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aminoglutethimide

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Description

Aminoglutethimide: An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

aminoglutethimide : A dicarboximide that is a six-membered cyclic compound having ethyl and 4-aminophenyl substituents at the 3-position. [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 CID2145
CHEMBL ID488
CHEBI ID2654
SCHEMBL ID4306
MeSH IDM0000944

Synonyms (201)

Synonym
AC-12456
AB00051935-11
BRD-A25234499-001-05-0
KBIO1_000884
DIVK1C_000884
NCI60_002900
ag-1
cytadren
orimeten
3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione
elipten
2-(p-aminophenyl)-2-ethylglutarimide
dl-aminoglutethimide
p-aminoglutethimide
nsc-330915
glutarimide, 2-(p-aminophenyl)-2-ethyl-
2, 3-(4-aminophenyl)-3-ethyl-
ba-16038
.alpha.-(p-aminophenyl)-.alpha.-ethylglutarimide
nsc330915
EU-0100124
SPECTRUM_000040
SMP1_000017
PRESTWICK2_000244
ccris 7562
einecs 204-756-4
aminoglutetimida [inn-spanish]
aminoglutethimidum [inn-latin]
brn 0210656
3-(4-aminophenyl)-3-ethyl-2,6-piperidindion
c 16038-ba
ba 16038
PRESTWICK_243
glutethimide, para-amino
2,6-piperidinedione, 3-(4-aminophenyl)-3-ethyl-
PRESTWICK3_000244
SPECTRUM5_000802
BSPBIO_001832
BPBIO1_000032
IDI1_000884
LOPAC0_000124
AB00051935
aminoglutethimide
125-84-8
C07617
3-ethyl-3-(p-aminophenyl)-2,6-dioxopiperidine
DB00357
smr000326785
aminoglutethimide ag, 4
bdbm9460
chembl488 ,
aminoglutetimide
MLS000859924
3-(4-aminophenyl)-3-ethyl-piperidine-2,6-dione
aminoglutethimide (ag)
alpha-(p-aminophenyl)-alpha-ethylglutarimide
D00574
aminoglutethimide (usp/inn)
cytadren (tn)
NCGC00093615-02
NCGC00093615-03
NCGC00093615-04
KBIO2_000400
KBIO2_002968
KBIO2_005536
KBIOSS_000400
KBIOGR_000588
KBIO3_001332
SPECTRUM3_000296
PRESTWICK1_000244
SPBIO_000046
SPECTRUM2_000093
SPBIO_002247
SPECTRUM4_000144
NINDS_000884
PRESTWICK0_000244
SPECTRUM1500115
BSPBIO_000028
NCGC00093615-05
(?)-p-aminoglutethimide
NCGC00093615-01
MLS001213216
NCGC00015110-02
A 9657 ,
HMS2091I09
( inverted question mark)-p-aminoglutethimide
HMS2090I05
NCGC00015110-07
(+/-)-p-aminoglutethimide
VU0243029-3
HMS502M06
CHEBI:2654 ,
aminoglutethimidum
aminoglutetimida
HMS1920C09
HMS1568B10
STK802074
A805433
AKOS004120070
HMS3259H10
HMS3260I10
HMS2095B10
0o54zq14i9 ,
hsdb 7494
aminoglutethimide [usp:inn:ban]
nsc 755868
unii-0o54zq14i9
nsc 330915
EN300-53368
dtxcid202589
NCGC00257263-01
dtxsid8022589 ,
tox21_303497
BBL010961
nsc755868
pharmakon1600-01500115
nsc-755868
tox21_110406
3-(4-aminophenyl)-3-ethyl-2,6-piperidinedione
HMS2231M19
CCG-38911
NCGC00015110-06
NCGC00015110-04
NCGC00015110-05
NCGC00015110-03
NCGC00015110-12
LP00124
HMS3372M07
gtpl7054
aminoglutethimide [inn]
aminoglutethimide [who-dd]
aminoglutethimide [ep impurity]
aminoglutethimide [usp impurity]
aminoglutethimide [mi]
aminoglutethimide [vandf]
aminoglutethimide [hsdb]
aminoglutethimide [ep monograph]
aminoglutethimide [mart.]
aminoglutethimide [orange book]
AB00051935-09
HY-B0237
AKOS022060651
NC00714
SCHEMBL4306
tox21_110406_1
NCGC00015110-09
(y)-p-aminoglutethimide
tox21_500124
NCGC00260809-01
W-108399
(a+/-)-p-aminoglutethimide
AB00051935_12
AB00051935_13
mfcd00010122
aminoglutethimide, european pharmacopoeia (ep) reference standard
SR-01000075596-1
sr-01000075596
aminoglutethimide, united states pharmacopeia (usp) reference standard
HMS3655O17
SR-01000075596-4
SR-01000075596-6
SBI-0050112.P004
(rs)-2-(4-amino-phenyl)-2-ethyl-glutarimide;(rs)-3-(4-amino-phenyl)-3-ethyl-2,6-dioxo-piperidine
HMS3712B10
SW196550-3
Z800191876
aminoglutethimide (cytadren)
FT-0773944
S1672
Q241150
3-carboxy-1,1-dimethyl-, (e)-2-propenyl
AS-13282
BCP28501
BRD-A25234499-001-09-2
SDCCGSBI-0050112.P005
NCGC00015110-21
AMY33415
D88489
PB48252
BA164155
aminoglutethimide- bio-x
mfcd03094024
(s)-3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione
SY294287
aminoglutethimidum (inn-latin)
orimetene
aminoglutethimide (mart.)
orimenten
aminoglutethimide (ep monograph)
aminoglutethimide (usp impurity)
aminoglutethimid
mamomit
aminoglutethimide (ep impurity)
rodazol
aminoglutetimida (inn-spanish)
aminoglutethimide (usp:inn:ban)
aminoblastin
alpha-(4-aminophenyl)-alpha-ethylglutarimide
(r)-3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione
SY344150
mfcd03094025

Research Excerpts

Overview

Aminoglutethimide is a steroidogenesis inhibitor and inhibits a cholesterol side-chain cleavage enzyme (CYP11A1) that converts cholesterol to pregnenolone in mitochondria. It is an effective endocrine therapy in advanced postmenopausal breast cancer, particularly for bone deposits.

