Target General Infomation
Target ID
T80896
Former ID
TTDS00250
Target Name
Estrogen receptor beta
Gene Name
ESR2
Synonyms
Beta-1; ER-beta; Erbeta; Oestrogen receptor beta; ESR2
Target Type
Successful
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Carcinoma [ICD9: 230-234; ICD10: D00-D09]
Cushing's disease [ICD9: 255; ICD10: E24.0]
Estrogen deficiency [ICD10: E28.39]
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Hepatitis virus infection [ICD9: 573.3; ICD10: K75.9]
Hot flashes [ICD10: N95.1]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Irregularities [ICD10: N92.6]
Menopause symptoms [ICD10: N95.0]
Ocular disease [ICD10: H00-H59]
Prostate hyperplasia [ICD10: N40]
Prostate cancer [ICD9: 185; ICD10: C61]
Sepsis [ICD9: 995.91; ICD10: A40, A41]
Trematode infection [ICD10: B66.9]
Vasomotor symptoms [ICD9: 627.2; ICD10: N95.1]
Function
Nuclear hormone receptor. binds estrogens with an affinity similar to that of esr1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability.
BioChemical Class
Nuclear hormone receptor
Target Validation
T80896
UniProt ID
Sequence
MDIKNSPSSLNSPSSYNCSQSILPLEHGSIYIPSSYVDSHHEYPAMTFYSPAVMNYSIPS
NVTNLEGGPGRQTTSPNVLWPTPGHLSPLVVHRQLSHLYAEPQKSPWCEARSLEHTLPVN
RETLKRKVSGNRCASPVTGPGSKRDAHFCAVCSDYASGYHYGVWSCEGCKAFFKRSIQGH
NDYICPATNQCTIDKNRRKSCQACRLRKCYEVGMVKCGSRRERCGYRLVRRQRSADEQLH
CAGKAKRSGGHAPRVRELLLDALSPEQLVLTLLEAEPPHVLISRPSAPFTEASMMMSLTK
LADKELVHMISWAKKIPGFVELSLFDQVRLLESCWMEVLMMGLMWRSIDHPGKLIFAPDL
VLDRDEGKCVEGILEIFDMLLATTSRFRELKLQHKEYLCVKAMILLNSSMYPLVTATQDA
DSSRKLAHLLNAVTDALVWVIAKSGISSQQQSMRLANLLMLLSHVRHASNKGMEHLLNMK
CKNVVPVYDLLLEMLNAHVLRGCKSSITGSECSPAEDSKSKEGSQNPQSQ
Drugs and Mode of Action
Drug(s) ARZOXIFENE Drug Info Approved Breast cancer [521695], [549961]
Conjugated Estrogens Drug Info Approved Vasomotor symptoms [529091], [536361]
Estrogen Drug Info Approved Menopause symptoms [551871]
Premarin Drug Info Approved Menopause [523937]
Trilostane Drug Info Approved Cushing's disease [538514], [541930]
MF-101 Drug Info Phase 3 Hepatitis virus infection [522672]
Premarin/Pravachol Drug Info Phase 3 Hyperlipidaemia [535747]
AUS-131 Drug Info Phase 2 Hot flashes [548914]
ERB-041 Drug Info Phase 2 Inflammatory bowel disease [521827], [541807]
Erteberel Drug Info Phase 2 Prostate hyperplasia [524322]
Genistein Drug Info Phase 2 Prostate cancer [536772], [539868]
VG-101 Drug Info Phase 1/2 Menopause symptoms [521993]
ERB-257 Drug Info Phase 1 Sepsis [522385]
NARINGENIN Drug Info Phase 1 Discovery agent [522980]
BITHIONOL Drug Info Withdrawn from market Trematode infection [539482], [551871]
HEXESTROL Drug Info Withdrawn from market Irregularities [533402], [534328], [539866]
EM-800 Drug Info Discontinued in Phase 3 Estrogen deficiency [546717]
ERB-196 Drug Info Discontinued in Phase 1 Inflammatory bowel disease [548018]
ICI-164384 Drug Info Terminated Breast cancer [544737]
LY-117018 Drug Info Terminated Discovery agent [544760]
ZK-119010 Drug Info Terminated Carcinoma [529380]
Inhibitor 1,2-Bis-(4-hydroxy-phenyl)-3H-inden-5-ol Drug Info [527738]
1,8-Dichloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-Bromo-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
1-CHLORO-6-(4-HYDROXYPHENYL)-2-NAPHTHOL Drug Info [551374]
1-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
2,3-diphenyl-1H-indole Drug Info [527797]
2-(2-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Butoxy-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Chloro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(3-Fluoro-4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info [526532]
2-(3-hydroxyphenyl)-1,2'-spirobi[1H-indene]-6-ol Drug Info [526532]
