237 articles for thisTarget
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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
Incyte
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.
Incyte
Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Incyte
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Incyte
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Incyte
Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer.
Incyte
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.
Incyte
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Incyte
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.
Incyte
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
Incyte
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Incyte
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.
Incyte
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Incyte
Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
Incyte
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Incyte
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Incyte
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Incyte
NOVEL MODULATORS OF THE 5-HYDROXYTRYPTAMINE RECEPTOR 7 AND THEIR METHOD OF USE
Temple University
HIGH-AFFINITY LIGANDS OF FIBROBLAST ACTIVATION PROTEIN FOR TARGETED DELIVERY APPLICATIONS
Philochem
7-, 8-, and 10-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use
Merck Sharp & Dohme
SUBSTITUTED OXOPYRIDINE DERIVATIVES FOR THE TREATMENT AND/OR PROPHYLAXIS OF THROMBOTIC OR THROMBOEMBOLIC DISORDERS AND/OR THROMBOTIC OR THROMBOEMBOLIC COMPLICATIONS
Bayer Aktiengesellschaft
Compound containing structure of a heteroaromatic ring, pharmaceutical composition thereof and application thereof
Shanghai Yingli Pharmaceutical Co.
3-CYCLOAMINO-INDOLE COMPOUNDS AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Mindset Pharma
Triazole bisphosphonate geranylgeranyl diphosphate synthase inhibitors
University of Nebraska
INHIBITION OF nSMase FOR THE TREATMENT OF HUMAN IMMUNODEFICIENCY VIRUS INFECTION
The Johns Hopkins University
CARBORANE HYDROXAMIC ACID MATRIX METALLOPROTEINASE INHIBITORS AND AGENTS FOR BORON NEUTRON CAPTURE THERAPY
Loyola University Of Chicago
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.
Ontario Institute for Cancer Research
COMPOSITIONS AND METHODS FOR THE TREATMENT AND PREVENTION OF NEUROLOGICAL DISORDERS
Kineta
4-ALKOXYPYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF
Biosplice Therapeutics
TRIAZOLE DERIVATIVES AND THEIR USE AS TANKYRASE INHIBITORS
Oslo Universitetssykehus
Carboxylic acid, acyl sulfonamide and acyl sulfamide-derivatized bicyclic aza-heteroaromatics as selective Mcl-1 inhibitors and as dual Mcl-1/Bcl-2 inhibitors
University of Maryland, Baltimore
5-substituted difluoropiperidine compounds with blood-brain barrier penetrable capability
Wayshine Biopharm Holding
Heterocyclic compounds, preparation methods therefor, and methods of uses thereof
Inventisbio
Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors
Astrazeneca
Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
Hoffmann-La Roche
Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders
Mindset Pharma
Methods of treatment using 4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators
Heptares Therapeutics
Triazolopyrimidine derivatives for use as ghrelin o-acyl transferase (GOAT) inhibitors
Boehringer Ingelheim International
Amide compounds as kinase inhibitors, compositions and methods of treatment
Translational Drug Development
Combination of pure 5-HT6 receptor antagonists with acetylcholinesterase inhibitors
Suven Life Sciences
Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors
Shenzhen Targetrx
Substituted 1,2,3,4-tetrahydroquinolines as inhibitors of repair enzyme 8-oxoguanine deoxyribonucleic acid glycosylase activity
The Leland Stanford Junior University
Bromodomain inhibitor compound and use thereof
Shanghai Institute of Material Medica, Chinese Academy of Sciences
Alcoxyamino derivatives for treating pain and pain related conditions
Esteve Pharmaceuticals
1,4-substituted isoquinoline inhibitors of KEAP1/NRF2 protein-protein interaction
University of Illinois
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
Beijing Tide Pharmaceutical
2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
Beijing Scitech Mq Pharmaceuticals
Imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase
University of Alberta
Composition for inhibiting growth of SARS-CoV-2 and method of preparing the same
Medicare Pharmaceuticals
Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having HIV integrase inhibitory activity
Shionogi
Phenylpyrazolylacetamide compounds and derivatives as CDK8/CDK19 inhibitors
Boehringer Ingelheim International
Substituted heterocyclyl derivatives as CDK inhibitors
Aurigene Discovery Technologies
4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament
Boehringer Ingelheim International
Substituted imidazoles as apoptosis signal regulating kinase 1 inhibitors
Jiangsu Hansoh Pharmaceutical Group
Processes for the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[B]indol-3-yl)acetic acid and salts thereof
Arena Pharmaceuticals
Substituted N-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
Sanofi
4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament
Boehringer Ingelheim International
Pyrimidine derivative compound, optical isomer thereof, or pharmaceutically acceptable salt thereof, and composition for preventing or treating Tyro 3 related disease comprising same as active ingredient
Korea Research Institute of Chemical Technology
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Arena Pharmaceuticals
1H-pyrrolo[2,3-c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
Incyte
2-oxoquinazoline derivatives as methionine adenosyltransferase 2A inhibitors
Ideaya Biosciences
Imidazopiperazine inhibitors of transcription activating proteins
University Of Texas
Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
Arvinas Operations
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors
Eli Lilly
Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
Legochem Biosciences
Quinoline and isoquinoline derivatives for treating pain and pain related conditions
Esteve Pharmaceuticals
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors
Boehringer Ingelheim International
Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same
Mebias Discovery
Crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
Kronos Bio
Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of ASGPR
Pfizer
Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use
Merck Sharp & Dohme
Use of agonists of formyl peptide receptor 2 for treating dermatological diseases
Allergan
2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases
Array Biopharma
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors
Boehringer Ingelheim International
Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones and their use as GluN2B receptor modulators
Janssen Pharmaceutica
Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
Boehringer Ingelheim International
Non-aromatic difluoro analogues of resorcylic acid lactones
University of North Carolina At Greensboro
Inhibitors of fatty acid amide hydrolase (FAAH) enzyme with improved oral bioavailability and their use as medicaments
University of California
Inhibitors of ACK1/TNK2 tyrosine kinase
H. Lee Moffitt Cancer Center and Research Institute
(Thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists
Eli Lilly
Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
Euroscreen
Substituted azoles, antiviral active component, pharmaceutical composition, method for preparation and use thereof
TBA
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
Merck Sharp & Dohme
Kinetic and in silico analysis of thiazolidin-based inhibitors of a-carbonic anhydrase isoenzymes.
