140 articles for thisTarget
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Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors.
Nanjing Chia-Tai Tianqing Pharmaceutical
Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.
Sun Yat-Sen University
Multiparameter Optimization of Naphthyridine Derivatives as Selective ?5-GABA
Gedeon Richter
Design of a Potent, Selective, and Brain-Penetrant Inhibitor of Wnt-Deactivating Enzyme Notum by Optimization of a Crystallographic Fragment Hit.
University College London
A Series of Substituted Bis-Aminotriazines Are Activators of the Natriuretic Peptide Receptor C.
University College London
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
Korea Research Institute of Chemical Technology
Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Bristol-Myers Squibb
Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.
Shenyang Pharmaceutical University
Discovery of Potential Neuroprotective Agents against Paclitaxel-Induced Peripheral Neuropathy.
National Cheng Kung University
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Novartis Institutes For Biomedical Research
Identification of triazolopyridine derivatives as a new class of AhR agonists and evaluation of anti-psoriasis effect in a mouse model.
Sichuan University
Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
Shandong University
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase ? (PI3K?).
Arcus Biosciences
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.
Zhuhai United Laboratories
Discovery of Novel Orally Bioavailable Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo.
Tongji University
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
Shanghai Institute of Materia Medica
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3K?.
Genentech
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.
Shanghai Institute of Materia Medica
Design, Synthesis, and Structure-Activity Relationship Studies of Bisamide Derivatives of Amphotericin B with Potent Efficacy and Low Toxicity.
Shanghai Institute of Materia Medica
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead
Merck Healthcare
Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4.
Bristol-Myers Squibb Research & Early Development
Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis.
Biocon-Bristol Myers Squibb Research and Development Center
Identification of novel indole derivatives as highly potent AMPK activators with anti-diabetic profiles.
Shionogi
Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD).
Wuxi Apptec
Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer.
Eternity Bioscience
Discovery and optimization of cyclohexane-1,4-diamines as allosteric MALT1 inhibitors.
Astrazeneca
Discovery of Substituted Di(pyridin-2-yl)-1,2,4-thiadiazol-5-amines as Novel Macrofilaricidal Compounds for the Treatment of Human Filarial Infections.
Bristol Myers Squibb
Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors
Shandong University
GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Constellation, A Morphosys
-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Janssen Research and Development
Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
Sichuan University
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.
Shenyang Pharmaceutical University
The development of HEC-866 and its analogues for the treatment of idiopathic pulmonary fibrosis.
Hec Pharma.
Improving the treatment of Parkinson's disease: Structure-based development of novel 5-HT
Yantai University
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction.
Astrazeneca
Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[
Guangzhou University of Chinese Medicine
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.
Incyte
Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies.
Epizyme
The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery.
University of Helsinki
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Bristol Myers Squibb Research and Early Development
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT
Hec Pharm Group
4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors.
Cardiff University
Discovery of novel biphenyl-substituted pyridone derivatives as potent non-nucleoside reverse transcriptase inhibitors with promising oral bioavailability.
Yanbian University College of Pharmacy
Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
Wuxi Apptec
Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
Wuxi Apptec
Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Crinetics Pharmaceuticals
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.
Universitat De Barcelona
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-Tyr
East China Normal University
Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease.
Pharmaxis
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Deciphera Pharmaceuticals
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).
Deciphera Pharmaceuticals
Discovery of benzodioxane analogues as lead candidates of AIMP2-DX2 inhibitors.
Institut Pasteur Korea
Potent and selective TYK2-JH1 inhibitors highly efficacious in rodent model of psoriasis.
Nimbus Therapeutics
Structure-Activity Studies of 1
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.
Pfizer
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.
East China Normal University
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Bristol Myers Squibb
Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
Carna Biosciences
Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.
Biogen
Discovery of SHR2415, a Novel Pyrrole-Fused Urea Scaffold ERK1/2 Inhibitor.
Shanghai Hengrui Pharmaceutical
Discovery of SHR5133, a Highly Potent and Novel HBV Capsid Assembly Modulator.