2-(4-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-1-p-tolyl-3H-inden-5-ol Drug Info [527738]
2-(4-Hydroxy-phenyl)-4-methoxy-quinolin-6-ol Drug Info [527681]
2-(4-Hydroxy-phenyl)-4-vinyl-quinolin-6-ol Drug Info [527681]
2-(4-Hydroxy-phenyl)-7-isopropyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-methoxy-benzofuran-5-ol Drug Info [527198]
2-(4-Hydroxy-phenyl)-7-methoxy-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-methyl-benzofuran-5-ol Drug Info [527198]
2-(4-Hydroxy-phenyl)-7-phenyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-propenyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-propyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzofuran-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
2-(4-Hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
2-(4-HYDROXY-PHENYL)BENZOFURAN-5-OL Drug Info [551374]
2-(4-hydroxyphenyl)-1,2'-spirobi[1H-indene]-5-ol Drug Info [526532]
2-(5-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-5-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-1-yl)-benzooxazol-6-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-5-ol Drug Info [527232]
2-(6-Hydroxy-naphthalen-2-yl)-benzooxazol-6-ol Drug Info [527232]
2-Naphthalen-1-yl-benzooxazol-6-ol Drug Info [527232]
2-phenyl-1,2'-spirobi[1H-indene]-5'-ol Drug Info [526532]
3'-Methoxy-4'Hydroxyclomiphene Drug Info [533383]
3,4,6-Trihydroxy-2-(4-hydroxy-phenyl)-inden-1-one Drug Info [527546]
3,6-Dihydroxy-2-(4-hydroxy-phenyl)-inden-1-one Drug Info [527546]
3,8-dihydroxy-4-methyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3,8-dihydroxy-7-methyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-(2-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info [527232]
3-(4-Hydroxy-phenyl)-4H-chromen-7-ol Drug Info [527550]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-5-ol Drug Info [527232]
3-(4-Hydroxy-phenyl)-benzo[d]isoxazol-6-ol Drug Info [527232]
3-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
3-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
3-chloro-4-(4-hydroxyphenyl)salicylaldoxime Drug Info [529314]
3-hydroxy-4,10-dimethyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-hydroxy-4,7-dimethyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-hydroxy-4-methyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-hydroxy-8,10-dimethyl-6H-benzo[c]chromen-6-one Drug Info [527966]
3-[1-ethyl-2-(3-hydroxyphenyl)butyl]phenol Drug Info [533407]
4',5,7-trihydroxy-6,8-dimethylisoflavone Drug Info [526493]
4,10-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,10-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,6,7-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,7,10-tetramethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,6,7-trimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
4-(2-phenyl-1H-benzo[d]imidazol-1-yl)phenol Drug Info [527797]
4-(2-phenyl-1H-indol-3-yl)phenol Drug Info [527797]
4-(3-(4-hydroxyphenyl)-1H-indol-2-yl)phenol Drug Info [527797]
4-(3-phenyl-1H-indol-2-yl)phenol Drug Info [527797]
4-(4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE OXIME Drug Info [551374]
4-(5-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info [527232]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,2-diol Drug Info [527232]
4-(6-Hydroxy-benzooxazol-2-yl)-benzene-1,3-diol Drug Info [527232]
4-Benzo[d]isoxazol-3-yl-benzene-1,3-diol Drug Info [527232]
4-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Ethyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
4-Naphthalen-2-yl-phenol Drug Info [527584]
