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.
ID Source | ID |
---|---|
PubMed CID | 27812 |
CHEMBL ID | 1868702 |
CHEBI ID | 89642 |
SCHEMBL ID | 217651 |
MeSH ID | M0009218 |
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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Gestrinone has been shown to reduce uterine volume and stop bleeding in women with uterine leiomyomata. It has antiestrogenic, antiprogesterone, and weak androgenic properties.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Class | Description |
---|---|
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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
acetylcholinesterase | Homo sapiens (human) | Potency | 9.7717 | 0.0025 | 41.7960 | 15,848.9004 | AID1347398 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 12.1997 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
SMAD family member 2 | Homo sapiens (human) | Potency | 20.1549 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
SMAD family member 3 | Homo sapiens (human) | Potency | 20.1549 | 0.1737 | 34.3047 | 61.8120 | AID1346859; AID1346924 |
TDP1 protein | Homo sapiens (human) | Potency | 11.3885 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 24.8225 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 5.5955 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID1259381; AID743035; AID743036; AID743040; AID743042; AID743053; AID743063 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 23.7101 | 0.0006 | 57.9133 | 22,387.1992 | AID1259378 |
progesterone receptor | Homo sapiens (human) | Potency | 0.0515 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1347036 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.2302 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 0.3790 | 0.0002 | 14.3764 | 60.0339 | AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 8.1337 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159553; AID1159555 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 25.1428 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 23.3156 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 20.5347 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 9.8276 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID1259383; AID743069; AID743075; AID743077; AID743079; AID743080; AID743091 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 0.9772 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 26.6011 | 0.0010 | 24.5048 | 61.6448 | AID743212 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 30.1065 | 0.0010 | 19.4141 | 70.9645 | AID743094 |
vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 28.7017 | 0.0237 | 23.2282 | 63.5986 | AID743222; AID743223 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 10.5909 | 0.0016 | 28.0151 | 77.1139 | AID1224895 |
nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 35.4813 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 12.3262 | 0.0391 | 47.5451 | 146.8240 | AID1224845; AID1224896 |
vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 89.1251 | 0.3548 | 28.0659 | 89.1251 | AID504847 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 24.6559 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 35.5320 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 16.1366 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 13.3332 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 13.2546 | 0.0033 | 9.1582 | 39.8107 | AID1347407 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 13.3332 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 13.4216 | 0.0119 | 17.9420 | 71.5630 | AID651632; AID720516 |
Ataxin-2 | Homo sapiens (human) | Potency | 11.8832 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
[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) |
---|---|---|---|---|---|---|---|
Sex hormone-binding globulin | Homo sapiens (human) | Kd | 0.0078 | 0.0002 | 0.3496 | 4.7863 | AID318680 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID1079936 | Choleostatic 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] | |||
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID1079935 | Cytolytic 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] | |||
AID74377 | Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 24 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID162613 | Relative binding affinity for progestin receptor of uterus of rabbit at 24 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID126435 | Relative binding affinity for mineralocorticoid receptor of rat kidney at 24 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID39320 | Relative binding affinity for androgen receptor of prostate of rat at 2 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID74375 | Relative binding affinity to glucocorticoid receptor on cytosol from liver at 24 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1150123 | Relative binding affinity to rabbit progesterone receptor | 1977 | Journal of medicinal chemistry, Sep, Volume: 20, Issue:9 | Quantitative relationships between steroid structure and binding to putative progesterone receptors. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID74378 | Relative binding affinity to glucocorticoid receptor on cytosol from thymus at 4 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID162462 | Relative binding affinity to the progesterone receptor. | 1994 | Journal 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. |
AID74389 | Relative binding affinity against glucocorticoid receptor | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Correspondence analysis applied to steroid receptor binding. |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID212922 | Relative binding affinity to the testosterone receptor. | 1994 | Journal 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. |
AID126441 | Relative binding affinity for the mineralocorticoid receptor | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Correspondence analysis applied to steroid receptor binding. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID69853 | Relative binding affinity against Estrogen receptor | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Correspondence analysis applied to steroid receptor binding. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID213396 | Glucocorticoid induced Tyrosine Aminotransferase activity relative to Dexamethasone | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID318680 | Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin | 2008 | Journal 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. |
AID39454 | Relative binding affinity against androgen receptor | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Correspondence analysis applied to steroid receptor binding. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID74374 | Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 4 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID1079931 | Moderate 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] | |||
AID1079933 | Acute 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 | |||
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1079938 | Chronic 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] | |||
AID74373 | Relative binding affinity to glucocorticoid receptor on cytosol from hepatoma tissue cells at 24 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID162617 | Relative binding affinity against progestin receptor | 1986 | Journal of medicinal chemistry, Jan, Volume: 29, Issue:1 | Correspondence analysis applied to steroid receptor binding. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID74376 | Relative binding affinity to glucocorticoid receptor on cytosol from liver at 4 hr | 1988 | Journal of medicinal chemistry, Jun, Volume: 31, Issue:6 | Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 60 (28.17) | 18.7374 |
1990's | 58 (27.23) | 18.2507 |
2000's | 59 (27.70) | 29.6817 |
2010's | 23 (10.80) | 24.3611 |
2020's | 13 (6.10) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (47.74) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 39 (17.73%) | 5.53% |
Reviews | 42 (19.09%) | 6.00% |
Case Studies | 5 (2.27%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 134 (60.91%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
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 2 | 100 participants (Anticipated) | Interventional | 2023-02-13 | Recruiting | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |