Page last updated: 2024-11-12
y134 compound
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Y134 compound: a selective estrogen receptor modulator derived from raloxifene; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 11784736 |
| CHEMBL ID | 178334 |
| CHEBI ID | 93654 |
| MeSH ID | M0508368 |
Synonyms (25)
| Synonym |
|---|
| HMS3269L21 , |
| BRD-K94832621-001-01-5 |
| NCGC00167826-01 |
| (6-hydroxy-2-(4-hydroxy-phenyl)benzo(b)thiophen-3-yl)-(4-(4-isopropylpiperazin-1-yl)-phenyl)methanone |
| y134 compound |
| bdbm50161698 |
| [6-hydroxy-2-(4-hydroxy-phenyl)-benzo[b]thiophen-3-yl]-[4-(4-isopropyl-piperazin-1-yl)-phenyl]-methanone |
| CHEMBL178334 , |
| y 134 |
| 849662-80-2 |
| 2-(4-hydroxyphenyl)-3-({4-[4-(propan-2-yl)piperazin-1-yl]phenyl}carbonyl)-1-benzothiophen-6-ol |
| y-134 |
| y134 |
| gtpl5430 |
| [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]methanone |
| AKOS024457235 |
| DTXSID20472568 |
| [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]-[4-(4-propan-2-ylpiperazin-1-yl)phenyl]methanone |
| CHEBI:93654 |
| [6-hydroxy-2-(4-hydroxyphenyl)benzothiophen-3-yl]-[4-(4-isopropylpiperazin-1-yl)phenyl]methanone |
| HMS3677P21 |
| Q27089255 |
| HMS3413P21 |
| HY-103457 |
| CS-0027928 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
| Class | Description |
|---|---|
| aromatic ketone | A ketone in which the carbonyl group is attached to an aromatic ring. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (4)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 35.4813 | 0.0040 | 23.8416 | 100.0000 | AID485290 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 35.4813 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
| [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) |
|---|---|---|---|---|---|---|---|
| Estrogen receptor | Homo sapiens (human) | IC50 (µMol) | 0.0003 | 0.0000 | 0.7237 | 32.7000 | AID241231; AID658134 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0339 | 0.0001 | 0.5294 | 32.7000 | AID241201; AID658135 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (44)
Molecular Functions (29)
Ceullar Components (13)
Bioassays (14)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID242967 | IC50 ratio of binding to estrogen receptor beta and alpha | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID658135 | Displacement of [3H]-17beta-estradiol from ERbeta | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Recent advances in the synthesis of raloxifene: a selective estrogen receptor modulator. |
| AID658136 | Selectivity ratio of IC50 for ERbeta to IC50 for ERalpha | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Recent advances in the synthesis of raloxifene: a selective estrogen receptor modulator. |
| AID658134 | Displacement of [3H]-17beta-estradiol from ERalpha | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Recent advances in the synthesis of raloxifene: a selective estrogen receptor modulator. |
| AID244482 | Bone mineral density of compound was determined in vivo against estrogen receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID241231 | Inhibition of estrogen receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID244483 | Uterine weight assay of compound was determined in vivo against estrogen receptor alpha | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID241201 | Inhibition of estrogen receptor beta | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID493017 | Wombat Data for BeliefDocking | 2005 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 15, Issue:5 | Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (40.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 12.87
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.87) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (20.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (80.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||