Page last updated: 2024-12-09

4E2RCat

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 CID2287238
CHEMBL ID1546414
CHEBI ID189654

Synonyms (17)

Synonym
AKOS000414508
HMS2626I15
smr000298763
5-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-2-chlorobenzoic acid
MLS000690029 ,
5-[5-[(e)-(3-benzyl-4-oxo-2-sulfanylidene-1,3-thiazolidin-5-ylidene)methyl]furan-2-yl]-2-chlorobenzoic acid
CHEBI:189654
5-[5-[(e)-(3-benzyl-4-oxo-2-thioxo-thiazolidin-5-ylidene)methyl]-2-furyl]-2-chloro-benzoic acid
2-chloro-5-[5-[(e)-[4-oxo-3-(phenylmethyl)-2-sulfanylidene-5-thiazolidinylidene]methyl]-2-furanyl]benzoic acid
bdbm48803
5-[5-[(e)-(3-benzyl-4-keto-2-thioxo-thiazolidin-5-ylidene)methyl]-2-furyl]-2-chloro-benzoic acid
cid_2287238
2-chloranyl-5-[5-[(e)-[4-oxidanylidene-3-(phenylmethyl)-2-sulfanylidene-1,3-thiazolidin-5-ylidene]methyl]furan-2-yl]benzoic acid
STL428447
5-{5-[(e)-(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]furan-2-yl}-2-chlorobenzoic acid
CHEMBL1546414
AKOS040741006
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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 (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency25.11890.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency5.01190.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency19.90540.140911.194039.8107AID2451
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency47.71730.125919.1169125.8920AID2549; AID2708
LuciferasePhotinus pyralis (common eastern firefly)Potency23.93410.007215.758889.3584AID588342
WRNHomo sapiens (human)Potency50.11870.168331.2583100.0000AID651768
phosphopantetheinyl transferaseBacillus subtilisPotency50.11870.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency25.11890.031637.5844354.8130AID743255
Microtubule-associated protein tauHomo sapiens (human)Potency10.00000.180013.557439.8107AID1460
thioredoxin glutathione reductaseSchistosoma mansoniPotency25.11890.100022.9075100.0000AID485364
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency0.08910.011212.4002100.0000AID1030
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency39.81070.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency12.58930.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency56.23410.006026.168889.1251AID540317
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency70.79460.010039.53711,122.0200AID1469; AID1479
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency39.81070.794321.275750.1187AID624246
importin subunit beta-1 isoform 1Homo sapiens (human)Potency5.31775.804836.130665.1308AID540253; AID540263
DNA polymerase betaHomo sapiens (human)Potency15.84890.022421.010289.1251AID485314
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency0.94660.168316.404067.0158AID720504
snurportin-1Homo sapiens (human)Potency5.31775.804836.130665.1308AID540253; AID540263
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency28.18380.010323.856763.0957AID2662
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency3.01310.425612.059128.1838AID504891
tumor susceptibility gene 101 proteinHomo sapiens (human)Potency11.22020.129810.833132.6090AID493005
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency5.62345.804816.996225.9290AID540253
DNA polymerase eta isoform 1Homo sapiens (human)Potency18.42720.100028.9256213.3130AID588591; AID720502
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency43.89120.050127.073689.1251AID588590; AID720496
DNA polymerase kappa isoform 1Homo sapiens (human)Potency79.43280.031622.3146100.0000AID588579
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency18.35640.058010.694926.6086AID651812; AID651813
DNA dC->dU-editing enzyme APOBEC-3F isoform aHomo sapiens (human)Potency10.02940.025911.239831.6228AID602313; AID651814; AID651815
neuropeptide S receptor isoform AHomo sapiens (human)Potency10.00000.015812.3113615.5000AID1461
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency56.23413.981146.7448112.2020AID720708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mcl-1Homo sapiens (human)IC50 (µMol)1.57460.40007.134454.0000AID1417; AID1418
eukaryotic translation initiation factor 4 gamma 1 isoform 4Homo sapiens (human)IC50 (µMol)15.10001.150012.620025.6529AID855
eukaryotic translation initiation factor 4E isoform 1Mus musculus (house mouse)IC50 (µMol)15.10001.150012.620025.6529AID855
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)1.70000.00052.773925.1700AID1418
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)1.70000.00052.891925.1700AID1418
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)1.70000.00052.747825.1700AID1418
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)1.70000.00052.780225.1700AID1418
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)1.70000.00053.314249.5000AID1418
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1409614Overall antiviral activity against SARS-CoV-2 (isolate France/IDF0372/2020) in the Vero E6 cell line at 48 h based on three assays 1) detection of viral RNA by qRT-PCR (targeting the N-gene), 2) plaque assay using lysate 3 days after addition of compound 2020Nature, 07, Volume: 583, Issue:7816
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's3 (50.00)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.35

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.35 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.30 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.35)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]