PMID
Article Title
Citation
Organization
Download
View Data
Discovery of novel SOS1 inhibitors using machine learning.
RSC Med Chem 15: 1392-1403 (2024)
University of Nottingham Ningbo China
Small molecules modulating RNA splicing: a review of targets and future perspectives.
RSC Med Chem 15: 1109-1126 (2024)
University of Bordeaux
A novel BODIPY-based theranostic agent for
RSC Med Chem 15: 1216-1224 (2024)
Shanghai Institute of Materia Medica
Progress in small-molecule inhibitors targeting PD-L1.
RSC Med Chem 15: 1161-1175 (2024)
Henan University
Design, synthesis,
RSC Med Chem 15: 1329-1347 (2024)
Central University of Punjab
Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity.
RSC Med Chem 15: 1247-1257 (2024)
University of Florence
1,5-Disubstituted tetrazoles as PD-1/PD-L1 antagonists.
RSC Med Chem 15: 1210-1215 (2024)
University of Groningen
Enhanced inhibitory activity of compounds containing purine scaffolds compared to protein kinase CK2α considering crystalline water.
RSC Med Chem 15: 1274-1282 (2024)
Kindai University
Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1.
RSC Med Chem 15: 1096-1108 (2024)
China Pharmaceutical University
Screening of efficient salicylaldoxime reactivators for DFP and paraoxon-inhibited acetylcholinesterase.
RSC Med Chem 15: 1225-1235 (2024)
Air Force Medical University
Discovery of CRN04894: A Novel Potent Selective MC2R Antagonist.
ACS Med Chem Lett 15: 478-485 (2024)
Crinetics Pharmaceuticals
In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
ACS Med Chem Lett 15: 540-545 (2024)
Pfizer
Novel Isoxazolidines as RIPK1 Inhibitors for Treating Alzheimer's Disease, Multiple Sclerosis, and Amyotrophic Lateral Sclerosis.
ACS Med Chem Lett 15: 447-448 (2024)
Smith, Gambrell & Russell
Structure-Based Optimization of Selective and Brain Penetrant CK1δ Inhibitors for the Treatment of Circadian Disruptions.
ACS Med Chem Lett 15: 486-492 (2024)
Janssen Research and Development
Macrocyclic Oxindole Peptide Epoxyketones-A Comparative Study of Macrocyclic Inhibitors of the 20S Proteasome.
ACS Med Chem Lett 15: 533-539 (2024)
Whitman College
Design, Synthesis, and Evaluation of 8-(
ACS Med Chem Lett 15: 518-523 (2024)
Huaqiao University
The Science and Art of Structure-Based Virtual Screening.
ACS Med Chem Lett 15: 436-440 (2024)
Astrazeneca
Novel ACC Inhibitors for Treating Acne.
ACS Med Chem Lett 15: 445-446 (2024)
Smith, Gambrell & Russell
Imidazole Bioisostere Activators of Endopeptidase Neurolysin with Enhanced Potency and Metabolic Stability.
ACS Med Chem Lett 15: 510-517 (2024)
University of Nebraska Medical Center
Novel Phosphorylpurinone Compounds for Treating Cancer.
ACS Med Chem Lett 15: 441-442 (2024)
Smith, Gambrell & Russell
Discovery of a New Class of 1-(4-Sulfamoylbenzoyl)piperidine-4-carboxamides as Human Carbonic Anhydrase Inhibitors.
ACS Med Chem Lett 15: 470-477 (2024)
University of Cagliari
Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.
ACS Med Chem Lett 15: 501-509 (2024)
University of Nottingham
Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable
ACS Med Chem Lett 15: 524-532 (2024)
Sanders Tri-Institutional Therapeutics
Novel PCSK9 Inhibitors for Treating Cardiovascular Diseases.
ACS Med Chem Lett 15: 443-444 (2024)
Smith, Gambrell & Russell
Facile Synthesis and First Antifungal Exploration of Tetracyclic Meroterpenoids: (+)-Aureol, (-)-Pelorol, and Its Analogs.
J Nat Prod 87: 1092-1102 (2024)
Guizhou University
Total Synthesis, Structure Reassignment, and Biological Evaluation of the Anti-Inflammatory Macrolactone 13-Hydroxy-14-deoxyoxacyclododecindione.
J Nat Prod 87: 1131-1149 (2024)
Johannes Gutenberg-University
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
J Med Chem 67: 5233-5258 (2024)
Galapagos
Model of P-Glycoprotein Ligand Binding and Validation with Efflux Substrate Matched Pairs.
