Page last updated: 2024-12-04

aniracetam

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

Cross-References

ID SourceID
PubMed CID2196
CHEMBL ID36994
CHEBI ID47943
SCHEMBL ID70998
MeSH IDM0111076

Synonyms (150)

Synonym
AC-15651
2-pyrrolidinone, 1-(4-methoxybenzoyl)-
1-(p-methoxybenzoyl)-2-pyrrolidinon [german]
1-anisoyl-2-pyrrolidinone
ro 13-5057
aniracetam [usan:inn:jan]
aniracetamun [inn-latin]
brn 4807205
1-p-anisoyl-2-pyrrolidinone
ro 135057
HMS3266L08
BRD-K88611939-001-02-6
MLS000079240 ,
smr000038438
DIVK1C_000403
KBIO1_000403
ampamet
reset
sarpul
ro-13-5057
draganon
EU-0100115
aniracetam, >=98%
SPECTRUM_001342
NCGC00021402-02
NCGC00015116-01
tocris-0867
lopac-a-9950
IDI1_000403
BIOMOL-NT_000222
SPECTRUM5_001609
BPBIO1_001316
BSPBIO_003026
72432-10-1
aniracetam ,
DB04599
1-p-anisoylpyrrolidin-2-one
aniracetam (jan/usan/inn)
1-(4-methoxybenzoyl)-2-pyrrolidinone
D01883
NCGC00021402-08
NCGC00021402-06
MLS000028591
KBIO2_006958
KBIO2_001822
KBIOSS_001822
KBIOGR_001142
KBIO2_004390
KBIO3_002526
NINDS_000403
SPECTRUM4_000761
SPECTRUM3_001553
SPECTRUM1503078
LOPAC0_000115
MLS001201800
NCGC00021402-05
NCGC00021402-07
NCGC00015116-02
CHEBI:47943 ,
1-(4-methoxybenzoyl)pyrrolidin-2-one
NCGC00015116-07
HMS2094K07
A 9950
HMS2089O17
NCGC00015116-11
nsc-758223
CHEMBL36994
memodrin
ro-135057
HMS501E05
AKOS005066313
NCGC00015116-10
A837527
HMS3260G12
1-(p-methoxybenzoyl)-2-pyrrolidinon
unii-5l16lkn964
5l16lkn964 ,
aniracetamun
nsc 758223
BCP9000303
nsc758223
pharmakon1600-01503078
tox21_110086
cas-72432-10-1
dtxsid5045128 ,
dtxcid3025128
1-(4-methoxybenzoyl)-2-pyrrolidone
CCG-204210
HMS2234E11
NCGC00015116-09
NCGC00015116-08
NCGC00015116-04
NCGC00015116-03
NCGC00015116-12
NCGC00015116-06
NCGC00015116-05
BCPP000399
FT-0649064
LP00115
AB04115
S1281
gtpl4133
1-[(4-methoxyphenyl)carbonyl]pyrrolidin-2-one
aniracetam [inn]
aniracetam [usan]
aniracetam [who-dd]
aniracetam [mart.]
aniracetam [mi]
aniracetam [jan]
CS-1793
HY-10932
SCHEMBL70998
NCGC00015116-13
tox21_110086_1
KS-5313
AB00053303-14
tox21_500115
NCGC00260800-01
1-(p-methoxybenzoyl)-2-pyrrolidinone
1-(4-methoxy-benzoyl)-pyrrolidin-2-one
ro-13-3057
1-(4-methoxybenzoyl)-2-pyrrolidinone #
HB0116
OPERA_ID_294
AB00053303_16
AB00053303_15
mfcd00153767
sr-01000003147
SR-01000003147-2
HMS3657G11
H10883
SR-01000003147-6
SR-01000003147-4
SR-01000003147-8
SBI-0050103.P004
HMS3713N20
SW199095-2
aniracetam; 1-p-anisoyl-2-pyrrolidinone
Q417630
HMS3675P17
aniracetam ,(s)
BCP02091
HMS3411P17
BRD-K88611939-001-13-3
SDCCGSBI-0050103.P005
HMS3884C09
NCGC00015116-24
aniracetam;p-methoxybenzoyl-2-pirrolidone
BA164183
SY052612

Research Excerpts

Overview

Aniracetam is a nootropic compound and an allosteric modulator of AMPA receptors (AMPARs) which mediate synaptic mechanisms of learning and memory. It has been clinically used in the treatment of behavioral and psychological symptoms of dementia following stroke and in Alzheimer's disease.

