Page last updated: 2024-12-05

2-amino-7-phosphonoheptanoic acid

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

2-Amino-7-phosphonoheptanoic acid (APHA) is a non-protein amino acid analog of glutamate that acts as a potent and selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5). It has been shown to exert neuroprotective effects in animal models of stroke, traumatic brain injury, and Alzheimer's disease. APHA is synthesized through a multi-step process involving the coupling of a protected amino acid with a phosphonoacetic acid derivative, followed by deprotection. Research on APHA focuses on its potential therapeutic applications in various neurological disorders due to its ability to modulate glutamate signaling. Studies are investigating its efficacy in reducing excitotoxicity, inflammation, and neuronal apoptosis, and its impact on cognitive function and memory. Furthermore, APHA is being explored as a potential tool for investigating the role of mGluR5 in neurological diseases and for developing novel therapeutic strategies.'

2-amino-7-phosphonoheptanoic acid: (D)-isomer active as an antagonist of N-methyl-D-aspartate excitation of central neurons; (L)-isomer inactive; RN given refers to cpd without isomeric designation [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3122
CHEMBL ID274440
SCHEMBL ID154303
MeSH IDM0098298

Synonyms (54)

Synonym
2-amino-7-phosphonoheptanoic acid
2-amino-7-phosphono-heptanoic acid
NCI60_025601
nsc-672105
nsc672105
EU-0100008
dl-2-amino-7-phosphonoheptanoic acid, ~95%
PDSP2_000129
heptanoic acid, 2-amino-7-phosphono-, (+-)-
brn 3544152
heptanoic acid, 2-amino-7-phosphono-
LOPAC0_000008
PDSP1_000130
NCGC00024469-02
(?)-2-amino-7-phosphonoheptanoic acid
NCGC00024469-03
NCGC00015013-04
A 5157
( inverted question mark)-2-amino-7-phosphonoheptanoic acid
( inverted question mark)-ap-7
NCGC00015013-06
85797-13-3
ap-7
CHEMBL274440 ,
AKOS005066193
2-amino-7-phosphono-heptanoic acid (ap7)
(aph)2-amino-7-phosphono-heptanoic acid
dl-ap7
bdbm50002363
HMS3260A17
CCG-204104
NCGC00015013-05
p34k80cusm ,
dl-2-amino-7-phosphonoheptanoic acid
unii-p34k80cusm
(+/-)-2-amino-7-phosphonoheptanoic acid
LP00008
SCHEMBL154303
MYDMWESTDPJANS-UHFFFAOYSA-N
NCGC00260693-01
tox21_500008
(y)-2-amino-7-phosphonoheptanoic acid
78966-69-5
sr-01000075448
SR-01000075448-1
FT-0771861
Q4653176
(+/-)-2-amino-7-phosphonoheptanoic
DTXSID501017823
SDCCGSBI-0049997.P002
2-amino-7-phosphonoheptanoic acid.
D-200
HY-100782
CS-0020420

Research Excerpts

Toxicity

ExcerptReferenceRelevance
") were also resistant to the toxic effects of quisqualic acid, indicating the possible involvement of NMDA receptors in quisqualic acid toxicity."( Quisqualic acid-induced neurotoxicity is protected by NMDA and non-NMDA receptor antagonists.
Pai, KS; Ravindranath, V, 1992
)
0.28

