Compounds > ccg 50014
Page last updated: 2024-11-09

ccg 50014

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Description

4-(4-fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione: a regulator of G protein signaling (RGS) inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2733079
CHEMBL ID1917204
SCHEMBL ID13516928
MeSH IDM0558263

Synonyms (43)

Synonym
883050-24-6
ccg 50014
OPREA1_536155
SR-01000639423-1
MAYBRIDGE1_007327
HMS562F01
4-[(4-fluorophenyl)methyl]-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
bdbm50384774
CCG-50014 ,
CHEMBL1917204 ,
ra72g28ve9 ,
unii-ra72g28ve9
S2901
4-((4-fluorophenyl)methyl)-2-(4-methylphenyl)-1,2,4-thiadiazolidine-3,5-dione
l-2-401
1,2,4-thiadiazolidine-3,5-dione, 4-((4-fluorophenyl)methyl)-2-(4-methylphenyl)-
l 2-401
gtpl7784
ccg50014
4-[(4-fluorophenyl)methyl]-2-(p-tolyl)-1,2,4-thiadiazolidine-3,5-dione
SCHEMBL13516928
4-(4-fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
c16h13fn2o2s
cyto9f11
AKOS024458228
J-513165
DTXSID30236951
HMS3651D08
SW219386-1
BCP06015
HY-13509
BS-17774
Q27075771
BRD-K08893438-001-02-3
A16432
NCGC00386221-06
4-(4-fluorobenzyl)-2-(p-tolyl)-1,2,4-thiadiazolidine-3,5-dione
EC-000.2523
CS-0007131
D83132
mfcd00113783
SY264847
A916163
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Replicase polyprotein 1abBetacoronavirus England 1IC50 (µMol)10.00000.00403.43889.5100AID1640022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)0.19000.00022.45859.9600AID1640021
Regulator of G-protein signaling 4Homo sapiens (human)IC50 (µMol)0.03010.03010.03010.0301AID663946
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
response to amphetamineRegulator of G-protein signaling 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRegulator of G-protein signaling 4Homo sapiens (human)
regulation of G protein-coupled receptor signaling pathwayRegulator of G-protein signaling 4Homo sapiens (human)
positive regulation of heart rateRegulator of G-protein signaling 4Homo sapiens (human)
response to cocaineRegulator of G-protein signaling 4Homo sapiens (human)
response to ethanolRegulator of G-protein signaling 4Homo sapiens (human)
negative regulation of G protein-coupled receptor signaling pathwayRegulator of G-protein signaling 4Homo sapiens (human)
regulation of calcium ion transportRegulator of G-protein signaling 4Homo sapiens (human)
negative regulation of dopamine receptor signaling pathwayRegulator of G-protein signaling 4Homo sapiens (human)
negative regulation of cell growth involved in cardiac muscle cell developmentRegulator of G-protein signaling 4Homo sapiens (human)
regulation of actin filament organizationRegulator of G-protein signaling 4Homo sapiens (human)
negative regulation of glycine import across plasma membraneRegulator of G-protein signaling 4Homo sapiens (human)
negative regulation of potassium ion transmembrane transportRegulator of G-protein signaling 4Homo sapiens (human)
dorsal root ganglion developmentRegulator of G-protein signaling 4Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialRegulator of G-protein signaling 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRegulator of G-protein signaling 8Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayRegulator of G-protein signaling 8Homo sapiens (human)
negative regulation of signal transductionRegulator of G-protein signaling 8Homo sapiens (human)
positive regulation of GTPase activityRegulator of G-protein signaling 8Homo sapiens (human)
regulation of dopamine receptor signaling pathwayRegulator of G-protein signaling 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
G-protein alpha-subunit bindingRegulator of G-protein signaling 4Homo sapiens (human)
GTPase activityRegulator of G-protein signaling 4Homo sapiens (human)
GTPase activator activityRegulator of G-protein signaling 4Homo sapiens (human)
calmodulin bindingRegulator of G-protein signaling 4Homo sapiens (human)
protein kinase bindingRegulator of G-protein signaling 4Homo sapiens (human)
GTPase activityRegulator of G-protein signaling 8Homo sapiens (human)
GTPase activator activityRegulator of G-protein signaling 8Homo sapiens (human)
protein bindingRegulator of G-protein signaling 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
plasma membraneRegulator of G-protein signaling 4Homo sapiens (human)
nucleusRegulator of G-protein signaling 4Homo sapiens (human)
cytoplasmRegulator of G-protein signaling 4Homo sapiens (human)
protein-containing complexRegulator of G-protein signaling 4Homo sapiens (human)
nucleusRegulator of G-protein signaling 8Homo sapiens (human)
plasma membraneRegulator of G-protein signaling 8Homo sapiens (human)
cytoplasmic side of plasma membraneRegulator of G-protein signaling 8Homo sapiens (human)
dendriteRegulator of G-protein signaling 8Homo sapiens (human)
neuronal cell body membraneRegulator of G-protein signaling 8Homo sapiens (human)
perikaryonRegulator of G-protein signaling 8Homo sapiens (human)
synapseRegulator of G-protein signaling 8Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID663948Selectivity ratio of IC50 for RGS8 to IC50 RGS42012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID663946Inhibition of RGS4 interaction with Galpha0 protein by flow cytometry protein interaction assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID628067Selectivity for RGS4 over RGS162011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Regulators of G protein signaling (RGS) proteins as drug targets: modulating G-protein-coupled receptor (GPCR) signal transduction.
AID663947Inhibition of RGS8 interaction with Galpha0 protein by flow cytometry protein interaction assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID1377230Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as disruption of RGS17 localization at cell membranes at 100 uM up to 30 mins by confocal microscopic analysis2017Journal of natural products, 07-28, Volume: 80, Issue:7
Natural Products Discovered in a High-Throughput Screen Identified as Inhibitors of RGS17 and as Cytostatic and Cytotoxic Agents for Lung and Prostate Cancer Cell Lines.
AID1377227Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 100 uM up to 30 mins by confocal microscopic analysis2017Journal of natural products, 07-28, Volume: 80, Issue:7
Natural Products Discovered in a High-Throughput Screen Identified as Inhibitors of RGS17 and as Cytostatic and Cytotoxic Agents for Lung and Prostate Cancer Cell Lines.
AID628066Selectivity for RGS4 over RGS82011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Regulators of G protein signaling (RGS) proteins as drug targets: modulating G-protein-coupled receptor (GPCR) signal transduction.
AID663949Activity at human muscarinic M3 receptor expressed in HEK293T cells assessed as increase in carbachol-induced intracellular calcium level at 10 uM after 30 to 45 mins by fluorimetry2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID1377233Induction of morphological changes in HEK293 cells assessed as cell shrinkage at 100 uM measured over 30 mins2017Journal of natural products, 07-28, Volume: 80, Issue:7
Natural Products Discovered in a High-Throughput Screen Identified as Inhibitors of RGS17 and as Cytostatic and Cytotoxic Agents for Lung and Prostate Cancer Cell Lines.
AID1346213Human regulator of G-protein signaling 8 (R4 family)2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID1346237Human regulator of G-protein signaling 4 (R4 family)2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
AID1346213Human regulator of G-protein signaling 8 (R4 family)2011Biochemistry, Apr-19, Volume: 50, Issue:15
A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins.
AID1346237Human regulator of G-protein signaling 4 (R4 family)2011Biochemistry, Apr-19, Volume: 50, Issue:15
A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (90.00)24.3611
2020's1 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.29