ExcerptReferenceRelevance
"Aniracetam is a positive AMPA-receptor modulator that has shown promise for improving memory under conditions when the brain has been damaged, but its effectiveness in improving memory in neurologically healthy subjects is unclear."( Aniracetam does not improve working memory in neurologically healthy pigeons.
Colombo, M; McDowell, A; Mielby, BS; Phillips, H; Tucker, IG, 2019
)
2.68
"Aniracetam is a nootropic compound and an allosteric modulator of AMPA receptors (AMPARs) which mediate synaptic mechanisms of learning and memory. "( Postnatal aniracetam treatment improves prenatal ethanol induced attenuation of AMPA receptor-mediated synaptic transmission.
Breese, CR; Carpenter, M; Dityatev, A; Shonesy, BC; Suppiramaniam, V; Vaglenova, J; Vaithianathan, T; Wijayawardhane, N, 2007
)
2.18
"Aniracetam is a member of the nootropic class of drugs, which have possible cognition enhancing effects. "( Aniracetam. An overview of its pharmacodynamic and pharmacokinetic properties, and a review of its therapeutic potential in senile cognitive disorders.
Benfield, P; Lee, CR, 1994
)
3.17
"Aniracetam is a pyrrolidinone-type cognition enhancer that has been clinically used in the treatment of behavioral and psychological symptoms of dementia following stroke and in Alzheimer's disease. "( Aniracetam: its novel therapeutic potential in cerebral dysfunctional disorders based on recent pharmacological discoveries.
Nakamura, K, 2002
)
3.2
"Aniracetam is a nootropic drug that has been shown to selectively enhance quisqualate receptor-mediated responses in Xenopus oocytes injected with brain mRNA and in hippocampal pyramidal cells [Ito, I., Tanabe, S., Kohda, A. "( Aniracetam reduces glutamate receptor desensitization and slows the decay of fast excitatory synaptic currents in the hippocampus.
Isaacson, JS; Nicoll, RA, 1991
)
3.17
"Aniracetam has proved to be a useful drug in slight-moderate brain decay treatment of the elderly."( [Efficacy and tolerance of aniracetam in elderly patients with primary or secondary mental deterioration].
Acito, R; Bertini, M; Canonico, V; Casini, A; Colonna, CV; Forgione, L; Paoletti, C; Rengo, F,
)
1.15

Effects

Aniracetam has been reported to be efficacious for treating poststroke depression, but no studies that basically examined the antidepressive effects have been made. It has proved to be a useful drug in slight-moderate brain decay treatment of the elderly.

ExcerptReferenceRelevance
"Aniracetam has been used to improve the mental condition of patients with cerebrovascular disease. "( Effects of aniracetam on bladder overactivity in rats with cerebral infarction.
Kodama, K; Komatsu, K; Nagasaka, Y; Nakada, Y; Namiki, M; Niikura, S; Yokoyama, O; Yotsuyanagi, S, 2000
)
2.14
"Aniracetam has been reported to be efficacious for treating poststroke depression, but no studies that basically examined the antidepressive effects have been made."( Antidepressant-like effects of aniracetam in aged rats and its mode of action.
Nakamura, K; Tanaka, Y, 2001
)
2.04
"Aniracetam has proved to be a useful drug in slight-moderate brain decay treatment of the elderly."( [Efficacy and tolerance of aniracetam in elderly patients with primary or secondary mental deterioration].
Acito, R; Bertini, M; Canonico, V; Casini, A; Colonna, CV; Forgione, L; Paoletti, C; Rengo, F,
)
1.15

Treatment

Aniracetam was able to completely prevent and reverse the development of acute antinociceptive tolerance to morphine. The drug increases the ED50 values (mumol/kg i.p., 15 min) for GYKI 52466-induced protection against sound-induced clonic seizures in DBA/2 mice.

