Page last updated: 2024-11-04

cycloleucine

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

Description

Cycloleucine, also known as 1-aminocyclopentanecarboxylic acid, is a cyclic amino acid that has garnered significant attention for its potential therapeutic applications. It exhibits a unique structural feature with a five-membered ring, distinguishing it from naturally occurring amino acids. Research into cycloleucine has primarily focused on its role in protein synthesis and its ability to modulate the activity of enzymes. Studies have demonstrated that cycloleucine can inhibit protein synthesis by interfering with the binding of tRNA to the ribosome. This inhibitory effect has prompted investigations into its potential as an anticancer agent, as uncontrolled protein synthesis is a hallmark of many cancer cells. Furthermore, cycloleucine has been found to inhibit the activity of certain enzymes, such as proteases and kinases, further expanding its therapeutic possibilities. The synthesis of cycloleucine often involves the cyclization of a linear amino acid precursor, utilizing various chemical reactions. Ongoing research aims to understand the precise mechanisms by which cycloleucine exerts its effects and to develop novel therapeutic strategies based on its unique properties.'

Cycloleucine: An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

1-aminocyclopentanecarboxylic acid : A non-proteinogenic alpha-amino acid that is cyclopentane substituted at position 1 by amino and carboxy groups. [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 CID2901
CHEMBL ID295830
CHEBI ID40547
SCHEMBL ID8495
MeSH IDM0005476

Synonyms (117)

Synonym
AC-2700
EN300-39470
DIVK1C_000723
KBIO1_000723
NCIMECH_000677
AC5 ,
SPECTRUM_001268
SPECTRUM5_001136
IDI1_000723
BIOMOL-NT_000201
BSPBIO_003187
NCGC00178218-01
einecs 200-144-6
wr 14,997
1-amino-cyclopentanecarboxylic acid
ai3-26442
hsdb 5195
brn 0636626
cyclopentanecarboxylic acid, 1-amino-, l-
1-aminocyclopentanecarboxylate
1-amino-1-cyclopentanecarboxylic acid
C03969
cyclopentanecarboxylic acid, 1-amino-
1-aminocyclopentane-1-carboxylic acid
cycloleucin
cycloleucine
nsc1026 ,
cb 1639
cyclopentanecarboxylic acid, l-amino
nsc-1026
wr 14997
wln: l5tj az avq
52-52-8
x 201
1-aminocyclopentanecarboxylic acid
cyclopentanecarboxylic acid, l-
nsc 1026
cycloleucine, 97%
1Y1M
DB04620
zinc00001234
cyclo-leucine
NCGC00094966-02
NCGC00094966-01
NCGC00163268-01
KBIOSS_001748
NCI60_000070
KBIO2_001748
KBIO2_004316
KBIO2_006884
KBIO3_002687
KBIOGR_000719
SPECTRUM2_000931
SPBIO_000862
NINDS_000723
SPECTRUM4_000340
SPECTRUM3_001514
SPECTRUM1502128
BPBIO1_001084
1-aminocyclopentane carboxylic acid
STK133034
leucine, cyclo-
3DD7E30B-2149-43D9-A44B-7A59D546A28B
A1063
AKOS000183252
CHEMBL295830 ,
chebi:40547 ,
cycloleucine1-amino-cyclopentanecarboxylic acid
HMS502E05
inchi=1/c6h11no2/c7-6(5(8)9)3-1-2-4-6/h1-4,7h2,(h,8,9)
nilqlfbwtxnuoe-uhfffaoysa-
HMS1921L08
bdbm50070638
NCGC00094966-04
NCGC00094966-03
AC1OCG3T ,
1-amino cyclopentane carboxylic acid
1-ammonio-1-cyclopentanecarboxylate
A829129 ,
CCG-35835
unii-0tqu7668ei
4-14-00-00974 (beilstein handbook reference)
0tqu7668ei ,
FT-0607341
AM20100281
FD1031
BBL020454
cb-1639
cycloleucin [who-dd]
cycloleucine [hsdb]
cycloleucine [mi]
CS-B0093
SCHEMBL8495
SY002601
mfcd00001381
J-504199
1-amino-1-carboxycyclopentane
1-amino-1-cyclopentane carboxylic acid
aminocyclopentanecarboxylic acid
1-amino-cyclopentane carboxylic acid
DTXSID5024475
J-802019
1-aminocyclopentane-1-carboxylate
(2e)-decenoyl-acp
acid, aminocyclopentanecarboxylic
acid, 1-aminocyclopentanecarboxylic
1 aminocyclopentanecarboxylic acid
1-amino-cyclopentanecarboxylate
cycloleucine1-amino-cyclopentanecarboxylate
1-amino-1-cyclopentanecarboxylate
F8881-4536
Q607775
AS-11677
h-nh(1)cpen-oh
1-aminocyclopentanecarboxylicacid
HY-30008
Z234896477

Research Excerpts

Overview

Cycloleucine is a synthetic amino acid. It produces, in vivo, biochemical abnoramlities comparable to those seen in human cystinuria-lysinuria.

