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Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.BDB
ACS Med Chem Lett 14: 199-210 (2023)
Ontario Institute for Cancer Research
Advanced approaches of developing targeted covalent drugs.EBI
RSC Med Chem 13: 1460-1475 (2022)
College Of Pharmacy
Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies.EBI
RSC Med Chem 13: 1644-1656 (2022)
Federal University Of Santa Catarina
Revisiting a challenging p53 binding site: a diversity-optimized HEFLib reveals diverse binding modes in T-p53C-Y220C.EBI
RSC Med Chem 13: 1575-1586 (2022)
Universit�T T�Bingene
Structure-activity relationship study of PROTACs against hematopoietic prostaglandin DEBI
RSC Med Chem 13: 1495-1503 (2022)
National Institute Of Health Sciences
A high-throughput effector screen identifies a novel small molecule scaffold for inhibition of ten-eleven translocation dioxygenase 2.EBI
RSC Med Chem 13: 1540-1548 (2022)
Tu Dortmund University
Pyrazolidine Carboxamide Analogs as Selective Agonists of the Cannabinoid 2 Receptor.EBI
ACS Med Chem Lett 13: 1837-1838 (2022)
Arrival Discovery
Effects of 6-Aminonicotinic Acid Esters on the Reprogrammed Epigenetic State of Distant Metastatic Pancreatic Carcinoma.EBI
ACS Med Chem Lett 13: 1892-1897 (2022)
Johns Hopkins University School Of Medicine
Identification of a Target Site for Covalent Inhibition of Protein Phosphohistidine Phosphatase 1.EBI
ACS Med Chem Lett 13: 1911-1915 (2022)
Ulsan National Institute of Science and Technology (UNIST)
Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448).EBI
ACS Med Chem Lett 13: 1856-1863 (2022)
The State University Of New York
Fragment-Sized Thiazoles in Fragment-Based Drug Discovery Campaigns: Friend or Foe?EBI
ACS Med Chem Lett 13: 1905-1910 (2022)
University Of Ljubljana
ACS Med Chem Lett 13: 1864-1869 (2022)
Fudan University
Identification of TUL01101: A Novel Potent and Selective JAK1 Inhibitor for the Treatment of Rheumatoid Arthritis.EBI
J Med Chem 65: 16716-16740 (2022)
Zhuhai United Laboratories
Discovery of Novel Orally Bioavailable Triazoles with Potent and Broad-Spectrum Antifungal Activity In Vitro and In Vivo.EBI
J Med Chem 65: 16665-16678 (2022)
Tongji University
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site.EBI
J Med Chem 65: 16372-16391 (2022)
Chinese Academy Of Medical Sciences And Peking Union Medical College
Structure-Based Design of a Dual-Targeted Covalent Inhibitor Against Papain-like and Main Proteases of SARS-CoV-2.EBI
J Med Chem 65: 16252-16267 (2022)
China Pharmaceutical University
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.EBI
J Med Chem 65: 16902-16917 (2022)
Shandong University
BAY-7081: A Potent, Selective, and Orally Bioavailable Cyanopyridone-Based PDE9A Inhibitor.EBI
J Med Chem 65: 16420-16431 (2022)
Discovery of Pan-peroxisome Proliferator-Activated Receptor Modulators from an Endolichenic Fungus, EBI
J Nat Prod 85: 2804-2816 (2022)
Seoul National University
Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.EBI
J Med Chem 65: 16651-16664 (2022)
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity.EBI
J Med Chem 65: 16860-16878 (2022)
Leipzig 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.EBI
J Med Chem 65: 16526-16540 (2022)
Shanghai Institute Of Materia Medica
The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation.EBI
J Med Chem 65: 16268-16289 (2022)
Max Planck Institute Of Molecular Physiology
Design, synthesis, and bioevaluation of imidazo [1,2-a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities.EBI
Bioorg Med Chem 76: (2022)
Southern Medical University
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3K?.EBI
J Med Chem 65: 16589-16621 (2022)
Discovery of Orally Bioavailable EBI
J Med Chem 65: 16622-16639 (2022)
China Pharmaceutical University
Computational design, synthesis and biological evaluation of PDE5 inhibitors based on NEBI
Bioorg Med Chem 76: (2022)
King Mongkut'S Institute Of Technology
