212 articles for thisTarget
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Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.
Merck
Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Merck
The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.
Merck
Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates.
Merck
Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists.
Merck
p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.
Merck
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Merck
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Merck
Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.
Merck
Discovery of Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with
Merck
Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Merck
Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.
Merck
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Merck
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.
Merck
Synthesis and optimization of N-heterocyclic pyridinones as catechol-O-methyltransferase (COMT) inhibitors.
Merck
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.
Merck
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.
Merck
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Merck
Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms.
Merck
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Merck
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.
Merck
(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.
Merck
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Merck
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Merck
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Merck
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Merck
An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration.
Merck
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.
Merck
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Merck
Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.
Merck
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Merck
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
Merck
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Merck
Thiophenyl oxime-derived phosphonates as nano-molar class C beta-lactamase inhibitors reducing MIC of imipenem against Pseudomonas aeruginosa and Acinetobacter baumannii.
Merck
Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
Merck
Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1.
Merck
Spiroimidazolidinone NPC1L1 inhibitors. Part 2: structure-activity studies and in vivo efficacy.
Merck
Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.
Merck
4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: first boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity.
Merck
Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.
Merck
Spiroimidazolidinone NPC1L1 inhibitors. 1: Discovery by 3D-similarity-based virtual screening.
Merck
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Merck
Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.
Merck
2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.
Merck
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Merck
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.
Merck
Discovery of MK-1468: A Potent, Kinome-Selective, Brain-Penetrant Amidoisoquinoline LRRK2 Inhibitor for the Potential Treatment of Parkinson's Disease.
Merck
Bradykinin B1 antagonists: biphenyl SAR studies in the cyclopropanecarboxamide series.
Merck
Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator.
Merck
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
Merck
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Merck
Discovery of non-boronic acid Arginase 1 inhibitors through virtual screening and biophysical methods.
Merck
Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1
Merck
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Merck
Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models.
Merck
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Merck
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Merck
Structure activity relationship of N-1 substituted 1,5-naphthyrid-2-one analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-9).
Merck
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.
Merck
Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.
Merck
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Merck
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i).
Merck
Discovery of Insulin/GLP-1/Glucagon Triagonists for the Treatment of Diabetes and Obesity.
Merck
Optimization and Mechanistic Investigations of Novel Allosteric Activators of PKG1α.
Merck
p38 MAP kinase inhibitors: metabolically stabilized piperidine-substituted quinolinones and naphthyridinones.
Merck
Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome.
Merck
Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology.
Merck
Phe19 modification of HDM2-p53 PPI inhibitors to alleviate CYP3A4 metabolism/mechanism-based inhibition liability.
Merck
The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.
Merck
Discovery of MK-1462: GLP-1 and Glucagon Receptor Dual Agonist for the Treatment of Obesity and Diabetes.
Merck
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Merck
Diminishing GSH-Adduct Formation of Tricyclic Diazepine-based Mutant IDH1 Inhibitors.
Merck
Chlorothiophenecarboxamides as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Merck
Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Merck
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.
Merck
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.
Merck
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Merck
Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa.
Merck
Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.
Merck
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Merck
Discovery of the First Non-cGMP Mimetic Small Molecule Activators of cGMP-Dependent Protein Kinase 1 α (PKG1α).
Merck
Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.
Merck
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Merck
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.
Merck
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.
Merck
Rapid Evaluation of Small Molecule Cellular Target Engagement with a Luminescent Thermal Shift Assay.
Merck
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.
Merck
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.
Merck
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.
Merck
Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Merck
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold.
Merck
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
Merck
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.
Merck
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Merck
Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.
Merck
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Merck
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Merck
Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors.
Merck
Fragment-based lead discovery of a novel class of small molecule antagonists of neuropeptide B/W receptor subtype 1 (GPR7).
Merck
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores.
Merck
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
Merck
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Merck
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Merck
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.
Merck
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Merck
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.
Merck
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Merck
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Merck
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.
Merck
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
Merck
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).
Merck
Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.
Merck
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.
Merck
Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.
Merck
Discovery of novel pan-genotypic HCV NS5A inhibitors containing a novel tetracyclic core.
Merck
5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.
Merck
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Merck
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).
Merck
Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.
Merck
Benzofuro[3,2-b]pyridines as mixed ET(A)/ET(B) and selective ET(B) endothelin receptor antagonists.
Merck
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.
Merck
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Merck
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
Merck
Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster.
Merck
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Merck
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.
Merck
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Merck
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR��t Allosteric Inhibitors for Autoimmune Diseases
Merck
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.
Merck
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
Merck
Design and evaluation of novel tetracyclic benzofurans as palm site allosteric inhibitors of HCV NS5B polymerase.
Merck
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
Merck
Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.
Merck
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Merck
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Merck
Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.
Merck
Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.
Merck
Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.
Merck
Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor.
Merck
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Merck
The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Merck
The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh
Merck
Concise syntheses and HCV NS5B polymerase inhibition of (2'R)-3 and (2'S)-2'-ethynyluridine-10 and related nucleosides.
Merck
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.
Merck
Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.
Merck
Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.
Merck
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
Merck
MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.
Merck
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.
Merck
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Merck
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Merck
Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.
Merck
Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts.
Merck
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.
Merck
