Page last updated: 2024-12-04

aminooxyacetic acid

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

Description

Aminooxyacetic acid (AOAA) is a potent and selective inhibitor of monoamine oxidase (MAO), an enzyme that plays a crucial role in the breakdown of neurotransmitters in the brain. Its synthesis involves the reaction of glycine with hydroxylamine. AOAA has been extensively studied for its potential therapeutic effects in a variety of neurological and psychiatric disorders. It has shown promise in treating depression, anxiety, and Parkinson's disease. However, its use is limited due to its toxicity. The compound's importance lies in its ability to modulate neurotransmitter levels in the brain, leading to changes in mood, cognition, and behavior. Further research is ongoing to investigate its potential benefits and risks.'

Aminooxyacetic Acid: A compound that inhibits aminobutyrate aminotransferase activity in vivo, thereby raising the level of gamma-aminobutyric acid in tissues. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(aminooxy)acetic acid : A member of the class of hydroxylamines that is acetic acid substituted at postion 2 by an aminooxy group. It is a compound which inhibits aminobutyrate aminotransferase activity in vivo, resulting in increased levels of gamma-aminobutyric acid in tissues. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID286
CHEMBL ID347862
CHEBI ID40823
MeSH IDM0000955

Synonyms (63)

Synonym
(o-carboxymethyl)hydroxylamine
(carboxymethoxy)amine
u 7524
brn 0878238
acetic acid, (aminooxy)-
NCGC00015058-01
lopac-a-4508
AOA ,
(aminooxy)acetic acid
CARBOXYMETHOXYLAMINE ,
645-88-5
aminoxyacetic acid
aminooxyacetic acid
aoaa
carboxymethoxyamine
DB02079
LOPAC0_000007
NCGC00162041-01
396FBBC5-D28E-448C-A696-BF9163EA8B1A
acetic acid, aminooxy-
NCGC00015058-03
aminooxy-acetic acid
CHEMBL347862
2-aminooxyacetic acid
CCG-204103
AKOS015919037
NCGC00015058-02
u-7524
14i68gi3oq ,
unii-14i68gi3oq
AB00172543-06
acetic acid,2-(aminooxy)-
carboxymethoxyamine-d2 hemihydrochloride
gtpl5136
2-(aminooxy)acetic acid
hydroxylamine acetic acid
aminoxy-acetic acid
amino-oxyacetic acid
2-(aminoxy)acetic acid
methoxyamine, 1-carboxy-
hydroxylamine, o-(carboxymethyl)-
J-650057
DTXSID50214756
sr-01000075676
SR-01000075676-1
Q4746466
aoa hemihydrochloride
2-(aminooxy)acetic acid pound>>aoaa pound>>u 7524 pound>>u7524; u-7524 pound>>hydroxylamine, o-(carboxymethyl)-
BCP30347
STL197511
SDCCGSBI-0049996.P002
NCGC00015058-04
aoa; aoaa; u 7524; alpha-aminooxyacetic acid
SB38109
AT14480
CHEBI:40823
2-aminooxyethanoic acid
A901703
2-(aminooxy)aceticacid
aoa; aoaa; u 7524; -aminooxyacetic acid
HY-107994A
CS-0031154
EN300-40734

Research Excerpts

Overview

Aminooxyacetic acid (AOAA) is a potent inhibitor of GABA-transaminase and increases GABA levels in the brain. It has been shown to protect the inner ear from loud noises.

ExcerptReferenceRelevance
"Aminooxyacetic acid (AOAA) is an inhibitor of aspartate aminotransferase in the aspartate-arginosuccinate shunt."( Aminooxyacetic acid attenuates post-infarct cardiac dysfunction by balancing macrophage polarization through modulating macrophage metabolism in mice.
Chen, W; Hui, J; Li, J; Pan, L; Shen, Z; Zhang, Y; Zhao, P; Zhao, Y; Zhou, W, 2020
)
2.72
"Aminooxyacetic acid (AOAA) is a potent inhibitor of GABA-transaminase and increases GABA levels in the brain."( Neonatal monosodium glutamate administration increases aminooxyacetic acid (AOA) susceptibility effects in adult mice.
Cadena Razo, A; Campos-Sepúlveda, AE; Martínez Enríquez, ME; Peláez, LE; Rodríguez Amézquita, AL; Rodríguez Arellanes, R, 2009
)
1.32
"Aminooxyacetic acid (AOAA) is an inhibitor of several pyridoxal phosphate-depedent enzymes in the brain. "( Aminooxyacetic acid results in excitotoxin lesions by a novel indirect mechanism.
Beal, MF; Finn, SF; Hyman, BT; Koroshetz, W; Storey, E; Swartz, KJ, 1991
)
3.17
"Aminooxyacetic acid (AOAA) is a transaminase inhibitor that has been shown to protect the inner ear from loud noises. "( A functional and histological study of the combined effects of gentamicin and aminooxyacetic acid on the organ of Corti of the guinea pig.
el Begermy, MA; Galic, M; Giebel, W, 1987
)
1.94

