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 SourceID
PubMed CID166562
CHEMBL ID24955
SCHEMBL ID225678
MeSH IDM0258868

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

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)IC50 (µMol)0.00830.00170.48807.5000AID207459; AID207757; AID207913; AID215795
3-oxo-5-alpha-steroid 4-dehydrogenase 1 Rattus norvegicus (Norway rat)Ki0.00800.00500.04010.0882AID207926
3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)IC50 (µMol)5.87500.00010.526710.0000AID205602; AID207443; AID207611; AID215798
3-oxo-5-alpha-steroid 4-dehydrogenase 2Rattus norvegicus (Norway rat)Ki10.00000.00501.711010.0000AID205622
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
urogenital system development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
liver development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen catabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
sex determination3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
male gonad development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to starvation3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to xenobiotic stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to muscle activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
diterpenoid metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
spinal cord development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
hippocampus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
thalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
hypothalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
pituitary gland development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cerebral cortex development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cell differentiation3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
male genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
female genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to follicle-stimulating hormone3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to insulin stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
serotonin metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
progesterone metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to estrogen3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
bone development3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to growth hormone3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
response to fungicide3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to cAMP3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to growth factor stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to estradiol stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to testosterone stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to dexamethasone stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cellular response to epinephrine stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
steroid biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
androgen biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
steroid catabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell-cell signaling3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
androgen metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
male gonad development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to xenobiotic stimulus3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
biphenyl metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
dibenzo-p-dioxin metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
phthalate metabolic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
hippocampus development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
hypothalamus development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell differentiation3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
male genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
female genitalia development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to nutrient levels3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to follicle-stimulating hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to testosterone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to peptide hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
response to steroid hormone3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
bone development3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
testosterone biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
steroid biosynthetic process3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
3-oxo-5-alpha-steroid 4-dehydrogenase activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
electron transfer activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
amide binding3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+) activity3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
NADPH binding3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
3-oxo-5-alpha-steroid 4-dehydrogenase activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
protein binding3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
amide binding3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
3-oxo-5alpha-steroid 4-dehydrogenase (NADP+) activity3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membrane3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
neuronal cell body3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
perinuclear region of cytoplasm3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
cell body fiber3-oxo-5-alpha-steroid 4-dehydrogenase 1Homo sapiens (human)
endoplasmic reticulum membrane3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
neuronal cell body3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
cell body fiber3-oxo-5-alpha-steroid 4-dehydrogenase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID207753Inhibitory activity against steroid 5-alpha-reductase type 2 in human prostate homogenates at 10 uM2000Journal 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.
AID207443Inhibition of recombinant human Steroid 5-alpha-reductase type 21995Journal 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.
AID215798Compound was tested for inhibition of Type II 5-alpha-reductase in Human Prostate Homogenates (HPH)1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
AID207611Compound was tested for inhibition against human Steroid 5-alpha-reductase type 22000Bioorganic & 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.
AID207926Binding affinity on rat 5-alpha reductase-1 isozyme1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID205602Inhibition of type 2 steroid-5-alpha-reductase1994Journal 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.
AID215795In vitro inhibition of DHT production in Hs 68 (human genital fibroblast) cells.1993Journal of medicinal chemistry, Feb-05, Volume: 36, Issue:3
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
AID207762Inhibitory activity against Steroid 5-alpha-reductase type I in human scalp homogenates2000Journal 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.
AID207459Inhibition of recombinant human Steroid 5-alpha-reductase type I1995Journal 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.
AID205622Binding affinity on rat 5-alpha reductase-2 isozyme1997Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9
Pharmacological options in the treatment of benign prostatic hyperplasia.
AID207913Inhibition of type 1 steroid-5-alpha-reductase1994Journal 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.
AID207757Inhibition of human Steroid 5-alpha-reductase type I2000Bioorganic & 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)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (66.67)18.2507
2000's2 (33.33)29.6817
2010's0 (0.00)24.3611
2020's0 (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.

MetricThis Compound (vs All)
Research Demand Index12.50 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]