Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T13260
(Former ID: TTDS00252)
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| Target Name |
Aromatase (CYP19A1)
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| Synonyms |
P-450AROM; Estrogen synthetase; Estrogen synthase; Cytochrome P450 19A1; Cytochrome P-450AROM; CYPXIX; CYP19; CYAR; ARO1
Click to Show/Hide
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| Gene Name |
CYP19A1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 2 | Cushing syndrome [ICD-11: 5A70] | |||||
| Function |
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
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| BioChemical Class |
Paired donor oxygen oxidoreductase
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| UniProt ID | ||||||
| EC Number |
EC 1.14.14.14
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| Sequence |
MVLEMLNPIHYNITSIVPEAMPAATMPVLLLTGLFLLVWNYEGTSSIPGPGYCMGIGPLI
SHGRFLWMGIGSACNYYNRVYGEFMRVWISGEETLIISKSSSMFHIMKHNHYSSRFGSKL GLQCIGMHEKGIIFNNNPELWKTTRPFFMKALSGPGLVRMVTVCAESLKTHLDRLEEVTN ESGYVDVLTLLRRVMLDTSNTLFLRIPLDESAIVVKIQGYFDAWQALLIKPDIFFKISWL YKKYEKSVKDLKDAIEVLIAEKRRRISTEEKLEECMDFATELILAEKRGDLTRENVNQCI LEMLIAAPDTMSVSLFFMLFLIAKHPNVEEAIIKEIQTVIGERDIKIDDIQKLKVMENFI YESMRYQPVVDLVMRKALEDDVIDGYPVKKGTNIILNIGRMHRLEFFPKPNEFTLENFAK NVPYRYFQPFGFGPRGCAGKYIAMVMMKAILVTLLRRFHVKTLQGQCVESIQKIHDLSLH PDETKNMLEMIFTPRNSDRCLEH Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T88LSZ | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Aminoglutethimide | Drug Info | Approved | Cushing disease | [2], [3] | |
| 2 | Anastrozole | Drug Info | Approved | Breast cancer | [4], [5] | |
| 3 | Exemestane | Drug Info | Approved | Hormonally-responsive breast cancer | [6], [7] | |
| 4 | FADROZOLE | Drug Info | Approved | Breast cancer | [8], [9], [10] | |
| 5 | Letrozole | Drug Info | Approved | Hormonally-responsive breast cancer | [11], [5] | |
| 6 | Testolactone | Drug Info | Approved | Breast cancer | [12], [7] | |
| Clinical Trial Drug(s) | [+] 5 Clinical Trial Drugs | + | ||||
| 1 | Atamestane + Toremifene | Drug Info | Phase 3 | Breast cancer | [13] | |
| 2 | LIAROZOLE | Drug Info | Phase 2/3 | Dermatological disease | [14], [15] | |
| 3 | BGS-649 | Drug Info | Phase 2 | Endometriosis | [16] | |
| 4 | Coumate | Drug Info | Phase 2 | Breast cancer | [17] | |
| 5 | Dextromethorphan+quinidine | Drug Info | Phase 2 | Diabetic neuropathy | [18] | |
| Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
| 1 | FORMESTANE | Drug Info | Withdrawn from market | Breast cancer | [9], [19] | |
| 2 | FINROZOLE | Drug Info | Discontinued in Phase 2 | Prostate disease | [20] | |
| 3 | NKS-01 | Drug Info | Discontinued in Phase 2 | Bladder cancer | [21] | |
| 4 | YM-511 | Drug Info | Discontinued in Phase 2 | Breast cancer | [22] | |
| 5 | MINAMESTANE | Drug Info | Terminated | Bladder cancer | [23] | |
| 6 | Rogletimide | Drug Info | Terminated | Breast cancer | [24] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 237 Inhibitor drugs | + | ||||
| 1 | Aminoglutethimide | Drug Info | [1] | |||
| 2 | Anastrozole | Drug Info | [25], [26] | |||
| 3 | Exemestane | Drug Info | [27] | |||
| 4 | FADROZOLE | Drug Info | [28] | |||
| 5 | Letrozole | Drug Info | [27] | |||
| 6 | Testolactone | Drug Info | [26], [29] | |||
| 7 | LIAROZOLE | Drug Info | [31] | |||
| 8 | BGS-649 | Drug Info | [32] | |||
| 9 | Coumate | Drug Info | [33] | |||
| 10 | Dextromethorphan+quinidine | Drug Info | [34] | |||
| 11 | NARINGENIN | Drug Info | [31] | |||
| 12 | FORMESTANE | Drug Info | [35] | |||
| 13 | FINROZOLE | Drug Info | [9], [36] | |||
| 14 | NKS-01 | Drug Info | [9], [37] | |||
| 15 | VOROZOLE | Drug Info | [38] | |||
| 16 | YM-511 | Drug Info | [39] | |||
| 17 | MINAMESTANE | Drug Info | [9], [40] | |||
| 18 | Rogletimide | Drug Info | [41] | |||
| 19 | (+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one | Drug Info | [42] | |||
| 20 | (+/-)-7-methoxy-2-phenylchroman-4-one | Drug Info | [43] | |||
| 21 | (2S)-5,7,2',4'-tetrahydroxyflavanone | Drug Info | [44] | |||
| 22 | (2S)-abyssinone II | Drug Info | [44] | |||
| 23 | (2S)-euchrenone a7 | Drug Info | [44] | |||
| 24 | 1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole | Drug Info | [45] | |||
