Page last updated: 2024-11-12

zj43

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

Description

ZJ43: N-acetylaspartylglutamate (NAAG) peptidase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11722553
CHEMBL ID596351
SCHEMBL ID17241614
MeSH IDM0466677

Synonyms (18)

Synonym
CHEMBL596351 ,
2-(3-((s)-1-carboxy-3-methylbutyl)ureido)pentanedioic acid
bdbm50304738
723331-20-2
zj 43
n-[[[(1s)-1-carboxy-3-methylbutyl]amino]carbonyl]-l-glutamic acid
AKOS024457234
SCHEMBL17241614
(2s)-2-[[(1s)-1-carboxy-3-methylbutyl]carbamoylamino]pentanedioic acid
DTXSID60471136
zj43
(2~{s})-2-[[(2~{s})-4-methyl-1-oxidanyl-1-oxidanylidene-pentan-2-yl]carbamoylamino]pentanedioic acid
d6e ,
cid 11722553
YDB33120
HY-103344
CS-0027693
PD070405

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Treatment with ZJ43 or 2-PMPA prior to acquisition trials increased long-term memory in mGluR2, but not mGluR3, ko mice."( NAAG Peptidase Inhibitors Act via mGluR3: Animal Models of Memory, Alzheimer's, and Ethanol Intoxication.
Balasubramanian, S; Bzdega, T; Craddock, KE; Der, EK; Hark, TJ; Janczura, KJ; Moussa, C; Neale, JH; O'Rourke, B; Olszewski, RT; Venzor, F, 2017
)
0.79
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate carboxypeptidase 2Homo sapiens (human)IC50 (µMol)0.00570.00030.83169.5000AID1515290; AID1861414
Glutamate carboxypeptidase 2Homo sapiens (human)Ki0.00080.00020.00460.0312AID1226540; AID454505; AID636712
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
proteolysisGlutamate carboxypeptidase 2Homo sapiens (human)
folic acid-containing compound metabolic processGlutamate carboxypeptidase 2Homo sapiens (human)
C-terminal protein deglutamylationGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
metallocarboxypeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
peptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
dipeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
metal ion bindingGlutamate carboxypeptidase 2Homo sapiens (human)
Ac-Asp-Glu bindingGlutamate carboxypeptidase 2Homo sapiens (human)
tetrahydrofolyl-poly(glutamate) polymer bindingGlutamate carboxypeptidase 2Homo sapiens (human)
carboxypeptidase activityGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
cytoplasmGlutamate carboxypeptidase 2Homo sapiens (human)
plasma membraneGlutamate carboxypeptidase 2Homo sapiens (human)
cell surfaceGlutamate carboxypeptidase 2Homo sapiens (human)
membraneGlutamate carboxypeptidase 2Homo sapiens (human)
extracellular exosomeGlutamate carboxypeptidase 2Homo sapiens (human)
plasma membraneGlutamate carboxypeptidase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID1226542Selectivity ratio, ratio of Ki for antiTEV-tagged GCP3 extracellular portion (aa 36-740) (unknown origin) to Ki for antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin)2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID1226540Inhibition of antiTEV-tagged GCP2 extracellular portion (aa 44-750) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID1515290Inhibition of N-terminally tagged human recombinant GCP2 (44 to 750 residues) extracellular domain expressed in Drosophila melanogaster S2 cells preincubated for 20 mins followed by [3H]-NAAG addition and measured after 20 mins by liquid scintillation cou2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Structural and computational basis for potent inhibition of glutamate carboxypeptidase II by carbamate-based inhibitors.
AID454505Inhibition of human cloned glutamate carboxypeptidase 22010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies.
AID1226541Inhibition of antiTEV-tagged GCP3 extracellular portion (aa 36-740) (unknown origin) using folyl-di-L-glutamate as substrate by HPLC-based enzymatic assay2015Journal of medicinal chemistry, May-28, Volume: 58, Issue:10
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
AID636712Inhibition of glutamate carboxypeptidase 2 in human LNCAP cells assessed as glutamate formation using NAAG as substrate after 60 mins by fluorometric analysis2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Novel substrate-based inhibitors of human glutamate carboxypeptidase II with enhanced lipophilicity.
AID1861414Inhibition of PSMA in human LNCaP cell extracts using NAAG as substrate by amplex red reagent based assay2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (35.00)29.6817
2010's12 (60.00)24.3611
2020's1 (5.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.11

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 Index22.11 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]