lg 121071 profile

ID Source	ID
PubMed CID	9839132
CHEMBL ID	390728
SCHEMBL ID	12158649
MeSH ID	M0301468

Synonym
bdbm18190
6-ethyl-4-(trifluoromethyl)-1h,2h,6h,7h,8h,9h-pyrido[3,2-g]quinolin-2-one
chembl390728 ,
lg121071
lg-121071
lgd-121071
SCHEMBL12158649
179897-70-2
6-ethyl-4-(trifluoromethyl)-1,2,6,7,8,9-hexahydropyrido[3,2-g]quinolin-2-one
AKOS034131304
6-ethyl-4-(trifluoromethyl)-6,7,8,9-tetrahydro-1h-pyrido[3,2-g]quinolin-2-one
242f29cp76 ,
szppqfartyxrku-uhfffaoysa-n
6-ethyl-6,7,8,9-tetrahydro-4-(trifluoromethyl)pyrido[3,2-g]quinolin-2(1h)-one
pyrido[3,2-g]quinolin-2(1h)-one, 6-ethyl-6,7,8,9-tetrahydro-4-(trifluoromethyl)-
4-ethyl-1,2,3,4-tetrahydro-6-(trifluoromethyl)-8-pyridono[5,6-g]quinoline
DTXSID501045799
Z3015233305

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Androgen receptor	Homo sapiens (human)	IC50 (µMol)	7.3537	0.0000	0.8753	10.0000	AID286657; AID38973; AID38982
Androgen receptor	Homo sapiens (human)	Ki	0.0126	0.0002	0.4240	7.2000	AID1797703; AID1885021; AID286658; AID39007; AID39140
[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)	0.0039	0.0000	0.2079	4.3000	AID1872317; AID1885023; AID286656; AID375618; AID38799; AID38803
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
negative regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
MAPK cascade	Androgen receptor	Homo sapiens (human)
in utero embryonic development	Androgen receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure	Androgen receptor	Homo sapiens (human)
epithelial cell morphogenesis	Androgen receptor	Homo sapiens (human)
transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
signal transduction	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Androgen receptor	Homo sapiens (human)
cell-cell signaling	Androgen receptor	Homo sapiens (human)
spermatogenesis	Androgen receptor	Homo sapiens (human)
single fertilization	Androgen receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of gene expression	Androgen receptor	Homo sapiens (human)
male somatic sex determination	Androgen receptor	Homo sapiens (human)
intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
intracellular receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of intracellular estrogen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
Leydig cell differentiation	Androgen receptor	Homo sapiens (human)
multicellular organism growth	Androgen receptor	Homo sapiens (human)
positive regulation of phosphorylation	Androgen receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Androgen receptor	Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
positive regulation of cell differentiation	Androgen receptor	Homo sapiens (human)
negative regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of integrin biosynthetic process	Androgen receptor	Homo sapiens (human)
positive regulation of DNA-templated transcription	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Androgen receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase III	Androgen receptor	Homo sapiens (human)
insulin-like growth factor receptor signaling pathway	Androgen receptor	Homo sapiens (human)
regulation of developmental growth	Androgen receptor	Homo sapiens (human)
animal organ formation	Androgen receptor	Homo sapiens (human)
male genitalia morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
negative regulation of epithelial cell proliferation	Androgen receptor	Homo sapiens (human)
positive regulation of NF-kappaB transcription factor activity	Androgen receptor	Homo sapiens (human)
activation of prostate induction by androgen receptor signaling pathway	Androgen receptor	Homo sapiens (human)
morphogenesis of an epithelial fold	Androgen receptor	Homo sapiens (human)
lateral sprouting involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
prostate gland growth	Androgen receptor	Homo sapiens (human)
prostate gland epithelium morphogenesis	Androgen receptor	Homo sapiens (human)
epithelial cell differentiation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
tertiary branching involved in mammary gland duct morphogenesis	Androgen receptor	Homo sapiens (human)
mammary gland alveolus development	Androgen receptor	Homo sapiens (human)
positive regulation of epithelial cell proliferation involved in prostate gland development	Androgen receptor	Homo sapiens (human)
cellular response to steroid hormone stimulus	Androgen receptor	Homo sapiens (human)
cellular response to estrogen stimulus	Androgen receptor	Homo sapiens (human)
cellular response to testosterone stimulus	Androgen receptor	Homo sapiens (human)
seminiferous tubule development	Androgen receptor	Homo sapiens (human)
non-membrane-bounded organelle assembly	Androgen receptor	Homo sapiens (human)
positive regulation of miRNA transcription	Androgen receptor	Homo sapiens (human)
regulation of protein localization to plasma membrane	Androgen receptor	Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway	Androgen receptor	Homo sapiens (human)
male gonad development	Androgen receptor	Homo sapiens (human)
intracellular steroid hormone receptor signaling pathway	Androgen receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
transcription cis-regulatory region binding	Androgen receptor	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
RNA polymerase II general transcription initiation factor binding	Androgen receptor	Homo sapiens (human)
transcription coactivator binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Androgen receptor	Homo sapiens (human)
chromatin binding	Androgen receptor	Homo sapiens (human)
DNA-binding transcription factor activity	Androgen receptor	Homo sapiens (human)
nuclear receptor activity	Androgen receptor	Homo sapiens (human)
G protein-coupled receptor activity	Androgen receptor	Homo sapiens (human)
signaling receptor binding	Androgen receptor	Homo sapiens (human)
steroid binding	Androgen receptor	Homo sapiens (human)
androgen binding	Androgen receptor	Homo sapiens (human)
protein binding	Androgen receptor	Homo sapiens (human)
beta-catenin binding	Androgen receptor	Homo sapiens (human)
zinc ion binding	Androgen receptor	Homo sapiens (human)
enzyme binding	Androgen receptor	Homo sapiens (human)
ATPase binding	Androgen receptor	Homo sapiens (human)
molecular adaptor activity	Androgen receptor	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Androgen receptor	Homo sapiens (human)
POU domain binding	Androgen receptor	Homo sapiens (human)
molecular condensate scaffold activity	Androgen receptor	Homo sapiens (human)
estrogen response element binding	Androgen receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