4-[1,2-bis(4-hydroxyphenyl)but-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)hex-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)pent-1-enyl]phenol Drug Info [526589]
4-[1,2-bis(4-hydroxyphenyl)vinyl]phenol Drug Info [526589]
4-[2,2-bis(4-hydroxyphenyl)-1-methylvinyl]phenol Drug Info [526589]
5,7-dihydroxy-3-phenyl-3H-quinazolin-4-one Drug Info [528131]
5-Bromo-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
5-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-6-ol Drug Info [527232]
5-Chloro-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info [527681]
6-(2,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2,6-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(2-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3,5-Difluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Chloro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Fluoro-4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(3-Hydroxy-phenyl)-naphthalen-1-ol Drug Info [527584]
6-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-2-methoxy-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-2-methyl-phenyl)-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-methoxy-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-methyl-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-nitro-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-1-phenyl-naphthalen-2-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-naphthalen-1-ol Drug Info [527584]
6-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527681]
6-Chloro-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
6-ethyl-4,7-dimethyl-6H-benzo[c]chromene-3,8-diol Drug Info [527966]
6-Phenyl-naphthalen-2-ol Drug Info [527584]
7-(3-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
7-(4-Hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
7-Allyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Bromo-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info [527198]
7-Bromo-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Butyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Chloro-2-(4-hydroxy-phenyl)-benzofuran-5-ol Drug Info [527198]
7-Ethyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-Ethynyl-2-(4-hydroxy-phenyl)-benzooxazol-5-ol Drug Info [527232]
7-hydroxy-1,2,9,9a-tetrahydrofluoren-3-one Drug Info [528152]
7-hydroxy-3-(4-hydroxyphenyl)-3H-quinazolin-4-one Drug Info [528131]
7-Phenyl-naphthalen-2-ol Drug Info [527584]
8-(2,2-dimethylpropyl)naringenin Drug Info [528557]
8-(2-methylpropyl)naringenin Drug Info [528557]
8-(3-methylbutyl)naringenin Drug Info [528557]
8-benzylnaringenin Drug Info [528557]
8-Chloro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
8-Fluoro-6-(4-hydroxy-phenyl)-naphthalen-2-ol Drug Info [527584]
8-methylnaringenin Drug Info [528557]
8-n-heptylnaringenin Drug Info [528557]
8-n-nonylnaringenin Drug Info [528557]
8-n-pentylnaringenin Drug Info [528557]
8-n-propylnaringenin Drug Info [528557]
8-n-undecylnaringenin Drug Info [528557]
Acetate Ion Drug Info [551393]
ANDROSTENEDIOL Drug Info [529061]
ARZOXIFENE Drug Info [528827]
BITHIONOL Drug Info [531262]
BROUSSONIN A Drug Info [530935]
COUMESTROL Drug Info [527550]
CP-394531 Drug Info [526345]
CP-409069 Drug Info [526345]
DIADZEIN Drug Info [526493]
DIHYDRORALOXIFENE Drug Info [525493]
Doxorubicin-Formaldehyde Conjugate Drug Info [526966]
EFFUSOL Drug Info [527966]
Estrogen platinum(II) hybrid derivative Drug Info [527267]
Geldanamycin-estradiol hybrid Drug Info [525501]
GNF-PF-3037 Drug Info [531262]
HEXESTROL Drug Info [551316]
ICI-164384 Drug Info [530807]
LY-117018 Drug Info [531906]
MORIN Drug Info [531262]
NAFOXIDINE Drug Info [534677]
NARINGENIN Drug Info [528557]
