196 articles for thisTarget
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Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM).
Janssen Pharmaceutica
A Prospective Virtual Screening Study: Enriching Hit Rates and Designing Focus Libraries To Find Inhibitors of PI3Kd and PI3K¿.
Janssen Pharmaceutica
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.
Janssen Pharmaceutica
1,4-Oxazineß-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Janssen Pharmaceutica
Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors.
Janssen Pharmaceutica
Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).
Janssen Pharmaceutica
Identification of a novel orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor with efficacy in animal models of schizophrenia.
Janssen Pharmaceutica
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
Janssen Pharmaceutica
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
Janssen Pharmaceutica
Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.
Janssen Pharmaceutica
Design and synthesis of bicyclic heterocycles as potent¿-secretase modulators.
Janssen Pharmaceutica
The design and synthesis of novel, phosphonate-containing transient receptor potential melastatin 8 (TRPM8) antagonists.
Janssen Pharmaceutica
Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists.
Janssen Pharmaceutica
Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.
Janssen Pharmaceutica
Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists.
Janssen Pharmaceutica
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.
Janssen Pharmaceutica
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Optimization of 1,4-Oxazine β-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Janssen Pharmaceutica
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
Janssen Pharmaceutica
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Janssen Pharmaceutica
DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLYL METHYL KETONE DERIVATIVE AND USE THEREOF
Jiangsu Nhwa Pharmaceutical Co.
Compounds, pharmaceutical compositions, and methods of preparing compounds and of their use as ATR kinase inhibitors
Repare Therapeutics
MACROCYCLIC 1,3-BRIDGED 6-CHLORO-7-PYRAZOL-4-YL-1 H-INDOLE-2-CARBOXYLATE AND 6-CHLORO-7-PYRIMIDIN-5-YL-1H-INDOLE-2-CARBOXYLATE DERIVATIVES AS MCL-1 INHIBITORS FOR THE TREATMENT OF CANCER
Janssen Pharmaceutica
PHENYLPIPERIDINE DERIVATIVES AS INHIBITORS OF GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE AND GLUTAMINYL-PEPTIDE CYCLOTRANSFERASE LIKE PROTEIN
Boehringer Ingelheim International
ALPHA PROTEIN KINASE 1 INHIBITORS FOR USE IN TREATING KAWASAKI DISEASE
Shanghai Yao Yuan Biotechnology Co.
INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE, COMPOSITIONS, AND METHODS OF USE
Bristol-Myers Squibb
ASGPR-BINDING COMPOUNDS FOR THE DEGRADATION OF EXTRACELLULAR PROTEINS
Avilar Therapeutics
BIPHENYL PYRROLIDINE AND BIPHENYL DIHYDROIMIDAZOLE DERIVATIVES FOR INHIBITING ACTIVITY OF 5-HT7 SEROTONIN RECEPTOR, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS ACTIVE INGREDIENT
Korea Institute of Science and Technology
AROMATIC ETHYLENE COMPOUND AND PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
Guangzhou Maxinovel Pharmaceuticals
ARYL SUBSTITUTED PYRROLO-PYRIDINONES AND THERAPEUTIC USES THEREOF
Bayer Aktiengesellschaft
HALOALKYLPYRIDYL TRIAZOLE MLL1-WDR5 PROTEIN-PROTEIN INTERACTION INHIBITOR
Huyabio International
Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors
D. E. Shaw Research
Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists
Chronos Therapeutics
Beta-amino acid derivative, kinase inhibitor and pharmaceutical composition containing the same, and method for performing an in vivo related application that benefits from the inhibition of a kinase
Industrial Technology Research Institute
Quinazoline compounds, preparation method, use, and pharmaceutical composition thereof
Institute of Materia Medica, Chinese Academy of Medical Sciences
Tri-substituted aryl and heteroaryl derivatives as modulators of PI3-kinase and autophagy pathways
Neuropore Therapies
Tri-substituted heteroaryl derivatives as Src homology-2 phosphatase inhibitors
