Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT05171
[1]
m6A modification ESR1 ESR1 FTO Demethylation : m6A sites Direct Enhancement Non-coding RNA miR-3492 ESR1  lncRNA       miRNA   circRNA
m6A Modification:
m6A Regulator Fat mass and obesity-associated protein (FTO) ERASER
m6A Target Estrogen receptor (ESR1)
Epigenetic Regulation that have Cross-talk with This m6A Modification:
Epigenetic Regulation Type Non-coding RNA (ncRNA)
Epigenetic Regulator hsa-miR-3492 microRNA View Details
Regulated Target Estrogen receptor (ESR1) View Details
Crosstalk Relationship m6A  →  ncRNA Enhancement
Crosstalk Mechanism m6A modification regulates the functionality of ncRNAs through by altering the methylation levels of shared targets
Crosstalk Summary Mechanistically, the risk allele of rs67734009 increased Estrogen receptor (ESR1) expression via hsa-miR-3492 binding and m6A modification which is regulated by FTO.
Responsed Disease Colorectal cancer ICD-11: 2B91
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
Estrogen receptor (ESR1) 290 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Estrone Approved [2]
Synonyms
Aquacrine; Crinovaryl; Cristallovar; Crystogen; Destrone; Disynformon; Endofolliculina; Esterone; Estrin; Estrol; Estron; Estrona; Estronum; Estrovarin; Estrugenone; Estrusol; Femidyn; Fermidyn; Folikrin; Folipex; Folisan; Follestrine; Follestrol; Folliculin; Folliculine; Follicunodis; Glandubolin; Hiestrone; Hormestrin; Hormofollin; Hormovarine; Kestrone; Ketodestrin; Ketohydroxyestrin; Ketohydroxyoestrin; Ketophydroxyestrin; Kolpon; Menagen; Menformon; Mestronaq; OESTRONE; Oestrin; Oestroform; Oestronum; Oestroperos; Ovifollin; Perlatan; Solliculin; Theelin; Thelestrin; Thelykinin; Thynestron; Tokokin; Unden; Unigen; Wehgen; Wynestron; Estrogenic Substance; Estrona [Spanish]; Femestrone injection; Follicular hormone; Folliculine benzoate; Hauck Brand of Estrone; Hyrex Brand of Estrone; Menformon A; Oestrone [Steroidal oestrogens]; Penncap M; Vortech Brand of Estrone; WynestronPencap M; CMC_13458; E 9750; E0026; E(sub 1); Estrona [INN-Spanish]; Estrone (E1); Estrone (TN); Estrone [USAN:INN]; Estrone-A; Estronum [INN-Latin]; Femestrone inj.; Ketohydroxy-Estratriene; NATURAL ESTROGENIC SUBSTANCE-ESTRONE; Oestrone, Estrone; Ovex (tablets); Unden (pharmaceutical); Unden (pharmaceutical) (VAN); Estrone (JAN/USP/INN); Estrone, (8 alpha)-Isomer; Estrone, (9 beta)-Isomer; Estrone, (+-)-Isomer; [2,4,6,7-3H]-E1; Delta-1,3,5-Estratrien-3beta-ol-17-one; Delta-1,3,5-Oestratrien-3beta-ol-17-one; Delta-1,3,5-estratrien-3-beta-ol-17-one; Delta-1,3,5-oestratrien-3-beta-ol-17-one; (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-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; 3-hydroxy-estra-1,3,5(10)-trien-17-one
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MOA Agonist
Activity EC50 = 0.7 nM
External Link
 Compound Name Conjugated estrogens b Approved [3]
Synonyms
Enjuvia (TN)
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MOA Modulator
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 Compound Name Raloxifene Approved [4]
Synonyms
Raloxifene (extended-release, CDT)
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MOA Modulator
Activity Ki = 0.03 nM
External Link
 Compound Name Ospemifene Approved [5]
Synonyms
128607-22-7; Osphena; FC-1271a; Deamino-hydroxytoremifene; Fc-1271; 2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol; UNII-B0P231ILBK; CCRIS 9205; B0P231ILBK; CHEBI:73275; 2-(p-((Z)-4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)ethanol; senshio; Ethanol, 2-[4-[(1Z)-4-chloro-1,2-diphenyl-1-butenyl]phenoxy]-; 2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}ethanol; Ophena; Ospemifene [USAN:INN:BAN]; Deaminotoremifene; Osphena (TN); Deaminohydroxytoremifene; AC1MI19T; C24H23ClO2
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MOA Modulator
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 Compound Name Estropipate Approved [6]
Synonyms
7280-37-7; Piperazine estrone sulfate; Harmogen; Ogen; Ortho-Est; UNII-SVI38UY019; Piperazine estronesulfate; Sulestrex; SVI38UY019; Estra-1,3,5(10)-trien-17-one, 3-(sulfooxy)-, compd. with piperazine (1:1); OGEN 2.5; Estropipate (USP); OGEN 5; Ogen (TN); OGEN .625; OGEN 1.25; EINECS 230-696-3; piperazine (8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl sulfate; Piperazine oestrone sulphate; Conjugated estrogens: piperazine estrone sulfate; Estrone hydrogen sulf
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MOA Modulator
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 Compound Name Quinestrol Approved [7]
Synonyms
EECPE; Eston; Estrovis; Estrovister; Plestrovis; Quilea; Quinestrolo; Quinestrolum; Quinestrolo [DCIT]; Estrovis 4000; W 3566; Estrovis (TN); Ethinyl Estradiol 3-Cyclopentyl Ether; Qui-Lea; Quinestrolum [INN-Latin]; W-3566; Quinestrol (USAN/INN); Quinestrol [USAN:INN:BAN]; Estradiol-17-beta 3-cyclopentyl ether; (8R,9S,13S,14S,17R)-3-cyclopentyloxy-17-ethynyl-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-ol; 17-alpha-Ethinylestradiol 3-cyclopentyl ether; 17ALPHA-ETHYLNYL-1,3,5[10]ESTRATRIENE-3,17BETA-DIOL 3-CYCLOPENTYL ETHER; 17alpha-Ethynyl-1,3,5(10)-estratriene-3,17beta-diol 3-cyclopentyl ether; 17alpha-Ethynylestradiol 3-cyclopentyl ether; 3-(Cyclopentyloxy)-19-nor-17-alpha-pregna-1,3,5(10)-trien-20-yn-17-ol; 3-(Cyclopentyloxy)-19-nor-17alpha-pregna-1,3,5(10)-trien-20-yn-17-ol; 3-(cyclopentyloxy)-17beta-ethynylestra-1,3,5(10)-trien-17-ol; 3-Cyclopentyloxy-17alpha-ethynylestra-1,3,5(10)-trien-17beta-ol
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MOA Modulator
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 Compound Name Toremifene Approved [8]
Synonyms
Acapodene; Estrimex; Farestone; Toremifeno; Toremifenum; Toremifene Base; Toremifeno [Spanish]; Toremifenum [Latin]; GTx 006; Acapodene (TN); FC-1157a; Fareston (TN); GTx-006; Toremifene (INN); Toremifene [INN:BAN]; Z-Toremifene; GTX-006 (Acapodene); Toremifene Citrate (1:1); {2-[4-(4-Chloro-1,2-diphenyl-but-1-enyl)-phenoxy]-ethyl}-dimethyl-amine; (Z)-2-(4-(4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine; 2-(p-[(Z)-4-chloro-1,2-diphenyl-1-butenyl]-phenoxy)-N,N-dimethyl-ethylamine citrate(1:1); 2-(para-((Z)-4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethylethylamine (IUPAC); 2-({4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenyl}oxy)-N,N-dimethylethanamine; 2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine; 2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine
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MOA Modulator
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 Compound Name Ethinyl Estradiol Approved [9]
Synonyms
Aethinyloestradiolum; Aethinyoestradiol; Amenoron; Amenorone; Anovlar; Certostat; Cyclosa; Dicromil; Diprol; Dyloform; Ertonyl; Esteed; Estigyn; Estinyl; Estopherol; Estoral; Estorals; Ethidol; Ethinoral; Ethinylestradiolum; Ethinylestriol; Ethinyloestradiol; Ethynylestradiol; Ethynyloestradiol; Eticyclin; Eticyclol; Eticylol; Etinestrol; Etinestryl; Etinilestradiol; Etinilestradiolo; Etinoestryl; Etistradiol; Etivex; Feminone; Follicoral; Ginestrene; Inestra; Kolpolyn; Linoral; Lynoral; Menolyn; Microfollin; Novestrol; Oradiol; Orestralyn; Orestrayln; Palonyl; Perovex; Primogyn; Prosexol; Spanestrin; Ylestrol; Aethinyoestradiol [German]; Component of Demulen; Component of Oracon; Component of Ortrel; Diogyn E; Effik Brand of Ethinyl Estradiol; Estoral [Orion]; Ethinyl Estradiol Hemihydrate; Ethinyl Estradiol [USP]; Ethinyl Oestradiol Effik; Ethinylestradiol Jenapharm; Ethinyloestradiol [Steroidal oestrogens]; Ethynyl estradiol; Etinilestradiolo [DCIT]; Jenapharm Brand of Ethinyl Estradiol; Microfollin Forte; Organon Brand of Ethinyl Estradiol; PUBERTAL ETHINYL ESTRADIOL STUDY; Primogyn C; Primogyn M; Progynon C; Progynon M; Schering Brand of Ethinyl Estradiol; EE2; Ethinyl E2; Ethy 11; Diognat-E; Diogyn-E; EE(sub 2); Estinyl (TN); Eston-E; Estoral (Orion); Estoral (VAN); Estradiol, Ethinyl; Estradiol, Ethynyl; Ethinyl estradiol (USP); Ethinyl-Oestradiol Effik; Ethinyl-oestranol; Ethinylestradiolum [INN-Latin]; Ethynylestradiol, Ethinyl Estradiol; Etinilestradiol [INN-Spanish]; Hemihydrate, Ethinyl Estradiol; Jenapharm, Ethinylestradiol; Neo-Estrone; Nogest-S; OVULEN-21; OVULEN-28; Ortho-Cyclen; Chee-O-Gen; Chee-O-Genf; Ethinylestradiol (JP15/INN); Ethinylestradiol [INN:BAN:JAN]; Ethinyl Estradiol, (8 alpha)-Isomer; 17 alpha-Ethinylestradiol; 17 alpha-Ethynylestradiol; 17 alpha-Ethynyloestradiol; 17 alpha-ethinyestradiol; 17-Ethinyl-3,17-estradiol; 17-Ethinyl-3,17-oestradiol; 17-Ethinylestradiol; 17-Ethynylestradiol; 17-Ethynyloestradiol; 17-alpha-Ethinyl-17-beta-estradiol; 17-alpha-Ethynyl-17-beta-oestradiol; 17-alpha-Ethynylestradiol; 17-alpha-Ethynylestradiol-17-beta; 17-alpha-Ethynylestradiol-l7-beta; 17-alpha-Ethynyloestradiol-17-beta; 17-alpha-ethynyl estradiol; 17.alpha.-Ethinyl-17.beta.-estradiol; 17.alpha.-Ethinylestradiol; 17.alpha.-Ethynyl-17.beta.-oestradiol; 17.alpha.-Ethynylestradiol; 17.alpha.-Ethynyloestradiol; 17a-Ethynylestradiol; 17alpha-Ethinyl estradiol; 17alpha-Ethinylestradiol; 17alpha-Ethinylestradiol-17beta; 17alpha-Ethynylestradiol; 17alpha-Ethynyloestradiol; 17alpha-Ethynyloestradiol-17beta
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MOA Agonist
Activity IC50 = 2 nM
External Link
 Compound Name Tamoxifen Approved [10]
Synonyms
10540-29-1; trans-Tamoxifen; Crisafeno; Soltamox; Tamoxifene; Diemon; Tamoxifenum; Tamoxifeno; Tamizam; Istubol; Tamoxen; Citofen; Oncomox; Valodex; Retaxim; Tamoxifene [INN-French]; Tamoxifenum [INN-Latin]; Tamoxifeno [INN-Spanish]; Tamoxifen (Z); Tamoxifen and its salts; Tamoxifen [INN:BAN]; ICI-46474; ICI 47699; TRANS FORM OF TAMOXIFEN; CCRIS 3275; UNII-094ZI81Y45; HSDB 6782; CHEMBL83; EINECS 234-118-0; 1-p-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; Nourytam; Novaldex; Tamone; Tamoxifeno;Tamoxifenum; Tomaxithen; Gen-Tamoxifen; Istubal (TN); Nolvadex (TN); Nolvadex-D; Novo-Tamoxifen; Pms-Tamoxifen; Tamoplex (TN); Tamoxifen (INN); Tamoxifen (TN); Valodex (TN); TAMOXIFEN (TAMOXIFEN CITRATE (54965-24-1)); Trans-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; (Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene; (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(4-(1,2-diphenylbut-1-enyl)phenoxy)-N,N-dimethylethanamine; (Z)-2-(para-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylamine (IUPAC); (Z)-2-[4-(1,2)-DIPHENYL-1-BUTENYL)-PHENOXY]-N,N-DIMETHYLETHANAMINE; (Z)-2-[p-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethylamine; 1-p-beta-Dimethylamino-ethoxyphenyl-trans-1,2-diphenylbut-1-ene; 1-para-beta-Dimethylaminoethoxyphenyl-trans-1,2-diphenylbut-1-ene; 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine; 2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine; Tamoxifen (Hormonal therapy); [3H]tamoxifen
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MOA Antagonist
Activity IC50 = 8 nM
External Link
 Compound Name Elacestrant Approved [11]
Synonyms
ER-306323; ER-308698; SERMs, Eisai/Radius; Selective estrogen receptor modulators, Eisai/Radius
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MOA Modulator
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 Compound Name Estradiol Valerate Approved [12]
Synonyms
Delestrogen
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MOA Modulator
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 Compound Name Estradiol Approved [2]
Synonyms
Aerodiol; Alora; Altrad; Aquadiol; Bardiol; Climaderm; Climara; Compudose; Corpagen; Dermestril; Destradiol; Dihydrofolliculin; Dihydromenformon; Dihydrotheelin; Dihydroxyesterin; Dihydroxyestrin; Dihydroxyoestrin; Dimenformon; Diogyn; Diogynets; Divigel; Elestrin; Encore; Esclim; Estrace; Estraderm; Estradiolo; Estradiolum; Estradot; Estraldine; Estrasorb; Estreva; Estrifam; Estring; Estroclim; Estrodiolum; Estrogel; Estrovite; Evamist; Evorel; Extrasorb; Femanest; Femestral; Femestrol; Fempatch; Femtran; Follicyclin; Gelestra; Ginedisc; Ginosedol; GynPolar; Gynergon; Gynestrel; Gynodiol; Gynoestryl; Innofem; Lamdiol; Macrodiol; Macrol; Menest; Menorest; Microdiol; Nordicol; Oesclim; Oestergon; Oestradiol; Oestradiolum; Oestrogel; Oestroglandol; Oestrogynal; Ovahormon; Ovasterol; Ovastevol; Ovociclina; Ovocyclin; Ovocycline; Ovocylin; Perlatanol; Polyestradiol; Primofol; Profoliol; Progynon; Syndiol; Systen; Tradelia; Trocosone; Vagifem; Vivelle; Zerella; Zesteem; Zesteen; Zumenon; Climara Forte; Component of Menrium; Estraderm MX; Estraderm TTS; Estradiolo [DCIT]; Estradiolum [INN]; Estring vaginal ring; Estrofem Forte; Oestradiol Berco; Oestradiol R; Progynon DH; Sandrena Gel; Sisare Gel; Trial SAT; CMC_11154; Compudose 200; Compudose 365; E 2; E 8875; E0025; Epiestriol 50; Estraderm TTS 100; Estraderm TTS 50; Estrapak 50; Estroclim 50; Estrofem 2; Sandrena 1; [3H]]estradiol; Activella (TN); Alora (TN); Alpha-Oestradiol; AngeliQ (TN); B-Estradiol; Beta-Estradiol; Beta-Oestradiol; Cis-Estradiol; Cis-Oestradiol; Climara (TN); D-Estradiol; D-Oestradiol; Divigel (TN); E(sub 2); Elestrin (TN); Estrace (TN); Estraderm (TN); Estraderm TTS (TN); Estradiol [USAN:INN]; Estradiol acetate (TN); Estradiol cypionate (TN); Estradiol valerate (TN); Estradiol-17 beta; Estradiol-17beta; Estrasorb (TN); Estrasorb Topical (TN); Estring (TN); Estrofem (TN); Estrogel (TN); EvaMist (TN); Femring (TN); Innofem (TN); Menostar (TN); Oestradiol-17beta; Progynon-DH; Progynova (TN); S-21400; SK-Estrogens; SL-1100; VIVELLE-DOT; Vagifem (TN); Vivelle (TN); [3H]-estradiol; Estradiol-17-beta; Estradiol-3,17beta; Oestradiol-17-beta; Vivelle-Dot (TN); D-3,17beta-Estradiol; [2,4,6,7-3H]-E2; 17 beta-Estradiol; 17-.BETA.-Estradiol; 17-beta-OH-estradiol; 17-beta-estradiol; 17.beta.-Estradiol; 17.beta.-Oestradiol; 17b-Oestradiol; 17beta oestradiol; 17beta-Estradiol; 17beta-Oestradiol; 3,17-beta-Estradiol; 3,17-beta-Oestradiol; 3,17.beta.-Estradiol; 3,17beta-Estradiol