J Med Chem 67: 5854-5865 (2024)
University of California
Transient Receptor Potential Melastatin 7 (TRPM7) Ion Channel Inhibitors: Preliminary SAR and Conformational Studies of Xenicane Diterpenoids from the Hawaiian Soft Coral
J Nat Prod 87: 783-797 (2024)
Huazhong University of Science and Technology
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
J Med Chem 67: 5216-5232 (2024)
Galapagos
Design and synthesis of novel chloropyridazine hybrids as promising anticancer agents acting by apoptosis induction and PARP-1 inhibition through a molecular hybridization strategy.
RSC Med Chem 15: 981-997 (2024)
Ain-Shams University
Deconvoluting low yield from weak potency in direct-to-biology workflows with machine learning.
RSC Med Chem 15: 1015-1021 (2024)
University of Cambridge
Design, synthesis and preliminary biological evaluation of rivastigmine-INDY hybrids as multitarget ligands against Alzheimer's disease by targeting butyrylcholinesterase and DYRK1A/CLK1 kinases.
RSC Med Chem 15: 963-980 (2024)
University of Rouen Normandy
Synthesis and bioactivity of psilocybin analogues containing a stable carbon-phosphorus bond.
RSC Med Chem 15: 998-1002 (2024)
Ghent University
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex.
RSC Med Chem 15: 1066-1071 (2024)
University of Toronto
-Arylsulfonamide-based adenosine analogues to target RNA cap
RSC Med Chem 15: 839-847 (2024)
University of Montpellier Cnrs
The medicinal chemistry evolution of antibody-drug conjugates.
RSC Med Chem 15: 809-831 (2024)
Abbvi
Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class of
RSC Med Chem 15: 1022-1037 (2024)
Jamia Millia Islamia (A Central University)
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors.
RSC Med Chem 15: 856-873 (2024)
South China University
Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.
RSC Med Chem 15: 788-808 (2024)
Tianjin University
Molecular editing of
RSC Med Chem 15: 937-962 (2024)
National Institute of Pharmaceutical Education and Research (NIPER)
Inhibition of N-type calcium channels by phenoxyaniline and sulfonamide analogues.
RSC Med Chem 15: 916-936 (2024)
Monash University
An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting M
Bioorg Med Chem Lett 103: (2024)
Ocean University of China
Discovery of Alternative Binding Poses through Fragment-Based Identification of DHODH Inhibitors.
ACS Med Chem Lett 15: 381-387 (2024)
Janssen Pharmaceutical Research and Development
Pyrrolidinone Derivatives as NIK Inhibitors for Treating Inflammatory and Autoimmune Diseases.
ACS Med Chem Lett 15: 322-323 (2024)
Smith, Gambrell & Russell
Advancements in Predictive Medicine: NLRP3 Inflammasome Inhibitors and AI-Driven Predictive Health Analytics.
ACS Med Chem Lett 15: 331-333 (2024)
Usona Institute
Combination of Allosteric and Orthosteric EGFR Inhibitors for Treating Non-Small-Cell Lung Cancer.
ACS Med Chem Lett 15: 342-343 (2024)
Smith, Gambrell & Russell
Novel Tetrahydropyrido[3,4-
ACS Med Chem Lett 15: 318-319 (2024)
Smith, Gambrell & Russell
Discovery and Characterization of Active CBP/EP300 Degraders Targeting the HAT Domain.
ACS Med Chem Lett 15: 355-361 (2024)
University of Zurich
Synthesis and Biophysical Characterization of Fingolimod Derivatives as Cardiac Troponin Antagonists.
ACS Med Chem Lett 15: 413-417 (2024)
King'S College London
Novel AT2R Antagonists for Treating Chronic Pain.
ACS Med Chem Lett 15: 326-327 (2024)
Smith, Gambrell & Russell
Terpenes and Terpenoids Conjugated with BODIPYs: An Overview of Biological and Chemical Properties.
J Nat Prod 87: 1306-1319 (2024)
Palacky University
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
J Med Chem 67: 4936-4949 (2024)
Mirati Therapeutics
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
J Med Chem 67: 4691-4706 (2024)
Max Planck Institute of Molecular Physiology
Identification of two novel chemical classes of Autotaxin (ATX) inhibitors using Enalos Asclepios KNIME nodes.
Bioorg Med Chem Lett 103: (2024)
Bsrc Alexander Fleming
Amide Alkaloids as Privileged Sources of Senomodulators for Therapeutic Purposes in Age-Related Diseases.
J Nat Prod 87: 617-628 (2024)
Sorbonne University
Microascones, Decahydrofluorene-Class Alkaloids from the Marine-Derived Fungus
J Nat Prod 87: 810-819 (2024)
Chinese Academy of Sciences
Sokotrasterol Sulfate Suppresses IFN-γ-Induced PD-L1 Expression by Inhibiting JAK Activity.
