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androstenedione

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Description

Androstenedione: A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

androst-4-ene-3,17-dione : A 3-oxo Delta(4)-steroid that is androst-4-ene substituted by oxo groups at positions 3 and 17. It is a steroid hormone synthesized in the adrenal glands and gonads. [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]

Cross-References

ID SourceID
PubMed CID6128
CHEMBL ID274826
CHEBI ID16422
SCHEMBL ID23272
MeSH IDM0001113

Synonyms (118)

Synonym
BIDD:PXR0101
adione
MLS002152886
gtpl2860
delta(4)-androsten-3,17-dione
CHEBI:16422 ,
delta(4)-androstene-3,17-dione
MLS000028510 ,
smr000058281
hsdb 7335
nsc 9563
einecs 200-554-5
LMST02020007
EU-0100114
D00051
androstenedione (jan)
skf 2170
.delta.4-androstene-3,17-dione
.delta.-(sup4)-androsten-3,17-dione
nsc-9563
3,17-dioxoandrost-4-ene
nsc9563
wln: l e5 b666 fv ov mutj a1 e1
4-androstene-3-17-dione
LOPAC0_000114
117598-81-9
delta-4-androsten-3,17-dione
androtex
(8r,9s,10r,13s,14s)-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthrene-3,17-dione
androsten-3,17-dione
delta(sup 4)-androstene-3,17-dione
fecundin
delta-4-androstenedione
17-ketotestosterone
delta-(sup4)-androsten-3,17-dione
4-androstenedione
NCGC00023902-04
NCGC00023902-03
C1015
4-androstene-3,17-dione
androst-4-ene-3,17-dione
C00280
63-05-8
androstenedione
DB01536
NCGC00023902-06
4-androsten-3,17-dione
NCGC00023902-07
SPECTRUM5_002059
NCGC00023902-05
delta4-androstene-3,17-dione
A 9630
androstendione
androstenedione; 3,17-dioxo-4-andostene
AC-11042
8F5F4DCB-1164-4F2C-B4E3-3B74F684B189
MLS000563086
CHEMBL274826 ,
FT-0657562
STK801871
AKOS005622710
NCGC00023902-08
NCGC00254238-01
NCGC00259818-01
tox21_202269
tox21_300579
A0845
dtxsid8024523 ,
cas-63-05-8
dtxcid204523
tox21_110893
CCG-204209
HMS2231F18
bdbm91713
androst-4-en-3,17-dione, 2
ec 200-554-5
unii-409j2j96vr
409j2j96vr ,
androstenedione [jan]
delta-4-androstene-3,17-dione
EPITOPE ID:135869
testosterone impurity a [ep impurity]
androstenedione [hsdb]
androstenedione [mart.]
androstenedione [who-dd]
androstenedione [vandf]
androstenedione [mi]
4-andendion
BBL033517
SCHEMBL23272
tox21_110893_1
NCGC00023902-09
(8r,9s,10r,13s,14s)-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-1h-cyclopenta[a]phenanthrene-3,17(2h,6h)-dione
androst-4-en-3,17-dione
W-104936
.delta.4-androsten-3,17-dione
AC-33197
OPERA_ID_1694
estr-5-ene-3,17-diol,(3b,17b)-
SR-01000003096-4
sr-01000003096
4-androstene-3,17-dione, vetranal(tm), analytical standard
androstenedione (androst-4-ene-3,17-dione) 1.0 mg/ml in acetonitrile
androst-4-ene-3,17-dione (androstenedione)
sr-01000075697
SR-01000075697-1
(4)-androsten-3,17-dione
d4-androstene-3,17-dione
[4-14c]androst-4-ene-3,17-dione
delta4-androstenedione
[4-14c]-androstenedione
Q411064
VS-12118
(3as,3br,9ar,9bs,11as)-9a,11a-dimethyl-1h,2h,3h,3ah,3bh,4h,5h,7h,8h,9h,9ah,9bh,10h,11h,11ah-cyclopenta[a]phenanthrene-1,7-dione
androst-4-ene-3,17-dione; 17-ketotestosterone; androstenedione; 4-androstene-3,17-dione; 4-androstenedione
testosterone ep impurity a
(8r,10r,13s)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-2h-cyclopenta[a]phenanthrene-3,17-dione
androstenedione, 1mg/ml in methanol

Research Excerpts

Overview

Androstenedione (AD) is a key intermediate in the body's steroid metabolism. It is used as a precursor for several steroid substances, such as testosterone, estradiol, testolactone, progesterone, cortisone, cortisol, prednisone, and prednisolone. D4-androstenedion (D4ASD) is an intermediate hormone of androgen biosynthesis by the gonads and the adrenal glands.

ExcerptReferenceRelevance
"Androstenedione is a steroidal hormone produced in male and female gonads, as well as in the adrenal glands, and it is known for its key role in the production of estrogen and testosterone. "( Androstenedione (a Natural Steroid and a Drug Supplement): A Comprehensive Review of Its Consumption, Metabolism, Health Effects, and Toxicity with Sex Differences.
Badawy, MT; Farag, MA; Sobeh, M; Xiao, J, 2021
)
3.51
"Androstenedione (AD) is a key intermediate in the body's steroid metabolism, used as a precursor for several steroid substances, such as testosterone, estradiol, ethinyl estradiol, testolactone, progesterone, cortisone, cortisol, prednisone, and prednisolone. "( Biotransformation of Phytosterols into Androstenedione-A Technological Prospecting Study.
Amaral, PFF; Ferreira, TF; Fraga, JL; Nunes, VO; Pessoa, FLP; Vanzellotti, NC, 2022
)
2.43
"D4-androstenedione (D4ASD) is an intermediate hormone of androgen biosynthesis by the gonads and the adrenal glands. "( Assessment of the Androstenedione Assay on a Roche Analytical Platform and Comparison with Different Methods.
Bizumukama, L; Cotton, F; Deprez, G; Duterme, C; Goff, CL; Peeters, S; Ruth, I; Wolff, F, 2023
)
1.87
"Androstenedione (AED) is a typical EDC."( An effect assessment of microplastics and nanoplastics interacting with androstenedione on mosquitofish (Gambusia affinis).
Wang, Q; Ye, B; Zhang, C; Zou, J; Zuo, Z, 2023
)
1.86
"Androstenedione (AD) is an important steroid medicine intermediate that is obtained via the degradation of phytosterols by mycobacteria. "( Improving phytosterol biotransformation at low nitrogen levels by enhancing the methylcitrate cycle with transcriptional regulators PrpR and GlnR of Mycobacterium neoaurum.
Luo, J; Shen, Y; Wang, L; Wang, M; Wang, X; Xia, M; Zhang, Y; Zhou, X, 2020
)
2
"Androstenedione (A4) is an adrenal and gonadal steroid biomarker, useful in the assessment of children in whom steroidogenic disorders are suspected. "( Prospective and Descriptive Study on Serum Androstenedione Concentration in Healthy Children from Birth until 18 Years of Age and Its Associated Factors.
Ballerini, MG; Chiesa, A; Gaido, V; Rodríguez, ME; Ropelato, MG, 2017
)
2.16
"Androstenedione (AED) is a naturally occurring steroid hormone. "( Masculinization and reproductive effects in western mosquitofish (Gambusia affinis) after long-term exposure to androstenedione.
Cheng, XM; Fang, GZ; Hou, LP; Shi, WJ; Shu, H; Xin, L; Yang, Y; Yao, L; Ying, GG; Zhao, JL, 2018
)
2.13
"Androstenedione is an androgen and intermediate in the biosynthesis of most adrenocortical, anabolic, sex and synthetic steroids, such as canrenone, eplerenone, norethindrone and spironolactone. "( Refining androstenedione and bisnorcholenaldehyde from mother liquor of phytosterol fermentation using macroporous resin column chromatography followed by crystallization.
Jiang, BH; Liu, ZZ; Ning, FH; Xu, HX; Xu, SD, 2018
)
2.34
"Androstenedione is an androgen produced as an intermediate product of the biosynthesis of testosterone and estradiol in testicles, ovaries and also in the adrenal cortex. "( Cross-method comparison of serum androstenedione measurement with respect to the validation of a new fully automated chemiluminescence immunoassay.
van Helden, J; Weiskirchen, R, 2018
)
2.2
"Androstenedione (A4) is an androgen that can be metabolized by aromatase to estrone, but the effects of A4 on endometrial cell proliferation either as an androgen or via conversion to estrogens are unknown. "( Inhibitory effects of androstenedione on endometrial cells: implications for poor reproductive outcome among women with androgen excess.
Han, M; Park, SB, 2013
)
2.15
"Androstenedione is an androgen hormone and a precursor for testosterone and estrone synthesis. "( Immunoanalytical profile of androstenedione.
Doggui, R, 2016
)
2.17
"Androstenedione (AD) is a steroid intermediate used in the pharmaceutical industry for the production of several important anabolic drugs. "( Rapid screening and isolation of a fungus for sitosterol to androstenedione biotransformation.
Gomes, J; Malaviya, A, 2009
)
2.04
"Androstenedione is an androgen steroid that is normally synthesized within men and women and may be metabolized to a more potent androgen or estrogen hormone. "( Toxicology and carcinogenesis studies of androstenedione (CAS No. 63-05-8) in F344/N rats and B6C3F1 mice (gavage studies).
, 2010
)
2.07
"Androstenedione is a steroid hormone and an intermediate in the synthetic pathway of both testosterone and estradiol in men and women. "( Effects of oral androstenedione administration on serum testosterone and estradiol levels in postmenopausal women.
Catlin, DH; Finkelstein, JS; Leblanc, KM; Leder, BZ; Lee, H; Longcope, C, 2002
)
2.1
"Androstenedione is an anabolic-androgenic steroid used to increase blood testosterone levels for the purposes of increasing strength, lean body mass, and sexual performance."( Anabolic-androgenic steroids and related substances.
Bahrke, MS; Yesalis, CE, 2002
)
1.04
"4-androstenedione is an androgen that binds AR, induces AR nuclear translocation, and promotes myogenesis in vitro, with substantially lower potency than dihydrotestosterone."( Delta-4-androstene-3,17-dione binds androgen receptor, promotes myogenesis in vitro, and increases serum testosterone levels, fat-free mass, and muscle strength in hypogonadal men.
Artaza, J; Bhasin, S; Davidson, T; Gonzalez-Cadavid, N; Jasuja, R; Lee, ML; Mac, RP; Miller, A; Ramaraj, P; Singh, AB; Singh, R; Sinha-Hikim, I; Storer, TW; Taylor, WE, 2005
)
0.89
"Androstenedione is a key intermediate of microbial steroid metabolism. "( Androstenedione production by biotransformation of phytosterols.
Gomes, J; Malaviya, A, 2008
)
3.23
"Androstenedione is a testosterone precursor used by athletes to enhance performance; the lay press has recently touted this substance as an over-the-counter sexual stimulant."( Priapism after androstenedione intake for athletic performance enhancement.
Henderson, SO; Kachhi, PN, 2000
)
1.38
"Androstenedione is an agent that has received a large amount of popular press in the last year, and this has led to an surge in its usage."( Performance-enhancing supplements.
Lombardo, JA; Pecci, MA, 2000
)
1.03
"Androstenedione is a steroid hormone and the major precursor to testosterone. "( Metabolism of orally administered androstenedione in young men.
Ahrens, B; Catlin, DH; Finkelstein, JS; Leder, BZ; Longcope, C; Schoenfeld, DA, 2001
)
2.03
"Androstenedione is a steroid hormone sold over-the-counter to individuals who expect that it will enhance strength and athletic performance. "( Effects of androstenedione administration on epitestosterone metabolism in men.
Ahrens, BD; Catlin, DH; Finkelstein, JS; Hatton, CK; Leder, BZ, 2002
)
2.15

Effects

Androstenedione has been popularized by high-profile sports stars. Initial studies cast doubt about its performance-enhancing potential.

