Page last updated: 2024-11-05

gestrinone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Gestrinone: A non-estrogenic contraceptive which is a weak progestin with strong anti-progesterone properties. It is effective if used once a week orally or can also be used in intravaginal devices. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID27812
CHEMBL ID1868702
CHEBI ID89642
SCHEMBL ID217651
MeSH IDM0009218

Synonyms (74)

Synonym
AB01275442-01
dimetriose
gestrinone
a-46745
r-2323
ru-2323
dimetrose
nemestran
(17alpha)-13-ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one
16320-04-0
D04317
gestrinone (usan/inn)
tridomose
13-ethyl-17-alpha-ethinyl-17-hydroxygon-4,9,11-trien-3-one
gestrigone
18,19-dinor-17-alpha-pregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-
gestrinona [inn-spanish]
pregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-18,19-dinor-, (17alpha)-
13-beta-ethyl-17-alpha-ethinyl-17-hydroxy-gona-4,9,11-triene-3-one
brn 5610726
ru 2323
a 46745
13-ethyl-17-hydroxy-18,19-dinor-17alpha-pregna-4,9,11-trien-20-yn-3-one
ethylnorgestrienone
gestrinonum [inn-latin]
18,19-dinorpregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-, (17-alpha)-
NCGC00167457-01
HMS2089K16
(8s,13s,14s,17r)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,14,15,16-octahydrocyclopenta[a]phenanthren-3-one
r 2323
1421533rcm ,
gestrinona
unii-1421533rcm
a 46 745
gestrinone [usan:inn:ban]
gestrinonum
cas-16320-04-0
dtxcid603094
dtxsid4023094 ,
tox21_112461
chebi:89642 ,
CHEMBL1868702
a-46-745
AKOS015894932
gestrinone [mi]
pregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-18,19-dinor-, (17.alpha.)-
gestrinone [jan]
gestrinone [inn]
18,19-dinorpregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-, (17.alpha.)-
gestrinone [who-dd]
gestrinone [mart.]
gestrinone [usan]
SCHEMBL217651
bdbm50423515
CCG-220967
NCGC00167457-02
tox21_112461_1
G0436
(10s,11s,14r,15s)-15-ethyl-14-ethynyl-14-hydroxytetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6,16-trien-5-one
sr-01000872705
SR-01000872705-1
13-ethyl-17a-ethynyl-17b-hydroxygona-4,9,11-trien-3-one
13-ethyl-17-hydroxy-18,19-dinor-17a-pregna-4,9,11-trien-20-yn-3-one
(17a)-13-ethyl-17-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one
J-010018
HMS3715A15
18,19-dinorpregna-4,9,11-trien-20-yn-3-one, 13-ethyl-17-hydroxy-, (17alpha)-
CS-6362
HY-101405
DB11619
Q3761406
3,5-di-tert-butyl-4-hydroxycinnamicacid
D90768
13-ethyl-17alpha-hydroxy-18,19-dinorpregna-4,9,11-trien-20-yn-3-one

Research Excerpts

Overview

Gestrinone is an effective antiestrogen that induces endometrial atrophy and/or amenorrhea. Gestrinone (R 2323) is a synthetic progestogen, and noteworthy agent for endometriosis treatment.

ExcerptReferenceRelevance
"Gestrinone is an effective antiestrogen that induces endometrial atrophy and/or amenorrhea."( Evaluation of safety and effectiveness of gestrinone in the treatment of endometriosis: a systematic review and meta-analysis.
de Mello Gindri, I; de Mello Roesler, CR; de Souza Pinto, LP; Dos Santos, IK; Ferrari, G, 2023
)
1.9
"Gestrinone is a synthetic steroid hormone with anti-estrogenic and anti-progesterone properties. "( Enzyme-linked immunosorbent assays for the synthetic steroid gestrinone.
Brun, EM; Hernández-Albors, A; Maquieira, A; Puchades, R; Ventura, R, 2010
)
2.04
"Gestrinone (R 2323) is a synthetic progestogen, and noteworthy agent for endometriosis treatment. "( [The effect of a synthetic progestin (R 2323) on gonadal and endometrial cells in vitro and in vivo].
Kadota, T; Okamura, Y; Otsuka, H; Yoshida, K, 1985
)
1.71

Effects

Gestrinone has been shown to reduce uterine volume and stop bleeding in women with uterine leiomyomata. It has antiestrogenic, antiprogesterone, and weak androgenic properties.