J Nat Prod 87: 713-721 (2024)
Fudan University
Phytochemical Characterization and TRPA1/TRPM8 Modulation Profile of the Cannabigerol-Rich
J Nat Prod 87: 722-732 (2024)
University of Naples Federico Ii
Multi-target potential of newly designed tacrine-derived cholinesterase inhibitors: Synthesis, computational and pharmacological study.
Bioorg Med Chem 101: (2024)
University of Belgrade-Institute of Chemistry
Research progress of LSD1-based dual-target agents for cancer therapy.
Bioorg Med Chem 101: (2024)
Xinxiang University
Synthesis, biological evaluation, and stability studies of raloxifene mono- and bis-sulfamates as dual-targeting agents.
Bioorg Med Chem 101: (2024)
University of Sharjah
Identification of benzothiazole derived monosaccharides as potent, selective, and orally bioavailable inhibitors of human and mouse galectin-3; a rare example of using a S···O binding interaction for drug design.
Bioorg Med Chem 101: (2024)
Bristol Myers Squibb
Antiviral Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3205-3231 (2024)
Wroclaw University
Discovery of dual-action phenolic 4-arylidene-isoquinolinones with antioxidant and α-glucosidase inhibition activities.
RSC Med Chem 15: 519-538 (2024)
National Autonomous University of Mexico
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.
RSC Med Chem 15: 539-552 (2024)
Zhejiang University
Small molecule WDR5 inhibitors down-regulate lncRNA expression.
RSC Med Chem 15: 636-640 (2024)
Max Planck Institute of Molecular Physiology
Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators.
RSC Med Chem 15: 607-611 (2024)
Dana-Farber Cancer Institute
Highly potent and selective phosphatidylinositol 4-kinase IIIβ inhibitors as broad-spectrum anti-rhinoviral agents.
RSC Med Chem 15: 704-719 (2024)
Korea Research Institute of Chemical Technology
Kinase inhibitor macrocycles: a perspective on limiting conformational flexibility when targeting the kinome with small molecules.
RSC Med Chem 15: 399-415 (2024)
University of Arkansas
Role of heterocycles in inhibition of VEGFR-2 - a recent update (2019-2022).
RSC Med Chem 15: 416-432 (2024)
Srmpp
Design, synthesis and biological evaluation of novel morpholinopyrimidine-5-carbonitrile derivatives as dual PI3K/mTOR inhibitors.
RSC Med Chem 15: 733-752 (2024)
Health Affairs Directorate - Giza
Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors.
RSC Med Chem 15: 720-732 (2024)
The Scripps Research Institute
Discovery of an ellipticine derivative as TLR3 inhibitor against influenza A virus and SARS-CoV-2.
Bioorg Med Chem Lett 101: (2024)
Southern Medical University
Discovery of 5-Hydroxy-1,4-naphthoquinone (Juglone) Derivatives as Dual Effective Agents Targeting Platelet-Cancer Interplay through Protein Disulfide Isomerase Inhibition.
J Med Chem 67: 3626-3642 (2024)
National Taiwan University
A Survey of Recently Discovered Naturally Occurring Organohalogen Compounds.
J Nat Prod 87: 1285-1305 (2024)
Dartmouth College
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor.
Bioorg Med Chem Lett 101: (2024)
Tianjin University
Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Bioorg Med Chem 101: (2024)
Shenyang Pharmaceutical University
PSMA-targeted SMART molecules outfitted with SN38.
Bioorg Med Chem Lett 101: (2024)
Washington State University
2-Phenylcyclopropylmethylamine (PCPMA) as a privileged scaffold for central nervous system drug design.
Bioorg Med Chem Lett 101: (2024)
Shanghaitech University
Synthesis and Evaluation of Natural and Unnatural Tetrahydrocannabiorcol for Its Potential Use in Neuropathologies.
J Nat Prod 87: 167-175 (2024)
Csir-Indian Institute of Integrative Medicine
Discovery of N-(1-(2-hydroxyethyl)quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl)methyl) urea as Mode-Selective TRPV1 antagonist.
Bioorg Med Chem Lett 101: (2024)
Seoul National University
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.
ACS Med Chem Lett 15: 302-309 (2024)
Vanderbilt University
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.
ACS Med Chem Lett 15: 189-196 (2024)
Bristol Myers Squibb
Novel Fused Triazole Compounds as RIPK1 Inhibitors for Treating Neurodegenerative, Autoimmune, and Inflammatory Diseases.
