Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T80896
(Former ID: TTDS00250)
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| Target Name |
Estrogen receptor beta (ESR2)
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| Synonyms |
Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; NR3A2; Erbeta; ESTRB; ER-beta; Beta-1
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| Gene Name |
ESR2
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 4 Target-related Diseases | + | ||||
| 1 | Breast cancer [ICD-11: 2C60-2C6Y] | |||||
| 2 | Cushing syndrome [ICD-11: 5A70] | |||||
| 3 | Menopausal disorder [ICD-11: GA30] | |||||
| 4 | Vasomotor/allergic rhinitis [ICD-11: CA08] | |||||
| Function |
Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual. Nuclear hormone receptor.
Click to Show/Hide
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| BioChemical Class |
Nuclear hormone receptor
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| UniProt ID | ||||||
| Sequence |
MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPS
NVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVN RETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGH NDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLH CAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTK LADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDL VLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDA DSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMK CKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| HIT2.0 ID | T05O6O | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
| 1 | ARZOXIFENE | Drug Info | Approved | Breast cancer | [2], [3] | |
| 2 | Conjugated Estrogens | Drug Info | Approved | Menopause symptom | [4] | |
| 3 | Estrogen | Drug Info | Approved | Menopause symptom | [5] | |
| 4 | Trilostane | Drug Info | Approved | Cushing disease | [6], [7] | |
| Clinical Trial Drug(s) | [+] 8 Clinical Trial Drugs | + | ||||
| 1 | MF-101 | Drug Info | Phase 3 | Hepatitis virus infection | [8] | |
| 2 | Premarin/Pravachol | Drug Info | Phase 3 | Hyperlipidaemia | [9] | |
| 3 | Genistein | Drug Info | Phase 2/3 | Menopause symptom | [10] | |
| 4 | AUS-131 | Drug Info | Phase 2 | Hot flushes | [11] | |
| 5 | ERB-041 | Drug Info | Phase 2 | Inflammatory bowel disease | [12], [13] | |
| 6 | Erteberel | Drug Info | Phase 2 | Prostate hyperplasia | [14] | |
| 7 | VG-101 | Drug Info | Phase 1/2 | Menopause symptom | [15] | |
| 8 | ERB-257 | Drug Info | Phase 1 | Sepsis | [16] | |
| Discontinued Drug(s) | [+] 8 Discontinued Drugs | + | ||||
| 1 | BITHIONOL | Drug Info | Withdrawn from market | Trematode infection | [5], [17] | |
| 2 | HEXESTROL | Drug Info | Withdrawn from market | Irregularities | [18], [19], [20] | |
| 3 | EM-800 | Drug Info | Discontinued in Phase 3 | Estrogen deficiency | [21] | |
| 4 | ERA-923 | Drug Info | Discontinued in Phase 2 | Breast cancer | [22] | |
| 5 | ERB-196 | Drug Info | Discontinued in Phase 1 | Inflammatory bowel disease | [23] | |
| 6 | HE2100 | Drug Info | Discontinued in Phase 1 | Thrombocytopenia | [24] | |
| 7 | ICI-164384 | Drug Info | Terminated | Breast cancer | [25] | |
| 8 | ZK-119010 | Drug Info | Terminated | Carcinoma | [26] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Inhibitor | [+] 158 Inhibitor drugs | + | ||||
| 1 | ARZOXIFENE | Drug Info | [27] | |||
| 2 | NARINGENIN | Drug Info | [38] | |||
| 3 | BITHIONOL | Drug Info | [39] | |||
| 4 | HEXESTROL | Drug Info | [40] | |||
| 5 | ERA-923 | Drug Info | [42] | |||
| 6 | HE2100 | Drug Info | [44] | |||
| 7 | ICI-164384 | Drug Info | [45] | |||
| 8 | LY-117018 | Drug Info | [46] | |||
| 9 | ZK-119010 | Drug Info | [47] | |||
| 10 | 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol | Drug Info | [48] | |||
| 11 | 1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 12 | 1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 13 | 1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL | Drug Info | [49], [50] | |||
| 14 | 1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 15 | 2,3-diphenyl-1H-indole | Drug Info | [51] | |||
| 16 | 2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 17 | 2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 18 | 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 19 | 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 20 | 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 21 | 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 22 | 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol | Drug Info | [53] | |||
| 23 | 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol | Drug Info | [53] | |||
| 24 | 2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 25 | 2-(4-Hydroxy-phenyl)-1-p-tolyl-3H-inden-5-ol | Drug Info | [48] | |||
| 26 | 2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol | Drug Info | [54] | |||
| 27 | 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol | Drug Info | [54] | |||
| 28 | 2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol | Drug Info | [52] | |||
| 29 | 2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol | Drug Info | [55] | |||
| 30 | 2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol | Drug Info | [52] | |||
| 31 | 2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol | Drug Info | [55] | |||
| 32 | 2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol | Drug Info | [52] | |||
| 33 | 2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol | Drug Info | [52] | |||
