The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28051871 |
100 |
Modulating Mineralocorticoid Receptor with Non-steroidal Antagonists. New Opportunities for the Development of Potent and Selective Ligands without Off-Target Side Effects. |
Instituto De Qu£Mica M£Dica (Iqm-Csic) |
27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
27919657 |
24 |
Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor. |
The Scripps Research Institute |
27810243 |
87 |
Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. |
Astrazeneca |
27994732 |
56 |
Development of |
Tokyo Medical and Dental University |
27665178 |
42 |
Development of 6-arylcoumarins as nonsteroidal progesterone antagonists. Structure-activity relationships and fluorescence properties. |
Ochanomizu University |
27326332 |
66 |
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist. |
Bristol-Myers Squibb |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26897089 |
39 |
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists. |
Vitae Pharmaceuticals |
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. |
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. |
Astrazeneca |
26218343 |
76 |
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site. |
Eli Lilly |
25978072 |
53 |
Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists. |
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. |
Seragon Pharmaceuticals |
25941555 |
75 |
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
25706100 |
65 |
2-Aryl-3-methyloctahydrophenanthrene-2,3,7-triols as potent dissociated glucocorticoid receptor agonists. |
TBA |
25599836 |
14 |
Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity. |
Boehringer Ingelheim (Canada) |
25121964 |
18 |
3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration. |
Novartis Institutes For Biomedical Research |
24980053 |
153 |
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists. |
Bristol-Myers Squibb |
25516791 |
177 |
Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate. |
Boehringer Ingelheim Pharmaceuticals |
25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
24755427 |
107 |
The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation. |
Astrazeneca |
24745969 |
36 |
Identification of the first potent, selective and bioavailable PPARa antagonist. |
Inception Sciences |
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. |
Pfizer |
24630411 |
38 |
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series. |
Merck Research Laboratories |
24656565 |
73 |
Discovery of a potent and dissociated non-steroidal glucocorticoid receptor agonist containing an alkyl carbinol pharmacophore. |
Boehringer Ingelheim Pharmaceuticals |
24506830 |
91 |
Identification of highly efficacious glucocorticoid receptor agonists with a potential for reduced clinical bone side effects. |
Boehringer Ingelheim Pharmaceuticals |
24446728 |
30 |
Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design. |
Eli Lilly |
24239189 |
85 |
Substituted phenyl as a steroid A-ring mimetic: providing agonist activity to a class of arylsulfonamide nonsteroidal glucocorticoid ligands. |
Boehringer Ingelheim Pharmaceuticals |
24215891 |
107 |
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals |
24157365 |
23 |
Design and synthesis of aryl sulfonamide-based nonsteroidal mineralocorticoid receptor antagonists. |
Pfizer |
24011644 |
81 |
Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core. |
Bristol-Myers Squibb |
23953070 |
146 |
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists. |
Ironwood Pharmaceuticals |
23916594 |
92 |
Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists. |
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. |
Takeda Pharmaceutical |
23777778 |
101 |
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists. |
Merck Research Laboratories |
23582449 |
20 |
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor. |
Institute of Organic Synthesis |
23466604 |
36 |
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. |
Universit£ |
23403082 |
28 |
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells. |
Broad Institute of Mit and Harvard |
23199485 |
34 |
Macrolactonolides: a novel class of anti-inflammatory compounds. |
Glaxosmithkline |
17616395 |
43 |
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics. |
Glaxosmithkline |
15999989 |
7 |
Design and synthesis of new nonsteroidal glucocorticoid modulators through application of an"agreement docking" method. |
Glaxosmithkline |
22917520 |
