Page last updated: 2024-12-08
ly 353381
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
LY 353381: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 179337 |
| CHEMBL ID | 226267 |
| SCHEMBL ID | 285277 |
| MeSH ID | M0296584 |
Synonyms (30)
| Synonym |
|---|
| 182133-25-1 |
| ly 353381 |
| ly353381 |
| ly-353381 |
| 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol |
| bdbm19442 |
| 2-(4-methoxyphenyl)-3-{4-[2-(piperidin-1-yl)ethoxy]phenoxy}-1-benzothiophen-6-ol |
| arzoxifene |
| CHEMBL226267 |
| benzo(b)thiophene-6-ol, 2-(4-methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)- |
| arzoxifene [inn] |
| 2-(p-methoxyphenyl)-3-(p-(2-piperidinoethoxy)phenoxy)benzo(b)thiophene-6-ol |
| e569wg6e60 , |
| unii-e569wg6e60 |
| arzoxifene [who-dd] |
| 2-(4-methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(b)thiophene-6-ol |
| arzoxifene [mi] |
| arzoxifene [mart.] |
| SCHEMBL285277 |
| 2-(4-methoxyphenyl)-3-(4-(2-(piperidin-1-yl)ethoxy)phenoxy)benzo[b]thiophen-6-ol |
| DTXSID10171255 |
| AKOS030631785 |
| Q4802769 |
| FT-0751607 |
| DB06249 |
| benzo[b]thiophene-6-ol, 2-(4-methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]- |
| SB19713 |
| CS-0007165 |
| HY-13556 |
| EN300-19634484 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " Adverse event reporting with arzoxifene was similar to that with raloxifene, as were hot flush and night sweat reporting." | ( Effects of arzoxifene on bone, lipid markers, and safety parameters in postmenopausal women with low bone mass. Cox, DA; Downs, RW; Dowsett, SA; Ghosh, A; Harper, K; Moffett, AM, 2010) | 0.36 |
| " The proportion of women reporting ≥ 1 adverse event did not differ between treatment groups, nor did vaginal bleeding." | ( Arzoxifene versus raloxifene: effect on bone and safety parameters in postmenopausal women with osteoporosis. Alam, J; Cox, DA; Dowsett, SA; Kendler, DL; Palacios, S; Stock, J; Zanchetta, J, 2012) | 0.38 |
Bioavailability
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Female rhesus macaques were ovariectomized and orally dosed with vehicle, estradiol 17beta, raloxifene or arzoxifene once per day by sipper bottles for 30 days." | ( Effects of oral estrogen, raloxifene and arzoxifene on gene expression in serotonin neurons of macaques. Bethea, CL; Michelson, D; Mirkes, SJ; Su, A, 2002) | 0.31 |
| " We also show that it is not necessary to administer Arz and 268 continuously during tumor progression to prevent cancer in the rat model because dosing of these drugs in combination for relatively short periods, each followed by drug-free rests, is highly effective." | ( The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer. Berchuck, A; Heyman, RA; Krajewski, S; Lamph, WW; Liby, K; Reed, JC; Rendi, MH; Risingsong, R; Royce, DB; Sporn, MB; Suh, N; Williams, CR, 2004) | 0.32 |
| " Factors that may contribute to poor compliance and persistence with current osteoporosis therapies include drug intolerance, complexity of dosing regimens, and poor understanding of the relative benefit and risk with treatment." | ( Current and emerging pharmacologic therapies for the management of postmenopausal osteoporosis. Lewiecki, EM, 2009) | 0.35 |
[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) |
|---|---|---|---|---|---|---|---|
| Estrogen receptor | Homo sapiens (human) | IC50 (µMol) | 0.0378 | 0.0000 | 0.7237 | 32.7000 | AID1228236; AID1797853; AID288628 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0985 | 0.0001 | 0.5294 | 32.7000 | AID1228237; AID1797853; AID288629 |
| [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) |
|---|---|---|---|---|---|---|---|
| Estrogen receptor | Homo sapiens (human) | EC50 (µMol) | 0.0002 | 0.0000 | 0.5305 | 4.4000 | AID1228205 |
| [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 (17)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1228236 | Displacement of [3H]-E2 from estrogen receptor-alpha (unknown origin) by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228239 | Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID288626 | Displacement of [3H]estradiol from human recombinant ERbeta relative to estradiol | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| AID288625 | Displacement of [3H]estradiol from human recombinant ERalpha relative to estradiol | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| AID1228205 | Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID288627 | Selectivity for human ERbeta over human ERbeta | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| AID1228310 | AUC in 17-beta estradiol pellets supplemented nu/nu mouse xenografted with tamoxifen-resistant human MCF7 cells at 100 mg/kg/day, po administered for 4 weeks measured on day 28 | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228206 | Induction of estrogen receptor-alpha degradation in human MCF7 cells at 5.12 x 10'-12 to 10'-5 M after 4 hrs by in-cell western assay relative to control | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228237 | Displacement of [3H]-E2 from estrogen receptor-beta (unknown origin) by scintillation counting analysis | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228306 | Antitumor activity against tamoxifen-resistant human MCF7 cells xenografted in nu/nu mouse supplemented with 17-beta estradiol pellets assessed as tumor volume at 100 mg/kg/day, po administered for 4 weeks measured twice weekly during compound dosing rela | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228208 | Induction of estrogen receptor-alpha degradation in human MCF7 cells at 5.12 x 10'-12 to 10'-5 M after 4 hrs by in-cell western assay relative to fulvestrant | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228235 | Cytotoxicity against human MCF7 cells assessed as cell viability at 0.000005 to 10 uM after 5 days by CellTiter-Glo assay relative to fulvestrant | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID1228308 | Antitumor activity against tamoxifen-resistant human MCF7 cells xenografted in nu/nu mouse supplemented with 17-beta estradiol pellets assessed as change in tumor volume at 100 mg/kg/day, po administered for 4 weeks measured twice weekly during compound d | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID288628 | Displacement of [3H]estradiol from human recombinant ERalpha | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| AID1228231 | Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay | 2015 | Journal of medicinal chemistry, Jun-25, Volume: 58, Issue:12 | Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. |
| AID288629 | Displacement of [3H]estradiol from human recombinant ERbeta | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| AID1797853 | Estrogen Receptor Binding Assay. from Article 10.1021/jm070079j: \\Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.\\ | 2007 | Journal of medicinal chemistry, May-31, Volume: 50, Issue:11 | Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (69)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (2.90) | 18.2507 |
| 2000's | 50 (72.46) | 29.6817 |
| 2010's | 17 (24.64) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 10.93
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 (10.93) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 12 (17.14%) | 5.53% |
| Reviews | 20 (28.57%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 38 (54.29%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||