| 34 | 2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol | Drug Info | [52] | |||
| 35 | 2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol | Drug Info | [52] | |||
| 36 | 2-(4-Hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 37 | 2-(4-Hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 38 | 2-(4-Hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 39 | 2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL | Drug Info | [50], [52] | |||
| 40 | 2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol | Drug Info | [53] | |||
| 41 | 2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 42 | 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 43 | 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 44 | 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 45 | 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 46 | 2-Naphthalen-1-yl-benzooxazol-6-ol | Drug Info | [52] | |||
| 47 | 2-phenyl-1,2'-spirobi[1H-indene]-5'-ol | Drug Info | [53] | |||
| 48 | 3'-Methoxy-4'Hydroxyclomiphene | Drug Info | [56] | |||
| 49 | 3,4,6-Trihydroxy-2-(4-hydroxy-phenyl)-inden-1-one | Drug Info | [57] | |||
| 50 | 3,6-Dihydroxy-2-(4-hydroxy-phenyl)-inden-1-one | Drug Info | [57] | |||
| 51 | 3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 52 | 3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 53 | 3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol | Drug Info | [52] | |||
| 54 | 3-(4-Hydroxy-phenyl)-4H-chromen-7-ol | Drug Info | [59] | |||
| 55 | 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol | Drug Info | [52] | |||
| 56 | 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol | Drug Info | [52] | |||
| 57 | 3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [52] | |||
| 58 | 3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [52] | |||
| 59 | 3-chloro-4-(4-hydroxyphenyl)salicylaldoxime | Drug Info | [60] | |||
| 60 | 3-hydroxy-4,10-dimethyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 61 | 3-hydroxy-4,7-dimethyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 62 | 3-hydroxy-4-methyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 63 | 3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one | Drug Info | [58] | |||
| 64 | 3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol | Drug Info | [61] | |||
| 65 | 4',5,7-trihydroxy-6,8-dimethylisoflavone | Drug Info | [62] | |||
| 66 | 4,10-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 67 | 4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 68 | 4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 69 | 4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 70 | 4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 71 | 4,7-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 72 | 4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol | Drug Info | [51] | |||
| 73 | 4-(2-phenyl-1H-indol-3-yl)phenol | Drug Info | [51] | |||
| 74 | 4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol | Drug Info | [51] | |||
| 75 | 4-(3-phenyl-1H-indol-2-yl)phenol | Drug Info | [51] | |||
| 76 | 4-(4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE OXIME | Drug Info | [50] | |||
| 77 | 4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol | Drug Info | [52] | |||
| 78 | 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol | Drug Info | [52] | |||
| 79 | 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol | Drug Info | [52] | |||
| 80 | 4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol | Drug Info | [52] | |||
| 81 | 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 82 | 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 83 | 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 84 | 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 85 | 4-Naphthalen-2-yl-phenol | Drug Info | [49] | |||
| 86 | 4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol | Drug Info | [63] | |||
| 87 | 4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol | Drug Info | [63] | |||
| 88 | 4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol | Drug Info | [63] | |||
| 89 | 4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol | Drug Info | [63] | |||
| 90 | 4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol | Drug Info | [63] | |||
| 91 | 5,7-dihydroxy-3-phenyl-3H-quinazolin-4-one | Drug Info | [64] | |||
| 92 | 5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 93 | 5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol | Drug Info | [52] | |||
| 94 | 5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol | Drug Info | [54] | |||
| 95 | 6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 96 | 6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 97 | 6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 98 | 6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 99 | 6-(2-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 100 | 6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 101 | 6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 102 | 6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 103 | 6-(3-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | [49] | |||
| 104 | 6-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 105 | 6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 106 | 6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 107 | 6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol | Drug Info | [49] | |||
| 108 | 6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol | Drug Info | [49] | |||
| 109 | 6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol | Drug Info | [49] | |||