ExcerptReferenceRelevance
"Aminoglutethimide (AG) is a common treatment of breast cancer."( Molecularly Imprinted Polymers Doped with Carbon Nanotube with Aid of Metal-Organic Gel for Drug Delivery Systems.
Chai, MH; Huang, YP; Liu, ZS; Yao, HF; Zhao, L, 2020
)
1.28
"Aminoglutethimide is a steroidogenesis inhibitor and inhibits a cholesterol side-chain cleavage enzyme (CYP11A1) that converts cholesterol to pregnenolone in mitochondria. "( Aminoglutethimide-induced lysosomal changes in adrenal gland in mice.
Asaoka, Y; Imura, N; Miyoshi, T; Mutsuga, M; Togashi, Y, 2017
)
3.34
"Aminoglutethimide (AMG) is an aromatic amine aromatase inhibitor associated with a high incidence of idiosyncratic blood dyscrasias, especially agranulocytosis. "( Effect of aminoglutethimide on neutrophils in rats: implications for idiosyncratic drug-induced blood dyscrasias.
Ng, W; Uetrecht, J, 2013
)
2.23
"Aminoglutethimide is a clinically available drug that suppresses steroid biosynthesis by inhibiting enzymes such as cytochrome P450scc and aromatase. "( Aminoglutethimide prevents excitotoxic and ischemic injuries in cortical neurons.
Akaike, A; Kaneko, S; Katsuki, H; Kume, T; Shirakawa, H, 2006
)
3.22
"Aminoglutethimide (AG) is a first-generation aromatase inhibitor used for estrogen-dependent breast cancer. "( Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis.
Bonini, MG; Ehrenshaft, M; Jiang, J; Mason, RP; Siraki, AG, 2007
)
3.23
"Aminoglutethimide is an important new modality in the treatment of advanced breast cancer."( Medical adrenalectomy with aminoglutethimide in the management of advanced breast cancer.
Jerums, G; Murray, RM; Pitt, P, 1981
)
1.28
"Aminoglutethimide is an effective endocrine therapy in advanced postmenopausal breast cancer, particularly for bone deposits."( Aminoglutethimide for the treatment of advanced postmenopausal breast cancer.
Coombes, RC; Ford, HT; Gazet, JC; Harmer, CL; Harris, AL; McKinna, JA; Morgan, M; Parsons, CA; Powles, TJ; Smith, IE; White, H, 1983
)
2.43
"Aminoglutethimide (AG) is a potent inhibitor of aromatization in placental microsomes and in peripheral tissues in postmenopausal women. "( Resistance of the ovary to blockade of aromatization with aminoglutethimide.
Samojlik, E; Santen, RJ; Wells, SA, 1980
)
1.95
"Aminoglutethimide (AG) is an inhibitor of P-450 linked steroid hydroxylation reactions including the cholesterol side chain cleavage, which is the rate-limiting step by which the synthesis of pregnenolone and also progesterone can be controlled. "( Inhibition of human placental progesterone synthesis by aminoglutethimide in vitro.
Rabe, D; Rabe, T; Runnebaum, B; Weidenhammer, K, 1982
)
1.95
"Aminoglutethimide is an effective endocrine therapy in advanced postmenopausal breast cancer, particularly for bone deposits."( Aminoglutethimide in the treatment of advanced postmenopausal breast cancer.
Harris, AL; Powles, TJ; Smith, IE, 1982
)
2.43
"Aminoglutethimide is an inhibitor of various steroid hydroxylation reactions in the adrenal gland, the ovary, the testis and the placenta; furthermore, the extraglandular estrogen synthesis is inhibited by blocking the aromatase in the subcutaneous fatty tissue."( [Aminoglutethimide - a new drug for the after care in breast cancer].
Rabe, D; Rabe, T; Runnebaum, B, 1981
)
2.62
"Aminoglutethimide (AG) is an effective chemical ablative form of therapy for metastatic breast cancer in postmenopausal women. "( Influence of estrogen receptor status on response of metastatic breast cancer to aminoglutethimide therapy.
Cox, CE; Harvey, HA; Lawrence, BV; Lipton, A; Santen, RJ; Smart, EK; Wells, SA; White, DS, 1980
)
1.93
"Aminoglutethimide (Ag) is a potent aromatase-enzyme inhibitor used in the treatment of patients with breast cancer. "( Adrenal effects of low-dose aminoglutethimide when used alone in postmenopausal women with advanced breast cancer.
Carella, MJ; Dimitrov, NV; Gossain, VV; Rovner, DR; Srivastava, L, 1994
)
2.03
"Aminoglutethimide is a steroid synthesis inhibitor which depletes adrenocortical hormones without these negative effects."( Dissociation of the effect of aminoglutethimide on corticosterone biosynthesis from ataxic and hypothermic effects in DBA and C57 mice.
Gallaher, EJ; Keith, LD; Roberts, AJ, 1993
)
1.3
"Aminoglutethimide (AG) is an inhibitor of P450 aromatase and is in clinical use for the treatment of estrogen-dependent breast cancer in postmenopausal women. "( Induction of cytochrome P450 2B1 in rat liver by the aromatase inhibitor aminoglutethimide.
Cantrill, E; Farrell, GC; Murray, M, 1993
)
1.96
"Aminoglutethimide is an inhibitor of adrenal steroid biosynthesis and blocks the conversion of cholesterol to pregnenolone, and therefore reduces levels of adrenal androgens, which are a source of estrogens in both premenopausal and postmenopausal women."( [Aromatase inhibitors--new possibilities in treatment of breast carcinoma].
Friedrichs, K; Jänicke, F, 1998
)
1.02
"Aminoglutethimide (AG) is an aromatase inhibitor used to treat estrogen-dependent breast cancer."( Induction of aromatase expression by aminoglutethimide, an aromatase inhibitor that is used to treat breast cancer in postmenopausal women.
Chen, S; Kao, YC; Okubo, T; Sun, XZ,
)
1.13
"Aminoglutethimide is an investigational agent of proven benefit in the treatment of metastatic breast carcinoma. "( Pancytopenia induced by aminoglutethimide in the treatment of breast cancer.
Hamilton, R; Harvey, HA; Lawrence, B; Lipton, A; Mercurio, T; Santen, RJ, 1978
)
2.01
"Aminoglutethimide is an aromatase inhibitor that is successfully used for endocrine treatment of advanced breast cancer. "( Aminoglutethimide enzyme induction: pharmacological and endocrinological implications.
Lønning, PE, 1990
)
3.16
"Aminoglutethimide (AG) is a drug that inhibits several steps of steroidogenesis; it is used in post-menopausal advanced breast cancer. "( [Aminoglutethimide and cancer of the prostate].
Bonneterre, J, 1986
)
2.62
"Aminoglutethimide is an effective treatment for advanced postmenopausal breast cancer, acting in a novel way. "( Aminoglutethimide--a new endocrine therapy in breast cancer. A cancer research review.
Harris, AL, 1985
)
3.15
"Aminoglutethimide (AG) is a drug that inhibits steroid synthesis; it is used in advanced breast cancer. "( [Aminoglutethimide-induced dyslipidemia. Experimental study].
Bonneterre, J; Demaille, A; Nguyen, M; Vanlerenberghe, J, 1985
)
2.62

Effects

Aminoglutethimide (AG) has been used clinically as a drug in the treatment of hormone-dependent metastatic breast cancer. It has antitumor activity similar to that of surgical adrenalectomy.

ExcerptReferenceRelevance
"Aminoglutethimide (AG) has been used clinically as a drug in the treatment of hormone-dependent metastatic breast cancer. "( [Chromatographic separation of aminoglutethimide enantiomers on cellulose tris(3,5-dimethylphenylcarbamate) chiral stationary phase].
Gong, R; Li, P; Lin, X; Yu, J, 2014
)
2.13
"Aminoglutethimide (AG) has antitumor activity in disseminated breast cancer similar to that of surgical adrenalectomy. "( The role of aromatase inhibitors in breast cancer.
Powles, TJ, 1983
)
1.71
"Aminoglutethimide (AG) has recently been introduced for endocrine therapy in patients with advanced breast and endometrial cancer. "( Aminoglutethimide and warfarin. A new important drug interaction.
Jahren, G; Kvinnsland, S; Lønning, PE, 1984
)
3.15
"Aminoglutethimide has produced antitumor response rates of 35% in unselected patients, most of whom have undergone prior therapy with either chemotherapy or hormonal manipulation."( [Aromatase inhibitors--new possibilities in treatment of breast carcinoma].
Friedrichs, K; Jänicke, F, 1998
)
1.02
"Aminoglutethimide has been administered to 24 patients with Cushing's disease for 1-6 months."( [Effect of aminoglutethimide on ACTH plasma levels in Cushing's disease and Nelson syndrome].
Jeske, W; Kasperlik-Załuska, AA; Migdalska, B; Niegowska, E; Wiśniewska-Woźniak, T,
)
1.24
"Aminoglutethimide (Ag) has been used in different dosages with and without combined treatment with glucocorticoids for the suppression of peripheral plasma levels of steroidal hormones. "( Endocrine effects of aminoglutethimide plus hydrocortisone versus effects of high dose of hydrocortisone alone in postmenopausal metastatic breast cancer.
Alexieva-Figusch, J; de Jong, FH; Klign, JG; Lamberts, WJ; van Gilse, HA, 1987
)
2.03
"Aminoglutethimide has little influence on the loss of serum LH bioactivity induced by the LHRH agonist while ketoconazole stimulates the concentration of serum bioactive LH in the absence or presence of simultaneous treatment with the LHRH agonist."( The rise in testicular androgens during the first days of treatment with an LHRH agonist in the dog can be blocked by aminoglutethimide or ketoconazole.
Belanger, A; Caron, S; Labrie, F; Lacoste, D; St-Arnaud, R, 1988
)
1.21
"Aminoglutethimide has been used in combination with hydrocortisone in patients with advanced prostatic cancer with the rationale that it causes a 'medical adrenalectomy'. "( The effects of aminoglutethimide and hydrocortisone, alone and combined, on androgen levels in post-orchiectomy prostatic cancer patients.
Dowsett, M; Jeffcoate, SL; Malone, P; Ponder, BA; Shearer, RJ, 1988
)
2.07