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MOA Agonist
Activity EC50 = 0.004 nM
External Link
 Compound Name Danazol Approved [13]
Synonyms
Anatrol; Chronogyn; Cyclomen; Danatrol; Danazant; Danazole; Danazolum; Danocrine; Danogen; Danokrin; Danol; Danoval; Danzol; Ladogal; Norciden; Panacrine; Winobanin; Alphapharm Brand of Danazol; Antigen Brand of Danazol; Kendrick Brand of Danazol; Ratiopharm Brand of Danazol; Sanofi Brand of Danazol; Sanofi Synthelabo Brand ofDanazol; Sanofi Winthrop Brand of Danazol; WIN 17757; Danazol-ratiopharm; Danazolum [INN-Latin]; Danocrine (TN); WIN 17,757; WIN-17757; Win 17, 757; Danazol (JAN/USP/INN); Danazol [USAN:BAN:INN:JAN];[1,2]oxazolo[4',5':2,3]-17alpha-pregn-4-en-20-yn-17-ol; (1R,3aS,3bR,10aR,10bS,12aS)-1-ethynyl-10a,12a-dimethyl-2,3,3a,3b,4,5,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d]isoxazol-1-ol; (1S,2R,13R,14S,17R,18S)-17-ethynyl-2,18-dimethyl-7-oxa-6-azapentacyclo[11.7.0.0^{2,10}.0^{4,8}.0^{14,18}]icosa-4(8),5,9-trien-17-ol; 1-Ethynyl-10a,12a-dimethyl-2,3,3a,3b,4,5,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d]isoxazol-1-ol; 17-alpha-2,4-Pregnadien-20-yno(2,3-d)isoxazol-17-ol; 17-alpha-Pregn-4-en-20-yno(2,3-d)isoxazol-17-ol; 17-alpha-Pregna-2,4-dien-20-yno(2,3-d)isoxazol-17-ol; 17.Alpha.-Pregna-2, {4-dien-20-yno[2,3-d]isoxazol-17-ol}; 17alpha-Pregna-2,4-dien-20-yno(2,3-d)isoxazol-17-ol
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MOA Antagonist
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 Compound Name Dienestrol Approved [14]
Synonyms
Agaldog; Cycladiene; Dehydrostilbestrol; Dehydrostilboestrol; Dienesterol; Dienestrolo; Dienestrolum; Dienoestrol; Dienol; Dinestrol; Dinovex; Estragard; Estraguard; Estrodienol; Estroral; Follidiene; Follormon; Gynefollin; Hormofemin; Isodienestrol; Oestrasid; Oestrodiene; Oestrodienol; Oestroral; Oestrovis; Restrol; Retalon; Sexadien; Synestrol; Teserene; Willnestrol; Dienestrolo [DCIT]; Dienoestrol [Nonsteroidal oestrogens]; Dienoestrol bp; Alpha-Dienestrol; DV (TN); Dienestrolum [INN-Latin]; Para-Dien; Restrol, Dienestrol; Dienestrol (E,E); Dienestrol (USP/INN); Dienestrol, (E,E)-Isomer; P,p'-(Diethylideneethylene)diphenol; Para,para'-(Diethylideneethylene)diphenol; Di(p-oxyphenyl)-2,4-hexadiene; Di(para-oxyphenyl)-2,4-hexadiene; Phenol, 4,4'-(1,2-diethylidene-1,2-ethanediyl)bis-, (E,E-(9CI); (E,E)-Dienestrol; 3,4-Bis(4-hydroxyphenyl)-2,4-hexadiene; 3,4-Bis(p-hydroxyphenyl)-2,4-hexadiene; 3,4-Bis(para-hydroxyphenyl)-2,4-hexadiene; 4,4'-(1,2-Diethylidene-1,2-ethanediyl)bisphenol; 4,4'-(2E,4E)-hexa-2,4-diene-3,4-diyldiphenol; 4,4'-(Diethylideneethylene)diphenol; 4,4'-Dihydroxy-gamma,delta-diphenyl-beta,delta-hexadiene; 4,4'-Hydroxy-gamma,delta-diphenyl-beta,delta-hexadiene; 4,4'-hexa-2,4-diene-3,4-diyldiphenol; 4-[(2E,4E)-4-(4-hydroxyphenyl)hexa-2,4-dien-3-yl]phenol
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MOA Agonist
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 Compound Name Conjugated estrogens a Approved [15]
Synonyms
Conestin (TN)
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MOA Modulator
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 Compound Name Promestriene Approved [16]
Synonyms
BCP9000134; VA11593; A824465; I06-0300
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MOA Modulator
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 Compound Name Clomifene Approved [17]
Synonyms
Androxal; Chlomaphene; Chloramifene; Cisclomifenum; Cisclomiphene; Clomifen; Clomifeno; Clomifenum; Clomifert; Clomiphene; Clostilbegit; Enclomifene; Enclomifeno; Enclomifenum; Enclomiphen; Enclomiphene; Klostilbegit; Transclomifenum; Transclomiphene; Zuclomifene; Zuclomifeno; Zuclomifenum; Zuclomiphene; Clomiphene B;Enclomiphene [USAN]; ISOMER B; Zuclomiphene [USAN]; Cis-Clomifene; Cis-Clomiphene; Clomid (TN); Clomifene (INN); Clomifene (TN); Clomifene [INN:BAN]; Clomifeno [INN-Spanish]; Clomifenum [INN-Latin]; En-Clomiphene; Enclomifeno [INN-Spanish]; Enclomifenum [INN-Latin]; Enclomiphene (USAN); Milophene (TN); RMI 16,289; RMI-16289; RMI-16312; Serophene (TN); Trans-Clomifene; Trans-Clomiphene; Zuclomifeno [INN-Spanish]; Zuclomifenum [INN-Latin]; Zuclomiphene (USAN); Cis-2-(p-(2-Chloro-1,2-diphenylvinyl)phenoxy)triethylamine; Trans-2-(p-(2-Chloro-1,2-diphenylvinyl)phenoxy)triethylamine; Cis-2-(4-(2-Chloro-1,2-diphenylethenyl)phenoxy)-N,N-diethylethanamine; Trans-2-(4-(2-Chloro-1,2-diphenylethenyl)phenoxy)-N,N-diethylethanamine; (E)-2-(p-(2-Chloro-1,2-diphenylvinyl)phenoxy)triethylamine; (Z)-2-(p-(2-Chloro-1,2-diphenylvinyl)phenoxy)triethylamine; (Z)-isomer; 1-(p-(beta-Diethylaminoethoxy)-phenyl)-1,2-diphenylchloroethylene; 2-(4-(2-Chloro-1,2-diphenylethenyl)phenoxy)-N,N-diethylethanamine; 2-(p-(2-Chloro-1,2-diphenylvinyl)phenoxy)triethylamine; 2-(p-(beta-Chloro-alpha-phenylstyryl)phenoxy)-triethylamine; 2-(p-(beta-chloro-alpha-phenylstyryl)phenoxy)triethylamine; 2-({4-[(Z)-2-chloro-1,2-diphenylethenyl]phenyl}oxy)-N,N-diethylethanamine; 2-[4-(2-chloro-1,2-diphenylethenyl)phenoxy]-N,N-diethylethanamine; 2-[4-[(E)-2-chloro-1,2-diphenylethenyl]phenoxy]-N,N-diethylethanamine; 2-[4-[(Z)-2-chloro-1,2-diphenylethenyl]phenoxy]-N,N-diethylethanamine; 2-{4-[(E)-2-chloro-1,2-diphenylethenyl]phenoxy}-N,N-diethylethanamine
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MOA Modulator
External Link
 Compound Name Clomiphene Citrate Approved [12]
Synonyms
Clomid; Milophene; Serophene
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MOA Modulator
External Link
 Compound Name Mestranol Approved [18]
Synonyms
Devocin; Menophase; Mestranolo; Mestranolum; Norquen; Ovastol; Component of Norinyl; Component of Norquen; Component of Ovulen; Ethynylestradiol methyl ether; Mestranol [Steroidal oestrogens]; Mestranolo [DCIT]; EE3ME; Ethinyl Estradiol 3 Methyl Ether; SC 4725; Component of Ortho-Novum; Delta-MVE; EE(sub3)ME; EthinylEstradiol 3-Methyl Ether; Ethinyloestradiol 3-methyl ether; Ethynylestradiol 3-methyl ether; Ethynyloestradiol 3-methyl ether; Inostral (steroid); Mestranolum [INN-Latin]; Mestranol (JP15/USP/INN); Mestranol [USAN:INN:BAN:JAN]; Alpha.-19-Norpregna-1,3,5(10)-trien-20-yn-17-ol, 3-meth; (17beta)-17-ethynyl-3-(methyloxy)estra-1,3,5(10)-trien-17-ol; 17-Ethynyl-3-methoxy-1,3,5(10)-oestratien-17-beta-ol; 17-Ethynyl-3-methoxyestra-1,3,5(10)-trien-17-ol; 17-Ethynylestradiol 3-methyl ether; 17-Ethynyloestradiol 3-methyl ether; 17-alpha-Ethinyl estradiol 3-methyl ether; 17-alpha-Ethinyl oestradiol 3-methyl ether; 17-alpha-Ethynyl-3-methoxy-1,3,5(10)-estratrien-17-beta-ol; 17-alpha-Ethynyloestradiol methyl ether; 17-ethynyl-3-methoxyestra-1(10),2,4-trien-17beta-ol; 17-ethynyl-3-methoxyoestra-1(10),2,4-trien-17beta-ol; 17alpha-Ethinyl estradiol 3-methyl ether; 17alpha-Ethinyl oestradiol 3-methyl ether; 17alpha-Ethinylestradiol 3-methyl ether; 17alpha-Ethynylestradiol 3-methyl ether; 17alpha-Ethynylestradiol methyl ether; 17alpha-Ethynyloestradiol 3-methyl ether; 17beta-Estradiol, 17-ethynyl-, 3-(methyl ether); 3-Methoxy-17-alpha-19-norpregna-1,3,5(10)-trien-20-yn-17-ol; 3-Methoxy-17-alpha-ethinylestradiol; 3-Methoxy-17-alpha-ethinyloestradiol; 3-Methoxy-17-alpha-ethynyl-1,3,5(10)-estratrien-17-beta-ol; 3-Methoxy-17-alpha-ethynyl-1,3,5(10)-oestratrien-17-beta-ol; 3-Methoxy-17-alpha-ethynylestradiol; 3-Methoxy-17-alpha-ethynyloestradiol; 3-Methoxy-17-ethynyloestradiol-17-beta; 3-Methoxy-17alpha-ethinylestradiol; 3-Methoxy-17alpha-ethinyloestradiol; 3-Methoxy-17alpha-ethynyl-1,3,5(10)-estratrien-17beta-ol; 3-Methoxy-17alpha-ethynyl-1,3,5(10)-oestratrien-17beta-ol; 3-Methoxy-17alpha-ethynylestradiol; 3-Methoxy-17alpha-ethynyloestradiol; 3-Methoxy-19-nor-17-alpha-pregna-1,3,5(10)-trien-20-yn-17-ol; 3-Methoxy-19-nor-17alpha-pregna-1,3,5(10)-trien-20-yn-17-ol; 3-Methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17beta-ol; 3-Methoxyethynylestradiol; 3-Methoxyethynyloestradiol; 3-Methylethynylestradiol; 3-Methylethynyloestradiol; 3-O-Methylethynylestradiol
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MOA Agonist
External Link
 Compound Name Fulvestrant Approved [19]
Synonyms
Faslodex; AstraZeneca brand of fulvestrant; Fulvestrant [USAN]; Ici 182780; ZD 182780; ZM 182780; Faslodex (TN); ZD-182780; ZD-9238; ZM-182780; Faslodex(ICI 182,780); Faslodex, ICI 182780, Fulvestrant; Fulvestrant (JAN/USAN/INN); (7R,13S,17S)-13-methyl-7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol; (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7R,8S,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl) nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol; (7alpha,17beta)-7-{9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl}estra-1,3,5(10)-triene-3,17-diol; 7-(9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl)estra-1,3,5(10)-triene-3,17-diol; 7alpha-(9-((4,4,5,5,5,-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-(9-((4,4,5,5,5-Pentafluoropentyl)sulfinyl)nonyl)estra-1,3,5(10)-triene-3,17beta-diol; 7alpha-[9[(4,4,5,5,5-Pentafluropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3, 17 beta diol; ICI
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MOA Antagonist
Activity IC50 = 0.06 nM
External Link
 Compound Name Fosfestrol Approved [20]
Synonyms
Diethylstilbestrol diphosphate; 522-40-7; Phosphestrol; Phosphoestrolum; Honvan; Stilbestrol diphosphate; Desdp; Diethylstilbestryl diphosphate; Diethylstilbesterol diphosphate; ST52-Asta; Fosfestrolum [INN-Latin]; UNII-A0E0NMA80F; CCRIS 2778; (E)-Hex-3-ene-3,4-diylbis(4,1-phenylene) bis(dihydrogen phosphate); C18H22O8P2; EINECS 208-328-8; A0E0NMA80F; CHEBI:4532; Diethylstilbestrol diphosphate [USP]; NCGC00181335-01; Stilphostrol (TN); alpha,alpha'-Diethyl-(E)-4,4'-stilbenediol bis(dihydrogen phosphate)
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MOA Modulator
External Link
 Compound Name Bazedoxifene Approved [21]
Synonyms
Brilence; Conbriza; Viviant; Bazedoxifene acetate; TSE-424; WAY-140424; WAY-TES 424
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MOA Modulator
Activity IC50 = 3.7 nM
External Link
 Compound Name Gestrinone Approved [15]
Synonyms
Dimetrose (TN)
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MOA Modulator
External Link
 Compound Name Cenestin Approved [22]
Synonyms
Sodium equilin sulfate; Equilin sodium sulfate; Climopax; Estratab; 16680-47-0; Sodium equilin 3-monosulfate; Emopremarin; Novoconestron; Climestrone; Promarit; Primarin; Premarose; Premaril; Menotrol; Ganeake; Estropan; Estrifol; Premarina; Palopause; Menogen; Mannest; Hyphorin; Formatrix; Estromed; Equigyne; Prempak; Oestrilin; Menotab; Kestrin; Glyestrin; Estroate; Equilin 3-Sulfate Sodium Salt; Conjugen; Conestron; Ayerogen; Theogen; Sukingpo
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MOA Agonist
External Link
 Compound Name Esterified estrogens Approved [23]
MOA Modulator
External Link
 Compound Name Premarin/Trimegestone Approved [24]
Synonyms
Conjugated estrogen tablets
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MOA Modulator
External Link
 Compound Name Estradiol Acetate Approved [12]
Synonyms
Femring
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MOA Modulator
External Link
 Compound Name Estradiol Cypionate Approved [12]
Synonyms
Depo-estradiol
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MOA Modulator
External Link
 Compound Name Nomegestrol acetate Approved [25]
Synonyms
Lutenyl (TN)
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MOA Modulator
External Link
 Compound Name Levormeloxifene Approved [26]
Synonyms
Centchroman; Centron; Ormeloxifene; Saheli; NNC-46-0020; Non-steroidal (oral, contraception/cancer); Non-steroidal (oral, contraception/cancer), Central Drug Research Institute (CDRI)
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MOA Modulator
External Link
 Compound Name Cyclofenil Approved [27]
Synonyms
2624-43-3; Ondogyne; Cyclofenyl; Cyclophenyl; Cyclopenil; Fertodur; Sanocrisin; Cyclophenil; Sexovar; Rehibin; Sexadieno; Sexovid; Ondonid; Oginex; (Cyclohexylidenemethylene)bis(4,1-phenylene) diacetate; Neoclym; ICI 48213; Cyclofenilum [INN-Latin]; Ciclofenilo [INN-Spanish]; NSC 86464; H 3452; F 6066; UNII-J468V64WZ1; Cyclofenil [INN:BAN:DCF:JAN]; 4,4'-(Cyclohexylidenemethylene)diphenol diacetate ester; C23H24O4; EINECS 220-089-1; Bis(p-hydroxyphenyl)cyclohexyldienemethane diacetate; BRN 2014687; AI3-52271; F-6066
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MOA Modulator
Activity EC50 = 26 nM
External Link
 Compound Name Diethylstilbestrol Approved [28]
Synonyms
