9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo(3,2-f)quinolin-7(6H)-one: an androgen receptor modulator; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 25195253 |
| CHEMBL ID | 5170697 |
| SCHEMBL ID | 4130914 |
| MeSH ID | M0529676 |
| Synonym |
|---|
| lgd-3303 |
| SCHEMBL4130914 |
| 1196133-39-7 |
| 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3,6-dihydro-7h-pyrrolo[3,2-f]quinolin-7-one , |
| omxgogxewuclfi-uhfffaoysa-n |
| unii-7n4e1x2rjm |
| lgd 3303 |
| lgd3303 |
| 917891-35-1 |
| 7N4E1X2RJM , |
| 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3h-pyrrolo(3,2-f)quinolin-7(6h)-one |
| BCP20806 |
| lgd-3033 |
| EX-A1672 |
| DB13937 |
| Q6458311 |
| CS-0028120 |
| HY-103576 |
| H11981 |
| 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3h-pyrrolo[3,2-f]quinolin-7(6h)-one |
| AKOS037515574 |
| A902697 |
| 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3,6-dihydro-pyrrolo[3,2-f]quinolin-7-one |
| 9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-6h-pyrrolo[3,2-f]quinolin-7-one |
| bdbm50594922 |
| DTXSID601028425 |
| CHEMBL5170697 , |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The mechanisms responsible for the tissue-selective activity of SARMs are not fully understood, and the pharmacokinetic (PK)/pharmacodynamic (PD) relationships are poorly described." | ( Pharmacokinetics and pharmacodynamics of LGD-3303 [9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator. Chang, WY; Chen, Y; Hill, R; Lee, KJ; Lee, YH; López, FJ; Meglasson, MD; O'Brien, Z; Rix, P; Vajda, EG, 2009) | 0.35 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Tissue-selective activity was maintained when LGD-3303 was dosed orally or by continuous infusion, two routes of administration with markedly different time versus exposure profiles." | ( Pharmacokinetics and pharmacodynamics of LGD-3303 [9-chloro-2-ethyl-1-methyl-3-(2,2,2-trifluoroethyl)-3H-pyrrolo-[3,2-f]quinolin-7(6H)-one], an orally available nonsteroidal-selective androgen receptor modulator. Chang, WY; Chen, Y; Hill, R; Lee, KJ; Lee, YH; López, FJ; Meglasson, MD; O'Brien, Z; Rix, P; Vajda, EG, 2009) | 0.35 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Androgen receptor | Homo sapiens (human) | Ki | 0.0009 | 0.0002 | 0.4240 | 7.2000 | AID1872321 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Androgen receptor | Homo sapiens (human) | EC50 (µMol) | 0.0036 | 0.0000 | 0.2079 | 4.3000 | AID1872322 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| plasma membrane | Androgen receptor | Homo sapiens (human) |
| nucleus | Androgen receptor | Homo sapiens (human) |
| nucleoplasm | Androgen receptor | Homo sapiens (human) |
| cytoplasm | Androgen receptor | Homo sapiens (human) |
| cytosol | Androgen receptor | Homo sapiens (human) |
| nuclear speck | Androgen receptor | Homo sapiens (human) |
| chromatin | Androgen receptor | Homo sapiens (human) |
| protein-containing complex | Androgen receptor | Homo sapiens (human) |
| nucleus | Androgen receptor | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1872322 | Activation of Androgen receptor-mediated transcription (unknown origin) in African green monkey CV-1 cells incubated for 40 hrs by Luciferase reporter gene assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021). |
| AID1872321 | Binding affinity to recombinant human Androgen receptor assessed as inhibition constant by competitive binding assay | 2022 | European journal of medicinal chemistry, Feb-15, Volume: 230 | Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021). |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (33.33) | 29.6817 |
| 2010's | 2 (33.33) | 24.3611 |
| 2020's | 2 (33.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (33.33%) | 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] | ||