Compounds > resatorvid
Page last updated: 2024-11-12

resatorvid

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 CID11703255
CHEMBL ID225157
SCHEMBL ID872197
MeSH IDM0575908

Synonyms (41)

Synonym
243984-11-4
HY-11109
tak-242
cli-095
resatorvid
tak 242
tak242
CHEMBL225157 ,
resatorvid [inn]
h2mz648c31 ,
unii-h2mz648c31
resatorvid (tak-242)
CS-0408
ethyl (6r)-6-((2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate
S7455
SCHEMBL872197
AC-31498
ethyl (6r)-6-[(2-chloro-4-fluorophenyl)sulfamoyl]cyclohexene-1-carboxylate
gtpl9036
mfcd11046362
AKOS027250774
bdbm50155929
tak-242 (resatorvid)
resatorvid; tak 242
ethyl (r)-6-(n-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate ,
ethyl (6r)-6-[n-(2-chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate
(r)-ethyl 6-(n-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
DB05943
Q27088534
AMY14748
tak-242; cli-095
(6r)-6-[[(2-chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid ethyl ester;tak-242
A904215
DTXSID00947269
AS-56190
EX-A3158
cli-095tak-242
nsc-839697
nsc839697
resatorvid; tak-242
(r)-ethyl6-(n-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-enecarboxylate
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Toll-like receptor 4Homo sapiens (human)IC50 (µMol)0.68000.00240.78061.4000AID1389561
Toll-like receptor 4 Mus musculus (house mouse)IC50 (µMol)0.00570.00570.56891.5400AID1286184
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (86)