Acnestrol; Agostilben; Antigestil; Apstil; Bufon; Climaterine; Comestrol; Cyren; DES; Desma; Destrol; Diaethylstilboestrolum; Diastyl; Dibestrol; Dicorvin; Diethylstilbesterol; Diethylstilbestrolum; Diethylstilboesterol; Dietilestilbestrol; Dietilstilbestrolo; Distilbene; Domestrol; Dyestrol; Estril; Estrobene; Estrogenine; Estromenin; Estrosyn; Fonatol; Grafestrol; Gynopharm; Hibestrol; Idroestril; Iscovesco; Makarol; Menostilbeen; Micrest; Microest; Milestrol; OeKolp; Oestrogenine; Oestrolmensil; Oestromenin; Oestromensil; Oestromensyl; Oestromienin; Oestromon; Pabestrol; Palestrol; Protectona; Sedestran; Serral; Sexocretin; Sibol; Sintestrol; Stibilium; Stilbestroform; Stilbestrol; Stilbestrone; Stilbetin; Stilboefral; Stilboestroform; Stilboestrol; Stilbofolin; Stilbofollin; Stilbol; Stilkap; Strobene; Synestrin; Synthestrin; Synthoestrin; Synthofolin; Syntofolin; Tampovagan; Tylosterone; Vagestrol; APS Brand of Diethylstilbestrol; Anti gestil; Co Pharma Brand of Diethylstilbestrol; Comestrol estrobene; Cyren A; Diethylstilbestrol BP; Dietilestilbestrol [Spanish]; Dietilstilbestrolo [DCIT]; Estilbin MCO; Gerda Brand of Diethylstilbestrol; Oestrol vetag; Percutatrine oestrogenique iscovesco; ST IL; Stilbene Estrogen; Tampovagan stilboestrol; DiBestrol 2 Premix; MG 137; Rumestrol 1; Rumestrol 2; Cis-Des; Cis-Diethylstilbesterol; Cis-Diethylstilbestrol; Co-Pharma Brand of Diethylstilbestrol; DES (synthetic estrogen); Dawe's destrol; Di-Estryl; Diethylstilbestrol (DES); Diethylstilbestrol [USAN:INN]; Diethylstilbestrol, Disodium Salt; Diethylstilbestrolum [INN-Latin]; Dietilestilbestrol [INN-Spanish]; E-Diethylstilbestrol; Estilbin (MCO); Estrogen, Stilbene; Hi-Bestrol; Neo-Oestranol 1; Neo-Oestranol I; Neo-oe stranol 1; New-Estranol 1; Stil-Rol; Stilbestrol (TN); TRANS-DIETHYSTILBESTEROL; TRANSGENIC MODEL EVALUATION (DES); Trans-Diethylstilbesterol; Trans-Diethylstilbestrol; Trans-Diethylstilboesterol; DiBestrol "2" Premix; Dibestrol '2' premix; Diethylstilbestrol (USP/INN); Alpha,alpha'-Diethylstilbenediol; Diethylstilbestrol, (Z)-Isomer; Alpha,alpha'-Diethyl-4,4'-stilbenediol; (E)-3,4-Bis(4-hydroxyphenyl)-3-hexene; (E)-4,4'-(hex-3-ene-3,4-diyl)diphenol; (E)-Diethylstilbestrol; 3,4'(4,4'-Dihydroxyphenyl)hex-3-ene; 3,4-Bis(p-hydroxyphenyl)-3-hexene; 3,4-bis(4-hydroxyphenyl)hex-3-ene; 4,4'-(3E)-hex-3-ene-3,4-diyldiphenol; 4,4'-Dihydroxydiethylstilbene; 4,4'-hex-3-ene-3,4-diyldiphenol
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MOA Agonist
Activity EC50 = 0.007 nM
External Link
 Compound Name Estriol Approved [2]
Synonyms
Aacifemine; Destriol; Estratriol; Estriel; Estriolo; Gynaesan; Hemostyptanon; Holin; Hormomed; Hormonin; Klimoral; Oestratriol; Oestriol; Oestriolum; Orestin; Orgastyptin; Overstin; Ovestin; Ovestrion; Stiptanon; Synapause; Theelol; Thulol; Tridestrin; Trihydroxyestrin; Trihydroxyoestrin; Triodurin; Triovex; Deuslon A; Estriolo [Italian]; Folicular hormone; Follicular hormone hydrate; Oestriol [Steroidal oestrogens]; A 13610; E0218; OE3; Deuslon-A; Estriel (TN); Estriol [USAN:JAN]; Estriol, unconjugated; Ortho-Gynest; Estriol (JP15/USP); Estra-1,3,5(10)-trien-3,16alpha,17beta-triol; Estra-1,3,5(10)-triene-3,16,17-triol; Estra-1,3,5(10)-triene-3,16alpha,17beta-triol; Oestra-1,3,5(10)-triene-3,16alpha,17beta-triol; Oestra-1,3,5(10)-triene-3,16-alpha,17-beta-triol; Estra-1,3,5(10)-trien-3,16.alpha., 17.beta.-triol; Estra-1,3,5(10)-trien-3,16.alpha.,17.beta.-triol; Estra-1,3,5(10)-triene-3,16.alpha., 17.beta.-triol; Estra-1,3,5(10)-triene-3,16.alpha.,17.beta.-triol; Oestra-1,3,5(10)-triene-3,16.alpha., 17.beta.-triol; Oestra-1,3,5(10)-triene-3,16.alpha.,17.beta.-triol; (16.alpha.,17.beta.)-Estra-1,3,5(10)-triene-3,16,17-triol; (16.alpha.,17.beta.)-Oestra-1,3,5(10)-triene-3,16,17-triol; (16alpha,17beta)-Estra-1,3,5(10)-triene-3,16,17-triol; (16alpha,17beta)-Oestra-1,3,5(10)-triene-3,16,17-triol; 1,3,5(10)-ESTRATRIENE-3,16,17-TRIOL; 1,3,5(10)-Estratriene-3,16-alpha,17beta-triol; 1,3,5(10)-Estratriene-3,16.alpha., 17.beta.-triol; 1,3,5(10)-Estratriene-3,16.alpha.,17.beta.-triol; 1,3,5(10)-Estratriene-3,16alpha,17beta-Triol; 1,3,5-Estratriene-3.beta.,16-.alpha.,17-.beta.-triol; 1,3,5-Estratriene-3beta,16alpha,17beta-triol; 1,3,5-Oestratriene-3-.beta.,16.alpha.,17.beta.-triol; 1,3,5-Oestratriene-3beta,16alpha,17beta-triol; 16,17-Epiestriol; 16-Epiestriol; 16-Hydroxyestradiol; 16-alpha,17-beta-Estriol; 16-alpha,17-beta-Oestriol; 16-alpha-Hydroxyestradiol; 16-alpha-Hydroxyoestradiol; 16.alpha.,17.beta.-Estriol; 16.alpha.,17.beta.-Oestriol; 16.alpha.-Estriol; 16.alpha.-Hydroxy-17.beta.-estradiol; 16.alpha.-Hydroxyestradiol; 16.alpha.-Hydroxyoestradiol; 16alpha,17beta-Estriol; 16alpha,17beta-Oestriol; 16alpha-Hydroxy-17beta-estradiol; 16alpha-Hydroxyestradiol; 16alpha-Hydroxyoestradiol; 3,16-alpha,17-beta-Estriol; 3,16-alpha,17-beta-Oestriol; 3,16-alpha,17-beta-Trihydroxy-delta-1,3,5-estratriene; 3,16-alpha,17-beta-Trihydroxy-delta-1,3,5-oestratriene; 3,16-alpha,17-beta-Trihydroxyestra-1,3,5(10)-triene; 3,16-alpha,17-beta-Trihydroxyoestra-1,3,5(10)-triene; 3,16.alpha.,17.beta.-Estriol; 3,16.alpha.,17.beta.-Trihydroxy-.delta.-1,3,5-estratriene; 3,16.alpha.,17.beta.-Trihydroxy-.delta.-1,3,5-oestratriene; 3,16.alpha.,17.beta.-Trihydroxy-1,3,5(10)-estratriene; 3,16.alpha.,17.beta.-Trihydroxyestra-1,3,5(10)-triene; 3,16alpha,17beta-Estriol; 3,16alpha,17beta-Trihydroxy-1,3,5(10)-estratriene; 3,16alpha,17beta-Trihydroxy-delta-1,3,5-oestratriene; 3,16alpha,17beta-trihydroxy-Delta(1,3,5)-estratriene
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MOA Agonist
Activity EC50 = 1.995 nM
External Link
 Compound Name Mitotane Approved [29]
Synonyms
Chloditan; Chlodithan; Chlodithane; Khloditan; Khlodithan; Lysodren; Mitotan; Mitotano; Mitotanum; Mytotan; Bristol Myers Squibb Brand of Mitotane; C 3010; CB 313; CB313; PS694_SUPELCO; Bristol-Myers Squibb Brand of Mitotane; CB-313; Lysodren (TN); Mitotano [INN-Spanish]; Mitotanum [INN-Latin]; Ortho,para DDD; Mitotane [USAN:INN:JAN]; O,p-DDD; O,p-Tde; Ortho,para-DDD; Mitotane (JAN/USP/INN); O,p'-DDD; O,p'-Dichlorodiphenyldichloroethane; O,p'-TDE; Ethane, 1,1-dichloro-2-(o-chlorophenyl)-2-(p-chlorophenyl)-(8CI); (+-)-1,1-Dichloro-2-(o-chlorophenyl)-2-(p-chlorophenyl)ethane; (2,4'-Dichlorodiphenyl)dichloroethane; (o,p)-DDD; 1,1-Dichloro-2,2-bis(2,4'-dichlorophenyl)ethane; 1,1-Dichloro-2-(o-chlorophenyl)-2-(p-chlorophenyl)ethane; 1,1-Dichloro-2-(p-chlorophenyl)-2-(o-chlorophenyl)ethane; 1-(2-Chlorophenyl)-1-(4-chlorophenyl)-2,2-dichloroethane; 1-Chloro-2-(2,2-dichloro-1-(4-chlorophenyl)ethyl)benzene; 1-Chloro-2-[2,2-dichloro-1-(4-chlorophenyl)ethyl]benzene; 2,2-Bis(2-chlorophenyl-4-chlorophenyl)-1,1-dichloroethane; 2,4'-Ddd; 2,4'-Dichlorodiphenyldichloroethane; 2,4'-Dichlorophenyldichlorethane; 2-(2-Chlorophenyl)-2-(4-chlorophenyl)-1,1-dichloroethane; 2-(o-Chlorophenyl)-2-(p-chlorophenyl)-1,1-dichloroethane
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MOA Binder
External Link
 Compound Name ARZOXIFENE Approved [30]
Synonyms
182133-25-1; UNII-E569WG6E60; LY 353381; E569WG6E60; 2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol; 2-(4-methoxyphenyl)-3-(4-(2-(piperidin-1-yl)ethoxy)phenoxy)benzo[b]thiophen-6-ol; Arzoxifene [INN]; LY-353381; SCHEMBL285277; CHEMBL226267; BDBM19442; DTXSID10171255; ZINC1544683; AC1L4522; AN-538; AKOS030631785; SB19713; KB-05502; FT-0751607; 124708-EP2295426A1; 124708-EP2295427A1; 124708-EP2292592A1; 124708-EP2292576A2; Benzo(b)thiophene-6-ol, 2-(4-methoxyphenyl)-3-(4-(2-(1-piperidinyl)
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MOA Inhibitor
Activity EC50 = 0.2 nM
External Link
 Compound Name Lasofoxifene Approved [31]
Synonyms
Oporia; 180916-16-9; rac-Lasofoxifene; CP 336156; Fablyn; UNII-337G83N988; (5R,6S)-6-phenyl-5-[4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,6,7,8-tetrahydronaphthalen-2-ol; CHEMBL328190; 337G83N988; (-)-cis-5,6,7,8-Tetrahydro-6-phenyl-5-(p-(2-(1-pyrrolidinyl)ethoxy)phenyl)-2-naphthol; 180915-78-0; CP-336,156; LASOFOXIFENE HCL; Lasofoxifene [INN:BAN]; AC1L50OI; SCHEMBL26815; GTPL7542; CTK8F1062; BDBM20606; DTXSID50171037; GXESHMAMLJKROZ-IAPPQJPRSA-N; ZINC3918428; BCP03626; AKOS030241621; AN-3516; BCP9000842; DB06202; Lasofoxifene [INN]; Cis-1R-(4'-pyrrolidinoethoxyphenyl)-2S-phenyl-6-hydroxy-1,2,3,4-tetrahydronaphthalene, tartrate salt; AZD9639
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MOA Modulator
Activity IC50 = 1.3 nM
External Link
 Compound Name Estrogen Approved [32]
MOA Agonist
External Link
 Compound Name Synthetic conjugated estrogen Phase 3 [33]
Synonyms
Bijuva; Bithena; DR-2041; SCE-A Vaginal Cream; Synthetic conjugated estrogen (cream, vulvovaginal atrophy); Synthetic conjugated estrogen (cream, vulvovaginal atrophy), Teva
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MOA Modulator
External Link
 Compound Name Trimegestone/ethinyl estradiol Phase 3 [34]
MOA Modulator
External Link
 Compound Name TZTX-001 Phase 3 [35]
Synonyms
Teverelix LA; TX 12-001-HR
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MOA Modulator
External Link
 Compound Name Acolbifene Phase 3 [36]
Synonyms
EM-652; 182167-02-8; UNII-815LJ9X0D1; 815LJ9X0D1; EM 652; Acolbifene [INN:BAN]; SCH 57068; AC1L4EAA; SCHEMBL406183; CHEMBL68055; CTK4F5320; SCH-57068; HY-16023A; ( )-(2S)-3-(4-Hydroxyphenyl)-4-methyl-2-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2H-1-benzopyran-7-ol; CS-0007143; (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol; (S)-3-(4-hydroxyphenyl)-4-methyl-2-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-2H-chromen-7-ol
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MOA Modulator
External Link
 Compound Name NE3107 Phase 3 [37]
MOA Inhibitor
External Link
 Compound Name Giredestrant Phase 3 [38]
Synonyms
(1R,3R)-1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)-3-AZETIDINYL)AMINO)PHENYL)-.BETA.,.BETA.-DIFLUORO-1,3,4,9-TETRAHYDRO-3-METHYL-2H-PYRIDO(3,4-B)INDOLE-2-PROPANOL; 1953133-47-5; 28P3DU6DB3; 2H-PYRIDO(3,4-B)INDOLE-2-PROPANOL, 1-(2,6-DIFLUORO-4-((1-(3-FLUOROPROPYL)-3-AZETIDINYL)AMINO)PHENYL)-.BETA.,.BETA.-DIFLUORO-1,3,4,9-TETRAHYDRO-3-METHYL-, (1R,3R)-; 2H-Pyrido(3,4-b)indole-2-propanol, 1-(2,6-difluoro-4-((1-(3-fluoropropyl)-3-azetidinyl)amino)phenyl)-beta,beta-difluoro-1,3,4,9-tetrahydro-3-methyl-, (1R,3R)-; 3-((1R,3R)-1-(2,6-Difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido(3,4-b)indol-2-yl)-2,2-difluoropropan-1-ol; 3-((1R,3R)-1-(2,6-Difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol; 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-2(9H)-yl)-2,2-difluoropropan-1-ol; 3-[(1R,3R)-1-(2,6-difluoro-4-{[1-(3-fluoropropyl)azetidin-3-yl]amino}phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol; 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoropropan-1-ol; 3-[(1R,3R)-1-[2,6-difluoro-4-[[1-(3-fluoropropyl)azetidin-3-yl]amino]phenyl]-3-methyl-1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl]-2,2-difluoro-propan-1-ol; AC-37111; AKOS040733254; AT22918; BDBM50572808; CHEMBL4650316; compound 35 [PMID: 34251202]; CS-0116370; EX-A3541; GDC9545; GDC-9545; Giredestrant; Giredestrant [INN]; Giredestrant [USAN:INN]; Giredestrant [USAN]; GIREDESTRANT [WHO-DD]; GTPL12715; HY-109176; MS-29682; NSC827275; NSC-827275; RG6171; RG-6171; RO7197597; RO-7197597; SCHEMBL17839430; UNII-28P3DU6DB3; WHO 11226; ZNM
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MOA Degrader
External Link
 Compound Name Imlunestrant Phase 3 [39]
Synonyms
(5R)-5-(4-(2-(3-(fluoromethyl)azetidin-1-yl)ethoxy)phenyl)-8-(trifluoromethyl)-5H-(1)benzopyrano(4,3-c)quinolin-2-ol; (5R)-5-[4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl]-8-(trifluoromethyl)-5H-chromeno[4,3-c]quinolin-2-ol; 2408840-26-4; 5H-(1)Benzopyrano(4,3-c)quinolin-2-ol, 5-(4-(2-(3-(fluoromethyl)-1-azetidinyl)ethoxy)phenyl)-8-(trifluoromethyl)-, (5R)-; 9CXQ3PF69U; BDBM443429; CHEMBL5095183; CS-0376104; EX-A6123; Example 1B {WO2020014435A1]; GLXC-26209; GTPL12896; HY-145572; Imlunestrant; IMLUNESTRANT [INN]; Imlunestrant [USAN]; Ly 3484356; LY3484356; LY-3484356; SCHEMBL22002569; UNII-9CXQ3PF69U; US10654866, Example 1A; UVBQMXOKKDCBJN-MUUNZHRXSA-N; WHO 12039
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MOA Degrader
External Link
 Compound Name NPC-01 Phase 3 [40]
Synonyms
LEP pill; Low dose estrogen progestin pill (dysmenorrhea), Nobelpharma
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MOA Modulator
External Link
 Compound Name Premarin/Pravachol Phase 3 [41]
Synonyms
Estrogen/pravastatin
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MOA Modulator
External Link
 Compound Name ARN-810 Phase 2 [42]
MOA Modulator
Activity Ki = 0.37 nM
External Link
 Compound Name SR 16234 Phase 2 [43]
Synonyms
229634-98-4; TS 108; TAS-108; SR16234; UNII-9B29N23K7E; 9B29N23K7E; SCHEMBL2836841; DTXSID30177512; C33H47NO3.C6H8O7; (7alpha)-21-(4-((Diethylamino)methyl)-2-methoxyphenoxy)-7-methyl-19-norpregna-1,3,5(10)-trien-3-ol 2-hydroxy-1,2,3-propanetricarboxylate; Y1847; 354808-47-2; (7R,8S,9S,13R,14S,17R)-17-(2-(4-((Diethylamino)methyl)-2-methoxyphenoxy)ethyl)-7,13-dimethyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-ol 2-hydroxypropane-1,2,3-tricarboxylate
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MOA Modulator
External Link
 Compound Name Afimoxifene Phase 2 [4]
Synonyms
4-Hydroxytamoxifen; (Z)-4-Hydroxytamoxifen; Hydroxytamoxifen; 4-Monohydroxytamoxifen; Tamogel; 68047-06-3; trans-4-Hydroxytamoxifen; Ici 79280; 68392-35-8; 65213-48-1; 4-OH-TAM; (Z)-4-(1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol; Z-4-hydroxytamoxifen; UNII-95K54647BZ; CHEMBL489; ICI 79,280; TAMOXIFEN, 4-HYDROXY-, (Z)-; BRN 4910749; (E/Z)-4-Hydroxy Tamoxifen; MLS000069742; C26H29NO2; CHEBI:44616; 95K54647BZ; SMR000058939; 4-(1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol
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MOA Modulator
Activity IC50 = 0.79 nM
