The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28242276 |
45 |
Synthesis of dihydroimidazole tethered imidazolinethiones and their activity as novel antagonists of the nuclear retinoic acid receptor-related orphan receptors (RORs). |
Torrey Pines Institute For Molecular Studies |
27815118 |
112 |
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists. |
Galderma R & D |
26990539 |
79 |
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist. |
Vitae Pharmaceuticals |
27080181 |
33 |
Discovery of biaryls as ROR¿ inverse agonists by using structure-based design. |
Biogen |
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 |
26048806 |
80 |
Discovery of biaryl carboxylamides as potent ROR¿ inverse agonists. |
Biogen Idec |
26048793 |
91 |
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists. |
Genentech |
26048789 |
143 |
Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists. |
Biogen |
26014484 |
12 |
Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure. |
The University of Tokyo |
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 |
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 |
24702856 |
84 |
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 |
24685544 |
75 |
Identification of tertiary sulfonamides as RORc inverse agonists. |
Genentech |
24559867 |
6 |
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors. |
The University of Tokyo |
24239186 |
84 |
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc. |
Genentech |
24900700 |
21 |
Identification of New Nonsteroidal ROR? Ligands; Related Structure-Activity Relationships and Docking Studies. |
Genfit |
32334911 |
22 |
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists. |
Bristol Myers Squibb |
32551004 |
32 |
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist. |
Bristol Myers Squibb |
30776227 |
38 |
Discovery of Second Generation ROR? Inhibitors Composed of an Azole Scaffold. |
Kyoto Prefectural University of Medicine |
27524313 |
33 |
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties. |
Genentech |
30964293 |
40 |
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable ROR? Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. |
Chinese Academy of Sciences |
31257087 |
243 |
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists. |
Bristol-Myers Squibb |
31272795 |
154 |
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions. |
Advinus Therapeutics |
31638797 |
193 |
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy. |
Bristol-Myers Squibb |
31729873 |
43 |
Structure-Based and Property-Driven Optimization of |
Global Discovery Chemistry |
31223457 |
71 |
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2. |
Astrazeneca |
30130103 |
90 |
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. |
Karo Pharma |
30301676 |
91 |
Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (ROR?t) inhibitor, S18-000003. |
Shionogi |
30077610 |
25 |
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity. |
The University of Tokyo |
29571573 |
34 |
Sulfoximines as potent ROR? inverse agonists. |
Nestle Skin Health |
29534930 |
34 |
Identification of an aminothiazole series of ROR? modulators. |
The Scripps Research Institute |
29233651 |
121 |
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (ROR?/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity. |
Bristol-Myers Squibb |
30095900 |
109 |
Potent and Orally Bioavailable Inverse Agonists of ROR?t Resulting from Structure-Based Design. |
Astrazeneca |
29990434 |
24 |
Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model. |
TBA |
18341296 |
7 |
Diversity-oriented fluorescence library approach (DOFLA) to the discovery of chymotrypsin sensor. |
New York University |
16827559 |
24 |
Synthesis of tetramic and tetronic acids as beta-secretase inhibitors. |
Darmstadt Technical University |
16621571 |
29 |
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists. |
Abbott Laboratories |