Effects

ExcerptReferenceRelevance
"Aminooxyacetic acid (AOAA) has been shown to confer protection against noise-induced cochlear trauma [3]. "( The potentiation of ototoxicity when aminooxyacetic acid and kanamycin are co-administered.
Alexander, A; Bryant, GM; Cronin-Schreiber, R; Guth, PS; Norris, CH; Quine, DB, 1984
)
1.98

Treatment

Aminooxyacetic acid (AOAA), a GABA transaminase inhibitor, antagonised picrotoxin-induced myoclonus. Pretreatment with AOAA at a dose which inhibits running fits induced by intracollicular injection of SC depressed the activity.

ExcerptReferenceRelevance
"Aminooxyacetic acid pretreatment significantly diminished compound A-induced increases in urine volume (19.7 +/- 3.5 ml/24 h vs."( Role of renal cysteine conjugate beta-lyase in the mechanism of compound A nephrotoxicity in rats.
Garton, K; Hankins, DC; Kharasch, ED; Kilty, CG; Thorning, D, 1997
)
1.02
"Pretreatment with aminooxyacetic acid at a dose which inhibits running fits induced by intracollicular injection of SC depressed the activity."( Running fits and gamma-aminobutyric acid of the superior colliculus of the mouse.
Hirata, Y; Yamashita, J, 1979
)
0.58
"Pretreatment with aminooxyacetic acid (AOAA), a GABA transaminase inhibitor, antagonised picrotoxin-induced myoclonus."( A functional interaction between GABA and 5-HT in inhibiting picrotoxin-induced myoclonus in rats.
Krishnamoorthy, MS; Paul, V, 1990
)
0.6

