Page last updated: 2024-12-11
era-923
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl)-1H-indol-5-ol: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 6433099 |
| CHEMBL ID | 44426 |
| SCHEMBL ID | 134583 |
| MeSH ID | M0405387 |
Synonyms (26)
| Synonym |
|---|
| era-923 |
| pipendoxifene |
| 2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl)-1h-indol-5-ol |
| CHEMBL44426 , |
| us8815934, no. 97 |
| 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(2-piperidin-1-yl-ethoxy)-benzyl]-1h-indol-5-ol |
| bdbm50099587 |
| us8815934, no. 107 |
| 2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol |
| 198480-55-6 |
| 1h-indol-5-ol, 2-(4-hydroxyphenyl)-3-methyl-1-((4-(2-(1-piperidinyl)ethoxy)phenyl)methyl)- |
| era 923 |
| pipendoxifene [inn] |
| unii-tpc5q8496g |
| 2-(p-hydroxyphenyl)-3-methyl-1-(p-(2-piperidinoethoxy)benzyl)indol-5-ol |
| tpc5q8496g , |
| JICOGKJOQXTAIP-UHFFFAOYSA-N |
| DB05414 |
| SCHEMBL134583 |
| pipendoxifene [who-dd] |
| 2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-(piperidin-1-yl)ethoxy)benzyl)-1h-indol-5-ol. |
| Q27095593 |
| DTXSID40870209 |
| CS-0007753 |
| 2-(4-hydroxyphenyl)-3-methyl-1-[[4-[2-(1-piperidinyl)ethoxy]phenyl]methyl]-1h-indol-5-ol |
| HY-13724 |
Research Excerpts
Toxicity
| Excerpt | Reference | Relevance |
|---|---|---|
| " ERA-923 was well tolerated, and adverse events were mild and reversible." | ( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002) | 1.44 |
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " In addition, pharmacokinetic analysis showed that a high-fat breakfast increased the extent of absorption." | ( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002) | 0.53 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " We describe the identification and characterization of a series of small-molecule, orally bioavailable SERDs which are potent antagonists and degraders of ER-α and in which the ER-α degrading properties were prospectively optimized." | ( Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. Aparicio, A; Bonnefous, C; Brigham, D; Darimont, B; Douglas, K; Govek, S; Grillot, K; Hager, JH; Heyman, R; Joseph, JD; Julien, J; Kahraman, M; Kaufman, J; Lai, A; Lee, KJ; Lu, N; Moon, MJ; Nagasawa, J; Prudente, R; Qian, J; Rix, PJ; Sensintaffar, J; Shao, G; Smith, ND, 2015) | 0.42 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Overall, ERA-923 was safe and well tolerated in postmenopausal women dosed for 28 days." | ( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002) | 0.93 |
[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) | 0.0078 | 0.0000 | 0.7237 | 32.7000 | AID102611; AID70008 |
| Estrogen receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.0400 | 0.0001 | 0.5294 | 32.7000 | AID70176 |
| [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) | 0.0001 | 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 (13)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| AID70176 | In vitro inhibitory concentration against [3H]17-beta-estradiol binding to human estrogen receptor 2 | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| AID70008 | In vitro inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID102611 | In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol | 2001 | Journal of medicinal chemistry, May-24, Volume: 44, Issue:11 | Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens. |
| [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 | 4 (80.00) | 29.6817 |
| 2010's | 1 (20.00) | 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: 12.22
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 (12.22) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (16.67%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (66.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||