Dosage Studied

ExcerptRelevanceReference
" Apomorphine-induced cage climbing behavior was partially decreased by lower dosages of GDEE, but was almost completely blocked by the highest dosage tested."( A possible role of AA2 excitatory amino acid receptors in the expression of stimulant drug effects.
Cannon-Spoor, HE; Freed, WJ, 1990
)
0.28
" APH caused motor incoordination at a dosage of 125 mg/kg, and a prolonged motor impairment was present after administration of APH, 250 mg/kg."( Impaired motor coordination in mice induced by 2-amino-7-phosphonoheptanoic acid (APH), glutamic acid diethyl ester (GDEE), and other compounds.
Freed, WJ, 1989
)
0.53
" Dose-response relationships showed a close association between seizure activity (measured by EEG) and extracellular Ca2+ changes in the injected area."( Quinolinic acid-induced seizures, but not nerve cell death, are associated with extracellular Ca2+ decrease assessed in the hippocampus by brain dialysis.
Angelico, P; Samanin, R; Stasi, MA; Vezzani, A; Wu, HQ, 1988
)
0.27
" To determine if acidic amino acid pathways were involved in this elevation, a low dosage of a selective NMDA antagonist, 2-amino-7-phosphonoheptanoic acid (APH) was injected intracerebroventricularly 4 min before having rats swim 4 laps."( 2-Amino-7-phosphonoheptanoic acid, a selective N-methyl-D-aspartate antagonist, blocks swim-induced elevation of cerebellar cyclic guanosine monophosphate.
McCaslin, PP; Morgan, WW, 1986
)
1.92
" Dose-response curves were evaluated by means of an ethological method in which behavioral sequences typical of S and R animals were quantitated."( NMDA-dependent audiogenic seizures are differentially regulated by inferior colliculus subnuclei.
Garcia-Cairasco, N; Terra, VC, 1994
)
0.29
" mexiletine, an orally active congener of lidocaine, on strychnine allodynia and compared the dose-response relationship of mexiletine in normal (noxious paw pinch) versus abnormal (i."( Comparable dose-dependent inhibition of AP-7 sensitive strychnine-induced allodynia and paw pinch-induced nociception by mexiletine in the rat.
Hodge, E; Khandwala, H; Loomis, CW, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency1.77830.100020.879379.4328AID588453
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency6.30960.28189.721235.4813AID2326
arylsulfatase AHomo sapiens (human)Potency0.03381.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.97690.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00500.540617.639296.1227AID2364; AID2528
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency398.10700.010039.53711,122.0200AID1479
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.48130.251215.843239.8107AID504327
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1459
neuropeptide S receptor isoform AHomo sapiens (human)Potency31.62280.015812.3113615.5000AID1461
[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)
Glutamate receptor 1Rattus norvegicus (Norway rat)Ki100.00000.00000.41052.7800AID92947
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.600310.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.94130.00030.86666.6900AID143148; AID145325
Glutamate receptor ionotropic, kainate 3Rattus norvegicus (Norway rat)Ki100.00000.00380.79754.1000AID91469
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.630610.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.94130.00030.68056.6900AID143148; AID145325
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)63.66050.00061.525710.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.94130.00030.70716.6900AID143148; AID145325
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.747210.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.94130.00030.81966.6900AID143148; AID145325
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.741110.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.94130.00030.70726.6900AID143148; AID145325
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.741110.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.94130.00030.70726.6900AID143148; AID145325
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)IC50 (µMol)63.66050.00071.741110.0000AID144604; AID144621; AID144761; AID144905; AID145027; AID145029; AID145038; AID145097; AID145098
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.94130.00030.70726.6900AID143148; AID145325
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (50)