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]

Bioassays (19)

Assay ID	Title	Year	Journal	Article
AID38799	Agonist activity to the human androgen receptor (hAR) in CV-1 cells	1999	Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9	4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
AID38973	Antagonistic activity against human androgen receptor (hAR) in CV-1 cells using cotransfection assay	1999	Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9	4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
AID38833	Percent efficacy for human Androgen receptor agonist activity compared to dihydrotestosterone	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
AID39007	Binding affinity for human Androgen receptor expressed in COS-1 cells	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
AID1885021	Binding affinity to human Androgen receptor	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID1885024	Agonist activity at human Androgen receptor relative to control	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID39140	Binding affinity to the human androgen receptor (hAR), using [3H]DHT as radioligand in a competitive binding assay	1999	Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9	4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
AID375618	Agonist activity at androgen receptor assessed as receptor transactivation by reporter gene assay	2009	Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12	Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
AID286657	Antagonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay	2007	Journal of medicinal chemistry, May-17, Volume: 50, Issue:10	Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID39159	Antagonistic activity against human androgen receptor (hAR) in CV-1 cells was determined as a function of maximal inhibition of dihydrotestosterone using cotransfection assay	1999	Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9	4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
AID38982	Antagonist activity against Human Androgen receptor expressed in CV-1 cells	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
AID286656	Agonist activity at human androgen receptor expressed in CV1 cells by transcriptional activation assay	2007	Journal of medicinal chemistry, May-17, Volume: 50, Issue:10	Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID38803	Agonist activity against Human Androgen receptor expressed in CV-1 cells	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
AID39155	Agonism of human androgen receptor (hAR) in CV-1 cells compared to that of dihydrotestosterone (100%)	1999	Bioorganic & medicinal chemistry letters, May-03, Volume: 9, Issue:9	4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
AID38834	Percent efficacy for human Androgen receptor antagonist activity compared to dihydrotestosterone	1999	Journal of medicinal chemistry, Jan-28, Volume: 42, Issue:2	Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
AID1885023	Agonist activity at human Androgen receptor	2022	Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13	Therapeutic Strategies to Target the Androgen Receptor.
AID286658	Displacement of [3H]DHT from human AR expressed in MDA-MB-453 cells	2007	Journal of medicinal chemistry, May-17, Volume: 50, Issue:10	Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
AID1872317	Agonist activity at human Androgen receptor transfected in African green monkey CV-1 cells 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).
AID1797703	AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm061329j: \\Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.\\	2007	Journal of medicinal chemistry, May-17, Volume: 50, Issue:10	Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.
[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	2 (33.33)	18.2507
2000's	2 (33.33)	29.6817
2010's	0 (0.00)	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	3 (50.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	3 (50.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
bicalutamide bicalutamide: approved for treatment of advanced prostate cancer. N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide : A member of the class of (trifluoromethyl)benzenes that is 4-amino-2-(trifluoromethyl)benzonitrile in which one of the amino hydrogens is substituted by a 3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanoyl group.. bicalutamide : A racemate comprising of equal amounts of (R)-bicalutamide and (S)-bicalutamide. It is an oral non-steroidal antiandrogen used in the treatment of prostate cancer and hirsutism.	4.43	2	(trifluoromethyl)benzenes; monocarboxylic acid amide; monofluorobenzenes; nitrile; sulfone; tertiary alcohol
nilutamide [no description available]	3.51	1	(trifluoromethyl)benzenes; C-nitro compound; imidazolidinone	androgen antagonist; antineoplastic agent