ExcerptReferenceRelevance
"Gestrinone has a biophysical antiestrogenic effect. "( Antiestrogenic effect of gestrinone as an inhibitor of [3H]-estradiol binding to nuclear type II sites.
Honjo, H; Hosoda, S; Kitagawa, I; Ohno, Y; Okada, H; Tamura, H; Yamashita, S, 1991
)
2.03
"Gestrinone has been shown to reduce uterine volume and stop bleeding in women with uterine leiomyomata. "( Gestrinone in the treatment of uterine leiomyomata: effects on uterine blood supply.
Giulini, S; Jasonni, VM; La Marca, A; Orvieto, R; Vito, G; Volpe, A, 2004
)
3.21
"1. Gestrinone has been used for treatment of pelvic endometriosis, in doses of 2.5 mg twice a week. "( Rationale for frequency and dose of administration in gestrinone therapy for pelvic endometriosis in the experimental model of rabbit uterus.
Ban, H; Imai, A; Mori, H; Tamaya, T; Wada, K, 1991
)
1.15
"Gestrinone has a biophysical antiestrogenic effect. "( Antiestrogenic effect of gestrinone as an inhibitor of [3H]-estradiol binding to nuclear type II sites.
Honjo, H; Hosoda, S; Kitagawa, I; Ohno, Y; Okada, H; Tamura, H; Yamashita, S, 1991
)
2.03
"Gestrinone has antiestrogenic, antiprogesterone, and weak androgenic properties."( [Antiprogestins].
Göretzlehner, G; Köhler, G, 1988
)
1
"Gestrinone has no significant antitumor activity in hormone-sensitive breast cancer."( Oral gestrinone: a novel antiprogestin with no antitumor activity in endocrine-sensitive breast cancer.
Coombes, RC; Cunningham, D; Ford, HT; Gazet, JC, 1987
)
1.51

Actions

ExcerptReferenceRelevance
"Gestrinone blocked the increase of estrogen binding of nuclear type II sites and uterine weight in the estrogen-treated immature rabbit."( Antiestrogenic effect of gestrinone as an inhibitor of [3H]-estradiol binding to nuclear type II sites.
Honjo, H; Hosoda, S; Kitagawa, I; Ohno, Y; Okada, H; Tamura, H; Yamashita, S, 1991
)
1.31

Treatment

ExcerptReferenceRelevance
"Treatment with gestrinone decreased serum concentrations of T during the second treatment cycle and effected a major decrease in SHBG during both treatment cycles, resulting in highly increased free T and free E2 indices."( Effect of gestrinone in endometriosis tissue and endometrium.
Isomaa, V; Kauppila, A; Rönnberg, L; Vierikko, P; Vihko, R, 1985
)
1.01

Toxicity

Gestrinone showed the same adverse events and increased the risk of acne and seborrhea. Based limited evidence available suggests that gestrinone appeared to be safe and may have some efficacy advantages over danazol.

ExcerptReferenceRelevance
"5 mg given twice a week for six months provides an effective and safe treatment for those women suffering from endometriosis."( The efficacy and safety of a 19 nor-steroid in the treatment of endometriosis.
Chang, SP; Chen, CR; Ng, HT; Tsan, SH; Yang, TS, 1996
)
0.29
" The secondary outcomes embrace hormones parameters, pregnancy rate and adverse events."( Evaluation of safety and effectiveness of gestrinone in the treatment of endometriosis: a systematic review and meta-analysis.
de Mello Gindri, I; de Mello Roesler, CR; de Souza Pinto, LP; Dos Santos, IK; Ferrari, G, 2023
)
1.17
" Regarding the side effects observed, gestrinone showed the same adverse events and increased the risk of acne and seborrhea when compared to other treatments."( Evaluation of safety and effectiveness of gestrinone in the treatment of endometriosis: a systematic review and meta-analysis.
de Mello Gindri, I; de Mello Roesler, CR; de Souza Pinto, LP; Dos Santos, IK; Ferrari, G, 2023
)
1.45
"Based limited evidence available suggests that gestrinone appeared to be safe and may have some efficacy advantages over danazol, as well as other therapeutic interventions for treating endometriosis."( Evaluation of safety and effectiveness of gestrinone in the treatment of endometriosis: a systematic review and meta-analysis.
de Mello Gindri, I; de Mello Roesler, CR; de Souza Pinto, LP; Dos Santos, IK; Ferrari, G, 2023
)
1.43
" After literature screening, data extraction and quality evaluation, effective rate, recurrence rate, pregnancy rate and adverse reaction rate were used as outcome indicators to evaluate the efficacy and safety of drugs."( Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: A systematic review and network meta-analysis.
Ma, R; Mao, H; Wang, L; Xu, H; Zhang, L; Zhao, R; Zheng, Y, 2023
)
0.91
" Adverse reaction rate: the application of dienogest, leuprolide, danazol, gestrinone, mifepristone and LNG-IUS after EMT fertility preservation surgery was higher than that of placebo."( Efficacy and safety of different subsequent therapies after fertility preserving surgery for endometriosis: A systematic review and network meta-analysis.
Ma, R; Mao, H; Wang, L; Xu, H; Zhang, L; Zhao, R; Zheng, Y, 2023
)
1.14

Compound-Compound Interactions

The aim of this study was to determine clinical performance of gestrinone combined with ultrasound-guided aspiration and ethanol injection in treating chocolate cyst of ovary.