45 |
Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents. |
Zydus Research Centre |
22280402 |
12 |
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer. |
Trinity College |
21257309 |
98 |
Discovery of a potent series of non-steroidal nona-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity. |
Glaxosmithkline |
21129964 |
28 |
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist. |
Merck Research Laboratories |
20812681 |
24 |
Synthesis and biochemical characterization of a series of 17a-perfluoroalkylated estradiols as selective ligands for estrogen receptora. |
Charles University In Prague |
20727743 |
64 |
Discovery of quinolines as selective glucocorticoid receptor agonists. |
Bayer Schering Pharma |
20469868 |
176 |
Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists. |
Glaxosmithkline |
20202837 |
51 |
The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. |
Medicines Research Centre |
19592247 |
26 |
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists. |
Glaxosmithkline |
18952422 |
5 |
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist. |
Glaxosmithkline |
18038970 |
122 |
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity. |
Glaxosmithkline |
16821781 |
106 |
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series. |
Glaxosmithkline |
23131342 |
55 |
Discovery of a novel non-steroidal GR antagonist with in vivo efficacy in the olanzapine-induced weight gain model in the rat. |
Corcept Therapeutics |
23079530 |
27 |
Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides. |
Pfizer |
22866979 |
19 |
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy. |
Pfizer |
22079253 |
16 |
Discovery of selective glucocorticoid receptor modulator MK-5932. |
Merck Research Laboratories |
22465636 |
125 |
Steroidal C-21 heteroaryl thioethers. Part 3: pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids). |
Merck Research Laboratories |
21073190 |
135 |
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists. |
Bristol-Myers Squibb |
20875743 |
90 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
Pfizer |
21158453 |
12 |
Ursodeoxycholic acid amides as novel glucocorticoid receptor modulators. |
Trinity College Dublin |
20735001 |
145 |
Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics. |
Boehringer Ingelheim Pharmaceuticals |
20684563 |
176 |
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. |
H. Lundbeck |
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. |
Pfizer |
20672820 |
92 |
Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists. |
Pfizer |
20638844 |
25 |
1-Methyl-1H-pyrrole-2-carbonitrile containing tetrahydronaphthalene derivatives as non-steroidal progesterone receptor antagonists. |
Pfizer |
20510622 |
142 |
Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists. |
Chinese Academy of Sciences |
20427184 |
36 |
5-Functionalized indazoles as glucocorticoid receptor agonists. |
Amri |
20355713 |
3 |
Imaging progesterone receptor in breast tumors: synthesis and receptor binding affinity of fluoroalkyl-substituted analogues of tanaproget. |
University of Illinois |
20334371 |
20 |
Virtual screening for the identification of novel nonsteroidal glucocorticoid modulators. |
Trinity College |
19863083 |
25 |
The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. |
Wyeth Research |
20047280 |
174 |
Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators. |
Bristol-Myers Squibb |
19217285 |
32 |
Synthesis and SAR study of novel pseudo-steroids as potent and selective progesterone receptor antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
19610652 |
26 |
Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides. |
University of Texas Southwestern Medical Center |
19321341 |
101 |
Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators. |
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. |
Wyeth Research |
18504132 |
51 |
7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists. |
Wyeth Research |
18412397 |
3 |
Alkaloids from the Australian rainforest tree Ochrosia moorei. |
Griffith University |
16643060 |
3 |
Sundaicumones A and B, polyprenylated acylphloroglucinol derivatives from Calophyllumsundaicum with weak activity against the glucocorticoid receptor. |
Merlion Pharmaceuticals |
18490170 |
3 |
High-throughput evaluation of relative cell permeability between peptoids and peptides. |
University of Texas Southwestern Medical Center |
18513967 |
103 |
Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines. |
