Page last updated: 2024-11-13

sr9009

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 CID57394020
CHEMBL ID1961796
MeSH IDM0574047

Synonyms (40)

Synonym
bdbm50366238
CHEMBL1961796 ,
sr9009 ,
S8692
CS-4669
1379686-30-2
ethyl 3-[[(4-chlorophenyl)methyl-[(5-nitrothiophen-2-yl)methyl]amino]methyl]pyrrolidine-1-carboxylate
HY-16989
AC-30219
sr-9009
sr 9009 [who-dd]
gtpl8901
1-pyrrolidinecarboxylic acid, 3-((((4-chlorophenyl)methyl)((5-nitro-2-thienyl)methyl)amino)methyl)-, ethyl ester
unii-x5dca09n30
sr 9009
x5dca09n30 ,
n'-[(1e)-1-(5-chloro-2-hydroxyphenyl)ethylidene]-3-(4-morpholinylsulfonyl)benzohydrazide
J-690150
EX-A726
ethyl 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-1-pyrrolidinecarboxylate
AKOS027470307
1-pyrrolidinecarboxylic acid, 3-[[[(4-chlorophenyl)methyl][(5-nitro-2-thienyl)methyl]amino]methyl]-, ethyl ester
mfcd29472236
NCGC00384202-01
stenabolic (sr9009)
BCP16215
DB14013
ethyl 3-(4-chlorobenzyl)((5-nitrothiophen-2-yl)methylaminomethyl)pyrrolidine-1-carboxylate
rev-erb agonist ii
stenabolic
Q15410184
ethyl 3-[[(4-chlorophenyl)methyl-[(5-nitro-2-thienyl)methyl]amino]methyl]pyrrolidine-1-carboxylate
SB19006
nsc810521
nsc-810521
CCG-269102
AS-55859
A886340
ethyl 3-(((4-chlorobenzyl)((5-nitrothiophen-2-yl)methyl)amino)methyl)pyrrolidine-1-carboxylate
DTXSID901045515

Research Excerpts

Treatment

SR9009 treatment significantly decreased the mRNA level of Pck1 in mouse hepatoma Hepa-1c1c7 cells. Treatment with SR9009 down-regulated the degree of myocardial injury and ferritinophagy/ferroptosis-related proteins expression.

ExcerptReferenceRelevance
"SR9009 treatment markedly inhibited prostate cancer subtype 1 (PCS1), the most lethal and aggressive PCa subtype, through FOXM1 pathway blockade, while it had no impacts on PCS2 and PCS3."( SR9009 inhibits lethal prostate cancer subtype 1 by regulating the LXRα/FOXM1 pathway independently of REV-ERBs.
Ai, J; Li, H; Liao, D; Tan, P; Wang, Y; Wei, Q; Xiong, X; Xu, H; Yang, L; Yang, Y; Yi, X; Zhang, J; Zheng, X, 2022
)
2.89
"SR9009 treatment significantly decreased the mRNA level of Pck1 in mouse hepatoma Hepa-1c1c7 cells, whereas other major enzymes involved in gluconeogenesis (pyruvate carboxylase, glucose-6-phosphatase, fructose bisphosphatase and Pck2) and in glycolysis (phosphofructokinase and hexokinase-1) were unaffected."( Rev-erbα activation down-regulates hepatic Pck1 enzyme to lower plasma glucose in mice.
Dong, D; Li, Z; Wu, B; Yuan, X, 2019
)
1.24
"SR9009 treatment reduced amyloid-β 1-40 and 1-42 levels in the cortex, which is consistent with improved cognitive function."( Pharmacological activation of the nuclear receptor REV-ERB reverses cognitive deficits and reduces amyloid-β burden in a mouse model of Alzheimer's disease.
Burris, TP; Farr, SA; Kermath, BA; Morley, JE; Musiek, ES; Niehoff, M; Roby, DA; Ruiz, F; Voorhees, JR; Zhang, J, 2019
)
1.24
"Treatment with SR9009 down-regulated the degree of myocardial injury and ferritinophagy/ferroptosis-related proteins expression compared to diabetic rats treated with or without Erastin."( Rev-erbs agonist SR9009 alleviates ischemia-reperfusion injury by heightening endogenous cardioprotection at onset of type-2 diabetes in rats: Down-regulating ferritinophagy/ferroptosis signaling.
Huang, Q; Lei, S; Qiu, Z; Tian, L; Xia, ZY; Zhao, B; Zhao, X, 2022
)
1.4
"Treatment with SR9009 also blocked tumor necrosis factor-induced IL-1β mRNA, IL-6 mRNA and MMP-9 mRNA."( Stimulation of nuclear receptor REV-ERBs suppresses production of pronociceptive molecules in cultured spinal astrocytes and ameliorates mechanical hypersensitivity of inflammatory and neuropathic pain of mice.
Hisaoka-Nakashima, K; Kodama, K; Morioka, N; Nakamura, Y; Nakata, Y; Saeki, M; Tomori, M; Yoshikawa, K; Zhang, FF, 2019
)
0.85

Bioavailability

ExcerptReferenceRelevance
" Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing."( Optimized chemical probes for REV-ERBα.
Blaikley, J; Boudjelal, M; Bresciani, S; Cooper, AW; Dawson, HC; Farrow, SN; Grant, D; Kashatus, JA; Loudon, A; Orband-Miller, LA; Ray, D; Tellam, JP; Tomkinson, NC; Trump, RP; Willson, TM; Wojno, J, 2013
)
0.39
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Long term dosing with SR9009 also suppresses orexinergic gene expression in mice.