ExcerptReferenceRelevance
"Aniracetam pre-treatment significantly increased alcohol-reinforced responses relative to vehicle treatment."( Enhanced AMPA receptor activity increases operant alcohol self-administration and cue-induced reinstatement.
Besheer, J; Cannady, R; Durant, B; Fisher, KR; Hodge, CW, 2013
)
1.11
"In Aniracetam treated group the score showed a significant improving during the first and second control."( [Efficacy and tolerance of aniracetam in elderly patients with primary or secondary mental deterioration].
Acito, R; Bertini, M; Canonico, V; Casini, A; Colonna, CV; Forgione, L; Paoletti, C; Rengo, F,
)
0.94
"Treatment with aniracetam, a well-established AMPAR PAM, was able to completely prevent and reverse the development of acute antinociceptive tolerance to morphine."( AMPA receptor positive allosteric modulators attenuate morphine tolerance and dependence.
Chen, H; Guo, X; He, Y; Hu, X; Tian, X; Wang, ZJ; Zhou, J, 2018
)
0.82
"Pretreatment with aniracetam (50 nmol i.c.v., 15 min before drugs) increases the ED50 values (mumol/kg i.p., 15 min) for GYKI 52466-induced protection against sound-induced clonic seizures in DBA/2 mice 7 fold, from 20.1 (11.9-33.9) to 142 (91.7-219), and for NBQX-induced protection 2 fold, from 39.7 (33.8-46.7) to 85.6 (63.9-115), respectively."( Aniracetam reverses the anticonvulsant action of NBQX and GYKI 52466 in DBA/2 mice.
al-Zubaidy, Z; Chapman, AG; Meldrum, BS, 1993
)
2.05
"pretreatment with aniracetam (50 nmol/mouse)."( GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice.
Chapman, AG; Chimirri, A; De Sarro, A; de Sarro, G; Gitto, R; Giusti, P; Grasso, S, 1995
)
0.61

Toxicity

ExcerptReferenceRelevance
" Persisting stimulation of mGluRs after the toxic exposure did not improve the survival of pyramidal or granular cells."( Activation of multiple metabotropic glutamate receptor subtypes prevents NMDA-induced excitotoxicity in rat hippocampal slices.
Consolandi, O; Memo, M; Pizzi, M; Spano, PF, 1996
)
0.29

Pharmacokinetics

ExcerptReferenceRelevance
" To describe the time course of the plasma levels of AP and its metabolites after iv administration, a pharmacokinetic model with seven compartments was applied, which included 10 first-order rate constants and one Michaelis-Menten constant."( Pharmacokinetics of aniracetam and its metabolites in rats.
Horibe, Y; Ikeda, K; Iwaki, M; Ogiso, T; Paku, T; Suzuki, H; Tanino, T, 1998
)
0.62
" The validated method has been applied to the pharmacokinetic study after a single oral administration of aniracetam dispersible tablets to human beings."( Determination of aniracetam's main metabolite, N-anisoyl-GABA, in human plasma by LC-MS/MS and its application to a pharmacokinetic study.
Cai, S; Wang, L, 2012
)
0.93

Compound-Compound Interactions

ExcerptReferenceRelevance
"In the present study, we aimed to evaluate the efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors (ChEIs), in terms of several neuropsychological parameters, in a considerable number of patients with dementia."( Clinical efficacy of aniracetam, either as monotherapy or combined with cholinesterase inhibitors, in patients with cognitive impairment: a comparative open study.
Koliaki, CC; Messini, C; Tsolaki, M, 2012
)
0.94

Bioavailability

ExcerptReferenceRelevance
" The applicability and accuracy of the methods were demonstrated by the analysis of over 1000 plasma samples from two bioavailability studies in healthy volunteers."( Determination of aniracetam and its main metabolite, N-anisoyl-GABA, in human plasma by high-performance liquid chromatography.
Guenzi, A; Zanetti, M, 1990
)
0.62
" Elimination of AP and ABA was rapid after oral dosing, and the bioavailability of AP was extremely small (11."( Pharmacokinetics of aniracetam and its metabolites in rats.
Horibe, Y; Ikeda, K; Iwaki, M; Ogiso, T; Paku, T; Suzuki, H; Tanino, T, 1998
)
0.62
" The AUC(0-t) values demonstrated nearly identical bioavailability of aniracetam from the examined formulations."( Pharmacokinetics and bioequivalence study of aniracetam after single-dose administration in healthy Chinese male volunteers.
Chen, Y; Feng, SD; Tian, Y; Zhang, JJ; Zhang, ZJ, 2008
)
0.84
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

50 mg kg-1 was the lowest oral dose to significantly ameliorate scopolamine-induced amnesia. Concomitant treatment with aniracetam (50 nmol/mouse) shifted to the right the dose-response curves. It can be estimated that IDRA 21 is approximately 10-fold more potent than anir acetam in antagonizing alprazolam-induced learning deficit.