| 25 | 1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole | Drug Info | [46] | |||
| 26 | 1-(2-phenoxybenzyl)-1H-imidazole | Drug Info | [47] | |||
| 27 | 1-(3-(4-fluorophenyl)propyl)-1H-imidazole | Drug Info | [31] | |||
| 28 | 1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole | Drug Info | [48] | |||
| 29 | 1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone | Drug Info | [49] | |||
| 30 | 1-(4-Cyanobenzyl)-5-methyl-1H-imidazole | Drug Info | [50] | |||
| 31 | 1-(4-nitro-2-phenoxybenzyl)-1H-imidazole | Drug Info | [47] | |||
| 32 | 1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole | Drug Info | [47] | |||
| 33 | 1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole | Drug Info | [51] | |||
| 34 | 1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole | Drug Info | [46] | |||
| 35 | 1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole | Drug Info | [31] | |||
| 36 | 1-(9H-fluoren-9-yl)-1H-imidazole | Drug Info | [46] | |||
| 37 | 1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole | Drug Info | [33] | |||
| 38 | 1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one | Drug Info | [52] | |||
| 39 | 1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole | Drug Info | [53] | |||
| 40 | 1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one | Drug Info | [52] | |||
| 41 | 1-Imidazol-1-ylmethylxanthen-9-one | Drug Info | [47] | |||
| 42 | 1-Naphthalen-2-yl-1H-imidazole | Drug Info | [48] | |||
| 43 | 1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole | Drug Info | [31] | |||
| 44 | 10-EPI-8-DEOXY-CUMAMBRIN B | Drug Info | [31] | |||
| 45 | 11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B | Drug Info | [31] | |||
| 46 | 2,3,4-Trimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 47 | 2,3,5-Trimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 48 | 2,3-Dimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 49 | 2,4-Dimethoxy-3'-amino-trans-stilbene | Drug Info | [49] | |||
| 50 | 2,4-Dimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 51 | 2,5-Dimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 52 | 2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone | Drug Info | [49] | |||
| 53 | 2-(3-hydroxyphenyl)-7-methoxychroman-4-one | Drug Info | [43] | |||
| 54 | 2-(4-hydroxyphenyl)-7-methoxychroman-4-one | Drug Info | [43] | |||
| 55 | 2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one | Drug Info | [54] | |||
| 56 | 2-Imidazol-1-ylmethylxanthen-9-one | Drug Info | [47] | |||
| 57 | 2-phenyl-2,3-dihydrobenzo[h]chromen-4-one | Drug Info | [43] | |||
| 58 | 2-Phenyl-3-pyridin-4-ylmethylene-chroman-4-one | Drug Info | [55] | |||
| 59 | 2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol | Drug Info | [51] | |||
| 60 | 3,4'-(Ethane-1,2-diyl)dibenzenamine | Drug Info | [49] | |||
| 61 | 3,4,5-Trimethoxy-3'-amino-trans-stilbene | Drug Info | [49] | |||
| 62 | 3,4,5-Trimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 63 | 3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one | Drug Info | [31] | |||
| 64 | 3,4-Dimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 65 | 3,5-Diacetoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 66 | 3,5-Diamino-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 67 | 3,5-Dihydroxyl-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 68 | 3,5-Dimethoxy-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 69 | 3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one | Drug Info | [47] | |||
| 70 | 3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | [56] | |||
| 71 | 3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine | Drug Info | [56] | |||
| 72 | 3-(2,2-Diphenyl-vinyl)-pyridine | Drug Info | [57] | |||
| 73 | 3-(3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [56] | |||
| 74 | 3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [56] | |||
| 75 | 3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione | Drug Info | [58] | |||
| 76 | 3-(4-Amino-phenyl)-3-butyl-piperidine-2,6-dione | Drug Info | [59] | |||
| 77 | 3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione | Drug Info | [58] | |||
| 78 | 3-(4-Amino-phenyl)-3-heptyl-piperidine-2,6-dione | Drug Info | [59] | |||
| 79 | 3-(4-Amino-phenyl)-3-hexyl-piperidine-2,6-dione | Drug Info | [59] | |||