oxandrolone Oxandrolone: A synthetic hormone with anabolic and androgenic properties.	4.43	2	17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid; oxa-steroid	anabolic agent; androgen
testosterone propionate Testosterone Propionate: An ester of TESTOSTERONE with a propionate substitution at the 17-beta position.. androgen : A sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.	3.14	1	steroid ester
medroxyprogesterone acetate [no description available]	3.51	1	20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; corticosteroid; steroid ester	adjuvant; androgen; antineoplastic agent; antioxidant; female contraceptive drug; inhibitor; progestin; synthetic oral contraceptive
fluoxymesterone Fluoxymesterone: An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women.	2.03	1	11beta-hydroxy steroid; 17beta-hydroxy steroid; 3-oxo-Delta(4) steroid; anabolic androgenic steroid; fluorinated steroid	anabolic agent; antineoplastic agent
dihydrotestosterone Dihydrotestosterone: A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.. 17beta-hydroxyandrostan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4-5 double bond has been reduced to a single bond with unspecified configuration at position 5.. 17beta-hydroxy-5alpha-androstan-3-one : A 17beta-hydroxy steroid that is testosterone in which the 4,5 double bond has been reduced to a single bond with alpha-configuration at position 5.	5.25	6	17beta-hydroxy steroid; 17beta-hydroxyandrostan-3-one; 3-oxo-5alpha-steroid	androgen; Daphnia magna metabolite; human metabolite; mouse metabolite
nitrogenase stabilizing-protective protein, bacteria [no description available]	4.13	2	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide	androgen antagonist; antineoplastic agent
hydroxyflutamide [no description available]	3.51	1
metribolone Metribolone: A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.. 17beta-hydroxy-17-methylestra-4,9,11-trien-3-one : A synthetic non-aromatisable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.	4.43	2	17beta-hydroxy steroid; 3-oxo steroid; anabolic androgenic steroid	androgen
(S)-bicalutamide (S)-bicalutamide : A N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide that is the (S)-enantiomer of bicalutamide.	3.51	1	N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
epi 001 EPI 001: an antineoplastic agent and androgen receptor antagonist; structure in first source. bisphenol A (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) ether : The (3-chloro-2-hydroxypropyl) (2,3-dihydroxypropyl) diether of bisphenol A; a small molecule that inhibits transactivation of the AR amino-terminal domain (NTD).	3.51	1	diether; organochlorine compound	androgen antagonist
pyrvinium pyrvinium: RN given refers to parent cpd; synonyms vanquin & vankin refer to pamoate[2:1]; structure in Merck Index, 9th ed, #7810. pyrvinium : A quinolinium ion that is 1-methylquinolinium substituted by dimethylamino group at position 6 and a (E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl at position 2. It is a anthelminthic drug active against pinworms. The salts of pyrvinium can also be used as anticancer agents.	3.51	1	quinolinium ion	anthelminthic drug; antineoplastic agent
tetrahydrogestrinone [no description available]	3.51	1	3-hydroxy steroid
andarine [no description available]	4.13	2	acetamides; anilide
trestolone trestolone: structure given in first source; RN given refers to (7alpha,17beta)-isomer	3.51	1
bms-564929 [no description available]	4.13	2
mk 2866 [no description available]	3.51	1
lgd 2226 [no description available]	4.8	3
mdv 3100 [no description available]	3.51	1	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
apalutamide [no description available]	3.51	1
pf 998425 [no description available]	3.51	1
lgd 3303 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	3.51	1
azd3514 AZD3514: in Phase I clinical trial in patients with castrate-resistant prostate cancer (2/2013); structure in first source	3.51	1

Condition	Relationship Strength	Studies
Age-Related Osteoporosis [description not available]	3.33	1
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	3.33	1
Androgen-Independent Prostatic Cancer [description not available]	3.33	1
Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.	3.33	1

lg 121071

Cross-References

Synonyms (18)

Protein Targets (1)

Inhibition Measurements

Activation Measurements

Biological Processes (56)

Molecular Functions (23)

Ceullar Components (8)

Bioassays (19)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.59

Study Types

lg 121071

Cross-References

Synonyms (18)

Protein Targets (1)

Inhibition Measurements

Activation Measurements

Biological Processes (56)

Molecular Functions (23)

Ceullar Components (8)

Bioassays (19)

Research

Studies (6)

Market Indicators

Research Demand Index: 17.59

Study Types

Related Drugs (24)

Related Conditions (4)