Design and Synthesis of Fibroblast Growth Factor Receptor (FGFR) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Cancer.EBI
J Med Chem 65: 16541-16569 (2022)
Sichuan University
Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties.EBI
J Med Chem 65: 16313-16337 (2022)
Martin-Luther University Of Halle-Wittenberg
Making Protein Degradation Visible: Discovery of Theranostic PROTACs for Detecting and Degrading NAMPT.EBI
J Med Chem 65: 15725-15737 (2022)
Second Military Medical University (Navy Medical University)
B-cell Lymphoma 6 Inhibitors: Current Advances and Prospects of Drug Development for Diffuse Large B-cell Lymphomas.EBI
J Med Chem 65: 15559-15583 (2022)
East China Normal University
Synthesis of full-length homodimer ?D-VxXXB that targets human ?7 nicotinic acetylcholine receptors.EBI
RSC Med Chem 13: 1410-1419 (2022)
The University Of Queensland
Efficient selective targeting of EBI
RSC Med Chem 13: 1322-1340 (2022)
University Of Sharjah
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.EBI
RSC Med Chem 13: 1300-1321 (2022)
Tianjin University
A fragment-based approach leading to the discovery of inhibitors of CK2? with a novel mechanism of action.EBI
RSC Med Chem 13: 1420-1426 (2022)
University Of Cambridge
Identification and Characterization of a Novel Indoleamine 2,3-Dioxygenase 1 Protein Degrader for Glioblastoma.EBI
J Med Chem 65: 15642-15662 (2022)
Northwestern University Feinberg School Of Medicine
The discovery of (1R, 3R)-1-(3-chloro-5-fluorophenyl)-3-(hydroxymethyl)-1,2,3,4-tetrahydroisoquinoline-6-carbonitrile, a potent and selective agonist of human transient receptor potential cation channel subfamily m member 5 (TRPM5) and evaluation of as a potential gastrointestinal prokinetic agent.EBI
Bioorg Med Chem 76: (2022)
Turning Point Therapeutics
Selective Inhibition of PTP1B by New Anthraquinone Glycosides from EBI
J Nat Prod 85: 2836-2844 (2022)
Binzhou Medical University
Novel bioactive hybrid Celecoxib-HDAC Inhibitor, induces apoptosis in human acute lymphoblastic leukemia cells.EBI
Bioorg Med Chem 75: (2022)
The Affiliated Hospital Of Southwest Medical University
Discovery of a Series of 5-Amide-1EBI
J Med Chem 65: 15967-15990 (2022)
China Pharmaceutical University
A New Naphthopyran Derivative Combines EBI
ACS Med Chem Lett 13: 1783-1790 (2022)
University Of Bayreuth
Covalent Modification of the JH2 Domain of Janus Kinase 2.EBI
ACS Med Chem Lett 13: 1819-1826 (2022)
Yale University
Identification of Inhibitors of the EBI
ACS Med Chem Lett 13: 1715-1722 (2022)
Imperial College London
Recent Discovery of PARP7 Inhibitors as Anticancer Agents.EBI
ACS Med Chem Lett 13: 1688-1690 (2022)
Usona Institute
Discovery of Selective Inhibitors of NaEBI
ACS Med Chem Lett 13: 1763-1768 (2022)
Siteone Therapeutics
Inhibition of ?-Amyloid Aggregation in Alzheimer's Disease: The Key Role of (Pro)electrophilic Warheads.EBI
ACS Med Chem Lett 13: 1812-1818 (2022)
Alma Mater Studiorum - University Of Bologna
(-)-Epigallocatechin Gallate is a Noncompetitive Inhibitor of NAD Kinase.EBI
ACS Med Chem Lett 13: 1699-1706 (2022)
Hangzhou Institute For Advanced Study
Discovery of ? Opioid Receptor (KOR)-Selective d-Tetrapeptides with Improved EBI
ACS Med Chem Lett 13: 1707-1714 (2022)
Novel TYK2 Inhibitors with an EBI
ACS Med Chem Lett 13: 1730-1738 (2022)
Nanjing University Of Science And Technology
Optimization of Pyrimidine Compounds as Potent JAK1 Inhibitors and the Discovery of R507 as a Clinical Candidate.EBI
ACS Med Chem Lett 13: 1805-1811 (2022)
Rigel Pharmaceuticals
Discovery of 5,7-Dihydro-6EBI
ACS Med Chem Lett 13: 1797-1804 (2022)
The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria.EBI
ACS Med Chem Lett 13: 1745-1754 (2022)
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.EBI
J Med Chem 65: 15679-15697 (2022)
Goethe University Frankfurt
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.EBI
J Med Chem 65: 15174-15207 (2022)
