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257 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28363748 8 Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.EBI Takeda Pharmaceutical
28051871 100 Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects.EBI Instituto De Qu£Mica M£Dica (Iqm-Csic)
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
27665178 42 Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties.EBI Ochanomizu University
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 Eli Lilly
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
26046313 20 Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.EBI Alla Chem
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
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
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
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
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
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
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
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
24446728 30 Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design.EBI Eli Lilly
24157365 23 Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists.EBI Pfizer
24900588 25 Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.EBI Tokyo Medical and Dental University
24044500 2 Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.EBI National Cancer Institute-Frederick
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
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
23777778 101 Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.EBI Merck Research Laboratories
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
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
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
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
23079530 27 Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.EBI Pfizer
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
22746350 41 Design, synthesis, and biological evaluation of nonsteroidal cycloalkane[d]isoxazole-containing androgen receptor modulators.EBI University of Eastern Finland
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
22310230 2 Methoxychalcone inhibitors of androgen receptor translocation and function.EBI National Cancer Institute-Bethesda
21073190 135 Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists.EBI Bristol-Myers Squibb
21050768 20 Design and synthesis of an androgen receptor pure antagonist (CH5137291) for the treatment of castration-resistant prostate cancer.EBI Chugai Pharmaceutical
21036041 22 Synthesis of potent, substituted carbazoles as selective androgen receptor modulators (SARMs).EBI Radius Health
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
20672820 92 Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.EBI Pfizer
20638844 25 1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists.EBI Pfizer
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
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
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
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
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
18442912 90 Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.EBI Ligand Pharmaceuticals
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
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£
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
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
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
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
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
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
8627601 169 Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.EBI Ligand Pharmaceuticals
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
9873735 111 5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators.EBI Ligand Pharmaceuticals
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
22197140 15 Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer.EBI Pfizer
22094279 75 Design, synthesis, and biological evaluation of 4-phenylpyrrole derivatives as novel androgen receptor antagonists.EBI Takeda Pharmaceutical
22074142 89 Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists.EBI Takeda Pharmaceutical
22047606 29 Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.EBI University of British Columbia
21936524 21 Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.EBI Pfizer
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
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
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
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
21115247 64 Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity.EBI Ligand Pharmaceuticals
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
20462217 17 Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery.EBI Pfizer
20430618 21 Optimisation of a pyrazole series of progesterone antagonists; Part 1.EBI Pfizer
20408553 27 Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.EBI Pfizer
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
19954971 40 Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.EBI Sumitomo Chemical
19616429 32 Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.EBI Glaxosmithkline
19595590 49 Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.EBI Glaxosmithkline
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
19432422 16 Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.EBI Gtx
19286380 49 Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.EBI Pfizer
19239259 66 Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration.EBI Pfizer
19201190 56 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.EBI Pfizer
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
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 Eli Lilly
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
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
17766112 22 Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.EBI Pfizer
17764935 32 Preparation of 4-aryl-2-trifluoromethylbenzonitrile derivatives as androgen receptor antagonists for topical suppression of sebum production.EBI Pfizer
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
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
15081010 66 Discovery of novel nonsteroidal glucocorticoid receptor modulators.EBI Abbott Laboratories
12954062 140 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.EBI Ligand Pharmaceuticals
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
32847363 66 Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.EBI Gifu Pharmaceutical University
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
27503683 12 Non-canonical modulators of nuclear receptors.EBI Vitae Pharmaceuticals
27437082 12 Identification of Novel Steroidal Androgen Receptor Degrading Agents Inspired by Galeterone 3?-Imidazole Carbamate.EBI University of Maryland
27563404 36 Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer.EBI University of Pittsburgh
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
30525603 162 New Generation of Selective Androgen Receptor Degraders: Our Initial Design, Synthesis, and Biological Evaluation of New Compounds with Enzalutamide-Resistant Prostate Cancer Activity.EBI University of Tennessee Health Science Center
31274313 95 Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).EBI Oric Pharmaceuticals
31940200 62 Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.EBI Genomics Institute of The Novartis Research Foundation (Gnf)
10230629 69 Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.EBI Ligand Pharmaceuticals
10230628 95 Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one.EBI Ligand Pharmaceuticals
29400967 136 Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.EBI Bristol-Myers Squibb
31185168 144 Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.EBI Rti International
9871534 95 New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.EBI Ligand Pharmaceuticals
31271960 1 Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines.EBI The Czech Academy of Sciences
9784110 81 5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists.EBI Ligand Pharmaceuticals
30925341 4 Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.EBI Sichuan University and Collaborative Innovation Center For Biotherapy
9464360 145 5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists.EBI Ligand Pharmaceuticals
26568144 8 Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.EBI Eli Lilly
25062331 81 Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor.EBI University of British Columbia
30193215 20 Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor.EBI Vancouver Prostate Centre (Vpc)
30189396 38 5'-Chloro-2,2'-dihydroxychalcone and related flavanoids as treatments for prostate cancer.EBI Kanazawa University
30144697 66 Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).EBI Marquette University
28594553 10 Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands.EBI National Institute of Health Sciences
29424542 138 Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile.EBI Astrazeneca
30091920 113 Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).EBI Oric Pharmaceuticals
30034593 58 Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton.EBI The University of Tokyo
29407970 1 High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex.EBI Nanjing Forestry University
29117897 3 Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents.EBI China Pharmaceutical University
28757062 6 Design, synthesis and biological evaluation of novel 3-oxo-4-oxa-5?-androst-17?-amide derivatives as dual 5?-reductase inhibitors and androgen receptor antagonists.EBI China Pharmaceutical University
28043796 84 Discovery of new selective glucocorticoid receptor agonist leads.EBI Bayer Pharma
28696695 77 Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.EBI Pfizer
29300474 45 Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.EBI Pfizer
28478926 2 Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles.EBI Chinese Academy of Sciences
28454849 48 Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.EBI Takeda Pharmaceutical
28385503 19 Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.EBI Drexel University College of Medicine
26878082 196 An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.BDB University of Bonn
28411406 16 Discovery of novel 2-substituted-4-(2-fluorophenoxy) pyridine derivatives possessing pyrazolone and triazole moieties as dual c-Met/VEGFR-2 receptor tyrosine kinase inhibitorsBDB China Pharmaceutical University
12237342 2 High affinity antagonists of the vanilloid receptor.BDB National Cancer Institute-Bethesda
8935801 586 Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding.BDB Janssen Research Foundation
16216042 10 Synthesis and biological evaluation of novel EG5 inhibitors.BDB University of Leipzig
1840645 85 Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine.BDB University of Toronto
16990005 11 Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.BDB Johnson & Johnson Pharmaceutical
15013001 10 Novel arylsulfonamides possessing sub-picomolar HIV protease activities and potent anti-HIV activity against wild-type and drug-resistant viral strains.BDB Glaxosmithkline