Compounds > lsp4-2022
Page last updated: 2024-11-13

lsp4-2022

Description

LSP4-2022: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71041983
CHEMBL ID3114673
SCHEMBL ID13975986
MeSH IDM0574018

Synonyms (13)

Synonym
CHEMBL3114673
lsp4-2022
gtpl6706
(2s)-2-amino-4-({[4-(carboxymethoxy)phenyl](hydroxy)methyl}(hydroxy)phosphoryl)butanoic acid
us9212196, derivative 2
bdbm196906
SCHEMBL13975986
(2s)-2-amino-4-({[4-(carboxymethoxy)phenyl] (hydroxy)methyl}-(hydroxy)phosphoryl)butanoic acid
Q27081933
1413405-33-0
HY-117764
CS-0067732
AKOS040748768
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Metabotropic glutamate receptor 8Homo sapiens (human)EC50 (µMol)29.20000.02300.97785.1000AID1455161
Metabotropic glutamate receptor 6Homo sapiens (human)EC50 (µMol)4.20000.05502.27864.9000AID1455162
Metabotropic glutamate receptor 4Homo sapiens (human)EC50 (µMol)0.11000.00401.71939.8000AID1455160
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (14)

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)
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 (6)

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 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 (8)

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 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 (10)

Assay IDTitleYearJournalArticle
AID1067411Selectivity for mGlu4 receptor (unknown origin) over mGlu8 receptor (unknown origin)2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
AID1067413Selectivity for mGlu4 receptor (unknown origin) over mGlu6 receptor (unknown origin)2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
AID1455165Selectivity ratio of EC50 for mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation to EC50 for mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID1455162Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID1067412Selectivity for mGlu4 receptor (unknown origin) over mGlu7 receptor (unknown origin)2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
AID1455160Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID1455161Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites.
AID1346285Human mGlu4 receptor (Metabotropic glutamate receptors)2012FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Apr, Volume: 26, Issue:4
A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential.
AID1346263Human mGlu7 receptor (Metabotropic glutamate receptors)2012FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Apr, Volume: 26, Issue:4
A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential.
AID1346272Human mGlu6 receptor (Metabotropic glutamate receptors)2012FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Apr, Volume: 26, Issue:4
A novel selective metabotropic glutamate receptor 4 agonist reveals new possibilities for developing subtype selective ligands with therapeutic potential.
[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's0 (0.00)29.6817
2010's8 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.31

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 Index12.31 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.31)

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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
amphetamine
Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine.		2.5520primary amine
imipramine
Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom.		2.1110dibenzoazepineadrenergic uptake inhibitor;
antidepressant;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
benzoxazoles
1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.		2.17101,3-benzoxazoles;
mancude organic heterobicyclic parent
cyclopentane
Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution.		2.1310cycloalkane;
cyclopentanes;
volatile organic compound		non-polar solvent
glutamic acid
Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.		2.1710glutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
2-amino-4-phosphonobutyric acid
(2S)-2-amino-4-phosphonobutanoic acid : A non-proteinogenc L-alpha-amino acid that is L-alpha-aminobutyric acid in which one of the hydrogens of the terminal methyl group has been replaced by a dihydroxy(oxido)-lambda(5)-phosphanyl group. It is a potent and selective agonist for the group III metabotropic glutamate receptors (mGluR4/6/7/8).		2.1710non-proteinogenic L-alpha-amino acid;
phosphonic acids		metabotropic glutamate receptor agonist
dizocilpine maleate
Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.		2.5520maleate salt;
tetracyclic antidepressant		anaesthetic;
anticonvulsant;
neuroprotective agent;
nicotinic antagonist;
NMDA receptor antagonist
1-aminocyclopentane-1,3,4-tricarboxylic acid
1-aminocyclopentane-1,3,4-tricarboxylic acid: metabolic glutamate receptor (mGluR) antagonist; structure in first source		2.1710
n,n'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine
N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: structure in first source		2.1310aryl sulfide
3,4-dicarboxyphenylglycine
[no description available]		2.1710
ConditionIndicatedRelationship StrengthStudiesTrials
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		03.0640
Mental Retardation, X-Linked
A class of genetic disorders resulting in INTELLECTUAL DISABILITY that is associated either with mutations of GENES located on the X CHROMOSOME or aberrations in the structure of the X chromosome (SEX CHROMOSOME ABERRATIONS).		02.1710
Anxiety
Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.		02.1710
Dementia Praecox
[description not available]		02.5520
Schizophrenia
A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.		02.5520
Chronic Illness
[description not available]		02.0810
Constriction, Pathological
[description not available]		02.0810
Allodynia
[description not available]		02.0810
Chronic Disease
Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).		02.0810
Constriction, Pathologic
The condition of an anatomical structure's being constricted beyond normal dimensions.		02.0810
Depression, Endogenous
[description not available]		02.1110
Depressive Disorder
An affective disorder manifested by either a dysphoric mood or loss of interest or pleasure in usual activities. The mood disturbance is prominent and relatively persistent.		02.1110
Dyskinesia, Medication-Induced
[description not available]		02.1310
Dyskinesia, Drug-Induced
Abnormal movements, including HYPERKINESIS; HYPOKINESIA; TREMOR; and DYSTONIA, associated with the use of certain medications or drugs. Muscles of the face, trunk, neck, and extremities are most commonly affected. Tardive dyskinesia refers to abnormal hyperkinetic movements of the muscles of the face, tongue, and neck associated with the use of neuroleptic agents (see ANTIPSYCHOTIC AGENTS). (Adams et al., Principles of Neurology, 6th ed, p1199)		02.1310
chemdatabank.com