Processvia Protein(s)Taxonomy
lipopolysaccharide-mediated signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of MAP kinase activityToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
lipopolysaccharide-mediated signaling pathwayToll-like receptor 4Homo sapiens (human)
response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
wound healing involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
B cell proliferation involved in immune responseToll-like receptor 4Homo sapiens (human)
nitric oxide production involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
regulation of dendritic cell cytokine productionToll-like receptor 4Homo sapiens (human)
MyD88-dependent toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
nitric oxide biosynthetic processToll-like receptor 4Homo sapiens (human)
phagocytosisToll-like receptor 4Homo sapiens (human)
immune responseToll-like receptor 4Homo sapiens (human)
I-kappaB phosphorylationToll-like receptor 4Homo sapiens (human)
JNK cascadeToll-like receptor 4Homo sapiens (human)
gene expressionToll-like receptor 4Homo sapiens (human)
positive regulation of platelet activationToll-like receptor 4Homo sapiens (human)
positive regulation of gene expressionToll-like receptor 4Homo sapiens (human)
astrocyte developmentToll-like receptor 4Homo sapiens (human)
microglia differentiationToll-like receptor 4Homo sapiens (human)
positive regulation of smooth muscle cell migrationToll-like receptor 4Homo sapiens (human)
detection of fungusToll-like receptor 4Homo sapiens (human)
positive regulation of B cell proliferationToll-like receptor 4Homo sapiens (human)
response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
detection of lipopolysaccharideToll-like receptor 4Homo sapiens (human)
negative regulation of type II interferon productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-17 productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-23 productionToll-like receptor 4Homo sapiens (human)
negative regulation of interleukin-6 productionToll-like receptor 4Homo sapiens (human)
negative regulation of tumor necrosis factor productionToll-like receptor 4Homo sapiens (human)
positive regulation of chemokine productionToll-like receptor 4Homo sapiens (human)
positive regulation of interferon-alpha productionToll-like receptor 4Homo sapiens (human)
positive regulation of interferon-beta productionToll-like receptor 4Homo sapiens (human)
positive regulation of type II interferon productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-1 beta productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-1 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-10 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-12 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-6 productionToll-like receptor 4Homo sapiens (human)
positive regulation of interleukin-8 productionToll-like receptor 4Homo sapiens (human)
positive regulation of tumor necrosis factor productionToll-like receptor 4Homo sapiens (human)
positive regulation of stress-activated MAPK cascadeToll-like receptor 4Homo sapiens (human)
toll-like receptor 4 signaling pathwayToll-like receptor 4Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayToll-like receptor 4Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusToll-like receptor 4Homo sapiens (human)
T-helper 1 type immune responseToll-like receptor 4Homo sapiens (human)
macrophage activationToll-like receptor 4Homo sapiens (human)
defense response to bacteriumToll-like receptor 4Homo sapiens (human)
positive regulation of macrophage activationToll-like receptor 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionToll-like receptor 4Homo sapiens (human)
innate immune responseToll-like receptor 4Homo sapiens (human)
MHC class II biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of MHC class II biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processToll-like receptor 4Homo sapiens (human)
negative regulation of osteoclast differentiationToll-like receptor 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIToll-like receptor 4Homo sapiens (human)
positive regulation of JNK cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of smooth muscle cell proliferationToll-like receptor 4Homo sapiens (human)
positive regulation of inflammatory responseToll-like receptor 4Homo sapiens (human)
defense response to Gram-negative bacteriumToll-like receptor 4Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activityToll-like receptor 4Homo sapiens (human)
stress-activated MAPK cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processToll-like receptor 4Homo sapiens (human)
intestinal epithelial structure maintenanceToll-like receptor 4Homo sapiens (human)
positive regulation of macrophage cytokine productionToll-like receptor 4Homo sapiens (human)
ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeToll-like receptor 4Homo sapiens (human)
nucleotide-binding oligomerization domain containing 1 signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of nucleotide-binding oligomerization domain containing 1 signaling pathwayToll-like receptor 4Homo sapiens (human)
nucleotide-binding oligomerization domain containing 2 signaling pathwayToll-like receptor 4Homo sapiens (human)
positive regulation of nucleotide-binding oligomerization domain containing 2 signaling pathwayToll-like receptor 4Homo sapiens (human)
cellular response to lipopolysaccharideToll-like receptor 4Homo sapiens (human)
cellular response to lipoteichoic acidToll-like receptor 4Homo sapiens (human)
cellular response to mechanical stimulusToll-like receptor 4Homo sapiens (human)
cellular response to type II interferonToll-like receptor 4Homo sapiens (human)
negative regulation of cold-induced thermogenesisToll-like receptor 4Homo sapiens (human)
cellular response to oxidised low-density lipoprotein particle stimulusToll-like receptor 4Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseToll-like receptor 4Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblyToll-like receptor 4Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionToll-like receptor 4Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic processToll-like receptor 4Homo sapiens (human)
positive regulation of cellular response to macrophage colony-stimulating factor stimulusToll-like receptor 4Homo sapiens (human)
positive regulation of matrix metallopeptidase secretionToll-like receptor 4Homo sapiens (human)
cellular response to amyloid-betaToll-like receptor 4Homo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 2 productionToll-like receptor 4Homo sapiens (human)
positive regulation of extrinsic apoptotic signaling pathwayToll-like receptor 4Homo sapiens (human)
inflammatory responseToll-like receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingToll-like receptor 4Homo sapiens (human)
amyloid-beta bindingToll-like receptor 4Homo sapiens (human)
lipopolysaccharide immune receptor activityToll-like receptor 4Homo sapiens (human)
transmembrane signaling receptor activityToll-like receptor 4Homo sapiens (human)
signaling receptor bindingToll-like receptor 4Homo sapiens (human)
protein bindingToll-like receptor 4Homo sapiens (human)
signaling receptor activityToll-like receptor 4Homo sapiens (human)
identical protein bindingToll-like receptor 4Homo sapiens (human)
protein heterodimerization activityToll-like receptor 4Homo sapiens (human)
NAD+ nucleotidase, cyclic ADP-ribose generatingToll-like receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
plasma membraneToll-like receptor 4Homo sapiens (human)
endosome membraneToll-like receptor 4Homo sapiens (human)
ruffleToll-like receptor 4Homo sapiens (human)
phagocytic cupToll-like receptor 4Homo sapiens (human)
cytoplasmToll-like receptor 4Homo sapiens (human)
early endosomeToll-like receptor 4Homo sapiens (human)
plasma membraneToll-like receptor 4Homo sapiens (human)
external side of plasma membraneToll-like receptor 4Homo sapiens (human)
cell surfaceToll-like receptor 4Homo sapiens (human)
endosome membraneToll-like receptor 4Homo sapiens (human)
receptor complexToll-like receptor 4Homo sapiens (human)
perinuclear region of cytoplasmToll-like receptor 4Homo sapiens (human)
lipopolysaccharide receptor complexToll-like receptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1389561Inhibition of human TLR4 signaling expressed in HEK-Blue cells co-expressing MD2/CD14 assessed as reduction in LPS-induced NF-kappaB activation-mediated SEAP production preincubated for 2 hrs followed by LPS stimulation for 20 hrs by colorimetric assay2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Development of benzoxazole deoxybenzoin oxime and acyloxylamine derivatives targeting innate immune sensors and xanthine oxidase for treatment of gout.
AID283020Suppression of serum TNF-alpha level in LPS-challenged BALB/c mouse endotoxin shock model at 0.1 to 3 mg/kg, iv2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID1286184Inhibition of TLR4 in LPS/INFgamma stimulated mouse peritoneal macrophages assessed as inhibition of IL1-beta after 20 hrs by ELISA analysis2016Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
Inhibiting the Inflammasome: A Chemical Perspective.
AID283021Suppression of serum IL6 level in LPS-challenged BALB/c mouse endotoxin shock model at 0.1 to 3 mg/kg, iv2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283017Inhibition of LPS-induced IL6 production in mouse RAW264.7 cells by ELISA2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283023Suppression of serum nitric oxide level in LPS-challenged BALB/c mouse endotoxin shock model at 0.1 to 3 mg/kg, iv2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283016Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells by ELISA2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID347531Antisepsis activity in LPS-induced ip dosed C57BL/6J mouse lethal endotoxin shock model assessed as survival after 4 days administered 30 before LPS challenge2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Glycolipids and benzylammonium lipids as novel antisepsis agents: synthesis and biological characterization.
AID283018Survival of LPS-challenged BALB/c mouse endotoxin shock model at 3 mg/kg, iv2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283022Suppression of serum IL1-beta level in LPS-challenged BALB/c mouse endotoxin shock model at 0.1 to 3 mg/kg, iv2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283015Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID283019Survival of LPS-challenged intravenously dosed BALB/c mouse endotoxin shock model2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Discovery of novel and potent small-molecule inhibitors of NO and cytokine production as antisepsis agents: synthesis and biological activity of alkyl 6-(N-substituted sulfamoyl)cyclohex-1-ene-1-carboxylate.
AID1345489Human TLR4 (Toll-like receptor family)2006Molecular pharmacology, Apr, Volume: 69, Issue:4
A novel cyclohexene derivative, ethyl (6R)-6-[N-(2-Chloro-4-fluorophenyl)sulfamoyl]cyclohex-1-ene-1-carboxylate (TAK-242), selectively inhibits toll-like receptor 4-mediated cytokine production through suppression of intracellular signaling.
[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]