Ondokuz Mayis University
Alpha-(3,5-dimethoxybenzylidene)-alpha′-hydrocarbyl methylene cyclic ketone and preparation method thereof
Pharmaxyn Laboratories
Diamide compounds having muscarinic receptor antagonist and BETA2 adrenergic receptor agonist activity
Theravance Respiratory
Synthesis and carbonic anhydrase inhibitory properties of novel coumarin derivatives.
Inonu University
Pyrimidinyl-pyridazinone derivatives for treating a disease which is influenced by inhibition of met kinase
Merck Patent
Substituted 1,2,3,4-tetrahydropyrido[3,4-E] pyrrolo[1,2-A]pyrimidines as kinase
Allergan
Synthesis and structure-activity relationship of novel conformationally restricted analogues of serotonin as 5-HT6 receptor ligands.
Suven Life Sciences
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
Galderma Research & Devlopment
Hetarylcoumarins: Synthesis and biological evaluation as potent a-glucosidase inhibitors.
Kinnaird College For Women
In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth.
Harvard School of Public Health
Inhibition of the ribonuclease H activity of HIV-1 reverse transcriptase by GSK5750 correlates with slow enzyme-inhibitor dissociation.
Mcgill University
Studies of the Binding of Modest Modulators of the Human Enzyme, Sirtuin 6, by STD NMR.
University At Albany
Synthesis and biological evaluation of benzimidazole derivatives as the G9a Histone Methyltransferase inhibitors that induce autophagy and apoptosis of breast cancer cells.
Shenyang Pharmaceutical University
Delineation of the Pasteurellaceae-specific GbpA-family of glutathione-binding proteins.
Ghent University
Design, synthesis, molecular docking, anti-Proteus mirabilis and urease inhibition of new fluoroquinolone carboxylic acid derivatives.
Minia University
A L-lysine transporter of high stereoselectivity of the amino acid-polyamine-organocation (APC) superfamily: production, functional characterization, and structure modeling.
Max Planck Institute of Biophysics
The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9.
Georg-August-University of Goettingen
Urea derivatives and their use as fatty-acid binding protein (FABP) inhibitors
Hoffmann-La Roche
C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Merck Sharp & Dohme
Histone deacetylase 6 structure and molecular basis of catalysis and inhibition
University of Pennsylvania
Some Anticancer Agents Act on Human Serum Paraoxonase-1 to Reduce Its Activity.
Ahi Evran University
2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-YL)picolinamide derivatives as orexin receptor antagonists
Actelion Pharmaceuticals
Tri-aryl/heteroaromatic cannabinoids and use thereof
The University of Tennessee Research Foundation
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
German Cancer Research Center (Dkfz)
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
University of Toronto
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies
Galderma Research & Development
Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
Boehringer Ingelheim International
Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor
Taiho Pharmaceutical
Structure-guided design of a high affinity inhibitor to human CtBP.
University of Massachusetts Medical School
Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
University of South Florida
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors.
University of North Carolina
Design and synthesis of conformationally constrained cyclophilin inhibitors showing a cyclosporin-A phenotype in C. elegans.
The University of Edinburgh
Heteroaryl substituted pyridyl compounds useful as kinase modulators
Bristol-Myers Squibb
Benzenesulfonamide derivatives as inverse agonists of retinoid-related orphan receptor gamma (RORγ(T))
Galderma Research & Development
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Pfizer
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Merck Frosst Canada
Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis.
Hong Kong University of Science and Technology
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.
Schering-Plough Research Institute
DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS
Parke-Davis Pharmaceutical Research