Toxicity

ExcerptReferenceRelevance
" Aminooxyacetic acid (AOAA), an inhibitor of cysteine conjugate beta-lyase, reduced the covalent binding of PCBC-equivalents to tubular protein by approximately 90% and decreased but did not prevent the toxic effects produced by PCBC on RPT respiration and cellular ATP levels."( Pentachlorobutadienyl-L-cysteine (PCBC) toxicity: the importance of mitochondrial dysfunction.
Groves, CE; Lock, EA; Schnellmann, RG; Sokol, PP; Steffens, TG, 1991
)
1.19
" DCVC was consistently found to be more toxic than DCVG, but the inclusion of gamma-glutamyltransferase (0."( Renal cysteine conjugate beta-lyase-mediated toxicity studied with primary cultures of human proximal tubular cells.
Chen, JC; Jones, TW; Stevens, JL; Trifillis, AL, 1990
)
0.28
" In contrast apical treatment with PCBD-NAC was only toxic at high concentrations (greater than 850 microM), and this effect could hardly be inhibited by AOAA."( Differential toxicity as a result of apical and basolateral treatment of LLC-PK1 monolayers with S-(1,2,3,4,4-pentachlorobutadienyl)glutathione and N-acetyl-S-(1,2,3,4,4-pentachlorobutadienyl)-L-cysteine.
Mertens, JJ; Spenkelink, B; Temmink, JH; van Bladeren, PJ; van Doorn, WJ; Weijnen, JG, 1988
)
0.27
" Previous studies have demonstrated that a toxic metabolite contributes to or is responsible for acute NDPS-induced nephrotoxicity."( Role of glutathione in acute N-(3,5-dichlorophenyl) succinimide-induced nephrotoxicity in Sprague-Dawley and Fischer 344 rats.
Bolton, B; Brown, PI; Rankin, GO; Teets, VJ; Yang, DJ, 1987
)
0.27
" S-(1,2-Dichlorovinyl)-L-glutathione is not toxic when the cells are pretreated with AT-125, an inhibitor of gamma-glutamyl transpeptidase."( The role of glutathione conjugate metabolism and cysteine conjugate beta-lyase in the mechanism of S-cysteine conjugate toxicity in LLC-PK1 cells.
Hayden, P; Stevens, J; Taylor, G, 1986
)
0.27
" However, several selenium compounds are known to be relatively toxic compounds."( Comparative cytotoxicity of 14 novel selenocysteine se-conjugates in rat renal proximal tubular cells.
Andreadou, I; Commandeur, JN; Nagelkerke, FJ; van de Water, B; Vermeulen, NP, 1996
)
0.29
"Carbon dioxide absorbents degrade both halothane and sevoflurane to toxic unsaturated compounds (CF2=CBrCl and CH2F-O-C[=CF2][CF3] [i."( Quantitative differences in the production and toxicity of CF2=BrCl versus CH2F-O-C(=CF2)(CF3) (compound A): the safety of halothane does not indicate the safety of sevoflurane.
Eger, EI; Gong, D; Ionescu, P; Kerschmann, RL; Laster, MJ; Weiskopf, RB, 1997
)
0.3
" The toxic process might also be mediated by glutathione (GSH) conjugates of ADCP, as suggested for the mechanism of 4-aminophenol nephrotoxicity."( 4-Amino-2,6-dichlorophenol nephrotoxicity in the Fischer 344 rat: protection by ascorbic acid, AT-125, and aminooxyacetic acid.
Anestis, DK; Ball, JG; Brown, PI; Hong, SK; Rankin, GO; Valentovic, MA, 1997
)
0.51
" Prior work has shown that the efficiency of the GSH-dependent renal detoxification of haloalkene derived mercapturates is significantly decreased upon their deacetylation because of rapid transformation of the deacetylated products into toxic compounds mediated by β-lyase."( Inhibition of aminoacylase 3 protects rat brain cortex neuronal cells from the toxicity of 4-hydroxy-2-nonenal mercapturate and 4-hydroxy-2-nonenal.
Abuladze, N; Bragin, A; Cascio, D; Damoiseaux, R; Faull, K; Pushkin, A; Schibler, MJ; Tsirulnikov, K, 2012
)
0.38
"Exposure to the industrial solvent trichloroethylene (TCE) has been associated with adverse pregnancy outcomes in humans and decreased fetal weight in rats."( N-Acetyl-L-cysteine and aminooxyacetic acid differentially modulate trichloroethylene reproductive toxicity via metabolism in Wistar rats.
Bergin, IL; Bjork, F; Lash, LH; Loch-Caruso, R; Su, AL, 2021
)
0.93
" S-(1,2-Dichlorovinyl)-L-cysteine (DCVC) is a metabolite of TCE formed downstream in TCE glutathione (GSH) conjugation and is upstream of several toxic metabolites."( N-Acetyl-L-cysteine and aminooxyacetic acid differentially modulate toxicity of the trichloroethylene metabolite S-(1,2-dichlorovinyl)-L-cysteine in human placental villous trophoblast BeWo cells.
Lash, LH; Loch-Caruso, R; Su, AL, 2023
)
1.22

