Page last updated: 2024-11-13

sr 8278

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

Description

SR 8278: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID53393127
CHEMBL ID4754504
SCHEMBL ID20488638
MeSH IDM0558017

Synonyms (25)

Synonym
sr8278
sr 8278
ethyl 2-{[5-(methylsulfanyl)thiophen-2-yl]carbonyl}-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
sr-8278
gtpl2904
1254944-66-5
1,2,3,4-tetrahydro-2-[[5-(methylthio)-2-thienyl]carbonyl]-3-isoquinolinecarboxylic acid ethyl ester
AKOS024458171
J-005234
DTXSID80693813
sr8278, >=98%, semisolid
ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate ,
SCHEMBL20488638
bdbm50560413
chembl4754504 ,
Q27088866
AS-16390
ethyl 2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1h-isoquinoline-3-carboxylate
CS-0003348
HY-14415
D80535
ethyl2-(5-methylsulfanylthiophene-2-carbonyl)-3,4-dihydro-1h-isoquinoline-3-carboxylate
A899051
EX-A4711
AC-36621

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" However, we had limited knowledge of the pharmacokinetic (PK) characteristics of SR8278."( A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats.
Dong, D; Li, Z; Sun, H; Wu, B; Wu, Z; Xue, Y, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
") injection at a dosage of 2mg/kg."( A validated ultra-performance liquid chromatography-tandem mass spectrometry method to identify the pharmacokinetics of SR8278 in normal and streptozotocin-induced diabetic rats.
Dong, D; Li, Z; Sun, H; Wu, B; Wu, Z; Xue, Y, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)EC50 (µMol)0.47000.40001.14442.3000AID1722008
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
cholesterol homeostasisNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group D member 1Homo sapiens (human)
intracellular glucose homeostasisNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
glycogen biosynthetic processNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
proteasomal protein catabolic processNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of lipid metabolic processNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
protein destabilizationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
circadian regulation of gene expressionNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of toll-like receptor 4 signaling pathwayNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cholesterol homeostasisNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of circadian sleep/wake cycleNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of circadian rhythmNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
steroid hormone mediated signaling pathwayNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
response to leptinNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of fat cell differentiationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of inflammatory responseNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
circadian temperature homeostasisNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of insulin secretion involved in cellular response to glucose stimulusNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
regulation of type B pancreatic cell proliferationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of astrocyte activationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
positive regulation of bile acid biosynthetic processNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cellular response to lipopolysaccharideNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cellular response to interleukin-1Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cellular response to tumor necrosis factorNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of neuroinflammatory responseNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
negative regulation of microglial cell activationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
hormone-mediated signaling pathwayNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
transcription corepressor bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
nuclear steroid receptor activityNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
heme bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
E-box bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleusNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
cytoplasmNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
dendriteNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
dendritic spineNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group D member 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1346801Human Rev-Erb-alpha (1D. Rev-Erb receptors)2011ACS chemical biology, Feb-18, Volume: 6, Issue:2
Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB.
AID1722008Antagonist activity at Rev-Erb alpha (unknown origin) by BMAL1-luciferase reporter assay2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
The transcriptional repressor REV-ERB as a novel target for disease.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

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 (50.00)24.3611
2020's9 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.76

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.76 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index4.70 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (5.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (94.44%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]