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267 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27769036 16 Green fluorescent protein chromophore derivatives as a new class of aldose reductase inhibitors.EBI Toho University
27836399 26 [2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.EBI Bristol-Myers Squibb Research and Development
27810243 87 Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators.EBI AstraZeneca
27994732 56 Development ofEBI Tokyo Medical and Dental University
27994731 3 Identification of Triptophenolide fromEBI Chinese Academy of Medical Science
27717544 75 Targeting prostate cancer with compounds possessing dual activity as androgen receptor antagonists and HDAC6 inhibitors.EBI Integral BioSciences Pvt. Ltd
27665178 42 Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties.EBI Ochanomizu University
27140653 2 Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract.EBI University of Colorado
27301368 4 Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.EBI Cardiff University
26819671 51 Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).EBI GlaxoSmithKline
26965862 3 7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer.EBI Cardiff University
26683992 25 2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.EBI Lilly Research Laboratories
26407012 80 Optimization of a Novel Binding Motif to (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 (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.EBI AstraZeneca
26295173 25 Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.EBI Ochanomizu University
26288692 37 Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.EBI Bristol Myers-Squibb Research and Development
26305181 13 Discovery of Potent 17ß-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.EBI University of Arizona
26218343 76 Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.EBI Eli Lilly Biotechnology Center
26046313 20 Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.EBI Alla Chem LLC
25890697 6 Thiazolidine-2,4-dione derivatives: programmed chemical weapons for key protein targets of various pathological conditions.EBI Punjabi University
25978072 53 Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.EBI TBA
25879485 60 Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.EBI Seragon Pharmaceuticals
25941555 75 Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.EBI Merck Research Laboratories
25706100 65 2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists.EBI TBA
25695864 35 Identification of novel aldose reductase inhibitors based on carboxymethylated mercaptotriazinoindole scaffold.EBI Slovak Academy of Sciences
25591066 23 Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.EBI University of Maryland
25375908 9 Targeting aldose reductase for the treatment of diabetes complications and inflammatory diseases: new insights and future directions.EBI Universit£ degli Studi di Messina
25646649 20 Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.EBI University of Gothenburg
25862209 31 Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I.EBI Takeda Pharmaceutical Company Ltd
25121964 18 3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.EBI Novartis Institutes for BioMedical Research
25025737 37 Discovery of 1H-indole-2-carboxamides as novel inhibitors of the androgen receptor binding function 3 (BF3).EBI University of British Columbia
24980053 153 Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.EBI Bristol-Myers Squibb Company
25440884 2 Synthetic derivatives of aromatic abietane diterpenoids and their biological activities.EBI Universidad de Valencia
25305688 41 Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t.EBI Phenex Pharmaceuticals AG
25187277 136 Discovery of 6-[5-(4-fluorophenyl)-3-methyl-pyrazol-4-yl]-benzoxazin-3-one derivatives as novel selective nonsteroidal mineralocorticoid receptor antagonists.EBI Takeda Pharmaceutical Company Limited
25152999 9 20(S)-Ginsenoside Rh2 as aldose reductase inhibitor from Panax ginseng.EBI Kyushu University
24755427 107 The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.EBI AstraZeneca
24738581 81 Identification of (R)-6-(1-(4-cyano-3-methylphenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)-2-methoxynicotinic acid, a highly potent and selective nonsteroidal mineralocorticoid receptor antagonist.EBI Pfizer Inc.
24726305 3 Preliminary investigations into triazole derived androgen receptor antagonists.EBI Deakin University
24630411 38 Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.EBI Merck Research Laboratories
24527807 82 1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile derivatives as potent and tissue selective androgen receptor modulators.EBI Pfizer Inc.
24446728 30 Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.EBI Lilly Research Laboratories
24157365 23 Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.EBI Pfizer Inc.