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 Index17.29 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.29)

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%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		2.1110aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
sanguinarine
benzophenanthridine alkaloid : A specific group of isoquinoline alkaloids that occur only in higher plants and are constituents mainly of the Papaveraceae family.		2.1510alkaloid antibiotic;
benzophenanthridine alkaloid;
botanical anti-fungal agent
celastrol
[no description available]		2.1510monocarboxylic acid;
pentacyclic triterpenoid		anti-inflammatory drug;
antineoplastic agent;
antioxidant;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Hsp90 inhibitor;
metabolite
cysteine
Cysteine: A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.. L-cysteinium : The L-enantiomer of cysteinium.. cysteine : A sulfur-containing amino acid that is propanoic acid with an amino group at position 2 and a sulfanyl group at position 3.		2.7930cysteiniumfundamental metabolite
enkephalin, ala(2)-mephe(4)-gly(5)-
Enkephalin, Ala(2)-MePhe(4)-Gly(5)-: An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.		2.1110
gambogic acid
gambogic acid: RN given refers to (1R-(1alpha,1(Z),3abeta,5alpha,11beta,14aS*))-isomer		2.1510pyranoxanthonesmetabolite
ConditionIndicatedRelationship StrengthStudiesTrials
Plasmodium falciparum Malaria
[description not available]		02.110
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		02.110
Cancer of Lung
[description not available]		02.1510
Cancer of Prostate
[description not available]		02.1510
Lung Neoplasms
Tumors or cancer of the LUNG.		02.1510
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.1510
Nociceptive Pain
Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.		02.1110
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.1110