Ligand Pharmaceuticals |
18032610 |
4 |
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. |
Ligand Pharmaceuticals |
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). |
Wyeth Research |
18226897 |
128 |
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity. |
Corcept Therapeutics |
17855092 |
18 |
Synthesis and identification of novel 11beta-aryl-4',5'-dihydrospiro[estra-4,9-diene-17beta,4'-oxazole] analogs with dissociated antiprogesterone activities. |
Rti International |
17822897 |
69 |
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists. |
Corcept Therapeutics |
17258455 |
22 |
Discovery of novel phosphorus-containing steroids as selective glucocorticoid receptor antagonist. |
Johnson & Johnson Pharmaceutical Research & Development |
17692519 |
108 |
Identification of dissociated non-steroidal glucocorticoid receptor agonists. |
Boehringer Ingelheim Pharmaceuticals |
17317167 |
50 |
Parallel synthesis and SAR study of novel oxa-steroids as potent and selective progesterone receptor antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
17118655 |
73 |
Alpha-methyltryptamine sulfonamide derivatives as novel glucocorticoid receptor ligands. |
Boehringer Ingelheim Pharmaceuticals |
17169557 |
20 |
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists. |
Johnson and Johnson Pharmaceutical Research and Development |
17070047 |
36 |
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists. |
Abbott Laboratories |
16987661 |
38 |
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists. |
Abbott Laboratories |
17181172 |
94 |
Quinol-4-ones as steroid A-ring mimetics in nonsteroidal dissociated glucocorticoid agonists. |
Boehringer Ingelheim Pharmaceuticals |
16250653 |
22 |
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
Universit£ |
16112571 |
93 |
Trifluoromethyl group as a pharmacophore: effect of replacing a CF3 group on binding and agonist activity of a glucocorticoid receptor ligand. |
Boehringer Ingelheim Pharmaceuticals |
15456242 |
30 |
11beta-alkyl-Delta9-19-nortestosterone derivatives: high-affinity ligands and potent partial agonists of the androgen receptor. |
The Pennsylvania State University |
15293993 |
172 |
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. |
Abbott Laboratories |
15261266 |
39 |
Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator. |
Abbott Laboratories |
15261265 |
38 |
Synthesis, activity, metabolic stability, and pharmacokinetics of glucocorticoid receptor modulator-statin hybrids. |
Abbott Laboratories |
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. |
Women'S Health Research Institute |
12036351 |
31 |
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists. |
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. |
Ligand Pharmaceuticals |
9667968 |
18 |
Preparation, resolution, and biological evaluation of 5-aryl-1, 2-dihydro-5H-chromeno[3,4-f]quinolines: potent, orally active, nonsteroidal progesterone receptor agonists. |
Ligand Pharmaceuticals |
8627601 |
169 |
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether. |
Ligand Pharmaceuticals |
2061919 |
5 |
Dexamethasone 21-(beta-isothiocyanatoethyl) thioether: a new affinity label for glucocorticoid receptors. |
Niddk |
15080982 |
122 |
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists. |
Abbott Laboratories |
12657271 |
71 |
Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists. |
Wyeth Research |
12824023 |
6 |
An evaluation of a C-glucuronide as a liver targeting group: conjugate of a glucocorticoid antagonist. |
Abbott Laboratories |
12781198 |
108 |
Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore. |
Ligand Pharmaceuticals |
12781197 |
59 |
Synthesis and biological activity of 5-methylidene 1,2-dihydrochromeno[3,4-f]quinoline derivatives as progesterone receptor modulators. |
Ligand Pharmaceuticals |
10743938 |
103 |
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines. |
Ligand Pharmaceuticals |
9873735 |
111 |
5-Alkyl 1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal progesterone receptor modulators. |
Ligand Pharmaceuticals |
22260770 |
12 |
Synthesis and antihormonal properties of novel 11ß-benzoxazole-substituted steroids. |
Research Triangle Institute |
22197391 |
44 |
Steroidal C-21 heteroaryl thioethers (Part 2): discovery of orally bioavailable selective glucocorticoid receptor modulators (dissociated steroids). |
Merck Research Laboratories |
22074142 |
89 |
Identification of benzoxazin-3-one derivatives as novel, potent, and selective nonsteroidal mineralocorticoid receptor antagonists. |
