Target Validation Information
TTD ID T13260
Target Name Aromatase (CYP19A1)
Type of Target
Successful
Drug Potency against Target Aminoglutethimide Drug Info IC50 = 18500 nM [36]
Anastrozole Drug Info IC50 = 15 nM [35]
Exemestane Drug Info IC50 = 5 nM [35]
Letrozole Drug Info IC50 = 0.8 nM [35]
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 1860 nM [14]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info IC50 = 8000 nM [15]
(2S)-5,7,2',4'-tetrahydroxyflavanone Drug Info IC50 = 2200 nM [2]
(2S)-abyssinone II Drug Info IC50 = 400 nM [2]
(2S)-euchrenone a7 Drug Info IC50 = 3400 nM [2]
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Drug Info IC50 = 950 nM [19]
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Drug Info IC50 = 3560 nM [22]
1-(2-phenoxybenzyl)-1H-imidazole Drug Info IC50 = 389.2 nM
1-(3-(4-fluorophenyl)propyl)-1H-imidazole Drug Info IC50 = 310 nM [25]
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Drug Info IC50 = 129 nM [8]
1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone Drug Info IC50 = 1840 nM
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Drug Info IC50 = 15 nM [16]
1-(4-nitro-2-phenoxybenzyl)-1H-imidazole Drug Info IC50 = 11.45 nM
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Drug Info IC50 = 5.59 nM
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Drug Info IC50 = 90 nM [4]
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Drug Info IC50 = 4000 nM [22]
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Drug Info IC50 = 74 nM [25]
1-(9H-fluoren-9-yl)-1H-imidazole Drug Info IC50 = 2850 nM [22]
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Drug Info IC50 = 210 nM [24]
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 89 nM [34]
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Drug Info IC50 = 205 nM [1]
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Drug Info IC50 = 970 nM [34]
1-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 150 nM
1-Naphthalen-2-yl-1H-imidazole Drug Info IC50 = 2821 nM [8]
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Drug Info IC50 = 160 nM [25]
10-EPI-8-DEOXY-CUMAMBRIN B Drug Info IC50 = 7 nM [25]
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Drug Info IC50 = 2 nM [25]
2,3,4-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 3570 nM
2,3,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 2280 nM
2,3-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 980 nM
2,4-Dimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 11140 nM
2,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 760 nM
2,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 1820 nM
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Drug Info IC50 = 190 nM
2-(3-hydroxyphenyl)-7-methoxychroman-4-one Drug Info IC50 = 3500 nM [15]
2-(4-hydroxyphenyl)-7-methoxychroman-4-one Drug Info IC50 = 3700 nM [15]
2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one Drug Info IC50 = 770 nM [7]
2-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 7900 nM
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Drug Info IC50 = 4300 nM [15]
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Drug Info IC50 = 430 nM [4]
3,4'-(Ethane-1,2-diyl)dibenzenamine Drug Info IC50 = 3210 nM
3,4,5-Trimethoxy-3'-amino-trans-stilbene Drug Info IC50 = 16420 nM
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 900 nM
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Drug Info IC50 = 1 nM [25]
3,4-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 14510 nM
3,5-Diacetoxy-4'-amino-trans-stilbene Drug Info IC50 = 2940 nM
3,5-Diamino-4'-amino-trans-stilbene Drug Info IC50 = 8510 nM
3,5-Dihydroxyl-4'-amino-trans-stilbene Drug Info IC50 = 5000 nM
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info IC50 = 590 nM
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Drug Info IC50 = 390 nM
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 1507 nM [11]
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info IC50 = 6045 nM [11]
3-(2,2-Diphenyl-vinyl)-pyridine Drug Info IC50 = 3630 nM [5]
3-(3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 4073 nM [11]
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 1787 nM [11]
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [29]
3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione Drug Info IC50 = 8400 nM [29]
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Drug Info IC50 = 10040 nM [29]
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Drug Info IC50 = 10200 nM [29]
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 3551 nM [11]
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 9107 nM [8]
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 1805 nM [8]
3-(6-Ethoxy-naphthalen-2-yl)-pyridine Drug Info IC50 = 6638 nM [8]
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Drug Info IC50 = 814 nM [11]
3-(6-methoxynaphthalen-2-yl)pyridine Drug Info IC50 = 600 nM [21]
3-(imidazolylmethyl)-4'-methoxyflavone Drug Info IC50 = 80 nM [13]
3-(imidazolylmethyl)-4'-nitroflavone Drug Info IC50 = 45 nM [13]
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Drug Info IC50 = 470 nM [13]
3-(imidazolylmethyl)flavone Drug Info IC50 = 71 nM [13]
3-(naphthalen-2-yl)pyridine Drug Info IC50 = 5700 nM [21]
