Page last updated: 2024-10-14

6,7-dichloro 3-(4-methylpiperazin-1-yl)quinoxalin-2(1h)-one

Description

6,7-dichloro 3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one: an NSAID; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11301441
CHEMBL ID260549
SCHEMBL ID602698
MeSH IDM0541879

Synonyms (9)

Synonym
6,7-dichloro-3-(4-methylpiperazin-1-yl)-1h-quinoxalin-2-one
CHEMBL260549 ,
vuf-10214
bdbm50361014
SCHEMBL602698
6,7-dichloro-3-(4-methylpiperazin-1-yl)quinoxalin-2(1 h)-one
848837-33-2
6,7-dichloro 3-(4-methylpiperazin-1-yl)quinoxalin-2(1h)-one
AKOS040746458
[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)
Histamine H4 receptorHomo sapiens (human)Ki0.00570.00060.478710.0000AID327691; AID408967; AID638337
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H4 receptorHomo sapiens (human)EC50 (µMol)0.02510.00740.601610.0000AID1573468
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (8)

Processvia Protein(s)Taxonomy
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID327691Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293T cells2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
AID408967Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.
AID638337Displacement of [3H]histamine from human H4 receptor expressed in HEK cell membranes2012Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
Ligand based design of novel histamine Hâ‚„ receptor antagonists; fragment optimization and analysis of binding kinetics.
AID327694Displacement of [3H]Nalpha-methyl-histamine from human histamine H3 receptor expressed in SK-NM-C cells at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
AID327693Displacement of [3H]aminopotentidine from human histamine H2 receptor expressed in COS7 cells at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
AID327692Displacement of [3H]mepyramine from human histamine H1 receptor expressed in NIH3T3 cells at 10 uM2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
AID1573468Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID1573469Agonist activity at histamine H4 receptor (unknown origin) expressed in human U2OS cells increase in beta-arrestin2 recruitment after 2 hrs by luminescence assay relative to control2018Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
AID327696Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, sc after 2 hrs2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
AID327698Antiinflammatory activity in Wistar rat assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, sc after 6 hrs2008Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8
Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (60.00)29.6817
2010's2 (40.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]