Actions

ExcerptReferenceRelevance
"Aminoglutethimide did not inhibit substrate binding."( High affinity binding of substrate and effector ligands to testicular microsomal cytochrome P-450.
Payne, AH; Quinn, PG, 1986
)
0.99

Treatment

Aminoglutethimide pretreatment, which blocks the early step of steroid synthesis, inhibited the antidepressant-like effect of Ro5-4864. The activities of G6PDH and malic enzyme decreased, while 20alpha-HSD activity was maintained at a very low level.

ExcerptReferenceRelevance
"Aminoglutethimide pretreatment, which blocks the early step of steroid synthesis, inhibited the antidepressant-like effect of Ro5-4864."( Antidepressant-like effect of Ro5-4864, a peripheral-type benzodiazepine receptor ligand, in forced swimming test.
Bressan, E; De Lima, TC; Duarte, FS; Farges, RC; Ferrara, P; Gavioli, EC, 2003
)
1.04
"Aminoglutethimide given during treatment with ACTH decreased urinary aldosterone and blood pressure and increased PRA, with minimal effects on plasma cortisol or urinary 17-hydroxycorticosteroids."( Overproduction of sodium-retaining steroids by the zona glomerulosa is adrenocorticotropin-dependent and mediates hypertension in dexamethasone-suppressible aldosteronism.
Bartter, FC; Gill, JR, 1981
)
0.98
"Aminoglutethimide-treated rats developed less pancreatic tumours than did untreated controls."( Effects of aminoglutethimide, alone and in combination with surgical castration, on pancreatic carcinogenesis in rats and hamsters.
Foekens, JA; Klijn, JG; Meijers, M; van Garderen-Hoetmer, A; Visser, CJ; Woutersen, RA, 1995
)
1.4
"In aminoglutethimide-treated rats, the activities of G6PDH and malic enzyme decreased, while 20alpha-HSD activity was maintained at a very low level."( An enzymologic study of corpora lutea in early pregnant rats treated with abortifacient agents.
Morikawa, H; Motohashi, T; Okamura, H; Okazaki, T; Yogo, I, 1976
)
0.77
"Aminoglutethimide treatment (10-20 mg twice daily 6 or 7 consecutive times) revealed decreased G6PDH and malic enzyme activities while 20 alpha-HSD activity was maintained at a very low level."( An enzymologic study of corpora lutea in early pregnant rats treated with abortifacient agents.
Morikawa, H; Motohashi, T; Okamura, H; Okazaki, T; Yogo, I, 1976
)
0.88
"In aminoglutethimide-treated rats, plasma ACTH increased only at doses much higher than those inhibiting plasma corticosterone, suggesting that adrenal enzyme blockers may themselves be stressful."( The adrenocortical system responds slowly to removal of corticosterone in the absence of concurrent stress.
Akana, SF; Cascio, CS; Dallman, MF; Jacobson, L; Scribner, K; Shinsako, J, 1989
)
0.79
"Aminoglutethimide treatment caused significant alterations in the metabolite profiles of estradiol and estrone but with large interindividual variations."( Alterations in the urine excretion of estrogen metabolites in breast cancer women treated with aminoglutethimide.
Lønning, PE; Skulstad, P, 1989
)
1.22
"Aminoglutethimide treatment results also in an increase in the number of neurophysin-immunoreactive nervous fibers localized in the internal layer of the median eminence."( Studies on hypothalamo-pituitary corticoliberin system. I. Localization of corticotropin-releasing factor (CRF)- and neurophysin-immunoreactive neurons in the Mongolian gerbil (Meriones unguiculatus).
Miśkowiak, B, 1987
)
0.99
"Treatment with aminoglutethimide (blocker of cytochrome P450scc; 1.5 x 10(-4)M), nitric oxide donor (spermine NONOate), and staurosporine increased bax expression in cells collected from both experimental periods."( Effect of progesterone on the expression of bax and bcl-2 and on caspase activity in bovine luteal cells.
Kotwica, J; Liszewska, E; Rekawiecki, R, 2005
)
0.67
"Treatment with aminoglutethimide of only four premenopausal breast cancer patients has been reported in which two patients responded."( Endocrine and therapeutic effects of aminoglutethimide in premenopausal patients with breast cancer.
Dowsett, M; Harris, AL; Jeffcoate, SL; McKinna, JA; Morgan, M; Smith, IE, 1982
)
0.88
"Treatment with aminoglutethimide alone on day 7 post hCG did not further depress the already low HMG-CoA reductase activity, but ACAT and cholesterol ester storage were stimulated while sterol esterase activity was not altered."( Regulation of ovarian cholesterol metabolism: control of 3-hydroxy-3-methylglutaryl coenzyme A reductase and acyl coenzyme A:cholesterol acyltransferase.
Schuler, LA; Strauss, JF; Toaff, ME, 1981
)
0.6
"Treatment with aminoglutethimide in vivo followed by electron paramagnetic resonance spectroscopic analysis of mitochondria (prepared in aminoglutethimide-free buffers) showed that incubation of isolated mitochondria at 37 C and pH 6.2 caused an increased high spin state (g = 8.2 signal) and a concomitant decreased low spin state."( Estrogen increases precursor for pregnenolone synthesis with temperature-sensitive occupancy of P-450scc in mitochondria of rabbit corpus luteum.
Ghosh, DK; Holt, JA; Menon, KM; Schreiber, JR; Wittmaack, FM, 1988
)
0.61
"Treatment with aminoglutethimide in the absence of cAMP had no effect on these enzyme activities."( Adenosine 3',5'-monophosphate-mediated induction of 17 alpha-hydroxylase and C 17-20 lyase activities in cultured mouse Leydig cells is enhanced by inhibition of steroid biosynthesis.
Payne, AH; Rani, CS, 1986
)
0.61