24071447 39 Synthesis and structure-activity relationship of 2-phenyliminochromene derivatives as inhibitors for aldo-keto reductase (AKR) 1B10.EBI Gifu Pharmaceutical University
24044500 2 Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.EBI SAIC Frederick, Inc.
23953070 146 Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.EBI Ironwood Pharmaceuticals
23916594 92 Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.EBI Bristol-Myers Squibb Company
23958516 61 Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.EBI Takeda Pharmaceutical Company Limited
23777778 101 Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.EBI Merck Research Laboratories
23683835 21 Synthesis of organic nitrates of luteolin as a novel class of potent aldose reductase inhibitors.EBI Xiangtan University
23768907 6 Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERa-selective antagonist.EBI The University of Tokyo
23727044 6 Discovery of non-LBD inhibitor for androgen receptor by structure-guide design.EBI Korea Research Institute of Chemical Technology
23713567 13 Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.EBI University of Maryland
23611768 34 The systematic structure-activity relationship to predict how flavones bind to human androgen receptor for their antagonistic activity.EBI Meijo University
23466225 2 Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer.EBI AstraZeneca
23462715 25 Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: selectivity switching by C/Si exchange.EBI The University of Tokyo
23199477 47 Design, synthesis, and biological evaluation of 3-aryl-3-hydroxy-1-phenylpyrrolidine derivatives as novel androgen receptor antagonists.EBI Takeda Pharmaceutical Company Ltd
23432095 160 Development of potent and selective indomethacin analogues for the inhibition of AKR1C3 (Type 5 17ß-hydroxysteroid dehydrogenase/prostaglandin F synthase) in castrate-resistant prostate cancer.EBI Vanderbilt University School of Medicine
23301637 63 Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives.EBI University of British Columbia
22280402 12 "True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.EBI Trinity College
20727743 64 Discovery of quinolines as selective glucocorticoid receptor agonists.EBI Bayer Schering Pharma AG
20469868 176 Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists.EBI GlaxoSmithKline
19856921 21 Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.EBI ACADIA Pharmaceuticals AB
19664922 35 2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists.EBI GlaxoSmithKline
18952422 5 The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.EBI GlaxoSmithKline
11150172 8 Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist.EBI Schering AG
23079530 27 Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.EBI Pfizer Inc.
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
22897611 2 Discovery of diarylhydantoins as new selective androgen receptor modulators.EBI GALAPAGOS, Parc Biocitech
22866979 19 Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.EBI Pfizer Inc.
21561086 21 Selective inhibition of the tumor marker aldo-keto reductase family member 1B10 by oleanolic acid.EBI Gifu Pharmaceutical University
22746350 41 Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.EBI University of Eastern Finland
22263837 262 Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17ß-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.EBI University of Pennsylvania
24900359 31 Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists.EBI TBA
22507964 17 Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer.EBI Perelman School of Medicine University of Pennsylvania
22377517 15 Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists.EBI Pfizer Inc.
22310230 2 Methoxychalcone inhibitors of androgen receptor translocation and function.EBI National Cancer Institute
21073190 135 Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.EBI Bristol-Myers Squibb Company
21050768 20 Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.EBI Chugai Pharmaceutical Co., Ltd
21036041 22 Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs).EBI Radius Health, Inc.
20888766 50 Novel selective anti-androgens with a diphenylpentane skeleton.EBI The University of Tokyo
20672822 108 Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.EBI Pfizer Inc.
20672820 92 Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.EBI Pfizer Inc.
20638844 25 1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.EBI Pfizer Inc.