| 80 | 3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione | Drug Info | [58] | |||
| 81 | 3-(4-Amino-phenyl)-3-pentyl-piperidine-2,6-dione | Drug Info | [59] | |||
| 82 | 3-(4-Amino-phenyl)-3-propyl-piperidine-2,6-dione | Drug Info | [59] | |||
| 83 | 3-(4-Amino-phenyl)-pyrrolidine-2,5-dione | Drug Info | [58] | |||
| 84 | 3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [56] | |||
| 85 | 3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | [48] | |||
| 86 | 3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine | Drug Info | [48] | |||
| 87 | 3-(6-Ethoxy-naphthalen-2-yl)-pyridine | Drug Info | [48] | |||
| 88 | 3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine | Drug Info | [56] | |||
| 89 | 3-(6-methoxynaphthalen-2-yl)pyridine | Drug Info | [60] | |||
| 90 | 3-(imidazolylmethyl)-4'-methoxyflavone | Drug Info | [61] | |||
| 91 | 3-(imidazolylmethyl)-4'-nitroflavone | Drug Info | [61] | |||
| 92 | 3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone | Drug Info | [61] | |||
| 93 | 3-(imidazolylmethyl)flavone | Drug Info | [61] | |||
| 94 | 3-(naphthalen-2-yl)pyridine | Drug Info | [60] | |||
| 95 | 3-Amino-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 96 | 3-Fluoren-9-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 97 | 3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol | Drug Info | [62] | |||
| 98 | 3-Indan-(1E)-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 99 | 3-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 100 | 3-Methoxyl-4'-amino-trans-stilbene | Drug Info | [49] | |||
| 101 | 3-Nitro-4'-nitro-trans-stilbene | Drug Info | [49] | |||
| 102 | 3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 103 | 3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 104 | 3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 105 | 3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 106 | 3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 107 | 3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 108 | 3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 109 | 3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 110 | 3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 111 | 3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 112 | 3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 113 | 3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 114 | 3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 115 | 3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 116 | 3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 117 | 3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 118 | 3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 119 | 3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 120 | 3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 121 | 3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 122 | 3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 123 | 3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 124 | 3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 125 | 4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol | Drug Info | [62] | |||
| 126 | 4'-(Pyridin-4-ylmethyl)biphenyl-3-amine | Drug Info | [62] | |||
| 127 | 4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone | Drug Info | [61] | |||
| 128 | 4'-bromo-3-(imidazolylmethyl)flavone | Drug Info | [61] | |||
| 129 | 4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone | Drug Info | [61] | |||
| 130 | 4'-cyano-3-(imidazolylmethyl)flavone | Drug Info | [61] | |||
| 131 | 4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one | Drug Info | [46] | |||
| 132 | 4-((1H-imidazol-1-yl)methyl)benzonitrile | Drug Info | [50] | |||
| 133 | 4-(1-Imidazol-1-yl-vinyl)-benzonitrile | Drug Info | [63] | |||
| 134 | 4-(2,2-Diphenyl-vinyl)-pyridine | Drug Info | [57] | |||
| 135 | 4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one | Drug Info | [46] | |||
| 136 | 4-(3,4,5-Trimethoxyphenethyl)aniline | Drug Info | [49] | |||
| 137 | 4-(3,4-Dimethoxyphenethyl)aniline | Drug Info | [49] | |||
| 138 | 4-(3,5-Dimethoxyphenethyl)benzenamine | Drug Info | [49] | |||
| 139 | 4-ANDROSTENE-3-17-DIONE | Drug Info | [64], [65] | |||
| 140 | 4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one | Drug Info | [52] | |||