ACS Med Chem Lett 15: 177-178 (2024)
Smith, Gambrell & Russell
3-Alkynyl Carboxamides as AEP Modulators for Treating Alzheimer's Disease.
ACS Med Chem Lett 15: 159-160 (2024)
Smith, Gambrell & Russell
Synthesis and Structural Optimization of ATG4B Inhibitors for the Attenuation of Autophagy in Glioblastoma.
ACS Med Chem Lett 15: 258-264 (2024)
Northwestern University
Synthesis and Biological Evaluation of β-Lactam Derivatives Targeting Speckle-Type POZ Protein (SPOP).
ACS Med Chem Lett 15: 270-279 (2024)
Nanjing University of Chinese Medicine
Innovative Therapeutic Strategies in TYK2-Targeted Treatments: From Cancer to Autoimmune Disorders.
ACS Med Chem Lett 15: 174-176 (2024)
Usona Institute
Novel PARP1 Inhibitors for Treating Cancer.
ACS Med Chem Lett 15: 161-162 (2024)
Smith, Gambrell & Russell
Nicotinamide Phosphoribosyltransferase Positive Allosteric Modulators Attenuate Neuronal Oxidative Stress.
ACS Med Chem Lett 15: 205-214 (2024)
University of Illinois At Chicago
Development of a GC-376 Based Peptidomimetic PROTAC as a Degrader of 3-Chymotrypsin-like Protease of SARS-CoV-2.
ACS Med Chem Lett 15: 250-257 (2024)
University of Florence
Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.
ACS Med Chem Lett 15: 181-188 (2024)
Bristol-Myers Squibb Research & Development
The Bis(1,2,3,4-tetrahydroisoquinoline) Alkaloids Cepharanthine and Berbamine Are Ligands of SK Channels.
ACS Med Chem Lett 15: 215-220 (2024)
University of Liege
Emopamil-Binding Protein Inhibitors for Treating Multiple Sclerosis.
ACS Med Chem Lett 15: 163-164 (2024)
Smith, Gambrell & Russell
Discovery of a novel series of pyridone amides as Na
Bioorg Med Chem Lett 101: (2024)
Sichuan University
Design, synthesis of new 3H-imidazo[4,5-b]pyridine derivatives and evaluation of their inhibitory properties as mixed lineage kinase 3 inhibitors.
Bioorg Med Chem Lett 101: (2024)
Chungnam National University
Rational design, synthesis and biological evaluation of novel HIV-1 protease inhibitors containing 2-phenylacetamide derivatives as P2 ligands with potent activity against DRV-Resistant HIV-1 variants.
Bioorg Med Chem Lett 101: (2024)
Xuzhou Medical University
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
J Med Chem 67: 2369-2378 (2024)
Calibr At Scripps Research Institute
Discovery of Anti-Hypercholesterolemia Agents Targeting LXRα from Marine Microorganism-Derived Natural Products.
J Nat Prod 87: 322-331 (2024)
Guangxi University of Chinese Medicine
Design, synthesis and biological evaluation of 2-phenylaminopyrimidine derivatives as EGFR inhibitors.
Bioorg Med Chem Lett 101: (2024)
Jiangnan University
Norterpene Cyclic Peroxides from the Marine Sponge
J Nat Prod 87: 358-364 (2024)
Korea Institute of Ocean Science and Technology
Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety.
J Med Chem 67: 3018-3038 (2024)
Romanian Academy
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J Med Chem 67: 2321-2336 (2024)
Nurix Therapeutics
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate.
J Med Chem 67: 4525-4540 (2024)
University of Oxford
Neopetrotaurines A-C, Isoquinoline Alkaloids with an Unprecedented Taurine Bridge from the Sponge
J Nat Prod 87: 332-339 (2024)
National Cancer Institute
PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
J Med Chem 67: 2619-2630 (2024)
Unidad Bics
First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity
J Med Chem 67: 2963-2985 (2024)
Taipei Medical University
Pyrazole derivatives as selective orexin-2 receptor antagonists (2-SORA): synthesis, structure-activity-relationship, and sleep-promoting properties in rats.
RSC Med Chem 15: 344-354 (2024)
Idorsia Pharmaceuticals
A survey of stapling methods to increase affinity, activity, and stability of ghrelin analogues.
RSC Med Chem 15: 254-266 (2024)
University of Western Ontario
The development of thymol-isatin hybrids as broad-spectrum antibacterial agents with potent anti-MRSA activity.
RSC Med Chem 15: 234-253 (2024)
Guru Nanak Dev University
Discovery of a dual-acting inhibitor of interleukin-1β and STATs for the treatment of inflammatory bowel disease.
