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Drug-Target Interaction

Drug

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PubChem ID:5870
Structure:
Synonyms:
(13S)-3-hydroxy-13-methyl-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]p
(13S)-3-hydroxy-13-methyl-7,8,9,11,12,13,15,16-octahydro-6H-cyclopenta[a]phenanthren-17(14H)-one
(8R,9S,13S,14S)-3-hydroxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one
1,3,5(10)-Estratrien-3-ol-17-one
1,3,5(10)-Oestratrien-3-ol-17-one
3-08-00-01171 (Beilstein Handbook Reference)
3-Hydroxy-1,3,5(10)-estratrien-17-one
3-Hydroxy-17-keto-estra-1,3,5-triene
3-Hydroxy-17-keto-oestra-1,3,5-triene
3-Hydroxy-oestra-1,3,5(10)-trien-17-one
3-Hydroxyestra-1,3,5(10)-trien-17-one
3-Hydroxyestra-1,3,5(10)-triene-17-one
37242-41-4
438-67-5 (SODIUM SULFATE)
46573_FLUKA
46573_RIEDEL
481-97-0 (HYDROGEN SULFATE)
53-16-7
AB00382990
ACon0_000083
ACon1_000122
AIDS-031083
AIDS031083
Aquacrine
BPBio1_000868
BRN 1915077
BSPBio_000788
C00468
C18H22O2
CCRIS 285
CHEBI:17263
CMC_13458
Crinovaryl
Cristallovar
Crystogen
D00067
DB00655
delta-1,3,5-estratrien-3-beta-ol-17-one
delta-1,3,5-Estratrien-3beta-ol-17-one
delta-1,3,5-oestratrien-3-beta-ol-17-one
delta-1,3,5-Oestratrien-3beta-ol-17-one
Destrone
Disynformon
E(sub 1)
E1274_SIGMA
E9750_SIGMA
EINECS 200-164-5
Endofolliculina
Esterone
estra-1(10),2,4-trien-17-one, 3-hydroxy-
Estra-1,3,5(10)-trien-17-one, 3-hydroxy-
ESTROGENIC SUBSTANCE
estrol
Estron
Estrona
Estrona [INN-Spanish]
Estrona [Spanish]
Estrone
Estrone (E1)
Estrone (JAN/USP/INN)
Estrone (TN)
Estrone [USAN:INN]
ESTRONE, U.S.P.
Estrone-A
Estronum [INN-Latin]
Estrovarin
Estrugenone
Estrusol
EU-0100513
Fem-O-Gen
Femestrone injection
Femidyn
Folikrin
Folipex
Folisan
Follestrine
Follestrol
Follicular hormone
Folliculin
Folliculine
Folliculine benzoate
Follicunodis
Glandubolin
Hiestrone
Hormestrin
Hormofollin
Hormovarine
HSDB 3324
Kestrone
Ketodestrin
Ketohydroxy-estratriene
Ketohydroxyestrin
Ketohydroxyoestrin
Kolpon
LMST02010004
Lopac0_000513
LS-64884
MEGxm0_000444
Menagen
Menformon
Menformon A
Mestronaq
MLS000028475
MLS001077340
NATURAL ESTROGENIC SUBSTANCE-ESTRONE
NCGC00023643-03
NCGC00023643-04
NCGC00023643-05
NCGC00023643-06
NCGC00179433-01
NCGC00179433-02
NCGC00179433-03
nchembio.76-comp37
NSC 9699
NSC9699
Oestrin
Oestroform
Oestrone
Oestrone [Steroidal oestrogens]
Oestrone, Estrone
Oestronum
Oestroperos
Ovex (tablets)
Ovifollin
Perlatan
Prestwick0_000914
Prestwick1_000914
Prestwick2_000914
Prestwick3_000914
SGCUT00128
SMP1_000123
SMR000058338
Solliculin
SPBio_002977
Spectrum5_002047
STOCK1N-57203
Theelin
Thelestrin
Thelykinin
Thynestron
Tokokin
to_000049
Unden
Unden (pharmaceutical)
Unden (pharmaceutical) (VAN)
Wynestron
[2,4,6,7-3H]-E1
ATC-Codes:

Target

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Uniprot ID:CP19A_RAT
Synonyms:
Aromatase
CYPXIX
Cytochrome P450 19A1
Estrogen synthetase
P-450AROM
EC-Numbers:1.14.14.1
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

8142297
Effect of aromatase inhibitors on estrogen 2-hydroxylase in rat liver.. H S Purba; E J King; P Richert; A S Bhatnagar (1994) The Journal of steroid biochemistry and molecular biology display abstract
The effect of aromatase inhibitors, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide on the inhibition of estrogen 2-hydroxylase activity in rat liver microsomes in vitro and on its induction in vivo has been examined. Estrogen 2-hydroxylase was found to have over twice the affinity for estradiol compared to estrone. Using high pressure liquid chromatography and employing estradiol as a substrate, the IC50 values were 2.2, 98, 110 and 908 microM for the reference compound ketoconazole and the aromatase inhibitors, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide, respectively. Similar IC50 values were obtained using estrone as a substrate and by a tritiated water method employing estradiol as a substrate. The Km value for estrogen 2-hydroxylase with estradiol as a substrate using a tritiated water method was 4.3 microM with a Vmax of 11.89 nmol/h/mg. Ketoconazole, CGS 16949A and aminoglutethimide exhibited non-competitive inhibition whereas 4-hydroxyandrostenedione appeared to be a competitive inhibitor of estrogen 2-hydroxylase. The Ki values were 2.6, 72, 114 and 958 microM for ketoconazole, 4-hydroxyandrostenedione, CGS 16949A and aminoglutethimide, respectively. All three aromatase inhibitors were weak inhibitors of estrogen 2-hydroxylase as compared to the reference drug, ketoconazole. Following treatment of rats with aminoglutethimide (40 mg/kg/day; i.p.; for 3 days), estrogen 2-hydroxylase activity was increased by 28 and 30% using estradiol and estrone as substrates, respectively. Following treatment of rats with CGS 16949A (2 mg/kg/day; p.o.; for 3 days), the corresponding increase in estrogen 2-hydroxylase activity was 48 and 44%. The results of this study indicate that the aromatase inhibitors, aminoglutethimide and CGS 16949A are only weak inhibitors of estrogen 2-hydroxylase activity in vitro and show no evidence of inhibition in vivo. On the contrary, there was some evidence to suggest that both aminoglutethimide and CGS 16949A induce estrogen metabolism following repeated administration. Therefore, aminoglutethimide and CGS 16949A may lower estrogen levels not only by primarily inhibiting their synthesis but also by inducing the metabolism of estrogens.