| 141 | 4-Fluoren-9-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 142 | 4-Imidazol-1-yl-2-phenyl-chroman-7-ol | Drug Info | [51] | |||
| 143 | 4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one | Drug Info | [52] | |||
| 144 | 4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one | Drug Info | [47] | |||
| 145 | 4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one | Drug Info | [47] | |||
| 146 | 4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one | Drug Info | [47] | |||
| 147 | 4-Imidazol-1-ylmethylthioxanthen-9-one | Drug Info | [47] | |||
| 148 | 4-Imidazol-1-ylmethylxanthen-9-one | Drug Info | [47] | |||
| 149 | 4-Indan-(1E)-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 150 | 4-Indan-(1Z)-ylidenemethyl-pyridine | Drug Info | [57] | |||
| 151 | 4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | [62] | |||
| 152 | 4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine | Drug Info | [62] | |||
| 153 | 4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 154 | 4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 155 | 4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 156 | 4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 157 | 4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 158 | 4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 159 | 4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 160 | 4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 161 | 4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 162 | 4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 163 | 4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine | Drug Info | [57] | |||
| 164 | 5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline | Drug Info | [46] | |||
| 165 | 5-(2-(1H-imidazol-1-yl)ethyl)quinoline | Drug Info | [46] | |||
| 166 | 5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one | Drug Info | [52] | |||
| 167 | 5-Indan-(1E)-ylidenemethyl-1H-imidazole | Drug Info | [66] | |||
| 168 | 5-Indan-(1Z)-ylidenemethyl-1H-imidazole | Drug Info | [66] | |||
| 169 | 5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one | Drug Info | [60] | |||
| 170 | 5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one | Drug Info | [60] | |||
| 171 | 5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole | Drug Info | [66] | |||
| 172 | 5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole | Drug Info | [66] | |||
| 173 | 5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine | Drug Info | [57] | |||
| 174 | 5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine | Drug Info | [57] | |||
| 175 | 5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole | Drug Info | [57] | |||
| 176 | 5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole | Drug Info | [57] | |||
| 177 | 6-((1H-imidazol-1-yl)methyl)-2H-chromene-2-thione | Drug Info | [46] | |||
| 178 | 6-Imidazol-1-yl-isoquinoline | Drug Info | [46] | |||
| 179 | 7,4'-Dihydroxyflavone | Drug Info | [31] | |||
| 180 | 7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one | Drug Info | [46] | |||
| 181 | 7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one | Drug Info | [46] | |||
| 182 | 7-((1H-imidazol-1-yl)methyl)isoquinoline | Drug Info | [46] | |||
| 183 | 7-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one | Drug Info | [67] | |||
| 184 | 7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one | Drug Info | [43] | |||
| 185 | 7-hydroxy-2-phenylchroman-4-one | Drug Info | [43] | |||
| 186 | 7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one | Drug Info | [52] | |||
| 187 | 8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one | Drug Info | [52] | |||
| 188 | 9-Hydroxy-7,8-benzoflavone | Drug Info | [31] | |||
| 189 | ALBANOL A | Drug Info | [44] | |||
| 190 | ALPHA-NAPHTHOFLAVONE | Drug Info | [31] | |||
| 191 | ANDROSTENEDONE | Drug Info | [68] | |||
| 192 | APIGENIN | Drug Info | [31] | |||
| 193 | Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine | Drug Info | [45] | |||
| 194 | biochanin A | Drug Info | [31] | |||
| 195 | Broussoflavonol F | Drug Info | [44] | |||
| 196 | CGS-18320B | Drug Info | [31] | |||
| 197 | Chrysin | Drug Info | [31] | |||
| 198 | DEHYDROLEUCODIN | Drug Info | [31] | |||
| 199 | Docosapentaenoic acid | Drug Info | [69] | |||
| 200 | flavone | Drug Info | [31] | |||