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
" Mean half-life and clearance rates were determined in six patients."( Serum aminoglutethimide levels: studies of serum half-life, clearance, and patient compliance.
Murray, FT; Samojlik, E; Santen, RJ; Santner, S,
)
0.61
" This report gives the results of a detailed pharmacokinetic and endocrine study of PyG in ten patients."( Endocrine, pharmacokinetic and clinical studies of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione ('pyridoglutethimide') in postmenopausal breast cancer patients.
Coombes, RC; Dowsett, M; Haynes, B; Jarman, M; Jones, A; Lonning, P; MacNeill, F; Mehta, A; Newton, C; Powles, TJ, 1991
)
0.28
" This study investigates the pharmacokinetics of pyridoglutethimide in the rat and the rabbit: the plasma half-life is 6 hr in the rat and 16."( Pyridoglutethimide [3-ethyl-3-(4-pyridyl)-piperidine-2,6-dione], an analogue of aminoglutethimide. Metabolism and pharmacokinetics.
Goss, PE; Griggs, LJ; Jarman, M; Seago, A, 1986
)
0.5
" The plasma half-life of the drug was markedly reduced (mean 43%) during multiple-dose administration as compared with a single dose, but only a moderate increase in total clearance (mean 26."( Single-dose and steady-state pharmacokinetics of aminoglutethimide.
Kvinnsland, S; Lønning, PE; Schanche, JS; Ueland, PM,
)
0.39
"3-fold) than that of R-AG and appears to be most likely the cause for the other pharmacokinetic differences observed."( Pharmacokinetics of S- and R-enantiomers of aminoglutethimide following oral administration of racemic drug in breast cancer patients.
Abd el-Warith, A; Alshowaier, IA; el-Yazigi, A; Ezzat, A; Nicholls, PJ, 1999
)
0.56

Compound-Compound Interactions

Study looked at effects of aromatase inhibitor aminoglutethimide on pancreatic carcinogenesis in rats and hamsters. Flutamide withdrawal is a therapeutically active approach in patients with prostate cancer.

ExcerptReferenceRelevance
"We studied the effects of hormonal manipulation by orchiectomy, alone or in combination with the aromatase inhibitor aminoglutethimide (AGT), and by luteinizing hormone-releasing hormone agonist (LH-RH-A) (goserelin) treatment on the development of early putative (pre)neoplastic lesions induced in the pancreas of rats and hamsters by azaserine and N-nitrosobis(2-oxopropyl)amine respectively."( Effects of castration, alone and in combination with aminoglutethimide, on growth of (pre)neoplastic lesions in exocrine pancreas of rats and hamsters.
Bakker, GH; de Jong, FH; Foekens, JA; Klijn, JG; Meijers, M; van Garderen-Hoetmer, A; Woutersen, RA, 1991
)
0.74
"Flutamide withdrawal, when combined with the simultaneous administration of aminoglutethimide, is a therapeutically active approach in patients with "hormone-refractory" prostate cancer."( Surprising activity of flutamide withdrawal, when combined with aminoglutethimide, in treatment of "hormone-refractory" prostate cancer.
Cooper, M; Figg, WD; Headlee, D; Linehan, WM; Myers, CE; Sartor, O; Steinberg, S; Thibault, A; Tompkins, A; Weinberger, M, 1994
)
0.76
"The present 12-month study was carried out to investigate the effects of the aromatase inhibitor aminoglutethimide, alone and in combination with orchiectomy, on pancreatic carcinogenesis in azaserine-treated rats and N-nitrosobis(2-oxopropyl)-amine-treated hamsters."( Effects of aminoglutethimide, alone and in combination with surgical castration, on pancreatic carcinogenesis in rats and hamsters.
Foekens, JA; Klijn, JG; Meijers, M; van Garderen-Hoetmer, A; Visser, CJ; Woutersen, RA, 1995
)
0.9

Bioavailability

Aminoglutethimide is a potent inducer of aminoglutEthimide metabolism. This produced a significant reduction in plasma bioavailability of oestrone sulphate. While this regimen effectively blocked adrenal function, it was complicated by a drug interaction.

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
)
0.73
" Our results, although preliminary, suggest that aminoglutethimide is a potent inducer of aminoglutethimide metabolism, thereby producing a significant reduction in plasma bioavailability of oestrone sulphate."( Alterations in the metabolism of oestrogens during treatment with aminoglutethimide in breast cancer patients. Preliminary findings.
Kvinnsland, S; Lønning, PE; Thorsen, T; Ueland, PM, 1987
)
0.76
"The bioavailability of aminoglutethimide tablets was examined using a spectrophotometric assay."( Aminoglutethimide bioavailability, pharmacokinetics, and binding to blood constituents.
Le Sher, AR; Thompson, TA; Vermeulen, JD; Wagner, WE, 1981
)
2.02
" Compared with the commercial AG tablet, the MMC-assisted MIP gave a markedly high relative bioavailability of 266."( Macromolecular crowding of molecular imprinting: A facile pathway to produce drug delivery devices for zero-order sustained release.
Huang, YP; Li, RS; Liu, ZS; Tang, L; Wang, XH; Yang, JR; Zhao, CY, 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
" Compared with commercial tablets, the relative bioavailability was 143."( Molecularly Imprinted Polymers Doped with Carbon Nanotube with Aid of Metal-Organic Gel for Drug Delivery Systems.
Chai, MH; Huang, YP; Liu, ZS; Yao, HF; Zhao, L, 2020
)
0.56

Dosage Studied

Aminoglutethimide without glucocorticoid has been shown to be a clinically effective treatment for postmenopausal breast cancer in low dosage (250 mg day-1) If correct, two clinically available aromatase inhibitors could potentially be given together at lower than usual dosage.

