Compounds > sr9009
Page last updated: 2024-08-03 20:48:49

sr9009

Description

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

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.6837AID1645841
GVesicular stomatitis virusPotency4.2534AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency3.0112AID1645840
Interferon betaHomo sapiens (human)Potency4.2534AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.2534AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.2534AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.2534AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)IC500.6833AID651466; AID651468; AID671970
Oxysterols receptor LXR-alphaHomo sapiens (human)IC506.3000AID747988
Nuclear receptor subfamily 1 group D member 2Homo sapiens (human)IC500.8000AID651467

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)EC5017.1067AID1722006; AID671968; AID747991
Nuclear receptor subfamily 1 group D member 1Homo sapiens (human)Kd0.8000AID651469

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
ISSN: 1521-0111		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
ISSN: 1091-6490		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
ISSN: 1091-6490		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
ISSN: 2472-5560		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
ISSN: 1521-0111		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1520-4804		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
ISSN: 1476-4687		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
ISSN: 1464-3405		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		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
ISSN: 1476-4687		Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
gsk4112
4
201220209.8medium000040
sr 8278
1
202020204.0low000010
sr9011
3
201220209.0medium000030
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
acetylcarnitine
1
O-acylcarnitinehuman metabolite201520159.0low000010
glycine
1
alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical		201920195.0low000010
pilocarpine
1
pilocarpineantiglaucoma drug202020204.0low000010
thiophenes
49
mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent201220235.0high00003217
catechin
1
catechinantioxidant;
plant metabolite		201520159.0low000010
adamantane
1
adamantanes;
polycyclic alkane		202220222.0low000001
thiazoles
1
1,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		201520159.0low000010
galactosamine
1
D-galactosamine;
primary amino compound		toxin201820186.0low000010
ribavirin
1
1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide		anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor		202220222.0low000001
oseltamivir
1
acetamides;
amino acid ester;
cyclohexenecarboxylate ester;
primary amino compound		antiviral drug;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
environmental contaminant;
prodrug;
xenobiotic		202220222.0low000001
wortmannin
1
acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent		201620168.0low000010
resveratrol
1
resveratrolantioxidant;
phytoalexin;
plant metabolite;
quorum sensing inhibitor;
radical scavenger		201520159.0low000010
stilbenes
1
stilbene201520159.0low000010
n-hydroxy-n'-(4-butyl-2-methylphenyl)formamidine
1
toluenes202120213.0low000001
kl001
1
202020204.0low000010
sirolimus
1
antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor		201620168.0low000010
gw 501516
1
1,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound		carcinogenic agent;
PPARbeta/delta agonist		201520159.0low000010
glycolipids
1
202220222.0low000001
gsk4112
1
201920195.0low000010
transforming growth factor beta
1
201620168.0low000010
sr9011
7
201220228.9high000061
amyloid beta-peptides
1
201920195.0low000010
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Abortion, Spontaneous0
1
202120213.0low000001
Abortion, Tubal0
1
202120213.0low000001
Absence Status0
1
202020204.0low000010
Acute Confusional Senile Dementia0
1
201920195.0low000010
Acute Hepatic Failure0
1
201820186.0low000010
Acute Liver Injury, Drug-Induced0
1
201820186.0low000010
Acute Lung Injury0
1
202320231.0low000001
Adjuvant Arthritis0
1
202020204.0low000010
Alcoholic Liver Diseases0
1
202120213.0low000001
Allergic Encephalomyelitis0
1
201920195.0low000010
Allergic Reaction0
1
201920195.0low000010
Allodynia0
1
201920195.0low000010
Alloxan Diabetes0
1
201920195.0low000010
Alzheimer Disease0
1
201920195.0low000010
Anxiety0
1
2014201410.0low000010
Arthritis, Rheumatoid0
1
202020204.0low000010
Astrocytoma, Grade IV0
1
201820186.0low000010
Astrocytosis0
1
202020204.0low000010
Benign Neoplasms0
1
201820186.0low000010
Benign Psychomotor Epilepsy, Childhood0
1
202020204.0low000010
Bladder Cancer0
1
202320231.0low000001
Bone Loss, Osteoclastic0
1
201820186.0low000010
Brain Inflammation0
1
202020204.0low000010
Cancer of Lung0
1
202020204.0low000010
Cancer of Prostate0
1
202220222.0low000001
Carcinoma, Small Cell Lung0
1
202020204.0low000010
Cardiac Failure0
1
201920195.0low000010
Cardiac Remodeling, Ventricular0
1
201720177.0low000010
Chemical and Drug Induced Liver Injury0
1
201820186.0low000010
Cirrhosis, Liver0
2
201620206.0low000020
Cognitive Decline0
1
201920195.0low000010
Cognitive Dysfunction0
1
201920195.0low000010
Colitis0
1
202320231.0low000001
Colitis Gravis0
1
202320231.0low000001
Colitis, Ulcerative0
1
202320231.0low000001
Congenital Zika Syndrome0
1
202020204.0low000010
Diabetes Mellitus, Adult-Onset0
1
202220222.0low000001
Diabetes Mellitus, Type 20
1
202220222.0low000001
Disease Models, Animal0
8
201220215.0low000053
Diseases of Immune System0
1
202020204.0low000010
Encephalitis0
1
202020204.0low000010
Epilepsy, Temporal Lobe0
1
202020204.0low000010
Fatty Liver0
1
202120213.0low000001
Fatty Liver, Nonalcoholic0
3
202020232.7low000012
Genetic Predisposition0
1
201820186.0low000010
Glioblastoma0
1
201820186.0low000010
Heart Disease, Ischemic0
2
201920223.5low000011
Heart Failure0
1
201920195.0low000010
Hyperlipemia0
1
202120213.0low000001
Hyperlipidemias0
1
202120213.0low000001
Hyperplasia0
1
202320231.0low000001
Hypersensitivity0
1
201920195.0low000010
Immune System Diseases0
1
202020204.0low000010
Inflammation0
7
201720234.0low000043
Injury, Ischemia-Reperfusion0
1
202320231.0low000001
Injury, Myocardial Reperfusion0
1
202220222.0low000001
Innate Inflammatory Response0
7
201720234.0low000043
Ischemia0
1
202320231.0low000001
Jet Lag0
1
202320231.0low000001
Liver Cirrhosis0
2
201620206.0low000020
Liver Diseases, Alcoholic0
1
202120213.0low000001
Liver Failure, Acute0
1
201820186.0low000010
Liver Steatosis0
1
202120213.0low000001
Lung Injury, Acute0
1
202320231.0low000001
Lung Neoplasms0
1
202020204.0low000010
Mole, Skin0
1
201820186.0low000010
MS (Multiple Sclerosis)0
1
201920195.0low000010
Multiple Sclerosis0
1
201920195.0low000010
Myocardial Ischemia0
2
201920223.5low000011
Neointima0
1
202320231.0low000001
Neoplasms0
1
201820186.0low000010
Nerve Pain0
2
201920214.0low000011
Neuralgia0
2
201920214.0low000011
Non-alcoholic Fatty Liver Disease0
3
202020232.7low000012
Obesity0
5
201220236.4low000032
Osteoarthritis of Knee0
1
202320231.0low000001
Osteoarthritis, Knee0
1
202320231.0low000001
Palmoplantaris Pustulosis0
1
202120213.0low000001
Peritonitis0
1
201820186.0low000010
Plica Syndrome0
1
202020204.0low000010
Pregnancy0
1
202120213.0low000001
Primary Peritonitis0
1
201820186.0low000010
Prostatic Neoplasms0
1
202220222.0low000001
Psoriasis0
1
202120213.0low000001
Reperfusion Injury0
1
202320231.0low000001
Retinal Degeneration0
1
202320231.0low000001
Rheumatoid Arthritis0
1
202020204.0low000010
Small Cell Lung Carcinoma0
1
202020204.0low000010
Status Epilepticus0
1
202020204.0low000010
Synovitis0
1
202020204.0low000010
Urinary Bladder Neoplasms0
1
202320231.0low000001
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (2)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019
Optimized chemical probes for REV-ERBα.
Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11		2013

Dosage (4)

ArticleYear
Targeting Rev-Erbα to protect against ischemia-reperfusion-induced acute lung injury in rats.
Respiratory research, , Oct-12, Volume: 24, Issue:1		2023
Pharmacological Targeting the REV-ERBs in Sleep/Wake Regulation.
PloS one, , Volume: 11, Issue:9		2016
Pharmacological and Genetic Modulation of REV-ERB Activity and Expression Affects Orexigenic Gene Expression.
PloS one, , Volume: 11, Issue:3		2016
Optimized chemical probes for REV-ERBα.
Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11		2013