Synonyms (64)

Synonym
CHEMBL88612 ,
BRD-K67439147-001-01-7
gtpl1432
6266-99-5
nsc36665
nsc-36665
mls002607995 ,
PDSP1_001571
EU-0101171
sib 1893, >99%, solid
LOPAC0_001171 ,
PDSP2_001555
sib1893
NCGC00025046-04
sib 1893
NCGC00025046-03
NCGC00025046-02
sib-1893
(e)-2-methyl-6-(2-phenylethenyl)pyridine
(e)-2-methyl-6-[2-phenylethenyl]pyridine
S 9311
NCGC00025046-05
(e)-2-methyl-6-styrylpyridine
2-methyl-6-styryl-pyridine(sib-1893)
2-methyl-6-((e)-styryl)-pyridine
bdbm50084141
smr000326914
L000561
2-methyl-6-(2-phenylethenyl)pyridine
2-methyl-6-[(e)-2-phenylethenyl]pyridine
NCGC00025046-06
HMS3263L03
AKOS006279967
CCG-205245
bdbm86715
cas_5311432
nsc_5311432
pyridine, 2-methyl-6-[(1e)-2-phenylethenyl]-
[e]-2-methyl-6-[2-phenylethenyl]pyridine
7370-21-0
LP01171
pyridine,2-methyl-6-(2-phenylethenyl)-
tox21_501171
NCGC00261856-01
CHEBI:93178
SR-01000076143-1
sr-01000076143
SR-01000076143-3
(e)-2-methyl-6-(2-phenylethyl)-pyridine
HMS3676O11
unii-4x2f5x24uk
trans-6-styryl-2-picoline
4x2f5x24uk ,
HMS3412O11
Q7390272
DTXSID801017353
SDCCGSBI-0051138.P002
NCGC00025046-09
nsc 36665
pyridine, 2-methyl-6-((1e)-2-phenylethenyl)-
(e/z)-sib-1893
HY-102094
CS-0024628
AKOS040745363

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The effect of these drugs was also examined in mice challenged with toxic doses of acetaminophen."( Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice.
Battaglia, G; Freitas, I; Griffini, P; Ngomba, RT; Nicoletti, F; Richelmi, P; Storto, M; Vairetti, M, 2003
)
0.32
") substantially reduced liver necrosis and the production of ROS, although it did not affect the conversion of acetaminophen into the toxic metabolite, N-acetylbenzoquinoneimine."( Selective blockade of mGlu5 metabotropic glutamate receptors is protective against acetaminophen hepatotoxicity in mice.
Battaglia, G; Freitas, I; Griffini, P; Ngomba, RT; Nicoletti, F; Richelmi, P; Storto, M; Vairetti, M, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (32)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency44.66840.003245.467312,589.2998AID2517
Chain A, Ferritin light chainEquus caballus (horse)Potency25.11895.623417.292931.6228AID485281
dopamine D1 receptorHomo sapiens (human)Potency0.00920.00521.30228.1995AID624455
ATAD5 protein, partialHomo sapiens (human)Potency10.23070.004110.890331.5287AID493106; AID493107
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency12.60820.001530.607315,848.9004AID1224819; AID1224820; AID1224821; AID1224823
luciferasePhoturis pensylvanica (Pennsylania firefly)Potency10.00000.891310.432820.5750AID1379
ParkinHomo sapiens (human)Potency3.66260.819914.830644.6684AID720573
arylsulfatase AHomo sapiens (human)Potency11.99551.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency28.18380.035520.977089.1251AID504332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency12.99530.01262.451825.0177AID485313
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency26.85450.134610.395030.1313AID1347049
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency11.66810.00669.809418.4927AID1347050
ras-related protein Rab-9AHomo sapiens (human)Potency11.22020.00022.621531.4954AID485297
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency16.94410.425612.059128.1838AID504536
survival motor neuron protein isoform dHomo sapiens (human)Potency15.84890.125912.234435.4813AID1458
M-phase phosphoprotein 8Homo sapiens (human)Potency63.09570.177824.735279.4328AID488949
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.00000.015812.3113615.5000AID1461
Ataxin-2Homo sapiens (human)Potency3.54810.011912.222168.7989AID588378
phosphoglycerate kinaseTrypanosoma brucei brucei TREU927Potency30.13130.07578.474229.0628AID504547
2,3-bisphosphoglycerate-independent phosphoglycerate mutaseLeishmania major strain FriedlinPotency23.93417.568615.230621.3313AID504548
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency15.10140.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 8Homo sapiens (human)Ki100.00000.06103.68859.5000AID107274
Metabotropic glutamate receptor 6Homo sapiens (human)Ki100.00000.40002.50005.8000AID107093
Luciferin 4-monooxygenasePhotinus pyralis (common eastern firefly)IC50 (µMol)31.26000.05893.142610.0000AID328181; AID328182; AID328183; AID328185; AID328186
Metabotropic glutamate receptor 5Homo sapiens (human)IC50 (µMol)1.46330.00050.439410.0000AID107057; AID109496; AID109497
Metabotropic glutamate receptor 5Homo sapiens (human)Ki0.29000.00050.54638.2000AID107059
Metabotropic glutamate receptor 1Homo sapiens (human)IC50 (µMol)100.00000.00052.01408.8000AID108651
Metabotropic glutamate receptor 1Homo sapiens (human)Ki100.00000.00033.536310.0000AID108489
Metabotropic glutamate receptor 2Homo sapiens (human)Ki100.00000.00270.71586.4000AID108833
Metabotropic glutamate receptor 7Homo sapiens (human)Ki100.00000.99000.99000.9900AID107261
Metabotropic glutamate receptor 3Homo sapiens (human)Ki100.00000.00130.61549.0000AID109164
Metabotropic glutamate receptor 4Homo sapiens (human)Ki26.00000.16001.15672.4000AID109341
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (57)