ExcerptRelevanceReference
" The dose-response curves for these compounds were bell-shaped."( Effects of N-(2,6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide (DM-9384) on learning and memory in rats.
Akashi, A; Kojima, H; Ojima, H; Sakurai, T; Yamasaki, T, 1989
)
0.28
" Generally, the dose-response curves were bell-shaped."( Effects of the novel compound aniracetam (Ro 13-5057) upon impaired learning and memory in rodents.
Bandle, EF; Cumin, R; Gamzu, E; Haefely, WE, 1982
)
0.55
" In a dose-response experiment it was demonstrated that 50 mg kg-1 was the lowest oral dose of aniracetam to significantly ameliorate scopolamine-induced amnesia."( Aniracetam reverses memory impairment in rats.
Jenck, F; Martin, JR; Moreau, JL, 1995
)
1.95
" From dose-response studies, it can be estimated that IDRA 21 is approximately 10-fold more potent than aniracetam in antagonizing alprazolam-induced learning deficit."( 7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide (IDRA 21), a congener of aniracetam, potently abates pharmacologically induced cognitive impairments in patas monkeys.
Costa, E; DiBella, M; Guidotti, A; Thompson, DM, 1995
)
0.73
" The dose-response relationship yielded a bell-shaped curve with a peak at 1 microM."( Enhancement of neuronal calcium channel currents by the nootropic agent, nefiracetam (DM-9384), in NG108-15 cells.
Watabe, S; Yoshii, M, 1994
)
0.29
" Concomitant treatment with aniracetam (50 nmol/mouse) shifted to the right the dose-response curves and significantly increased the ED50 values for GYKI 52466, 2,3-BZ-2 and 2,3-BZ-2M."( GYKI 52466 and related 2,3-benzodiazepines as anticonvulsant agents in DBA/2 mice.
Chapman, AG; Chimirri, A; De Sarro, A; de Sarro, G; Gitto, R; Giusti, P; Grasso, S, 1995
)
0.59
" Furthermore, cyclothiazide shifted the dose-response relationship of the equilibrium current to the right, but slightly suppressed the kainate-induced sustained current."( Modulation of desensitization at glutamate receptors in isolated crucian carp horizontal cells by concanavalin A, cyclothiazide, aniracetam and PEPA.
Lu, T; Shen, Y; Yang, XL, 1999
)
0.51
" The high brain levels of PD and the low levels of AP suggest that the clinical efficacy of dosed AP may partly result from PD penetrating into the brain."( Pharmacokinetics of aniracetam and its metabolites in rat brain.
Iwakai, M; Ogiso, T; Suzuki, H; Tanino, T; Uchiyama, K; Uno, S; Yoshimoro, M, 2000
)
0.63
" The results were as follows: (1) intrahippocampal treatment of aniracetam reversibly enhanced basal synaptic transmission in perforant path to dentate gyrus in a dosage dependent manner; (2) aniracetam produced improvement in Y-maze learning performance when administration occurred 5 min prior to maze learning; (3) aniracetam administration significantly facilitated behavioral LTP in dentate gyrus, while the maximal amplitude of LTP has no significant difference when compared to saline group."( Effects of intrahippocampal aniracetam treatment on Y-maze avoidance learning performance and behavioral long-term potentiation in dentate gyrus in rat.
Rao, Y; Xiao, P; Xu, S, 2001
)
0.84
" Nefiracetam at very high concentrations (approximately 10 microM) also potentiated alpha 4 beta 2-type currents but to a lesser extent, indicative of a bell-shaped dose-response relationship."( Nootropic drug modulation of neuronal nicotinic acetylcholine receptors in rat cortical neurons.
Kuryatov, A; Lindstrom, JM; Narahashi, T; Yeh, JZ; Zhao, X, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
N-acylpyrrolidine
pyrrolidin-2-onesA pyrrolidinone in which the oxo group is at position 2 of the pyrrolidine ring.
[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]

