The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28252961 |
13 |
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery. |
Goethe-University Frankfurt |
| 28235703 |
13 |
Synthesis and biological evaluations of chalcones, flavones and chromenes as farnesoid x receptor (FXR) antagonists. |
Chinese Academy of Medical Sciences and Peking Union Medical College |
| 28190654 |
24 |
Discovery and optimization of benzimidazole derivatives as a novel chemotype of farnesoid X receptor (FXR) antagonists. |
Hiroshima International University |
| 27372840 |
2 |
Novel FXR (farnesoid X receptor) modulators: Potential therapies for cholesterol gallstone disease. |
Beckman Research Institute |
| 27268696 |
56 |
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties. |
Phenex Pharmaceuticals |
| 27240466 |
2 |
Novel approaches to map small molecule-target interactions. |
Max Planck Institute of Molecular Physiology |
| 26821210 |
4 |
The Halicylindramides, Farnesoid X Receptor Antagonizing Depsipeptides from a Petrosia sp. Marine Sponge Collected in Korea. |
Daegu-Gyeongbuk Medical Innovation Foundation |
| 26819665 |
16 |
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist. |
Zydus Research Centre |
| 26819660 |
82 |
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor. |
Central Pharmaceutical Research Institute |
| 26905831 |
11 |
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317. |
The University of Tokyo |
| 26321361 |
56 |
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists. |
Genentech |
| 26337021 |
40 |
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists. |
East China University of Science and Technology |
| 26048793 |
91 |
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists. |
Genentech |
| 25583100 |
107 |
Anthranilic acid derivatives as nuclear receptor modulators--development of novel PPAR selective and dual PPAR/FXR ligands. |
Goethe-University Frankfurt |
| 25934227 |
12 |
Fragmentation of GW4064 led to a highly potent partial farnesoid X receptor agonist with improved drug-like properties. |
Goethe-University Frankfurt |
| 25815138 |
58 |
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action. |
Genentech |
| 25017032 |
62 |
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists. |
Genentech |
| 24502334 |
123 |
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc). |
Genentech |
| 25499883 |
18 |
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists. |
Glaxosmithkline |
| 25453817 |
130 |
A reversed sulfonamide series of selective RORc inverse agonists. |
Argenta Discovery |
| 25305688 |
41 |
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORß and ROR¿t. |
Phenex Pharmaceuticals |
| 25255039 |
45 |
Extending the structure-activity relationship of anthranilic acid derivatives as farnesoid X receptor modulators: development of a highly potent partial farnesoid X receptor agonist. |
Goethe-University Frankfurt |
| 25247751 |
4 |
Exploitation of cholane scaffold for the discovery of potent and selective farnesoid X receptor (FXR) and G-protein coupled bile acid receptor 1 (GP-BAR1) ligands. |
University of Naples&Quot;Federico Ii&Quot |
| 24775917 |
59 |
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor. |
Beckman Research Institute |
| 24685112 |
13 |
Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR). |
Goethe-University Frankfurt |
| 24387325 |
2 |
Design, synthesis, and biological evaluation of potent dual agonists of nuclear and membrane bile acid receptors. |
Istituto Italiano Di Tecnologia |
| 24513188 |
22 |
Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists. |
East China University of Science and Technology |
| 24239186 |
84 |
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc. |
Genentech |
| 23688559 |
30 |
Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. |
City of Hope National Medical Center |
| 23684233 |
10 |
Asymmetric synthesis of the four diastereoisomers of a novel non-steroidal farnesoid X receptor (FXR) agonist: role of the chirality on the biological activity. |
Universit£ |
| 23656455 |
3 |
Binding mechanism of the farnesoid X receptor marine antagonist suvanine reveals a strategy to forestall drug modulation on nuclear receptors. Design, synthesis, and biological evaluation of novel ligands. |
Istituto Italiano Di Tecnologia |
| 24900564 |
46 |
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists. |
Pfizer |
| 23040732 |
12 |
Discovery of new non-steroidal FXR ligands via a virtual screening workflow based on Phase shape and induced fit docking. |
East China University of Science and Technology |
| 24900463 |
15 |
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators. |
TBA |
| 22564381 |
27 |
Pyrazole[3,4-e][1,4]thiazepin-7-one derivatives as a novel class of Farnesoid X Receptor (FXR) agonists. |
Universit£ |
| 22583617 |
12 |
E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: structural development study and separation from farnesoid X receptor-agonistic activity. |
The University of Tokyo |
| 21142112 |
7 |