Para-Mercury-Benzenesulfonic Acid Drug Info [551393]
Pipendoxifene Drug Info [526057]
SOPHORAFLAVANONE B Drug Info [528557]
THIOGENISTEIN Drug Info [528131]
TUPICHINOL C Drug Info [530935]
WAY-169916 Drug Info [527327]
ZK-119010 Drug Info [531064]
ZK-164015 Drug Info [527179]
[1,1':2',1'']Terphenyl-4'-carbaldehyde oxime Drug Info [526711]
Agonist AUS-131 Drug Info [527547]
bisphenol A Drug Info [532398]
diarylpropionitril Drug Info [526191]
ERB-002 Drug Info [543899]
ERB-041 Drug Info [532547], [551871]
ERB-196 Drug Info [528229]
ERB-257 Drug Info [548900]
Erteberel Drug Info [549074]
Estrogen Drug Info [534944]
GTx-878 Drug Info [543899]
KB-9520 Drug Info [543899]
NDC-1022 Drug Info [543899]
VG-101 Drug Info [544204]
WAY200070 Drug Info [527232]
Antagonist Conjugated Estrogens Drug Info [535660], [536952]
EM-800 Drug Info [538072]
HPTE Drug Info [525459]
MF-101 Drug Info [529943]
PHTPP Drug Info [528623]
Premarin Drug Info [535660], [536952]
R,R-THC Drug Info [525532]
Trans-hydroxytamoxifen Drug Info [535376]
Modulator Estrogen receptor beta modulators Drug Info [543899]
Genistein Drug Info
GTx-822 Drug Info [543899]
Premarin/Pravachol Drug Info [535747]
Trilostane Drug Info [556264]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Estrogen signaling pathway
Prolactin signaling pathway
Pathway Interaction Database Plasma membrane estrogen receptor signaling
Validated nuclear estrogen receptor beta network
Validated nuclear estrogen receptor alpha network
Reactome Nuclear Receptor transcription pathway
WikiPathways SIDS Susceptibility Pathways
Ovarian Infertility Genes
Integrated Pancreatic Cancer Pathway
Nuclear Receptors
References
Ref 521695ClinicalTrials.gov (NCT00190697) A Study of LY353381 (Arzoxifene) for Patients Who Benefitted From This Drug in Other Oncology Trials and Wished to Continue Treatment. U.S. National Institutes of Health.
Ref 521827ClinicalTrials.gov (NCT00318500) Study Evaluating the Safety and Efficacy of ERB-041 on Reduction of Symptoms Associated With Endometriosis in Reproductive-Aged Women. U.S. National Institutes of Health.
Ref 521993ClinicalTrials.gov (NCT00453089) VG101 Phase I/II to Treat Vulvar and Vaginal Atrophy in Post-Menopausal Women. U.S. National Institutes of Health.
Ref 522385ClinicalTrials.gov (NCT00722202) Study Evaluating the Safety and Pharmacokinetics (PK) of Ascending Single IV Doses of ERB-257 in Healthy Japanese Males. U.S. National Institutes of Health.
Ref 522672ClinicalTrials.gov (NCT00906308) A Study of MF101 in Postmenopausal Women. U.S. National Institutes of Health.
Ref 522980ClinicalTrials.gov (NCT01091077) A Pilot Study of the Grapefruit Flavonoid Naringenin for HCV Infection. U.S. National Institutes of Health.
Ref 523937ClinicalTrials.gov (NCT01613170) Premarin Versus Toviaz for Treatment of Overactive Bladder. U.S. National Institutes of Health.
Ref 524322ClinicalTrials.gov (NCT01874756) The Efficacy and Safety of a Selective Estrogen Receptor Beta Agonist (LY500307) for Negative Symptoms and Cognitive Impairment Associated With Schizophrenia. U.S. National Institutes of Health.
Ref 529091Roles of hormone replacement therapy and iron in proliferation of breast epithelial cells with different estrogen and progesterone receptor status. Breast. 2008 Apr;17(2):172-9. Epub 2007 Oct 24.
Ref 529380Pharmacological characterization of a novel oestrogen antagonist, ZK 119010, in rats and mice. J Endocrinol. 1991 Sep;130(3):409-14.
Ref 533402Carcinogenicity and metabolic activation of hexestrol. Chem Biol Interact. 1985 Oct;55(1-2):157-76.
Ref 534328Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology. 1997 Mar;138(3):863-70.
