The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27815118 |
112 |
Discovery of phenoxyindazoles and phenylthioindazoles as ROR¿ inverse agonists. |
Galderma R & D |
| 27043267 |
51 |
Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new ROR¿ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation. |
Jilin University |
| 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 |
| 26396680 |
6 |
RORc Modulators for the Treatment of Autoimmune Diseases. |
Therachem Research Medilab (India) |
| 26321361 |
56 |
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists. |
Genentech |
| 26191367 |
39 |
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR¿t Inhibitors. |
Fudan University |
| 26277758 |
48 |
Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR¿t inverse agonists. |
Fudan University |
| 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 |
| 25815138 |
58 |
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action. |
Genentech |
| 25840886 |
25 |
Discovery of 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide analogs as new RORC modulators. |
Boehringer Ingelheim Pharmaceuticals |
| 25147600 |
8 |
ROR¿t Modulators Are Potentially Useful for the Treatment of the Immune-Mediated Inflammatory Diseases. |
Therachem Research Medilab (India) |
| 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 |
| 24704616 |
86 |
Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new ROR¿ inhibitors using virtual screening, synthesis and biological evaluation. |
Chinese Academy of Sciences |
| 24559867 |
6 |
Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors. |
The University of Tokyo |
| 24900774 |
40 |
Discovery of Tertiary Amine and Indole Derivatives as Potent ROR?t Inverse Agonists. |
Glaxosmithkline |
| 24388993 |
76 |
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent ROR¿t inhibitors. |
Glaxosmithkline |
| 24239186 |
84 |
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc. |
Genentech |
| 24040486 |
30 |
Identification of Potent and Selective Diphenylpropanamide ROR? Inhibitors. |
New York University School of Medicine |
| 23232056 |
16 |
Small molecule amides as potent ROR-¿ selective modulators. |
The Scripps Research Institute |
| 32334911 |
22 |
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists. |
Bristol Myers Squibb |
| 32005415 |
81 |
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR?t. |
Reata Pharmaceuticals |
| 32334912 |
130 |
Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach. |
Phenex Pharmaceuticals |
| 32336498 |
324 |
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 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 |
| 27542308 |
8 |
Recent progress on nuclear receptor ROR? modulators. |
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 |
| 31821760 |
53 |
Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Inverse Agonists. |
Technische Universiteit Eindhoven |
| 30652849 |
28 |
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor ?t (ROR?t) Agonist Structure-Based Functionality Switching Approach from In House ROR?t Inverse Agonist to ROR?t Agonist. |
Takeda Pharmaceutical |
| 31425906 |
52 |
Discovery of aryl-substituted indole and indoline derivatives as ROR?t agonists. |
Fudan University |
| 31272795 |
154 |
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions. |
Advinus Therapeutics |
| 32292560 |
15 |
Discovery of [1,2,4]Triazolo[1,5- |
Teijin Pharma |
| 31010722 |
69 |
3-Substituted Quinolines as ROR?t Inverse Agonists. |
Janssen Research and Development |
| 30891142 |
121 |
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists. |
Bristol-Myers Squibb |
| 30743096 |
36 |
Discovery of N-indanyl benzamides as potent ROR?t inverse agonists. |
Fudan University |
| 32071676 |
52 |
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR??t Allosteric Inhibitors for Autoimmune Diseases |
Merck |
| 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 |
| 30143422 |
49 |
Identification of potent ROR? modulators: Scaffold variation. |
The Scripps Research Institute |
| 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 |
| 29477813 |
4 |
Targeting RORs nuclear receptors by novel synthetic steroidal inverse agonists for autoimmune disorders. |
University of Padova |
| 29342416 |
54 |
Identification of novel quinazolinedione derivatives as ROR?t inverse agonist. |