RSC Med Chem 15: 193-206 (2024)
Guangzhou Medical University
Recent advances of phenotypic screening strategies in the application of anti-influenza virus drug discovery.
RSC Med Chem 15: 70-80 (2024)
Shandong University
Novel indolyl 1,2,4-triazole derivatives as potential anti-proliferative agents:
RSC Med Chem 15: 293-308 (2024)
Misr International University
Physicochemical characterization of
RSC Med Chem 15: 119-126 (2024)
Tokyo Medical and Dental University
Highly efficient, catalyst-free, one-pot sequential four-component synthesis of novel spiroindolinone-pyrazole scaffolds as anti-Alzheimer agents:
RSC Med Chem 15: 207-222 (2024)
Persian Gulf University
Scaffold hopping based designing of selective ALDH1A1 inhibitors to overcome cyclophosphamide resistance: synthesis and biological evaluation.
RSC Med Chem 15: 309-321 (2024)
Punjabi University
Latest developments in coumarin-based anticancer agents: mechanism of action and structure-activity relationship studies.
RSC Med Chem 15: 10-54 (2024)
Csir-Central Glass & Ceramic Research Institute
Solubilizer Tag Effect on PD-L1/Inhibitor Binding Properties for
ACS Med Chem Lett 15: 36-44 (2024)
Jagiellonian University
Fluorinated Isoindolinone-Based Glucosylceramide Synthase Inhibitors with Low Human Dose Projections.
ACS Med Chem Lett 15: 123-131 (2024)
Merck
Discovery of Malarial Threonyl tRNA Synthetase Inhibitors by Screening of a Focused Fragment Library.
ACS Med Chem Lett 15: 76-80 (2024)
Latvian Institute of Organic Synthesis
Discovery of Novel PDEδ Autophagic Degraders: A Case Study of Autophagy-Tethering Compound (ATTEC).
ACS Med Chem Lett 15: 29-35 (2024)
East China University of Science and Technology
Synthesis, Antiacetylcholinesterase Activity, and Molecular Dynamics Simulation of Aporphine-benzylpyridinium Conjugates.
ACS Med Chem Lett 15: 132-142 (2024)
Chulabhorn Research Institute
Structure-Based Design and Evaluation of Reversible KRAS G13D Inhibitors.
ACS Med Chem Lett 15: 21-28 (2024)
Genentech
Chemical Catalysis Guides Structural Identification for the Major
ACS Med Chem Lett 15: 107-115 (2024)
Baylor College of Medicine
Positive Allosteric Modulators of alpha7 Nicotinic Acetylcholine Receptor for the Treatment of Several Central Nervous System Diseases.
ACS Med Chem Lett 15: 6-8 (2024)
Therachem Research Medilab
Novel Pyrazolopyridine Inhibitors of Monoacylglycerol Lipase for the Treatment of Neurodegenerative Diseases and Neuroinflammation.
ACS Med Chem Lett 15: 19-20 (2024)
Arrival Discovery
Ligand-Based Competition Binding by Real-Time
J Med Chem 67: 1115-1126 (2024)
University of Bologna
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase.
J Med Chem 67: 1061-1078 (2024)
Imperial College London
Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
J Med Chem 67: 864-884 (2024)
Astrazeneca
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
J Med Chem 67: 1580-1610 (2024)
Jagiellonian University Medical College
Fragment Merging, Growing, and Linking Identify New Trypanothione Reductase Inhibitors for Leishmaniasis.
J Med Chem 67: 402-419 (2024)
Sapienza University of Rome
A Simple Chiral
J Nat Prod 87: 77-84 (2024)
National and Kapodistrian University of Athens
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J Med Chem 67: 774-781 (2024)
Mirati Therapeutics
Coriaceumins A-D, the First Nitrogen-Containing Crenulide Diterpenoids from the Brown Alga
J Nat Prod 87: 121-131 (2024)
The Second Affiliated Hospital of Nanchang University
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
J Med Chem 67: 380-401 (2024)
Galapagos
Discovery and characterization of novel TRPML1 agonists.
Bioorg Med Chem Lett 98: (2024)
Arkuda Therapeutics
Diaporaustalides A-L, Austalide Meroterpenoids from a Plant Endophytic
J Nat Prod 87: 141-151 (2024)
Huazhong University of Science and Technology
Target Separation and Potential Anticancer Activity of Withanolide-Based Glucose Transporter Protein 1 Inhibitors from
J Nat Prod 87: 2-13 (2024)
China Pharmaceutical University
Novel IRAK4 Inhibitors for Treating Asthma, COPD, Cancer, Autoinflammatory Diseases, and Autoimmune Diseases.