External Link
 Compound Name GTx-758 Phase 2 [44]
MOA Modulator
External Link
 Compound Name ICARITIN Phase 2 [45]
Synonyms
118525-40-9; UNII-UFE666UELY; UFE666UELY; CHEMBL498485; 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one; 3,5,7-Trihydroxy-2-(4-methoxyphenyl)-8-(3-methyl-2-buten-1-yl)-4H-1-benzopyran-4-one; Icartin; Anhydroicaritin; AC1NSXIV; Icaritin(Anhydroicaritin); MLS006010055; BIDD:ER0021; SCHEMBL4223542; Icaritin, > DTXSID00152154; MolPort-020-006-012; TUUXBSASAQJECY-UHFFFAOYSA-N; HY-N0678; ZINC14762797; BDBM50272527; AKOS015896858; CS-3679; DB12672; NCGC00345813-01; AK168251; SMR004701218
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MOA Modulator
External Link
 Compound Name Estetrol Phase 2 [46]
Synonyms
Estetrol (oral, contraception/hormone deficiency/osteoporosis/cardiovascular disease/autoimmune disease/breast cancer/prostate cancer); Estetrol (oral, contraception/hormone deficiency/osteoporosis/cardiovascular disease/autoimmune disease/breast cancer/prostate cancer), Pantarhei; Estrogen receptor modulator (oral, contraception/hormone deficiency/autoimmune disease/breast cancer/prostate cancer/osteoporosis/cardiovascular disease), Pantarhei
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MOA Modulator
External Link
 Compound Name Endoxifen Phase 2 [4]
Synonyms
Endoxifen (topical formulation, cancer); Endoxifen (topical formulation, cancer), Jina Pharmaceuticals; Tamoxifen metabolite (topical formulation, cancer), Jina Pharmaceuticals
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MOA Modulator
External Link
 Compound Name AZD9833 Phase 2 [47]
Synonyms
AZD-9833; UNII-JUP57A8EPZ; JUP57A8EPZ; 2222844-89-3; Camizestrant; Camizestrant [USAN]; SCHEMBL20089710; NSC828717; WHO 11592; NSC-828717; HY-136255; AZ14066724; CS-0121043; 3-Pyridinamine, N-(1-(3-fluoropropyl)-3-azetidinyl)-6-((6S,8R)-6,7,8,9-tetrahydro-8-methyl-7-(2,2,2-trifluoroethyl)-3H-pyrazolo(4,3-F)isoquinolin-6-yl)-
    Click to Show/Hide
MOA Degrader
External Link
 Compound Name H3B-6545 Phase 1/2 [48]
Synonyms
JPFTZIJTXCHJNE-HMOQVRKWSA-N; SCHEMBL18261010; HY-112596; CS-0047714; (2e)-N,N-dimethyl-4-{[2-({5-[(1z)-4,4,4-trifluoro-1-(3-fluoro-1h-indazol-5-yl)-2-phenylbut-1-en-1-yl]pyridin-2-yl}oxy)ethyl]amino}but-2-enamide
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MOA Antagonist
External Link
 Compound Name ZN-c5 Phase 1/2 [49]
MOA Degrader
External Link
 Compound Name OP-1250 Phase 1/2 [50]
MOA Antagonist
External Link
 Compound Name CC-8490 Phase 1 [51]
MOA Modulator
External Link
 Compound Name CHF-4227 Phase 1 [52]
Synonyms
CHF-3316; CHF-4056; SERMs, Chiesi; Selective estrogen receptor modulators, Chiesi; CHF-3316.01
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MOA Modulator
External Link
 Compound Name ATD transdermal gel Phase 1 [4]
MOA Inhibitor
External Link
 Compound Name D-0502 Phase 1 [53]
MOA Degrader
External Link
 Compound Name TTC-352 Phase 1 [48]
MOA Agonist
External Link
 Compound Name AZD9496 Phase 1 [48]
Synonyms
DFBDRVGWBHBJNR-BBNFHIFMSA-N; 1639042-08-2; UNII-DA9P7LN909; DA9P7LN909; CHEMBL3623004; AZD-9496; (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid; (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido(3,4-b)indol-1-yl)phenyl)acrylic acid; SCHEMBL16266273; SCHEMBL16266275; MolPort-044-560-384; EX-A1326; s8372; BDBM50125052; ZINC219669733; AKOS030526632; AC-29011; HY-12870; Selective estrogen
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MOA Antagonist
Activity IC50 = 0.138 nM
External Link
 Compound Name G1T-48 Phase 1 [54]
MOA Degrader
External Link
 Compound Name LY3484356 Phase 1 [55]
MOA Degrader
External Link
 Compound Name AC0682 Phase 1 [56]
MOA Degrader
External Link
 Compound Name SCO-120 Phase 1 [57]
MOA Degrader
External Link
 Compound Name TTC-352 Phase 1 [58]
Synonyms
Sherpa TTC-352; UNII-65ILH3Y0MI; 65ILH3Y0MI; CHEMBL3763743; 1607819-68-0; 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)-1-benzothiophene-6-ol; 3-(4-Fluorophenyl)-2-(4-hydroxyphenoxy)-benzo[b]thiophene-6-ol; SCHEMBL15658409; BDBM50145856; J3.603.123I; 2-(4-Hydroxyphenoxy)-3-(4-fluorophenyl)benzo[b]thiophene-6-ol; 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)-1-benzothiophen-6-ol; 3-(4-Fluorophenyl)-2-(4-hydroxyphenoxy)benzo(b)thiophene-6-ol; 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)benzo[b]thiophen-6-ol; 3-(4-fluorophenyl)-2-(4-hydroxyphenoxyl)benzo[b]thiophen-6-ol; Selective human estrogen-receptor alpha partial agonist TTC-352; Benzo(b)thiophene-6-ol, 3-(4-fluorophenyl)-2-(4-hydroxyphenoxy)-; V9J
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MOA Agonist
External Link
 Compound Name Chlorotrianisene Withdrawn from market [59]
Synonyms
Anisene; Chloortrianisestrol; Chlorestrolo; Chlorotrianisenum; Chlorotrianisestrol; Chlorotrianisine; Chlorotrianizen; Chlorotrisin; Chlortrianisen; Chlortrianisene; Chlortrianisenum; Chlortrianisestrol; Chlortrianisoestrolum; Chlortrianizen; Clorestrolo; Clorotrianisene; Clorotrianiseno; Clorotrisin; Hormonisene; Khlortrianizen; Merbentul; Metace; Rianil; TACE; Triagen; Trianisestrol; Chlorotrianisene [Nonsteroidal oestrogens]; Clorotrianisene [DCIT]; Chlorotrianisene (INN); Chlorotrianisene [BAN:INN]; Chlorotrianisene [INN:BAN]; Chlorotrianisenum [INN-Latin]; Clorotrianiseno [INN-Spanish]; TACE (TN); Tace (pharmaceutical); Tace-fn; Chlorotris(p-methoxyphenyl)ethylene; Tri-p-anisylchloroethylene; Tris(p-methoxyphenyl)chloroethylene; 1,1',1''-(1-Chloro-1-ethenyl-2-ylidene)-tris(4-methoxybenzene); 1,1',1''-(2-chloroethene-1,1,2-triyl)tris(4-methoxybenzene); 1,1',1''-(2-chloroethene-1,1,2-triyl)tris[4-(methyloxy)benzene]; 1-[1-chloro-2,2-bis(4-methoxyphenyl)ethenyl]-4-methoxybenzene
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MOA Binder
External Link
 Compound Name HEXESTROL Withdrawn from market [60]
Synonyms
Dihydrodiethylstilbestrol; Vitestrol; Hexoestrolum; Exestrol; 5635-50-7; Stilbestrol, dihydro-; 4,4'-(1,2-Diethylethylene)diphenol; 4,4'-(hexane-3,4-diyl)diphenol; Synoestrolum; Hexanestrol; Cycloestrol; Esestrolo [DCIT]; Phenol, 4,4'-(1,2-diethyl-1,2-ethanediyl)bis-; Hexestrolum [INN-Latin]; Hexane, 3,4-bis(4-hydroxyphenyl)-; EINECS 227-082-2; 3,4-Bis(p-hydroxyphenyl)hexane; Hormoestrol; Syntrogene; Synthovo; Phenol, 4,4'-(1,2-diethylethylene)di-; CHEBI:31669; PBBGSZCBWVPOOL-UHFFFAOYSA-N; Hexestrol [INN]
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MOA Inhibitor
External Link
 Compound Name BITHIONOL Withdrawn from market [61]
Synonyms
97-18-7; Actamer; Bithin; 2,2'-Thiobis(4,6-dichlorophenol); Lorothidol; Bitionol; Bithionol sulfide; Bisoxyphen; Bidiphen; Lorothiodol; Bitin; Nobacter; Bithionolate; Neopellis; Vancide BL; Usaf B-22; Bithional; Bithionolum; 2-Hydroxy-3,5-dichlorophenyl sulfide; TKhsd; Bis(2-hydroxy-3,5-dichlorophenyl) sulfide; Bis(3,5-dichloro-2-hydroxyphenyl) sulfide; 2,2'-sulfanediylbis(4,6-dichlorophenol); Caswell No. 852; Bitionol [INN-Spanish]; XL 7; Bithionolum [INN-Latin]; 2,2'-Dihydroxy-3,3',5,5'-tetrachlorodiphenyl sulfide
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MOA Inhibitor
External Link
 Compound Name IoGen Discontinued in Phase 3 [4]
Synonyms
Oral iodine-based therapy (fibrocystic breast disease), Symbollon; Oral iodine-based therapy (fibrocystic breast disease), Symbollon/Gardant
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MOA Modulator
External Link
 Compound Name Miproxifene Discontinued in Phase 3 [62]
Synonyms
Miproxifene phosphate; TAT-59
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MOA Modulator
External Link
 Compound Name Idoxifene Discontinued in Phase 3 [63]
Synonyms
CB-7432; SB-223030
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MOA Modulator
External Link
 Compound Name EM-800 Discontinued in Phase 3 [64]
Synonyms
UNII-XCR716LECP; XCR716LECP; 182167-03-9; Em 800; SCH 57050; BIDD:ER0061; SCHEMBL1821303; CHEMBL308234; 189021-25-8; (s)-(+)-4-[7-(2,2-dimethyl-1-oxopropoxy)-4-meth-yl-2-[4-[2-(1-piperidinyl)-ethoxy]phenyl]-2h-1-benzopyran-3-yl]-phenyl 2,2-dimethylpropanoate
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MOA Antagonist
External Link
 Compound Name NP-50301 Discontinued in Phase 2 [65]
Synonyms
IDESTRIN; Estrogen ester (eyedrop, dry eye syndrome), Nascent
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MOA Modulator
External Link
 Compound Name SR-90067 Discontinued in Phase 2 [66]
Synonyms
Estradiol spray (menopausis), Sanofi-Synthelabo
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MOA Agonist
External Link
 Compound Name Panomifene Discontinued in Phase 2 [67]
Synonyms
Panomifine; EGIS-5650
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MOA Modulator
External Link
 Compound Name SERM-3339 Discontinued in Phase 2 [68]
Synonyms
HMR-3339; SERM compound, Aventis
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MOA Modulator
External Link
 Compound Name Droloxifene Discontinued in Phase 2 [69]
Synonyms
E-droloxifene; FK-435; K-060; K-060E; RP-60850; K-21.060E; 3-hydroxytamoxifen
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MOA Modulator
External Link
 Compound Name ERA-923 Discontinued in Phase 2 [70]
Synonyms
Pipendoxifene; UNII-TPC5Q8496G; 198480-55-6; CHEMBL44426; TPC5Q8496G; Pipendoxifene [INN]; ERA 923; AC1O5FKF; SCHEMBL134583; JICOGKJOQXTAIP-UHFFFAOYSA-N; ZINC602799; BDBM50099587; AKOS030631784; DB05414; 2-(4-hydroxyphenyl)-3-methyl-1-(4-(2-piperidin-1-yl-ethoxy)-benzyl)-1H-indol-5-ol; US8815934, No 97; US8815934, No 107; 2-(p-Hydroxyphenyl)-3-methyl-1-(p-(2-piperidinoethoxy)benzyl)indol-5-ol; 2-(4-hydroxyphenyl)-3-methyl-1-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]indol-5-ol
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MOA Inhibitor
Activity EC50 = 0.1 nM
External Link
 Compound Name HRT Discontinued in Phase 1 [71]
Synonyms
HRT (oral); IP-1162; IP-1163; IP-1164; HRT (oral), Shire
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MOA Agonist
External Link
 Compound Name MX-4509 Discontinued in Phase 1 [72]
Synonyms
17alpha-Estradiol; 57-91-0; Alfatradiol; Epiestradiol; 17-alpha-Estradiol; 3,17-Dihydroxyestratriene; 17a-estradiol; Estradiol-17alpha; Epiestrol; 17-Epiestradiol; Estra-1,3,5(10)-triene-3,17alpha-diol; 17alpha estradiol; NSC 20293; UNII-3VQ38D63M7; Alfatradiol [INN]; Oestradiol-17alpha; 17alpha-Oestradiol; Estradiol, 17alpha-; CHEBI:17160; VOXZDWNPVJITMN-SFFUCWETSA-N; 3VQ38D63M7; 17-epi-Estradiol; Alfatradiol (INN); Oestradiol-17-alpha; MITO-4509; Parkinsons therapeutics, MitoKor; Drug screening (Parkinsons), MitoKor; Estrogen analogs (Parkinsons), Mitokor
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MOA Inhibitor
Activity EC50 = 1.5 nM
External Link
 Compound Name HE2100 Discontinued in Phase 1 [73]
Synonyms
Androstenediol; Hermaphrodiol; 5-Androstenediol; Androst-5-enediol; 521-17-5; Androst-5-ene-3beta,17beta-diol; Neumune; 3beta,17beta-Dihydroxyandrost-5-ene; delta(sup 5)-Androstenediol; Androstenediol [JAN]; UNII-95PS51EMXY; Androst-5-enediol (VAN); (3beta,17beta)-androst-5-ene-3,17-diol; 5-AED; 3beta,17beta-Dihydroxy-5-androstene; androst-5-en-3beta,17beta-diol; EINECS 208-306-8; NSC 12163; 95PS51EMXY; ANDROST-5-ENE-3-beta,17-beta-DIOL; CHEMBL440283; CHEBI:2710; (3-beta,17-beta)-Androst-5-ene-3,17-diol; delta(sup
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MOA Inhibitor
Activity EC50 = 26 nM
External Link
 Compound Name BN-AO-014 Preclinical [74]
Synonyms
Selective estrogen receptor modulators (genitourinary atrophy); Selective estrogen receptor modulators (genitourinary atrophy), Bionovo
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MOA Modulator
External Link
 Compound Name BN-OD-026 Preclinical [75]
Synonyms
Selective estrogen receptor modulators (colon/breast cancer); BN-RP-006-OHA; Selective estrogen receptor modulators (colon/breast cancer), Bionovo
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MOA Modulator
External Link
 Compound Name BN-DF-037 Preclinical [74]
Synonyms
Selective estrogen receptor modulators (osteoporosis); BN-EU-036; Selective estrogen receptor modulators (osteoporosis), Bionovo; BN-AM-008-XG; BN-PC-049-BK
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MOA Modulator
External Link
 Compound Name BN-AA-003-NY Preclinical [74]
Synonyms
Selective estrogen receptor modulators (menopause symptoms); Selective estrogen receptor modulators (menopause symptoms), Bionovo
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MOA Modulator
External Link
 Compound Name BN-CB-045 Preclinical [74]
Synonyms
Selective estrogen receptor modulators (female sexual dysfunction); BN-ES-022; Selective estrogen receptor modulators (female sexual dysfunction), Bionovo
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MOA Modulator
External Link
 Compound Name BN-GU-005-DHP Preclinical [74]
Synonyms
Selective estrogen receptor modulators (arthralgia); Selective estrogen receptor modulators (arthralgia), Bionovo
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MOA Modulator
External Link
 Compound Name Tamoxifen methyl iodide Terminated [76]
Synonyms
Tamoxifen methiodide; CHEMBL1213783; MLS002701640; AC1MHWIV; N-Methyltamoxifen iodide; 107256-99-5; PXJJOGITBQXZEQ-JTHROIFXSA-M; NSC630510; NSC-630510; (Z)-2-(4-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N,N-trimethylethanaminium iodide; 2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]ethyl-trimethylazanium iodide; Ethanaminium, 2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-N,N,N-trimethyl-, iodide, (Z)-