3-Amino-4'-amino-trans-stilbene Drug Info IC50 = 7470 nM
3-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 4810 nM [5]
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Drug Info IC50 = 2693 nM [26]
3-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 2040 nM [5]
3-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 3550 nM [5]
3-Methoxyl-4'-amino-trans-stilbene Drug Info IC50 = 3080 nM
3-Nitro-4'-nitro-trans-stilbene Drug Info IC50 = 8330 nM
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3680 nM [5]
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2800 nM [5]
3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4060 nM [5]
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 130 nM [5]
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 230 nM [5]
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1810 nM [5]
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 180 nM [5]
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4720 nM [5]
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 12630 nM [5]
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7830 nM [5]
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 7370 nM [5]
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4260 nM [5]
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 4050 nM [5]
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 7080 nM [5]
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 7680 nM [5]
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 2540 nM [5]
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 2490 nM [5]
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 4310 nM [5]
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 5570 nM [5]
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 6360 nM [5]
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3930 nM [5]
3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 4600 nM [5]
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 9740 nM [5]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Drug Info IC50 = 2440 nM [26]
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Drug Info IC50 = 2830 nM [26]
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 4100 nM [13]
4'-bromo-3-(imidazolylmethyl)flavone Drug Info IC50 = 440 nM [13]
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Drug Info IC50 = 1800 nM [13]
4'-cyano-3-(imidazolylmethyl)flavone Drug Info IC50 = 69 nM [13]
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 2100 nM [22]
4-((1H-imidazol-1-yl)methyl)benzonitrile Drug Info IC50 = 15 nM [16]
4-(1-Imidazol-1-yl-vinyl)-benzonitrile Drug Info IC50 = 0.7 nM [31]
4-(2,2-Diphenyl-vinyl)-pyridine Drug Info IC50 = 100 nM [5]
4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info IC50 = 760 nM [22]
4-(3,4,5-Trimethoxyphenethyl)aniline Drug Info IC50 = 2790 nM
4-(3,4-Dimethoxyphenethyl)aniline Drug Info IC50 = 670 nM
4-(3,5-Dimethoxyphenethyl)benzenamine Drug Info IC50 = 2760 nM
4-ANDROSTENE-3-17-DIONE Drug Info Ki = 20 nM [30]
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Drug Info IC50 = 940 nM [34]
4-Fluoren-9-ylidenemethyl-pyridine Drug Info IC50 = 2740 nM [5]
4-Imidazol-1-yl-2-phenyl-chroman-7-ol Drug Info IC50 = 40 nM [4]
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Drug Info IC50 = 40 nM [34]
4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one Drug Info IC50 = 16.5 nM
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Drug Info IC50 = 53 nM
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Drug Info IC50 = 1900 nM
4-Imidazol-1-ylmethylthioxanthen-9-one Drug Info IC50 = 3.98 nM
4-Imidazol-1-ylmethylxanthen-9-one Drug Info IC50 = 17 nM
4-Indan-(1E)-ylidenemethyl-pyridine Drug Info IC50 = 6700 nM [5]
4-Indan-(1Z)-ylidenemethyl-pyridine Drug Info IC50 = 12730 nM [5]
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 663 nM [26]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info IC50 = 3070 nM [26]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3400 nM [5]
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 5430 nM [5]
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1990 nM [5]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1550 nM [5]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 800 nM [5]
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 3960 nM [5]
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 3720 nM [5]
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 280 nM [5]
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 770 nM [5]
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info IC50 = 1280 nM [5]
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info IC50 = 1710 nM [5]
5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline Drug Info IC50 = 170 nM [22]
5-(2-(1H-imidazol-1-yl)ethyl)quinoline Drug Info IC50 = 350 nM [22]
5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one Drug Info IC50 = 2100 nM [34]
5-Indan-(1E)-ylidenemethyl-1H-imidazole Drug Info IC50 = 955 nM [6]
5-Indan-(1Z)-ylidenemethyl-1H-imidazole Drug Info IC50 = 130 nM [6]
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 27 nM [6]
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Drug Info IC50 = 100 nM [6]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Drug Info IC50 = 7450 nM [5]