Protein Targets (28)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.00160.003245.467312,589.2998AID2517
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.81070.177814.390939.8107AID2147
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency0.22390.125919.1169125.8920AID2549
acetylcholinesteraseHomo sapiens (human)Potency43.64860.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency21.13170.006038.004119,952.5996AID1159521
Fumarate hydrataseHomo sapiens (human)Potency3.16230.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency14.12540.031637.5844354.8130AID743255
Microtubule-associated protein tauHomo sapiens (human)Potency0.56230.180013.557439.8107AID1468
EWS/FLI fusion proteinHomo sapiens (human)Potency33.17340.001310.157742.8575AID1259252
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency19.98260.003041.611522,387.1992AID1159552; AID1159555
polyproteinZika virusPotency3.16230.00308.794948.0869AID1347053
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency11.88230.023723.228263.5986AID743222
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02240.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00400.540617.639296.1227AID2364; AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
cytochrome P450 2C19 precursorHomo sapiens (human)Potency1.99530.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency6.30960.00636.904339.8107AID883
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency1.12200.010039.53711,122.0200AID1479
gemininHomo sapiens (human)Potency1.25890.004611.374133.4983AID624297
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency79.43280.00419.962528.1838AID2675
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]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor 3Homo sapiens (human)EC50 (µMol)1,000.00001.66004.40677.9000AID536769
Glutamate receptor 4Homo sapiens (human)EC50 (µMol)1,000.00000.29002.87727.6000AID536769
[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)
Glutamate receptor 1Rattus norvegicus (Norway rat)EC2x (µMol)1,440.00001.60001.60001.6000AID92192
Glutamate receptor 1Rattus norvegicus (Norway rat)EC5X (µMol)3,000.00009.80009.80009.8000AID92196
Glutamate receptor 2Rattus norvegicus (Norway rat)EC2x (µMol)1,440.00001.60001.60001.6000AID92192
Glutamate receptor 2Rattus norvegicus (Norway rat)EC5X (µMol)3,000.00009.80009.80009.8000AID92196
Glutamate receptor 3Rattus norvegicus (Norway rat)EC2x (µMol)1,440.00001.60001.60001.6000AID92192
Glutamate receptor 3Rattus norvegicus (Norway rat)EC5X (µMol)3,000.00009.80009.80009.8000AID92196
Glutamate receptor 4Rattus norvegicus (Norway rat)EC2x (µMol)1,440.00001.60001.60001.6000AID92192
Glutamate receptor 4Rattus norvegicus (Norway rat)EC5X (µMol)3,000.00009.80009.80009.8000AID92196
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (28)