Tuberatolides, potent FXR antagonists from the Korean marine tunicate Botryllus tuberatus. |
Seoul National University |
| 16408003 |
7 |
Diversity-oriented synthesis: exploring the intersections between chemistry and biology. |
Memorial Sloan-Kettering Cancer Center |
| 19911773 |
57 |
Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes. |
Universite Louis Pasteur |
| 20014870 |
14 |
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. |
Universita Di Perugia |
| 18815030 |
13 |
Pyrazolidine-3,5-dione derivatives as potent non-steroidal agonists of farnesoid X receptor: virtual screening, synthesis, and biological evaluation. |
Graduate School of The Chinese Academy of Sciences |
| 18307294 |
80 |
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies. |
Centre National de la Recherche Scientifique/INSERM/ULP |
| 16905319 |
6 |
Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp. |
Seoul National University |
| 16821780 |
12 |
Back door modulation of the farnesoid X receptor: design, synthesis, and biological evaluation of a series of side chain modified chenodeoxycholic acid derivatives. |
Universit£ |
| 16617018 |
4 |
Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: preparation of FXR and PPAR ligands. |
University of Tokyo |
| 16250653 |
22 |
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study. |
Universit£ |
| 16134928 |
34 |
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry. |
The Scripps Research Institute |
| 16107136 |
7 |
Farnesoid X receptor: from structure to potential clinical applications. |
Universit£ |
| 15317466 |
26 |
Bile acid derivatives as ligands of the farnesoid X receptor. Synthesis, evaluation, and structure-activity relationship of a series of body and side chain modified analogues of chenodeoxycholic acid. |
Universit£ |
| 12166927 |
6 |
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. |
TBA |
| 10956205 |
11 |
Identification of a chemical tool for the orphan nuclear receptor FXR. |
Glaxo Wellcome Research & Development |
| 12749886 |
7 |
Binding mode of 6ECDCA, a potent bile acid agonist of the farnesoid X receptor (FXR). |
Universit£ |
| 22014750 |
1 |
Pharmacophore-based discovery of FXR-agonists. Part II: identification of bioactive triterpenes from Ganoderma lucidum. |
University of Innsbruck |
| 21890356 |
30 |
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene. |
Glaxosmithkline |
| 21786805 |
130 |
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1. |
Vitae Pharmaceuticals |
| 21459580 |
8 |
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3a,7a-dihydroxy-6a-ethyl-24-nor-5β-cholan-23-amine. |
Universit£ |
| 21256005 |
51 |
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene. |
Glaxosmithkline |
| 21269824 |
112 |
Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties. |
F. Hoffmann-La Roche |
| 21134747 |
18 |
Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia& diabetes. |
F. Hoffmann-La Roche |
| 20864344 |
110 |
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1. |
Vitae Pharmaceuticals |
| 20638278 |
145 |
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists. |
Phenex Pharmaceuticals |
| 20095622 |
41 |
Improvement of physiochemical properties of the tetrahydroazepinoindole series of farnesoid X receptor (FXR) agonists: beneficial modulation of lipids in primates. |
Wyeth Research |
| 19683924 |
18 |
Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR). |
Wyeth Research |
| 19586769 |
46 |
FXR agonist activity of conformationally constrained analogs of GW 4064. |
Glaxosmithkline |
| 19410460 |
80 |
Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064. |
Glaxosmithkline |
| 17988093 |
7 |
Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity. |
Seoul National University |
| 15893927 |
102 |
Hologram quantitative structure-activity relationships for a series of farnesoid X receptor activators. |
Universidade De SãO Paulo |
| 28845983 |
81 |
A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis. |
Goethe-University Frankfurt |
| 9459568 |
32 |
[3H]Rauwolscine: an antagonist radioligand for the cloned human 5-hydroxytryptamine2b (5-HT2B) receptor. |
Eli Lilly |
| 9459566 |
23 |
Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. |
UniversitÄT WÜRzburg |
| 9459024 |
9 |
Adenosine receptor agonists: synthesis and biological evaluation of the diastereoisomers of 2-(3-hydroxy-3-phenyl-1-propyn-1-yl)NECA. |
UniversitÀ |
| 8381183 |
35 |
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists. |
Abbott Laboratories |
| 19329331 |
16 |
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs. |
Absolute Science |
| 17477519 |
10 |
Design, synthesis, and in vitro testing of alpha-methylacyl-CoA racemase inhibitors. |
University of Liverpool |
| 17649988 |
97 |
Structure-activity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinehexanamides, a class of 5-HT7 receptor agents. 2. |
Universita Degli Studi Di Bari |
| 17697781 |
29 |
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. |
Amgen |
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