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Drug Info IC50 = 790 nM [5]
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Drug Info IC50 = 4330 nM [5]
5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole Drug Info IC50 = 4830 nM [5]
6-Imidazol-1-yl-isoquinoline Drug Info IC50 = 3060 nM [22]
7,4'-Dihydroxyflavone Drug Info IC50 = 2 nM [25]
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info IC50 = 680 nM [22]
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Drug Info IC50 = 100 nM [22]
7-((1H-imidazol-1-yl)methyl)isoquinoline Drug Info IC50 = 1380 nM [22]
7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one Drug Info IC50 = 3400 nM [15]
7-hydroxy-2-phenylchroman-4-one Drug Info IC50 = 3800 nM [15]
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Drug Info IC50 = 3700 nM [34]
8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one Drug Info IC50 = 1100 nM [34]
9-Hydroxy-7,8-benzoflavone Drug Info IC50 = 20 nM [25]
ALBANOL A Drug Info IC50 = 7500 nM [2]
ALPHA-NAPHTHOFLAVONE Drug Info IC50 = 70 nM [25]
ANDROSTENEDONE Drug Info Ki = 120 nM [27]
APIGENIN Drug Info IC50 = 900 nM [25]
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Drug Info IC50 = 1200 nM [19]
biochanin A Drug Info IC50 = 10.2 nM [25]
Broussoflavonol F Drug Info IC50 = 9700 nM [2]
CGS-18320B Drug Info IC50 = 3 nM [25]
Chrysin Drug Info IC50 = 1 nM [25]
Coumate Drug Info IC50 = 300 nM [24]
DEHYDROLEUCODIN Drug Info IC50 = 15 nM [25]
Docosapentaenoic acid Drug Info IC50 = 16800 nM [12]
FADROZOLE Drug Info IC50 = 17 nM [9]
flavone Drug Info IC50 = 8 nM [25]
Gamma-mangostin Drug Info IC50 = 4970 nM [17]
GARCINONE D Drug Info IC50 = 5200 nM [17]
GOSSYPETIN Drug Info IC50 = 11000 nM [18]
Isogemichalcone C Drug Info IC50 = 7100 nM [2]
ISOLICOFLAVONOL Drug Info IC50 = 100 nM [2]
LIAROZOLE Drug Info IC50 = 5 nM [25]
LIQUIRTIGENIN Drug Info IC50 = 340 nM [18]
LUDARTIN Drug Info IC50 = 55 nM [25]
MDL-18962 Drug Info IC50 = 56.2 nM [32]
MONODICTYOCHROMONE B Drug Info IC50 = 16500 nM [20]
MORACHALCONE A Drug Info IC50 = 4600 nM [2]
MR-16089 Drug Info IC50 = 40 nM [25]
MR-20492 Drug Info IC50 = 200 nM [25]
MR-20494 Drug Info IC50 = 110 nM [25]
MR-20496 Drug Info Ki = 10.3 nM [33]
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2670 nM [10]
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 910 nM [10]
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Drug Info IC50 = 2510 nM [10]
N-[2-(4'-Nitrophenyl)ethyl]-imidazole Drug Info IC50 = 160 nM [25]
NARINGENIN Drug Info IC50 = 2.9 nM [25]
NSC-122427 Drug Info IC50 = 15500 nM [23]
NSC-12999 Drug Info Ki = 25.5 nM [22]
NSC-131736 Drug Info IC50 = 1400 nM [22]
NSC-289311 Drug Info Ki = 6.5 nM [22]
NSC-356483 Drug Info IC50 = 3100 nM [22]
NSC-356781 Drug Info IC50 = 2100 nM [22]
NSC-368272 Drug Info Ki = 5.6 nM [22]
NSC-368280 Drug Info Ki = 1.9 nM [22]
NSC-369087 Drug Info IC50 = 55 nM [22]
NSC-613604 Drug Info Ki = 385 nM [23]
NSC-625409 Drug Info Ki = 52.7 nM [22]
NSC-666292 Drug Info Ki = 33.4 nM [22]
NSC-683634 Drug Info Ki = 15.1 nM [22]
NSC-75308 Drug Info IC50 = 5600 nM [22]
NSC-93358 Drug Info Ki = 266 nM [23]
NSC-94258 Drug Info IC50 = 30.5 nM [25]
NSC-94891 Drug Info IC50 = 9800 nM [23]
Rogletimide Drug Info Ki = 14000 nM [28]
YM-511 Drug Info IC50 = 0.5 nM [3]
Action against Disease Model Testolactone Drug Info Potency and selectivity of aromatase inhibition are parameters which ultimately influence the therapeutic efficacy of aromatase inhibitors. This report describes an in vitro model which allows an assessment of the selectivity with which aromatase inhibitors inhibit estrogen biosynthesis. Estrogen production was stimulated by incubating adult female hamster ovarian tissue with ovine LH. The production rates of estrogens (E), testosterone (T) and progesterone (P) were determined using radioimmunoassays to measure the amount of these steroids released into the incubation medi uM over a 4-hour incubation period. The selectivity of aromatase inhibition was assessed by determining the IC50S with which each inhibitor inhibited the production of E (end product), T (immediateprecursor of E) and P (early precursor of E). Selectivity was studied for each of the 4 aromatase inhibitors, CGS 16949A (a new non-steroidal compound), 4-OH-androstenedione, aminoglutethimide and testolactone. CGS 16949A was the most potent of the four, followed by 4-OH-androstenedione, aminoglutethimide and testolactone. As far as selectivity was concerned, both CGS 16949A and 4-OH-androstenedione selectively inhibited aromatase judging from the IC50s for E and P production (CGS 16949A: IC50 for E & P = 0.03 & 160 microM, resp.; 4-OH-androstenedione: IC50 for E & P = 0.88 & greater than or equal to 330 microM, resp.). Aminoglutethimide was the least selective inhibitor of aromatase (IC50 for E & P = 13 & 60 microM, resp.). For testolactone, the least potent of the four (IC50 for E = 130microM), no conclusive data were obtained concerning the selectivity of aromatase inhibition. Thus a simple, effective and reproducible method is described for assessing the selectivity with which aromatase inhibitors inhibit aromatase. [37]
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