ExcerptReferenceRelevance
"Androstenedione intake has been speculated to increase plasma testosterone levels and muscle anabolism."( Androstenedione does not stimulate muscle protein anabolism in young healthy men.
Gore, DC; Rasmussen, BB; Volpi, E; Wolfe, RR, 2000
)
2.47
"Androstenedione has been popularized by high-profile sports stars, but initial studies cast doubt about its performance-enhancing potential."( Performance-enhancing substances in adolescent athletes.
Gomez, JE, 2002
)
1.04

Actions

Androstenedione did not increase cell growth in wild-type MCF-7 cells which contained relatively low aromatase activity and produced 4-fold more estrone than estradiol. Androstenedion levels were lower on both days in sows receiving DXM but not in those given ACTH compared to control values on day 19.

ExcerptReferenceRelevance
"Androstenedione levels were lower (P<0.001) and increased less after ACTH treatment in ovariectomized mares, as compared to when intact (P<0.05)."( Effect of ACTH (tetracosactide) on steroid hormone levels in the mare. Part B: effect in ovariectomized mares (including estrous behavior).
Dalin, AM; Forsberg, M; Hedberg, Y; Hoffmann, B; Kindahl, H; Ludwig, C; Lundeheim, N; Sandh, G, 2007
)
1.06
"The androstenedione level was lower in subgroup IV compared with subgroup III."( Correlation of Kupperman's index with estrogen and androgen levels, according to weight and body fat distribution in postmenopausal women from Mexico City.
Carranza-Lira, S; Chán Verdugo, R; Herrera, J; Olivares, A; Velasco Díaz, G,
)
0.61
"Androstenedione did not increase cell growth in wild-type MCF-7 cells which contained relatively low aromatase activity and produced 4-fold more estrone than estradiol."( Effect of androstenedione on growth of untransfected and aromatase-transfected MCF-7 cells in culture.
Chen, S; Korsunsky, Z; Martel, J; Santen, RJ; Santner, SJ; Zhou, D, 1993
)
1.41
"Androstenedione values were lower (p less than 0.05) on both days in sows receiving DXM but not in those given ACTH compared to control values on day 19."( Morphometric and steroid hormone changes associated with experimental anovulatory follicles in the sow.
Gee, CM; Geissinger, HD; Liptrap, RM, 1991
)
1

Treatment

Androstenedione treatment of pregnant monkeys at 0.8 of gestation reproduces endocrine, biophysical, and biochemical changes similar to those measured during spontaneous, term labor. Androstenedion or E2 treatment after fetectomy restored serum GH to 20.8 +/- 1.1 and 22.4 +/- 0.6 ng/ml, respectively.

ExcerptReferenceRelevance
"In androstenedione-treated rat ovaries, follicular cysts were formed, and apoptotic cells were found in the inner part of granulosa cell layers of antral follicles. "( Exogenous androstenedione induces formation of follicular cysts and premature luteinization of granulosa cells in the ovary.
Ishizuka, B; Itoh, MT; Okutsu, Y; Takahashi, N, 2010
)
1.38
"Androstenedione treatments increased the follicle diameters, reduced survival rates of follicles, and promoted the formation of follicles with abnormal morphology, including misshapen oocyte."( Androstenedione induces abnormalities in morphology and function of developing oocytes, which impairs oocyte meiotic competence.
Horiuchi, T; Ishizuka, B; Itoh, MT; Okutsu, Y; Takahashi, N; Tarumi, W; Tsukamoto, S, 2012
)
2.54
"Androstenedione and estradiol treatment resulted in a 75% decrease (P < 0.01) in placental whole villous CS-3 mRNA and CS protein levels, determined by Northern and Western blot analysis, on d 60, and a corresponding decrease in syncytiotrophoblast CS protein and maternal serum CS levels."( Functional differentiation of the placental syncytiotrophoblast: Effect of estrogen on chorionic somatomammotropin expression during early primate pregnancy.
Albrecht, ED; Musicki, B; Pepe, GJ, 2003
)
1.04
"Androstenedione treatment also produced changes in the level of selected free fatty acids (FFAs) in the maternal blood, brain, liver and fetal brain."( Distribution of androstenedione and its effects on total free fatty acids in pregnant rats.
Collins, TF; Flynn, TJ; Johnson, WD; Kim, CS; O'Neilll, RK; Ross, IA; Sahu, SC; Sapienza, P; Sprando, RL; Wiesenfeld, PL, 2007
)
1.41
"FF androstenedione (untreated, 50.7 +/- 30 ng/ml; clomiphene-treated, 73.4 +/- 23.4 ng/ml; hMG-treated, 60.2 +/- 19.8 ng/ml) and testosterone (6.66 +/- 2.45, 5.98 +/- 1.46, and 6.39 +/- 2.16 ng/ml, respectively) concentrations in all three patient groups were similar."( Correlation of human follicular fluid inhibin activity with spontaneous and induced follicle maturation.
Brown, J; Campeau, JD; diZerega, GS; Lobo, R; Marrs, RP; Nakamura, RM; Ujita, EL, 1984
)
0.78
"3, androstenedione treatment did not influence (P > .10) the number of CL or the number and recovery rates of d-11.5 blastocysts."( Administration of testosterone from day 13 of the estrous cycle to estrus increased the number of corpora lutea and conceptus survival in gilts.
Cárdenas, H; Pope, WF, 1997
)
0.81
"Androstenedione treatment significantly increased basal fetal plasma ACTH and decreased basal fetal plasma cortisol concentration."( Modulation of ovine fetal adrenocorticotropin secretion by androstenedione and 17beta-estradiol.
Saoud, CJ; Wood, CE, 1997
)
1.26
"Androstenedione treatment of pregnant monkeys at 0.8 of gestation reproduces endocrine, biophysical, and biochemical changes similar to those measured during spontaneous, term labor in the pregnant monkey. "( Androstenedione treatment of pregnant baboons at 0.7-0.8 of gestation promotes a premature forward shift in the nocturnal maternal plasma estradiol surge relative to progesterone and increases myometrial contraction activity.
Giussani, DA; Jenkins, SL; Nathanielsz, PW; Tame, JD; Winter, JA, 2000
)
3.19
"Androstenedione or E2 treatment after fetectomy restored serum GH to 20.8 +/- 1.1 and 22.4 +/- 0.6 ng/ml, respectively."( Influence of the fetus and estrogen on maternal serum growth hormone, insulin-like growth factor-II, and epidermal growth factor concentrations during baboon pregnancy.
Albrecht, ED; Henson, MC; Pepe, GJ; Putney, DJ, 1991
)
1
"Androstenedione treatment partially restored the normal appearance of the gland and also some secretory activity."( Pharmacologically induced ultrastructural and immunohistochemical changes in the prostate of the castrated dog.
Aumüller, G; el Etreby, MF; Habenicht, UF, 1987
)
0.99
"In androstenedione-treated baboons at midgestation the conversion of E----F (8%) was lower (P less than 0.05) than the oxidation of F----E (27%) and not different from that in untreated baboons at term (E----F = 13%; F----E = 28%)."( The regulation of transplacental cortisol-cortisone metabolism by estrogen in pregnant baboons.
Albrecht, ED; Pepe, GJ; Stahl, SJ; Waddell, BJ, 1988
)
0.79
"Upon treatment with androstenedione, there were increased associations of AIB1 and CBP with the pS2 promoter in the HER-2-overexpressing compared with control MCF-7/CA cells."( ErbB receptor signaling and therapeutic resistance to aromatase inhibitors.
Arteaga, CL; Miller, T; Shin, I, 2006
)
0.65
"Treatment with androstenedione, which was reported to be inactive in the hepatoma tissue culture cells, did not interfere with the inhibitory effect of dexamethasone at all."( Mechanisms of anti-inflammatory action of dexamethasone: blockade by hydrocortisone mesylate and actinomycin D of the inhibitory effect of dexamethasone on leukocyte infiltration in inflammatory sites.
Kurihara, A; Ojima, F; Tsurufuji, S, 1984
)
0.61
"Treatment with androstenedione (500nM) significantly (p<0.05) increased the Bmax value by 35% compared to control and hydroxyflutamide completely antagonized this effect of androstenedione."( Androstenedione increases thromboxane A2 receptors in human erythroleukemia cells.
Halushka, PV; Higashiura, K; Mathur, RS; Zucker, TP, 1996
)
2.08
"Treatment with androstenedione (300 mg/kg body weight), the first metabolite of DHEA, did not cause any significant increase in the expression of PCNA in either sham-operated controls or partially hepatectomized rats."( Dehydroepiandrosterone (DHEA) facilitates liver regeneration after partial hepatectomy in rats.
Kiba, T; Kitamura, T; Morita, K; Numata, K; Saito, S; Sekihara, H; Tanaka, K, 1999
)
0.64
"Treatment with androstenedione (Group II) resulted in stromal hyperplasia in the caudal lobe and an increase in epithelial cell height in all zones except in the central zone of the caudal lobe."( Effects of long-term administration of androgens and estrogen on rhesus monkey prostate: possible induction of benign prostatic hyperplasia.
Jeyaraj, DA; Pal, PC; Rajalakshmi, M; Sharma, RS; Udayakumar, TS,
)
0.47

Toxicity

ExcerptReferenceRelevance
"Xenobiotics may cause long-term adverse effects in humans, especially at the embryonic level, raising questions about their levels of exposure, combined effects, and crucial endpoints."( Cytotoxic effects and aromatase inhibition by xenobiotic endocrine disrupters alone and in combination.
Benachour, N; Moslemi, S; Seralini, GE; Sipahutar, H, 2007
)
0.34
"Mono-(2-ethylhexyl) phthalate (MEHP) is the most toxic metabolite of di-(2-ethylhexyl) phthalate (DEHP)."( Evaluation of ovarian toxicity of mono-(2-ethylhexyl) phthalate (MEHP) using cultured rat ovarian follicles.
Chihara, K; Fukuda, C; Funabashi, H; Inada, H; Kimura, J; Kunimatsu, T; Miyano, T; Miyawaki, I; Tateishi, Y; Yamashita, A, 2012
)
0.38
" A major interest into fungal steroid action has been provoked since research has proven that steroid hormones are toxic to fungi and affect the host/fungus relationship."( Steroid toxicity and detoxification in ascomycetous fungi.
Cvelbar, D; Kobal, K; Zakelj-Mavrič, M; Zigon, D; Zist, V, 2013
)
0.39

