Page last updated: 2024-12-08

esi-05

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

Description

ESI-05: an Epac inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID272513
CHEMBL ID2313653
SCHEMBL ID9001218
MeSH IDM000595232

Synonyms (29)

Synonym
nsc116966
nsc-116966
5184-64-5
2,4,4',6-tetramethyldiphenylsulfone
1,3,5-trimethyl-2-(p-tolylsulfonyl)benzene
SR-01000644199-1
1,3,5-trimethyl-2-(4-methylphenyl)sulfonylbenzene
AKOS024338261
CCG-55157
CHEMBL2313653 ,
bdbm50425555
SCHEMBL9001218
esi-05
DTXSID00297630
CGPHOZWFSFNOEQ-UHFFFAOYSA-N
1,3,5-trimethyl-2-(toluene-4-sulfonyl)-benzene
mesityl p-tolyl sulfone
1,3,5-trimethyl-2-[(4-methylphenyl)sulfonyl]benzene
esi 05
esi-05, >=98% (hplc)
HY-117656
E76526
mesityl (4-methylphenyl) sulfone
nsc 116966
CS-0066755
MS-23902
1,3,5-trimethyl-2-tosylbenzene
nsc 116966nsc 116966
1,3,5-trimethyl-2-(4-methylbenzenesulfonyl)benzene
[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)
Rap guanine nucleotide exchange factor 4Homo sapiens (human)IC50 (µMol)0.45000.40000.45000.5000AID1138159; AID723507
[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 (9)

Assay IDTitleYearJournalArticle
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).
AID723504Inhibition of PKA1 (unknown origin) assessed as inhibition of cAMP-induced activation at 25 uM by spectrophotometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID723503Inhibition of PKA2 (unknown origin) assessed as inhibition of cAMP-induced activation at 25 uM by spectrophotometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID723505Inhibition of recombinant EPAC1 (unknown origin) assessed as inhibition of cAMP-mediated RAP1-GDP exchange activity at 25 uM by spectrofluorometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID723507Antagonist activity at recombinant EPAC2 (unknown origin) assessed 8-NBD-cAMP substrate fluorescence intensity by substrate competing assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID723506Inhibition of recombinant EPAC2 (unknown origin) assessed as inhibition of cAMP-mediated guanine nucleotide exchange factor activity at 25 uM by spectrofluorometric analysis2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID723508Ratio of cAMP IC50 to compound IC50 for recombinant EPAC2 (unknown origin)2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Identification and characterization of small molecules as potent and specific EPAC2 antagonists.
AID1138159Inhibition of EPAC2 (unknown origin)2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Recent advances in the discovery of small molecules targeting exchange proteins directly activated by cAMP (EPAC).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's11 (91.67)24.3611
2020's1 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 31.66

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 Index31.66 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index71.90 (26.88)
Search Engine Supply Index3.88 (0.95)

This Compound (31.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]