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 Source | ID |
|---|---|
| PubMed CID | 57394020 |
| CHEMBL ID | 1961796 |
| MeSH ID | M0574047 |
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.
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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.
| Excerpt | Relevance | Reference |
|---|---|---|
| " 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
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.6837 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 4.2534 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 3.0112 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 4.2534 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.2534 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.2534 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.2534 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Nuclear receptor subfamily 1 group D member 1 | Homo sapiens (human) | IC50 (µMol) | 0.6833 | 0.6200 | 0.6920 | 0.7900 | AID651466; AID651468; AID671970 |
| Oxysterols receptor LXR-alpha | Homo sapiens (human) | IC50 (µMol) | 6.3000 | 0.0090 | 1.0604 | 9.9000 | AID747988 |
| Nuclear receptor subfamily 1 group D member 2 | Homo sapiens (human) | IC50 (µMol) | 0.8000 | 0.5600 | 0.6800 | 0.8000 | AID651467 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Nuclear receptor subfamily 1 group D member 1 | Homo sapiens (human) | EC50 (µMol) | 17.1067 | 0.4000 | 1.1444 | 2.3000 | AID1722006; AID671968; AID747991 |
| Nuclear receptor subfamily 1 group D member 1 | Homo sapiens (human) | Kd | 0.8000 | 0.8000 | 0.8000 | 0.8000 | AID651469 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (107)
Molecular Functions (35)
Ceullar Components (28)
Bioassays (93)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID651487 | Change in plasma triglycerides in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651535 | Effect on SF1(NR5A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651492 | Change in plasma leptin in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651516 | Effect on TR2(NR2C1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID1722006 | Agonist activity at Rev-Erb alpha (unknown origin) by FRET assay | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | The transcriptional repressor REV-ERB as a novel target for disease. |
| AID651523 | Effect on ESR1(NR3A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651512 | Effect on HNF4G(NR2A2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651477 | Plasma concentration after 2 hours at 100mg/kg ip dose (10mg/ml solution in 15% Cremophor) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651526 | Effect on ERR2(NR3B2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651521 | Effect on TFCOUP2(NR2F2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651482 | Decreased expression of REV-ERB responsive gene Srebf1 in mouse liver after 6 days at 100 mg/kg | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671973 | Plasma concentration in C57BL/6 mouse at 50 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651539 | Effect on GCNF(NR6A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651489 | Change in plasma NEFA (non-esterified fatty acids) in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651524 | Effect on ESR2(NR3A2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651491 | Change in plasma insulin in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651536 | Effect on CPF(NR5A2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651498 | Effect on RARG(NR1B3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747988 | Binding affinity to LXRalpha (unknown origin) by radioligand displacement assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651500 | Effect on PPARD(NR1C2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651466 | Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651514 | Effect on RXRB(NR2B2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651504 | Effect on RORG(NR1F3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651508 | Effect on VDR(NR1I1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651509 | Effect on PXR(NR1I2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651518 | Effect on TLX(NR2E1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651483 | Decreased expression of REV-ERB responsive gene Serpine1 in mouse liver after 6 days at 100 mg/kg | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651531 | Effect on AR(NR3C4) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671976 | Ratio of drug uptake in brain to plasma of C57BL/6 mouse at 50 mg/kg, ip relative to control | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651470 | Recruitment of co-repressor NcoR1 to REV-ERB-alpha | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651499 | Effect on PPARA(NR1C1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671970 | Agonist 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 assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651515 | Effect on RXRG(NR2B3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651511 | Effect on HNF4A(NR2A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651530 | Effect on PGR(NR3C3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651488 | Change in total plasma cholesterol in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747989 | Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as biotinylated PGC1-beta peptide recruitment after 20 mins by Greiner assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651525 | Effect on ERR1(NR3B1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651472 | Plasma concentration after 2 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651513 | Effect on RXRA(NR2B1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651495 | Effect on THRB(NR1A2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651471 | Plasma concentration after 1 hour at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651519 | Effect on PNR(NR2E3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651490 | Change in plasma glucose in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671975 | Ratio 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 control | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651532 | Effect on GFRP1(NR4A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651494 | Effect on THRA(NR1A1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651467 | Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651475 | Brain concentration after 8 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651474 | Plasma concentration after 8 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651527 | Effect on ERR3(NR3B3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651522 | Effect on EAR2(NR2F6) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671971 | Plasma concentration in C57BL/6 mouse at 10 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID671968 | Agonist activity at Rev-Erbalpha expressed in HEK293 cells coexpressing BamII promoter assessed as repression of transcription after 24 hrs by dual-Glo luciferase assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651473 | Plasma concentration after 4 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651517 | Effect on TR4(NR2C2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651496 | Effect on RARA(NR1B1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747984 | Agonist 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 control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651507 | Effect on BAR(NR1H4) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651486 | Increased weight loss in diet-induced obese mice over 30 days at 100 mg/kg ip compared to vehicle control | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651478 | Plasma concentration after 8 hours at 100mg/kg ip dose (10mg/ml solution in 15% Cremophor) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651510 | Effect on CAR(NR1I3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671972 | Drug uptake in C57BL/6 mouse brain at 10 mg/kg, ip measured after 2 hrs by LC-MS/MS analysis | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651537 | Effect on DAX1(NR0B1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651481 | Decreased expression of REV-ERB responsive gene Cyp7a1 in mouse liver after 6 days at 100 mg/kg | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651493 | Change in plasma IL-6 in diet-induced obese mice over 30 days at 100 mg/kg ip | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651505 | Effect on LXRB(NR1H2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671969 | Agonist 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 control | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651497 | Effect on RARB(NR1B2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651534 | Effect on NOR1(NR4A3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651506 | Effect on LXRA(NR1H3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651520 | Effect on TFCOUP1(NR2F1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651502 | Effect on RORA(NR1F1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747983 | Agonist 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 control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651468 | REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651503 | Effect on RORB(NR1F2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747991 | Agonist activity at biotinylated REV-ERBalpha (unknown origin) assessed as increase in biotinylated NCOR peptide recruitment after 1 hr by FRET assay | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651528 | Effect on GCR(NR3C1) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651469 | Dissociation constant for binding to REV-ERB-alpha by circular dichroism | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651538 | Effect on SHP(NR0B2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651501 | Effect on PPARG(NR1C3) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID747990 | Agonist 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 control | 2013 | Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11 | Optimized chemical probes for REV-ERBα. |
| AID651533 | Effect on NURR1(NR4A2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID671974 | Drug uptake in C57BL/6 mouse brain at 50 mg/kg, ip measured after 8 hrs by LC-MS/MS analysis | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα. |
| AID651529 | Effect on MCR(NR3C2) dependent reporter activity in HEK293 cells at 20 uM | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID651476 | Brain concentration after 2 hours at 10mg/kg ip dose (10mg/ml suspension in 10%DMSO/10%Tween80) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID1346801 | Human Rev-Erb-alpha (1D. Rev-Erb receptors) | 2012 | Nature, Mar-29, Volume: 485, Issue:7396 | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. |
| AID1346747 | Human Rev-Erb-beta (1D. Rev-Erb receptors) | 2012 | Nature, 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 27 (42.19) | 24.3611 |
| 2020's | 37 (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.
| This Compound (42.81) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (3.08%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 63 (96.92%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||