Pharmacokinetics

ExcerptReferenceRelevance
" The formulated material achieved a significantly higher mean peak concentration (88% greater than that obtained using the unformulated powder) and a higher mean AUC (not significant)."( Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men.
Dowsett, M; Lloyd, P, 1990
)
0.5
"Preovulatory bovine follices (n = 73) were collected at different times after the onset of oestrus until shortly before ovulation, which occurred at 24 +/- 1 X 4 h after the peak concentration of LH in the peripheral blood."( Steroid and pituitary hormone concentrations in the fluid of preovulatory bovine follicles relative to the peak of LH in the peripheral blood.
Bevers, MM; Dieleman, SJ; Poortman, J; van Tol, HT, 1983
)
0.27
"Using constant infusion of unlabeled steroid, we have studied the metabolic clearance rate (MCR), half-life (T 1/2), and conversion ratio of androstenedione (A) into androgens and estrogens throughout human pregnancy."( The metabolism of androstenedione in human pregnancy: the use of constant infusion of unlabeled steroid to assess its metabolic clearance rate, its production rate, and its conversion into androgens and estrogens.
Belisle, S; Brault, J; Lehoux, JG, 1980
)
0.8
" injection of 14C-formestane, the unchanged drug disappeared rapidly from plasma, the terminal elimination half-life being 18+/-2 min (N=3)."( Pharmacokinetics and metabolism of formestane in breast cancer patients.
Blum, W; Faigle, JW; Galli, B; Geisler, J; Gschwind, HP; Johannessen, DC; Kriemler, HP; Lønning, PE; Miller, WR; Schneider, W; Waldmeier, F; Winkler, T, 2001
)
0.31
" A comparison of liquid and freeze-dried rHCG and freeze-dried uHCG showed pharmacokinetic bioequivalence."( Pharmacokinetics and pharmacodynamics of recombinant human chorionic gonadotrophin in healthy male and female volunteers.
Khan, A; Munafo, A; Porchet, HC; Trinchard-Lugan, I,
)
0.13
"Benign prostatic hyperplasia and prostate cancer can be treated with the 5α-reductase inhibitors, finasteride and dutasteride, when pharmacodynamic biomarkers are useful in assessing response."( Simultaneous pharmacokinetic and pharmacodynamic analysis of 5α-reductase inhibitors and androgens by liquid chromatography tandem mass spectrometry.
Andrew, R; Faqehi, AM; Homer, NZ; Hughes, KA; Naredo, G; Stewart, LH; Upreti, R; Walker, BR, 2015
)
0.42

Compound-Compound Interactions

The effect of gestodene 75 micrograms (GTD) versus desogestrel 150 microgram's (DSG) combined with 30 microgramS of ethinylestradiol (EE) on acne lesions and plasma androstenedione (A) was evaluated in an open study. The validity of AMH toward the diagnosis of PCOS was estimated by receiver operating characteristic (ROC)curves.

ExcerptReferenceRelevance
"The effect of gestodene 75 micrograms (GTD) versus desogestrel 150 micrograms (DSG) combined with 30 micrograms of ethinylestradiol (EE) on acne lesions and plasma androstenedione (A), total testosterone (T), sex hormone binding globulin (SHBG) and "free androgen index" (FAI) was evaluated in an open study on 19 patients aged 18-35 years affected with postpubertal or persistent non-severe acne vulgaris."( Clinical and hormonal effects of ethinylestradiol combined with gestodene and desogestrel in young women with acne vulgaris.
Mango, D; Manna, P; Miggiano, GA; Ricci, S; Serra, GB, 1996
)
0.49
" They aimed to evaluate the effect of GTD and DSG combined with low doses of EE on acne lesions and on hormone levels."( Clinical and hormonal effects of ethinylestradiol combined with gestodene and desogestrel in young women with acne vulgaris.
Mango, D; Manna, P; Miggiano, GA; Ricci, S; Serra, GB, 1996
)
0.29
"In order to explore the effects of metformin combined with cyproterone acetate (CPA) on the clinical features, endocrine and metabolism of the patients with polycystic ovarian syndrome (PCOS), 50 cases of non-obese PCOS were randomly subjected to CPA (CPA treatment group, n = 25) and CPA+ metformin (n = 25) treatment for 6 months."( Effects of metformin combined with cyproterone acetate on clinical features, endocrine and metabolism of non-obese women with polycystic ovarian syndrome.
Liu, Y; Lv, L; Sun, Y; Tan, K, 2005
)
0.33
" In this study, we developed a new approach for endogenous metabolite quantification by the postcolumn infused-internal standard (PCI-IS) method combined with the matrix normalization factor (MNF) method."( Quantification of endogenous metabolites by the postcolumn infused-internal standard method combined with matrix normalization factor in liquid chromatography-electrospray ionization tandem mass spectrometry.
Chen, GY; Kuo, CH; Liao, HW; Liao, WC; Tsai, IL; Wu, MS, 2015
)
0.42
"To establish a cutoff level of AMH which could help for the diagnosis of PCOS, to investigate the predictive value of AMH combined with androgens in Chinese women to diagnose PCOS."( Diagnostic value of anti-Müllerian hormone combined with androgen-levels in Chinese patients with polycystic ovary syndrome.
Cheng, J; Gu, M; Jiang, L; Li, Y; Liu, L; Mueck, AO; Ruan, X; Wang, Y; Wang, Z; Xu, C; Yang, Y, 2023
)
0.91
" The validity of AMH toward the diagnosis of PCOS, or AMH combined with total testosterone, free testosterone, bioavailable testosterone and androstenedione was estimated by receiver operating characteristic (ROC)curves, and correlations between paired variables was estimated by Spearman's rank correlation coefficient."( Diagnostic value of anti-Müllerian hormone combined with androgen-levels in Chinese patients with polycystic ovary syndrome.
Cheng, J; Gu, M; Jiang, L; Li, Y; Liu, L; Mueck, AO; Ruan, X; Wang, Y; Wang, Z; Xu, C; Yang, Y, 2023
)
1.11

Bioavailability

DHEA is well absorbed and rapidly metabolized to its sulfate (DHEAS), androstenedione, and consequently to testosterone and estradiol.

ExcerptReferenceRelevance
" While this regimen effectively blocked adrenal function, it was complicated by a drug interaction in which aminoglutethimide accelerated the metabolism and reduced the bioavailability of dexamethasone."( Kinetic, hormonal and clinical studies with aminoglutethimide in breast cancer.
Harvey, H; Kendall, J; Lipton, A; Ruby, EB; Samojlik, E; Santen, RJ; Wells, SA, 1977
)
0.26
" The method has been validated for sensitivity, accuracy and precision and was found to be suitable for application to pharmacokinetic and bioavailability studies of peroral formulations of 4-OHA."( Determination of 4-hydroxyandrostenedione in plasma and urine by extractive alkylation and electron-capture gas chromatography.
Degen, PH; Schneider, W, 1991
)
0.58
"Serum levels of cortisol (C), androstenedione (A), dehydroepiandrosterone (D), estrone (E1) and estradiol (E2) were chosen as parameters to compare the bioavailability of megestrol acetate (MA) and medroxyprogesterone acetate (MPA) in postmenopausal patients with advanced breast cancer."( Adrenal steroids as parameters of the bioavailability of MA and MPA.
Dikkeschei, LD; Sleijfer, DT; Tjabbes, T; van Veelen, H; Willemse, PH, 1990
)
0.57
" A mild and heterogeneous hyperandrogenism was found in 70% of women, thus, a greater steroid bioavailability for peripheral conversion and/or a direct stimulation of the pilosebaceous unit can be postulated."( [Androgenic evaluation of women with late-onset or persistent acne].
Maneschi, F; Martorana, A; Noto, G; Palisi, F; Pandolfo, MC, 1989
)
0.28
" This model of peripheral aromatization was utilized to evaluate in vivo pharmacological parameters of MDL 18,962 (10-(2-propynyl)estr-4-ene-3,17-dione) such as bioavailability of several formulations, time course and dose responses following different routes of drug administration, pharmacokinetics and tissue distribution of [14C]MDL 18,962."( Human trophoblast xenografts in athymic mice: a model for peripheral aromatization.
Johnston, JO; Shumaker, RC; Wright, CL, 1989
)
0.28
" Adrenal steroids may serve as endocrine regulators of androgen bioavailability and bioactivity."( Endocrine interactions: adrenal steroids and precursors.
Pitha, J; Scherrer, J; Taylor, GT; Weiss, J, 1994
)
0.29
"The choice of treatment for elderly breast cancer patients needs particular care because the presence of physiological functional impairments can modify the drug bioavailability in an unpredictable manner."( Steroidal aromatase inhibitors in elderly patients.
Bajetta, E; Bichisao, E; Pozzi, P; Toffolatti, L; Zilembo, N, 2000
)
0.31
" It was found that DHEA is well absorbed and rapidly metabolized to its sulfate (DHEAS), androstenedione, and consequently to testosterone and estradiol."( Effects of transdermal application of DHEA on the levels of steroids, gonadotropins and lipids in men.
Ceska, R; Hampl, R; Hill, M; Masek, Z; Novácek, A; Stárka, L; Sulcová, J, 2000
)
0.53
" The impact of aging and of estrogen replacement therapy, particularly oral ERT, significantly reduces androgen bioavailability after menopause."( Estrogen replacement therapy: effects on the endogenous androgen milieu.
Simon, JA, 2002
)
0.31
" This may be due to a slower rate of absorption and/or a reduced diuresis, resulting in a longer period for the metabolites to accumulate in the urine."( Influence of delivery mode on the urinary excretion of nandrolone metabolites.
Dunster, PM; Grace, PB; Houghton, E; Judkins, C; Maughan, RJ; Watson, P, 2010
)
0.36
"17α-ethynyl-5α-androstane-3α, 17β-diol (HE3235, Apoptone) is an orally bioavailable synthetic analogue of 3β-androstanediol, that is active in rodent models of prostate and breast cancer, and is in Phase IIa clinical trials for the treatment of early- and late-stage prostate cancer."( 17α-alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism.
Ahlem, C; Bell, D; Delorme, E; Frincke, J; Kennedy, M; Page, T; Reading, C; Stickney, D; Villegas, S; White, S, 2012
)
0.38
" The bioavailability of ASP9521 after oral administration (1 mg/kg) was 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively."( In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
Azami, H; Baskin-Bey, E; Enjo, K; Furutani, T; Heeringa, M; Kamiyama, Y; Kikuchi, A; Kuromitsu, S; Niimi, T; Ouatas, T; Watanabe, K, 2014
)
0.4
"ASP9521 is a potent, selective, orally bioavailable AKR1C3 inhibitor."( In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
Azami, H; Baskin-Bey, E; Enjo, K; Furutani, T; Heeringa, M; Kamiyama, Y; Kikuchi, A; Kuromitsu, S; Niimi, T; Ouatas, T; Watanabe, K, 2014
)
0.4
" This implies that alterations in placental steroidogenesis and, subsequently, in the functionality or bioavailability of placental aromatase may be mechanistically involved in the pathophysiology of PE."( Placental Aromatase Is Deficient in Placental Ischemia and Preeclampsia.
Dobierzewska, A; España-Perrot, PP; Figueroa-Diesel, H; González, MI; Guzmán-Rojas, AM; Illanes, SE; Irarrazabal, CE; Monteiro, LJ; Palominos-Rivera, M; Perez-Sepulveda, A; Varas-Godoy, M; Venegas-Araneda, P, 2015
)
0.42
"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

No significant correlations between blood pressure and serum renin, androstenedione and 17-OHP levels and fludrocortisone dosage were found. Total testosterone, estrone, estradiol, and sex hormone-binding globulin were not related to prostate cancer. Calculation of the ED50 data from dose-response curves of both peptides show that AVP is about 10(4)-fold more active than OXT.