ExcerptReferenceRelevance
"The aim of this study was to determine clinical performance of gestrinone combined with ultrasound-guided aspiration and ethanol injection in treating chocolate cyst of ovary."( Gestrinone combined with ultrasound-guided aspiration and ethanol injection for treatment of chocolate cyst of ovary.
Wu, X; Xu, Y, 2015
)
2.1
"Gestrinone combined with ultrasound-guided aspiration and ethanol injection therapy is an effective treatment for ovarian chocolate cyst with low recurrence rate."( Gestrinone combined with ultrasound-guided aspiration and ethanol injection for treatment of chocolate cyst of ovary.
Wu, X; Xu, Y, 2015
)
3.3

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Treatment of endometriosis with gestrinone offers the advantage of effective clearing of lesions with relatively low dosage. Tetrahydrogestrinone and trenbolone displayed a bell-shaped dose-response curve. maximal effects observed at 3 and 30 microM, respectively.

ExcerptRelevanceReference
" Treatment of endometriosis with gestrinone offers the advantage of effective clearing of lesions with relatively low dosage and frees the patient from the daily administration of drugs required by similar conservative hormonal therapies."( Treatment of endometriosis with gestrinone (R-2323), a synthetic antiestrogen, antiprogesterone.
Coutinho, EM, 1982
)
0.83
" The efficacy, dosing regimens, effects on menstruation and fertility, recurrence rates and potential adverse effects, with particular emphasis on bone loss, of alternative therapies are compared."( Considerations in selecting appropriate medical therapy for endometriosis.
Dawood, MY, 1993
)
0.29
" Three unknown peaks were found by HPLC which are probably the metabolites of gestrinone, and conjugated gestrinone in dosed human urine."( Determination and excretion study of gestrinone in human urine by high performance liquid chromatography and gas chromatography/mass spectrometry.
Kim, M; Kim, Y; Lee, W; Lee, Y; Yim, YH, 2000
)
0.81
" When the chromatograms of blank, spiked urine and dosed urine were compared by HPLC, two unknown metabolites were found and these were excreted as the conjugated forms."( Determination of the metabolites of gestrinone in human urine by high performance liquid chromatography, liquid chromatography/mass spectrometry and gas chromatography/mass spectrometry.
Kim, M; Kim, Y; Lee, W; Lee, Y; Yim, YH, 2000
)
0.58
" Tetrahydrogestrinone and trenbolone displayed a bell-shaped dose-response curve, with maximal effects observed at 3 and 30 microM, respectively."( Induction of micronuclei in V79 cells by the anabolic doping steroids tetrahydrogestrinone and trenbolone.
Bolt, HM; Degen, GH; Diel, P; Dorn, SB; Thevis, M, 2008
)
0.96
"To investigate the incidence, influencing factors and intervention of gestrinone-related abnormal uterine bleeding at different dosage of gestrinone in the clinical treatment."( [Research of gestrinone-related abnormal uterine bleeding and the intervention in the treatment: a multi-center, randomized, controlled clinical trial].
Cao, LR; Chen, L; Duan, H; Hao, M; Peng, YZ; Tang, J; Wang, S; Wang, X; Yu, JJ; Zhang, SC, 2016
)
1.04
" (2) Univariate analysis showed that the dosage and ovarian size were the significant factors for abnormal uterine bleeding (OR=0."( [Research of gestrinone-related abnormal uterine bleeding and the intervention in the treatment: a multi-center, randomized, controlled clinical trial].
Cao, LR; Chen, L; Duan, H; Hao, M; Peng, YZ; Tang, J; Wang, S; Wang, X; Yu, JJ; Zhang, SC, 2016
)
0.8
" It is a more optimied dosage of gestrinone and without severe side effects."( [Research of gestrinone-related abnormal uterine bleeding and the intervention in the treatment: a multi-center, randomized, controlled clinical trial].
Cao, LR; Chen, L; Duan, H; Hao, M; Peng, YZ; Tang, J; Wang, S; Wang, X; Yu, JJ; Zhang, SC, 2016
)
1.08
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oxo steroid
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (35)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency9.77170.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency12.19970.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency20.15490.173734.304761.8120AID1346859; AID1346924
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID504865
SMAD family member 3Homo sapiens (human)Potency20.15490.173734.304761.8120AID1346859; AID1346924
TDP1 proteinHomo sapiens (human)Potency11.38850.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency24.82250.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency5.59550.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID743035; AID743036; AID743040; AID743042; AID743053; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency23.71010.000657.913322,387.1992AID1259378
progesterone receptorHomo sapiens (human)Potency0.05150.000417.946075.1148AID1346784; AID1347036
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.23020.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.37900.000214.376460.0339AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency8.13370.003041.611522,387.1992AID1159552; AID1159553; AID1159555
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency25.14280.001530.607315,848.9004AID1224848; AID1224849; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency23.31560.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency20.53470.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency9.82760.000229.305416,493.5996AID1259244; AID1259248; AID1259383; AID743069; AID743075; AID743077; AID743079; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency0.97720.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency26.60110.001024.504861.6448AID743212
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency30.10650.001019.414170.9645AID743094
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.70170.023723.228263.5986AID743222; AID743223
thyroid stimulating hormone receptorHomo sapiens (human)Potency10.59090.001628.015177.1139AID1224895
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency35.48130.10009.191631.6228AID1346983
Histone H2A.xCricetulus griseus (Chinese hamster)Potency12.32620.039147.5451146.8240AID1224845; AID1224896
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.65590.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency35.53200.000627.21521,122.0200AID743202; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency16.13660.005612.367736.1254AID624032
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency13.33320.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency13.25460.00339.158239.8107AID1347407
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency13.33320.001551.739315,848.9004AID1259244
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency13.42160.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency11.88320.011912.222168.7989AID651632
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sex hormone-binding globulinHomo sapiens (human)Kd0.00780.00020.34964.7863AID318680
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (48)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
androgen bindingSex hormone-binding globulinHomo sapiens (human)
protein bindingSex hormone-binding globulinHomo sapiens (human)
steroid bindingSex hormone-binding globulinHomo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionSex hormone-binding globulinHomo sapiens (human)
extracellular exosomeSex hormone-binding globulinHomo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (72)