ExcerptRelevanceReference
" 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
)
0.65
" On subsequent repeated dosing with PyG, both the Km (4."( Pharmacokinetics and pharmacodynamics of the aromatase inhibitor 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione in patients with postmenopausal breast cancer.
Coombes, RC; Dowsett, M; Griggs, LJ; Haynes, BP; Jarman, M; Jones, A; Lønning, PE; Mehta, A; Powles, T; Stein, R, 1991
)
0.28
" On repeated dosing with the drug, tolerance to these various activities occurred."( Development of tolerance to the CNS effects of aminoglutethimide in mice.
Ahmad, B; Nicholls, PJ, 1990
)
0.54
" The lower dosage was better tolerated without apparent compromise in therapeutic efficacy."( Aminoglutethimide in patients with metastatic breast cancer.
Dao, TL; Nemoto, T; Patel, JK; Rosner, D, 1989
)
1.72
" Adrenal failure due to glucocorticoid deficiency was also present and required an increased dosage of cortisone."( Aminoglutethimide-induced hyperkalaemia.
Bentley, P; Davies, JP; Ghose, RR, 1989
)
1.72
" This dosage regimen appears of comparable efficacy to previously reported higher dosage regimens with reduced toxicity compared to low dose regimens without hydrocortisone."( Phase II study of low dose aminoglutethimide 250 mg/day plus hydrocortisone in advanced postmenopausal breast cancer.
Cantwell, BM; Carmichael, J; Dawes, P; Farndon, J; Harris, AL; Robinson, A; Wilson, R, 1989
)
0.57
" The oestrone sulphate terminal elimination rate constant (lambda z) was concurrently increased (mean of 46 and 79%, respectively, with the 2 dosage regimens)."( Alterations in the metabolism of oestrogens during treatment with aminoglutethimide in breast cancer patients. Preliminary findings.
Kvinnsland, S; Lønning, PE; Thorsen, T; Ueland, PM, 1987
)
0.51
" Patients were then treated with aminoglutethimide according to one of two dosage regimens: (a) aminoglutethimide 1000 mg/day + hydrocortisone 20 mg/day, and (b) aminoglutethimide 250 mg/day."( Correlation of breast tumour aromatase activity and response to aromatase inhibition with aminoglutethimide.
Bezwoda, WR; Dansey, R; Mansoor, N, 1987
)
0.78
" These data show that there is a dose-response relationship between AG dose and induction of warfarin metabolism."( The influence of a graded dose schedule of aminoglutethimide on the disposition of the optical enantiomers of warfarin in patients with breast cancer.
Kvinnsland, S; Lønning, PE; Ueland, PM, 1986
)
0.53
" The lower toxicity and maintained efficacy suggest that this should be the standard dosage regimen."( Low dose aminoglutethimide (125 mg twice daily) with hydrocortisone for the treatment of advanced postmenopausal breast cancer.
Cantwell, BM; Dawes, PJ; Evans, RG; Farndon, J; Harris, AL; Needham, G; Sainsbury, JR; Wilson, R, 1986
)
0.69
" Drug intervention should be on a regular schedule--avoid prn dosage of pain medications."( Dilemmas in managing prostate carcinoma (Part II): Metastatic disease.
Ahmann, FR, 1985
)
0.27
" The slope of the dose-response curve in different individual fish was found to be distinctly uniform and parallel."( Bioassay of fish gonadotrophin by ovarian mitochondrial cholesterol depletion.
Bhadra, R; Bhattacharya, S; Datta, AG; Deb, S; Jamaluddin, M, 1985
)
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
)
1.99
" Side-effects were less at the lowest dosage and were age-related."( Aminoglutethimide dose and hormone suppression in advanced breast cancer.
Dowsett, M; Harris, AL; Jeffcoate, SL; Smith, IE, 1983
)
1.71
" There is a tendency towards an increased response-rate with increased dosage of progestin, in both endometrial and breast carcinoma, while the route of administration appears to be of minor importance."( Progestin therapy of endometrial, breast and ovarian carcinoma. A review of clinical observations.
Kauppila, A, 1984
)
0.27
" Progesterone decreased the secretion of hCG in a dose-response manner (r = -0."( Suppression of human chorionic gonadotropin by progestational steroids.
Dickson, LR; Jawad, MJ; Wilson, EA, 1980
)
0.26
" 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
)
0.83
" These findings led to development of a practical regimen of escalating aminoglutethimide dosage in combination with hydrocortisone for treatment of patients with breast carcinoma."( In vivo and in vitro pharmacological studies of aminoglutethimide as an aromatase inhibitor.
Rosen, HR; Samojlik, E; Santen, RJ; Santner, SJ; Tilsen-Mallett, N; Veldhuis, JD, 1982
)
0.75
"Aminoglutethimide (Elipten), at a dosage between 250 and 1500 mg/d by mouth, was administered in a clinical phase II study to 17 patients with metastasizing carcinoma of the breast resistant to hormones and cytostatic drugs."( [Aminoglutethimide in metastasizing carcinoma of the breast resistant to hormonal and cytostatic treatment (author's transl)].
Rieche, K, 1981
)
2.62
" There may be a trend toward a dose-response effect, which represents a suitable topic for a future prospective trial."( Hormonal palliation of chemoresistant ovarian cancer: three consecutive phase II trials of the Mid-Atlantic Oncology Program.
Ahlgren, JD; Alt, D; Ellison, NM; Gottlieb, RJ; Laluna, F; Lokich, JJ; Sinclair, PR; Ueno, W; Wampler, GL; Yeung, KY, 1993
)
0.29
" Furthermore, patients who are receiving this agent at a dosage of 1000 mg/d or greater should have their serum thyrotropin levels monitored, and replacement therapy with levothyroxine should be initiated when abnormally elevated levels are noted."( Hypothyroidism associated with aminoglutethimide in patients with prostate cancer.
Calis, KA; Cooper, MR; Figg, WD; Headlee, D; Mays, D; Sartor, AO; Thibault, A, 1994
)
0.57
" In the present experiments, dose-response relationships were determined for the effects of aminoglutethimide on corticosterone levels, motor coordination, and body temperature in C57 and DBA mice."( Dissociation of the effect of aminoglutethimide on corticosterone biosynthesis from ataxic and hypothermic effects in DBA and C57 mice.
Gallaher, EJ; Keith, LD; Roberts, AJ, 1993
)
0.79
" While a pregnenolone surge was demonstrated by radioimmunoassay, dose-response testing with exogenous pregnenolone and progesterone (0."( Aminoglutethimide, a corticosteroid synthesis inhibitor, facilitates brain stimulation reward in food-restricted rats: an investigation of underlying mechanisms.
Abrahamsen, GC; Carr, KD; Kandawire, MJ, 1997
)
1.74
" Both chromatographic methods were successful and on an analytical point of view the validations of aminoglutethimide dosing were suitable in both cases."( Aminoglutethimide included in nanocapsules suspension: comparison of GC-MS and HPLC methods for control.
Andre, D; Berrabah, M; Lafont, O; Verite, P; Zahidi, A, 2004
)
1.98
" The bioassay was applied for a dose-response study of mono(2-ethylhexyl)phthalate (MEHP), a chemical known to disrupt several steroidogenic enzymes."( Steroidogenesis-disrupting compounds can be effectively studied for major fertility-related endpoints using in vitro cultured mouse follicles.
Lenie, S; Smitz, J, 2009
)
0.35
" However, current treatments require frequent dosing that results in unstable plasma concentration and low bioavailability, risking serious adverse reactions."( Molecularly Imprinted Polymers Doped with Carbon Nanotube with Aid of Metal-Organic Gel for Drug Delivery Systems.
Chai, MH; Huang, YP; Liu, ZS; Yao, HF; Zhao, L, 2020
)
0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
adrenergic agentAny agent that acts on an adrenergic receptor or affects the life cycle of an adrenergic transmitter.
EC 1.14.14.14 (aromatase) inhibitorAn EC 1.14.14.* (oxidoreductase acting on paired donors, incorporating of 1 atom of oxygen, with reduced flavin or flavoprotein as one donor) inhibitor which interferes with the action of aromatase (EC 1.14.14.14) and so reduces production of estrogenic steroid hormones.
anticonvulsantA drug used to prevent seizures or reduce their severity.
[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
dicarboximideAn imide in which the two acyl substituents on nitrogen are carboacyl groups.
piperidones
substituted aniline
