Page last updated: 2024-11-13

(2R)-4-(2,6-difluorophenyl)sulfonyl-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine

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 CID25243728
CHEMBL ID1092782
CHEBI ID92217
SCHEMBL ID2241559

Synonyms (9)

Synonym
NCGC00181800-01
smr001317730
MLS002264429
CHEMBL1092782
HMS2199D21
SCHEMBL2241559
CHEBI:92217
(2r)-4-(2,6-difluorophenyl)sulfonyl-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazine
Q27163986
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
sulfonamideAn amide of a sulfonic acid RS(=O)2NR'2.
[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 (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Smad3Homo sapiens (human)Potency15.84890.00527.809829.0929AID588855
pyruvate kinase PKLR isoform 1 [Homo sapiens]Homo sapiens (human)Potency22.10611.41251.41251.4125AID1543; AID1782
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency25.11893.548119.542744.6684AID743266
pyruvate kinase PKM isoform aHomo sapiens (human)Potency1.60140.04017.459031.6228AID1540; AID1751
pyruvate kinase PKLR isoform 2Homo sapiens (human)Potency19.78312.51194.65797.9433AID1541; AID1781
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Pyruvate kinase PKMHomo sapiens (human)AC503.10000.03802.25409.1800AID476343
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
programmed cell deathPyruvate kinase PKMHomo sapiens (human)
canonical glycolysisPyruvate kinase PKMHomo sapiens (human)
positive regulation of sprouting angiogenesisPyruvate kinase PKMHomo sapiens (human)
positive regulation of cytoplasmic translationPyruvate kinase PKMHomo sapiens (human)
glycolytic processPyruvate kinase PKMHomo sapiens (human)
cellular response to insulin stimulusPyruvate kinase PKMHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
magnesium ion bindingPyruvate kinase PKMHomo sapiens (human)
RNA bindingPyruvate kinase PKMHomo sapiens (human)
mRNA bindingPyruvate kinase PKMHomo sapiens (human)
protein tyrosine kinase activityPyruvate kinase PKMHomo sapiens (human)
pyruvate kinase activityPyruvate kinase PKMHomo sapiens (human)
protein bindingPyruvate kinase PKMHomo sapiens (human)
ATP bindingPyruvate kinase PKMHomo sapiens (human)
MHC class II protein complex bindingPyruvate kinase PKMHomo sapiens (human)
potassium ion bindingPyruvate kinase PKMHomo sapiens (human)
cadherin bindingPyruvate kinase PKMHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
extracellular regionPyruvate kinase PKMHomo sapiens (human)
nucleusPyruvate kinase PKMHomo sapiens (human)
cytoplasmPyruvate kinase PKMHomo sapiens (human)
mitochondrionPyruvate kinase PKMHomo sapiens (human)
rough endoplasmic reticulumPyruvate kinase PKMHomo sapiens (human)
cytosolPyruvate kinase PKMHomo sapiens (human)
ciliumPyruvate kinase PKMHomo sapiens (human)
vesiclePyruvate kinase PKMHomo sapiens (human)
secretory granule lumenPyruvate kinase PKMHomo sapiens (human)
collagen-containing extracellular matrixPyruvate kinase PKMHomo sapiens (human)
extracellular exosomePyruvate kinase PKMHomo sapiens (human)
extracellular vesiclePyruvate kinase PKMHomo sapiens (human)
ficolin-1-rich granule lumenPyruvate kinase PKMHomo sapiens (human)
cytoplasmPyruvate kinase PKMHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (22)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
AID476343Activation of PKM2 assessed as ATP product formation by luminescent pyruvate kinase-luciferase coupled assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476350Activation of PKM1 assessed as ATP product formation by luminescent pyruvate kinase-luciferase coupled assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476497Activation of PKL assessed as pyruvate formation by fluorescent pyruvate kinase-lactate dehydrogenase coupled assay relative to control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476346Activation of Leishmania mexicana PKM2 by quantitative high throughput screening assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476498Activation of PKL assessed as ATP product formation by luminescent pyruvate kinase-luciferase coupled assay relative to control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476349Activation of PKM1 assessed as pyruvate formation by fluorescent pyruvate kinase-lactate dehydrogenase coupled assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476344Activation of PKM2 assessed as ATP product formation at 57 uM by luminescent pyruvate kinase-luciferase coupled assay relative to fructose-1,6-bis-phosphate2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476495Activation of PKR assessed as pyruvate formation by fluorescent pyruvate kinase-lactate dehydrogenase coupled assay relative to control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
AID476496Activation of PKR assessed as ATP product formation by luminescent pyruvate kinase-luciferase coupled assay relative to control2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
[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's4 (66.67)24.3611
2020's1 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.41

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 Index12.41 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.41)

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]