Selective TASK-1 Inhibitor with a Defined Structure-Activity Relationship Reduces Cancer Cell Proliferation and Viability.EBI
J Med Chem 65: 15014-15027 (2022)
Centro De Estudios En Alimentos Procesados-Ceap
Development of Macrocyclic PRMT5-Adaptor Protein Interaction Inhibitors.EBI
J Med Chem 65: 15300-15311 (2022)
Max Planck Institute Of Molecular Physiology
Structure-Activity Studies of 1EBI
J Med Chem 65: 15238-15262 (2022)
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of novel N-(1-benzyl-1H-imidazol-2-yl)amide derivatives as melanocortin 1 receptor agonists.EBI
Bioorg Med Chem Lett 78: (2022)
Mitsubishi Tanabe Pharma
Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors.EBI
J Med Chem 65: 15374-15390 (2022)
Jinan University
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.EBI
J Med Chem 65: 15433-15442 (2022)
Prelude Therapeutics
Two Binding Sites of SARS-CoV-2 Macrodomain 3 Probed by Oxaprozin and Meclomen.EBI
J Med Chem 65: 15227-15237 (2022)
University Of Science And Technology Of China
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring EBI
J Med Chem 65: 15140-15164 (2022)
Jinan University
Development of Fluorinated Peptoid-Based Histone Deacetylase (HDAC) Inhibitors for Therapy-Resistant Acute Leukemia.EBI
J Med Chem 65: 15457-15472 (2022)
University Of Bonn
Exploration and Biological Evaluation of Bispecific Peptides Derived from Anti-HER2 Antibodies and Peptide-Camptothecin Conjugates for HER2-Positive Breast Cancer.EBI
J Med Chem 65: 15123-15139 (2022)
China Pharmaceutical University
Discovery, Optimization, and Evaluation of Selective CDK4/6 Inhibitors for the Treatment of Breast Cancer.EBI
J Med Chem 65: 15102-15122 (2022)
China Pharmaceutical University
Design, synthesis, and biological studies of dual URAT1 inhibitor and FXR agonist based on benzbromarone.EBI
Bioorg Med Chem 75: (2022)
Guangdong Pharmaceutical University
Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities.EBI
J Med Chem 65: 14971-14999 (2022)
West China Hospital
Phenotypic Discovery of Triazolo[1,5-EBI
J Med Chem 65: 15263-15281 (2022)
Technical University Dortmund
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.EBI
J Med Chem 65: 15208-15226 (2022)
Tri-Institutional Institutional Therapeutics Discovery Institute
Exploring the NCS-382 Scaffold for CaMKII? Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKII? Hub Domain.EBI
J Med Chem 65: 15066-15084 (2022)
University Of Copenhagen
Synthesis and in vitro biological evaluation of 3-ethyl-1,5-naphthyridin-2(1H)-one derivatives as potent PARP-1 selective inhibitors and PARP-1 DNA trappers.EBI
Bioorg Med Chem Lett 78: (2022)
China Pharmaceutical University
Photoredox-based late-stage functionalization in SAR study for in vivo potent glucosylceramide synthase inhibitor.EBI
Bioorg Med Chem Lett 77: (2022)
Takeda Pharmaceutical
Covalently Conjugated NOD2/TLR7 Agonists Are Potent and Versatile Immune Potentiators.EBI
J Med Chem 65: 15085-15101 (2022)
University Of Ljubljana
Synthesis, evaluation and mechanism exploration of 2-(N-(3-nitrophenyl)-N-phenylsulfonyl)aminoacetohydroxamic acids as novel urease inhibitors.EBI
Bioorg Med Chem Lett 78: (2022)
National Demonstration Center For Experimental Chemistry Education
Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2.EBI
J Med Chem 65: 15443-15456 (2022)
University Of California Riverside
A 1,2,3-Triazole Derivative of Quinazoline Exhibits Antitumor Activity by Tethering RNF168 to SQSTM1/P62.EBI
J Med Chem 65: 15028-15047 (2022)
Shenzhen University School Of Medicine
Targeting osteoarthritis-associated galectins and an induced effector class by a ditopic bifunctional reagent: Impact of its glycan part on binding measured in the tissue context.EBI
Bioorg Med Chem 75: (2022)
Ludwig-Maximilians-University Munich
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.EBI
J Med Chem 65: 15473-15486 (2022)
University Of The Pacific
Structure-based discovery of potent inhibitors of Axl: design, synthesis, and biological evaluation.EBI