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MOA Inhibitor
Activity Ki = 46.29 nM
External Link
 Compound Name Zindoxifene Terminated [77]
Synonyms
D-16726
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MOA Modulator
External Link
 Compound Name ICI-164384 Terminated [78]
Synonyms
Ici 164384; 98007-99-9; UNII-84LT43726C; ICI M164384; ICI 164,384; CHEMBL1222035; N-n-Butyl-N-methyl-11-(3,17beta-dihydroxyestra-1,3,5(10)-trien-7alpha-yl)undecanamide; 84LT43726C; N-BUTYL-11-[(7R,8R,9S,13S,14S,17S)-3,17-DIHYDROXY-13-METHYL-7,8,9,11,12,13,14,15,16,17-DECAHYDRO-6H-CYCLOPENTA[A]PHENANTHREN-7-YL]-N-METHYLUNDECANAMIDE; Estra-1,3,5(10)-triene-7-undecanamide, N-butyl-3,17-dihydroxy-N-methyl-, (7alpha,17beta)-; AOE
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MOA Inhibitor
Activity IC50 = 50 nM
External Link
 Compound Name ZK-119010 Terminated [79]
Synonyms
ZK 119010; UNII-80Z22M837F; CHEMBL46903; 80Z22M837F; 127451-69-8; AC1L2YAG; 2-(4-Hydroxyphenyl)-3-methyl-1-(6-(1-pyrrolidinyl)hexyl)indol-5-ol; SCHEMBL9028173; DTXSID50155574; zk119010; BDBM50099586; 1H-Indol-5-ol, 2-(4-hydroxyphenyl)-3-methyl-1-(6-(1-pyrrolidinyl)hexyl)-; LS-191850; 2-(4-hydroxyphenyl)-3-methyl-1-(6-pyrrolidin-1-ylhexyl)indol-5-ol
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MOA Inhibitor
Activity IC50 = 25 nM
External Link
 Compound Name LY-117018 Terminated [80]
Synonyms
Lilly 117018; LY 117018; 63676-25-5; CHEBI:90187; LY 139478; [6-hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(pyrrolidin-1-yl)ethoxy]phenyl}methanone; 6-Hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl 4-(2-(1-pyrrolidinyl)ethoxy) phenyl ketone; Methanone, (6-hydroxy-2-(4-hydroxyphenyl)benzo(b)thien-3-yl)(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-; PHENETHIPYLONE; 6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl 4-[2-(1-pyrrolidinyl)ethoxy] phenyl ketone; LY117018; AC1L2XRN; AC1Q5D9H; CHEMBL10030
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name JNJ-17148066 Investigative [81]
Synonyms
CHEMBL1088485; SCHEMBL14277842; BDBM50310388
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 11 nM
External Link
 Compound Name N-benzyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL203860
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 242 nM
External Link
 Compound Name 2-AMINO-1-METHYL-6-PHENYLIMIDAZO[4,5-B]PYRIDINE Investigative [83]
Synonyms
PhIP; 105650-23-5; 1-methyl-6-phenyl-1H-imidazo[4,5-b]pyridin-2-amine; 2-Amino-1-methyl-6-phenylimidazo(4,5-b)pyridine; UNII-909C6UN66T; CHEBI:76290; 909C6UN66T; 1-Methyl-6-phenyl-1H-imidazo(4,5-b)pyridin-2-amine; PIQ; 2-AMINO-1-METHYL-6-PHENYL-IMIDAZO [4,5-b] PYRIDINE; 1H-Imidazo(4,5-b)pyridin-2-amine, 1-methyl-6-phenyl- (9CI); CCRIS 2954; HSDB 7768; BRN 5951264; ACMC-1BRGI; AC1Q4WMI; (3H)PhIP; AC1L1BO3; SCHEMBL151718; CHEMBL1213271; DTXSID3037628; CTK0I0185
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MOA Inhibitor
External Link
 Compound Name SNG-8006 Investigative [4]
Synonyms
Estrogen receptor alpha-36 antagonist (osteoporosis), Shenogen Pharma
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MOA Antagonist
External Link
 Compound Name N-cyclohexyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL382873
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MOA Inhibitor
Activity EC50 = 534 nM
External Link
 Compound Name 3-CHLORO-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Investigative [83]
Synonyms
848142-62-1; 3-chloro-2-(4-hydroxyphenyl)indazol-5-ol; CHEMBL180071; CTK2I5101; DTXSID40463812; Indazole-Cl, > ZINC13609473; AKOS030536245; DB07708; 2-(p-Hydroxyphenyl)-3-chloro-2H-indazole-5-ol; 2H-Indazol-5-ol, 3-chloro-2-(4-hydroxyphenyl)-
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MOA Inhibitor
External Link
 Compound Name 2,4-diisobutylamino-6-isopentylpyrimidine Investigative [84]
Synonyms
CHEMBL347927; ZINC13559143; BDBM50138886
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MOA Inhibitor
Activity Ki = 2800 nM
External Link
 Compound Name JNJ-26529152 Investigative [81]
Synonyms
CHEMBL1088483; BDBM50310372
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MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name SNG-8033 Investigative [4]
Synonyms
Estrogen receptor alpha 36 inhibitor (leukemia), Shenogen Pharma
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MOA Inhibitor
External Link
 Compound Name 2,4-Dibenzylamino-6-isopentylpyrimidine Investigative [84]
Synonyms
CHEMBL494121
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MOA Inhibitor
Activity Ki = 4100 nM
External Link
 Compound Name SNG-8023 Investigative [4]
Synonyms
Estrogen receptor alpha 36 inhibitor (breast cancer), Shenogen Pharma; Monoclonal antibody (breast cancer), Shenogen Pharma
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External Link
 Compound Name LTERHKILHRLLQEGSPSD Investigative [85]
MOA Inhibitor
External Link
 Compound Name GW7604 Investigative [86]
MOA Antagonist
Activity EC50 = 1.7 nM
External Link
 Compound Name 4-benzyl-2,6-diisobutylamino-pyrimidine Investigative [84]
Synonyms
CHEMBL493703
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MOA Inhibitor
Activity Ki > 7300 nM
External Link
 Compound Name 7-Cyclopentyloxy-3-(4-hydroxyphenyl)chromen-4-one Investigative [87]
Synonyms
SCHEMBL1700973
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MOA Inhibitor
External Link
 Compound Name N,N,N-Triisobutyl-pyrimidine-2,4,6-triamine Investigative [84]
Synonyms
CHEMBL494706; BDBM50253380
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MOA Inhibitor
Activity IC50 = 2400 nM
External Link
 Compound Name Carboron Cluster with phenol Investigative [88]
MOA Inhibitor
External Link
 Compound Name 4-[1-(4-hydroxyphenyl)-2-phenylvinyl]phenol Investigative [89]
Synonyms
CHEMBL415864; 1,1-Bis(4-hydroxyphenyl)-2-phenylethylene; 4,4'-(2-Phenylethene-1,1-Diyl)diphenol; 66422-18-2; Bhpe-1,1; SCHEMBL641985; AC1MI565; CTK5C4724; 4-(1,2-diphenyl-vinyl)-phenol; BDBM50023749; ZINC13492380; Phenol, 4,4'-(phenylethenylidene)bis-; 1,1-bis(4-hydroxyphenyl)-2-phenylethene; 4-[1-(4-hydroxyphenyl)-2-phenylethenyl]phenol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 150 nM
External Link
 Compound Name MPrP Investigative [90]
MOA Inhibitor
Activity IC50 = 20 nM
External Link
 Compound Name Tamoxifen isopropyl bromide Investigative [76]
MOA Inhibitor
Activity Ki = 25.43 nM
External Link
 Compound Name 17-METHYL-17-ALPHA-DIHYDROEQUILENIN Investigative [83]
Synonyms
2b1z; ZINC5048688; DB06871; 17beta-Methyl-17alpha-dihydroequilenin; 17M; (13alpha,17beta)-17-methylestra-1(10),2,4,6,8-pentaene-3,17-diol
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MOA Inhibitor
External Link
 Compound Name 4-hydroxy-N-neopentyl-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL203515
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MOA Inhibitor
Activity IC50 = 1371 nM
External Link
 Compound Name SNG-163 Investigative [4]
Synonyms
SGIC-163; ER-a36 inhibitor (cancer), Shenogen
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MOA Inhibitor
External Link
 Compound Name GSK-5182 Investigative [91]
Synonyms
GSK5182; GSK 5182; 877387-37-6; (Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL; TXF; 4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol; 2ewp; AC1OA9V8; GTPL8908; CHEMBL201013; SCHEMBL20534177; BDBM22435; AOB1629; EX-A2580; ZINC14978677; 4-hydroxytamoxifen (4-OHT) analog, 15; 4-[(z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-hydroxy-2-phenylpent-1-enyl]phenol; 4-[(Z)-1-[4-(2-dimethylaminoethyloxy)phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
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MOA Inhibitor
Activity IC50 = 320 nM
External Link
 Compound Name N-ethyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL379234; Enamine_001944; Oprea1_552384; AC1M697W; SCHEMBL10904389; MolPort-004-000-970; HMS1399I08; ZINC3251814; BDBM50177761; AKOS008967166; MCULE-9434872926; N-ethyl-4-hydroxy-N-phenylbenzene-1-sulfonamide; Z56821525
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MOA Inhibitor
Activity IC50 = 404 nM
External Link
 Compound Name JNJ-19398990 Investigative [81]
Synonyms
CHEMBL1085429; BDBM50310424
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MOA Inhibitor
Activity IC50 = 64 nM
External Link
 Compound Name 4-(1-benzyl-7-chloro-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity EC50 = 390 nM
External Link
 Compound Name 3-ETHYL-2-(4-HYDROXYPHENYL)-2H-INDAZOL-5-OL Investigative [83]
Synonyms
CHEMBL180517
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MOA Inhibitor
External Link
 Compound Name N-allyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL426849
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MOA Inhibitor
Activity IC50 = 235 nM
External Link
 Compound Name 4-(7-chloro-1-propyl-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity IC50 = 52 nM
External Link
 Compound Name Tamoxifen ethyl bromide Investigative [76]
MOA Inhibitor
Activity Ki = 13.66 nM
External Link
 Compound Name 6-butyl-2,4-dipropylaminopyrimidine Investigative [84]
Synonyms
CHEMBL352024; BDBM50138883; ZINC13559144
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MOA Inhibitor
Activity IC50 = 13000 nM
External Link
 Compound Name RG6046 Investigative [93]
MOA Modulator
External Link
 Compound Name STX Investigative [4]
Synonyms
Selective estrogen receptor modulator (menopause-associated symptoms), Oregon Health & Science University
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MOA Modulator
External Link
 Compound Name 4-(1-cyclopentyl-7-fluoro-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity IC50 = 18 nM
External Link
 Compound Name 3-(4-Hydroxyphenyl)-7-isobutoxychromen-4-one Investigative [87]
Synonyms
SCHEMBL1701136
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MOA Inhibitor
External Link
 Compound Name SERMs Investigative [4]
Synonyms
SERMs (cancer); SERMs (cancer), CEAMED; Selective estrogen receptor modulators (cancer), CEAMAD
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MOA Modulator
External Link
 Compound Name 6-ethyl-2,4-diisobutylaminopyrimidine Investigative [84]
Synonyms
CHEMBL484451
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MOA Inhibitor
Activity IC50 = 7300 nM
External Link
 Compound Name 4-(7-chloro-1-cyclohexyl-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity IC50 = 37 nM
External Link
 Compound Name Org-37663 Investigative [94]
MOA Modulator
External Link
 Compound Name 4-hydroxy-N-isopropyl-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL204664
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MOA Inhibitor
Activity EC50 = 1985 nM
External Link
 Compound Name 4-(7-methyl-1-propyl-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity IC50 = 40 nM
External Link
 Compound Name 4-(6-HYDROXY-1H-INDAZOL-3-YL)BENZENE-1,3-DIOL Investigative [83]
MOA Inhibitor
Activity IC50 = 48 nM
External Link
 Compound Name 4-[1-(4-hydroxyphenyl)-2-phenylbut-1-enyl]phenol Investigative [89]
Synonyms
91221-46-4; 1,1-Bis(4-hydroxyphenyl)-2-phenylbut-1-ene; 1,1-Bis(4-hydroxyphenyl)-2-phenyl-1-butene; CHEMBL149791; 4,4'-(2-phenylbut-1-ene-1,1-diyl)diphenol; Tamoxifen bis-phenol; 1,1-Bhpe; Tamoxifenbisphenol; AC1L1YAG; SCHEMBL639225; CTK5G9076; DTXSID50238452; BPKSDMHGDYTXLI-UHFFFAOYSA-N; ZINC1849484; BDBM50121317; AKOS030254689; KB-09832; 4,4'-(2-Phenyl-1-butenylidene)bisphenol; B5114; FT-0663304; Phenol, 4,4'-(2-phenyl-1-butenylidene)bis-
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MOA Inhibitor
Activity EC50 = 0.015 nM
External Link
 Compound Name 4-hydroxy-N-phenyl-N-propylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL205070
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MOA Inhibitor
Activity EC50 = 1430 nM
External Link
 Compound Name N-butyl-4-hydroxy-N-phenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL203810; BDBM50177754
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MOA Inhibitor
Activity EC50 = 705 nM
External Link
 Compound Name 3-(4-Hydroxyphenyl)-7-isopropoxychromen-4-one Investigative [87]
Synonyms
CHEMBL115109; 97846-18-9; 4H-1-Benzopyran-4-one, 3-(4-hydroxyphenyl)-7-(1-methylethoxy)-; ACMC-20m1ro; SCHEMBL1701110; CTK3G8070; DTXSID70440494; 7-Isopropoxy-4'-hydroxyisoflavone; BDBM50104874; ZINC13864225; AKOS030553087; 3-(4-Hydroxy-phenyl)-7-isopropoxy-chromen-4-one
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MOA Inhibitor
External Link
 Compound Name 4-[1-(4-hydroxyphenyl)-2-phenylpent-1-enyl]phenol Investigative [89]
Synonyms
CHEMBL357824; SCHEMBL19158863; BDBM50121321
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MOA Inhibitor
Activity IC50 = 50 nM
External Link
 Compound Name 4-(1-butyl-7-chloro-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity IC50 = 25 nM
External Link
 Compound Name 4-[1-(4-hydroxyphenyl)-2-phenylprop-1-enyl]phenol Investigative [89]
Synonyms
CHEMBL150461; SCHEMBL18882768
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MOA Inhibitor
Activity IC50 = 30 nM
External Link
 Compound Name Tamoxifen butyl bromide Investigative [76]
MOA Inhibitor
Activity Ki = 13.01 nM
External Link
 Compound Name Estriol E3 Investigative [95]
Synonyms
Estriol E3 (oral formulation, multiple sclerosis)
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MOA Modulator
External Link
 Compound Name 4-(1,2-Diphenyl-but-1-enyl)-phenol Investigative [89]
Synonyms
