Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T13260 | ||||
Target Name | Cytochrome P450 19 | ||||
Target Type | Successful |
||||
Drug Potency against Target | 1-Imidazol-1-ylmethylxanthen-9-one | Drug Info | IC50 = 150 nM | ||
5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one | Drug Info | IC50 = 2100 nM | [535139] | ||
1-(4-nitro-2-phenoxybenzyl)-1H-imidazole | Drug Info | IC50 = 11.45 nM | |||
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one | Drug Info | IC50 = 390 nM | |||
MDL-18962 | Drug Info | IC50 = 56.2 nM | [534514] | ||
2,4-Dimethoxy-3'-amino-trans-stilbene | Drug Info | IC50 = 11140 nM | |||
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one | Drug Info | IC50 = 40 nM | [535139] | ||
4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one | Drug Info | IC50 = 16.5 nM | |||
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one | Drug Info | IC50 = 940 nM | [535139] | ||
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol | Drug Info | IC50 = 2440 nM | [531085] | ||
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | IC50 = 3070 nM | [531085] | ||
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | IC50 = 663 nM | [531085] | ||
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | IC50 = 814 nM | [528109] | ||
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole | Drug Info | IC50 = 5.59 nM | |||
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole | Drug Info | IC50 = 210 nM | [530712] | ||
3,5-Dimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 590 nM | |||
3,4,5-Trimethoxy-3'-amino-trans-stilbene | Drug Info | IC50 = 16420 nM | |||
1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone | Drug Info | IC50 = 1840 nM | |||
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | IC50 = 1787 nM | [528109] | ||
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 1550 nM | [527456] | ||
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 180 nM | [527456] | ||
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole | Drug Info | IC50 = 15 nM | [529291] | ||
1-(2-phenoxybenzyl)-1H-imidazole | Drug Info | IC50 = 389.2 nM | |||
2,3,5-Trimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 2280 nM | |||
3-Amino-4'-amino-trans-stilbene | Drug Info | IC50 = 7470 nM | |||
2,4-Dimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 760 nM | |||
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4720 nM | [527456] | ||
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 9740 nM | [527456] | ||
4-Fluoren-9-ylidenemethyl-pyridine | Drug Info | IC50 = 2740 nM | [527456] | ||
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 3400 nM | [527456] | ||
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 1280 nM | [527456] | ||
1-Naphthalen-2-yl-1H-imidazole | Drug Info | IC50 = 2821 nM | [527801] | ||
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine | Drug Info | IC50 = 790 nM | [527456] | ||
4-(2,2-Diphenyl-vinyl)-pyridine | Drug Info | IC50 = 100 nM | [527456] | ||
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 7680 nM | [527456] | ||
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 130 nM | [527456] | ||
3-Fluoren-9-ylidenemethyl-pyridine | Drug Info | IC50 = 4810 nM | [527456] | ||
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 12630 nM | [527456] | ||
4-Indan-(1E)-ylidenemethyl-pyridine | Drug Info | IC50 = 6700 nM | [527456] | ||
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 5430 nM | [527456] | ||
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | IC50 = 6045 nM | [528109] | ||
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 3720 nM | [527456] | ||
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 1990 nM | [527456] | ||
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 6360 nM | [527456] | ||
3-(naphthalen-2-yl)pyridine | Drug Info | IC50 = 5700 nM | [529834] | ||
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 2540 nM | [527456] | ||
3-(3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | IC50 = 4073 nM | [528109] | ||
N-[2-(4'-Nitrophenyl)ethyl]-imidazole | Drug Info | IC50 = 160 nM | [530867] | ||
ALPHA-NAPHTHOFLAVONE | Drug Info | IC50 = 70 nM | [530867] | ||
3,5-Diacetoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 2940 nM | |||
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole | Drug Info | IC50 = 90 nM | [527222] | ||