| 201 | Gamma-mangostin | Drug Info | [70] | |||
| 202 | GARCINONE D | Drug Info | [70] | |||
| 203 | GOSSYPETIN | Drug Info | [71] | |||
| 204 | Isogemichalcone C | Drug Info | [44] | |||
| 205 | ISOLICOFLAVONOL | Drug Info | [44] | |||
| 206 | LIQUIRTIGENIN | Drug Info | [71] | |||
| 207 | LUDARTIN | Drug Info | [31] | |||
| 208 | MDL-18962 | Drug Info | [72] | |||
| 209 | MONODICTYOCHROMONE B | Drug Info | [73] | |||
| 210 | MORACHALCONE A | Drug Info | [44] | |||
| 211 | MR-16089 | Drug Info | [31] | |||
| 212 | MR-20492 | Drug Info | [31] | |||
| 213 | MR-20494 | Drug Info | [31] | |||
| 214 | MR-20496 | Drug Info | [74] | |||
| 215 | MR-20814 | Drug Info | [74] | |||
| 216 | N-(2-benzyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | [75] | |||
| 217 | N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | [76] | |||
| 218 | N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | [76] | |||
| 219 | N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide | Drug Info | [76] | |||
| 220 | N-[2-(4'-Nitrophenyl)ethyl]-imidazole | Drug Info | [31] | |||
| 221 | NSC-122427 | Drug Info | [77] | |||
| 222 | NSC-12999 | Drug Info | [46] | |||
| 223 | NSC-131736 | Drug Info | [46] | |||
| 224 | NSC-289311 | Drug Info | [46] | |||
| 225 | NSC-356483 | Drug Info | [46] | |||
| 226 | NSC-356781 | Drug Info | [46] | |||
| 227 | NSC-368272 | Drug Info | [46] | |||
| 228 | NSC-368280 | Drug Info | [46] | |||
| 229 | NSC-369087 | Drug Info | [46] | |||
| 230 | NSC-613604 | Drug Info | [77] | |||
| 231 | NSC-625409 | Drug Info | [46] | |||
| 232 | NSC-666292 | Drug Info | [46] | |||
| 233 | NSC-683634 | Drug Info | [46] | |||
| 234 | NSC-75308 | Drug Info | [46] | |||
| 235 | NSC-93358 | Drug Info | [77] | |||
| 236 | NSC-94258 | Drug Info | [31] | |||
| 237 | NSC-94891 | Drug Info | [77] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Atamestane + Toremifene | Drug Info | [30] | |||
| 2 | Org-33201 | Drug Info | [78] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: Testosterone | Ligand Info | |||||
| Structure Description | HUMAN PLACENTAL AROMATASE CYTOCHROME P450 (CYP19A1) COMPLEXED WITH TESTOSTERONE | PDB:5JKW | ||||
| Method | X-ray diffraction | Resolution | 3.00 Å | Mutation | No | [79] |
| PDB Sequence |
SSIPGPGYCM
54 GIGPLISHGR64 FLWMGIGSAC74 NYYNRVYGEF84 MRVWISGEET94 LIISKSSSMF 104 HIMKHNHYSS114 RFGSKLGLQC124 IGMHEKGIIF134 NNNPELWKTT144 RPFFMKALSG 154 PGLVRMVTVC164 AESLKTHLDR174 LEEVTNESGY184 VDVLTLLRRV194 MLDTSNTLFL 204 RIPLDESAIV214 VKIQGYFDAW224 QALLIKPDIF234 FKISWLYKKY244 EKSVKDLKDA 254 IEVLIAEKRR264 RISTEEKLEE274 CMDFATELIL284 AEKRGDLTRE294 NVNQCILEML 304 IAAPDTMSVS314 LFFMLFLIAK324 HPNVEEAIIK334 EIQTVIGERD344 IKIDDIQKLK 354 VMENFIYESM364 RYQPVVDLVM374 RKALEDDVID384 GYPVKKGTNI394 ILNIGRMHRL 404 EFFPKPNEFT414 LENFAKNVPY424 RYFQPFGFGP434 RGCAGKYIAM444 VMMKAILVTL 454 LRRFHVKTLQ464 GQCVESIQKI474 HDLSLHPDET484 KNMLEMIFTP494 RN |
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| Ligand Name: Exemestane | Ligand Info | |||||
| Structure Description | Crystal structure of human placental aromatase complexed with breast cancer drug exemestane | PDB:3S7S | ||||
| Method | X-ray diffraction | Resolution | 3.21 Å | Mutation | No | [80] |
| PDB Sequence |
SSIPGPGYCM
54 GIGPLISHGR64 FLWMGIGSAC74 NYYNRVYGEF84 MRVWISGEET94 LIISKSSSMF 104 HIMKHNHYSS114 RFGSKLGLQC124 IGMHEKGIIF134 NNNPELWKTT144 RPFFMKALSG 154 PGLVRMVTVC164 AESLKTHLDR174 LEEVTNESGY184 VDVLTLLRRV194 MLDTSNTLFL 204 RIPLDESAIV214 VKIQGYFDAW224 QALLIKPDIF234 FKISWLYKKY244 EKSVKDLKDA 254 IEVLIAEKRR264 RISTEEKLEE274 CMDFATELIL284 AEKRGDLTRE294 NVNQCILEML 304 IAAPDTMSVS314 LFFMLFLIAK324 HPNVEEAIIK334 EIQTVIGERD344 IKIDDIQKLK 354 VMENFIYESM364 RYQPVVDLVM374 RKALEDDVID384 GYPVKKGTNI394 ILNIGRMHRL 404 EFFPKPNEFT414 LENFAKNVPY424 RYFQPFGFGP434 RGCAGKYIAM444 VMMKAILVTL 454 LRRFHVKTLQ464 GQCVESIQKI474 HDLSLHPDET484 KNMLEMIFTP494 RN |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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There is no similarity protein (E value < 0.005) for this target
|
| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| Steroid hormone biosynthesis | hsa00140 | Affiliated Target |
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| Class: Metabolism => Lipid metabolism | Pathway Hierarchy | ||