Takeda Pharmaceutical |
| 29477887 |
27 |
Discovery of carbazole carboxamides as novel ROR?t inverse agonists. |
Fudan University |
| 29262987 |
44 |
Discovery of orally efficacious ROR?t inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds. |
Takeda Pharmaceutical |
| 29258712 |
32 |
Discovery of orally efficacious ROR?t inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives. |
Takeda Pharmaceutical |
| 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 |
| 29079472 |
66 |
6-Substituted quinolines as ROR?t inverse agonists. |
Janssen Research and Development |
| 29909341 |
4 |
Identification of fused pyrimidines as interleukin 17 secretion inhibitors. |
Norwegian University of Science and Technology |
| 30095900 |
109 |
Potent and Orally Bioavailable Inverse Agonists of ROR?t Resulting from Structure-Based Design. |
Astrazeneca |
| 30034593 |
58 |
Novel Nonsteroidal Progesterone Receptor (PR) Antagonists with a Phenanthridinone Skeleton. |
The University of Tokyo |
| 29456799 |
30 |
From ROR?t Agonist to Two Types of ROR?t Inverse Agonists. |
Fudan University |
| 29990434 |
24 |
Optimizing a Weakly Binding Fragment into a Potent ROR?t Inverse Agonist with Efficacy in an in Vivo Inflammation Model. |
TBA |
| 29412659 |
15 |
Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy. |
Fudan University |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 28318945 |
68 |
Identification and structure activity relationships of quinoline tertiary alcohol modulators of ROR?t. |
Janssen Pharmaceutica |
| 10454469 |
6 |
Native gamma-aminobutyric acid type A receptors from rat hippocampus, containing both alpha 1 and alpha 5 subunits, exhibit a single benzodiazepine binding site with alpha 5 pharmacological properties. |
Universidad De Sevilla |
| 3033464 |
11 |
Characterization of the binding of a morphine (mu) receptor-specific ligand: Tyr-Pro-NMePhe-D-Pro-NH2, [3H]-PL17. |
Burroughs Wellcome |
| 1930610 |
41 |
Affinities of fluoxetine, its enantiomers, and other inhibitors of serotonin uptake for subtypes of serotonin receptors. |
Eli Lilly |
| 16183025 |
6 |
Structure-based discovery of a boronic acid bioisostere of combretastatin A-4. |
University of Virginia |
| 11590022 |
13 |
Predicting and harnessing protein flexibility in the design of species-specific inhibitors of thymidylate synthase. |
University of California San Francisco |
| 9818151 |
33 |
Design and selection of DMP 850 and DMP 851: the next generation of cyclic urea HIV protease inhibitors. |
Dupont Pharmaceuticals |
| 19767211 |
20 |
Synthesis and structure-activity relationships of dehydroaltenusin derivatives as selective DNA polymerase alpha inhibitors. |
Kyoto Prefectural University |
| 19256508 |
25 |
Novel adenosine-derived inhibitors of 70 kDa heat shock protein, discovered through structure-based design. |
Vernalis (R&D) |
| 15826183 |
33 |
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction. |
Yale University |
| 16630722 |
13 |
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists. |
Johnson & Johnson Pharmaceutical |
| 16078828 |
25 |
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone. |
Inotek Pharmaceuticals |
| 15947036 |
80 |
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. |
Vrije Universiteit Amsterdam |
| 16621571 |
29 |
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists. |
Abbott Laboratories |
| 18154266 |
3 |
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects. |
University of Central Florida College of Medicine |
| 17531483 |
39 |
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. |
Berlex Biosciences |
| 10387041 |
7 |
Molecular recognition of macrocyclic peptidomimetic inhibitors by HIV-1 protease. |
University of Queensland |
| 10866394 |
30 |
Carbocyclic influenza neuraminidase inhibitors possessing a C3-cyclic amine side chain: synthesis and inhibitory activity. |
Gilead Sciences |
| 10522696 |
8 |
Stereospecific synthesis of a GS 4104 metabolite: determination of absolute stereochemistry and influenza neuraminidase inhibitory activity. |
Gilead Sciences |
| 11495584 |
76 |
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity. |
Wyeth-Ayerst Research |
| 11931611 |
7 |
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase. |
Sapienza University of Rome |
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