CHEMBL50995; 4-(1,2-Diphenyl-1-butenyl)phenol; Monophenoltamoxifen; 4-[(Z)-1,2-diphenylbut-1-enyl]phenol; AC1O4GB8; SCHEMBL5354173; BDBM50121319; ZINC29469549; 69967-80-2; LS-104581
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7 nM
External Link
 Compound Name 4-(7-chloro-1-cyclopentyl-1H-indazol-3-yl)phenol Investigative [92]
MOA Inhibitor
Activity EC50 = 98 nM
External Link
 Compound Name TSERaM Investigative [4]
Synonyms
TSERaM (menopausal weight gain); TSERaM (menopausal weight gain), Bionovo; Tissue-selective estrogen receptor alpha modulators (menopausal weight gain), Bionovo
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MOA Modulator
External Link
 Compound Name JNJ-26529126 Investigative [81]
Synonyms
CHEMBL1088343; BDBM50310407
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MOA Inhibitor
Activity IC50 = 76 nM
External Link
 Compound Name 5-hydroxy-2-phenylisoindoline-1,3-dione Investigative [96]
Synonyms
CHEMBL276030; 4-Hydroxy-N-phenylphthalimide; 3975-50-6; 5-hydroxy-2-phenyl-isoindole-1,3-dione; SCHEMBL8615277; CTK1B3719; DTXSID80445430; HCUAWJNHCZEMJS-UHFFFAOYSA-N; ZINC26020837; BDBM50088673; 5-hydroxy-2-phenyl-1H-isoindole-1,3(2H)-dione; 1H-Isoindole-1,3(2H)-dione, 5-hydroxy-2-phenyl-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2700 nM
External Link
 Compound Name 4-[1-(4-hydroxyphenyl)-2-phenylhex-1-enyl]phenol Investigative [89]
Synonyms
CHEMBL356693
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MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name methyl-piperidino-pyrazole Investigative [97]
MOA Antagonist
Activity Ki = 2.7 nM
External Link
 Compound Name propylpyrazoletriol Investigative [98]
MOA Agonist
Activity EC50 = 0.1 nM
External Link
 Compound Name 4-hydroxy-N,N-diphenylbenzenesulfonamide Investigative [82]
Synonyms
CHEMBL203061; SCHEMBL2114599
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MOA Inhibitor
Activity EC50 = 1543 nM
External Link
 Compound Name 3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol Investigative [99]
Synonyms
Metahexes trol; 3,3'-Hexestrol; Metahexestrol; 3,3'-Hes; 68266-24-0; meso-3,4-Bis(3'-hydroxyphenyl)hexane; BRN 3971661; NSC-297,170; meso-3,3'-(1,2-Diethylethylene)diphenol; NSC-297170; (R*,S*)-3,3'-(1,2-Diethyl-1,2-ethanediyl)bisphenol; Phenol, 3,3'-(1,2-diethyl-1,2-ethanediyl)bis-, (R*,S*)-; Phenol, 3,3'-((1R,2S)-1,2-diethyl-1,2-ethanediyl)bis-, rel-; UNII-DSF584X94B; DSF584X94B; NSC 297170; 3-[4-(3-hydroxyphenyl)hexan-3-yl]phenol; AC1L2OPY; 1,2-Diethyl-1,2-bis(3'-hydroxyphenyl)ethane; AC1Q79WV; CHEMBL18268; SCHEMBL5014485
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MOA Inhibitor
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-quinolin-6-ol Investigative [100]
MOA Inhibitor
Activity Ki = 310 nM
External Link
 Compound Name Nafoxidine Investigative [101]
Synonyms
1845-11-0; Nafoxidine [INN]; Nafoxidinum [INN-Latin]; Nafoxidina [INN-Spanish]; UNII-4RIY10WM82; U-11000A; BRN 1440873; CHEMBL28211; 4RIY10WM82; CHEBI:34881; NSC 70735; C29H31NO2; JEYWNNAZDLFBFF-UHFFFAOYSA-N; 1-(2-(p-(3,4-Dihydro-6-methoxy-2-phenyl-1-naphthyl)phenoxy)ethyl)pyrrolidine; Pyrrolidine, 1-(2-(4-(3,4-dihydro-6-methoxy-2-phenyl-1-naphthalenyl)phenoxy)ethyl)-; 1-[2-[4-(6-methoxy-2-phenyl-3,4-dihydronaphthalen-1-yl)phenoxy]ethyl]pyrrolidine; Pyrrolidine, 1-(2-(p-(3,4-dihydro-6-methoxy-2-phenyl-1-naphthyl
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name [1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Investigative [102]
MOA Inhibitor
External Link
 Compound Name 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 780 nM
External Link
 Compound Name 6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL206547; SCHEMBL6828050
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MOA Inhibitor
Activity IC50 = 101 nM
External Link
 Compound Name 4-(3-phenyl-1H-indol-2-yl)phenol Investigative [105]
Synonyms
CHEMBL199766; SCHEMBL7040440; BDBM50175418
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MOA Inhibitor
Activity IC50 = 8310 nM
External Link
 Compound Name 4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Investigative [106]
Synonyms
CHEMBL34709
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MOA Inhibitor
External Link
 Compound Name 4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL206582; SCHEMBL6924719
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MOA Inhibitor
Activity IC50 = 1030 nM
External Link
 Compound Name 7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 727 nM
External Link
 Compound Name 6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195389; SCHEMBL4077781; YIKDKHNOMWERET-UHFFFAOYSA-N; ZINC13645062; BDBM50168377
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MOA Inhibitor
Activity IC50 = 40 nM
External Link
 Compound Name 1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL Investigative [107]
Synonyms
CHEMBL364092; 1-chloro-6-(4-hydroxyphenyl)naphthalen-2-ol; 4NA; 1yy4; AC1O0UUG; 1-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol; SCHEMBL3933824; YHEHVRSGKUYDON-UHFFFAOYSA-N; ZINC13645009; BDBM50168323
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 91 nM
External Link
 Compound Name 5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 2765 nM
External Link
 Compound Name 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Investigative [103]
Synonyms
CHEMBL183367; SCHEMBL3933889; GLVGKXBQPYTMGJ-UHFFFAOYSA-N; ZINC3817709; BDBM50154056; 2-(6-hydroxynaphthalen-1-yl)benzo[d]oxazol-5-ol
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MOA Inhibitor
Activity IC50 = 153 nM
External Link
 Compound Name 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative [108]
Synonyms
CHEMBL24950; SCHEMBL6286195; BDBM50123206; 2-(3-hydroxyphenyl)-1,2''-spirobi[1H-indene]-5-ol
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MOA Inhibitor
Activity IC50 = 35 nM
External Link
 Compound Name 3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Investigative [109]
MOA Inhibitor
External Link
 Compound Name 2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL Investigative [103]
Synonyms
2-(4-Hydroxy-phenyl)-benzofuran-5-ol; 2-(4-hydroxyphenyl)-1-benzofuran-5-ol; CHEMBL367588; 52814-86-5; 2-(4-Hydroxyphenyl)benzofuran-5-ol; AC1LCVQT; 1u9e; SCHEMBL3922677; CTK1G1983; DTXSID60349669; SNNNDCMXZYWCCI-UHFFFAOYSA-N; ZINC3816519; BDBM50152627; SBB096959; AKOS030555876; DB07032; 2-(4-hydroxyphenyl)benzo[b]furan-5-ol; 5-Benzofuranol,
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MOA Inhibitor
Activity IC50 = 176 nM
External Link
 Compound Name COUMESTROL Investigative [110]
Synonyms
479-13-0; Cumoestrol; Cumoesterol; Cumostrol; Coumesterol; 3,9-Dihydroxy-6H-[1]benzofuro[3,2-c]chromen-6-one; 7,12-Dihydroxycoumestan; 3,9-Dihydroxycoumestan; UNII-V7NW98OB34; NSC 22842; CCRIS 7311; NSC22842; 6H-Benzofuro[3,2-c][1]benzopyran-6-one, 3,9-dihydroxy-; EINECS 207-525-6; BRN 0266702; CHEMBL30707; MLS000738006; V7NW98OB34; CHEBI:3908; ZZIALNLLNHEQPJ-UHFFFAOYSA-N; 3,9-Dihydroxy-6H-benzofuro(3,2-c)(1)benzopyran-6-one; 6H-Benzofuro(3,2-c)(1)benzopyran-6-one, 3,9-dihydroxy-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 11 nM
External Link
 Compound Name 4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Investigative [106]
Synonyms
CHEMBL38266
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MOA Inhibitor
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 775 nM
External Link
 Compound Name 5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
MOA Inhibitor
Activity IC50 = 632 nM
External Link
 Compound Name 2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 3800 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 1200 nM
External Link
 Compound Name 6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195311; SCHEMBL3932692; FNSIACDWDZGUHN-UHFFFAOYSA-N; BDBM50168347; ZINC13645053
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MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name DIHYDRORALOXIFENE Investigative [111]
Synonyms
CHEMBL14955; BDBM50217538; ZINC15919388
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MOA Inhibitor
External Link
 Compound Name 2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Investigative [108]
Synonyms
CHEMBL144431; SCHEMBL6283932; BDBM50123207; 2-(3-hydroxyphenyl)-1,2''-spirobi[1H-indene]-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 31 nM
External Link
 Compound Name 4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Investigative [106]
Synonyms
Ici-3188; 1,1,2-Tris(4-hydroxyphenyl)prop-1-ene; 68373-13-7; 4-[1,1-bis(4-hydroxyphenyl)prop-1-en-2-yl]phenol; Phenol, 4,4',4''-(1-methyl-1-ethenyl-2-ylidene)tris-; Ici 3188; AC1MJ4DX; CHEMBL38103; CTK2F3093; DTXSID20218504; AKOS030547870
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MOA Inhibitor
External Link
 Compound Name 7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 498 nM
External Link
 Compound Name 8-(2,2-dimethylpropyl)naringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 216 nM
External Link
 Compound Name 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 82 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Investigative [113]
Synonyms
CHEMBL361226; SCHEMBL3928011; KEWMBPCQWDVBAS-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 483 nM
External Link
 Compound Name 3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 3000 nM
External Link
 Compound Name R,R-THC Investigative [114]
Synonyms
(R,R)-THC; 138090-06-9; (R,R)-cis-Diethyl tetrahydro-2,8-chrysenediol; CHEMBL282489; 221368-54-3; (5R,11R)-5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol; (R,R)-5,11-DIETHYL-5,6,11,12-TETRAHYDRO-2,8-CHRYSENEDIOL; (R,R)-cis-Diethyltetrahydro-2,8-chrysenediol; (R,R)-5,11-CIS-DIETHYL-5,6,11,12-TETRAHYDROCHRYSENE-2,8-DIOL; Lopac-D-8690; AC1L9K5Y; Lopac0_000463; MLS002153151; BIDD:ER0043; GTPL2822; DTXSID6040749; SCHEMBL13352540; CTK4E8744; MolPort-003-941-174; HMS3268D03; HMS3261M08; HMS2232C18; ZINC3940885; Tox21_500463
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MOA Agonist
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 390 nM
External Link
 Compound Name 1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL192876; SCHEMBL4456831; YTFVBUBYMJJWQZ-UHFFFAOYSA-N; ZINC13645103; BDBM50168322
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 43 nM
External Link
 Compound Name 6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 464 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 2557 nM
External Link
 Compound Name 8-n-undecylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 1017 nM
External Link
 Compound Name 7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative [113]
Synonyms
CHEMBL184448; SCHEMBL3922992
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MOA Inhibitor
Activity IC50 = 6.8 nM
External Link
 Compound Name BROUSSONIN A Investigative [115]
Synonyms
73731-87-0; CHEMBL465879; Biooussonin A; AC1NST4K; 2-[3-(4-hydroxyphenyl)propyl]-5-methoxyphenol; SCHEMBL774802; MSNVBURPCQDLEP-UHFFFAOYSA-N; MolPort-019-937-120; BDBM50251012; ZINC13341109; MCULE-7164788732
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 1590 nM
External Link
 Compound Name 4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Investigative [106]
Synonyms
CHEMBL38222
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MOA Inhibitor
External Link
 Compound Name 7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 537 nM
External Link
 Compound Name WAY200070 Investigative [103]
Synonyms
WAY 200070; 440122-66-7; WAY-200070; CHEMBL188528; 7-BROMO-2-(4-HYDROXYPHENYL)-1,3-BENZOXAZOL-5-OL; 7-Bromo-2-(4-hydroxy-phenyl)-benzooxazol-5-ol; SCHEMBL3930187; ZINC9308; GTPL4052; CTK1D2551; DTXSID80432027; MolPort-023-276-777; BAAILVWEAXFTSF-UHFFFAOYSA-N; BCP28989; WAY-00005; BDBM50154088; ZINC138816775; AKOS024457585; CS-6398; HY-101271; RT-016254; B7386; 7-bromo-2-(4-hydroxyphenyl)-5-benzoxazolol; 5-Benzoxazolol, 7-bromo-2-(4-hydroxyphenyl)-; 7-bromo-2-(4-hydroxyphenyl)benzo[d]oxazol-5-ol; WAY-200070, &gt
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MOA Inhibitor
Activity IC50 = 155 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative [100]
Synonyms
CHEMBL191974; 6-(4-hydroxyphenyl)-2-naphthol; SCHEMBL2699234; SKPPZWVFPOQPOT-UHFFFAOYSA-N; ZINC13644983
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MOA Inhibitor
Activity IC50 = 211 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 1300 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL372030; SCHEMBL3927148; FGIUXCLAHODWKV-UHFFFAOYSA-N; BDBM50168320; ZINC13645024
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MOA Inhibitor
Activity IC50 = 282 nM
External Link
 Compound Name 8-methylnaringenin Investigative [112]
Synonyms
CHEMBL426154; MolPort-039-339-073; ZINC14814929; 5,7,4'-Trihydroxy-8-methylflavanone
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MOA Inhibitor
Activity IC50 = 5245 nM
External Link
 Compound Name 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 819 nM
External Link
 Compound Name 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 5000 nM
External Link
 Compound Name 8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL363367; SCHEMBL3923941; IVJIWGTXXHDRCU-UHFFFAOYSA-N; BDBM50168384; ZINC13645099
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MOA Inhibitor
Activity IC50 = 30 nM
External Link
 Compound Name 4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 6100 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 902 nM
External Link