ExcerptReferenceRelevance
"Cycloleucine is a synthetic amino acid which produces, in vivo, biochemical abnoramlities comparable to those seen in human cystinuria-lysinuria. "( Effect of cycloleucine on amino acid accumulation by human diploid fibroblasts.
Feneant, M; Gautier, M; Lemonnier, A; Lemonnier, F; Moatti, N, 1978
)
2.1

Actions

ExcerptReferenceRelevance
"Cycloleucine was used to inhibit the formation of internal N6-methyladenosine residues in the messenger ribonucleic acid transcripts from cultured methotrexate resistant mouse sarcoma cells. "( Inhibition of 6-methyladenine formation decreases the translation efficiency of dihydrofolate reductase transcripts.
Pan, T; Tuck, MT; Wiehl, PE, 1999
)
1.75

Treatment

ExcerptReferenceRelevance
"Cycloleucine treatment caused a 50% decline in SAM levels with both hepatocyte preparations and SAM levels were lowest in the pyrazole-treated hepatocytes."( A decrease in S-adenosyl-L-methionine potentiates arachidonic acid cytotoxicity in primary rat hepatocytes enriched in CYP2E1.
Zhuge, J, 2008
)
1.07

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
" In contrast, neither QA up to 5 mM nor trans-ACPD had a significant toxic effect in either KCl group."( NMDA and non-NMDA receptor-mediated excitotoxicity are potentiated in cultured striatal neurons by prior chronic depolarization.
Chen, Q; Reiner, A; Surmeier, DJ, 1999
)
0.3
"The potential toxic effects of the metabotropic glutamate receptor agonist (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid (ACPD) and its interactions with the N-methyl-D-aspartate (NMDA) receptor were studied in hippocampal brain slice cultures, using densitometric measurements of the cellular uptake of propidium iodide (PI) to quantify neuronal degeneration."( The metabotropic glutamate receptor agonist 1S,3R-ACPD stimulates and modulates NMDA receptor mediated excitotoxicity in organotypic hippocampal slice cultures.
Blaabjerg, M; Bonde, C; Kristensen, BW; Zimmer, J, 2001
)
0.31

Bioavailability

ExcerptReferenceRelevance
"To investigate the postnatal development of the carrier-mediated transport process by which certain amino acids are absorbed from the air space of the lung into the blood-stream, a solution of the 14C-labeled nonmetabolized amino acid cycloleucine was administered into the lungs of anesthetized rats of various ages and the rate of absorption of the compound measured."( Postnatal development of carrier-mediated absorption of a foreign amino acid from the rat lung.
Hemberger, JA; Schanker, LS, 1984
)
0.45
" The partial beneficial effects might also be explained by the age-related limited bioavailability of exogenous SAMe, a finding, to our knowledge, not yet reported elsewhere."( Biochemical analysis of myelin lipids and proteins in a model of methyl donor pathway deficit: effect of S-adenosylmethionine.
Bellasio, R; Bianchi, R; Calzi, F; Savaresi, S; Sciarretta-Birolo, R; Tacconi, MT; Tsankova, V, 1999
)
0.3
" Icofungipen shows nearly complete oral bioavailability in a variety of species, and its in vivo efficacy indicates its potential for the oral treatment of yeast infections."( In vitro activity and in vivo efficacy of icofungipen (PLD-118), a novel oral antifungal agent, against the pathogenic yeast Candida albicans.
Ergovic, G; Galic, T; Geschke, U; Hasenoehrl, A; Marsic, N; Mittendorf, J; Schmidt, A; Schoenfeld, W; Skerlev, M, 2006
)
0.33