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.00090.003245.467312,589.2998AID2517
thioredoxin reductaseRattus norvegicus (Norway rat)Potency21.23650.100020.879379.4328AID588453
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.96400.01237.983543.2770AID1645841
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency39.20350.001530.607315,848.9004AID1224841; AID1224849
pregnane X nuclear receptorHomo sapiens (human)Potency54.48270.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.58000.000229.305416,493.5996AID743069; AID743075
IDH1Homo sapiens (human)Potency16.36010.005210.865235.4813AID686970
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency27.30600.001723.839378.1014AID743083
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency54.947719.739145.978464.9432AID1159509
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)Potency5.01190.01789.637444.6684AID588834
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency0.89130.794321.275750.1187AID624246
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency6.01200.425612.059128.1838AID504536
gemininHomo sapiens (human)Potency0.79430.004611.374133.4983AID624297
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency31.62280.031610.279239.8107AID884; AID885
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency31.62281.000012.224831.6228AID885
[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)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Sterol O-acyltransferase 1Rattus norvegicus (Norway rat)IC50 (µMol)50.00000.00580.66266.0000AID195026
Bile salt export pumpHomo sapiens (human)IC50 (µMol)566.50000.11007.190310.0000AID1449628; AID1473738
Triosephosphate isomeraseOryctolagus cuniculus (rabbit)Ki1.41001.41002.00502.6000AID238451
Steroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)IC50 (µMol)60.00000.00200.98184.7300AID87273
AromataseHomo sapiens (human)IC50 (µMol)70,459,514.06110.00001.290410.0000AID1307750; AID1467352; AID1467355; AID159823; AID1796390; AID1798975; AID1799682; AID1855795; AID241414; AID242139; AID243423; AID261079; AID288830; AID357965; AID366344; AID38919; AID38923; AID38924; AID39053; AID418721; AID436515; AID479369; AID53391; AID53393; AID53400; AID53401; AID53541; AID53543; AID53544; AID53545; AID53546; AID53549; AID53554; AID53570; AID53572; AID53574; AID601095; AID84877; AID87272
AromataseHomo sapiens (human)Ki1.36150.00000.60469.5010AID1270803; AID1796327; AID1796373; AID1796374; AID238451; AID244080; AID53394; AID53395; AID53739; AID53748; AID53871; AID53893; AID54049
Ribosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)IC50 (µMol)0.27000.00271.62879.9000AID1798975
AromataseRattus norvegicus (Norway rat)IC50 (µMol)20.10000.00181.85646.2000AID53392; AID54069
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)18.50000.00091.230410.0000AID1796390; AID213139
Cytochrome P450 11B2, mitochondrialRattus norvegicus (Norway rat)IC50 (µMol)70.00000.11100.35550.6000AID195025; AID195026
Delta-type opioid receptorMus musculus (house mouse)IC50 (µMol)0.27000.00010.729810.0000AID288830
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[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)
AromataseRattus norvegicus (Norway rat)EC50 (µMol)0.26000.05500.83504.1000AID54068
[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)Ka app0.13000.13000.20500.2800AID54046
AromataseHomo sapiens (human)Km0.09000.02000.13240.7600AID239729; AID244081
AromataseHomo sapiens (human)Ks app0.13000.13000.13000.1300AID53904
AromataseHomo sapiens (human)Log IC500.00340.00340.00400.0045AID243262
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (74)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
C21-steroid hormone biosynthetic processCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
cholesterol metabolic processCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
vitamin D metabolic processCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
steroid biosynthetic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
androgen biosynthetic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
glucocorticoid biosynthetic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
sex differentiationSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
steroid metabolic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
hormone biosynthetic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
progesterone metabolic processSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
C21-steroid hormone biosynthetic processCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
cholesterol metabolic processCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
sterol metabolic processCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
vitamin D metabolic processCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
cellular response to peptide hormone stimulusCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
cortisol metabolic processCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
glucocorticoid biosynthetic processCholesterol side-chain cleavage enzyme, mitochondrialHomo 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)
quinone catabolic processRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
iron ion bindingCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
cholesterol monooxygenase (side-chain-cleaving) activityCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
heme bindingCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
steroid 17-alpha-monooxygenase activitySteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
iron ion bindingSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
oxygen bindingSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
heme bindingSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
17-alpha-hydroxyprogesterone aldolase activitySteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
iron ion bindingCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
protein bindingCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
cholesterol monooxygenase (side-chain-cleaving) activityCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
heme bindingCholesterol side-chain cleavage enzyme, mitochondrialHomo 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)
dihydronicotinamide riboside quinone reductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
zinc ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
electron transfer activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
oxidoreductase activity, acting on other nitrogenous compounds as donorsRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
chloride ion bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
protein homodimerization activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
FAD bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
melatonin bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
resveratrol bindingRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
NAD(P)H dehydrogenase (quinone) activityRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
mitochondrionCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
mitochondrial inner membraneCholesterol side-chain cleavage enzyme, mitochondrial Bos taurus (cattle)
endoplasmic reticulumSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
endoplasmic reticulum membraneSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
axonSteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
neuronal cell bodySteroid 17-alpha-hydroxylase/17,20 lyaseHomo sapiens (human)
mitochondrionCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
mitochondrial inner membraneCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
mitochondrial matrixCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
mitochondrial inner membraneCholesterol side-chain cleavage enzyme, mitochondrialHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
nucleoplasmRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
extracellular exosomeRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
cytosolRibosyldihydronicotinamide dehydrogenase [quinone]Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (276)