ExcerptRelevanceReference
" When the testicular tissue pieces were incubated with different doses of HCG or dibutyryl cAMP and testosterone production was measured, identical dose-response curves for old and young tissue were obtained."( In vitro and in vivo studies on Leydig cell function in old rats.
Geiss, M; Pirke, KM; Vogt, HJ, 1978
)
0.26
" The dose-response curves of all the test agents expressed in terms of percentage inhibition were approximately parallel to each other."( Anti-androgen TSAA-291. I. Anti-androgenic effects of a new steroid TSAA-291 (16 beta-ethyl-17 beta-hydroxy-4-oestren-3-one) and its derivatives.
Masaki, T; Masuoka, M; Nakayama, R; Shimamoto, K, 1979
)
0.26
" A logarithmic dose-response was obtained with female hypophyseal extract."( Influence of a novel hypophyseal factor on steroid metabolism in cultured hepatoma cells.
Gustafsson, JA; Larsson, A; Skett, P; Stenberg, A, 1975
)
0.25
" These results confirm the dose-response relation previously established with plasma oestrogen measurements alone."( The influence of intramuscular 4-hydroxyandrostenedione on peripheral aromatisation in breast cancer patients.
Dowsett, M; Jacobs, S; Jones, AL; Lonning, PE; MacNeill, F; Powles, TJ, 1992
)
0.55
" These findings suggest a dose-response relationship between plasma oestrogen suppression at low postmenopausal levels and objective tumour response in breast cancer."( Influence of aminoglutethimide on plasma oestrogen levels in breast cancer patients on 4-hydroxyandrostenedione treatment.
Dowsett, M; Ekse, D; Jacobs, S; Johannessen, DC; Jones, A; Lønning, PE; McNeil, F; Powles, TJ, 1992
)
0.5
" In a second experiment, the dose-response curve for oestradiol was examined."( Comparison of the adverse effects of adrenal and ovarian steroids on early pregnancy in mice.
de Catanzaro, D; MacNiven, E; Ricciuti, F, 1991
)
0.28
" Dose-response depression in both hCG- and db-cAMP-stimulated T production were seen with Cd2+, Co2+, Cu2+, Hg2+, Ni2+, and Zn2+ treatment."( Effect of cadmium and other metal cations on in vitro Leydig cell testosterone production.
Laskey, JW; Phelps, PV, 1991
)
0.28
" Dose-response curves for insulin and insulin-like growth factor I (IGF-I) were parallel, but IGF-I was approximately 23-fold more potent than insulin, suggesting that insulin was acting through IGF-I receptors."( Luteinization of porcine thecal cells in vitro.
Armstrong, DT; Engelhardt, H; Gore-Langton, RE, 1991
)
0.28
" Doubling the dose of either drug did not enhance hormone suppression, indicating that the drug dosage is maximally suppressive."( Adrenal steroids as parameters of the bioavailability of MA and MPA.
Dikkeschei, LD; Sleijfer, DT; Tjabbes, T; van Veelen, H; Willemse, PH, 1990
)
0.28
" A dose-response relationship was seen in the endocrine and clinical performance of the CVR."( Clinical performance and endocrine profiles of contraceptive vaginal rings releasing 3-keto-desogestrel and ethinylestradiol.
Alapiessa, U; Apter, D; Assendorp, R; Cacciatore, B; Stenman, UH, 1990
)
0.28
" We conclude that a physiologic replacement dosage of cortisone acetate given once daily is not effective in controlling excessive adrenal androgen secretion in congenital adrenal hyperplasia."( Inappropriate adrenal androgen secretion with once-a-day corticosteroid therapy for congenital adrenal hyperplasia.
Clayton, GW; Eberle, AE; Keenan, BS; Lin, TH, 1990
)
0.28
" In this study, total testosterone, estrone, estradiol, and sex hormone-binding globulin were not related to prostate cancer, but plasma androstenedione showed a positive dose-response gradient."( A prospective, population-based study of androstenedione, estrogens, and prostatic cancer.
Barrett-Connor, E; Garland, C; Khaw, KT; McPhillips, JB; Wingard, DL, 1990
)
0.75
"Previous studies have shown that after dosing with tri-o-cresyl phosphate (TOCP), the testis contains more active intermediate (saligenin cyclic-o-tolyl phosphate; SCOTP) than do other organs or blood."( The interaction of Sertoli and Leydig cells in the testicular toxicity of tri-o-cresyl phosphate.
Burka, LT; Chapin, RE; Heindel, JJ; Phelps, JL; Somkuti, SG, 1990
)
0.28
" The dose-response of DHT was biphasic in the presence and absence of FSH, such that progesterone production in the presence of 8 micrograms/ml DHT was similar to basal progesterone production."( Comparative effects of androgens and catecholestrogens on progesterone production by porcine granulosa cells.
Hammond, JM; Spicer, LJ, 1988
)
0.27
" A dose-response relationship between estradiol output and the concentration of LH in media was not apparent in theca cells from F2-F5."( Ovarian steroidogenesis during follicular maturation in the domestic fowl (Gallus domesticus).
Etches, RJ; Robinson, FE, 1986
)
0.27
" A dose-response relation was apparent for these hormones; mean plasma levels increased concomitantly with cigarette consumption."( Cigarette smoking and levels of adrenal androgens in postmenopausal women.
Barrett-Connor, E; Khaw, KT; Tazuke, S, 1988
)
0.27
"40), but not for MPA and estrone, indicating better adrenal suppression by higher MPA dosage and plasma levels."( Endocrine effects of medroxyprogesterone acetate: relation between plasma levels and suppression of adrenal steroids in patients with breast cancer.
Doorenbos, H; Sleijfer, DT; Sluiter, WJ; van Veelen, H; Willemse, PH, 1985
)
0.27
" This increase was minimal and unrelated to the dose of LH at the mid-sequence stage, but a dose-response relationship was observed in hens injected following the terminal oviposition of a series."( Plasma levels of progesterone in the domestic hen related to the maturation of ovarian follicles, and changes in the secretion of progesterone by granulosa cells cultured for 24 hours.
Williams, J, 1988
)
0.27
" Calculation of the ED50 data from dose-response curves of both peptides show that AVP is about 10(4)-fold more active than OXT in inhibiting in vitro progesterone and androstenedione secretion."( Inhibitory effect of oxytocin and vasopressin on steroid release by cultured porcine luteal cells.
Jarry, H; Pitzel, L; Probst, I; Wuttke, W, 1988
)
0.47
" In the cigarette smokers, a dose-response relationship was apparent for these hormones with mean levels increasing with increasing reported cigarette consumption."( Cigarette smoking and increased endogenous estrogen levels in men.
Barrett-Connor, E; Khaw, KT, 1987
)
0.27
"Aminoglutethimide without glucocorticoid has been shown to be a clinically effective treatment for postmenopausal breast cancer in low dosage (250 mg day-1)."( Effective inhibition by low dose aminoglutethimide of peripheral aromatization in postmenopausal breast cancer patients.
Dowsett, M; Jeffcoate, SL; Santen, RJ; Santner, SJ; Smith, IE, 1985
)
0.27
" The dose-response curve for in vitro inhibition of [(3)H]thymidine uptake in leukemic blasts correlated closely with the binding affinity of glucocorticoids to the SBP, providing additional support for an essential physiologic role for SBP in steroid action."( Glucocorticoid-binding proteins in human acute lymphoblastic leukemic blast cells.
Halterman, RH; Leventhal, BG; Lippman, ME; Perry, S; Thompson, EB, 1973
)
0.25
" This latter dosage was calculated to be within the physiologic range of prolactin in blood."( Prolactin stimulates and potentiates adrenal steroid secretion in vitro.
Eldridge, JC; Lymangrover, JR, 1984
)
0.27
" LH-FSH basal levels, prolactin, TSH, TBG, thyroxine, cortisol, and androstenedione were not changed by either dosage or duration of danazol therapy."( Danazol: endocrine and endometrial effects.
Floyd, WS, 1980
)
0.5
" The lack of major effects on testosterone levels long term at this dosage probably explain why few androgen-related side effects with this drug were previously reported."( Site of action of low dose ketoconazole on androgen biosynthesis in men.
Brugmans, J; DeCoster, R; Santen, RJ; Symoens, J; Van den Bossche, H, 1983
)
0.27
" Dose-response curves were similar for each steroid, and the GnRH analogue and GnRH gave parallel curves with minimal effective concentrations being 1 and 10 ng/ml, respectively."( Effect of gonadotrophin releasing hormone upon the pattern of steroidogenesis in isolated preovulatory rat follicles.
Ekholm, C; Hedin, L; Hillensjö, T, 1984
)
0.27
"A radioimmunological method for simultaneous dosage of androstenedione, testosterone and dihyhydrotestosterone is described."( [Simultaneous radioimmunoassay of androstenedione, testosterone and dihydrotestosterone. Application to the study of Leydig cell function].
Courty, Y; Morat, M, 1980
)
0.79
" Dose-response curves showed that a maximum (or near maximum effect) was achieved at a steroid concentration of 12."( Structural requirements for steroid inhibition of sheep lymphocyte mitogenesis in vitro.
Brown, D; Heap, RB; Marrs, RW; Staples, LD, 1984
)
0.27
" If correct, two clinically available aromatase inhibitors, aminoglutethimide (AG) and testololactone (TL) could potentially be given together at lower than usual dosage with reduction of patient side effects and preservation of aromatase inhibition."( Additive effects of aminoglutethimide, testololactone, and 4-hydroxyandrostenedione as inhibitors of aromatase.
Osawa, Y; Rosen, H; Santen, RJ; Santner, SJ, 1984
)
0.5
" Long-term therapy (up to 6 months) with the 250-mg dosage showed continual suppression of estrone with no escape being observed."( In vivo effects of delta 1-testololactone on peripheral aromatization.
Barone, RM; Gambone, JC; Judd, HL; Lasley, BL; Laufer, LR; Monfort, SL, 1982
)
0.26
"Thirty-two hirsute, oligomenorrheic patients and 18 volunteer women underwent in the early follicular phase ultrasonographic evaluation of ovarian volume, echodensity, and follicle number; transvaginal color Doppler measurement of the uterine and intraovarian vessel variations; and radioimmunologic dosage of luteinizing hormone, follicle-stimulating hormone, estradiol, progesterone, testosterone, androstenedione, and other hormonal compartments."( The role of color Doppler imaging in the diagnosis of polycystic ovary syndrome.
Artini, PG; Battaglia, C; D'Ambrogio, G; Genazzani, AD; Genazzani, AR, 1995
)
0.46
" To distinguish between these possibilities, we have analyzed the ovarian steroid responses to nafarelin for the apparent efficiency of the steroidogenic steps and the apparent dose-response relationships between blood LH and steroid levels."( Studies of the nature of 17-hydroxyprogesterone hyperresonsiveness to gonadotropin-releasing hormone agonist challenge in functional ovarian hyperandrogenism.
Barnes, RB; Ehrmann, DA; Rosenfield, RL, 1994
)
0.29
" Six families acknowledged difficulty in adhering to the daily dosing schedule."( Long-term testolactone therapy for precocious puberty in girls with the McCune-Albright syndrome.
Cutler, GB; Feuillan, PP; Jones, J, 1993
)
0.29
" At the single dosage administered, estrone and estradiol produced all females at a male-producing incubation temperature."( The relative effectiveness of androstenedione, testosterone, and estrone, precursors to estradiol, in sex reversal in the red-eared slider (Trachemys scripta), a turtle with temperature-dependent sex determination.
Bergeron, JM; Cantú, AR; Crews, D; Rhen, T, 1995
)
0.58
"A LA dose-response study was done in women receiving depot LA plus estrogen-progestin replacement."( Dose-response effect of depot leuprolide acetate on serum androgens in hirsute women.
Arab, DM; Lehman, L; Rittmaster, RS, 1996
)
0.29
" Dose-response studies revealed that the concentration of 5 alpha-androstane-3, 17-dione present in FF form normal dominant follicles (79."( A mechanism for the suppression of estrogen production in polycystic ovary syndrome.
Agarwal, SK; Judd, HL; Magoffin, DA, 1996
)
0.29
" Further investigation of these 2 agents, including the higher dosage of formestane (500mg), is necessary to confirm their relative efficacies."( Formestane. A review of its pharmacological properties and clinical efficacy in the treatment of postmenopausal breast cancer.
Goa, KL; Wiseman, LR, 1996
)
0.29
" No differences between males and females were noted throughout this time with regard to: (a) A or 17-OHP levels (neither of which were suppressed to 'control values'); (b) the dosage of cortisone received (13."( Growth pattern during the first 36 months of life in congenital adrenal hyperplasia (21-hydroxylase deficiency).
Argenziano, A; Di Maio, S; Franzese, A; Gasparini, N; Salerno, M; Tenore, A, 1997
)
0.3
"For both flutamide and Casodex, no consistent difference was found between the effects of once daily and thrice daily oral dosing in the rat."( Daily dosing with flutamide or Casodex exerts maximal antiandrogenic activity.
Candas, B; Chen, C; Labrie, C; Labrie, F; Luo, S; Martel, C; Singh, SM, 1997
)
0.3
" Another finding is that once daily dosing with flutamide exhibits an effectiveness comparable to thrice daily dosing; such data may have potential significance in facilitating compliance by administration of flutamide once daily instead of the current thrice daily schedule in men."( Daily dosing with flutamide or Casodex exerts maximal antiandrogenic activity.
Candas, B; Chen, C; Labrie, C; Labrie, F; Luo, S; Martel, C; Singh, SM, 1997
)
0.3
" As expected, a dose-response stimulation of luciferase activity was observed in cells treated with estradiol."( Dehydroepiandrosterone stimulates the estrogen response element.
Bruder, JM; Oettel, M; Sobek, L, 1997
)
0.3
" The biphasic nature of the theca cell response to LH emphasises the exquisite sensitivity of theca cells to LH stimulation and highlights the importance of dose-response relationships in the gonadotrophic control of ovarian function."( Effects of dose of LH on androgen production and luteinization of ovine theca cells cultured in a serum-free system.
Baird, DT; Campbell, BK; Webb, R, 1998
)
0.3
" The purpose of this study was to examine the temporal effect of chronic cyclosporine dosing on P450 protein expression and metabolic activity in a rat model of chronic cyclosporine nephropathy."( Cyclosporine suppresses rat hepatic cytochrome P450 in a time-dependent manner.
Bennett, WM; Brunner, LJ; Koop, DR, 1998
)
0.3
" Thus, use of a steroidal and a non-steroidal aromatase inhibitors in concert may be one way to improve breast cancer treatment and may also provide important information to a better understanding of the dose-response relationship between estrogen suppression and clinical effects."( Pharmacological profiles of exemestane and formestane, steroidal aromatase inhibitors used for treatment of postmenopausal breast cancer.