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves for stimulation of phosphoinositide (PI) hydrolysis by the selective metabotropic glutamate receptor (mGluR) agonist, (1S,3R)-1-aminocyclopentane dicarboxylic acid [(1S,3R)-ACPD] were performed with cortical slices from mice treated with lorazepam or vehicle for 7 days and subject to 0, 1, 2, 3, 4 and 7 days of withdrawal."( The effect of lorazepam tolerance and withdrawal on metabotropic glutamate receptor function.
Mortensen, M; Suzdak, PD; Thomsen, C, 1995
)
0.29
" Both antagonists produced parallel shifts in agonist dose-response curves."( Pharmacological antagonism of the actions of group II and III mGluR agonists in the lateral perforant path of rat hippocampal slices.
Bushell, TJ; Collingridge, GL; Garthwaite, J; Jane, DE; Tse, HW; Watkins, JC, 1996
)
0.29
" CPPG produces rightward parallel shifts of the dose-response curves for both L-AP4- and (1S,3S)-ACPD, with Schild slope in each case close to unity, consistent with a competitive mechanism of antagonism."( Potent antagonists at the L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord.
Jane, DE; Thomas, NK; Tse, HW; Watkins, JC, 1996
)
0.29
" Guanylyl imidodiphosphate (Gpp(NH)p) causes an affinity shift on the L-glutamate dose-response curve, increasing the IC50 value."( Characterization of metabotropic glutamate receptors in rat C6 glioma cells.
Albasanz, JL; Martín, M; Ros, M, 1997
)
0.3
" The NMDA receptor antagonist D-AP5 reversed this effect, leaving the (1S,3R)-ACPD dose-response curve unchanged in naive animals."( mGluR activation reveals a tonic NMDA component in inflammatory hyperalgesia.
Berthele, A; Boxall, SJ; Tölle, TR; Urban, L; Zieglgänsberger, W, 1998
)
0.3
"Chronic dosing with the glycine partial NMDA agonist, 1-aminocyclopropanecarboxylic acid (ACPC) elicited an altered allosteric regulation of cortical NMDA receptor binding."( Chronic dosing with 1-aminocyclopropanecarboxylic acid, a glycine partial agonist, modulates NMDA inhibition of muscarinic-coupled PI hydrolysis in rat cortical slices.
Boje, KM; Lakhman, SS, 1998
)
0.3
" These mGluRs are functionally active on catecholamine (CA) secretion in chromaffin cells because both (1S, 3R)-1-aminocyclopentane-1,3-dicarboxylic acid (t-ACPD) and the specific agonist of Group I mGluRs, (S)-3,5-dihydroxyphenylglycine (DHPG), were able to stimulate the release of CAs (adrenaline and noradrenaline) in a dose-response manner."( Expression and functional properties of group I metabotropic glutamate receptors in bovine chromaffin cells.
Aránguez, I; Arce, C; Del Campo, AB; Figueroa, S; González, MP; López, E; Oset-Gasque, MJ, 2004
)
0.32
" PLD-118 demonstrated nonlinear plasma pharmacokinetics across the investigated dosage range, as was evident from a dose-dependent increase in plasma clearance and a dose-dependent decrease in the area under the plasma concentration-time curve."( Efficacy of PLD-118, a novel inhibitor of candida isoleucyl-tRNA synthetase, against experimental oropharyngeal and esophageal candidiasis caused by fluconazole-resistant C. albicans.
Bacher, J; Groll, AH; Kelaher, AM; Mickiene, D; Petraitiene, R; Petraitis, V; Sarafandi, AA; Sein, T; Walsh, TJ, 2004
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 2.5.1.6 (methionine adenosyltransferase) inhibitorAn EC 2.5.1.* (non-methyl-alkyl or aryl transferase) inhibitor that interferes with the action of methionine adenosyltransferase (EC 2.5.1.6).
[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 (1)

ClassDescription
non-proteinogenic alpha-amino acidAny alpha-amino acid which is not a member of the group of 23 proteinogenic amino acids.
[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 (5)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Glutamate [NMDA] receptor subunit zeta 1Rattus norvegicus (Norway rat)Ki15,300.00004.80005,378.600015,300.0000AID977610
Chain A, Glutamate [NMDA] receptor subunit zeta 1Rattus norvegicus (Norway rat)Ki15,300.00004.80005,378.600015,300.0000AID977610
Chain A, Glutamate [NMDA] receptor subunit zeta 1Rattus norvegicus (Norway rat)Ki15,300.00004.80005,378.600015,300.0000AID977610
S-adenosylmethionine synthase isoform type-1Rattus norvegicus (Norway rat)Ki516.00004.00004.00004.0000AID200227
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

Processvia Protein(s)Taxonomy
S-adenosylmethionine biosynthetic processS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
one-carbon metabolic processS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
protein hexamerizationS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
protein heterooligomerizationS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
cellular response to methionineS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
positive regulation of TORC1 signalingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
cellular response to leukemia inhibitory factorS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
methionine adenosyltransferase activityS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
protein bindingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
ATP bindingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
small molecule bindingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
identical protein bindingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
metal ion bindingS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
cytosolS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
methionine adenosyltransferase complexS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
cytosolS-adenosylmethionine synthase isoform type-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (32)