3-(6-methoxynaphthalen-2-yl)pyridine | Drug Info | IC50 = 600 nM | [529834] | ||
3-(6-Ethoxy-naphthalen-2-yl)-pyridine | Drug Info | IC50 = 6638 nM | [527801] | ||
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | IC50 = 9107 nM | [527801] | ||
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 1710 nM | [527456] | ||
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine | Drug Info | IC50 = 2830 nM | [531085] | ||
5-Indan-(1E)-ylidenemethyl-1H-imidazole | Drug Info | IC50 = 955 nM | [527475] | ||
4-(1-Imidazol-1-yl-vinyl)-benzonitrile | Drug Info | IC50 = 0.7 nM | [534057] | ||
7-((1H-imidazol-1-yl)methyl)isoquinoline | Drug Info | IC50 = 1380 nM | [529860] | ||
3,5-Diamino-4'-amino-trans-stilbene | Drug Info | IC50 = 8510 nM | |||
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | IC50 = 2510 nM | [528035] | ||
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | IC50 = 910 nM | [528035] | ||
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole | Drug Info | IC50 = 129 nM | [527801] | ||
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole | Drug Info | IC50 = 27 nM | [527475] | ||
5-Indan-(1Z)-ylidenemethyl-1H-imidazole | Drug Info | IC50 = 130 nM | [527475] | ||
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | IC50 = 1507 nM | [528109] | ||
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 7830 nM | [527456] | ||
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 230 nM | [527456] | ||
2,5-Dimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 1820 nM | |||
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole | Drug Info | IC50 = 205 nM | [525448] | ||
7-hydroxy-2-phenylchroman-4-one | Drug Info | IC50 = 3800 nM | [529180] | ||
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one | Drug Info | IC50 = 1860 nM | [528848] | ||
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 3960 nM | [527456] | ||
5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole | Drug Info | IC50 = 4830 nM | [527456] | ||
3-(2,2-Diphenyl-vinyl)-pyridine | Drug Info | IC50 = 3630 nM | [527456] | ||
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4260 nM | [527456] | ||
3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4060 nM | [527456] | ||
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole | Drug Info | IC50 = 4330 nM | [527456] | ||
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone | Drug Info | IC50 = 4100 nM | [528327] | ||
1-(9H-fluoren-9-yl)-1H-imidazole | Drug Info | IC50 = 2850 nM | [529860] | ||
3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4600 nM | [527456] | ||
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 1810 nM | [527456] | ||
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 7080 nM | [527456] | ||
3-Indan-(1E)-ylidenemethyl-pyridine | Drug Info | IC50 = 2040 nM | [527456] | ||
NSC-368272 | Drug Info | Ki = 5.6 nM | [529860] | ||
3-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | IC50 = 3550 nM | [527456] | ||
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 3930 nM | [527456] | ||
5-(2-(1H-imidazol-1-yl)ethyl)quinoline | Drug Info | IC50 = 350 nM | [529860] | ||
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4310 nM | [527456] | ||
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 2490 nM | [527456] | ||
4-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | IC50 = 12730 nM | [527456] | ||
NSC-369087 | Drug Info | IC50 = 55 nM | [529860] | ||
3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione | Drug Info | IC50 = 8400 nM | [533480] | ||
6-Imidazol-1-yl-isoquinoline | Drug Info | IC50 = 3060 nM | [529860] | ||
Letrozole | Drug Info | IC50 = 0.8 nM | [552393] | ||
2-Imidazol-1-ylmethylxanthen-9-one | Drug Info | IC50 = 7900 nM | |||
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | IC50 = 2670 nM | [528035] | ||
4-(3,4,5-Trimethoxyphenethyl)aniline | Drug Info | IC50 = 2790 nM | |||
4-Imidazol-1-ylmethylxanthen-9-one | Drug Info | IC50 = 17 nM | |||
Gamma-mangostin | Drug Info | IC50 = 4970 nM | [529538] | ||
NSC-19028 | Drug Info | IC50 = 8 nM | [530867] | ||
3,4-Dimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 14510 nM | |||
NSC-93358 | Drug Info | Ki = 266 nM | [530190] | ||
NSC-613604 | Drug Info | Ki = 385 nM | [530190] | ||
YM-511 | Drug Info | IC50 = 0.5 nM | [526667] | ||
ANDROSTENEDIONE | Drug Info | Ki = 20 nM | [533863] | ||
MR-16089 | Drug Info | IC50 = 40 nM | [530867] | ||