Lønning, PE, 1998
)
0.3
" Dose-response curves were analyzed for 5alpha-dihydrotestosterone, the most active androgen in normal prostate, and androstenedione, a major androgen derived from the adrenals."( Functional characterization of mutant androgen receptors from androgen-independent prostate cancer.
Balk, SP; Bubley, GJ; Fenton, MA; Fertig, AM; Kolvenbag, G; Shuster, TD; Taplin, ME, 1997
)
0.51
" Nine natural and synthetic androgens were tested for their effectiveness in inducing postnatal prostatic development using 808 newborn rat APs in 68 dose-response experiments."( Efficacy of various natural and synthetic androgens to induce ductal branching morphogenesis in the developing anterior rat prostate.
Cunha, GR; Foster, BA, 1999
)
0.3
" The responsiveness of the steroids of interest to ACTH (defined as the slope of the dose-response curve over the linear portion of the dose-response curve) also was similar among younger and older women."( Effects of aging on adrenal function in the human: responsiveness and sensitivity of adrenal androgens and cortisol to adrenocorticotropin in premenopausal and postmenopausal women.
Azziz, R; Bae, S; Boots, LR; Crabbe, SL; Hines, GA; Parker, CR; Slayden, SM, 2000
)
0.31
" dosing confirmed a sustained release of formestane from the site of injection."( Pharmacokinetics and metabolism of formestane in breast cancer patients.
Blum, W; Faigle, JW; Galli, B; Geisler, J; Gschwind, HP; Johannessen, DC; Kriemler, HP; Lønning, PE; Miller, WR; Schneider, W; Waldmeier, F; Winkler, T, 2001
)
0.31
" Consequences of oral dosing at 1 mg/kg on the urinary and plasma androgen profile of mare and gelding have been evaluated with an analytical method involving conjugate fractionation and selective hydrolysis, group separation, and quantitation by gas chromatography-mass spectrometry with selected ion monitoring of trimethylsilyl ethers."( Human nutritional supplements in the horse. Dehydroepiandrosterone versus androstenedione: comparative effects on the androgen profile and consequences for doping analysis.
Bonnaire, Y; Dehennin, L; Plou, P,
)
0.36
" In the remaining non-CC resistant metformin failure cases the dosage of metformin was incrersed to 500 mg three times daily for investigating menstrual cycle."( [Effects of metformin on the plasminogen activator system, endocrine, metabolic profiles in patients with polycystic ovary syndrome and clomiphene resistant cases].
Huang, Z; Li, J; Shen, H; Song, J; Zhang, Y, 2002
)
0.31
" In others 6 metformin failure cases the dosage of metformin was increased to 500 mg three times daily, one restored menstrual cycle and became pregnant."( [Effects of metformin on the plasminogen activator system, endocrine, metabolic profiles in patients with polycystic ovary syndrome and clomiphene resistant cases].
Huang, Z; Li, J; Shen, H; Song, J; Zhang, Y, 2002
)
0.31
" Analyses of the DAX1 gene in the dosage sensitive sex reversal locus on chromosome Xp21 by Southern blot analysis showed no duplications."( Familial ovarian dysgerminomas (Swyer syndrome) in females associated with 46 XY-karyotype.
Engels, H; Kempe, A; Meindl, A; Plath, H; Rhiem, K; Schmutzler, RK; Schubert, R; Schwanitz, G; van der Ven, K, 2002
)
0.31
" In cases of inadequate dosage there were side effects like sleepiness,restlessness, headache, acne/hirsutism, effluvium or odors in a percentage of 34, 17, 9, 31, 21 and 11% of the women, respectively."( [Adrenopause and dehydroepiandrosterone: pharmacological therapy versus replacement therapy].
Römmler, A, 2003
)
0.32
" Melatonin dosage was increased in eight dogs but only one had improved hair re-growth."( Adrenal steroid hormone concentrations in dogs with hair cycle arrest (Alopecia X) before and during treatment with melatonin and mitotane.
Frank, LA; Hnilica, KA; Oliver, JW, 2004
)
0.32
"Mussels (Mytilus galloaprovincialis) were exposed to different concentrations of estradiol (20, 200, and 2000 ng/L) in a semi-static regime (1-day dosing intervals) for up to 7 days in an attempt to see how mussels deal with exogenous estrogenic compounds."( Effects of 17beta-estradiol exposure in the mussel Mytilus galloprovincialis: a possible regulating role for steroid acyltransferases.
Janer, G; Lavado, R; Porte, C; Thibaut, R, 2005
)
0.33
"A 14-day oral administration of a widely used, standardized ginkgo extract at a generally advocated dosage of 240 mg/day did not significantly alter concentrations of major circulating steroids in men and women."( Effect of Ginkgo biloba extract on plasma steroid concentrations in healthy volunteers: a pilot study.
Chavin, KD; DeVane, CL; Donovan, JL; Lewis, JG; Markowitz, JS; Wang, JS, 2005
)
0.33
" Dose-response experiments with chondrosarcoma cultured cells were done with estrogen, androstenedione, and exemestane."( Estrogen signaling is active in cartilaginous tumors: implications for antiestrogen therapy as treatment option of metastasized or irresectable chondrosarcoma.
Baelde, HJ; Bovée, JV; Cleton-Jansen, AM; Hogendoorn, PC; Karperien, M; van Beerendonk, HM, 2005
)
0.55
" Both diols induced hER-mediated reporter gene transactivation in a dose-response manner, similar to that induced by oestradiol, though with lower potency, an effect that was abolished by ICI-182 780."( Enhanced formation of non-phenolic androgen metabolites with intrinsic oestrogen-like gene transactivation potency in human breast cancer cells: a distinctive metabolic pattern.
Borja-Cacho, E; Damián-Matsumura, P; García-Becerra, R; González, L; Larrea, F; Lemus, AE; Pérez-Palacios, G; Santillán, R, 2006
)
0.33
"Eight prenatally androgenized (PA) and 5 control female rhesus monkeys of similar age, body weight and body mass index received an oral placebo daily for 6-7 months followed, after at least 90 days, by daily oral dosing with pioglitazone (3mg/kg) for an additional 6-7 months."( Pioglitazone improves insulin action and normalizes menstrual cycles in a majority of prenatally androgenized female rhesus monkeys.
Abbott, DH; Bird, IM; Bruns, CM; Dumesic, DA; Goodfriend, TL; Kemnitz, JW; Zhou, R,
)
0.13
" Dose-response curves were constructed for the aromatase inhibitor formestane and for herceptin, and a 3-(4,5-dimethylthiazol)-2,5-diphenyltetrazolium bromide assay was done for combined treatment."( In vitro expansion of human breast cancer epithelial and mesenchymal stromal cells: optimization of a coculture model for personalized therapy approaches.
Cavaliere, C; Ciardiello, F; Corvigno, S; Criniti, V; De Placido, S; Limite, G; Nardone, A; Picarelli, S; Tortora, G; Veneziani, BM, 2007
)
0.34
" Young (28 day) C57Bl/6Hsd female mice were dosed daily with vehicle or VCD (160 mg/kg/d, IP) for 15 days (n = 6-7/group) and monitored by vaginal cytology for ovarian failure."( Comparison of skeletal effects of ovariectomy versus chemically induced ovarian failure in mice.
Bouxsein, ML; Christian, PJ; Funk, JL; Hoyer, PB; Rivera, Z; Van Alstine, WG; Wright, LE, 2008
)
0.35
" Female B6C3F1 mice (age, 28 days) were dosed daily for 20 days with either vehicle or VCD (160 mg kg(-1) day(-1)) to induce ovarian failure."( Steroidogenic capacity of residual ovarian tissue in 4-vinylcyclohexene diepoxide-treated mice.
Brooks, HL; Christian, PJ; Hoyer, PB; Marion, SL; Rivera, Z, 2009
)
0.35
" Correlations between blood pressures and serum renin levels, and the dosage of fludrocortisone were calculated."( Blood pressure in the first year of life in children with congenital adrenal hyperplasia due to 21-hydroxylase deficiency: a pilot study.
Claahsen-van der Grinten, HL; Kapusta, L; Mooij, CF; Otten, BJ, 2010
)
0.36
" No significant correlations between blood pressure and serum renin, androstenedione and 17-OHP levels and fludrocortisone dosage were found."( Blood pressure in the first year of life in children with congenital adrenal hyperplasia due to 21-hydroxylase deficiency: a pilot study.
Claahsen-van der Grinten, HL; Kapusta, L; Mooij, CF; Otten, BJ, 2010
)
0.6
"Mussels (Mytilus galloprovincialis) were exposed to different concentrations of testosterone (T: 20, 200 and 2000ng/L) in a semi-static water regime (1-day dosing intervals) for up to 5 days in an attempt to see whether endogenous steroid levels and steroid metabolism were altered by exogenous exposure to testosterone."( Does exposure to testosterone significantly alter endogenous metabolism in the marine mussel Mytilus galloprovincialis?
Bordonali, S; Fernandes, D; Navarro, JC; Porte, C; Riva, C, 2010
)
0.36
" All rats survived to the end of the study, and the mean body weights of dosed groups were similar to those of the vehicle control groups."( Toxicology and carcinogenesis studies of androstenedione (CAS No. 63-05-8) in F344/N rats and B6C3F1 mice (gavage studies).
, 2010
)
0.63
" The letrozole group had lower dosage of HMG (P<0."( Sequential use of letrozole and gonadotrophin in women with poor ovarian reserve: a randomized controlled trial.
Chan, CC; Ho, PC; Lee, VC; Ng, EH; Yeung, WS, 2011
)
0.37
" In conclusion, we suggest non-linear dose-response effect of Halowax 1051 on steroidogenesis and steroidogenic enzymes activity and protein expression."( Halowax 1051 affects steroidogenesis, 17β-hydroxysteroid dehydrogenase (17β-HSD) and cytochrome P450arom (CYP19) activity, and protein expression in porcine ovarian follicles.
Falandysz, J; Gregoraszczuk, EŁ; Jerzak, J; Rak-Mardyła, A, 2011
)
0.37
" At the end of the chronic stress session, the extent of adrenals activation in response to acute dosed stress was lowered in androgenized 45-day old females and increased gradually in stressed ones."( [The dynamics of hormonal changes in female rats exposed to chronic stress and androgen excess during pubescence].
Hanzhyĭ, IIu; Nosenko, ND; Reznikov, OH; Sachyns'ka, OV; Sinitsyn, PV; Tarasenko, LV, 2012
)
0.38
" The effects of NE were further evaluated in a dose-response study."( Norepinephrine stimulates progesterone production in highly estrogenic bovine granulosa cells cultured under serum-free, chemically defined conditions.
Collares, CA; Montrezor, LH; Piccinato, CA; Rosa e Silva, AA; Vireque, AA, 2012
)
0.38
"A randomized dose-response pilot study."( Endocrine effects of hCG supplementation to recombinant FSH throughout controlled ovarian stimulation for IVF: a dose-response study.
Loft, A; Nyboe Andersen, A; Smitz, J; Thuesen, LL, 2013
)
0.39
"This was a prospective randomized dose-response study conducted at Copenhagen University Hospital, Rigshospitalet, Denmark."( Intrafollicular endocrine milieu after addition of hCG to recombinant FSH during controlled ovarian stimulation for in vitro fertilization.
Andersen, AN; Loft, A; Smitz, J; Thuesen, LL, 2014
)
0.4
" Different dose-response curves for steroids and proteins in the adrenal and testis reveal novel adverse outcome pathways in intact and castrated male rats."( Novel molecular events associated with altered steroidogenesis induced by exposure to atrazine in the intact and castrate male rat.
Best, D; Cooper, RL; Jayaraman, S; Klinefelter, GR; Laws, SC; Riffle, BW; Suarez, J; Swank, A; Winnik, WM, 2014
)
0.4
" To examine possible complex dose-response effects of maternal androgens on chick development, we experimentally administered three different androgen doses of the naturally occurring mixture of yolk testosterone and androstenedione to spotless starling eggs (Sturnus unicolor)."( Diverse dose-response effects of yolk androgens on embryo development and nestling growth in a wild passerine.
Gil, D; Muriel, J; Pérez-Rodríguez, L; Puerta, M, 2015
)
0.6
" Several dioxin congeners exhibited strong significant dose-response relationships with salivary DHEA and serum A-dione levels."( A relationship in adrenal androgen levels between mothers and their children from a dioxin-exposed region in Vietnam.
Anh, LT; Honma, S; Kido, T; Koike, I; Manh, HD; Minh, NH; Nakagawa, H; Nakayama, SF; Nhu, DD; Okamoto, R; Oyama, Y; Phuc, HD; Son, LK; Toan, NV, 2017
)
0.46
" We continued the standard dosage of corticosteroid treatment."( Aromatase Inhibitor as Treatment for Severely Advanced Bone Age in Congenital Adrenal Hyperplasia: A Case Report.
Goedegebuure, WJ; Hokken-Koelega, ACS, 2019
)
0.51
" We suggest continuing the same corticosteroid dosage during AI treatment and accepting higher serum androgen levels."( Aromatase Inhibitor as Treatment for Severely Advanced Bone Age in Congenital Adrenal Hyperplasia: A Case Report.
Goedegebuure, WJ; Hokken-Koelega, ACS, 2019
)
0.51
" Nevanimibe hydrochloride (ATR-101), which selectively inhibits adrenal cortex function, might reduce androgen excess independent of ACTH and thus allow for lower glucocorticoid dosing in CAH."( A Phase 2, Multicenter Study of Nevanimibe for the Treatment of Congenital Adrenal Hyperplasia.
Auchus, RJ; Chang, AY; El-Maouche, D; Joyal, EG; Lin, VH; Merke, DP; Mohideen, P; Plaunt, MR; Turcu, AF; Vogiatzi, MG; Weintraub, L, 2020
)
0.56
" We also conducted a dose-response meta-analysis of prospective studies of circulating estrone and estradiol with colorectal, colon, and rectal cancer risk in postmenopausal women."( Endogenous Circulating Sex Hormone Concentrations and Colon Cancer Risk in Postmenopausal Women: A Prospective Study and Meta-Analysis.
Ardanaz, E; Aune, D; Bueno-de-Mesquita, B; Colorado-Yohar, SM; Cross, AJ; Dimou, N; Fortner, RT; Fournier, A; Gicquiau, A; Gram, IT; Gunter, MJ; Harbs, J; Harlid, S; Jakszyn, P; Kaaks, R; Keski-Rahkonen, P; Krogh, V; Kvaskoff, M; Masala, G; Mori, N; Murphy, N; Panico, S; Rinaldi, S; Sacerdote, C; Sánchez, MJ; Schulze, MB; Severi, G; Travis, R; Tsilidis, KK; Tumino, R; Van Guelpen, B; Waaseth, M; Watts, EL, 2021
)
0.62
" Although under a supraphysiological dosage injection, yolk testosterone decreased within 2 days and was metabolized into androstenedione, conjugated testosterone, etiocholanolone and other components that were unidentifiable due to methodological limitation."( Dynamics of maternal androgens and its metabolites during early embryonic development: embryonic modification of a maternal effect.
Groothuis, TGG; Kema, I; Pranger, A; Riedstra, B; van Faassen, M; Wang, Y, 2023
)
1.12
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
androgenA sex hormone that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors.
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
Daphnia magna metaboliteA Daphnia metabolite produced by the species Daphnia magna.
mouse metaboliteAny mammalian metabolite produced during a metabolic reaction in a mouse (Mus musculus).
[role 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]