Market Indicators

Research Demand Index: 31.76

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 Index31.76 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.42 (4.65)
Search Engine Demand Index35.06 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (31.76)

All Compounds (24.57)

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]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
glyburide
Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.		3.2310monochlorobenzenes;
N-sulfonylurea		anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent
probenecid
Probenecid: The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.. probenecid : A sulfonamide in which the nitrogen of 4-sulfamoylbenzoic acid is substituted with two propyl groups.		3.2310benzoic acids;
sulfonamide		uricosuric drug
colchicine
(S)-colchicine : A colchicine that has (S)-configuration. It is a secondary metabolite, has anti-inflammatory properties and is used to treat gout, crystal-induced joint inflammation, familial Mediterranean fever, and many other conditions.		2.1710alkaloid;
colchicine		anti-inflammatory agent;
gout suppressant;
mutagen
pralnacasan
pralnacasan: NSAID, ICE inhibitor & metastasis inhibitor; RN & structure in first source		3.2310
isoliquiritigenin
[no description available]		2.1710chalconesantineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist
3,4-methylenedioxy-beta-nitrostyrene
3,4-methylenedioxy-beta-nitrostyrene: tyrosine kinase inhibitor that prevents platelet glycoprotein IIb/IIIa activation; structure in first source		3.2310
mcc-950
[no description available]		3.2310
allopurinol
Allopurinol: A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.. allopurinol : A bicyclic structure comprising a pyrazole ring fused to a hydroxy-substituted pyrimidine ring.		2.1710nucleobase analogue;
organic heterobicyclic compound		antimetabolite;
EC 1.17.3.2 (xanthine oxidase) inhibitor;
gout suppressant;
radical scavenger
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Poisoning
[description not available]		02.4420
Sepsis
Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.		14.4420
Endotoxin Shock
[description not available]		02.0510
Shock, Septic
Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.		02.0510
Innate Inflammatory Response
[description not available]		03.0410
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		03.0410
Gout
Metabolic disorder characterized by recurrent acute arthritis, hyperuricemia and deposition of sodium urate in and around the joints, sometimes with formation of URIC ACID calculi.		02.1710