Processvia Protein(s)Taxonomy
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
visual perceptionMetabotropic glutamate receptor 8Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 8Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 8Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 6Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 6Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 6Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 6Homo sapiens (human)
detection of visible lightMetabotropic glutamate receptor 6Homo sapiens (human)
detection of light stimulus involved in visual perceptionMetabotropic glutamate receptor 6Homo sapiens (human)
retina development in camera-type eyeMetabotropic glutamate receptor 6Homo sapiens (human)
positive regulation of calcium ion import across plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 6Homo sapiens (human)
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)
G protein-coupled receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 1Homo sapiens (human)
locomotory behaviorMetabotropic glutamate receptor 1Homo sapiens (human)
sensory perception of painMetabotropic glutamate receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of sensory perception of painMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 1Homo sapiens (human)
cellular response to electrical stimulusMetabotropic glutamate receptor 1Homo sapiens (human)
L-glutamate import across plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 1Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 1Homo sapiens (human)
negative regulation of adenylate cyclase activityMetabotropic glutamate receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
gene expressionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of glutamate secretionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of dopamine secretionMetabotropic glutamate receptor 2Homo sapiens (human)
behavioral response to nicotineMetabotropic glutamate receptor 2Homo sapiens (human)
response to cocaineMetabotropic glutamate receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMetabotropic glutamate receptor 2Homo sapiens (human)
long-term synaptic depressionMetabotropic glutamate receptor 2Homo sapiens (human)
intracellular glutamate homeostasisMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of response to drugMetabotropic glutamate receptor 2Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 2Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 2Homo sapiens (human)
behavioral fear responseMetabotropic glutamate receptor 7Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 7Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 7Homo sapiens (human)
sensory perception of soundMetabotropic glutamate receptor 7Homo sapiens (human)
negative regulation of glutamate secretionMetabotropic glutamate receptor 7Homo sapiens (human)
axon developmentMetabotropic glutamate receptor 7Homo sapiens (human)
glycosylationMetabotropic glutamate receptor 7Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 7Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 7Homo sapiens (human)
negative regulation of adenylate cyclase activityMetabotropic glutamate receptor 3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 3Homo sapiens (human)
chemical synaptic transmissionMetabotropic glutamate receptor 3Homo sapiens (human)
gene expressionMetabotropic glutamate receptor 3Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMetabotropic glutamate receptor 3Homo sapiens (human)
regulation of synaptic transmission, glutamatergicMetabotropic glutamate receptor 3Homo sapiens (human)
G protein-coupled glutamate receptor signaling pathwayMetabotropic glutamate receptor 3Homo 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)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
group III metabotropic glutamate receptor activityMetabotropic glutamate receptor 8Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 6Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 6Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 6Homo sapiens (human)
protein homodimerization activityMetabotropic glutamate receptor 6Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 6Homo sapiens (human)
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)
G protein-coupled receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 1Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
adenylate cyclase inhibiting G protein-coupled glutamate receptor activityMetabotropic glutamate receptor 1Homo sapiens (human)
neurotransmitter receptor activity involved in regulation of postsynaptic cytosolic calcium ion concentrationMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor activity involved in regulation of postsynaptic membrane potentialMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
calcium channel regulator activityMetabotropic glutamate receptor 2Homo sapiens (human)
protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
scaffold protein bindingMetabotropic glutamate receptor 2Homo sapiens (human)
group II metabotropic glutamate receptor activityMetabotropic glutamate receptor 2Homo sapiens (human)
group III metabotropic glutamate receptor activityMetabotropic glutamate receptor 7Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 7Homo sapiens (human)
adenylate cyclase inhibitor activityMetabotropic glutamate receptor 7Homo sapiens (human)
protein dimerization activityMetabotropic glutamate receptor 7Homo sapiens (human)
serine bindingMetabotropic glutamate receptor 7Homo sapiens (human)
G protein-coupled receptor activityMetabotropic glutamate receptor 3Homo sapiens (human)
calcium channel regulator activityMetabotropic glutamate receptor 3Homo sapiens (human)
glutamate receptor activityMetabotropic glutamate receptor 3Homo sapiens (human)
scaffold protein bindingMetabotropic glutamate receptor 3Homo sapiens (human)
group II metabotropic glutamate receptor activityMetabotropic glutamate receptor 3Homo 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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (33)