Nikang Therapeutics
Imidazooxazole derivative having antitumor effect, and pharmaceutical composition including same
Korea Institute of Science and Technology
9-substituted amino triazolo quinazoline derivatives as adenosine receptor antagonists, pharmaceutical compositions and their use
Merck Sharp & Dohme
Substituted 6-(1H-pyrazol-1-yl)pyrimidin-4-amine derivatives and uses thereof
Bayer Aktiengesellschaft
N-((het)arylmethyl)-heteroaryl-carboxamides compounds as kallikrein inhibitors
Kalvista Pharmaceuticals
6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes
Sprint Bioscience
Substituted carboxamides as inhibitors of WDR5 protein-protein binding
Propellon Therapeutics
Pyrimido-diazepinone kinase scaffold compounds and methods for treating PI3K-mediated disorders
Dana-Farber Cancer Institute
Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders
AchÉ
Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient
Korea Research Institute of Chemical Technology
Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors
Merck Sharp & Dohme
Substituted fused pyrazole compounds and their use as LRRK2 inhibitors
Glaxosmithkline Intellectual Property Development
Benzothiazol compounds and methods using the same for treating neurodegenerative disorders
1St Biotherapeutics
Combinations comprising a pyrrolidine-2,5-dione IDO1 inhibitor and an anti-body
Pfizer
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
Ogeda
Bicyclic imidazole derivatives useful for the treatment of renal diseases, cardiovascular diseases and fibrotic diseases
Boehringer Ingelheim International
Oxoalkyl-substituted phenyltriazole derivatives and uses thereof
Bayer Pharma Aktiengesellschaft
Potent Noncovalent Inhibitors of the Main Protease of SARS-CoV-2 from Molecular Sculpting of the Drug Perampanel Guided by Free Energy Perturbation Calculations
Yale University
Benzimidazolone and benzothiazolone compounds and their use as AMPA receptor modulators
Janssen Pharmaceutica
Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
Abbvie
Synthesis and characterisation of two novel proton transfer compounds and their inhibition studies on carbonic anhydrase isoenzymes.
Dumlupinar University
Transition state analogues of Plasmodium falciparum and human orotate phosphoribosyltransferases.
Albert Einstein College of Medicine
FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas.
The Scripps Research Institute
Crystal structure of 3-hydroxybenzoate 6-hydroxylase uncovers lipid-assisted flavoprotein strategy for regioselective aromatic hydroxylation.
Wageningen University
Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
Jiangsu Hansoh Pharmaceutical
Synthesis, biological evaluation, and molecular docking studies of new pyrazol-3-one derivatives with aromatase inhibition activities.
Yueyang Vocational Technical College
Therapeutic compounds for blocking DNA synthesis of POX viruses
University of Pennsylvania
Boronic acid bearing liphagane compounds as inhibitors of P13K-α and/or β
Counsel of Scientific & Industrial Research
The synthesis of novel pyrazole-3,4-dicarboxamides bearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II.
Dumlupinar University
Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo.
Broad Institute
A Fungal-Selective Cytochrome bc1 Inhibitor Impairs Virulence and Prevents the Evolution of Drug Resistance.
Massachusetts Institute of Technology
Beta carboline derivatives useful in the treatment of proliferative disorders
Facultes Universitaires Notre Dame De La Paix
Cosmetic compositions containing substituted azole and methods for improving the appearance of aging skin
The Procter & Gamble
Treatment of hyperproliferative disorders with diarylhydantoin compounds
University of California
Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase
National Taiwan University
N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors
Galderma Research & Development
Synthesis, Biological Evaluation, and Molecular Docking of (R)-2-((8-(3-aminopiperidin-1-yl)-3-methyl-7-(3-methylbut-2-en-1-yl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl)methyl)benzonitrile as Dipeptidyl Peptidase IV Inhibitors.