Assay IDTitleYearJournalArticle
AID1132881Antitrypanosomal activity against Trypanosoma cruzi infected in albino CF1 mouse assessed as reduction in number of parasites in blood at 52 mg/kg/day, intramuscular treatment started on day 10 of infection up to day 141977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
In search of anti-Trypanosoma cruzi drugs: new leads from a mouse model.
AID1145677Antibacterial activity against sensitive Pediococcus cerevisiae ATCC 808 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145688Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as active dose required to increase of 100% in mean survival time1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145678Antibacterial activity against chlorguanide triazine-resistant Pediococcus cerevisiae ATCC 808 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1885189Inhibition of MAT2A in human Huh-7 cells assessed as inhibition of S-adenosyl methionine production measured after 6 hrs by Rapid Fire Mass Spectrometry analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors.
AID430782Displacement of [3H]glycine from strychnine-insensitive glycine recognition site of NMDA receptor in rat brain cortex membrane2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Drug design, in vitro pharmacology, and structure-activity relationships of 3-acylamino-2-aminopropionic acid derivatives, a novel class of partial agonists at the glycine site on the N-methyl-D-aspartate (NMDA) receptor complex.
AID1885188Inhibition of MAT2A in human NCI-H520 cells transfected with MAT2A empty vector assessed as inhibition of S-adenosyl methionine production measured after 6 hrs by Rapid Fire Mass Spectrometry analysis2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors.
AID409960Inhibition of bovine brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID1149047Inhibition of growth of rat Jensen sarcoma cells assessed as new cells at 50 ug/ml after 72 hrs in presence of 25 ug/ml threonine and 26 ug/ml serine (Rvb = 100%)1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Racemic diastereoisomers of 1-amino-2-hydroxycyclopentanecarboxylic acid.
AID1149044Inhibition of growth of rat Jensen sarcoma cells assessed as new cells at 50 ug/ml after 72 hrs in presence of 26 ug/ml serine (Rvb = 100%)1976Journal of medicinal chemistry, Feb, Volume: 19, Issue:2
Racemic diastereoisomers of 1-amino-2-hydroxycyclopentanecarboxylic acid.
AID1145689Antimalarial activity against Plasmodium berghei infected in sc dosed mouse assessed as dose required to survivors for period of 60 days1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1885184Inhibition of rat liver MAT isozymes assessed as S-adenosyl methionine production using L-methionine as substrate in presence of ATP2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors.
AID1885185Inhibition of rat novikoff liver hepatoma MAT isozymes assessed as S-adenosyl methionine production using L-methionine as substrate in presence of ATP2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Overview of Methionine Adenosyltransferase 2A (MAT2A) as an Anticancer Target: Structure, Function, and Inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1145680Antibacterial activity against sensitive Escherichia coli ATCC 10536 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID409958Inhibition of bovine brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID200227Compound was evaluated for its inhibitory activity against recombinant S-adenosyl L-Methionine synthetase (alpha-isoform) in rat liver1998Bioorganic & medicinal chemistry letters, Jul-07, Volume: 8, Issue:13
A new series of cyclic amino acids as inhibitors of S-adenosyl L-methionine synthetase.
AID1145674Antibacterial activity against sensitive Lactobacillus casei ATCC 7469 assessed as reduction1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145675Antibacterial activity against chlorguanide triazine-resistant Lactobacillus casei ATCC 7469 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1132883Antitrypanosomal activity against Trypanosoma cruzi infected in albino CF1 mouse assessed as reduction in number of parasites in blood at 13 mg/kg/day, intramuscular treatment started on day 10 of infection up to day 141977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
In search of anti-Trypanosoma cruzi drugs: new leads from a mouse model.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID1132880Antitrypanosomal activity against Trypanosoma cruzi infected in albino CF1 mouse assessed as reduction in number of parasites in blood at 104 mg/kg/day, intramuscular treatment started on day 10 of infection up to day 141977Journal of medicinal chemistry, Jun, Volume: 20, Issue:6
In search of anti-Trypanosoma cruzi drugs: new leads from a mouse model.
AID1145671Antibacterial activity against sensitive Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID1145672Antibacterial activity against chlorguanide triazine-resistant Streptococcus faecium ATCC 8043 assessed as reduction in growth1977Journal of medicinal chemistry, Feb, Volume: 20, Issue:2
Antifolate studies. Activities of 40 potential antimalarial compounds against sensitive and chlorguanide triazine resistant strains of folate-requiring bacteria and Escherichia coli.
AID227699Virtual screen for compounds with anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1811Experimentally measured binding affinity data derived from PDB2005Neuron, Jul-07, Volume: 47, Issue:1
Mechanism of partial agonist action at the NR1 subunit of NMDA receptors.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2005Neuron, Jul-07, Volume: 47, Issue:1
Mechanism of partial agonist action at the NR1 subunit of NMDA receptors.
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 (1,209)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990203 (16.79)18.7374
1990's743 (61.46)18.2507
2000's200 (16.54)29.6817
2010's51 (4.22)24.3611
2020's12 (0.99)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.39

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 Index23.39 (24.57)
Research Supply Index7.13 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (0.32%)5.53%
Reviews18 (1.45%)6.00%
Case Studies1 (0.08%)4.05%
Observational0 (0.00%)0.25%
Other1,215 (98.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]