Processvia Protein(s)Taxonomy
cholesterol biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
response to toxic substanceLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol effluxLiver carboxylesterase 1Homo sapiens (human)
negative regulation of cholesterol storageLiver carboxylesterase 1Homo sapiens (human)
epithelial cell differentiationLiver carboxylesterase 1Homo sapiens (human)
cholesterol homeostasisLiver carboxylesterase 1Homo sapiens (human)
reverse cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
medium-chain fatty acid metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid biosynthetic processLiver carboxylesterase 1Homo sapiens (human)
cellular response to cholesterolLiver carboxylesterase 1Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusLiver carboxylesterase 1Homo sapiens (human)
cholesterol ester hydrolysis involved in cholesterol transportLiver carboxylesterase 1Homo sapiens (human)
positive regulation of cholesterol metabolic processLiver carboxylesterase 1Homo sapiens (human)
regulation of bile acid secretionLiver carboxylesterase 1Homo sapiens (human)
lipid catabolic processLiver carboxylesterase 1Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
calcium-mediated signalingGlutamate receptor 3Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 3Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 3Homo sapiens (human)
protein homotetramerizationGlutamate receptor 3Homo sapiens (human)
protein heterotetramerizationGlutamate receptor 3Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
long-term synaptic potentiationGlutamate receptor 3Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 3Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 3Homo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
monoatomic ion transmembrane transportGlutamate receptor 4Homo sapiens (human)
negative regulation of smooth muscle cell apoptotic processGlutamate receptor 4Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor 4Homo sapiens (human)
regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
modulation of chemical synaptic transmissionGlutamate receptor 4Homo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
sterol esterase activityLiver carboxylesterase 1Homo sapiens (human)
methylumbelliferyl-acetate deacetylase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylesterase activityLiver carboxylesterase 1Homo sapiens (human)
carboxylic ester hydrolase activityLiver carboxylesterase 1Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 3Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 3Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor 3Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 3Homo sapiens (human)
amyloid-beta bindingGlutamate receptor 4Homo sapiens (human)
glutamate-gated receptor activityGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor activityGlutamate receptor 4Homo sapiens (human)
ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
plasma membraneGlutamate receptor 1Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
cytoplasmLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulum lumenLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
cytosolLiver carboxylesterase 1Homo sapiens (human)
lipid dropletLiver carboxylesterase 1Homo sapiens (human)
endoplasmic reticulumLiver carboxylesterase 1Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic membraneGlutamate receptor 3Homo sapiens (human)
parallel fiber to Purkinje cell synapseGlutamate receptor 3Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 3Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 3Homo sapiens (human)
dendritic spineGlutamate receptor 3Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendriteGlutamate receptor 4Homo sapiens (human)
endocytic vesicle membraneGlutamate receptor 4Homo sapiens (human)
neuronal cell bodyGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
extracellular vesicleGlutamate receptor 4Homo sapiens (human)
AMPA glutamate receptor complexGlutamate receptor 4Homo sapiens (human)
postsynaptic density membraneGlutamate receptor 4Homo sapiens (human)
plasma membraneGlutamate receptor 4Homo sapiens (human)
dendritic spineGlutamate receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (114)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
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 SIRPĪ±-CD47 interaction inhibitors.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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 SIRPĪ±-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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 SIRPĪ±-CD47 interaction inhibitors.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID175394Effect on duration of the postsynaptic excitatory potentials induced by electric stimulation in rat hippocampal slices1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aci
AID477245Activity at recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of glutamate-induced current at 5 mM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477247Activity at recombinant GluA2A4 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of glutamate-induced current at 5 mM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477244Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of glutamate-induced current at 5 mM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID581111Inhibition of STAT3 in human HeLa cells after 24 hrs by luciferase reporter gene assay2010ACS medicinal chemistry letters, Dec-09, Volume: 1, Issue:9
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID125743Amnesia-reversal activity (AA) evaluated in ECS-induced amnesia model of mice at a dose of 100 mg/kg1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID125741Amnesia-reversal activity in ECS-induced amnesia model of mice at 1 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID92192Concentration of drug giving a 2-fold increase of the magnitude of the current induced by Ionotropic glutamate receptor AMPA (30 uM) and measured in Xenopus Oocytes expressing Rat Cortex AMPA Receptors1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aci
AID456232Activity at human recombinant CES1 expressed in baculovirus-infected Spodoptera frugiperda Sf21 cells assessed as substrate hydrolysis by fluorescence assay2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
In silico prediction of human carboxylesterase-1 (hCES1) metabolism combining docking analyses and MD simulations.
AID477246Activity at recombinant GluA2A4 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of glutamate-induced current at 5 mM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID92196concentration of drug giving a 5-fold increase of the magnitude of the current induced by Ionotropic glutamate receptor AMPA (30 uM) and measured in Xenopus Oocytes expressing Rat Cortex AMPA Receptors1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aci
AID459004Binding affinity to subsite B/B' and subsite C/C' in S1S2 domain of GluA2 receptor expressed in Escherichia coli by crystallography2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors.
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.
AID536774Agonist activity at rat AMPA receptor assessed as AMPA-induced calcium uptake2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Positive allosteric modulators of the Ī±-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
AID602704Positive allosteric modulation at AMPA receptor in Sprague-Dawley rat embryonic hippocampal neuron assessed as concentration required to double the steady-state current induced by glutamate by patch-clamp assay2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Benzoxazinones as potent positive allosteric AMPA receptor modulators: part I.
AID125744Amnesia-reversal activity in scopolamine-induced amnesia model of mice at 1 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID459001Binding affinity to subsite A in S1S2 domain of GluA2 receptor expressed in Escherichia coli by crystallography2010Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5
Piracetam defines a new binding site for allosteric modulators of alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors.
AID536769Inhibition of GluR3/4 expressed in Xenopus oocyte2010Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20
Positive allosteric modulators of the Ī±-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
AID125742Amnesia-reversal activity in ECS-induced amnesia model of mice at 10 mg/kg i.p.1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
Synthesis and amnesia-reversal activity of a series of 7- and 5-membered 3-acylamino lactams.
AID231900Ratio between the D50 value and the A50 value; not determined1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aci
AID169272Effect on amplitude of the postsynaptic excitatory potentials induced by electric stimulation in rat hippocampal slices; Not determined1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2, 4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic aci
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (226)

TimeframeStudies, This Drug (%)All Drugs %
pre-199030 (13.27)18.7374
1990's87 (38.50)18.2507
2000's65 (28.76)29.6817
2010's34 (15.04)24.3611
2020's10 (4.42)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 43.09

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

MetricThis Compound (vs All)
Research Demand Index43.09 (24.57)
Research Supply Index5.50 (2.92)
Research Growth Index4.71 (4.65)
Search Engine Demand Index130.39 (26.88)
Search Engine Supply Index3.91 (0.95)

This Compound (43.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (4.27%)5.53%
Reviews8 (3.42%)6.00%
Case Studies3 (1.28%)4.05%
Observational0 (0.00%)0.25%
Other213 (91.03%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]