RSC Med Chem 13: 1246-1264 (2022)
Hunan Normal University
-Methylamide-structured SB366791 derivatives with high TRPV1 antagonistic activity: toward PET radiotracers to visualize TRPV1.EBI
RSC Med Chem 13: 1197-1204 (2022)
Riken Center For Biosystems Dynamics Research
Synthesis and biological evaluation of paeoveitol D derivatives as new melatonin receptor agonists with antidepressant activities.EBI
RSC Med Chem 13: 1212-1224 (2022)
Chinese Academy Of Sciences
New ?-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.EBI
RSC Med Chem 13: 1064-1076 (2022)
University Shihezi
Orally Bioavailable Quinoxaline Inhibitors of 15-Prostaglandin Dehydrogenase (15-PGDH) Promote Tissue Repair and Regeneration.EBI
J Med Chem 65: 15327-15343 (2022)
Ut Southwestern Medical Center
Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis.EBI
J Med Chem 65: 15000-15013 (2022)
Interrogation of the Pathogen Box reveals small molecule ligands against the mycobacterial trehalose transporter LpqY-SugABC.EBI
RSC Med Chem 13: 1225-1233 (2022)
University Of Warwick
Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: EBI
J Med Chem 65: 14456-14480 (2022)
University Federico Ii Of Naples
Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition.EBI
J Med Chem 65: 14599-14613 (2022)
Taisho Pharmaceutical
Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers.EBI
J Med Chem 65: 14409-14423 (2022)
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI
J Med Chem 65: 14326-14336 (2022)
Janssen Research & Development
The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones.EBI
Bioorg Med Chem Lett 77: (2022)
North-West University
Selective butyrylcholinesterase inhibition by isatin dimers and 3-indolyl-3-hydroxy-2-oxindole dimers.EBI
Bioorg Med Chem Lett 77: (2022)
The Behrend College
Development of a Highly Potent Transthyretin Amyloidogenesis Inhibitor: Design, Synthesis, and Evaluation.EBI
J Med Chem 65: 14673-14691 (2022)
Universitat Aut£Noma De Barcelona
First-in-Class Dual Mechanism Ferroptosis-HDAC Inhibitor Hybrids.EBI
J Med Chem 65: 14764-14791 (2022)
University Of Toledo
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.EBI
J Med Chem 65: 14391-14408 (2022)
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASEBI
J Med Chem 65: 14614-14629 (2022)
Boehringer Ingelheim Rcv
Design, synthesis, and biological evaluation of 2-arylamino-4-(piperidin-4-yloxy)pyrimidines as potent EGFREBI
Bioorg Med Chem 74: (2022)
Shenyang Pharmaceutical University
Potent Uncompetitive Inhibitors of Nicotinamide EBI
J Med Chem 65: 14642-14654 (2022)
Harvard University
Screening of a Halogen-Enriched Fragment Library Leads to Unconventional Binding Modes.EBI
J Med Chem 65: 14539-14552 (2022)
Eberhard Karls Universit£T T£Bingen
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.EBI
J Med Chem 65: 14957-14969 (2022)
China Pharmaceutical University
Callintegers A and B, Unusual Tricyclo[
J Nat Prod 85: 2675-2681 (2022)
Yunnan Research & Development Center For Natural Products
Exploratory study of oxatomide derivatives with high P2XEBI
Bioorg Med Chem Lett 77: (2022)
Takasaki University Of Health And Welfare
Discovery of 4-methyl-3-(pyridin-2-ylamino)benzamide derivatives as C-Abl inhibitors with potential neuroprotective effect.EBI
Bioorg Med Chem 74: (2022)
Southern Medical University
Discovery of a Highly Potent and Orally Bioavailable STAT3 Dual Phosphorylation Inhibitor for Pancreatic Cancer Treatment.EBI
J Med Chem 65: 15487-15511 (2022)
East China Normal University
Novel Aryl Alkamidazole Derivatives as Multifunctional Antifungal Inhibitors: Design, Synthesis, and Biological Evaluation.EBI
J Med Chem 65: 14916-14937 (2022)
Liaocheng University
Overcoming Preclinical Safety Obstacles to Discover (EBI
J Med Chem 65: 14721-14739 (2022)
Jecure Therapeutics
Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-EBI
J Med Chem 65: 14809-14831 (2022)
Jinan University