Takeda Pharmaceutical |
21944381 |
42 |
Steroidal C-21 mercapto derivatives as dissociated steroids: discovery of an inhaled dissociated steroid. |
Merck Research Laboratories |
21963986 |
162 |
Non-steroidal dissociated glucocorticoid agonists: indoles as A-ring mimetics and function-regulating pharmacophores. |
Boehringer Ingelheim Pharmaceuticals |
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-791 |
Bristol-Myers Squibb |
21916484 |
41 |
6-arylcoumarins as novel nonsteroidal type progesterone antagonists: an example with receptor-binding-dependent fluorescence. |
Ochanomizu University |
21880489 |
15 |
Design and synthesis of long acting inhaled corticosteroids for the treatment of asthma. |
Pfizer |
21786805 |
130 |
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1. |
Vitae Pharmaceuticals |
21324689 |
74 |
Nonsteroidal 2,3-dihydroquinoline glucocorticoid receptor agonists with reduced PEPCK activation. |
Ligand Pharmaceuticals |
21349714 |
118 |
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation. |
Ligand Pharmaceuticals |
21316964 |
108 |
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists. |
Ligand Pharmaceuticals |
24900294 |
72 |
Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids |
TBA |
19364854 |
24 |
Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity. |
Monash University (Parkville Campus) |
21115247 |
64 |
Tetrahydroquinoline glucocorticoid receptor agonists: discovery of a 3-hydroxyl for improving receptor selectivity. |
Ligand Pharmaceuticals |
20864344 |
110 |
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1. |
Vitae Pharmaceuticals |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
20465278 |
27 |
Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). |
Amgen |
20462217 |
17 |
Rational design of a topical androgen receptor antagonist for the suppression of sebum production with properties suitable for follicular delivery. |
Pfizer |
20430618 |
21 |
Optimisation of a pyrazole series of progesterone antagonists; Part 1. |
Pfizer |
20408553 |
27 |
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines. |
Pfizer |
19595590 |
49 |
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists. |
Glaxosmithkline |
19606870 |
53 |
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs). |
Merck Research Laboratories |
19239259 |
66 |
Octahydrophenanthrene-2,7-diol analogues as dissociated glucocorticoid receptor agonists: discovery and lead exploration. |
Pfizer |
19019676 |
94 |
Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists. |
Medicines Research Centre |
18691892 |
52 |
Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat. |
Merck Research Laboratories |
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. |
Ligand Pharmaceuticals |
18334300 |
3 |
Expanding the repertoire of small molecule transcriptional activation domains. |
University of Michigan |
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. |
Eli Lilly |
17703938 |
55 |
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones. |
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. |
Wyeth Research |
17587578 |
45 |
Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators. |
Argenta Discovery |
17583952 |
5 |
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum. |
Griffith University |
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. |
Ligand Pharmaceuticals |
16759088 |
38 |
The discovery of new 11beta-hydroxysteroid dehydrogenase type 1 inhibitors by common feature pharmacophore modeling and virtual screening. |
University of Innsbruck |
16263276 |
2 |
A concise asymmetric route for the synthesis of a novel class of glucocorticoid mimetics containing a trifluoromethyl-substituted alcohol. |
Boehringer Ingelheim Pharmaceuticals |
15911283 |
62 |
Novel ketal ligands for the glucocorticoid receptor: in vitro and in vivo activity. |
Merck Research Laboratories |
15808489 |
60 |
Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy. |
Merck Research Laboratories |
15380227 |
66 |
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands. |
University of California San Francisco |
15261264 |
47 |
Optimization and metabolic stabilization of a class of nonsteroidal glucocorticoid modulators. |
Abbott Laboratories |
15081010 |
66 |
Discovery of novel nonsteroidal glucocorticoid receptor modulators. |
Abbott Laboratories |
15026058 |
61 |
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators. |
Abbott Laboratories |
12954062 |