ACS Med Chem Lett 14: 1617-1618 (2023)
Smith, Gambrell & Russell
Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors.
ACS Med Chem Lett 14: 1673-1681 (2023)
Pfizer
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
ACS Med Chem Lett 14: 1848-1856 (2023)
Astrazeneca
Novel Fused Pyrazole Amide Analogs as Glucosylceramide Synthase Inhibitors for Treating Lysosomal Storage Diseases, Neurodegenerative Diseases, Cystic Diseases, and Cancer.
ACS Med Chem Lett 14: 1621-1622 (2023)
Smith, Gambrell & Russell
2-Amino-5-arylethynyl-thiophen-3-yl-(phenyl)methanones as A
ACS Med Chem Lett 14: 1640-1646 (2023)
National Institute of Diabetes and Digestive and Kidney Disease
Novel Indane-Containing NBTIs with Potent Anti-Gram-Negative Activity and Minimal hERG Inhibition.
ACS Med Chem Lett 14: 1791-1799 (2023)
Roche Pharma Research & Early Development
Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors.
ACS Med Chem Lett 14: 1863-1868 (2023)
University of Bonn
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase.
ACS Med Chem Lett 14: 1631-1639 (2023)
Novartis Institutes for Biomedical Research
Novel Adenosine Receptor Antagonists for Treating Cancer and Immune-Related Disorders.
ACS Med Chem Lett 14: 1619-1620 (2023)
Smith, Gambrell & Russell
Phenyl-quinoline-xxo-butyric Acid Inhibitors of Histone Lysine Demethylase for the Treatment of Cancer.
ACS Med Chem Lett 14: 1623-1624 (2023)
Arrival Discovery
Discovery of Potent and Oral Bioavailable MAT2A Inhibitors for the Treatment of MTAP-Deleted Tumors.
ACS Med Chem Lett 14: 1876-1881 (2023)
Hubei Bio-Pharmaceutical Industrial Technological Institute
Novel PARP7 Inhibitors for Treating Cancer.
ACS Med Chem Lett 14: 1615-1616 (2023)
Smith, Gambrell & Russell
Fragment-Based Screening Identifies New Quinazolinone-Based Inositol Hexakisphosphate Kinase (IP6K) Inhibitors.
ACS Med Chem Lett 14: 1760-1766 (2023)
Lieber Institute For Brain Development
Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal
ACS Med Chem Lett 14: 1700-1706 (2023)
Rigel Pharmaceuticals
Nanomolar Benzothiazole-Based Inhibitors of 17β-HSD10 with Cellular Bioactivity.
ACS Med Chem Lett 14: 1724-1732 (2023)
University of Hradec Kralove
Discovery of Novel NLRP3 Inflammasome Inhibitors Composed of an Oxazole Scaffold Bearing an Acylsulfamide.
ACS Med Chem Lett 14: 1833-1838 (2023)
Japan Tobacco
The Promiscuity of Disulfiram in Medicinal Research.
ACS Med Chem Lett 14: 1610-1614 (2023)
Palacky University
Synthesis and Evaluation of Small Molecule Inhibitors of the Androgen Receptor N-Terminal Domain.
ACS Med Chem Lett 14: 1800-1806 (2023)
University of Strathclyde
Novel Pyrido[3,2-
ACS Med Chem Lett 14: 1627-1628 (2023)
Smith, Gambrell & Russell
Development of Allosteric NIK Ligands from Fragment-Based NMR Screening.
ACS Med Chem Lett 14: 1815-1820 (2023)
University of Minnesota
Electrophilic MiniFrags Revealed Unprecedented Binding Sites for Covalent HDAC8 Inhibitors.
J Med Chem 67: 572-585 (2024)
Hun-Ren Research Centre for Natural Sciences
Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
J Med Chem 67: 17-37 (2024)
National Research Council of Italy
Aurones and derivatives as promising New Delhi metallo-β-lactamase (NDM-1) inhibitors.
Bioorg Med Chem 97: (2024)
Univ. Grenoble Alpes
Discovery of Novel PD-L1 Inhibitors That Induce the Dimerization, Internalization, and Degradation of PD-L1 Based on the Fragment Coupling Strategy.
J Med Chem 66: 16807-16827 (2023)
China Pharmaceutical University
Synthesis, biological and molecular modelling for 1,3,4-thiadiazole sulfonyl thioureas: bacterial and fungal activity.