Assay IDTitleYearJournalArticle
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC 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.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
AID226409Relative potency as IC50 compared to aminoglutethimide IC50=18.5 uM2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.
AID418724Cytotoxicity against human LNCAP cells after 72 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
AID194205Partial remission of DMBA-induced hormone dependent mammary carcinoma rats at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID87273In vitro inhibition of progesterone production in hamster ovarian tissue1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID229813Ratio of androstenedione-Ki to testosterone-Ki for human placental cytochrome P450 19A11987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID194281Percentage inhibition of rat ovarian estrogen secretion as E2 concentration in right ventricle 8 hr after subcutaneous dose1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID196132Unchanged DMBA-induced hormone dependent mammary tumor area in rats at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID190721Complete+partial regression of DMBA-induced mammary tumors in rats at 100 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID56617Inhibition of bovine adrenal desmolase (IC50) relative to aminoglutethimide1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID191062Progression of DMBA-induced mammary tumors in rats at 30 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID194201Complete remission of DMBA-induced hormone dependent mammary carcinoma in rats at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID418721Inhibition of aromatase after 30 mins by fluorescence assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
AID54069In vitro inhibition of rat ovarian microsomal Cytochrome P450 19A11995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID146826In vitro inhibition of O-demethylase (p-nitroanisol) in rat hepatic microsomes1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID186284Reduction in plasma estradiol (E2) in PMSG(pregnant mares serum gonadotropin)-stimulated female rats after 6 hr at 8.61 umol/kg subcutaneous dose1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID159824Inhibition of human placental aromatase1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID53393Inhibition of human placental cytochrome P450 19A1 with androstenedione1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID56609Inhibition of bovine cholesterol side-chain cleavage desmolase, cytochrome P450 11A11983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Analogues of aminoglutethimide: selective inhibition of cholesterol side-chain cleavage.
AID53731Inhibition of human placental aromatase Cytochrome P450 19A11983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Analogues of aminoglutethimide: selective inhibition of cholesterol side-chain cleavage.
AID53394Inhibition of human placental cytochrome P450 19A1 with testosterone1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID184591Tested for its effect on estradiol concentration in the pregnant mare serum gonadotropin (PMSG) primed SD rats plasma obtained from ovarian vein at 796 pg/mL1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID53546Inhibition of Cytochrome P450 19A1 in human placenta1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Crystallographic and molecular modeling studies on 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione and its butyl analogue, inhibitors of mammalian aromatase. Comparison with natural substrates: prediction of enantioselectivity for N-alkyl derivatives.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID225465Effect 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.
AID204490Initial DMBA-induced mammary tumor number in rats at 100mg/kgx42(po), (control = 20 tumors)1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID53549Inhibition of human placental microsome cytochrome P450 19A11991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
AID503308Antiproliferative activity against human PC3 cells at 30 uM after 120 hrs by MTT assay relative to DMSO2006Nature chemical biology, Jun, Volume: 2, Issue:6
Identifying off-target effects and hidden phenotypes of drugs in human cells.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID186283Reduction in plasma estradiol (E2) in PMSG(pregnant mares serum gonadotropin)-stimulated female rats after 1 hr at 8.61 umol/kg subcutaneous dose1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID436515Inhibition of human placental aromatase assessed as conversion of [1-beta-3H]androstenedione to [1beta-3H]estrone after 20 mins by liquid scintillation counting2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
AID56611Inhibition of bovine adrenal desmolase1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
AID53871Inhibition of Cytochrome P450 19A1 against testosterone at 1.5 uM (Km=0.13 uM)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
AID191059Progression of DMBA-induced mammary tumors in rats at 100 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID1270803Inhibition of human aromatase extracted from placental microsomes using [1,2-3H]androstenedione as substrate after 30 mins2015European journal of medicinal chemistry, Nov-13, Volume: 105Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.
AID54197Percent inhibition of human placental Cytochrome P450 19A1 at 3:1 inhibitor: androstenedione (0.7 uM) ratio1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives.
AID243262Inhibitory concentration against human placental aromatase as logIC502004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID53748Competitive inhibition of human placental Cytochrome P450 19A11991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
AID241414Inhibitory concentration against human placental aromatase2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID288830Inhibition of human aromatase2007Journal of medicinal chemistry, Jun-14, Volume: 50, Issue:12
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
AID53545Inhibition of Cytochrome P450 19A1 against testosterone at 1.5 uM (Km=0.13 uM)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
AID230572Relative potency calculated from the values of IC50 and relative to AG in human placental aromatase1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID56618Inhibition of bovine adrenal desmolase cytochrome P450 11A1 at 50 ug/mL1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Analogues of aminoglutethimide: selective inhibition of aromatase.
AID1467355Inhibition of CYP19 in human placental microsome using [1beta-3H]-androstenedione as substrate after 15 mins in presence of NADPH by liquid scintillation counter method2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity.
AID327555Displacement of [131I]IMTO from CYP450c 11 in Wistar rat adrenal membrane2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
New selective inhibitors of steroid 11beta-hydroxylation in the adrenal cortex. Synthesis and structure-activity relationship of potent etomidate analogues.
AID53543Inhibition of Human placental Cytochrome P450 19A11995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID84877In vitro inhibition of estrogen production in hamster ovarian tissue1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID46888Inhibition of Bovine adrenal cholesterol side chain cleavage cytochrome P450 at 50 ug/mL1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID195784Final DMBA-induced hormone dependent mammary tumor number in rats at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID39054Inhibition of human placental aromatase, cytochrome P450 19A1 at 20 uM1999Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.
AID1307750Inhibition of human aromatase transfected in human MCF7 cells2016Journal of medicinal chemistry, 06-09, Volume: 59, Issue:11
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID53391In vitro inhibitory concentration against human placental Cytochrome P450 19A was determined using [1-beta,2beta-3H]testosterone as radioligand1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID227621In vitro inhibition of aldosterone production in rat adrenal tissue1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID418725Cytotoxicity against human Lu cells after 72 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
AID177888Inhibition of aromatase-mediated androstenedione-induced uterine hypertrophy in immature rats1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID53572In vitro inhibition of [1,2,6,7-3H]-androstenedione binding to human placental microsome cytochrome P450 19A12002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.
AID32953Compound was tested for percent inhibition of bovine adrenal desmolase1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID343719Inhibition of aromatase in human placental microsomes at 50 uM relative to control2008Journal of natural products, Jul, Volume: 71, Issue:7
Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity.
AID53392Inhibition of rat ovarian Cytochrome P450 19A1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID39053Inhibition of aromatase activity in human placental microsomes2002Bioorganic & medicinal chemistry letters, Oct-21, Volume: 12, Issue:20
Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.
AID53544Inhibition of Cytochrome P450 19A1 against Androstenedione at 0.25 uM (Km=55 nM)1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID243073Ratio of apparent Ki and Km value against human aromatase2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID418722Cytotoxicity against mouse Hepa-1c1c7 cells after 72 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID159823Inhibition of human placental aromatase1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID56604Inhibition of bovine desmolase, cytochrome P450 11A11987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID195025In vitro inhibition of ACTH-stimulated aldosterone biosynthesis in rat adrenal slices1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID409955Inhibition of mouse liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID194280Percentage inhibition of rat ovarian estrogen secretion as E2 concentration in right ventricle 1 hr after subcutaneous dose1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID409953Inhibition of mouse liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID601095Inhibition of aromatase in human placental microsomes assessed as inhibition of aromatization of [1,2,6,7-3H] androstenedione by flow scintillation analysis2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID418723Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
AID357965Inhibition of aromatase from human placental microsomes2001Journal of natural products, Oct, Volume: 64, Issue:10
Aromatase inhibitors from Broussonetia papyrifera.
AID53395Inhibition of human placental cytochrome P450 19A1 with androstenedione1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID230573Relative potency for human placental aromatase P450 19A1 compared to aminoglutethimide1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID53714Inhibition of Cytochrome P450 19A1 at the concentration of 1.5 uM1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
AID194208Progression of DMBA-induced hormone dependent mammary carcinoma in rats at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID183091Inhibition of androstenedione-induced P450 19A1 aromatase-mediated uterotrophic effect1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID38393In vitro inhibition of Aminopyrine N-Demethylase in rat hepatic microsomes1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID54198Percent inhibition of human placental Cytochrome P450 19A1 at 6:1 inhibitor: androstenedione (0.7 uM) ratio1985Journal of medicinal chemistry, Jun, Volume: 28, Issue:6
Aromatase inhibitors. Synthesis and biological activity of androstenedione derivatives.
AID53563Inhibition of Cytochrome P450 19A1 activity 6 hr after oral administration1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Mechanism and inhibition of cytochrome P-450 aromatase.
AID479369Inhibition of human placental microsome CYP192010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19).
AID187713Inhibition of PMSG-primed rat ovarian estrogen secretion as E2 concentration in right ventricle after subcutaneous dose1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID376616Inhibition of aromatase in human placental microsomes at 50 uM by radiometric method relative to control2006Journal of natural products, Apr, Volume: 69, Issue:4
Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
AID261080Potency against CYP19 relative to aminoglutethimide2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors.
AID195781Initial DMBA-induced hormone dependent mammary tumor number in rats number at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID53570Inhibition of human placental microsome cytochrome P450 19A1 aromatase2001Journal of medicinal chemistry, Mar-01, Volume: 44, Issue:5
A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
AID1467352Inhibition of human CYP19 using [1beta-3H]-androstenedione as substrate after 15 mins in presence of NADPH by liquid scintillation counter method2017Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12
Evaluation of synthesized coumarin derivatives on aromatase inhibitory activity.
AID239729Apparent Km against human aromatase2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID53893Apparent inhibition constant (Ki) for cytochrome P450 19A11988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
AID190568Percent response towards stable disease of DMBA-induced mammary tumors in rats at 30 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID366344Inhibition of aromatase in human placental microsomes2008Bioorganic & medicinal chemistry letters, Aug-15, Volume: 18, Issue:16
Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors.
AID261079Inhibition of CYP192006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and biological evaluation of 5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles: potent and selective aromatase inhibitors.
AID38923Concentration inhibiting Aromatase1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
AID54046Apparent inhibitory constant (Ka) for Cytochrome P450 19A11985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Analogues of aminoglutethimide: selective inhibition of aromatase.
AID53554Inhibition of cytochrome P450 19A1 of human placental microsomes with [1-beta,2beta-3H]testosterone2003Bioorganic & medicinal chemistry letters, May-05, Volume: 13, Issue:9
Preparation and pharmacological profile of 7-(alpha-azolylbenzyl)-1H-indoles and indolines as new aromatase inhibitors.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID204487Median range of new DMBA-induced mammary tumors present after 30.0 mg/kg therapy1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID39058Inhibition of cytochrome P450 Aromatase (IC50) relative to aminoglutethimide1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
AID243423Inhibitory concentration against human placental aromatase by deutirium oxide release2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID38919Inhibition of human placental aromatase, cytochrome P450 19A11999Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.
AID53739Binding affinity was measured on Cytochrome P450 19A11990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Mechanism and inhibition of cytochrome P-450 aromatase.
AID190565Percent response towards stable disease of DMBA-induced mammary tumors in rats at 100 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID243026Ratio of apparent Ki and Km for human placental aromatase2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID244080Inhibitory constant against human placental atomatase at pH 7.0 and 37 degree C2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID53541In vitro inhibition of human placental Cytochrome P450 19A11993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.
AID1191271Inhibition of human aromatase in term placenta microsome assessed as radioactivity2015European journal of medicinal chemistry, Jan-27, Volume: 90Bioactive benzofuran derivatives: moracins A-Z in medicinal chemistry.
AID238451Apparent Ki against human aromatase2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID184751Tested for its effect on estradiol concentration in the pregnant mare serum gonadotropin (PMSG) primed SD rats plasma obtained from right ventricle at 260 pg/mL1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID54049Inhibitory constant (Ki) for Cytochrome P450 19A11985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Analogues of aminoglutethimide: selective inhibition of aromatase.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID213139Inhibition of Thromboxane-A synthase2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID53712Inhibition of Cytochrome P450 19A1 at the concentration of 0.25 uM1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID225646Inhibition of 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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID187714Inhibition of PMSG-primed rat ovarian estrogen secretion as E2 concentration in right ventricle 1 hr after subcutaneous dose1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID234694Relative potency against human placental aromatase cytochrome P450 19A1 compared to aminoglutethimide IC50 =18.5 uM1999Bioorganic & medicinal chemistry letters, Jul-19, Volume: 9, Issue:14
1-[(Benzofuran-2-yl)phenylmethyl]-triazoles and -tetrazoles - potent competitive inhibitors of aromatase.
AID173444In vivo aromatase inhibition as minimum inhibitory oral dose in gonadotropin-induced uterotrophic assay in immature rats1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID242139Inhibitory concentration against human placental aromatase by deutirium oxide release2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID244081Michaelis-Menten constant against human placental aromatase at pH 7.0 and 37 degree C2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID204493Initial DMBA-induced mammary tumor number in rats at 30.0 mg/kg x42 (p.o.), (control = 20 tumors)1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID54068In vitro inhibition of cytochrome P450 19A1 by rat ovarian microsomes incubated with [3H]androstenedione and NADPH-generating system.1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID87272In vitro inhibition of estrogen production in hamster ovarian tissue1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID219559Inhibition of bovine adrenal cholesterol side chain cleavage(CSCC) cytochrome P450 11A11988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
AID53401Inhibition of human placental cytochrome P450 19A1 with testosterone1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
AID159826Potency for human placental aromatase relative to aminoglutethimide1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
AID53400Inhibition of human placental cytochrome P450 19A1 with androstenedione1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
AID409956Inhibition of mouse brain MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID84878In vitro inhibition of progesterone production in hamster ovarian tissue1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1855795Inhibition of aromatase in human breast tumor2022European journal of medicinal chemistry, Nov-05, Volume: 241An overview on Estrogen receptors signaling and its ligands in breast cancer.
AID38924In vitro inhibition of cytochrome P450 19A1 Aromatase1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID159825Inhibition of human placental aromatase cytochrome P450 19A1 enzyme1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID56607Inhibition of bovine cholesterol side-chain cleavage desmolase, cytochrome P450 11A11983Journal of medicinal chemistry, Jan, Volume: 26, Issue:1
Analogues of aminoglutethimide: selective inhibition of cholesterol side-chain cleavage.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID227622In vitro inhibition of corticosterone production in rat adrenal tissue1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID187717Inhibition of PMSG-primed rat ovarian estrogen secretion as E2 concentration in right ventricle 8 hr after subcutaneous dose1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
New aromatase inhibitors. Synthesis and biological activity of pyridyl-substituted tetralone derivatives.
AID194198Percent change in DMBA-induced hormone dependent mammary tumor area in rats after 28 day therapy at 10.0 mg/kg1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans, and tetralins.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID56616Inhibition of bovine adrenal desmolase at 25 uM1992Journal of medicinal chemistry, Jun-12, Volume: 35, Issue:12
Synthesis and aromatase inhibition of 3-cycloalkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID53727Inhibition of Cytochrome P450 19A1 at 20 ug/mL1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Analogues of aminoglutethimide: selective inhibition of aromatase.
AID53904Apparent dissociation constant(Ks) for cytochrome P450 19A11988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Analogues of aminoglutethimide based on 1-phenyl-3-azabicyclo[3.1.0]hexane-2,4-dione: selective inhibition of aromatase activity.
AID53713Inhibition of Cytochrome P450 19A1 at the concentration of 0.75 uM1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
AID204484Median range of new DMBA-induced mammary tumors present after 100 mg/kg therapy1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID190724Complete+partial regression of DMBA-induced mammary tumors in rats at 30 mg/kg oral dose1991Journal of medicinal chemistry, Apr, Volume: 34, Issue:4
Synthesis and aromatase inhibitory activity of novel 1-(4-aminophenyl)-3-azabicyclo[3.1.0]hexane- and -[3.1.1]heptane-2,4- diones.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID53574Inhibitory activity against human placental cytochrome P450 19A11987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID195026In vitro inhibition of ACTH-stimulated aldosterone biosynthesis in rat adrenal slices1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1799682Aromatase Assay from Article 10.1080/14756360400015256: \\Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.\\2005Journal of enzyme inhibition and medicinal chemistry, Apr, Volume: 20, Issue:2
Benzofuran- and furan-2-yl-(phenyl)-3-pyridylmethanols: synthesis and inhibition of P450 aromatase.
AID1796373CYP19 Assay from Article 10.1016/j.bmc.2005.03.050: \\Synthesis and characterization of azole isoflavone inhibitors of aromatase.\\2005Bioorganic & medicinal chemistry, Jun-02, Volume: 13, Issue:12
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
AID1796390Aromatase Assay from Article 10.1021/jm991180u: \\1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.\\2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID1796374CYP19 Assay from Article 10.1016/j.bmc.2005.07.038: \\Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.\\2005Bioorganic & medicinal chemistry, Dec-01, Volume: 13, Issue:23
Lead optimization of 7-benzyloxy 2-(4'-pyridylmethyl)thio isoflavone aromatase inhibitors.
AID1796327CYP19 Assay from Article 10.1021/jm0306024: \\Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.\\2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.
AID1798975QR2 Assay and IC50 Value Determination from Article 10.1021/jm801335z: \\Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.\\2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1345280Human CYP19A1 (CYP11, CYP17, CYP19, CYP20 and CYP21 families)2009The Journal of clinical endocrinology and metabolism, Aug, Volume: 94, Issue:8
In vitro kinetic properties of the Thr201Met variant of human aromatase gene CYP19A1: functional responses to substrate and product inhibition and enzyme inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,407)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990904 (64.25)18.7374
1990's295 (20.97)18.2507
2000's139 (9.88)29.6817
2010's53 (3.77)24.3611
2020's16 (1.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.93

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.93 (24.57)
Research Supply Index7.39 (2.92)
Research Growth Index4.11 (4.65)
Search Engine Demand Index77.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials135 (9.07%)5.53%
Reviews139 (9.34%)6.00%
Case Studies95 (6.38%)4.05%
Observational0 (0.00%)0.25%
Other1,120 (75.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
"A Phase II Trial of Early Medical Adrenalectomy for D0.5 Prostate Cancer" [NCT00006371]Phase 22 participants (Actual)Interventional2000-05-31Terminated(stopped due to low accrual)
A Randomized Phase III Study Comparing Tamoxifen vs. Tamoxifen + Aminoglutethimide in Postmenopausal, Hormone Receptor-positive Patients [NCT00309491]Phase 32,021 participants (Actual)Interventional1990-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]