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B | Drug Info | IC50 = 2 nM | [530867] | ||
LIAROZOLE | Drug Info | IC50 = 5 nM | [530867] | ||
MR-20492 | Drug Info | IC50 = 200 nM | [530867] | ||
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one | Drug Info | IC50 = 1 nM | [530867] | ||
NSC-94891 | Drug Info | IC50 = 9800 nM | [530190] | ||
NSC-356781 | Drug Info | IC50 = 2100 nM | [529860] | ||
LUDARTIN | Drug Info | IC50 = 55 nM | [530867] | ||
APIGENIN | Drug Info | IC50 = 900 nM | [530867] | ||
CHRYSIN | Drug Info | IC50 = 1 nM | [530867] | ||
NSC-12999 | Drug Info | Ki = 25.5 nM | [529860] | ||
NSC-131736 | Drug Info | IC50 = 1400 nM | [529860] | ||
DEHYDROLEUCODIN | Drug Info | IC50 = 15 nM | [530867] | ||
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one | Drug Info | IC50 = 680 nM | [529860] | ||
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole | Drug Info | IC50 = 3560 nM | [529860] | ||
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one | Drug Info | IC50 = 100 nM | [529860] | ||
NSC-289311 | Drug Info | Ki = 6.5 nM | [529860] | ||
NSC-368280 | Drug Info | Ki = 1.9 nM | [529860] | ||
4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one | Drug Info | IC50 = 760 nM | [529860] | ||
5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline | Drug Info | IC50 = 170 nM | [529860] | ||
ISOLICOFLAVONOL | Drug Info | IC50 = 100 nM | [526180] | ||
CGS-18320B | Drug Info | IC50 = 3 nM | [530867] | ||
(2S)-5,7,2',4'-tetrahydroxyflavanone | Drug Info | IC50 = 2200 nM | [526180] | ||
MORACHALCONE A | Drug Info | IC50 = 4600 nM | [526180] | ||
NSC-625409 | Drug Info | Ki = 52.7 nM | [529860] | ||
2,3-Dimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 980 nM | |||
4-(3,4-Dimethoxyphenethyl)aniline | Drug Info | IC50 = 670 nM | |||
ALBANOL A | Drug Info | IC50 = 7500 nM | [526180] | ||
1-(3-(4-fluorophenyl)propyl)-1H-imidazole | Drug Info | IC50 = 310 nM | [530867] | ||
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole | Drug Info | IC50 = 160 nM | [530867] | ||
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole | Drug Info | IC50 = 74 nM | [530867] | ||
BIOCHANIN | Drug Info | IC50 = 10.2 nM | [530867] | ||
2-(4-hydroxyphenyl)-7-methoxychroman-4-one | Drug Info | IC50 = 3700 nM | [529180] | ||
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 770 nM | [527456] | ||
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 2800 nM | [527456] | ||
NSC-75308 | Drug Info | IC50 = 5600 nM | [529860] | ||
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine | Drug Info | IC50 = 7450 nM | [527456] | ||
3-(imidazolylmethyl)flavone | Drug Info | IC50 = 71 nM | [528327] | ||
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone | Drug Info | IC50 = 470 nM | [528327] | ||
3-(imidazolylmethyl)-4'-methoxyflavone | Drug Info | IC50 = 80 nM | [528327] | ||
(2S)-euchrenone a7 | Drug Info | IC50 = 3400 nM | [526180] | ||
10-EPI-8-DEOXY-CUMAMBRIN B | Drug Info | IC50 = 7 nM | [530867] | ||
NSC-666292 | Drug Info | Ki = 33.4 nM | [529860] | ||
4-(3,5-Dimethoxyphenethyl)benzenamine | Drug Info | IC50 = 2760 nM | |||
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole | Drug Info | IC50 = 100 nM | [527475] | ||
MR-20496 | Drug Info | Ki = 10.3 nM | [534789] | ||
MR-20494 | Drug Info | IC50 = 110 nM | [530867] | ||
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one | Drug Info | IC50 = 2100 nM | [529860] | ||
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one | Drug Info | IC50 = 970 nM | [535139] | ||
(+/-)-7-methoxy-2-phenylchroman-4-one | Drug Info | IC50 = 8000 nM | [529180] | ||
9-Hydroxy-7,8-benzoflavone | Drug Info | IC50 = 20 nM | [530867] | ||
2-(3-hydroxyphenyl)-7-methoxychroman-4-one | Drug Info | IC50 = 3500 nM | [529180] | ||
8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one | Drug Info | IC50 = 1100 nM | [535139] | ||
7,4'-Dihydroxyflavone | Drug Info | IC50 = 2 nM | [530867] | ||
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol | Drug Info | IC50 = 2693 nM | [531085] | ||
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one | Drug Info | IC50 = 89 nM | [535139] | ||
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one | Drug Info | IC50 = 3700 nM | [535139] | ||
NSC-94258 | Drug Info | IC50 = 30.5 nM | [530867] | ||
NARINGENIN | Drug Info | IC50 = 2.9 nM | [530867] | ||