Processvia Protein(s)Taxonomy
plasma membraneMetabotropic glutamate receptor 8Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 8Homo sapiens (human)
Golgi membraneMetabotropic glutamate receptor 6Homo sapiens (human)
endoplasmic reticulum membraneMetabotropic glutamate receptor 6Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
dendriteMetabotropic glutamate receptor 6Homo sapiens (human)
new growing cell tipMetabotropic glutamate receptor 6Homo sapiens (human)
synapseMetabotropic glutamate receptor 6Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 6Homo sapiens (human)
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)
nucleusMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
dendriteMetabotropic glutamate receptor 1Homo sapiens (human)
Schaffer collateral - CA1 synapseMetabotropic glutamate receptor 1Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor dimeric complexMetabotropic glutamate receptor 1Homo sapiens (human)
G protein-coupled receptor homodimeric complexMetabotropic glutamate receptor 1Homo sapiens (human)
postsynaptic density membraneMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 1Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 2Homo sapiens (human)
axonMetabotropic glutamate receptor 2Homo sapiens (human)
dendriteMetabotropic glutamate receptor 2Homo sapiens (human)
presynaptic membraneMetabotropic glutamate receptor 2Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 2Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 2Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 2Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 7Homo sapiens (human)
cell cortexMetabotropic glutamate receptor 7Homo sapiens (human)
membraneMetabotropic glutamate receptor 7Homo sapiens (human)
axonMetabotropic glutamate receptor 7Homo sapiens (human)
dendriteMetabotropic glutamate receptor 7Homo sapiens (human)
asymmetric synapseMetabotropic glutamate receptor 7Homo sapiens (human)
dendritic shaftMetabotropic glutamate receptor 7Homo sapiens (human)
postsynaptic membraneMetabotropic glutamate receptor 7Homo sapiens (human)
presynaptic active zoneMetabotropic glutamate receptor 7Homo sapiens (human)
receptor complexMetabotropic glutamate receptor 7Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 7Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 3Homo sapiens (human)
postsynaptic densityMetabotropic glutamate receptor 3Homo sapiens (human)
axonMetabotropic glutamate receptor 3Homo sapiens (human)
presynaptic membraneMetabotropic glutamate receptor 3Homo sapiens (human)
dendritic spineMetabotropic glutamate receptor 3Homo sapiens (human)
postsynaptic membraneMetabotropic glutamate receptor 3Homo sapiens (human)
astrocyte projectionMetabotropic glutamate receptor 3Homo sapiens (human)
glutamatergic synapseMetabotropic glutamate receptor 3Homo sapiens (human)
plasma membraneMetabotropic glutamate receptor 3Homo 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)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID109341Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4)2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID328182Inhibition of Photinus pyralis luciferase2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID328183Inhibition of Photinus pyralis luciferase by Easy lite assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID328181Inhibition of Photinus pyralis luciferase by PK-Light assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID267553Inhibition of [3H]MPEP binding to mGluR5 in rat brain membrane2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
AID107059Agonist potency against cloned metabotropic glutamate receptor 52000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID108833Antagonist potency against cloned Metabotropic glutamate receptor 22000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID107057Tested in vitro binding affinity for displacement of [3H]M-MPEP from membrane of L(-tk) cells expressing the Metabotropic glutamate receptor 5, activity expressed as IC502002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
AID108651Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor.1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.
AID107093Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID109497In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated phosphoinositide (PI) hydrolysis2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
AID107274Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID109496Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5)1999Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
Modeling of amino-terminal domains of group I metabotropic glutamate receptors: structural motifs affecting ligand selectivity.
AID328186Inhibition of Photinus pyralis luciferase by BrightGlo reporter gene assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID328184Inhibition of luciferase Photuris pennsylvanica by Promega Kinase-Glo assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID107261Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID328187Inhibition of Renilla reniformis luciferase2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID109164Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3).2000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID108489Agonist potency against cloned human metabotropic glutamate receptor 12000Journal of medicinal chemistry, Jul-13, Volume: 43, Issue:14
Ligands for glutamate receptors: design and therapeutic prospects.
AID328185Inhibition of Photinus pyralis luciferase by Steady-Glo reporter gene assay2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Characterization of chemical libraries for luciferase inhibitory activity.
AID1346269Human mGlu5 receptor (Metabotropic glutamate receptors)1999The Journal of pharmacology and experimental therapeutics, Jul, Volume: 290, Issue:1
SIB-1757 and SIB-1893: selective, noncompetitive antagonists of metabotropic glutamate receptor type 5.
AID1346285Human mGlu4 receptor (Metabotropic glutamate receptors)2003British journal of pharmacology, Mar, Volume: 138, Issue:6
Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP.
AID1346269Human mGlu5 receptor (Metabotropic glutamate receptors)2002Bioorganic & medicinal chemistry letters, Feb-11, Volume: 12, Issue:3
[(3)H]-M-MPEP, a potent, subtype-selective radioligand for the metabotropic glutamate receptor subtype 5.
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).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (5.26)18.2507
2000's20 (52.63)29.6817
2010's10 (26.32)24.3611
2020's6 (15.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.10

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.10 (24.57)
Research Supply Index3.76 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (2.38%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other41 (97.62%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]