Page last updated: 2024-11-11

1-aminocyclopentane-1,3,4-tricarboxylic acid

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Description

1-aminocyclopentane-1,3,4-tricarboxylic acid: metabolic glutamate receptor (mGluR) antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6604820
CHEMBL ID288635
CHEMBL ID285043
CHEMBL ID1440629
SCHEMBL ID659587
SCHEMBL ID659588
SCHEMBL ID3328641
MeSH IDM0281272

Synonyms (41)

Synonym
bdbm50076395
(1r,2s,4r)-4-amino-cyclopentane-1,2,4-tricarboxylic acid
gtpl1408
NCGC00025007-01 ,
tocris-1113
acpt-ii
NCGC00025006-04
NCGC00025006-03
CHEMBL288635 ,
CHEMBL285043 ,
(1s,2r,4s)-4-aminocyclopentane-1,2,4-tricarboxylic acid
(1s,2r,4s)-4-amino-cyclopentane-1,2,4-tricarboxylic acid
(1r,2s,4s)-4-aminocyclopentane-1,2,4-tricarboxylic acid
4-amino-cyclopentane-1,2,4-tricarboxylic acid
(1r,2s)-4-aminocyclopentane-1,2,4-tricarboxylic acid
bdbm50060137
acpt-1
acpt-i
1-aminocyclopentane-1,3,4-tricarboxylic acid
SCHEMBL659587
SCHEMBL659588
SCHEMBL3328641
AKOS024456389
(1s,3r,4s)-1-aminocyclopentane-1,3,4-tricarboxylic acid
(1r,3r,4s)-1-aminocyclopentane-1,3,4-tricarboxylic acid
195209-04-2
194918-76-8
CHEMBL1440629
AKOS024456388
sr-01000597385
SR-01000597386-1
SR-01000597385-1
sr-01000597386
J-012643
rel-(1r,2s,4r)-4-aminocyclopentane-1,2,4-tricarboxylic acid
Q27074158
HY-101387
CS-0021274
rel-acpt-i
HY-101387A
CS-0021275
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (22)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency11.22020.003245.467312,589.2998AID2517
phosphopantetheinyl transferaseBacillus subtilisPotency53.17640.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency8.91250.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686978; AID686979
regulator of G-protein signaling 4Homo sapiens (human)Potency1.68340.531815.435837.6858AID504845
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency25.11890.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.39810.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency6.30960.00636.904339.8107AID883
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.30960.00638.235039.8107AID883
[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 1Rattus norvegicus (Norway rat)IC50 (µMol)115.00000.00020.58878.9900AID108514
Metabotropic glutamate receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)88.00000.02320.11160.2000AID108989
[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 8Homo sapiens (human)EC50 (µMol)5.10000.02300.97785.1000AID1455155
Metabotropic glutamate receptor 6Homo sapiens (human)EC50 (µMol)11.00000.05502.27864.9000AID1455158
Metabotropic glutamate receptor 2Rattus norvegicus (Norway rat)EC50 (µMol)1,000.00000.00061.42627.7000AID271017
Metabotropic glutamate receptor 4Rattus norvegicus (Norway rat)EC50 (µMol)36.31330.00902.54409.4900AID246695; AID271018; AID476357
Metabotropic glutamate receptor 5Rattus norvegicus (Norway rat)EC50 (µMol)1,000.00000.00151.653710.0000AID271019
Metabotropic glutamate receptor 6Rattus norvegicus (Norway rat)EC50 (µMol)14.50000.05502.40307.6000AID271020; AID476363
Metabotropic glutamate receptor 7Rattus norvegicus (Norway rat)EC50 (µMol)740.00000.14600.82301.5000AID271021; AID476365
Metabotropic glutamate receptor 8Rattus norvegicus (Norway rat)EC50 (µMol)7.60000.03101.18138.0000AID271022; AID476367
Metabotropic glutamate receptor 7Homo sapiens (human)EC50 (µMol)280.00000.15850.66921.1800AID1455159
Metabotropic glutamate receptor 4Homo sapiens (human)EC50 (µMol)5.30000.00401.71939.8000AID109326; AID109331; AID1455157
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

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)
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)
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 (15)

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 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 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 (24)

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)
plasma membraneMetabotropic glutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneMetabotropic glutamate receptor 4Rattus norvegicus (Norway rat)
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 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 (37)

Assay IDTitleYearJournalArticle
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.
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.
AID109339Antagonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID108986Ratio between the measured EC50 and the glutamate EC50 measured against Metabotropic glutamate receptor 2; No effect1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID108989Inhibitory activity against Metabotropic glutamate receptor 2 in the rat HEK 293 cells.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID108673Agonist activity against Metabotropic glutamate receptor 2 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation; No effect at 1 mM1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID109327Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation; No effect at 1 mM1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID108356Agonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation; No effect at 1 mM1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID108487Antagonist activity against Metabotropic glutamate receptor 1 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID108514Inhibitory activity against Metabotropic glutamate receptor 1 in the rat LLC-PK1/HEK 293 cells.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID108507Ratio between the measured EC50 and the glutamate EC50 measured against Metabotropic glutamate receptor 1; No effect1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Agonist selectivity of mGluR1 and mGluR2 metabotropic receptors: a different environment but similar recognition of an extended glutamate conformation.
AID108826Antagonist activity against Metabotropic glutamate receptor 2 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID476363Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
AID476367Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
AID1455164Selectivity ratio of EC50 for mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation to EC50 for mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i prote2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID271020Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID108655Potency at Metabotropic glutamate receptor 1, measured as the ratio of EC50 to IC50; No effect at 1 mM2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID109480Potency at Metabotropic glutamate receptor 4, measured as the ratio of EC50 to IC502002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID271021Activity at rat mGluR7 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID1455158Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID271019Activity at rat mGluR5 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID1455155Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID476365Agonist activity at rat mGlu7 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
AID108827Antagonist activity against Metabotropic glutamate receptor 2 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation; No effect at 1 mM1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID246695Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Virtual screening workflow development guided by the "receiver operating characteristic" curve approach. Application to high-throughput docking on metabotropic glutamate receptor subtype 4.
AID109326Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
AID271022Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID476357Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
AID1455157Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID271018Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID271028Activity at rat mGluR3 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID109331Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay2000Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.
AID1455159Agonist activity at mGlu7 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID271017Activity at rat mGluR2 receptor measured as intracellular calcium concentration in HEK293 cells2006Bioorganic & medicinal chemistry letters, Sep-15, Volume: 16, Issue:18
Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): identification of a new group III metabotropic glutamate receptor selective agonist.
AID109009Potency at Metabotropic glutamate receptor 2, measured as the ratio of EC50 to IC50; No effect at 1 mM2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Common and selective molecular determinants involved in metabotopic glutamate receptor agonist activity.
AID1346251Rat mGlu8 receptor (Metabotropic glutamate receptors)2000European journal of pharmacology, Apr-07, Volume: 394, Issue:1
Pharmacological characterization of the rat metabotropic glutamate receptor type 8a revealed strong similarities and slight differences with the type 4a receptor.
AID1346283Rat mGlu4 receptor (Metabotropic glutamate receptors)1997Journal of medicinal chemistry, Sep-12, Volume: 40, Issue:19
Synthesis and pharmacological characterization of aminocyclopentanetricarboxylic acids: new tools to discriminate between metabotropic glutamate receptor subtypes.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (11.76)18.2507
2000's7 (41.18)29.6817
2010's6 (35.29)24.3611
2020's2 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.75

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.75 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.75)

All Compounds (24.57)

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%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]