Ref 535747Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536772New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
Ref 538514FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018719.
Ref 539482(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2338).
Ref 539866(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2823).
Ref 539868(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2826).
Ref 541807(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6700).
Ref 541930(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6850).
Ref 544737Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000792)
Ref 544760Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000893)
Ref 546717Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009862)
Ref 548018Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021229)
Ref 548914Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030256)
Ref 549961Clinical pipeline report, company report or official report of Lilly.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525459Signalling by CXC-chemokine receptors 1 and 2 expressed in CHO cells: a comparison of calcium mobilization, inhibition of adenylyl cyclase and stimulation of GTPgammaS binding induced by IL-8 and GROalpha. Br J Pharmacol. 1999 Feb;126(3):810-8.
Ref 525493Bioorg Med Chem Lett. 1999 Apr 19;9(8):1137-40.Synthesis and biological activity of trans-2,3-dihydroraloxifene.
Ref 525501Bioorg Med Chem Lett. 1999 May 3;9(9):1233-8.Synthesis and evaluation of geldanamycin-estradiol hybrids.
Ref 525532Estrogen receptor subtype-selective ligands: asymmetric synthesis and biological evaluation of cis- and trans-5,11-dialkyl- 5,6,11, 12-tetrahydrochrysenes. J Med Chem. 1999 Jul 1;42(13):2456-68.
Ref 526057J Med Chem. 2001 May 24;44(11):1654-7.Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Ref 526191Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues. J Med Chem. 2001 Nov 22;44(24):4230-51.
Ref 526345J Med Chem. 2002 Jun 6;45(12):2417-24.Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Ref 526493J Nat Prod. 2002 Dec;65(12):1749-53.Isolation and structure elucidation of an isoflavone and a sesterterpenoic acid from Henriettella fascicularis.
Ref 526532Bioorg Med Chem Lett. 2003 Feb 10;13(3):479-83.2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
Ref 526589J Med Chem. 2003 Apr 10;46(8):1484-91.Antiestrogenically active 1,1,2-tris(4-hydroxyphenyl)alkenes without basic side chain: synthesis and biological activity.
Ref 526711J Med Chem. 2003 Sep 11;46(19):4032-42.Novel estrogen receptor ligands based on an anthranylaldoxime structure: role of the phenol-type pseudocycle in the binding process.
Ref 526966J Med Chem. 2004 Feb 26;47(5):1193-206.Design, synthesis, and biological evaluation of doxorubicin-formaldehyde conjugates targeted to breast cancer cells.
Ref 527179Bioorg Med Chem Lett. 2004 Sep 20;14(18):4659-63.Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
Ref 527198Bioorg Med Chem Lett. 2004 Oct 4;14(19):4925-9.7-Substituted 2-phenyl-benzofurans as ER beta selective ligands.
Ref 527232J Med Chem. 2004 Oct 7;47(21):5021-40.Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Ref 527267Bioorg Med Chem Lett. 2004 Dec 6;14(23):5919-24.Biological evaluation of novel estrogen-platinum(II) hybrid molecules on uterine and ovarian cancers-molecular modeling studies.
Ref 527327J Med Chem. 2004 Dec 16;47(26):6435-8.Synthesis and activity of substituted 4-(indazol-3-yl)phenols as pathway-selective estrogen receptor ligands useful in the treatment of rheumatoid arthritis.
Ref 527546Bioorg Med Chem Lett. 2005 Jun 15;15(12):3137-42.Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones.
Ref 527547S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
Ref 527550J Med Chem. 2005 May 19;48(10):3463-6.Structure-based virtual screening for plant-based ERbeta-selective ligands as potential preventative therapy against age-related neurodegenerative diseases.
Ref 527584J Med Chem. 2005 Jun 16;48(12):3953-79.ERbeta ligands. 3. Exploiting two binding orientations of the 2-phenylnaphthalene scaffold to achieve ERbeta selectivity.
Ref 527681Bioorg Med Chem Lett. 2005 Oct 15;15(20):4520-5.ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.
Ref 527738J Med Chem. 2005 Sep 22;48(19):5989-6003.Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.
