Discovery of ERD-308 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Estrogen Receptor (ER).
来源期刊：Journal of medicinal chemistryDOI：10.1021/ACS.JMEDCHEM.8B01572
Ligand-Based Fluorine NMR Screening: Principles and Applications in Drug Discovery Projects.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01210
Novel Allosteric Activators for Ferroptosis Regulator Glutathione Peroxidase 4.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b00315
A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00723
Antimicrobial Peptides with High Proteolytic Resistance for Combating Gram-Negative Bacteria.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01348
DDX3X Helicase Inhibitors as a New Strategy To Fight the West Nile Virus Infection.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01403
3-[(1 S,2 S,3 R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00719
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00134
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity
来源期刊：Journal of Medicinal ChemistryDOI：10.1021/acs.jmedchem.8b01947
Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12).
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01958
Pharmacological Chaperones for the Treatment of α-Mannosidosis.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00153
De Novo Designed Amphipathic α-Helical Antimicrobial Peptides Incorporating Dab and Dap Residues on the Polar Face To Treat the Gram-Negative Pathogen, Acinetobacter baumannii.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01785
Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01925
Multistage Screening Reveals 3-substituted Indolin-2-one Derivatives as Novel and Isoform Selective c-Jun N-terminal kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00537
Environment-Sensitive Near-Infrared Probe for Fluorescent Discrimination of Aβ and Tau Fibrils in AD Brain.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00672
From Phenylthiazoles to Phenylpyrazoles: Broadening the Antibacterial Spectrum towards Carbapenem-Resistant Bacteria.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00720
Novel Benzohydroxamate-based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis and Biological Evaluation.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01194
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01714
Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01540
(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase.
来源期刊：Journal of Medicinal ChemistryDOI：10.2210/PDB6OAC/PDB
Crown Ethers as Transthyretin Amyloidogenesis Inhibitors.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01700
Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00274
Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01573
Epidermal Growth Factor Receptor-Targeted Multifunctional Photosensitizers for Bladder Cancer Imaging and Photodynamic Therapy.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01927
Synthesis and evaluation of novel TLR2 agonists as potential adjuvants for cancer vaccines.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01044
Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01862
Exposing Small-molecule Nano-entities By a Nuclear Magnetic Resonance Relaxation Assay.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00653
Development of Robust 17(R),18(S)-Epoxyeicosatetraenoic Acid (17,18-EEQ) Analogs as Potential Clinical Antiarrhythmic Agents.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00952
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b02021
Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate to Induce Apoptosis-Ferroptosis M2-TAMs Polarization for Combined Cancer Therapy.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00644
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01891
Glucopyranosylidene-spiro-imidazolinones, a New Ring System: Synthesis and Evaluation as Glycogen Phosphorylase Inhibitors by Enzyme Kinetics and X-ray Crystallography.
来源期刊：Journal of Medicinal ChemistryDOI：10.2210/PDB6QA7/PDB
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-based Design.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00891
A novel agonist of the type 1 lysophosphatidic acid receptor (LPA1), UCM-05194, shows efficacy in neuropathic pain amelioration.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01287
Sugar Kick Prevents Memory Impairment.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01668
In Silico Prediction of Hemolytic Toxicity on the Human Erythrocytes for Small Molecules by Machine-Learning and Genetic Algorithm.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00853
Rapid Metabolization of Protectin D1 by β-Oxidation of Its Polar Head Chain.
来源期刊：Journal of Medicinal ChemistryDOI：10.1021/ACS.JMEDCHEM.9B01463
Synthesis, Biological, and Structural Explorations of New Zwitterionic Derivatives of 14-O-Methyloxymorphone, as Potent μ/δ Opioid Agonists and Peripherally Selective Antinociceptives
来源期刊：Journal of Medicinal ChemistryDOI：10.1021/acs.jmedchem.8b01327
Defining Structure-Functional Selectivity Relationships (SFSR) for a Class of Non-Catechol Dopamine D1 Receptor Agonists.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00351
Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00625
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00673
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AGRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00860
Design, Synthesis and Evaluation of 18F-labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00936
Drug Metabolism by the Mitochondrial Amidoxime Reducing Component (mARC): Rapid Assay and Identification of New Substrates.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01483
Targeting the Side-Chain Convergence of Hydrophobic α-Helical Hot Spots to Design Small-Molecule Mimetics: Key Binding Features for i, i + 3 and i + 7.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01324
Influence of non-natural cationic amino acids on the biological activity profile of innate defence regulator peptides.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01344
New Therapeutic Targets for Brain Function and Disease.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01947
Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agents Targeting Transforming Growth Factor β Type I Receptor (TβRI).
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b00708
SAR by 1D NMR.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.9b01688
Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes.
来源期刊：Journal of medicinal chemistryDOI：10.1021/acs.jmedchem.8b01465
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