Design, synthesis and biological evaluation of novel pyrazinone derivatives as PI3K/HDAC dual inhibitors.EBI
Bioorg Med Chem 74: (2022)
Lanzhou University
Scaffold hopping via ring opening enables identification of acyclic compounds as new complement Factor D inhibitors.EBI
Bioorg Med Chem 74: (2022)
Biocryst Pharmaceuticals
Discovery and Structure-Activity Relationship Studies of Novel Adenosine AEBI
J Med Chem 65: 14864-14890 (2022)
University Of Bern
Discovery and Structure-Based Design of Potent Covalent PPAR? Inverse-Agonists EBI
J Med Chem 65: 14843-14863 (2022)
Broad Institute Of Mit And Harvard
Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.EBI
Bioorg Med Chem 74: (2022)
China Pharmaceutical University
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.EBI
Bioorg Med Chem 74: (2022)
China Pharmaceutical University
Rational Design, Synthesis, and Biological Evaluation of Novel S1PR2 Antagonists for Reversing 5-FU-Resistance in Colorectal Cancer.EBI
J Med Chem 65: 14553-14577 (2022)
Ocean University Of China
New Dual P-Glycoprotein (P-gp) and Human Carbonic Anhydrase XII (hCA XII) Inhibitors as Multidrug Resistance (MDR) Reversers in Cancer Cells.EBI
J Med Chem 65: 14655-14672 (2022)
University Of Florence
Identification and Biochemical Characterization of Pyrrolidinediones as Novel Inhibitors of the Bacterial Enzyme MurA.EBI
J Med Chem 65: 14740-14763 (2022)
Saarland University
Novel Lactams as Cbl-b Inhibitors for Treating Cancer.EBI
ACS Med Chem Lett 13: 1556-1557 (2022)
Smith, Gambrell & Russell
Boron-Containing Pyrazole Compounds as JAK Inhibitors for Treating Inflammation, Autoimmune Diseases, and Cancer.EBI
ACS Med Chem Lett 13: 1554-1555 (2022)
Smith, Gambrell & Russell
Factor XI Activation Inhibitors for Treating Thromboses, Embolism, Hypercoagulability, or Fibrotic Changes.EBI
ACS Med Chem Lett 13: 1548-1549 (2022)
Smith, Gambrell & Russell
ALK Inhibitors for Treating Cancer, Blood, and Kidney Diseases.EBI
ACS Med Chem Lett 13: 1539-1541 (2022)
Usona Institute
Selective Cyclin-Dependent Kinase Inhibitors and Their Application in Cancer Therapy.EBI
ACS Med Chem Lett 13: 1561-1563 (2022)
Usona Institute
Novel Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors.EBI
ACS Med Chem Lett 13: 1537-1538 (2022)
Smith, Gambrell & Russell
The Pursuit of Enzyme Activation: A Snapshot of the Gold Rush.EBI
J Med Chem 65: 14289-14304 (2022)
Baylor College Of Medicine
Development of Noncovalent Small-Molecule Keap1-Nrf2 Inhibitors by Fragment-Based Drug Discovery.EBI
J Med Chem 65: 14481-14526 (2022)
University Of Copenhagen
Small Molecule Inhibitors of Lymphocyte Perforin as Focused Immunosuppressants for Infection and Autoimmunity.EBI
J Med Chem 65: 14305-14325 (2022)
University Of Auckland
Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20.EBI
ACS Med Chem Lett 13: 1648-1654 (2022)
The University Of Chicago
Novel Substituted Cyclopropyl Compounds as CFTR Modulators for Treating Cystic Fibrosis.EBI
ACS Med Chem Lett 13: 1552-1553 (2022)
Smith, Gambrell & Russell
Development of Esterase-Resistant and Highly Active Ghrelin Analogs via Thiol-Ene Click Chemistry.EBI
ACS Med Chem Lett 13: 1655-1662 (2022)
Tongji University
Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization.EBI
ACS Med Chem Lett 13: 1634-1641 (2022)
Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates.EBI
ACS Med Chem Lett 13: 1568-1573 (2022)
Kyoto Prefectural University Of Medicine
Design, Synthesis, and Monoamine Oxidase B Selective Inhibitory Activity of EBI
ACS Med Chem Lett 13: 1582-1590 (2022)
Osaka University
Synthesis and Structural Characterization of Novel Trihalo-sulfone Inhibitors of WNK1.EBI
ACS Med Chem Lett 13: 1678-1684 (2022)
The University Of Texas Southwestern Medical Center At Dallas
Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader.EBI
ACS Med Chem Lett 13: 1621-1627 (2022)
University Of Minnesota
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.EBI
ACS Med Chem Lett 13: 1591-1597 (2022)