 Compound Name 7-(4-Hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL191715; 7-(4-Hydroxyphenyl)-2-naphthol; SCHEMBL3932603; NSCZTZNRMFWAIY-UHFFFAOYSA-N; ZINC13645002; BDBM50168330
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MOA Inhibitor
Activity IC50 = 442 nM
External Link
 Compound Name 8-(3-methylbutyl)naringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name 4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL378798; SCHEMBL6830103
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MOA Inhibitor
Activity IC50 = 4610 nM
External Link
 Compound Name 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 1570 nM
External Link
 Compound Name 3'-Methoxy-4'Hydroxyclomiphene Investigative [116]
Synonyms
CHEMBL955; 3-Methoxy-4-hydroxyclomiphene; AC1MIWC3; SCHEMBL20193223; 3''-Methoxy-4''Hydroxyclomiphene; BDBM50020285; 4-{2-Chloro-1-[4-(2-diethylamino-ethoxy)-phenyl]-2-phenyl-vinyl}-2-methoxy-phenol; Phenol, 4-(2-chloro-1-(4-(2-(diethylamino)ethoxy)phenyl)-2-phenylethenyl)-2-methoxy-; 4-[(Z)-2-chloro-1-[4-(2-diethylaminoethyloxy)phenyl]-2-phenylethenyl]-2-methoxyphenol; 4-(2-Chloro-1-(4-(2-(diethylamino)ethoxy)phenyl)-2-phenylethenyl)-2-methoxyphenol
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 8430 nM
External Link
 Compound Name 3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 815 nM
External Link
 Compound Name Trans-hydroxytamoxifen Investigative [97]
MOA Antagonist
External Link
 Compound Name 3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Investigative [104]
Synonyms
CHEMBL206600; SCHEMBL6828078
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MOA Inhibitor
Activity IC50 = 654 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Investigative [113]
Synonyms
CHEMBL365290; SCHEMBL1119325; FUWUZPRNKPGRGX-UHFFFAOYSA-N
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 114 nM
External Link
 Compound Name 4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 2410 nM
External Link
 Compound Name 6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195878; SCHEMBL3926652; MAFQDFZNSVYFEW-UHFFFAOYSA-N; ZINC13645034; BDBM50168350
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 24 nM
External Link
 Compound Name 8-benzylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 503 nM
External Link
 Compound Name 2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 6240 nM
External Link
 Compound Name 8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL192386; SCHEMBL3924505; KBQSRNQTSRTYGN-UHFFFAOYSA-N; ZINC13645086; BDBM50168353
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MOA Inhibitor
Activity IC50 = 22 nM
External Link
 Compound Name 2-Naphthalen-1-yl-benzooxazol-6-ol Investigative [103]
Synonyms
CHEMBL188527; 2-(naphthalen-1-yl)benzo[d]oxazol-6-ol; SCHEMBL6311736; LYJKLNQQSXCGDI-UHFFFAOYSA-N; BDBM50154077; ZINC12353755
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1880 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195788; SCHEMBL3935673; MYVOVZDBAWARDP-UHFFFAOYSA-N; ZINC13645031; BDBM50168340
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MOA Inhibitor
Activity IC50 = 709 nM
External Link
 Compound Name 4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL204025; SCHEMBL6827956
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MOA Inhibitor
Activity IC50 = 468 nM
External Link
 Compound Name 3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Investigative [104]
Synonyms
CHEMBL206226
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MOA Inhibitor
Activity IC50 = 1170 nM
External Link
 Compound Name 6-(3-Hydroxy-phenyl)-naphthalen-1-ol Investigative [107]
Synonyms
CHEMBL193010; 6-(3-hydroxyphenyl)-1-naphthol; SCHEMBL3010784; HXKYTCGOCJUQSE-UHFFFAOYSA-N; ZINC13644987
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1452 nM
External Link
 Compound Name 4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Investigative [106]
Synonyms
CHEMBL37775
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MOA Inhibitor
Activity EC50 = 0.15 nM
External Link
 Compound Name 4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Investigative [105]
Synonyms
CHEMBL200483; SCHEMBL6440186
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MOA Inhibitor
Activity IC50 = 1800 nM
External Link
 Compound Name 5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
MOA Inhibitor
Activity IC50 = 1140 nM
External Link
 Compound Name 8-n-heptylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 392 nM
External Link
 Compound Name 4-(2-phenyl-1H-indol-3-yl)phenol Investigative [105]
Synonyms
CHEMBL371012; SCHEMBL7041571; OITCYCYIUVYFKQ-UHFFFAOYSA-N; BDBM50175419; 4-(2-Phenyl-1H-indol-3-yl)-phenol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 24 nM
External Link
 Compound Name 2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 5280 nM
External Link
 Compound Name 6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL365999; SCHEMBL4012132; UVRXGDFVCKYIGU-UHFFFAOYSA-N; BDBM50168370; ZINC13645074
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 107 nM
External Link
 Compound Name 7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Investigative [113]
Synonyms
CHEMBL183782; SCHEMBL3927964; UBYHIUUMRHTEFF-UHFFFAOYSA-N
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MOA Inhibitor
Activity IC50 = 1.5 nM
External Link
 Compound Name 4-Naphthalen-2-yl-phenol Investigative [107]
Synonyms
4-(naphthalen-2-yl)phenol; 6336-82-9; 4-(2-Naphthyl)phenol; 4-naphthalen-2-ylphenol; CHEMBL194772; NSC-39892; 2-(4-HYDROXYPHENYL)NAPHTHALENE; NSC39892; AC1L5XK9; AC1Q7B9I; SCHEMBL234529; KS-00000ORV; CTK5B8841; DTXSID70284931; NIRHUNSXEDESLN-UHFFFAOYSA-N; MolPort-015-145-553; ZINC1671629; MFCD18312886; KM0737; BDBM50168385; ANW-73541; AKOS016007751; IMED1575423883; KB-40006; AK-50357; AJ-29221; TC-162286; AX8212912; 4CH-024303
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 638 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Investigative [100]
MOA Inhibitor
Activity IC50 = 6630 nM
External Link
 Compound Name 8-n-pentylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 383 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195786; SCHEMBL5980579; DSBWWPDVDPKMHN-UHFFFAOYSA-N; ZINC13645027; BDBM50168344
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 884 nM
External Link
 Compound Name 6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL191716; SCHEMBL3934682; DZGRIHNLLUZLTL-UHFFFAOYSA-N; BDBM50168366; ZINC13645080
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 92 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 1227 nM
External Link
 Compound Name 4',5,7-trihydroxy-6,8-dimethylisoflavone Investigative [117]
Synonyms
CHEMBL512579; AC1LCTEG; SCHEMBL571136; BDBM50250906; 4'',5,7-trihydroxy-6,8-dimethylisoflavone; 5,7-dihydroxy-3-(4-hydroxyphenyl)-6,8-dimethylchromen-4-one; 5,7-dihydroxy-3-(4-hydroxyphenyl)-6,8-dimethyl-4H-chromen-4-one; 5,7-Dihydroxy-3-(4-hydroxy-phenyl)-6,8-dimethyl-chromen-4-one; 4H-1-benzopyran-4-one, 5,7-dihydroxy-3-(4-hydroxyphenyl)-6,8-dimethyl-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10200 nM
External Link
 Compound Name 2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Investigative [108]
Synonyms
CHEMBL439806; SCHEMBL6283895; BDBM50123212; 2-phenyl-1,2''-spirobi[1H-indene]-5''-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 58 nM
External Link
 Compound Name 4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL381337; SCHEMBL6828067
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MOA Inhibitor
Activity IC50 = 335 nM
External Link
 Compound Name 4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL206584; SCHEMBL6830345
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 237 nM
External Link
 Compound Name ZK-164015 Investigative [118]
Synonyms
ZK 164015; 177583-70-9; 2-(4-HYDROXYPHENYL)-3-METHYL-1-[10-(PENTYLSULFONYL)DECYL]-1H-INDOL-5-OL; CHEMBL184074; SCHEMBL7133598; CHEBI:92087; CTK4D6535; DTXSID00430964; MolPort-006-822-606; HMS3268P09; ZINC8022535; AKOS024456974; NCGC00092322-01; RT-016336; B6960; J-011295; BRD-K05151076-001-01-8
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL427180; SCHEMBL3932725; TWSSGPRRAGPVKD-UHFFFAOYSA-N; BDBM50168373; ZINC13645059
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MOA Inhibitor
Activity IC50 = 174 nM
External Link
 Compound Name 2,3-diphenyl-1H-indole Investigative [105]
Synonyms
2,3-Diphenylindole; 3469-20-3; 1H-Indole, 2,3-diphenyl-; CHEMBL200719; GYGKJNGSQQORRG-UHFFFAOYSA-N; Indole, 2,3-diphenyl-; NSC17363; EINECS 222-432-0; Indole,3-diphenyl-; Cyto5A2; AC1Q1HUE; 1H-Indole,3-diphenyl-; AC1Q4W1P; AC1L2S6L; Oprea1_738570; 2,3-Diphenyl-1H-indole #; SCHEMBL3864662; CTK1C3291; KS-00000FNK; DTXSID50188241; MolPort-001-804-408; ZINC1036850; STK080838; BDBM50175411; RW3400; NSC-17363; CCG-46312; AKOS001022174; ACM3469203; MCULE-8938765915; VI30149; ACN-036136; 7J-655S; QC-2111; CC-07034; AK-81890
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 6950 nM
External Link
 Compound Name 4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 190 nM
External Link
 Compound Name Doxorubicin-Formaldehyde Conjugate Investigative [119]
MOA Inhibitor
External Link
 Compound Name 7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 481 nM
External Link
 Compound Name 3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 2353 nM
External Link
 Compound Name 1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL194936; SCHEMBL3936480; IPBYYNRPJBGKET-UHFFFAOYSA-N; ZINC13645011; BDBM50168334
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 266 nM
External Link
 Compound Name 4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Investigative [104]
Synonyms
CHEMBL380362
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1210 nM
External Link
 Compound Name 7-Phenyl-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL194718; 7-Phenyl-2-naphthol; 7-Phenylnaphthalene-2-ol; SCHEMBL5981104; MLFRZWHPLMDWES-UHFFFAOYSA-N; BDBM50168338
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 3405 nM
External Link
 Compound Name 3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Investigative [104]
Synonyms
CHEMBL380720
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 585 nM
External Link
 Compound Name 2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 117 nM
External Link
 Compound Name 4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Investigative [105]
Synonyms
Phenol, 4,4'-indole-2,3-diyldi-; BRN 1541731; 4,4'-Indole-2,3-diyldiphenol; CHEMBL200232; 5890-93-7; SCHEMBL7037980; AC1L46D4; DTXSID90207642; ZINC3638330; BDBM50175412; LS-104733; 4,4'-[1H-Indole-2,3-diyl]bis(phenol)
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 94.8 nM
External Link
 Compound Name 6-Phenyl-naphthalen-2-ol Investigative [107]
Synonyms
6-phenyl-2-naphthol; 6-Phenylnaphthalene-2-ol; CHEMBL191714; SCHEMBL3019399; PZOXFBPKKGTQDZ-UHFFFAOYSA-N; ZINC13644999
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1345 nM
External Link
 Compound Name 6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL192621; SCHEMBL3924515; AUZLISXBMGKYGA-UHFFFAOYSA-N; ZINC13645047; BDBM50168333
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 10.3 nM
External Link
 Compound Name 2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 139 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL192102; SCHEMBL3927262; INNGVLJQICTRAF-UHFFFAOYSA-N; BDBM50168362
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1231 nM
External Link
 Compound Name 8-n-propylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 155 nM
External Link
 Compound Name 3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Investigative [103]
MOA Inhibitor
Activity IC50 = 5110 nM
External Link
 Compound Name 2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 1900 nM
External Link
 Compound Name EFFUSOL Investigative [104]
Synonyms
73166-28-6; NSC 371300; 5-ethenyl-1-methyl-9,10-dihydrophenanthrene-2,7-diol; UNII-S436Y000RU; CHEMBL205119; S436Y000RU; 1-methyl-5-vinyl-9,10-dihydrophenanthrene-2,7-diol; NSC-371300; 2,7-Phenanthrenediol, 5-ethenyl-9,10-dihydro-1-methyl-; NSC371300; AC1L2PII; AC1Q7B8H; CTK8D4698; DTXSID00223419; MolPort-042-624-482; ZINC1588038; BDBM50180512; FT-0667825
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 240 nM
External Link
 Compound Name 8-n-nonylnaringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 436 nM
External Link
 Compound Name 2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Investigative [108]
Synonyms
CHEMBL281499; SCHEMBL6286186; BDBM50123205; 2-(4-hydroxyphenyl)-1,2''-spirobi[1H-indene]-5-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 4.3 nM
External Link
 Compound Name 6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL193727; SCHEMBL3924993; QTDYCKGQBCKMGC-UHFFFAOYSA-N; ZINC13645068; BDBM50168372
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 92 nM
External Link
 Compound Name 6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL195289; SCHEMBL3930290; VLJUOFGVEJAFFK-UHFFFAOYSA-N; ZINC13645040; BDBM50168359
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 27 nM
External Link
 Compound Name 8-(2-methylpropyl)naringenin Investigative [112]
MOA Inhibitor
Activity IC50 = 80 nM
External Link
 Compound Name WAY-169916 Investigative [92]
MOA Inhibitor
Activity IC50 = 93 nM
External Link
 Compound Name 2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Investigative [103]
Synonyms