20584610 90 Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.EBI Bristol-Myers Squibb Company
20510622 142 Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.EBI Chinese Academy of Sciences
20381361 43 Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.EBI Chugai Pharmaceutical Co., Ltd
20355713 3 Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget.EBI University of Illinois
19863083 25 The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144.EBI Wyeth Research
20047280 174 Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.EBI Bristol-Myers Squibb Company
19321341 101 Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.EBI Bristol-Myers Squibb
18722119 55 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.EBI Wyeth Research
18504132 51 7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.EBI Wyeth Research
18492610 9 Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.EBI Universit£ di Messina
18400499 53 Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.EBI Ligand Pharmaceuticals
18513967 103 Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.EBI Ligand Pharmaceuticals
18032610 4 Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.EBI Ligand Pharmaceuticals
17911242 1 A surface on the androgen receptor that allosterically regulates coactivator binding.EBI University of California
17606915 4 Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.EBI The Scripps Research Institute
18318463 53 Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).EBI Wyeth Research
18165015 18 Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.EBI Monash University
18442912 90 Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.EBI Ligand Pharmaceuticals
18087047 3 Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10.EBI Universitat Aut£noma de Barcelona
18291644 62 Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
17890084 86 Androstene-3,5-dienes as ER-beta selective SERMs.EBI Merck Research Laboratories
17448656 80 Bridged androstenediol analogs as ER-beta selective SERMs.EBI Merck Research Laboratories
17064916 61 Discovery of 7alpha-substituted dihydrotestosterones as androgen receptor pure antagonists and their structure-activity relationships.EBI Chugai Pharmaceutical Co., Ltd
16309907 129 Androstenediol analogs as ER-beta-selective SERMs.EBI Merck Research Laboratories
16250653 22 Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.EBI Universit£ di Perugia
15771445 22 Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.EBI University of Ferrara
15456251 8 Soft docking and multiple receptor conformations in virtual screening.EBI University of California-San Francisco
15456242 30 11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor.EBI The Pennsylvania State University
15293993 172 Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.EBI Abbott Laboratories
12540241 5 Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.EBI Aristotle University of Thessaloniki
14613328 10 Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate.EBI University of Colorado
12238914 48 6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.EBI Women's Health Research Institute
12036351 31 Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.EBI Pfizer Global Research and Development
10737739 11 Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.EBI National Eye Institute
10212133 93 5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.EBI Ligand Pharmaceuticals, Inc.
9925725 9 Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).EBI Ligand Pharmaceuticals, Inc.
9484511 111 Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.EBI Ligand Pharmaceuticals, Inc.
8627601 169 Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.EBI Ligand Pharmaceuticals, Inc.
8027986 30 Novel spirosuccinimide aldose reductase inhibitors derived from isoquinoline-1,3-diones: 2-[(4-bromo-2-fluorophenyl)methyl]-6- fluorospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrone and congeners. 1.EBI Wyeth-Ayerst Research
1613744 68 Hydantoin bioisosteres. In vivo active spiro hydroxy acetic acid aldose reductase inhibitors.EBI Pfizer Inc.
1900532 44 A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.EBI Pfizer Inc.
2113948 11 Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.EBI Pfizer Central Research
3121857 128 Spiro hydantoin aldose reductase inhibitors.EBI Pfizer Central Research
15081005 30 Novel pyrrole-containing progesterone receptor modulators.EBI Wyeth Research
15080982 122 Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.EBI Abbott Laboratories
12781198 108 Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.EBI Ligand Pharmaceuticals
12781197 59 Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators.EBI Ligand Pharmaceuticals
10743938 103 Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.EBI Ligand Pharmaceuticals
10340624 72 4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.EBI Ligand Pharmaceuticals, Inc.
9873735 111 5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.EBI Ligand Pharmaceuticals, Inc.
22391033 69 Design, synthesis, and biological evaluation of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole derivatives as novel androgen receptor antagonists.EBI Takeda Pharmaceutical Company Ltd
22197140 15 Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer.EBI Pfizer Inc.
22104435 54 Design, synthesis, and biological evaluation of novel (1-thioxo-1,2,3,4-tetrahydro-ß-carbolin-9-yl)acetic acids as selective inhibitors for AKR1B1.EBI University of Toyama
22261024 21 Construction of an Indonesian herbal constituents database and its use in Random Forest modelling in a search for inhibitors of aldose reductase.EBI King's College London
22236472 51 Design, synthesis and evaluation of caffeic acid phenethyl ester-based inhibitors targeting a selectivity pocket in the active site of human aldo-keto reductase 1B10.EBI Gifu Pharmaceutical University
22094279 75 Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.EBI Takeda Pharmaceutical Company Ltd
22074142 89 Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.EBI Takeda Pharmaceutical Company Ltd.
