Page last updated: 2024-11-13
sr9238
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
SR9238: liver-selective LXR inverse agonist that suppresses hepatic steatosis; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 71478195 |
| CHEMBL ID | 4284414 |
| SCHEMBL ID | 15773678 |
| MeSH ID | M000600738 |
Synonyms (17)
| Synonym |
|---|
| SCHEMBL15773678 |
| ethyl 5-[[[4-(3-methylsulfonylphenyl)phenyl]methyl-(2,4,6-trimethylphenyl)sulfonylamino]methyl]furan-2-carboxylate |
| sr9238 |
| gtpl8692 |
| sr 9238 |
| 1416153-62-2 |
| ethyl 5-[[[[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]methyl][(2,4,6-trimethylphenyl)sulfonyl]amino]methyl]-2-furancarboxylate |
| AKOS027470306 |
| EX-A3559 |
| ethyl 5-(((2,4,6-trimethyl-n-((3'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)methyl)phenyl)sulfonamido)methyl)furan-2-carboxylate |
| HY-101442 |
| CS-0021352 |
| BS-15090 |
| Q27088868 |
| D80447 |
| CHEMBL4284414 , |
| bdbm50465712 |
Research Excerpts
Actions
| Excerpt | Reference | Relevance |
|---|---|---|
| "SR9238 displays high potency for both LXRα and LXRβ (40-200 nM IC50) and was designed to display liver specificity so as to avoid potential side effects due to suppression of LXR in the periphery." | ( A liver-selective LXR inverse agonist that suppresses hepatic steatosis. Burris, TP; El-Gendy, Bel-D; Griffett, K; Kamenecka, TM; Solt, LA, 2013) | 1.11 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Oxysterols receptor LXR-beta | Homo sapiens (human) | IC50 (µMol) | 0.0715 | 0.0079 | 0.9285 | 9.9000 | AID1414115; AID1743596 |
| Oxysterols receptor LXR-beta | Homo sapiens (human) | Ki | 0.3520 | 0.0022 | 0.0730 | 0.3520 | AID1562690 |
| Oxysterols receptor LXR-alpha | Homo sapiens (human) | IC50 (µMol) | 0.1870 | 0.0090 | 1.0604 | 9.9000 | AID1414116; AID1743594 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (43)
Molecular Functions (14)
Ceullar Components (7)
Bioassays (10)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1562690 | Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Identify liver X receptor β modulator building blocks by developing a fluorescence polarization-based competition assay. |
| AID1743594 | Inverse agonist activity at human LXRalpha transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors. |
| AID1743595 | Inverse agonist activity at human LXRalpha transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay relative | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors. |
| AID1743596 | Inverse agonist activity at human LXRbeta transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors. |
| AID1414115 | Inverse agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells 24 hrs by Dual-Glo luciferase assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Recent Advances in the Medicinal Chemistry of Liver X Receptors. |
| AID1743597 | Inverse agonist activity at human LXRbeta transfected in human HEK293T cells co-transfected with pSG5 and pGL3/(DR-4)-c-fos-FF-luc/pCMV/Renilla-luc assessed as receptor transactivation incubated for 20 hrs by dual luciferase reporter gene assay relative t | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors. |
| AID1414116 | Inverse agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells 24 hrs by Dual-Glo luciferase assay | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Recent Advances in the Medicinal Chemistry of Liver X Receptors. |
| AID1414122 | Reduction in hepatic collagen deposition in mouse at 30 mg/kg, ip for 30 days | 2018 | Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24 | Recent Advances in the Medicinal Chemistry of Liver X Receptors. |
| AID1346765 | Mouse Liver X receptor-alpha (1H. Liver X receptor-like receptors) | 2013 | ACS chemical biology, Mar-15, Volume: 8, Issue:3 | A liver-selective LXR inverse agonist that suppresses hepatic steatosis. |
| AID1346776 | Mouse Liver X receptor-beta (1H. Liver X receptor-like receptors) | 2013 | ACS chemical biology, Mar-15, Volume: 8, Issue:3 | A liver-selective LXR inverse agonist that suppresses hepatic steatosis. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (7)
| 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 | 4 (57.14) | 24.3611 |
| 2020's | 3 (42.86) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 20.12
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (20.12) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (14.29%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (85.71%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||