Assay IDTitleYearJournalArticle
AID180491Tested for inhibition of NMDA-induced cyclic GMP increase in rat cerebellar slices1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate.
AID145098Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]TCP as the radioligand.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID91469Binding affinity towards Ionotropic glutamate receptor kainate using [3H]-kainic acid as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID196560In vitro antagonist activity by its ability to inhibit glutamate-induced accumulation of [45Ca2+]- in cultured rat cortical neurons.1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
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.
AID132435Functional NMDA antagonist activity was confirmed in vivo in mice (intraperitoneally) using an NMDA-induced lethality assay2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID74396Concentration required to inhibit glucosamine-6-phosphate synthase (GFAT) isolated from Candida albicans2002Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18
Multisubstrate analogue inhibitors of glucosamine-6-phosphate synthase from Candida albicans.
AID144905Inhibitory activity evaluated by its ability to displace [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat cortical membranes at 10E-5 concentration of the compound1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
AID25861Potentiometric pKa(in 25 mL of water) of the compound.1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate.
AID131241NMDA receptor antagonist activity of compound was demonstarted in vivo by the inhibition of NMDA-induced lethality in mouse tested in vivo1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID145027NMDA receptor antagonistic activity was assessed from the ability to displace [3H]CPP29,30 from rat cortical membranes.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID145029NMDA receptor antagonistic activity was assessed in vitro by deteriming the ability to inhibit glutamate-induced accumulation of [Ca2+] in cultured rat cortical neurons.1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID145097Tested for binding affinity against NMDA receptor, from rat synaptic membrane, using [3H]-CPP as the radioligand.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID145038Inhibition of [3H]CPP binding to rat N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
AID131239NMDA antagonist activity was measured as ataxia (the inability of the mice to cling to screen platform upon its inversion.) tested in vivo1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
AID144456Displacement of [3H]CPP from N-methyl-D-aspartate glutamate receptor in rat brain membrane1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Generation of N-methyl-D-aspartate agonist and competitive antagonist pharmacophore models. Design and synthesis of phosphonoalkyl-substituted tetrahydroisoquinolines as novel antagonists.
AID92947Binding affinity towards AMPA receptor using [3H]AMPA as radioligand; Inactive1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID180480Percent inhibition of glutamate activity against cGMP was determined1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID143148Compound was evaluated for its ability to displace [3H]-CGS- 19755 ligand from N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Modeling of competitive phosphono amino acid NMDA receptor antagonists.
AID144761Functional NMDA antagonist activity(at 100 uM) in vitro, using a stimulated 3[H]-TCP binding assay2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID115599Ability to protect against NMDA-induced lethality in mice after intraperitoneal administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.
AID144621Inhibition of N-methyl-D-aspartate glutamate receptor by using [3H]CPP as a radioligand from the rat cortical membranes.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
AID26606potentiometric pKa(in 25 mL of 1 M NaCl) of the compound.1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate.
AID112373Tested in vivo for inhibition of NMDA induced lethality, in male Swiss-Albino mice after ip administration.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
AID145325Displacement of [3H]CPP or [3H]-CGS- 19755 from rat N-methyl-D-aspartate glutamate receptor1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Modeling of competitive phosphono amino acid NMDA receptor antagonists.
AID114178Effective dose against NMDA-induced lethality in male Swiss-albino mice1992Journal of medicinal chemistry, Dec-11, Volume: 35, Issue:25
Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
AID144056Compound was evaluated for the inhibition of the binding of [3H]CPP against NMDA in mice1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists.
AID144604Competitive inhibition (at 100 uM) of NMDA receptor site was assessed by its ability to displace [3H]CPP from its binding site in rat synaptic membranes2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
AID143309In vitro binding affinity towards N-methyl-D-aspartate glutamate receptor of the glutamate receptor using [3H]CPP as radioligand in rat cerebral cortical membranes.1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
AID25334Dissociation constant (pKa)1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
A unified approach to systematic isosteric substitution for acidic groups and application to NMDA antagonists related to 2-amino-7-phosphonoheptanoate.
AID144334Binding affinity for glutamate-stimulated TCP binding site of N-methyl-D-aspartate glutamate receptor from rat brain by using [3H]-TCP as radioligand; ant = antagonist1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
New and versatile approaches to the synthesis of CPP-related competitive NMDA antagonists. Preliminary structure-activity relationships and pharmacological evaluation.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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 (373)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990116 (31.10)18.7374
1990's173 (46.38)18.2507
2000's50 (13.40)29.6817
2010's28 (7.51)24.3611
2020's6 (1.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 8.40

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 Index8.40 (24.57)
Research Supply Index5.98 (2.92)
Research Growth Index4.38 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (8.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews5 (1.27%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other390 (98.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]