Drug Classes (3)

ClassDescription
17-oxo steroidAny oxo steroid carrying the oxo group at position 17.
androstanoidAny steroid based on an androstane skeleton and its derivatives.
3-oxo-Delta(4) steroidA 3-oxo steroid conjugated to a C=C double bond at the alpha,beta position.
[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]

Pathways (33)

PathwayProteinsCompounds
Metabolism14961108
Metabolism of lipids500463
Metabolism of steroids111135
Metabolism of steroid hormones2537
Androgen biosynthesis916
Estrogen biosynthesis612
Biological oxidations150276
Phase I - Functionalization of compounds69175
Cytochrome P450 - arranged by substrate type30110
Endogenous sterols1838
Androgen and Estrogen Metabolism1230
17-beta Hydroxysteroid Dehydrogenase III Deficiency1230
Aromatase Deficiency1230
Disease1278231
Androstenedione Metabolism1823
Diseases of metabolism69121
Metabolic disorders of biological oxidation enzymes647
Defective CYP19A1 causes AEXS04
Male steroid hormones in cardiomyocyte energy metabolism1119
Sulfatase and aromatase pathway1414
estradiol biosynthesis I59
androgen biosynthesis715
estradiol biosynthesis I (via estrone)29
superpathway of cholesterol degradation II (cholesterol dehydrogenase)3058
superpathway of cholesterol degradation I (cholesterol oxidase)1755
cholesterol degradation to androstenedione I (cholesterol oxidase)1931
cholesterol degradation to androstenedione II (cholesterol dehydrogenase)1334
testosterone and androsterone degradation to androstendione36
androstenedione degradation3439
sitosterol degradation to androstenedione033
superpathway of testosterone and androsterone degradation1136
Biochemical pathways: part I0466
Classical pathway of steroidogenesis with glucocorticoid and mineralocorticoid metabolism325
Alternative pathway of fetal androgen synthesis717