CHEMBL189077; 2-(6-hydroxynaphthalen-1-yl)benzo[d]oxazol-6-ol; SCHEMBL3926798; ZRGCERZQAHMXNC-UHFFFAOYSA-N; BDBM50154135; 595566-69-1; 6-Benzoxazolol,2-(6-hydroxy-1-naphthalenyl)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 35 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Investigative [103]
MOA Inhibitor
Activity IC50 = 447 nM
External Link
 Compound Name 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Investigative [120]
Synonyms
CHEMBL26865
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 7 nM
External Link
 Compound Name 1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
CHEMBL192782; SCHEMBL3925203; VQATUPWMFYRKSD-UHFFFAOYSA-N; BDBM50168380; ZINC13645014
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 77 nM
External Link
 Compound Name 7-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
7-(3-hydroxyphenyl)-2-naphthol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2642 nM
External Link
 Compound Name 4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
Synonyms
4-chloro-2-(4-hydroxyphenyl)quinolin-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 213 nM
External Link
 Compound Name 4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
Synonyms
4-bromo-2-(4-hydroxyphenyl)quinolin-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 212 nM
External Link
 Compound Name 4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
Synonyms
4-ethynyl-2-(4-hydroxyphenyl)quinolin-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1500 nM
External Link
 Compound Name 4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Investigative [100]
Synonyms
4-ethyl-2-(4-hydroxyphenyl)quinolin-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 634 nM
External Link
 Compound Name 6-(4-Hydroxy-phenyl)-naphthalen-1-ol Investigative [107]
Synonyms
6-(4-hydroxyphenyl)-1-naphthol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 22 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Investigative [100]
Synonyms
2-(4-hydroxyphenyl)-4-vinylquinolin-6-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 504 nM
External Link
 Compound Name SOPHORAFLAVANONE B Investigative [112]
Synonyms
8-Prenylnaringenin; 53846-50-7; Flavaprenin; (-)-(2S)-8-dimethylallylnaringenin; (S)-8-dimethylallylnaringenin; YS04; CHEMBL376915; CHEBI:50207; (-)-(2S)-5,7-dihydroxy-2-(4-hydroxyphenyl)-8-(3-methylbut-2-enyl)chroman-4-one; (2S)-5,7-dihydroxy-2-(4-hydroxyphenyl)-8-(3-methylbut-2-en-1-yl)-2,3-dihydro-4H-chromen-4-one; (s)-8-prenylnaringenin; 8-dimethylallylnaringenin; AC1LA3DM; UNII-5L872SZR8X; 8-prenylnaringenin (8-PN); BIDD:ER0149; cid_509245; SCHEMBL1171435; 5L872SZR8X; ZINC39452; CTK5J8800; BDBM19460
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 57 nM
External Link
 Compound Name Geldanamycin-estradiol hybrid Investigative [121]
MOA Inhibitor
External Link
 Compound Name CP-409069 Investigative [122]
Synonyms
CHEMBL78625; SCHEMBL3114566; BDBM50113780; (2R,4aS,10aR)-4a-benzyl-2-(prop-1-ynyl)-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-2,7-diol
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CP-394531 Investigative [122]
Synonyms
UNII-227D9ED2SI; CHEMBL77779; 227D9ED2SI; 305822-63-3; SCHEMBL3111189; BDBM50113783; 2,7-Phenanthrenediol, 2-(chloroethynyl)-1,2,3,4,4a,9,10,10a-octahydro-4a-(phenylmethyl)-, (2R,4aS,10aR)-; 2,7-Phenanthrenediol, 2-(2-chloroethynyl)-1,2,3,4,4a,9,10,10a-octahydro-4a-(phenylmethyl)-, (2R,4aS,10aR)-; 4a-Benzyl-2-chloroethynyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-2,7-diol(CP-394531)
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 6-(3-Hydroxy-phenyl)-naphthalen-2-ol Investigative [107]
Synonyms
6-(3-hydroxyphenyl)-2-naphthol; 6-(3-hydroxyphenyl)naphthalen-2-ol
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 230 nM
External Link
 Compound Name daidzein Investigative [117]
Synonyms
486-66-8; 4',7-Dihydroxyisoflavone; Daidzeol; 7,4'-Dihydroxyisoflavone; 7-hydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one; 4H-1-Benzopyran-4-one, 7-hydroxy-3-(4-hydroxyphenyl)-; 7-Hydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one; 7-hydroxy-3-(4-hydroxyphenyl)chromen-4-one; 7-Hydroxy-3-(4-hydroxyphenyl)-4-benzopyrone; UNII-6287WC5J2L; CCRIS 7600; K 251b; 4,7-Dihydroxyisoflavone; EINECS 207-635-4; BRN 0231523; CHEMBL8145; 4',7-Dihydroxy-iso-flavone; d-(+)-alpha-methylbenzylamine; ,7-Dihydroxyisoflavone; DIADZEIN
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 450 nM
External Link
2B91: Colorectal cancer 25 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Retifanlimab Approved [123]
Synonyms
INCMGA0012; Retifanlimab
    Click to Show/Hide
External Link
 Compound Name Aflibercept Approved [93]
Synonyms
Ziv-Aflibercept; Zaltrap (TN); VEGF Trap; VEGF Trap-Eye
    Click to Show/Hide
External Link
 Compound Name Regorafenib Approved [124]
Synonyms
755037-03-7; BAY 73-4506; Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY73-4506; Regorafenib (BAY 73-4506); UNII-24T2A1DOYB; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY-73-4506; 24T2A1DOYB; CHEMBL1946170; CHEBI:68647; Stivarga (TN); BAY73-4506 hydrochloride; Regorafenib [USAN:INN]
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [48]
Synonyms
Bevacizumab (ophthalmic slow-release tissue tablet)
    Click to Show/Hide
External Link
 Compound Name SYM-004 Phase 3 [48]
Synonyms
Chimeric IgG1 antibody 1024 (cancer), Symphogen; Chimeric IgG1 antibody 992 (cancer), Symphogen; Chimeric IgG1 antibodies992 + 1024 (cancer), Symphogen
    Click to Show/Hide
External Link
 Compound Name Bevacizumab + Erlotinib Phase 3 [125]
External Link
 Compound Name CPI-613 Phase 3 [48]
Synonyms
95809-78-2; 6,8-bis(benzylthio)octanoic acid; CPI 613; MLS006010202; SCHEMBL1062218; 6,8-Bis(benzylsulfanyl)octanoic acid; Octanoic acid, 6,8-bis((phenylmethyl)thio)-; Octanoic acid, 6,8-bis[(phenylMethyl)thio]-; 6,8-Bis[(phenylmethyl)thio]octanoic acid; CPI613; CHEMBL3186849; QCR-193; AOB1058; MolPort-023-219-128; HMS3656L06; C22H28O2S2; BCP04663; EX-A2043; s2776; AKOS025142095; BCP9000552; DB12109; RL06062; CS-0961; NCGC00344764-01; SMR004701300; AS-16613; BC261916; AK174899; HY-15453; BCP0726000030; KB-293127; AB0035874
    Click to Show/Hide
External Link
 Compound Name Bevacizumab Approved [93]
External Link
 Compound Name AlloStim Phase 2/3 [126]
Synonyms
AlloStim (TN)
    Click to Show/Hide
External Link
 Compound Name Sibrotuzumab Phase 2 [127]
External Link
 Compound Name CV301 Phase 2 [128]
External Link
 Compound Name Efatutazone Phase 2 [129]
Synonyms
Inolitazone; 223132-37-4; 5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-yl]methoxy]phenyl]methyl]-2,4-Thiazolidinedione; Efatutazone [INN]; RS5444; CS-7017; SCHEMBL3246054; CHEMBL3545280; JCYNMRJCUYVDBC-UHFFFAOYSA-N; Efatutazone;CS-7017;RS5444; BCP07478; AKOS030526729; DB11894; CS-0778; KB-77905; DA-07988; HY-14792; QC-10456; 4CA-1384; FT-0737589; 5-[4-[6-(4-amino-3 ,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]benzyl]thiazolidine-2,4-dione
    Click to Show/Hide
External Link
 Compound Name LOR-2040 Phase 2 [130]
External Link
 Compound Name RG7221 Phase 2 [131]
External Link
 Compound Name PEG-SN38 Phase 2 [132]
Synonyms
EZN-2208
    Click to Show/Hide
External Link
 Compound Name MEGF0444A Phase 2 [133]
External Link
 Compound Name Encapsulated cell therapy Phase 1/2 [134]
External Link
 Compound Name AB928 Phase 1/2 [135]
External Link
 Compound Name MGD007 Phase 1 [131]
External Link
 Compound Name BNC-101 Phase 1 [136]
External Link
 Compound Name Navicixizumab Phase 1 [48]
External Link
 Compound Name RG7160 Discontinued in Phase 2 [137]
External Link
 Compound Name Nimesulide Terminated [138]
Synonyms
51803-78-2; N-(4-Nitro-2-phenoxyphenyl)methanesulfonamide; Mesulid; Flogovital; Sulidene; Nimed; R-805; 4-NITRO-2-PHENOXYMETHANESULFONANILIDE; Nisulid; Nimesulidum [INN-Latin]; Nimesulida [INN-Spanish]; R 805; UNII-V4TKW1454M; 4-Nitro-2-phenoxy-methanesulfonanilide; 4'-Nitro-2'-phenoxymethanesulfonanilide; Methanesulfonamide, N-(4-nitro-2-phenoxyphenyl)-; EINECS 257-431-4; 4'-Nitro-2'-phenoxymethansulfonanilid; BRN 2421175; CHEMBL56367; MLS000069680; V4TKW1454M; Methanesulfonanilide, 4'-nitro-2'-phenoxy-; CHEBI:44445; Dulanermin
    Click to Show/Hide
External Link
 Compound Name Saracatinib Phase 2 [139]
External Link
 Compound Name G3139 + Irinotecan Investigative [140]
External Link
References
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Ref 39 ClinicalTrials.gov (NCT04975308) EMBER-3: A Phase 3, Randomized, Open-Label Study of Imlunestrant, Investigator's Choice of Endocrine Therapy, and Imlunestrant Plus Abemaciclib in Patients With Estrogen Receptor Positive, HER2 Negative Locally Advanced or Metastatic Breast Cancer Previously Treated With Endocrine Therapy. U.S.National Institutes of Health.
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Ref 42 Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. J Med Chem.2015 Jun 25;58(12):4888-904.
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Ref 52 Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen. J Pharmacol Exp Ther. 2002 Oct;303(1):196-203.
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Ref 54 G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020 Apr;180(3):635-646.
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Ref 61 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
Ref 62 Estrogen agonistic/antagonistic effects of miproxifene phosphate (TAT-59)Shibata J1, Toko T, Saito H, Lykkesfeldt AE, Fujioka A, Sato K, Hashimoto A, Wierzba K, Yamada Y.Author information1Hanno Research Center, Taiho Pharmaceutical Co., Ltd., 1-27 Misugidai, Hanno-City, Saitama, 357-8527, Japan.Erratum inCancer Chemother Pharmacol 2000;46(2):172. AbstractPURPOSE: We evaluated miproxifene phosphate (TAT-59) to elucidate its efficacy in antiestrogen therapy for breast cancer patients and to assess its tissue-selective estrogenic/antiestrogenic activity.METHODS: Using DP-TAT-59, a major and active metabolite of TAT-59, an in vitro cell growth inhibition test was performed. Antitumor activity was determined using TAT-59 against human tumor xenografts of the MCF-7 and the Br-10 cell lines andMCF-7-derived tamoxifen-resistant cell lines, R-27 and FST-1. The antitumor activity of DP-TAT-59 and DM-DP-TAT-59, major metabolites of TAT-59 found in human blood following a TAT-59 dose, was also examined after intravenous administration to experimental animals. The residual estrogenic activity of TAT-59, evaluated in terms of bone and lipid metabolism in ovariectomized rats, was then comparedwith that of tamoxifen.RESULTS: DP-TAT-59 significantly inhibited the proliferation of estrogen receptor-positive MCF-7 and T-47D tumor cells in the presence of 1 nM estradiol. TAT-59, given to mice bearing MCF-7 or Br-10 xenografts, at the dose level of 5 mg/kg, exerted a significant growth inhibitory effect that was stronger than that of tamoxifen. Moreover, R-27 and FST-1 tumors, which show a resistance to tamoxifen, responded strongly to TAT-59, suggesting that TAT-59 might be effective against tumors resistant to tamoxifen. The metabolites of TAT-59, DP-TAT-59 and DM-DP-TAT-59, showed similar antitumor activity. Both TAT-59 and tamoxifen suppressed the decrease in bone density and reduced the blood cholesterol levels in ovariectomized rats, suggesting that the estrogenic activity of TAT-59 is comparable to that of tamoxifen.CONCLUSIONS: On the basis of the above results, one may expect TAT-59 to become an effective drug in patients with tumors less sensitive to tamoxifen, while its estrogenic activity as determined by bone and lipid metabolism is similar to that of tamoxifen.PMID: 10663628 [PubMed - indexed for MEDLINE] ShareMeSH Terms, SubstancesMeSH TermsAnimalsAntineoplastic Agents, Hormonal/pharmacologyBreast Neoplasms/pathology*Cell Division/drug effectsDrug Screening Assays, AntitumorEstradiol/pharmacologyEstrogen Antagonists/pharmacology*FemaleHumansLipid MetabolismMiceMice, Inbred BALB CRatsRats, Sprague-DawleyReceptors, Estrogen/physiologyTamoxifen/analogs & derivatives*Tamoxifen/pharmacologyTransplantation, HeterologousTumor Cells, Cultured/drug effectsSubstancesAntineoplastic Agents, HormonalEstrogen AntagonistsReceptors, EstrogenTamoxifenTAT 59EstradiolLinkOut - more resourcesOther Literature SourcesAccess more work from the authors - ResearchGateMedicalBreast Cancer - MedlinePlus Health InformationMiscellaneousESTRADIOL - Hazardous Substances Data BankTAMOXIFEN - Hazardous Substances Data BankPubMed Commons home Cancer Chemother Pharmacol. 2000;45(2):133-41.
Ref 63 Idoxifene: a novel selective estrogen receptor modulator prevents bone loss and lowers cholesterol levels in ovariectomized rats and decreases uterine weight in intact rats. Endocrinology. 1998 Dec;139(12):5224-34.
Ref 64 EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8.
Ref 65 Therapeutic targets in dry eye syndrome. Drug News Perspect. 2008 Apr;21(3):166-76.
Ref 66 US patent application no. 2010,0278,784, Methods and compositions for treating skin conditions.
Ref 67 Species differences in metabolism of panomifene, an analogue of tamoxifen. Drug Metab Dispos. 1997 Dec;25(12):1370-8.
Ref 68 CN patent application no. 102406650, Sex steroid precursors alone or in combination with selective estrogen receptor modulator for prevention and treatment of vaginal dryness and sexual dysfunction in postmenop.
Ref 69 Droloxifene, a new antiestrogen: its role in metastatic breast cancer. Breast Cancer Res Treat. 1994;31(1):83-94.
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