22047696 17 Structure-activity relationships of ganoderma acids from Ganoderma lucidum as aldose reductase inhibitors.EBI Sepuluh Nopember Institute of Technology
22047606 29 Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.EBI University of British Columbia
22037047 1 (2-Benzyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indol-8-yl)-acetic acid: an aldose reductase inhibitor and antioxidant of zwitterionic nature.EBI Slovak Academy of Sciences
21944852 79 Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.EBI AstraZeneca R&D Charnwood
21936524 21 Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.EBI Pfizer Inc.
21916510 167 Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.EBI Merck Serono S.A.
21899328 244 Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791EBI Bristol-Myers Squibb Company
21916484 41 6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence.EBI Ochanomizu University
21831636 75 Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.EBI Pfizer Inc.
21846139 12 Inhibitors of androgen receptor activation function-2 (AF2) site identified through virtual screening.EBI University of British Columbia
21506597 6 Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.EBI The University of Tennessee
19250825 4 Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.EBI The Institute for Diabetes Discovery, LLC
21324689 74 Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation.EBI Ligand Pharmaceuticals
21316964 108 Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.EBI Ligand Pharmaceuticals
24900290 7 Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140EBI TBA
24900294 72 Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine FibroidsEBI TBA
21256748 8 Furoxan nitric oxide donor coupled chrysin derivatives: synthesis and vasculoprotection.EBI Central South University
21129963 23 In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors.EBI University of Messina
21115247 64 Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.EBI Ligand Pharmaceuticals
20805028 32 6,7-Dihydroxy-4-phenylcoumarin as inhibitor of aldose reductase 2.EBI University of Toyama
20826091 6 20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth.EBI Universität Leipzig
20813948 63 Spiroindolones, a potent compound class for the treatment of malaria.EBI Swiss Tropical and Public Health Institute
20638278 145 Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.EBI Phenex Pharmaceuticals AG
20304656 31 Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.EBI Gifu Pharmaceutical University
20462217 17 Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.EBI Pfizer Global Research& Development
20430618 21 Optimisation of a pyrazole series of progesterone antagonists; Part 1.EBI Pfizer PharmaTherapeutics Division
20408553 27 Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.EBI Pfizer Global Research& Development
20071057 4 Evaluation of aldose reductase inhibition and docking studies of 6'-nitro and 6',6''-dinitrorosmarinic acids.EBI National Hellenic Research Foundation
20226658 5 Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.EBI Meijo University
20144545 19 LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.EBI The University of Tokyo
20189816 8 Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.EBI Aristotle University of Thessaloniki
19954971 40 Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.EBI Sumitomo Chemical Co., Ltd
19616429 32 Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.EBI GlaxoSmithKline Pharmaceuticals
19595590 49 Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.EBI GlaxoSmithKline Pharmaceuticals
19606870 53 Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).EBI Merck Research Laboratories
19592245 11 Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay.EBI Meijo University
8699190 9 Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.EBI Fukuyama University
 22 Benzothiazol-2-ylcarboxylic acids with diverse spacers: A novel class of potent, orally active aldose reductase inhibitorsEBI TBA
19432422 16 Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.EBI GTx, Inc.
19286380 49 Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.EBI Pfizer Global Research and Development
19239259 66 Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.EBI Pfizer Global Research & Development
19201190 56 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.EBI Pfizer Global Research and Development
18976928 1 Inhibition of aldose reductase from cataracted eye lenses by finger millet (Eleusine coracana) polyphenols.EBI Central Food Technological Research Institute
18707892 2 Design and synthesis of carborane-containing androgen receptor (AR) antagonist bearing a pyridine ring.EBI Tohoku Pharmaceutical University
18571420 71 4-(Anilino)pyrrole-2-carboxamides: Novel non-steroidal/non-anilide type androgen antagonists effective upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.EBI The University of Tokyo
18553958 28 A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.EBI Ligand Pharmaceuticals Inc.