Protein Targets (60)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency25.11890.025120.237639.8107AID886
interleukin 8Homo sapiens (human)Potency74.97800.047349.480674.9780AID651758
acetylcholinesteraseHomo sapiens (human)Potency68.93590.002541.796015,848.9004AID1347397; AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency22.32190.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency31.51580.173734.304761.8120AID1346859
SMAD family member 3Homo sapiens (human)Potency31.51580.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency26.20480.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency16.26550.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency7.78650.000221.22318,912.5098AID1259243; AID1259247; AID1259381; AID588515; AID743035; AID743036; AID743040; AID743042; AID743053; AID743054; AID743063
Smad3Homo sapiens (human)Potency6.30960.00527.809829.0929AID588855
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency0.01260.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency47.71950.000657.913322,387.1992AID1259377
progesterone receptorHomo sapiens (human)Potency4.34310.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency0.00600.531815.435837.6858AID504845
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency17.37680.01237.983543.2770AID1645841
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency35.48130.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency21.94210.000214.376460.0339AID588532; AID588533; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency38.53790.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency39.04780.000817.505159.3239AID1159527; AID1159531; AID588544
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency51.71940.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency41.57820.375827.485161.6524AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency38.53440.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.30260.000229.305416,493.5996AID588514; AID743069; AID743075; AID743077; AID743078; AID743079; AID743080
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency46.64160.001024.504861.6448AID588534; AID588535; AID743212; AID743227
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency54.03480.001019.414170.9645AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.28450.023723.228263.5986AID743222; AID743223; AID743241
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.37740.001723.839378.1014AID743083
Histone H2A.xCricetulus griseus (Chinese hamster)Potency89.16590.039147.5451146.8240AID1224845; AID1224896
Caspase-7Cricetulus griseus (Chinese hamster)Potency26.83460.006723.496068.5896AID1346980
Bloom syndrome protein isoform 1Homo sapiens (human)Potency251.18900.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921423.934123.934123.9341AID1967
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency31.62280.01789.637444.6684AID588834
caspase-3Cricetulus griseus (Chinese hamster)Potency26.83460.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency34.25580.000323.4451159.6830AID743065; AID743067
importin subunit beta-1 isoform 1Homo sapiens (human)Potency6.51315.804836.130665.1308AID540253
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID995
nuclear factor NF-kappa-B p105 subunit isoform 1Homo sapiens (human)Potency31.62284.466824.832944.6684AID651749
snurportin-1Homo sapiens (human)Potency6.51315.804836.130665.1308AID540253
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency43.25250.000627.21521,122.0200AID651741; AID743202; AID743219
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.51315.804816.996225.9290AID540253
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency19.14990.00798.23321,122.0200AID2551
gemininHomo sapiens (human)Potency28.30380.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.18150.005612.367736.1254AID624032
survival motor neuron protein isoform dHomo sapiens (human)Potency1.58430.125912.234435.4813AID1458
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency0.10000.00419.962528.1838AID2675
lamin isoform A-delta10Homo sapiens (human)Potency10.00000.891312.067628.1838AID1487
neuropeptide S receptor isoform AHomo sapiens (human)Potency0.25120.015812.3113615.5000AID1461
Nuclear receptor ROR-gammaHomo sapiens (human)Potency33.49150.026622.448266.8242AID651802
TAR DNA-binding protein 43Homo sapiens (human)Potency35.48131.778316.208135.4813AID652104
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Beta-glucuronidaseEscherichia coli K-12IC50 (µMol)430.00001.60002.60003.6000AID1803083
CholinesteraseHomo sapiens (human)IC50 (µMol)1.55000.00001.559910.0000AID1799735
Corticosteroid-binding globulinHomo sapiens (human)Ki1.73780.01323.248110.0000AID51055
AromataseHomo sapiens (human)IC50 (µMol)0.28000.00001.290410.0000AID53551; AID654681
AromataseHomo sapiens (human)Ki0.02750.00000.60469.5010AID1270809; AID53887
Androgen receptorRattus norvegicus (Norway rat)IC50 (µMol)0.67610.00101.979414.1600AID255211; AID39178
Testosterone 17-beta-dehydrogenase 3Homo sapiens (human)IC50 (µMol)0.68260.00261.76469.3000AID215939; AID215940; AID215941; AID215943; AID242395
Alpha-synucleinHomo sapiens (human)IC50 (µMol)85.90000.19003.82049.8000AID1695728
[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)Kd0.03470.00020.34964.7863AID318680
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AromataseHomo sapiens (human)Km0.04920.02000.13240.7600AID254561; AID53899; AID53901
AromataseHomo sapiens (human)Ks0.10500.10500.21400.3240AID159831
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Km0.05750.05750.05750.0575AID254561
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (138)

Processvia Protein(s)Taxonomy
glucuronoside catabolic processBeta-glucuronidaseEscherichia coli K-12
carbohydrate metabolic processBeta-glucuronidaseEscherichia coli K-12
glucuronoside catabolic processBeta-glucuronidaseEscherichia coli K-12
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
glucocorticoid metabolic processCorticosteroid-binding globulinHomo sapiens (human)
negative regulation of endopeptidase activityCorticosteroid-binding globulinHomo sapiens (human)
negative regulation of chronic inflammatory responseAromataseHomo sapiens (human)
steroid biosynthetic processAromataseHomo sapiens (human)
estrogen biosynthetic processAromataseHomo sapiens (human)
androgen catabolic processAromataseHomo sapiens (human)
syncytium formationAromataseHomo sapiens (human)
negative regulation of macrophage chemotaxisAromataseHomo sapiens (human)
sterol metabolic processAromataseHomo sapiens (human)
female genitalia developmentAromataseHomo sapiens (human)
mammary gland developmentAromataseHomo sapiens (human)
uterus developmentAromataseHomo sapiens (human)
prostate gland growthAromataseHomo sapiens (human)
testosterone biosynthetic processAromataseHomo sapiens (human)
positive regulation of estradiol secretionAromataseHomo sapiens (human)
female gonad developmentAromataseHomo sapiens (human)
response to estradiolAromataseHomo sapiens (human)
androgen biosynthetic processTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
male genitalia developmentTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
testosterone biosynthetic processTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
steroid biosynthetic processTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
xenobiotic metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of glucose metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
regulation of steroid metabolic processNuclear receptor ROR-gammaHomo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor ROR-gammaHomo sapiens (human)
circadian regulation of gene expressionNuclear receptor ROR-gammaHomo sapiens (human)
cellular response to sterolNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of circadian rhythmNuclear receptor ROR-gammaHomo sapiens (human)
regulation of fat cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor ROR-gammaHomo sapiens (human)
adipose tissue developmentNuclear receptor ROR-gammaHomo sapiens (human)
T-helper 17 cell differentiationNuclear receptor ROR-gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor ROR-gammaHomo sapiens (human)
negative regulation of protein phosphorylationTAR DNA-binding protein 43Homo sapiens (human)
mRNA processingTAR DNA-binding protein 43Homo sapiens (human)
RNA splicingTAR DNA-binding protein 43Homo sapiens (human)
negative regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
regulation of protein stabilityTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of insulin secretionTAR DNA-binding protein 43Homo sapiens (human)
response to endoplasmic reticulum stressTAR DNA-binding protein 43Homo sapiens (human)
positive regulation of protein import into nucleusTAR DNA-binding protein 43Homo sapiens (human)
regulation of circadian rhythmTAR DNA-binding protein 43Homo sapiens (human)
regulation of apoptotic processTAR DNA-binding protein 43Homo sapiens (human)
negative regulation by host of viral transcriptionTAR DNA-binding protein 43Homo sapiens (human)
rhythmic processTAR DNA-binding protein 43Homo sapiens (human)
regulation of cell cycleTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA destabilizationTAR DNA-binding protein 43Homo sapiens (human)
3'-UTR-mediated mRNA stabilizationTAR DNA-binding protein 43Homo sapiens (human)
nuclear inner membrane organizationTAR DNA-binding protein 43Homo sapiens (human)
amyloid fibril formationTAR DNA-binding protein 43Homo sapiens (human)
regulation of gene expressionTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (65)