| Ovarian steroidogenesis | hsa04913 | Affiliated Target |
|
| Class: Organismal Systems => Endocrine system | Pathway Hierarchy | ||
| Degree | 12 | Degree centrality | 1.29E-03 | Betweenness centrality | 2.99E-04 |
|---|---|---|---|---|---|
| Closeness centrality | 1.62E-01 | Radiality | 1.24E+01 | Clustering coefficient | 5.00E-01 |
| Neighborhood connectivity | 1.08E+01 | Topological coefficient | 2.76E-01 | Eccentricity | 11 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| BioCyc | [+] 3 BioCyc Pathways | + | ||||
| 1 | Superpathway of steroid hormone biosynthesis | |||||
| 2 | Estradiol biosynthesis II | |||||
| 3 | Estradiol biosynthesis I | |||||
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Steroid hormone biosynthesis | |||||
| 2 | Metabolic pathways | |||||
| 3 | Ovarian steroidogenesis | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | FSH Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | Androgen/estrogene/progesterone biosynthesis | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Androgen and Estrogen Metabolism | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Endogenous sterols | |||||
| WikiPathways | [+] 8 WikiPathways | + | ||||
| 1 | Metapathway biotransformation | |||||
| 2 | Tryptophan metabolism | |||||
| 3 | Oxidation by Cytochrome P450 | |||||
| 4 | Ovarian Infertility Genes | |||||
| 5 | Metabolism of steroid hormones and vitamin D | |||||
| 6 | FSH signaling pathway | |||||
| 7 | Integrated Breast Cancer Pathway | |||||
| 8 | Phase 1 - Functionalization of compounds | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chem Res Toxicol. 2007 Jul;20(7):1038-45. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7054). | |||||
| REF 3 | Breakdown of Th cell immune responses and steroidogenic CYP11A1 expression in CD4+ T cells in a murine model implanted with B16 melanoma. Cell Immunol. 2000 Nov 25;206(1):7-15. | |||||
| REF 4 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5137). | |||||
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| REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7073). | |||||
| REF 7 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 8 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8311). | |||||
| REF 9 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000824) | |||||
| REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5209). | |||||
| REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7303). | |||||
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| REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000733) | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010074) | |||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003076) | |||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002721) | |||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002545) | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001207) | |||||
| REF 25 | Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. J Pediatr Endocrinol Metab. 2002;15 Suppl 3:945-8. | |||||
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| REF 30 | Toremifene-atamestane; alone or in combination: predictions from the preclinical intratumoral aromatase model. J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):1-7. | |||||
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| REF 42 | Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer. J Med Chem. 2007 Jun 14;50(12):2799-806. | |||||
| REF 43 | New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation. Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. | |||||
| REF 44 | Aromatase inhibitors from Broussonetia papyrifera. J Nat Prod. 2001 Oct;64(10):1286-93. | |||||
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| REF 47 | Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation. J Med Chem. 2010 Jul 22;53(14):5347-51. | |||||
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| REF 54 | Synthesis and characterization of azole isoflavone inhibitors of aromatase. Bioorg Med Chem. 2005 Jun 2;13(12):4063-70. | |||||
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| REF 78 | Org 33201: a new highly selective orally active aromatase inhibitor. J Steroid Biochem Mol Biol. 1993 Mar;44(4-6):681-2. | |||||
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