18038968 26 (S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.EBI Lilly Research Laboratories
17870536 28 Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.EBI Università di Modena e Reggio Emilia
17827000 6 (1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.EBI Pfizer Global Research and Development
17804229 31 Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.EBI Chugai Pharmaceutical Co. Ltd.
17766112 22 Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.EBI Pfizer Global Research and Development
17764935 32 Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.EBI Pfizer Global Research and Development
17703938 55 Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.EBI Ligand Pharmaceuticals
17681796 21 5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.EBI Wyeth Research
17574413 24 Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.EBI Bristol-Myers Squibb Research and Development
17553679 148 5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.EBI Ligand Pharmaceuticals
17292608 48 Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.EBI Pharmaceutical Research Institute
17197181 3 Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.EBI Johnson & Johnson Pharmaceutical Research and Development
17149866 4 Identification of the brominated flame retardant 1,2-dibromo-4-(1,2-dibromoethyl)cyclohexane as an androgen agonist.EBI Orebro University
16107153 10 Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.EBI Monash University (Parkville Campus)
16019211 14 Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities.EBI The University of Tokyo
15603960 84 Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15603938 54 Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15546739 60 The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15509168 10 Studies of targeting and intracellular trafficking of an anti-androgen doxorubicin-formaldehyde conjugate in PC-3 prostate cancer cells bearing androgen receptor-GFP chimera.EBI University of Colorado
15317464 4 High-resolution structures of human aldose reductase holoenzyme in complex with stereoisomers of the potent inhibitor Fidarestat: stereospecific interaction between the enzyme and a cyclic imide type inhibitor.EBI Monash University (Parkville Campus)
15081010 66 Discovery of novel nonsteroidal glucocorticoid receptor modulators.EBI Abbott Laboratories
14667216 48 Rational design of an indolebutanoic acid derivative as a novel aldose reductase inhibitor based on docking and 3D QSAR studies of phenethylamine derivatives.EBI Yonsei University
14613323 10 Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.EBI Instituto Biomar, S.A.
12954062 140 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.EBI Ligand Pharmaceuticals Inc.
12873487 5 Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor.EBI The University of Tokyo
12620078 132 Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.EBI Abbott Laboratories
11520196 81 Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.EBI Abbott Laboratories
11356108 3 Homology modeling using multiple molecular dynamics simulations and docking studies of the human androgen receptor ligand binding domain bound to testosterone and nonsteroidal ligands.EBI The University of Tennessee-Health Science Center
10882376 7 A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.EBI Rational Drug Design Laboratories
10743937 66 Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quin olines.EBI Ligand Pharmaceuticals
10230629 69 Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.EBI Ligand Pharmaceuticals, Inc.
10230628 95 Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.EBI Ligand Pharmaceuticals
9871534 95 New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.EBI Ligand Pharmaceuticals
9784110 81 5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.EBI Ligand Pharmaceuticals, Inc.
9767647 47 Novel, highly potent aldose reductase inhibitors: (R)-(-)-2-(4-bromo-2-fluorobenzyl)-1,2,3,4- tetrahydropyrrolo[1,2-a]pyrazine -4-spiro-3'-pyrrolidine-1,2',3,5'-tetrone (AS-3201) and its congeners.EBI Dainippon Pharmaceutical Company, Ltd.
9464360 145 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.EBI Ligand Pharmaceuticals, Inc.
6779009 1 Synthesis and aldose reductase inhibitory activity of 7-sulfamoylxanthone-2-carboxylic acids.EBI TBA
3934383 6 Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.EBI TBA
3925146 43 Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.EBI TBA
3097317 19 Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.EBI TBA
2498517 31 Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.EBI Pfizer Inc.