Shanghai Hengrui Pharmaceutical
Discovery of a Partial Glucokinase Activator Clinical Candidate: Diethyl ((3-(3-((5-(Azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-isopropoxybenzamido)-1
Bristol Myers Squibb
Synthesis and Evaluation of Novel Tetrahydronaphthyridine CXCR4 Antagonists with Improved Drug-like Profiles.
Emory University
Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer.
Guizhou Medical University
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of Non-Nucleotide Small-Molecule STING Agonists
Bristol Myers Squibb Research and Development
Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
Fudan University
Enhancing monoamine oxidase B inhibitory activity via chiral fluorination: Structure-activity relationship, biological evaluation, and molecular docking study.
Central China Normal University
Synthesis, biological, and structural explorations of a series of ?-opioid receptor (MOR) agonists with high G protein signaling bias.
Yantai University
Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.
Shenyang Pharmaceutical University
Identification of a Novel 2,8-Diazaspiro[4.5]decan-1-one Derivative as a Potent and Selective Dual TYK2/JAK1 Inhibitor for the Treatment of Inflammatory Bowel Disease.
Sichuan University and Collaborative Innovation Center of Biotherapy
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid ? In Vivo.
Janssen Research & Development
Discovery of spiro amide SHR902275: A potent, selective, and efficacious RAF inhibitor targeting RAS mutant cancers.
Eternity Bioscience
Discovery of a First-in-Class Inhibitor of the Histone Methyltransferase SETD2 Suitable for Preclinical Studies.
Epizyme
Synthesis, Characterization, and Preclinical Evaluation of a Small-Molecule Prostate-Specific Membrane Antigen-Targeted Monomethyl Auristatin E Conjugate.
Lomonosov Moscow State University
Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA
Bristol Myers Squibb
Discovery of the Next-Generation Pan-TRK Kinase Inhibitors for the Treatment of Cancer.
Yantai University
Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
Fudan University
Dynamics-Based Discovery of Novel, Potent Benzoic Acid Derivatives as Orally Bioavailable Selective Estrogen Receptor Degraders for ER?+ Breast Cancer.
Nanjing University of Chinese Medicine
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Shionogi
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Janssen Research & Development
Discovery of a Series of Hydroxamic Acid-Based Microtubule Destabilizing Agents with Potent Antitumor Activity.
West China Hospital of Sichuan University
Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT
Jagiellonian University Medical College
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Glaxosmithkline
Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.
Shenyang Pharmaceutical University
Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with
The Ohio State University
Discovery of the Oxadiazine FRM-024: A Potent CNS-Penetrant Gamma Secretase Modulator.
Forum Pharmaceuticals
Discovery of VU6028418: A Highly Selective and Orally Bioavailable M
Vanderbilt University
Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.
Newlink Genetics
Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective
Northeastern University
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous
Agios Pharmaceuticals
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3K? Immunomodulators.
Merck
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Drugs For Neglected Diseases Initiative (Dndi)
Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas.
Chinese Academy of Sciences
Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy.
Cytokinetics
AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Astrazeneca
Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.
Shenyang Pharmaceutical University
Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
Yantai University
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.
University of Tennessee Health Science Center
Discovery of the Selective Protein Kinase C-? Kinase Inhibitor, CC-90005.
Bristol Myers Squibb
GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.
Genentech
Discovery of 4-aminopyrimidine analogs as highly potent dual P70S6K/Akt inhibitors.
Emd Serono Research and Development Institute
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Bristol Myers Squibb Research and Development
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
University of Illinois At Chicago
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Emd Serono Research & Development Institute
Tricyclic-Carbocyclic ROR?t Inverse Agonists-Discovery of BMS-986313.
Bristol Myers Squibb
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.
Spanish National Cancer Research Centre (Cnio)
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.
Taipei Medical University
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.
Chinese Academy of Sciences
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.
Anhui Medical University
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Medicines For Malaria Venture
Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation.
University of South Australia
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based ?-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Janssen Research & Development
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Incyte
Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation.
Baruch S. Blumberg Institute
Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT).
Gsk
Identification of 2,2-Dimethylbutanoic Acid (HST5040), a Clinical Development Candidate for the Treatment of Propionic Acidemia and Methylmalonic Acidemia.
Hemoshear Therapeutics
Structure-Activity Relationship of Heterocyclic P2Y
National Institute of Diabetes and Digestive and Kidney Diseases