Page last updated: 2024-11-11

4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide

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

Description

4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6603828
CHEMBL ID1097940
SCHEMBL ID1171583
MeSH IDM0281158

Synonyms (47)

Synonym
EU-0100800
2,6-difluoro-4-[2-(phenylsul??fonyl??amino)??ethyl??thio]??phenoxy??acet??amide, >=98% (hplc), solid
lopac-d-8941
NCGC00015379-01 ,
LOPAC0_000800
NCGC00094134-01
2,6-difluoro-4-[2-(phenylsulfonylamino)ethylthio]phenoxyacetamide
NCGC00094134-02
NCGC00015379-02
pepa
D 8941
2-[2,6-difluoro-4-({2-[(phenylsulfonyl)amino]ethyl}sulfanyl)phenoxy]acetamide
p99 ,
NCGC00015379-04
CHEMBL1097940
2-[4-[2-(benzenesulfonamido)ethylsulfanyl]-2,6-difluorophenoxy]acetamide
HMS3262O22
CCG-204884
NCGC00015379-03
141286-78-4
2,6-difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide
LP00800
SCHEMBL1171583
tox21_500800
CS-3633
NCGC00261485-01
2-[2,6-difluoro-4-[[2-[(phenylsulfonyl)amino]ethyl]thio]phenoxy]acetamide
DTXSID60424960
2-(2,6-difluoro-4-((2-((phenylsulfonyl)amino)ethyl)thio)phenoxy)acetamide
HY-12509
AKOS024457340
mfcd04974493
4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide
J-007478
SR-01000076010-1
sr-01000076010
4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluoropheno-xyacetamide
BCP16187
Q7118990
SDCCGSBI-0050777.P002
NCGC00015379-09
A910880
MS-26854
8s4pr7a8js ,
pepa (drug)
unii-8s4pr7a8js
acetamide, 2-[2,6-difluoro-4-[[2-[(phenylsulfonyl)amino]ethyl]thio]phenoxy]-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Dose-response analysis for GluRCflop revealed that 100 microM PEPA produced a sevenfold increase in AMPA receptor affinity for glutamate."( A novel allosteric potentiator of AMPA receptors: 4--2-(phenylsulfonylamino)ethylthio--2,6-difluoro-phenoxyaceta mide.
Chiba, Y; Fleck, MW; Mayer, ML; Sekiguchi, M; Takeo, J; Wada, K; Yamashita, S, 1997
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (32)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID886
endonuclease IVEscherichia coliPotency0.50120.707912.432431.6228AID1708
thioredoxin reductaseRattus norvegicus (Norway rat)Potency10.62130.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency3.54810.02827.055915.8489AID895; AID928
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.38720.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency25.11890.00137.762544.6684AID914; AID915
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency12.58930.28189.721235.4813AID2326
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.71010.001530.607315,848.9004AID1224819; AID1224820
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency11.22020.035520.977089.1251AID504332
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency95.283423.934123.934123.9341AID1967
cytochrome P450 2C9 precursorHomo sapiens (human)Potency31.62280.00636.904339.8107AID883
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency12.58930.031610.279239.8107AID884; AID885
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency6.38360.00106.000935.4813AID943; AID944
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.62280.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency12.58931.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency13.45910.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID477547Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477563Activity at rat recombinant GluA2A3 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477565Activity at rat recombinant GluA2A4 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477552Activity at recombinant GluA2A3 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477555Activity at recombinant GluA2 receptor flop/GluA3 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477259Activity at rat recombinant GluA3 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477256Activity at rat recombinant GluA1 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477564Activity at rat recombinant GluA2A4 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477257Activity at rat recombinant GluA1 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477258Activity at rat recombinant GluA3 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477562Activity at rat recombinant GluA2A3 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477261Activity at rat recombinant GluA4 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477111Activity at rat recombinant GluA1A2 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477551Activity at recombinant GluA1A2 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477554Activity at recombinant GluA1 receptor flop/GluA2 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477561Activity at rat recombinant GluA1A2 receptor flop isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477260Activity at rat recombinant GluA4 receptor flip isoform expressed in HEK293 cells assessed as potentiation of 3000 uM glutamate-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477556Activity at recombinant GluA2 receptor flip/GluA3 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477548Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477553Activity at recombinant GluA1 receptor flip/GluA2 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
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.
AID477549Activity at recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
AID477550Activity at recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes assessed as potentiation of 10 uM AMPA-induced current at 100 uM relative to control2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Developing a complete pharmacology for AMPA receptors: a perspective on subtype-selective ligands.
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 SIRPα-CD47 interaction inhibitors.
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.
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.
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.
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.
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.
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 SIRPα-CD47 interaction 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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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 SIRPα-CD47 interaction 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.
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.
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 (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (11.11)18.2507
2000's8 (29.63)29.6817
2010's9 (33.33)24.3611
2020's7 (25.93)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.52

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 Index11.52 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.89 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.52)

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%
Other28 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]