140 articles for thisTarget
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Discovery of a 2'-fluoro-2'-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties.
Gilead Sciences
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
Gilead Sciences
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
Gilead Sciences
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Gilead Sciences
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kd Selective Inhibitors.
Gilead Sciences
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
Gilead Sciences
Highly Selective Phosphatidylinositol 4-Kinase IIIß Inhibitors and Structural Insight into Their Mode of Action.
Gilead Sciences
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Gilead Sciences
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350).
Gilead Sciences
Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region.
Gilead Sciences
Identification and optimization of pteridinone Toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis.
Gilead Sciences
Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1.
Gilead Sciences
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
Gilead Sciences
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.
Gilead Sciences
GS-9191 is a novel topical prodrug of the nucleotide analog 9-(2-phosphonylmethoxyethyl)guanine with antiproliferative activity and possible utility in the treatment of human papillomavirus lesions.
Gilead Sciences
Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Gilead Sciences
Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.
Gilead Sciences
Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.
Gilead Sciences
Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors.
Gilead Sciences
Phosphonic acid-containing analogues of mycophenolic acid as inhibitors of IMPDH.
Gilead Sciences
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I
Gilead Sciences
Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.
Gilead Sciences
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
Gilead Sciences
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Gilead Sciences
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Gilead Sciences
Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi
Gilead Sciences
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Gilead Sciences
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Gilead Sciences
Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor.
Gilead Sciences
New series of potent, orally bioavailable, non-peptidic cyclic sulfones as HIV-1 protease inhibitors.
Gilead Sciences
Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Gilead Sciences
Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1.
Gilead Sciences
Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase.
Gilead Sciences
Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.
Gilead Sciences
Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor.
Gilead Sciences
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Gilead Sciences
Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.
Gilead Sciences
USE OF SOS1 INHIBITORS TO TREAT MALIGNANCIES WITH SHP2 MUTATIONS
Revolution Medicines
3-ARYLOXYL-3-FIVE-MEMBERED HETEROARYL PROPYLAMINE COMPOUND AND USE THEREOF
Shanghai Leado Pharmatech Co.
PYRAZOLOTHIAZOLE CARBOXAMIDES AND THEIR USES AS PDGFR INHIBITORS
Actelion Pharmaceuticals
PYRAZOLO DERIVATIVES AS HUMAN DIHYDROOROTATE DEHYDROGENASE (HDHODH) INHIBITORS FOR USE AS ANTIVIRALS
Drug Discovery and Clinic
SUBSTITUTED DIARYLAMINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
Suzhou Yabao Pharmaceutical R&D
INDOLO HEPTAMYL OXIME ANALOG CRYSTAL AS PARP INHIBITOR AND METHOD FOR PREPARING SAME
Chia Tai Tianqing Pharmaceutical Group
Cyclic ether derivatives of pyrazolo[1,5-A]pyrimidine-3-carboxyamide
Boehringer Ingelheim International
Indazoles as hematopoietic progenitor kinase 1 (HPK1) inhibitors and methods using same
1St Biotherapeutics
Selective D3 dopamine receptor agonists and methods of their use
The United States of America, As Represented By The Secretary, Department of Health and Human Services
Synthesis of peptide borate ester compound and use thereof
Jiangsu Chia Tai Fenghai Pharmaceutical
Pharmaceutical compounds for treatment of medical disorders
Achillion Pharmaceuticals
Heteroaryl amide derivatives as selective inhibitors of histone deacetylases 1 and/or 2(HDAC1-2)
Medibiofarma
Imidazopyridinyl compounds and use thereof for treatment of neurodegenerative disorders
1St Biotherapeutics
Protein kinase inhibitors, preparation method and medical use thereof
Gan & Lee Pharmaceuticals
Bicyclic nitrogen-containing heterocyclic derivatives and pharmaceutical composition comprising the same
Shionogi
Urea-substituted aromatic ring-linked dioxane-quinazoline and -linked dioxane-quinoline compounds, preparation method therefor and use thereof
Beijing Scitech-Mq Pharmaceuticals
Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
Array Biopharma
Matrix metalloproteinase (MMP) inhibitors and methods of use thereof
Foresee Pharmaceuticals
N-(phenylsulfonyl)benzamides and related compounds as bcl-2 inhibitors
The Regents of The University of Michigan
Substituted pyrazolo[l,5-a]pyrimidine compounds as Trk kinase inhibitors
Array Biopharma
FGFR3 fusion gene and pharmaceutical drug targeting same
Chugai Seiyaku Kabushiki Kaisha
Substituted pyrrolidines as factor XIa inhibitors for the treatment thromboembolic diseases
Ono Pharmaceutical
Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof
Arromax Pharmatech
Histone deacetylase inhibitors and compositions and methods of use thereof
Chdi Foundation
Design, synthesis and biological evaluation of novel inosine 5'-monophosphate dehydrogenase (IMPDH) inhibitors.
Nycomed
(3,4-Dihydroxyphenyl)(2,3,4-trihydroxyphenyl)methanone and its derivatives as carbonic anhydrase isoenzymes inhibitors.
Ataturk University
Dihalogenated sulfanilamides and benzolamides are effective inhibitors of the three ß-class carbonic anhydrases from Mycobacterium tuberculosis.
Universit�� Degli Studi Di Firenze
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Abbvie
Fused heteroaryl pyridyl and phenyl benzenesuflonamides as CCR2 modulators for the treatment of inflammation
Chemocentryx
Effects of dopaminergic compounds on carbonic anhydrase isozymes I, II, and VI.
Agri Ibrahim Cecen University
Substituted quinolines as bruton's tyrosine kinases inhibitors
Hangzhouderenyucheng Biotechnology
Differential Coupling of Binding, ATP Hydrolysis, and Transport of Fluorescent Probes with P-Glycoprotein in Lipid Nanodiscs.
University of Washington
An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms.
Universitätsklinikum Frankfurt
Optically active diazabicyclooctane derivatives and process for preparing the same
Meiji Seika Pharma
Orally available viridiofungin derivative possessing anti-HCV activity
Chugai Seiyaku Kabushiki Kaisha
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia
Albert Einstein College of Medicine
Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.
Beni-Suef University
Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
Senhwa Biosciences
Bivalent ligands for the treatment of neurological disorders
Virginia Commonwealth University
Pyrazolopyrimidines as metabotropic glutamate 5 receptor antagonists
Boehringer Ingelheim International
(4-{4-[5-(benzooxazol-2-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid useful for treating or preventing conditions or disorders associated with DGAT1 activity
Novartis
Cytoskeletal active rho kinase inhibitor compounds, composition and use
Inspire Pharmaceuticals
Farnesyl diphosphate synthase inhibitors from in silico screening.
University of California San Diego
Targeting Tumour Proliferation with a Small-Molecule Inhibitor of AICAR Transformylase Homodimerization.
University of Southampton
Selective COX-2 inhibition and cardiovascular effects: a review of the rofecoxib development program.
University of Maryland Hospital
Development and biological evaluation of a novel aurora A kinase inhibitor.
Parc De Recerca Biomedica De Barcelona
[125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors.
U. 109
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins.
Center For Bio-Pharmaceutical Sciences
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands.
Purdue University