1956050 18 Gossypol and derivatives: a new class of aldose reductase inhibitors.EBI University of New Mexico School of Medicine
1899452 90 Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.EBI Pfizer Inc.
1738141 63 Potent, orally active aldose reductase inhibitors related to zopolrestat: surrogates for benzothiazole side chain.EBI Pfizer Inc
1613743 27 Orally active aldose reductase inhibitors: indazoleacetic, oxopyridazineacetic, and oxopyridopyridazineacetic acid derivatives.EBI Pfizer Inc
1597858 56 Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.EBI Tanabe Seiyaku Co., Ltd.
28287700 17 Price for Opening the Transient Specificity Pocket in Human Aldose Reductase upon Ligand Binding: Structural, Thermodynamic, Kinetic, and Computational Analysis.BDB Philipps-Universität Marburg
27359042 29 IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 InhibitorsBDB Institut de Ge´ne´tique et de Biologie Mole´culaire et Cellulaire
24607578 11 Development of novel pyrazolone derivatives as inhibitors of aldose reductase: an eco-friendly one-pot synthesis, experimental screening and in silico analysis.BDB Swami Ramanand Teerth Marathwada University, Nanded (MS), India
24004176 16 Selectively targeting prostate cancer with antiandrogen equipped histone deacetylase inhibitors.BDB Georgia Institute of Technology
23988122 7 Modulation of aldose reductase inhibition by halogen bond tuning.BDB Academy of Sciences of the Czech Republic
19645433 37 Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription.BDB St. Jude Research Hospital
19351168 14 N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.BDB Bristol-Myers Squibb Company
18921992 9 Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications.BDB Pfizer
16078847 30 Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.BDB Abbott Laboratories
16420057 33 (+)-(2R,5S)-4-[4-cyano-3-(trifluoromethyl)phenyl]-2,5-dimethyl-N-[6-(trifluoromethyl)pyridin-3- yl]piperazine-1-carboxamide (YM580) as an orally potent and peripherally selective nonsteroidal androgen receptor antagonist.BDB Astellas Pharma Inc.
17705362 43 Synthesis and characterization of nonsteroidal glucocorticoid receptor modulators for multiple myeloma.BDB Ligand Pharmaceuticals Inc.
17267219 36 Novel selective androgen receptor modulators: SAR studies on 6-bisalkylamino-2-quinolinones.BDB Ligand Pharmaceuticals Inc.
17257838 40 Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.BDB Ligand Pharmaceuticals Inc.
17034117 12 Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.BDB Ligand Pharmaceuticals Inc.
17887661 12 Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.BDB Ligand Pharmaceuticals Inc.
17439112 46 Novel series of potent, nonsteroidal, selective androgen receptor modulators based on 7H-[1,4]oxazino[3,2-g]quinolin-7-ones.BDB Ligand Pharmaceuticals Inc.
17552509 17 Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications.BDB Bristol-Myers Squibb Pharmaceutical Research Institute
17181141 12 Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.BDB Bristol-Myers Squibb Company
16190759 60 A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.BDB Pfizer
15857120 81 Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.BDB The Institute for Diabetes Discovery
12773033 17 A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.BDB Pfizer
17083960 39 Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.BDB Medical College of Wiscosin
17418233 9 Evidence for a novel binding site conformer of aldose reductase in ligand-bound state.BDB University of Marburg
17368668 8 Structural and thermodynamic study on aldose reductase: nitro-substituted inhibitors with strong enthalpic binding contribution.BDB University of Marburg
16134934 4 Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.BDB UMR 7104 du CNRS
16337231 4 High-resolution crystal structure of aldose reductase complexed with the novel sulfonyl-pyridazinone inhibitor exhibiting an alternative active site anchoring group.BDB Philipps-University Marburg