Astex Pharmaceuticals
Design and Characterization of Novel Small Molecule Activators of Excitatory Amino Acid Transporter 2.EBI
ACS Med Chem Lett 13: 1628-1633 (2022)
Drexel University College Of Medicine
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.EBI
ACS Med Chem Lett 13: 1574-1581 (2022)
Chinese Academy Of Sciences
Amino-cyclohexane Carboxylic Acid Inhibitors of Arginase.EBI
ACS Med Chem Lett 13: 1550-1551 (2022)
Arrival Discovery
BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe.EBI
J Med Chem 65: 14366-14390 (2022)
Bayer Pharma
Identification of 1,4-Benzodiazepine-2,5-dione Derivatives as Potential Protein Synthesis Inhibitors with Highly Potent Anticancer Activity.EBI
J Med Chem 65: 14891-14915 (2022)
Tsinghua University
Therapeutic Activity of the Lansoprazole Metabolite 5-Hydroxy Lansoprazole Sulfide in Triple-Negative Breast Cancer by Inhibiting the Enoyl Reductase of Fatty Acid Synthase.EBI
J Med Chem 65: 13681-13691 (2022)
Indiana University School Of Medicine
Structure-Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens.EBI
J Med Chem 65: 14144-14179 (2022)
University Of Minnesota
Discovery of EBI
J Med Chem 65: 14180-14200 (2022)
Helmholtz-Institute For Pharmaceutical Research Saarland (Hips)
Target-Focused Library Design by Pocket-Applied Computer Vision and Fragment Deep Generative Linking.EBI
J Med Chem 65: 13771-13783 (2022)
Umr7200 Cnrs-Universit£
Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of EBI
J Med Chem 65: 13813-13832 (2022)
University Of Texas Md Anderson Cancer Center
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.EBI
J Med Chem 65: 13629-13644 (2022)
Kalvista Pharmaceuticals
Discovery of Chlorofluoroacetamide-Based Covalent Inhibitors for Severe Acute Respiratory Syndrome Coronavirus 2 3CL Protease.EBI
J Med Chem 65: 13852-13865 (2022)
Kyushu University
Discovery of a new class of valosine containing protein (VCP/P97) inhibitors for the treatment of colorectal cancer.EBI
Bioorg Med Chem 74: (2022)
Nanjing Normal University
Potent and Specific Activators for Mitochondrial Sirtuins Sirt3 and Sirt5.EBI
J Med Chem 65: 14015-14031 (2022)
University Of Bayreuth
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.EBI
J Med Chem 65: 13714-13735 (2022)
Medical College Of Wisconsin
Synthesis, In Vitro Profiling, and In Vivo Evaluation of Benzohomoadamantane-Based Ureas for Visceral Pain: A New Indication for Soluble Epoxide Hydrolase Inhibitors.EBI
J Med Chem 65: 13660-13680 (2022)
Universitat De Barcelona
Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer.EBI
J Med Chem 65: 13645-13659 (2022)
Fudan University
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of EBI
J Med Chem 65: 14121-14143 (2022)
Inhibition of glutathione S-transferases by photoactive calix[4]arene ?-ketophosphonic acids.EBI
Bioorg Med Chem Lett 77: (2022)
V.P. Kukhar Institute Of Bioorganic Chemistry And Petrochemistry Of The National Academy Of Sciences Of Ukraine
Fluorophenylalkyl-substituted cyanoguanidine derivatives as bacteria-selective MATE transporter inhibitors for the treatment of antibiotic-resistant infections.EBI
Bioorg Med Chem 74: (2022)
Setsunan University
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.EBI
Bioorg Med Chem Lett 76: (2022)
Guru Nanak Dev University
Zinc-dependent deacetylases (HDACs) as potential targets for treating Alzheimer's disease.EBI
Bioorg Med Chem Lett 76: (2022)
Guizhou Medical University
Design and evaluation of novel analogs of 2-amino-4-boronobutanoic acid (ABBA) as inhibitors of human gamma-glutamyl transpeptidase.EBI
Bioorg Med Chem 73: (2022)
State University Of New York
Discovery and optimization of orally bioavailable and potent plasma Kallikrein inhibitors bearing a quaternary carbon.EBI
Bioorg Med Chem 73: (2022)
Biocryst Pharmaceuticals
Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery.EBI
J Med Chem 65: 13483-13504 (2022)
The University Of Sydney
Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.EBI