ExcerptRelevanceReference
" Long term dosing with SR9009 also suppresses orexinergic gene expression in mice."( Pharmacological and Genetic Modulation of REV-ERB Activity and Expression Affects Orexigenic Gene Expression.
Amador, A; Banerjee, S; Burris, TP; Kameneka, TM; Solt, LA; Wang, Y, 2016
)
0.74
" In these studies, our aim was to further investigate the therapeutic potential of targeting the REV-ERBs for regulation of sleep by characterizing efficacy, and optimal dosing time of the REV-ERB agonist SR9009 using electroencephalographic (EEG) recordings."( Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation.
Amador, A; Burris, TP; Huitron-Resendiz, S; Kamenecka, TM; Roberts, AJ; Solt, LA, 2016
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency4.25340.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.01120.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency4.25340.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.25340.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.25340.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.25340.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)IC50 (µMol)0.68330.62000.69200.7900AID651466; AID651468; AID671970
Oxysterols receptor LXR-alphaHomo sapiens (human)IC50 (µMol)6.30000.00901.06049.9000AID747988
Nuclear receptor subfamily 1 group D member 2Homo sapiens (human)IC50 (µMol)0.80000.56000.68000.8000AID651467
[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)
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)EC50 (µMol)17.10670.40001.14442.3000AID1722006; AID671968; AID747991
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)Kd0.80000.80000.80000.8000AID651469
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (107)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
negative regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
hormone-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of triglyceride biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol effluxOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cholesterol storageOxysterols receptor LXR-alphaHomo sapiens (human)
intracellular receptor signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of lipid transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of cholesterol transportOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transporter activityOxysterols receptor LXR-alphaHomo sapiens (human)
response to progesteroneOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of toll-like receptor 4 signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
phosphatidylcholine acyl-chain remodelingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
regulation of circadian rhythmOxysterols receptor LXR-alphaHomo sapiens (human)
mRNA transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of macrophage activationOxysterols receptor LXR-alphaHomo sapiens (human)
apoptotic cell clearanceOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of fatty acid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of proteolysisOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipid biosynthetic processOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pinocytosisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of inflammatory responseOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of lipoprotein lipase activityOxysterols receptor LXR-alphaHomo sapiens (human)
positive regulation of protein metabolic processOxysterols receptor LXR-alphaHomo sapiens (human)
lipid homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
sterol homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayOxysterols receptor LXR-alphaHomo sapiens (human)
triglyceride homeostasisOxysterols receptor LXR-alphaHomo sapiens (human)
cellular response to lipopolysaccharideOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of pancreatic juice secretionOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of secretion of lysosomal enzymesOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of cold-induced thermogenesisOxysterols receptor LXR-alphaHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressOxysterols receptor LXR-alphaHomo sapiens (human)
cell differentiationOxysterols receptor LXR-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
regulation of lipid metabolic processNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
regulation of circadian rhythmNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
circadian behaviorNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
regulation of inflammatory responseNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
negative regulation of inflammatory responseNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
lipid homeostasisNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
energy homeostasisNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
regulation of skeletal muscle cell differentiationNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group D member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group D member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
hormone-mediated signaling pathwayNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
transcription cis-regulatory region bindingOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificOxysterols receptor LXR-alphaHomo sapiens (human)
DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
nuclear receptor activityOxysterols receptor LXR-alphaHomo sapiens (human)
protein bindingOxysterols receptor LXR-alphaHomo sapiens (human)
zinc ion bindingOxysterols receptor LXR-alphaHomo sapiens (human)
cholesterol bindingOxysterols receptor LXR-alphaHomo sapiens (human)
chromatin DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
sterol response element bindingOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
nucleoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytoplasmOxysterols receptor LXR-alphaHomo sapiens (human)
cytosolOxysterols receptor LXR-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexOxysterols receptor LXR-alphaHomo sapiens (human)
chromatinOxysterols receptor LXR-alphaHomo sapiens (human)
receptor complexOxysterols receptor LXR-alphaHomo sapiens (human)
nucleusOxysterols receptor LXR-alphaHomo sapiens (human)
nucleusNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
cytoplasmNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group D member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (93)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651487Change in plasma triglycerides in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651535Effect on SF1(NR5A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651492Change in plasma leptin in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651516Effect on TR2(NR2C1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID1722006Agonist activity at Rev-Erb alpha (unknown origin) by FRET assay2020Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17
The transcriptional repressor REV-ERB as a novel target for disease.