Assay IDTitleYearJournalArticle
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID74377Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID162613Relative binding affinity for progestin receptor of uterus of rabbit at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID126435Relative binding affinity for mineralocorticoid receptor of rat kidney at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID39320Relative binding affinity for androgen receptor of prostate of rat at 2 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID74375Relative binding affinity to glucocorticoid receptor on cytosol from liver at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1150123Relative binding affinity to rabbit progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID74378Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID162462Relative binding affinity to the progesterone receptor.1994Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
PRO_LIGAND: an approach to de novo molecular design. 2. Design of novel molecules from molecular field analysis (MFA) models and pharmacophores.
AID74389Relative binding affinity against glucocorticoid receptor1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Correspondence analysis applied to steroid receptor binding.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID212922Relative binding affinity to the testosterone receptor.1994Journal of medicinal chemistry, Nov-11, Volume: 37, Issue:23
PRO_LIGAND: an approach to de novo molecular design. 2. Design of novel molecules from molecular field analysis (MFA) models and pharmacophores.
AID126441Relative binding affinity for the mineralocorticoid receptor1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Correspondence analysis applied to steroid receptor binding.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID69853Relative binding affinity against Estrogen receptor1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Correspondence analysis applied to steroid receptor binding.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID213396Glucocorticoid induced Tyrosine Aminotransferase activity relative to Dexamethasone1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID318680Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
An updated steroid benchmark set and its application in the discovery of novel nanomolar ligands of sex hormone-binding globulin.
AID39454Relative binding affinity against androgen receptor1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Correspondence analysis applied to steroid receptor binding.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID74374Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID74373Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 24 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID162617Relative binding affinity against progestin receptor1986Journal of medicinal chemistry, Jan, Volume: 29, Issue:1
Correspondence analysis applied to steroid receptor binding.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID74376Relative binding affinity to glucocorticoid receptor on cytosol from liver at 4 hr1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (213)

TimeframeStudies, This Drug (%)All Drugs %
pre-199060 (28.17)18.7374
1990's58 (27.23)18.2507
2000's59 (27.70)29.6817
2010's23 (10.80)24.3611
2020's13 (6.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 47.74

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index47.74 (24.57)
Research Supply Index5.56 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index75.68 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (47.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials39 (17.73%)5.53%
Reviews42 (19.09%)6.00%
Case Studies5 (2.27%)4.05%
Observational0 (0.00%)0.25%
Other134 (60.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase II, Randomized, Placebo-controlled, Double-blind, Multicenter Study to Investigate the Safety and Exploratory Efficacy of a Subdermal Implant-bioabsorbable Gestrinone Pellet for Pelvic Pain Secondary to Endometriosis Treatment [NCT05570786]Phase 2100 participants (Anticipated)Interventional2023-02-13Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]