PMID

Data

Article Title

Organization

Discovery of Highly Potent Liver X Receptorß Agonists.

Bristol-Myers Squibb

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.

Vitae Pharmaceuticals

Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.

Bristol-Myers Squibb

Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency andß-selectivity of liver X receptor agonist.

Kowa

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.

Vitae Pharmaceuticals

Identification and in Vivo Evaluation of Liver X Receptorß-Selective Agonists for the Potential Treatment of Alzheimer's Disease.

Wuxi Apptec

Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.

The University Of Tokyo

Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.

The University Of Tokyo

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.

Genentech

Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.

Daiichi Sankyo Rd Novare

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.

Genentech

Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptorß-selective agonists.

Kowa

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

Genentech

Design and discovery of 2-oxochromene derivatives as liver X receptorß-selective agonists.

Kowa

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.

Genentech

Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-¿ (ROR¿ or RORc).

Genentech

A reversed sulfonamide series of selective RORc inverse agonists.

Argenta Discovery

Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRß.

Bristol-Myers Squibb

Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (ROR¿)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.

The University Of Tokyo

Identification of tertiary sulfonamides as RORc inverse agonists.

Genentech

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.

Genentech

Cyanidin, a natural flavonoid, is an agonistic ligand for liver X receptor alpha and beta and reduces cellular lipid accumulation in macrophages and hepatocytes.

Korea University

Optimized chemical probes for REV-ERBa.

Glaxosmithkline

Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages.

Korea University

Identification of Potent and Selective Diphenylpropanamide ROR? Inhibitors.

New York University School Of Medicine

Discovery of tertiary sulfonamides as potent liver X receptor antagonists.

Glaxosmithkline

Ethyl 2,4,6-trihydroxybenzoate is an agonistic ligand for liver X receptor that induces cholesterol efflux from macrophages without affecting lipid accumulation in HepG2 cells.

Korea University

Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6H-dibenz[b,e]azepin-6-one skeleton.

The University Of Tokyo

Discovery of a new binding mode for a series of liver X receptor agonists.

Amgen

Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.

Johnson & Johnson Pharmaceutical Research And Development

3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.

Wyeth Pharmaceuticals

Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters.

Merck Research Laboratories

Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.

Phenex Pharmaceuticals

Synthesis of 4-(3-biaryl)quinoline sulfones as potent liver X receptor agonists.

Wyeth Pharmaceuticals

Identification of phenylsulfone-substituted quinoxaline (WYE-672) as a tissue selective liver X-receptor (LXR) agonist.

Wyeth Pharmaceuticals

1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.

Wyeth Pharmaceuticals

Quinoline-3-carboxamide containing sulfones as liver X receptor (LXR) agonists with binding selectivity for LXRbeta and low blood-brain penetration.

Wyeth Pharmaceuticals

4-(3-Aryloxyaryl)quinoline sulfones are potent liver X receptor agonists.

Wyeth Pharmaceuticals

The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages.

Glaxosmithkline

Separation of alpha-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenyl phthalimide analogs and generation of LXRalpha-selective antagonists.

The University Of Tokyo

Discovery and SAR of cinnolines/quinolines as liver X receptor (LXR) agonists with binding selectivity for LXRbeta.

Wyeth Research

Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.

Astrazeneca R&D SöDertäLje

Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity.

Glaxosmithkline

Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.

Merck Research Laboratories

Diterpenoid, steroid, and triterpenoid agonists of liver X receptors from diversified terrestrial plants and marine sources.

Merck Research Laboratories

Guttiferone I, a new prenylated benzophenone from Garcinia humilis as a liver X receptor ligand.

Merck Research Laboratories

Carboxylic acid based quinolines as liver X receptor modulators that have LXRbeta receptor binding selectivity.

Wyeth Pharmaceuticals

Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors.

University Of Tokyo

Synthesis and evaluation of anilinohexafluoroisopropanols as activators/modulators of LXRalpha and beta.

F. Hoffmann-La Roche

SAR studies: designing potent and selective LXR agonists.

Merck Research Laboratories

Discovery and optimization of a novel series of liver X receptor-alpha agonists.

Amgen

Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis.

Merck Research Laboratories

Bisubstrate inhibitors of the enzyme catechol O-methyltransferase (COMT): efficient inhibition despite the lack of a nitro group.

Laboratorium FÜR Organische Chemie

Molecular biology of 5-HT receptors.

University Of Alberta

Species orthologs of the alpha-2A adrenergic receptor: the pharmacological properties of the bovine and rat receptors differ from the human and porcine receptors.

University Of Nebraska

Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.

Yamanouchi Pharmaceutical

Characterization of Type II Ligands in CYP2C9 and CYP3A4.

Astrazeneca