Processvia Protein(s)Taxonomy
androgen bindingSex hormone-binding globulinHomo sapiens (human)
protein bindingSex hormone-binding globulinHomo sapiens (human)
steroid bindingSex hormone-binding globulinHomo sapiens (human)
hydrolase activity, hydrolyzing O-glycosyl compoundsBeta-glucuronidaseEscherichia coli K-12
beta-glucuronidase activityBeta-glucuronidaseEscherichia coli K-12
hydrolase activity, acting on glycosyl bondsBeta-glucuronidaseEscherichia coli K-12
identical protein bindingBeta-glucuronidaseEscherichia coli K-12
carbohydrate bindingBeta-glucuronidaseEscherichia coli K-12
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
steroid bindingCorticosteroid-binding globulinHomo sapiens (human)
serine-type endopeptidase inhibitor activityCorticosteroid-binding globulinHomo sapiens (human)
iron ion bindingAromataseHomo sapiens (human)
steroid hydroxylase activityAromataseHomo sapiens (human)
electron transfer activityAromataseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenAromataseHomo sapiens (human)
oxygen bindingAromataseHomo sapiens (human)
heme bindingAromataseHomo sapiens (human)
aromatase activityAromataseHomo sapiens (human)
estradiol 17-beta-dehydrogenase [NAD(P)] activityTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
testosterone dehydrogenase [NAD(P)] activityTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
testosterone 17-beta-dehydrogenase (NADP+) activityTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
17-beta-hydroxysteroid dehydrogenase (NADP+) activityTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificNuclear receptor ROR-gammaHomo sapiens (human)
DNA-binding transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
protein bindingNuclear receptor ROR-gammaHomo sapiens (human)
oxysterol bindingNuclear receptor ROR-gammaHomo sapiens (human)
zinc ion bindingNuclear receptor ROR-gammaHomo sapiens (human)
ligand-activated transcription factor activityNuclear receptor ROR-gammaHomo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor ROR-gammaHomo sapiens (human)
nuclear receptor activityNuclear receptor ROR-gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
double-stranded DNA bindingTAR DNA-binding protein 43Homo sapiens (human)
RNA bindingTAR DNA-binding protein 43Homo sapiens (human)
mRNA 3'-UTR bindingTAR DNA-binding protein 43Homo sapiens (human)
protein bindingTAR DNA-binding protein 43Homo sapiens (human)
lipid bindingTAR DNA-binding protein 43Homo sapiens (human)
identical protein bindingTAR DNA-binding protein 43Homo sapiens (human)
pre-mRNA intronic bindingTAR DNA-binding protein 43Homo sapiens (human)
molecular condensate scaffold activityTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
extracellular regionSex hormone-binding globulinHomo sapiens (human)
extracellular exosomeSex hormone-binding globulinHomo sapiens (human)
cytosolBeta-glucuronidaseEscherichia coli K-12
protein-containing complexBeta-glucuronidaseEscherichia coli K-12
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
extracellular regionCorticosteroid-binding globulinHomo sapiens (human)
extracellular spaceCorticosteroid-binding globulinHomo sapiens (human)
extracellular exosomeCorticosteroid-binding globulinHomo sapiens (human)
extracellular spaceCorticosteroid-binding globulinHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulumTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
endoplasmic reticulum membraneTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
intracellular membrane-bounded organelleTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
endoplasmic reticulumTestosterone 17-beta-dehydrogenase 3Homo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
nucleoplasmNuclear receptor ROR-gammaHomo sapiens (human)
nuclear bodyNuclear receptor ROR-gammaHomo sapiens (human)
chromatinNuclear receptor ROR-gammaHomo sapiens (human)
nucleusNuclear receptor ROR-gammaHomo sapiens (human)
intracellular non-membrane-bounded organelleTAR DNA-binding protein 43Homo sapiens (human)
nucleusTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
perichromatin fibrilsTAR DNA-binding protein 43Homo sapiens (human)
mitochondrionTAR DNA-binding protein 43Homo sapiens (human)
cytoplasmic stress granuleTAR DNA-binding protein 43Homo sapiens (human)
nuclear speckTAR DNA-binding protein 43Homo sapiens (human)
interchromatin granuleTAR DNA-binding protein 43Homo sapiens (human)
nucleoplasmTAR DNA-binding protein 43Homo sapiens (human)
chromatinTAR DNA-binding protein 43Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (115)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID179320Effect on androgen-Stimulated Uterine Growth at 30 micro/kg in immature female SD rats1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID194833Effect on androgen-stimulated uterine growth in immature female SD rats of uterus wet weight (0.043 mg)/body weight (g) *100 at 30 mg/kg in experiment 31995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID27326Apparent Km value was determined1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Synthesis and biochemical studies of 7-substituted 4,6-androstadiene-3,17-diones as aromatase inhibitors.
AID215943Inhibitory concentration against type-3 17-beta-HSD expressed in HEK293 cells2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID417689Inhibition of human 17beta-HSD5 expressed in HEK293 cells assessed as enzyme-mediated transformation of [14C]-4-androstene-3,17-dione in to [14C]-testosterone at 3 uM after 18 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities.
AID51054Binding affinity for corticosteroid binding globulin is expressed as log(1/k)1996Journal of medicinal chemistry, May-24, Volume: 39, Issue:11
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
AID194832Effect on androgen-stimulated uterine growth in immature female SD rats of uterus wet weight (0.043 mg)/body weight (g) *100 at 30 mg/kg in experiment 21995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID243968Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 0.3 uM 37 degree C pH 7.42005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship.
AID1695728Inhibition of alpha-synuclein aggregation (unknown origin) incubated for 8 days by thioflavin S based fluorescence assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Toward the discovery and development of effective modulators of α-synuclein amyloid aggregation.
AID1150124Relative binding affinity to guinea pig progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID255211Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals.
AID53887Binding affinity for aromatase cytochrome P45019A1 by analysis of Dixon plot1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
AID220020Binding affinity towards human corticosteroid binding globulin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID212737Binding affinity against testosterone-binding globulin (TeBG)1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
AID1150121Relative binding affinity to human progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID397122Inhibition of HIV1 RT
AID215940Ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity transfected in human embryonic kidney (HEK)-293 cells experiment 22002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis and optimization of a new family of type 3 17 beta-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry.
AID654681Inhibition of aromatase2012Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8
Development of a new class of aromatase inhibitors: design, synthesis and inhibitory activity of 3-phenylchroman-4-one (isoflavanone) derivatives.
AID53899Binding affinity for Cytochrome P450 19A11990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Mechanism and inhibition of cytochrome P-450 aromatase.
AID215939Ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity transfected in human embryonic kidney (HEK)-293 cells experiment 12002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis and optimization of a new family of type 3 17 beta-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry.
AID417688Inhibition of human 17beta-HSD5 expressed in HEK293 cells assessed as enzyme-mediated transformation of [14C]-4-androstene-3,17-dione in to [14C]-testosterone at 0.3 uM after 18 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Steroidal lactones as inhibitors of 17beta-hydroxysteroid dehydrogenase type 5: chemical synthesis, enzyme inhibitory activity, and assessment of estrogenic and androgenic activities.
AID53901Km for Cytochrome P450 19A11990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Mechanism and inhibition of cytochrome P-450 aromatase.
AID51052In silico binding affinity to corticosteroid binding globulin (CBG)1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 1. Method and validations.
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.
AID215941Ability to inhibit the Type-3 17-beta- hydroxysteroid dehydrogenase activity transfected in human embryonic kidney (HEK)-293 cells experiment 32002Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3
Synthesis and optimization of a new family of type 3 17 beta-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry.
AID51055Binding affinity to human CBG receptor (corticosteroid-binding globulins)2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR.
AID212931Binding affinity towards human testosterone binding globulin.1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
AID212920Binding affinity against transport protein testosterone binding globulin.1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Compass: predicting biological activities from molecular surface properties. Performance comparisons on a steroid benchmark.
AID228061Binding affinity towards human testosterone binding globulin.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
QSAR's from similarity matrices. Technique validation and application in the comparison of different similarity evaluation methods.
AID51059Binding affinity to corticosteroid binding globulin1998Journal of medicinal chemistry, Jul-02, Volume: 41, Issue:14
Three-dimensional quantitative similarity-activity relationships (3D QSiAR) from SEAL similarity matrices.
AID194831Effect on androgen-stimulated uterine growth in immature female SD rats of uterus wet weight (0.043 mg)/body weight (g) *100 at 30 mg/kg in experiment 11995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID39178In vitro antagonist activity against rat prostatic androgen receptor (AR)1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
AID215949Percent inhibition against type-3 17-beta-HSD expressed in HEK293 cells at 3 uM2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.
AID243963Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 3 uM 37 degree C pH 7.42005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship.
AID51048In silico binding affinity to human corticosteriod binding globulin1997Journal of medicinal chemistry, Sep-26, Volume: 40, Issue:20
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
AID159828Maximum absorbance for formation of reversible-enzyme-ligand complexes with human placental aromatase (PL1)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID51062In silico steroid binding affinity to transport protein corticosteroid binding globulin1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Compass: predicting biological activities from molecular surface properties. Performance comparisons on a steroid benchmark.
AID53551In vitro competitive inhibitory activity was measured on Cytochrome P450 19A1 of human placental microsomes1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID215948Percent inhibition against type-3 17-beta-HSD expressed in HEK293 cells at 0.3 uM2000Bioorganic & medicinal chemistry letters, Nov-20, Volume: 10, Issue:22
Androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID39451Binding affinity against cytosolic androgen receptor from ventral prostate of rats using [3H]MIB competitive binding assay (relative to dihydro testosterone)2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor.
AID1241422Inhibition of 17beta-HSD3 in rat testes microsomes using [14C]-4-androstene-3,17-dione as substrate after 2 hrs2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Design, chemical synthesis and biological evaluation of 3-spiromorpholinone/3-spirocarbamate androsterone derivatives as inhibitors of 17β-hydroxysteroid dehydrogenase type 3.
AID51049Binding affinity against corticosteroid-binding globulin1993Journal of medicinal chemistry, Feb-19, Volume: 36, Issue:4
Structure-activity relationships from molecular similarity matrices.
AID51058Binding affinity towards corticosteroid-binding globulin (CBG)2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Mapping property distributions of molecular surfaces: algorithm and evaluation of a novel 3D quantitative structure-activity relationship technique.
AID1270809Competitive inhibition of human aromatase extracted from placental microsomes after 5 mins by Dixon plot analysis in presence of [1beta-3H]AD2015European journal of medicinal chemistry, Nov-13, Volume: 105Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.
AID159831Binding affinity constant for formation of reversible enzyme-ligand complex with human placental aromatase (PL1)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Interactions of thiol-containing androgens with human placental aromatase.
AID212919Binding affinity towards testosterone binding globulin is expressed as log(1/k).1996Journal of medicinal chemistry, May-24, Volume: 39, Issue:11
Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
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.
AID242395Inhibition of type-3 17 beta-hydroxysteroid dehydrogenase expressed in HEK293 cells at 37 degree C pH7.4 2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
Androsterone 3alpha-ether-3beta-substituted and androsterone 3beta-substituted derivatives as inhibitors of type 3 17beta-hydroxysteroid dehydrogenase: chemical synthesis and structure-activity relationship.
AID51056Binding affinity to the corticosteroid-binding globulin (CBG) receptor.2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
GRid-INdependent descriptors (GRIND): a novel class of alignment-independent three-dimensional molecular descriptors.
AID1150122Relative binding affinity to sheep progesterone receptor1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Quantitative relationships between steroid structure and binding to putative progesterone receptors.
AID254561Michaelis-Menten constant against Aromatase2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Structure-activity relationships of new A,D-ring modified steroids as aromatase inhibitors: design, synthesis, and biological activity evaluation.
AID50906Inhibition of mouse constitutive androstane receptor (mCAR) activity at 10 uM was determined as percent remaining activity2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Molecular determinants of steroid inhibition for the mouse constitutive androstane receptor.
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.
AID1803083β-Glucuronidase Inhibition Assay from Article 10.3109/14756366.2011.590804: \\Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and u00DF-glucuronidase inhibitory activity of transformed products.\\2012Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 27, Issue:3
Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and β-glucuronidase inhibitory activity of transformed products.
AID1802450Oatp1d1 Transport Assay from Article 10.1074/jbc.M113.518506: \\Molecular characterization of zebrafish Oatp1d1 (Slco1d1), a novel organic anion-transporting polypeptide.\\2013The Journal of biological chemistry, Nov-22, Volume: 288, Issue:47
Molecular characterization of zebrafish Oatp1d1 (Slco1d1), a novel organic anion-transporting polypeptide.
AID1799735Cholinesterase Inhibition Assay from Article 10.1080/14756360802236393: \\Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.\\2009Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 24, Issue:2
Butyrylcholinesterase inhibitory activity of testosterone and some of its metabolites.
AID1346911Rat Androgen receptor (3C. 3-Ketosteroid receptors)2003Chemical research in toxicology, Oct, Volume: 16, Issue:10
Study of 202 natural, synthetic, and environmental chemicals for binding to the androgen receptor.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6,921)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903107 (44.89)18.7374
1990's1578 (22.80)18.2507
2000's1183 (17.09)29.6817
2010's815 (11.78)24.3611
2020's238 (3.44)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 78.26

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

MetricThis Compound (vs All)
Research Demand Index78.26 (24.57)
Research Supply Index8.93 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index150.53 (26.88)
Search Engine Supply Index2.09 (0.95)

This Compound (78.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials377 (5.25%)5.53%
Reviews252 (3.51%)6.00%
Case Studies261 (3.64%)4.05%
Observational13 (0.18%)0.25%
Other6,272 (87.41%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]