AID651523Effect on ESR1(NR3A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651512Effect on HNF4G(NR2A2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651477Plasma concentration after 2 hours at 100mg/kg ip dose (10mg/ml solution in 15% Cremophor)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651526Effect on ERR2(NR3B2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651521Effect on TFCOUP2(NR2F2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651482Decreased expression of REV-ERB responsive gene Srebf1 in mouse liver after 6 days at 100 mg/kg2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671973Plasma concentration in C57BL/6 mouse at 50 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651539Effect on GCNF(NR6A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651489Change in plasma NEFA (non-esterified fatty acids) in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651524Effect on ESR2(NR3A2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651491Change in plasma insulin in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651536Effect on CPF(NR5A2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651498Effect on RARG(NR1B3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747988Binding affinity to LXRalpha (unknown origin) by radioligand displacement assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651500Effect on PPARD(NR1C2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651466Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651514Effect on RXRB(NR2B2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651504Effect on RORG(NR1F3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651508Effect on VDR(NR1I1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651509Effect on PXR(NR1I2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651518Effect on TLX(NR2E1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651483Decreased expression of REV-ERB responsive gene Serpine1 in mouse liver after 6 days at 100 mg/kg2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651531Effect on AR(NR3C4) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671976Ratio of drug uptake in brain to plasma of C57BL/6 mouse at 50 mg/kg, ip relative to control2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651470Recruitment of co-repressor NcoR1 to REV-ERB-alpha2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651499Effect on PPARA(NR1C1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671970Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing Gal4 ligand binding domain assessed as inhibition of transcription after 24 hrs by dual-Glo luciferase assay2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651515Effect on RXRG(NR2B3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651511Effect on HNF4A(NR2A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651530Effect on PGR(NR3C3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651488Change in total plasma cholesterol in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747989Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as biotinylated PGC1-beta peptide recruitment after 20 mins by Greiner assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651525Effect on ERR1(NR3B1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651472Plasma concentration after 2 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651513Effect on RXRA(NR2B1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651495Effect on THRB(NR1A2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651471Plasma concentration after 1 hour at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651519Effect on PNR(NR2E3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651490Change in plasma glucose in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671975Ratio of drug uptake in brain to plasma of C57BL/6 mouse at 10 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis relative to control2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651532Effect on GFRP1(NR4A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651494Effect on THRA(NR1A1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651467Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651475Brain concentration after 8 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651474Plasma concentration after 8 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651527Effect on ERR3(NR3B3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651522Effect on EAR2(NR2F6) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671971Plasma concentration in C57BL/6 mouse at 10 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID671968Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651473Plasma concentration after 4 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651517Effect on TR4(NR2C2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651496Effect on RARA(NR1B1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747984Agonist activity at REV-ERBalpha in human U2OS cells assessed as suppression of BMAL1 expression at 20 uM after 40 hrs by luciferase reporter gene assay relative to DMSO-treated control2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651507Effect on BAR(NR1H4) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651486Increased weight loss in diet-induced obese mice over 30 days at 100 mg/kg ip compared to vehicle control2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651478Plasma concentration after 8 hours at 100mg/kg ip dose (10mg/ml solution in 15% Cremophor)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651510Effect on CAR(NR1I3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671972Drug uptake in C57BL/6 mouse brain at 10 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651537Effect on DAX1(NR0B1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651481Decreased expression of REV-ERB responsive gene Cyp7a1 in mouse liver after 6 days at 100 mg/kg2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651493Change in plasma IL-6 in diet-induced obese mice over 30 days at 100 mg/kg ip2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651505Effect on LXRB(NR1H2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671969Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription at 10 uM after 24 hrs by dual-Glo luciferase assay relative to control2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651497Effect on RARB(NR1B2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651534Effect on NOR1(NR4A3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651506Effect on LXRA(NR1H3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651520Effect on TFCOUP1(NR2F1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651502Effect on RORA(NR1F1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747983Agonist activity at REV-ERBalpha in human U2OS cells assessed as delay of peak of second cycle at 20 uM by luciferase reporter gene assay relative to DMSO-treated control2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651468REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651503Effect on RORB(NR1F2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747991Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment after 1 hr by FRET assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651528Effect on GCR(NR3C1) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651469Dissociation constant for binding to REV-ERB-alpha by circular dichroism2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651538Effect on SHP(NR0B2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651501Effect on PPARG(NR1C3) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID747990Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment at 10 mM after 1 hr by FRET assay relative to control2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Optimized chemical probes for REV-ERBα.
AID651533Effect on NURR1(NR4A2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID671974Drug uptake in C57BL/6 mouse brain at 50 mg/kg, ip measured after 8 hrs by LC-MS/MS analysis2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.
AID651529Effect on MCR(NR3C2) dependent reporter activity in HEK293 cells at 20 uM2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID651476Brain concentration after 2 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID1346801Human Rev-Erb-alpha (1D. Rev-Erb receptors)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
AID1346747Human Rev-Erb-beta (1D. Rev-Erb receptors)2012Nature, Mar-29, Volume: 485, Issue:7396
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (64)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's27 (42.19)24.3611
2020's37 (57.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.81

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

MetricThis Compound (vs All)
Research Demand Index42.81 (24.57)
Research Supply Index4.19 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index123.78 (26.88)
Search Engine Supply Index3.91 (0.95)

This Compound (42.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (3.08%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other63 (96.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]