J Med Chem 65: 13705-13713 (2022)
Cardiff University
Targeting Extracellular Signal-Regulated Protein Kinase 1/2 (ERK1/2) in Cancer: An Update on Pharmacological Small-Molecule Inhibitors.EBI
J Med Chem 65: 13561-13573 (2022)
Southwest Jiaotong University
Natural Product-Inspired Targeted Protein Degraders: Advances and Perspectives.EBI
J Med Chem 65: 13533-13560 (2022)
Tongji University School Of Medicine
Discovery of BT8009: A Nectin-4 Targeting Bicycle Toxin Conjugate for the Treatment of Cancer.EBI
J Med Chem 65: 14337-14347 (2022)
Discovery, Chemistry, and Preclinical Development of Pritelivir, a Novel Treatment Option for Acyclovir-Resistant Herpes Simplex Virus Infections.EBI
J Med Chem 65: 13614-13628 (2022)
Aicuris Anti-Infective Cures
Synthesis and antidepressant activity of novel 1-(1-benzoylpiperidin-4-yl) methanamine derivatives selectively targeting SSRI/5-HTEBI
Bioorg Med Chem Lett 76: (2022)
Shanghai Institute Of Pharmaceutical Industry
Development of a putative ZnEBI
Bioorg Med Chem Lett 76: (2022)
Graz University Of Technology
Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.EBI
J Med Chem 65: 13946-13966 (2022)
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists.EBI
J Med Chem 65: 14082-14103 (2022)
Czech Academy Of Sciences
Lectin-Targeted Prodrugs Activated by EBI
J Med Chem 65: 13988-14014 (2022)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.EBI
J Med Chem 65: 13879-13891 (2022)
Artios Pharma
Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.EBI
J Med Chem 65: 14237-14260 (2022)
Icahn School Of Medicine At Mount Sinai
Structure-Based Design of Active-Site-Directed, Highly Potent, Selective, and Orally Bioavailable Low-Molecular-Weight Protein Tyrosine Phosphatase Inhibitors.EBI
J Med Chem 65: 13892-13909 (2022)
Eli Lilly
Synthesis of capuramycin and its analogues via a Ferrier-type I reaction and their biological evaluation.EBI
Bioorg Med Chem 73: (2022)
Hokkaido University
Discovery of novel compounds as potent activators of Sirt3.EBI
Bioorg Med Chem 73: (2022)
Pmc Isochem
Discovery of 2-Methyl-2-(4-(2-methyl-8-(1EBI
J Med Chem 65: 12781-12801 (2022)
West China Hospital Of Sichuan University
Structure-activity relationship studies in a new series of 2-amino-N-phenylacetamide inhibitors of Slack potassium channels.EBI
Bioorg Med Chem Lett 76: (2022)
University Of North Texas Health Science Center
Structure-based design and modular synthesis of novel PI4K class II inhibitors bearing a 4-aminoquinazoline scaffold.EBI
Bioorg Med Chem Lett 76: (2022)
Institute Of Organic Chemistry And Biochemistry Of The Czech Academy Of Sciences
Identification of PI3K/HDAC Dual-targeted inhibitors with subtype selectivity as potential therapeutic agents against solid Tumors: Building HDAC6 potency in a Quinazolinone-based PI3K?-selective template.EBI
Bioorg Med Chem 73: (2022)
Anhui University Of Chinese Medicine
Isatoic anhydrides as novel inhibitors of monoamine oxidase.EBI
Bioorg Med Chem 73: (2022)
North-West University
Diastereomeric Resolution Yields Highly Potent Inhibitor of SARS-CoV-2 Main Protease.EBI
J Med Chem 65: 13328-13342 (2022)
Bio-Techne (Tocris)
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.EBI
J Med Chem 65: 13052-13073 (2022)
F. Hoffmann-La Roche
Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.EBI
J Med Chem 65: 13013-13028 (2022)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie
Selective deuteration of bupropion slows epimerization and reduces metabolism.EBI
Bioorg Med Chem Lett 76: (2022)
University Of Washington
Synthesis and biological evaluation of (4-hydroxy-2-(substitued sulfonamido)pyrimidine-5-carbonyl)glycines as oral erythropoietin secretagogues.EBI
Bioorg Med Chem Lett 76: (2022)
Tianjin Institute Of Medical & Pharmaceutical Sciences
Structure-Based Optimization of Coumestan Derivatives as Polyketide Synthase 13-Thioesterase(Pks13-TE) Inhibitors with Improved hERG Profiles for EBI
J Med Chem 65: 13240-13252 (2022)