Dosage Studied

ExcerptRelevanceReference
"0 mg/kg AOAA significantly potentiated the effects of diazepam, as indicated by a significant shift to the left in the diazepam dose-response curve relative to diazepam alone."( Potentiation of the anticonflict effects of diazepam, but not pentobarbital and phenobarbital, by aminooxyacetic acid (AOAA).
Beshears, JF; Commissaris, RL; Halas, NA; McCloskey, TC, 1988
)
0.49
" Muscimol (2 mg/kg) and THIP (5 and 10 mg/kg) exerted the antiimmobility effect even after single dosing 1 h before the test."( Effect of GABAergic drugs in the behavioral 'despair' test in rats.
Borsini, F; Evangelista, S; Meli, A, 1986
)
0.27
" Dopa accumulation was significantly inhibited at a high dosage by nipecotic acid alone and by low dosages of nipecotic acid in rats pretreated with either aminooxyacetic acid or gabaculine."( Use of gamma-aminobutyric acid (GABA)-transaminase inhibitors and a GABA uptake inhibitor to investigate the influence of GABA neurons on dopamine-containing amacrine cells of the rat retina.
Morgan, WW; Proll, MA, 1983
)
0.46
" Toxic symptoms occurred in all seven patients when AOAA dosage was increased beyond 2 mg per kilogram per day, and included drowsiness, ataxia, seizures, and psychotic behavior."( Failure of aminooxyacetic acid therapy in Huntington disease.
Allan, BM; Baird, PA; Hansen, S; MacLeod, PM; Perry, TL; Wright, JM, 1980
)
0.65
" Studies with [35S]-PAP-GSH at 40 mumol kg-1 showed selective retention of radioactivity in the kidney, relative to other organs 24 h after dosing and that some radioactivity was covalently bound to renal proteins."( Nephrotoxicity of 4-amino-3-S-glutathionylphenol and its modulation by metabolism or transport inhibitors.
Foster, JR; Fowler, LM; Lock, EA, 1994
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
nootropic agentAny compound that improves mental functions such as cognition, memory, intelligence, motivation, attention, and concentration.
EC 4.2.1.22 (cystathionine beta-synthase) inhibitorAn EC 4.2.1.* (hydro-lyases) inhibitor that interferes with the action of cystathionine beta-synthase (EC 4.2.1.22).
EC 2.6.1.19 (4-aminobutyrate--2-oxoglutarate transaminase) inhibitorAn EC 2.6.1.* (transaminase) inhibitor that interferes with the action of 4-aminobutyrate--2-oxoglutarate transaminase (EC 2.6.1.19).
anticonvulsantA drug used to prevent seizures or reduce their severity.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (3)

ClassDescription
amino acidA carboxylic acid containing one or more amino groups.
hydroxylaminesHydroxylamine, H2N-OH, and its hydrocarbyl derivatives.
monocarboxylic acidAn oxoacid containing a single carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (1)

PathwayProteinsCompounds
TCA cycle in senescence011

Protein Targets (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency5.80480.00521.30228.1995AID624455
thioredoxin reductaseRattus norvegicus (Norway rat)Potency3.23360.100020.879379.4328AID488773; AID588453
ThrombopoietinHomo sapiens (human)Potency5.01190.02517.304831.6228AID917; AID918
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926; AID938
regulator of G-protein signaling 4Homo sapiens (human)Potency0.75120.531815.435837.6858AID504845
arylsulfatase AHomo sapiens (human)Potency0.06011.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency5.97280.035520.977089.1251AID504332
D(1A) dopamine receptorHomo sapiens (human)Potency0.14580.02245.944922.3872AID488982
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency0.84920.134610.395030.1313AID1347049
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency2.23870.00106.000935.4813AID944
[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)
Cystathionine gamma-lyaseHomo sapiens (human)IC50 (µMol)2.28500.57002.86098.0000AID1506493; AID1506495
Cystathionine beta-synthaseHomo sapiens (human)IC50 (µMol)5.27501.00005.15718.9000AID1412123; AID1412124; AID1506492; AID1506494
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (32)