RSC Med Chem 14: 2751-2767 (2023)
Vietnam National University
Novel pyrazolo[3,4-
RSC Med Chem 14: 2640-2657 (2023)
Misr University for Science and Technology (MUST)
Naphthyl bearing 1,3,4-thiadiazoleacetamides targeting the parasitic folate pathway as anti-infectious agents:
RSC Med Chem 14: 2768-2781 (2023)
Jamia Millia Islamia
Discovery of novel tubulin CBSI
RSC Med Chem 14: 2738-2750 (2023)
Fudan University
Overview of CFTR activators and their recent studies for dry eye disease: a review.
RSC Med Chem 14: 2459-2472 (2023)
Shenyang Pharmaceutical University
Diversely functionalized isoquinolines and their core-embedded heterocyclic frameworks: a privileged scaffold for medicinal chemistry.
RSC Med Chem 14: 2509-2534 (2023)
Mahatma Gandhi University
A covalent fragment-based strategy targeting a novel cysteine to inhibit activity of mutant EGFR kinase.
RSC Med Chem 14: 2731-2737 (2023)
Daiichi Sankyo Co.
Research status of indole-modified natural products.
RSC Med Chem 14: 2535-2563 (2023)
Yanbian University
Development of trisubstituted thiophene-3-arboxamide selenide derivatives as novel EGFR kinase inhibitors with cytotoxic activity.
RSC Med Chem 14: 2677-2698 (2023)
National Institute of Pharmaceutical Education and Research (NIPER)
A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response.
RSC Med Chem 14: 2625-2639 (2023)
Yunnan University
Discovery of a Hidden Pocket beneath the NES Groove by Novel Noncovalent CRM1 Inhibitors.
J Med Chem 66: 17044-17058 (2023)
Sichuan University
Discovery of potential scaffolds for glutaminyl cyclase inhibitors: Virtual screening, synthesis, and evaluation.
Bioorg Med Chem 97: (2024)
Shenzhen University Medical School
Linker optimization and activity validation of a cell surface vimentin targeted homo-dimeric peptoid antagonist for lung cancer stem cells.
Bioorg Med Chem 97: (2024)
University of Houston
Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells.
RSC Med Chem 14: 2611-2624 (2023)
University of Edinburgh
Design, synthesis, and biological evaluation of novel 8-substituted quercetin derivatives targeting the β‑catenin/B-cell lymphoma 9 interaction.
Bioorg Med Chem Lett 98: (2024)
Tongji University
Exploration of macrocyclic peptide binders to the extracellular CRD domain of human receptor tyrosine kinase-like orphan receptor 1 (ROR1).
Bioorg Med Chem Lett 98: (2024)
Princeton University
Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs).
J Med Chem 66: 16704-16727 (2023)
University of Arizona
One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp
J Med Chem 66: 16939-16952 (2023)
Boehringer Ingelheim Rcv
Development of MPS1 Inhibitors: Recent Advances and Perspectives.
J Med Chem 66: 16484-16514 (2023)
Guizhou University
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.
J Med Chem 66: 16187-16200 (2023)
China Pharmaceutical University
Small Molecule Inhibitors Targeting the "Undruggable" Survivin: The Past, Present, and Future from a Medicinal Chemist's Perspective.
J Med Chem 66: 16515-16545 (2023)
University of Toledo College of Medicine and Life Sciences
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Bioorg Med Chem Lett 98: (2024)
Shanghai Institute of Materia Medica
Discovery of Orally Available and Brain Penetrant AEP Inhibitors.
J Med Chem 66: 17026-17043 (2023)
Roche Innovation Center Basel
Discovery and Mechanistic Study of Novel
J Med Chem 66: 16597-16614 (2023)
Sichuan University
Optimization of the Antibacterial Spectrum and the Developability Profile of the Novel-Class Natural Product Corramycin.
J Med Chem 66: 16869-16887 (2023)
Evotec
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1.
J Med Chem 66: 16464-16483 (2023)
Shandong University
Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors.
J Med Chem 66: 16783-16806 (2023)
Institute of Chemical Biology
Design and Development of IKZF2 and CK1α Dual Degraders.
J Med Chem 66: 16953-16979 (2023)
Harvard University
Optimization of Pharmacokinetic and In Vitro Safety Profile of a Series of Pyridine Diamide Indirect AMPK Activators.
J Med Chem 66: 17086-17104 (2023)
Rigel Pharmaceuticals
Pioneering 4,11-Dioxo-4,11-dihydro-1
J Med Chem 66: 16843-16868 (2023)
Shanghai Jiao Tong University
Discovery and biological evaluation of novel dual PTP1B and ACP1 inhibitors for the treatment of insulin resistance.
