Page last updated: 2024-12-08
ly 300502
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 166562 |
| CHEMBL ID | 24955 |
| SCHEMBL ID | 225678 |
| MeSH ID | M0258868 |
Synonyms (32)
| Synonym |
|---|
| ly-191704 |
| D03107 |
| bexlosteride (usan/inn) |
| 148905-78-6 |
| bexlosteride |
| CHEMBL24955 , |
| ly300502 |
| ly-300502 |
| (4ar,10br)-8-chloro-4-methyl-1,2,4a,5,6,10b-hexahydrobenzo[f]quinolin-3-one |
| bexlosteride [usan:inn] |
| bezo(f)quinolin-3(2h)-one, 8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-, (4ar-trans) |
| (4ar,10br)-8-chloro-1,4,4a,5,6,10b-hexahydro-4-methylbenzo(f)quinolin-3(2h)-one |
| unii-36x732p4p0 |
| 36x732p4p0 , |
| bdbm50368782 |
| bexlosteride [inn] |
| bexlosteride [usan] |
| benzo(f)quinolin-3(2h)-one, 8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-, (4ar-trans) |
| (4ar,10br)-8-chloro-1,4,4a,5,6,10b-hexahydro-4-methylbenzo[f]quinolin-3(2h)-one |
| SCHEMBL225678 |
| (4ar) -(10br)-8-chloro-4-methyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolin-3-one |
| WQBIOEFDDDEARX-CHWSQXEVSA-N |
| (4ar)-(10br)-8-chloro-4-methyl-1,2,3,4,4a,5,6,10b-octahydrobenzo[f]quinolin-3-one |
| (4ar,10br)-8-chloro-4-methyl-1h,2h,3h,4h,4ah,5h,6h,10bh-benzo[f]quinolin-3-one |
| Q4899812 |
| bexlosterid |
| HY-118091A |
| DTXSID00869972 |
| CS-0198293 |
| 148905-79-7 |
| AKOS040756854 |
| benzo[f]quinolin-3(2h)-one, 8-chloro-1,4,4a,5,6,10b-hexahydro-4-methyl-, (4ar,10br)- |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (4)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0083 | 0.0017 | 0.4880 | 7.5000 | AID207459; AID207757; AID207913; AID215795 |
| 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Rattus norvegicus (Norway rat) | Ki | 0.0080 | 0.0050 | 0.0401 | 0.0882 | AID207926 |
| 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Homo sapiens (human) | IC50 (µMol) | 5.8750 | 0.0001 | 0.5267 | 10.0000 | AID205602; AID207443; AID207611; AID215798 |
| 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 0.0050 | 1.7110 | 10.0000 | AID205622 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (7)
Ceullar Components (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| endoplasmic reticulum membrane | 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) |
| neuronal cell body | 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) |
| perinuclear region of cytoplasm | 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) |
| cell body fiber | 3-oxo-5-alpha-steroid 4-dehydrogenase 1 | Homo sapiens (human) |
| endoplasmic reticulum membrane | 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Homo sapiens (human) |
| neuronal cell body | 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Homo sapiens (human) |
| cell body fiber | 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (12)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID207753 | Inhibitory activity against steroid 5-alpha-reductase type 2 in human prostate homogenates at 10 uM | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1. |
| AID207443 | Inhibition of recombinant human Steroid 5-alpha-reductase type 2 | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17 | 4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency. |
| AID215798 | Compound was tested for inhibition of Type II 5-alpha-reductase in Human Prostate Homogenates (HPH) | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase. |
| AID207611 | Compound was tested for inhibition against human Steroid 5-alpha-reductase type 2 | 2000 | Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4 | Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1. |
| AID207926 | Binding affinity on rat 5-alpha reductase-1 isozyme | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9 | Pharmacological options in the treatment of benign prostatic hyperplasia. |
| AID205602 | Inhibition of type 2 steroid-5-alpha-reductase | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | 4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase. |
| AID215795 | In vitro inhibition of DHT production in Hs 68 (human genital fibroblast) cells. | 1993 | Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3 | Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase. |
| AID207762 | Inhibitory activity against Steroid 5-alpha-reductase type I in human scalp homogenates | 2000 | Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20 | Benzo[c]quinolizin-3-ones: a novel class of potent and selective nonsteroidal inhibitors of human steroid 5alpha-reductase 1. |
| AID207459 | Inhibition of recombinant human Steroid 5-alpha-reductase type I | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17 | 4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency. |
| AID205622 | Binding affinity on rat 5-alpha reductase-2 isozyme | 1997 | Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9 | Pharmacological options in the treatment of benign prostatic hyperplasia. |
| AID207913 | Inhibition of type 1 steroid-5-alpha-reductase | 1994 | Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23 | 4,7 beta-Dimethyl-4-azacholestan-3-one (MK-386) and related 4-azasteroids as selective inhibitors of human type 1 5 alpha-reductase. |
| AID207757 | Inhibition of human Steroid 5-alpha-reductase type I | 2000 | Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4 | Synthesis of 8-chloro-benzo[c]quinolizin-3-ones as potent and selective inhibitors of human steroid 5alpha-reductase 1. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (66.67) | 18.2507 |
| 2000's | 2 (33.33) | 29.6817 |
| 2010's | 0 (0.00) | 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: 12.50
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 (12.50) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||