140 |
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators. |
Ligand Pharmaceuticals |
12657272 |
47 |
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists. |
Wyeth Research |
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. |
Abbott Laboratories |
11728194 |
98 |
Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. |
Abbott Laboratories |
11520196 |
81 |
Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity. |
Abbott Laboratories |
11170650 |
4 |
Novel glucocorticoid antedrugs possessing a 17beta-(gamma-lactone) ring. |
Glaxo Wellcome Research and Development |
30596500 |
182 |
Identification of Mineralocorticoid Receptor Modulators with Low Impact on Electrolyte Homeostasis but Maintained Organ Protection. |
Pharmaron-Beijing |
10633034 |
5 |
Selective plasma hydrolysis of glucocorticoid gamma-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism. |
Glaxo Wellcome Research and Development |
31274313 |
95 |
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633). |
Oric Pharmaceuticals |
31940200 |
62 |
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. |
Genomics Institute of The Novartis Research Foundation (Gnf) |
10230628 |
95 |
Nonsteroidal androgen receptor agonists based on 4-(trifluoromethyl)-2H-pyrano[3,2-g]quinolin-2-one. |
Ligand Pharmaceuticals |
31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
9871534 |
95 |
New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone. |
Ligand Pharmaceuticals |
9784110 |
81 |
5-Benzylidene 1,2-dihydrochromeno[3,4-f]quinolines, a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
31104995 |
22 |
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization. |
Merck |
30929949 |
2 |
Profiling withanolide A for therapeutic targets in neurodegenerative diseases. |
University of Basel |
9464360 |
145 |
5-Aryl-1,2-dihydrochromeno[3,4-f]quinolines: a novel class of nonsteroidal human progesterone receptor agonists. |
Ligand Pharmaceuticals |
30594433 |
90 |
Discovery of potent and selective PPAR?/? dual antagonists and initial biological studies. |
Inception Sciences |
30384041 |
18 |
Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor. |
European Institute of Chemistry and Biology (Iecb) |
30359818 |
2 |
Quantitative and systems pharmacology 4. Network-based analysis of drug pleiotropy on coronary artery disease. |
Guangzhou University of Chinese Medicine |
31729873 |
43 |
Structure-Based and Property-Driven Optimization of |
Global Discovery Chemistry |
31188592 |
39 |
Why Some Targets Benefit from beyond Rule of Five Drugs. |
Boston University |
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. |
Eli Lilly |
26546213 |
56 |
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile. |
Corcept Therapeutics |
30144697 |
66 |
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs). |
Marquette University |
29424542 |
138 |
Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile. |
Astrazeneca |
29741897 |
62 |
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases. |
TBA |
30091920 |
113 |
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101). |
Oric Pharmaceuticals |
30034593 |
58 |
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton. |
The University of Tokyo |
28368581 |
82 |
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. |
Corcept Therapeutics |
28043796 |
84 |
Discovery of new selective glucocorticoid receptor agonist leads. |
Bayer Pharma |
28506584 |
29 |
Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold. |
The University of Tokyo |
28937774 |
107 |
Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. |
Astrazeneca |
29300474 |
45 |
Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists. |
Pfizer |
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. |
Takeda Pharmaceutical |
27250740 |
15 |
Electrostatic Control of Isoform Selective Inhibitor Binding in Nitric Oxide Synthase. |
University of California Irvine |
26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
18086152 |
18 |
Selective mapping of chemical space for Pseudomonas aeruginosa deacetylase LpxC inhibitory potential. |
National Institute of Pharmaceutical Education and Research |
| 21 |
Host properties of cyclodextrins towards anion constituents of antigenic determinants. A thermodynamic study in water and in N,N-dimethylformamide |
University of Surrey |
19827831 |
83 |
Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes. |
Novartis |
17915848 |
48 |
Small molecule inhibitors of integrin alpha2beta1. |
University of Pennsylvania |