Processvia Protein(s)Taxonomy
cysteine metabolic processCystathionine gamma-lyaseHomo sapiens (human)
lipid metabolic processCystathionine gamma-lyaseHomo sapiens (human)
protein-pyridoxal-5-phosphate linkage via peptidyl-N6-pyridoxal phosphate-L-lysineCystathionine gamma-lyaseHomo sapiens (human)
cysteine biosynthetic process via cystathionineCystathionine gamma-lyaseHomo sapiens (human)
cysteine biosynthetic processCystathionine gamma-lyaseHomo sapiens (human)
transsulfurationCystathionine gamma-lyaseHomo sapiens (human)
endoplasmic reticulum unfolded protein responseCystathionine gamma-lyaseHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCystathionine gamma-lyaseHomo sapiens (human)
protein sulfhydrationCystathionine gamma-lyaseHomo sapiens (human)
protein homotetramerizationCystathionine gamma-lyaseHomo sapiens (human)
hydrogen sulfide biosynthetic processCystathionine gamma-lyaseHomo sapiens (human)
positive regulation of aortic smooth muscle cell differentiationCystathionine gamma-lyaseHomo sapiens (human)
cellular response to leukemia inhibitory factorCystathionine gamma-lyaseHomo sapiens (human)
negative regulation of apoptotic signaling pathwayCystathionine gamma-lyaseHomo sapiens (human)
endochondral ossificationCystathionine beta-synthaseHomo sapiens (human)
blood vessel remodelingCystathionine beta-synthaseHomo sapiens (human)
L-serine metabolic processCystathionine beta-synthaseHomo sapiens (human)
L-serine catabolic processCystathionine beta-synthaseHomo sapiens (human)
superoxide metabolic processCystathionine beta-synthaseHomo sapiens (human)
regulation of nitric oxide mediated signal transductionCystathionine beta-synthaseHomo sapiens (human)
cysteine biosynthetic process via cystathionineCystathionine beta-synthaseHomo sapiens (human)
cysteine biosynthetic processCystathionine beta-synthaseHomo sapiens (human)
transsulfurationCystathionine beta-synthaseHomo sapiens (human)
L-cysteine catabolic processCystathionine beta-synthaseHomo sapiens (human)
cerebellum morphogenesisCystathionine beta-synthaseHomo sapiens (human)
DNA protectionCystathionine beta-synthaseHomo sapiens (human)
negative regulation of apoptotic processCystathionine beta-synthaseHomo sapiens (human)
homocysteine catabolic processCystathionine beta-synthaseHomo sapiens (human)
homocysteine metabolic processCystathionine beta-synthaseHomo sapiens (human)
response to folic acidCystathionine beta-synthaseHomo sapiens (human)
maternal process involved in female pregnancyCystathionine beta-synthaseHomo sapiens (human)
cartilage development involved in endochondral bone morphogenesisCystathionine beta-synthaseHomo sapiens (human)
hydrogen sulfide biosynthetic processCystathionine beta-synthaseHomo sapiens (human)
cellular response to hypoxiaCystathionine beta-synthaseHomo sapiens (human)
blood vessel diameter maintenanceCystathionine beta-synthaseHomo sapiens (human)
cysteine biosynthetic process from serineCystathionine beta-synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
cystathionine gamma-lyase activityCystathionine gamma-lyaseHomo sapiens (human)
protein bindingCystathionine gamma-lyaseHomo sapiens (human)
calmodulin bindingCystathionine gamma-lyaseHomo sapiens (human)
pyridoxal phosphate bindingCystathionine gamma-lyaseHomo sapiens (human)
identical protein bindingCystathionine gamma-lyaseHomo sapiens (human)
L-cystine L-cysteine-lyase (deaminating)Cystathionine gamma-lyaseHomo sapiens (human)
homocysteine desulfhydrase activityCystathionine gamma-lyaseHomo sapiens (human)
L-cysteine desulfhydrase activityCystathionine gamma-lyaseHomo sapiens (human)
selenocystathionine gamma-lyase activityCystathionine gamma-lyaseHomo sapiens (human)
cystathionine beta-synthase activityCystathionine beta-synthaseHomo sapiens (human)
protein bindingCystathionine beta-synthaseHomo sapiens (human)
oxygen bindingCystathionine beta-synthaseHomo sapiens (human)
enzyme bindingCystathionine beta-synthaseHomo sapiens (human)
heme bindingCystathionine beta-synthaseHomo sapiens (human)
pyridoxal phosphate bindingCystathionine beta-synthaseHomo sapiens (human)
ubiquitin protein ligase bindingCystathionine beta-synthaseHomo sapiens (human)
identical protein bindingCystathionine beta-synthaseHomo sapiens (human)
protein homodimerization activityCystathionine beta-synthaseHomo sapiens (human)
metal ion bindingCystathionine beta-synthaseHomo sapiens (human)
nitrite reductase (NO-forming) activityCystathionine beta-synthaseHomo sapiens (human)
carbon monoxide bindingCystathionine beta-synthaseHomo sapiens (human)
nitric oxide bindingCystathionine beta-synthaseHomo sapiens (human)
modified amino acid bindingCystathionine beta-synthaseHomo sapiens (human)
S-adenosyl-L-methionine bindingCystathionine beta-synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolCystathionine gamma-lyaseHomo sapiens (human)
extracellular exosomeCystathionine gamma-lyaseHomo sapiens (human)
cytoplasmCystathionine gamma-lyaseHomo sapiens (human)
nucleusCystathionine beta-synthaseHomo sapiens (human)
cytoplasmCystathionine beta-synthaseHomo sapiens (human)
cytosolCystathionine beta-synthaseHomo sapiens (human)
cytoplasmCystathionine beta-synthaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (40)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