Bioorg Med Chem 97: (2024)
The Affiliated Hospital of Yangzhou University
Design, synthesis and anti-rheumatoid arthritis activity of target TLR4 inhibitors.
Bioorg Med Chem 97: (2024)
Chongqing Chemical Industry Vocational College
Discovery of flavone-derivatives as the new skeleton of transient receptor potential vanilloid 3 channel antagonists.
Bioorg Med Chem Lett 98: (2024)
Qingdao University Medical College
Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation.
Bioorg Med Chem Lett 98: (2024)
Daiichi Sankyo Co.
Structural Fusion of Natural and Synthetic Ligand Features Boosts RXR Agonist Potency.
J Med Chem 66: 16762-16771 (2023)
Goethe University Frankfurt
Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
J Med Chem 66: 16991-17025 (2023)
Shanghai Institute of Materia Medica
Discovery of Dual Function Agents That Exhibit Anticancer Activity via Catastrophic Nicotinamide Adenine Dinucleotide Depletion.
J Med Chem 66: 16694-16703 (2023)
Nanchang University
Discovery of YSR734: A Covalent HDAC Inhibitor with Cellular Activity in Acute Myeloid Leukemia and Duchenne Muscular Dystrophy.
J Med Chem 66: 16658-16679 (2023)
University of Toronto Mississauga
Discovery of Selective and Orally Available Galectin-1 Inhibitors.
J Med Chem 66: 16980-16990 (2023)
Galecto Biotech
Bifunctional backbone modified squaramide dipeptides as amyloid beta (Aβ) aggregation inhibitors.
Bioorg Med Chem 97: (2024)
National Institute of Pharmaceutical Education and Research (NIPER)-Ahmedabad
Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer.
J Med Chem 66: 16917-16938 (2023)
East China Normal University
Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.
J Med Chem 66: 16303-16329 (2023)
Shandong University
Design, synthesis, biological evaluation and molecular docking of alkoxyaurones as potent pancreatic lipase inhibitors.
Bioorg Med Chem Lett 98: (2024)
University of Medicine and Pharmacy At Ho Chi Minh City
PSMA-targeted small-molecule drug-conjugates with valine-citrulline and phosphoramidate cleavable linkers.
Bioorg Med Chem Lett 98: (2024)
Washington State University
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
J Med Chem 66: 15648-15670 (2023)
Perha Pharmaceuticals
Harnessing the Reactivity of Duclauxin toward Obtaining
J Med Chem 66: 16222-16234 (2023)
National Autonomous University of Mexico
Small Molecule Ligands of the BET-like Bromodomain,
J Med Chem 66: 15801-15822 (2023)
University of Oxford
Discovery of a First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis.
J Med Chem 66: 15926-15943 (2023)
TBA
Discovery of Inhibitory Fragments That Selectively Target Spire2-FMN2 Interaction.
J Med Chem 66: 15715-15727 (2023)
Jagiellonian University
Thiamine analogues featuring amino-oxetanes as potent and selective inhibitors of pyruvate dehydrogenase.
Bioorg Med Chem Lett 98: (2024)
University of Cambridge
Discovery of Potent, Selective, and Orally Bioavailable DYRK2 Inhibitors for the Treatment of Prostate Cancer.
J Med Chem 66: 16235-16256 (2023)
China Pharmaceutical University
Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.
J Med Chem 66: 16342-16363 (2023)
Ewha Womans University
Discovery of Novel 2,3-Dihydro-1
J Med Chem 66: 16141-16167 (2023)
Ocean University of China
α-Aminophosphonate inhibitors of metallo-β-lactamases NDM-1 and VIM-2.
RSC Med Chem 14: 2277-2300 (2023)
Uppsala University
Novel styryl-thiazole hybrids as potential anti-Alzheimer's agents.
RSC Med Chem 14: 2315-2326 (2023)
University of Athens
Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer.
J Med Chem 66: 16168-16186 (2023)
Icahn School of Medicine At Mount Sinai
A Novel Bifunctional μOR Agonist and σ
J Med Chem 66: 16257-16275 (2023)
Sichuan University
Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
J Med Chem 66: 16410-16425 (2023)
Novartis Pharma
Orthogonal Reversed-Phase C
J Nat Prod 86: 2638-2650 (2023)
University of Copenhagen
Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2).
J Med Chem 66: 15750-15760 (2023)
Bristol Myers Squibb
Synthesis, in vitro Α-Glucosidase, and acetylcholinesterase inhibitory activities of novel Indol-Fused Pyrano[2,3-D]Pyrimidine compounds.
Bioorg Med Chem Lett 98: (2024)
Vietnam Academy of Science and Technology
Curated by BindingDB
Curated by ChEMBL