Ref 527797Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. Epub 2005 Oct 10.Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Ref 527966Bioorg Med Chem Lett. 2006 Mar 15;16(6):1468-72. Epub 2006 Jan 18.6H-Benzo[c]chromen-6-one derivatives as selective ERbeta agonists.
Ref 528131J Med Chem. 2006 Apr 20;49(8):2440-55.Synthesis and characterization of 3-arylquinazolinone and 3-arylquinazolinethione derivatives as selective estrogen receptor beta modulators.
Ref 528152Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2.The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.
Ref 528229WAY-202196, a selective estrogen receptor-beta agonist, protects against death in experimental septic shock. Crit Care Med. 2006 Aug;34(8):2188-93.
Ref 528557J Med Chem. 2006 Dec 14;49(25):7357-65.Subtle side-chain modifications of the hop phytoestrogen 8-prenylnaringenin result in distinct agonist/antagonist activity profiles for estrogen receptors alphaand beta.
Ref 528623Structure-guided optimization of estrogen receptor binding affinity and antagonist potency of pyrazolopyrimidines with basic side chains. J Med Chem. 2007 Jan 25;50(2):399-403.
Ref 528827J Med Chem. 2007 May 31;50(11):2682-92. Epub 2007 May 10.Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
Ref 529061Bioorg Med Chem Lett. 2007 Nov 15;17(22):6295-8. Epub 2007 Sep 7.Androstene-3,5-dienes as ER-beta selective SERMs.
Ref 529314J Med Chem. 2008 Mar 13;51(5):1344-51. Epub 2008 Feb 13.Monoaryl-substituted salicylaldoximes as ligands for estrogen receptor beta.
Ref 529943MF101, a selective estrogen receptor beta modulator for the treatment of menopausal hot flushes: a phase II clinical trial. Menopause. 2009 May-Jun;16(3):458-65.
Ref 530807J Med Chem. 1991 May;34(5):1624-30.Synthesis and biological activity of new halo-steroidal antiestrogens.
Ref 530935Bioorg Med Chem Lett. 2010 Jun 15;20(12):3764-7. Epub 2010 Apr 19.New estrogenic compounds isolated from Broussonetia kazinoki.
Ref 531064J Med Chem. 1991 Jul;34(7):2145-52.2-Phenylindole-linked [2-(aminoalkyl)pyridine]dichloroplatinum(II): complexes with a selective action on estrogen receptor positive mammary tumors.
Ref 531262Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6. Epub 2010 Oct 21.In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
Ref 531906J Med Chem. 1990 Dec;33(12):3222-9.Structure-activity relationship of antiestrogens. Phenolic analogues of 2,3-diaryl-2H-1-benzopyrans.
Ref 532398Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERalpha-selective antagonist. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4031-6.
Ref 532547Erb-041, an estrogen receptor-beta agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
Ref 533383J Med Chem. 1989 Jan;32(1):192-7.Phenolic metabolites of clomiphene: [(E,Z)-2-[4-(1,2-diphenyl-2-chlorovinyl)phenoxy]ethyl]diethylamine. Preparation, electrophilicity, and effects in MCF 7 breast cancer cells.
Ref 533407J Med Chem. 1986 Sep;29(9):1668-74.Influence of alkyl chain ramification on estradiol receptor binding affinity and intrinsic activity of 1,2-dialkylated 1,2-bis(4- or 3-hydroxyphenyl)ethane estrogens and antiestrogens.
Ref 534677J Med Chem. 1998 Jul 30;41(16):2928-31.Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
Ref 534944Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6.
Ref 535376Antagonists selective for estrogen receptor alpha. Endocrinology. 2002 Mar;143(3):941-7.
Ref 535660Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 535747Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.
Ref 536952Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85. Epub 2008 Nov 26.
Ref 538072EM-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 543899(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 621).
Ref 544204Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.
Ref 548900Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030075)
Ref 549074Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
Ref 551316Bone targeted drugs 2. synthesis of estrogens with hydroxyapatite affinity, Bioorg. Med. Chem. Lett. 6(9):1047-1050 (1996).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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