AID1506499Antiproliferative activity against human NCM356 cells assessed as decrease in cell viability after 24 hrs by CCK8 assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID73510Percent of enzyme inhibition by Gamma-amino-N-butyrate transaminase assay method1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1412123Inhibition of full-length GST-fused human CBS assessed as reduction in H2S production using 2 mM S-methylcysteine as substrate preincubated for 3 mins followed by substrate addition2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1412125Non-competitive inhibition of full-length GST-fused human CBS using S-methylcysteine as substrate by Lineweaver-burk plot analysis2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID74657Percent of enzyme inhibition by Glutamate decarboxylase assay method; ND means no data1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID71453Displacement of [3H]- muscimol from GABA-A receptor from rat cerebellum membrane (ND = not determined)1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1412145Antitumor activity against human HT-29 cells xenografted in BALB/c nude mouse assessed as reduction in tumor weight at 10 mg/kg, sc administered once daily for 6 days followed by 1 day interval and subsequent dosing for 6 days relative to control2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1506498Antiproliferative activity against human HT-29 cells assessed as decrease in cell viability after 24 hrs by CCK8 assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID1412134Antiproliferative activity against human HT-29 cells after 24 hrs by CCK8 assay2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1412143Antitumor activity against human HT-29 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 10 mg/kg, sc administered once daily for 6 days followed by 1 day interval and subsequent dosing for 6 days2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1412135Antiproliferative activity against human HT-29 cells harboring CBS SiRNA after 24 hrs by CCK8 assay2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1506495Inhibition of N-terminal His-tagged CSE extracted from human HepG2 cells expressed in Escherichia coli BL21 (DE3) using cysteine as substrate assessed as decrease in H2S production preincubated for 3 mins in presence of lead nitrate followed by cysteine a2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID1506493Inhibition of N-terminal His-tagged CSE extracted from human HepG2 cells expressed in Escherichia coli BL21 (DE3) using methylcysteine as substrate measured for 10 mins by CPM probe-based fluorescence assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID40838Percent inhibition of [3H]- Diazepam binding to GABA-A Benzodiazepine receptor of rat frontal cortex membranes (ND = no data)1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
AID1412141Toxicity in BALB/c nude mouse xenografted with human HT-29 cells assessed as effect on body weight at 10 mg/kg, sc administered once daily for 6 days followed by 1 day interval and subsequent dosing for 6 days2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
AID1506492Inhibition of full-length GST-fused human CBS using methylcysteine as substrate measured for 10 mins by CPM probe-based fluorescence assay2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1506494Inhibition of full-length GST-fused human CBS using cysteine/homocysteine as substrate assessed as decrease in H2S production preincubated for 3 mins in presence of homocysteine and lead nitrate followed by cysteine addition2017MedChemComm, Jan-01, Volume: 8, Issue:1
Discovery of selective cystathionine β-synthase inhibitors by high-throughput screening with a fluorescent thiol probe.
AID1412124Inhibition of full-length GST-fused human CBS assessed as reduction in H2S production using 20 mM S-methylcysteine as substrate preincubated for 3 mins followed by substrate addition2018MedChemComm, Jan-01, Volume: 9, Issue:1
Antitumor effect of sikokianin C, a selective cystathionine β-synthase inhibitor, against human colon cancer
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.
AID1345267Human Cystathionine beta-synthase (Hydrogen sulphide synthesis)2013British journal of pharmacology, Jun, Volume: 169, Issue:4
Selectivity of commonly used pharmacological inhibitors for cystathionine β synthase (CBS) and cystathionine γ lyase (CSE).
AID1345185Human Cystathionine gamma-lyase (Hydrogen sulphide synthesis)2013British journal of pharmacology, Jun, Volume: 169, Issue:4
Selectivity of commonly used pharmacological inhibitors for cystathionine β synthase (CBS) and cystathionine γ lyase (CSE).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (838)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990483 (57.64)18.7374
1990's173 (20.64)18.2507
2000's79 (9.43)29.6817
2010's82 (9.79)24.3611
2020's21 (2.51)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.28

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 Index29.28 (24.57)
Research Supply Index6.78 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index40.78 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.28)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (0.46%)5.53%
Reviews12 (1.37%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other859 (98.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]