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole | Drug Info | IC50 = 4000 nM | [529860] | ||
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 280 nM | [527456] | ||
NSC-683634 | Drug Info | Ki = 15.1 nM | [529860] | ||
NSC-356483 | Drug Info | IC50 = 3100 nM | [529860] | ||
3-(imidazolylmethyl)-4'-nitroflavone | Drug Info | IC50 = 45 nM | [528327] | ||
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | IC50 = 3680 nM | [527456] | ||
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 800 nM | [527456] | ||
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 7370 nM | [527456] | ||
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 4050 nM | [527456] | ||
ANDROSTENEDONE | Drug Info | Ki = 120 nM | [533387] | ||
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione | Drug Info | IC50 = 10040 nM | [533480] | ||
Isogemichalcone C | Drug Info | IC50 = 7100 nM | [526180] | ||
4-((1H-imidazol-1-yl)methyl)benzonitrile | Drug Info | IC50 = 15 nM | [529291] | ||
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | IC50 = 3551 nM | [528109] | ||
2,3,4-Trimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 3570 nM | |||
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one | Drug Info | IC50 = 1900 nM | |||
NSC-122427 | Drug Info | IC50 = 15500 nM | [530190] | ||
3-Nitro-4'-nitro-trans-stilbene | Drug Info | IC50 = 8330 nM | |||
3,4'-(Ethane-1,2-diyl)dibenzenamine | Drug Info | IC50 = 3210 nM | |||
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione | Drug Info | IC50 = 10040 nM | [533480] | ||
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol | Drug Info | IC50 = 430 nM | [527222] | ||
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine | Drug Info | IC50 = 1200 nM | [529684] | ||
Anastrozole | Drug Info | IC50 = 15 nM | [552393] | ||
Exemestane | Drug Info | IC50 = 5 nM | [552393] | ||
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione | Drug Info | IC50 = 10200 nM | [533480] | ||
GARCINONE D | Drug Info | IC50 = 5200 nM | [529538] | ||
(2S)-abyssinone II | Drug Info | IC50 = 400 nM | [526180] | ||
Rogletimide | Drug Info | Ki = 14000 nM | [533470] | ||
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | IC50 = 5570 nM | [527456] | ||
7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one | Drug Info | IC50 = 3400 nM | [529180] | ||
FADROZOLE | Drug Info | IC50 = 17 nM | [527856] | ||
Docosapentaenoic acid | Drug Info | IC50 = 16800 nM | [528166] | ||
3-Methoxyl-4'-amino-trans-stilbene | Drug Info | IC50 = 3080 nM | |||
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | IC50 = 1805 nM | [527801] | ||
COUMATE | Drug Info | IC50 = 300 nM | [530712] | ||
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole | Drug Info | IC50 = 950 nM | [529684] | ||
4'-cyano-3-(imidazolylmethyl)flavone | Drug Info | IC50 = 69 nM | [528327] | ||
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone | Drug Info | IC50 = 1800 nM | [528327] | ||
4'-bromo-3-(imidazolylmethyl)flavone | Drug Info | IC50 = 440 nM | [528327] | ||
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone | Drug Info | IC50 = 190 nM | |||
MONODICTYOCHROMONE B | Drug Info | IC50 = 16500 nM | [529759] | ||
Aminoglutethimide | Drug Info | IC50 = 18500 nM | [552532] | ||
4-Imidazol-1-ylmethylthioxanthen-9-one | Drug Info | IC50 = 3.98 nM | |||
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one | Drug Info | IC50 = 53 nM | |||
3,4,5-Trimethoxy-4'-amino-trans-stilbene | Drug Info | IC50 = 900 nM | |||
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one | Drug Info | IC50 = 4300 nM | [529180] | ||
Broussoflavonol F | Drug Info | IC50 = 9700 nM | [526180] | ||
4-Imidazol-1-yl-2-phenyl-chroman-7-ol | Drug Info | IC50 = 40 nM | [527222] | ||
2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one | Drug Info | IC50 = 770 nM | [527565] | ||
LIQUIRTIGENIN | Drug Info | IC50 = 340 nM | [529679] | ||
GOSSYPETIN | Drug Info | IC50 = 11000 nM | [529679] | ||
3,5-Dihydroxyl-4'-amino-trans-stilbene | Drug Info | IC50 = 5000 nM | |||
Action against Disease Model | Testolactone | 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. | [553113] | Drug Info | |
References | |||||
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Ref 534514 | J Med Chem. 1997 Sep 26;40(20):3263-70.6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase. | ||||
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