| 110 | 6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol | Drug Info | [49] | |||
| 111 | 6-(4-Hydroxy-phenyl)-naphthalen-1-ol | Drug Info | [49] | |||
| 112 | 6-(4-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [54] | |||
| 113 | 6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 114 | 6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol | Drug Info | [58] | |||
| 115 | 6-Phenyl-naphthalen-2-ol | Drug Info | [49] | |||
| 116 | 7-(3-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 117 | 7-(4-Hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 118 | 7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 119 | 7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol | Drug Info | [55] | |||
| 120 | 7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 121 | 7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol | Drug Info | [55] | |||
| 122 | 7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 123 | 7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol | Drug Info | [52] | |||
| 124 | 7-hydroxy-1,2,9,9a-tetrahydrofluoren-3-one | Drug Info | [65] | |||
| 125 | 7-hydroxy-3-(4-hydroxyphenyl)-3H-quinazolin-4-one | Drug Info | [64] | |||
| 126 | 7-Phenyl-naphthalen-2-ol | Drug Info | [49] | |||
| 127 | 8-(2,2-dimethylpropyl)naringenin | Drug Info | [38] | |||
| 128 | 8-(2-methylpropyl)naringenin | Drug Info | [38] | |||
| 129 | 8-(3-methylbutyl)naringenin | Drug Info | [38] | |||
| 130 | 8-benzylnaringenin | Drug Info | [38] | |||
| 131 | 8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 132 | 8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol | Drug Info | [49] | |||
| 133 | 8-methylnaringenin | Drug Info | [38] | |||
| 134 | 8-n-heptylnaringenin | Drug Info | [38] | |||
| 135 | 8-n-nonylnaringenin | Drug Info | [38] | |||
| 136 | 8-n-pentylnaringenin | Drug Info | [38] | |||
| 137 | 8-n-propylnaringenin | Drug Info | [38] | |||
| 138 | 8-n-undecylnaringenin | Drug Info | [38] | |||
| 139 | Acetate Ion | Drug Info | [66] | |||
| 140 | BROUSSONIN A | Drug Info | [68] | |||
| 141 | COUMESTROL | Drug Info | [59] | |||
| 142 | CP-394531 | Drug Info | [69] | |||
| 143 | CP-409069 | Drug Info | [69] | |||
| 144 | daidzein | Drug Info | [62] | |||
| 145 | DIHYDRORALOXIFENE | Drug Info | [71] | |||
| 146 | Doxorubicin-Formaldehyde Conjugate | Drug Info | [72] | |||
| 147 | EFFUSOL | Drug Info | [58] | |||
| 148 | Geldanamycin-estradiol hybrid | Drug Info | [74] | |||
| 149 | GNF-PF-3037 | Drug Info | [39] | |||
| 150 | MORIN | Drug Info | [39] | |||
| 151 | Nafoxidine | Drug Info | [76] | |||
| 152 | Para-Mercury-Benzenesulfonic Acid | Drug Info | [66] | |||
| 153 | SOPHORAFLAVANONE B | Drug Info | [38] | |||
| 154 | THIOGENISTEIN | Drug Info | [64] | |||
| 155 | TUPICHINOL C | Drug Info | [68] | |||
| 156 | WAY-169916 | Drug Info | [80] | |||
| 157 | ZK-164015 | Drug Info | [81] | |||
| 158 | [1,1':2',1'']Terphenyl-4'-carbaldehyde oxime | Drug Info | [82] | |||
| Antagonist | [+] 7 Antagonist drugs | + | ||||
| 1 | Conjugated Estrogens | Drug Info | [1], [28] | |||
| 2 | MF-101 | Drug Info | [31] | |||
| 3 | EM-800 | Drug Info | [41] | |||
| 4 | HPTE | Drug Info | [75] | |||
| 5 | PHTPP | Drug Info | [77] | |||
| 6 | R,R-THC | Drug Info | [78] | |||
| 7 | Trans-hydroxytamoxifen | Drug Info | [79] | |||
| Agonist | [+] 14 Agonist drugs | + | ||||
| 1 | Estrogen | Drug Info | [29] | |||
| 2 | AUS-131 | Drug Info | [33] | |||
| 3 | ERB-041 | Drug Info | [5], [34] | |||
| 4 | Erteberel | Drug Info | [35] | |||
| 5 | VG-101 | Drug Info | [36] | |||
| 6 | ERB-257 | Drug Info | [37] | |||
| 7 | ERB-196 | Drug Info | [43] | |||
| 8 | bisphenol A | Drug Info | [67] | |||
| 9 | diarylpropionitril | Drug Info | [70] | |||
| 10 | ERB-002 | Drug Info | [73] | |||
| 11 | GTx-878 | Drug Info | [73] | |||
| 12 | KB-9520 | Drug Info | [73] | |||
| 13 | NDC-1022 | Drug Info | [73] | |||
| 14 | WAY200070 | Drug Info | [52] | |||
| Modulator | [+] 4 Modulator drugs | + | ||||
| 1 | Trilostane | Drug Info | [30] | |||
| 2 | Premarin/Pravachol | Drug Info | [9] | |||
| 3 | Genistein | Drug Info | [32] | |||
| 4 | GTx-822 | Drug Info | [73] | |||
| 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-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Estrogen signaling pathway | |||||
| 2 | Prolactin signaling pathway | |||||
| PID Pathway | [+] 3 PID Pathways | + | ||||
| 1 | Plasma membrane estrogen receptor signaling | |||||
| 2 | Validated nuclear estrogen receptor beta network | |||||
| 3 | Validated nuclear estrogen receptor alpha network | |||||
| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Nuclear Receptor transcription pathway | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | SIDS Susceptibility Pathways | |||||
| 2 | Ovarian Infertility Genes | |||||
| 3 | Integrated Pancreatic Cancer Pathway | |||||
| 4 | Nuclear Receptors | |||||
| Target-Related Models and Studies | Top | |||||
|---|---|---|---|---|---|---|
| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85. | |||||
| REF 2 | Clinical pipeline report, company report or official report of Lilly. | |||||
| REF 3 | ClinicalTrials.gov (NCT00190697) A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment. U.S. National Institutes of Health. | |||||
| REF 4 | ClinicalTrials.gov (NCT01613170) Premarin Versus Toviaz for Treatment of Overactive Bladder. U.S. National Institutes of Health. | |||||
| REF 5 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
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