West China Hospital
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.
Dana-Farber Cancer Institute
Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents.
Shandong University
Histone deacetylase inhibitor of benzamides and use thereof
Shanghai Institute of Pharmaceutical Industry
Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1.
University of North Carolina at Chapel Hill
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.
University of California Berkeley
[1,3,4] oxadiazole derivative and application thereof
Huazhong University of Science & Technology
Thermodynamics of binding of structurally similar ligands to histone deacetylase 8 sheds light on challenges in the rational design of potent and isozyme-selective inhibitors of the enzyme.
North Dakota State University
2,3-Dihydroquinazolin-4(1H)-one derivatives as potential non-peptidyl inhibitors of cathepsins B and H.
Kurukshetra University
6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof
Jiangsu Hengrui Medicine
Therapeutic applications in the cardiovascular field of quinazolinedione derivatives
Sanofi
Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer.
Chinese Academy of Sciences
High-speed synthesis of potent C2-symmetric HIV-1 protease inhibitors by in-situ aminocarbonylations.
Uppsala University
Human cytochrome P450 2E1 structures with fatty acid analogs reveal a previously unobserved binding mode.
The University of Kansas
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.
Takeda Pharmaceutical
Effects of hydroxybenzyl alcohols on melanogenesis in melanocyte-keratinocyte co-culture and monolayer culture of melanocytes.
National Tsing Hua University
Discovery of a small molecule PDI inhibitor that inhibits reduction of HIV-1 envelope glycoprotein gp120.
Riken Advanced Science Institute
Characterization of a tropane radioligand, [(3)H]2beta-propanoyl-3beta-(4-tolyl) tropane ([(3)H]PTT), for dopamine transport sites in rat brain.
Wake Forest University
Agonist high and low affinity state ratios predict drug intrinsic activity and a revised ternary complex mechanism at serotonin 5-HT(2A) and 5-HT(2C) receptors.
Albany Medical College
Novel structure having antagonist actions at both the glycine site of the N-methyl-D-aspartate receptor and neuronal voltage-sensitive sodium channels: biochemical, electrophysiological, and behavioral characterization.
University of Colorado
Comparison of the pharmacological properties of cloned rat, human, and bovine norepinephrine transporters.
The University of Queensland
Pharmacological characterization of nicotine's interaction with cocaine and cocaine analogs.
Virginia Commonwealth University
Characterization of (2S,2'R,3'R)-2-(2',3'-[3H]-dicarboxycyclopropyl)glycine binding in rat brain.
F. Hoffmann-La Roche
Ortho- and para-(Difuoromethyl)aryl-beta-D-glucosides: A new class of enzyme-activated irreversible inhibitors of beta-glucosidases
Merrell Dow Research Institute
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: indazole and benzimidazolone derivatives.
Eli Lilly
Pharmacological profile of antidepressants and related compounds at human monoamine transporters.
Mayo Clinic
(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist.
Smithkline Beecham Pharmaceuticals
[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits.
National Institute of Diabetes and Digestive and Kidney Diseases
Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs.
TBA
Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.
Duke University
Prostacyclin receptors of a neuronal hybrid cell line. Divalent citations and ligand-receptor coupling.
Royal Postgraduate Medical School
Pyrone-based inhibitors of metalloproteinase types 2 and 3 may work as conformation-selective inhibitors.
University of California San Diego
Psychotomimetic opiate receptors labeled and visualized with (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine.
TBA
CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activity.
Ciba-Geigy
Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases.
The Johns Hopkins University
Sequencing, modeling, and selective inhibition of Trypanosoma brucei hexokinase.
Universite Paul Sabatier
De Novo Parallel Design, Synthesis and Evaluation of Inhibitors against the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 and Drug-Resi
Bar-Ilan University
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Bristol-Myers Squibb Pharmaceutical Research Institute