East China Normal University
Development of MAO-A and 5-HTEBI
J Med Chem 65: 13385-13400 (2022)
China Pharmaceutical University
Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.EBI
J Med Chem 65: 14032-14048 (2022)
Jinan University
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.EBI
J Med Chem 65: 13305-13327 (2022)
National And Kapodistrian University Of Athens
Discovery of Orally Bioavailable SOS1 Inhibitors for Suppressing KRAS-Driven Carcinoma.EBI
J Med Chem 65: 13158-13171 (2022)
Wuhan University Of Science And Technology
Boronic Acid: A Novel Pharmacophore Targeting Src Homology 2 (SH2) Domain of STAT3.EBI
J Med Chem 65: 13094-13111 (2022)
Sun Yat-Sen University
Linker-Dependent Folding Rationalizes PROTAC Cell Permeability.EBI
J Med Chem 65: 13029-13040 (2022)
Uppsala University
Hypoxia-Activated Prodrugs with Dual COX-2/CA Inhibitory Effects on Attenuating Cardiac Inflammation under Hypoxia.EBI
J Med Chem 65: 13436-13451 (2022)
Southeast University
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.EBI
J Med Chem 65: 12956-12969 (2022)
The University Of Queensland
Identification of Novel 2,4,5-Trisubstituted Pyrimidines as Potent Dual Inhibitors of Plasmodial EBI
J Med Chem 65: 13172-13197 (2022)
University Of North Carolina At Chapel Hill
Design, Synthesis, Biological Activity, and Structural Analysis of Novel Des-C-Ring and Aromatic-D-Ring Analogues of 1?,25-Dihydroxyvitamin DEBI
J Med Chem 65: 13112-13124 (2022)
University Of Santiago De Compostela
Piptide Chemotypes for Perturbation of the Interaction of Urokinase with Its Receptor.EBI
J Med Chem 65: 12925-12932 (2022)
Texas A&M University
Design, synthesis, in-vitro, in-vivo and ex-vivo pharmacology of thiazolidine-2,4-dione derivatives as selective and reversible monoamine oxidase-B inhibitors.EBI
Bioorg Med Chem Lett 76: (2022)
Comsats University Islamabad
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-EBI
J Med Chem 65: 12701-12724 (2022)
University Of Turin
Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease.EBI
J Med Chem 65: 12626-12638 (2022)
Galecto Biotech
Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases.EBI
J Med Chem 65: 12933-12955 (2022)
Helmholtz Center For Infection Research (Hzi)
Discovery of 2-(1-(3-Chloro-4-cyanophenyl)-1EBI
J Med Chem 65: 13074-13093 (2022)
Zhejiang University
Histone Deacetylase and Enhancer of Zeste Homologue 2 Dual Inhibitors Presenting a Synergistic Effect for the Treatment of Hematological Malignancies.EBI
J Med Chem 65: 12838-12859 (2022)
China Pharmaceutical University
A high quality, industrial data set for binding affinity prediction: performance comparison in different early drug discovery scenarios.BDB
J Comput Aided Mol Des 36: 753-765 (2022)
F. Hoffmann-La Roche
Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.EBI
Bioorg Med Chem 73: (2022)
Peking Union Medical College And Chinese Academy Of Medical Sciences
Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors.EBI
Bioorg Med Chem 73: (2022)
Southern Medical University
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2EBI
J Med Chem 65: 13967-13987 (2022)
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation.EBI
J Med Chem 65: 13365-13384 (2022)
Eberhard Karls University T£Bingen
Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput.EBI
J Med Chem 65: 13288-13304 (2022)
Leiden University Medical Center
New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus.EBI
Bioorg Med Chem 73: (2022)
Al-Azhar University
Subtilisin-like Serine Protease 1 (SUB1) as an Emerging Antimalarial Drug Target: Current Achievements in Inhibitor Discovery.EBI
J Med Chem 65: 12535-12545 (2022)
Latvian Institute Of Organic Synthesis
Discovery of Highly Potent and Selective Matrix Metalloproteinase-7 Inhibitors by Hybridizing the S1' Subsite Binder with Short Peptides.EBI
J Med Chem 65: 13253-13263 (2022)
Taisho Pharmaceutical
Mechanism of Action and Structure-Activity Relationship of ?-Conotoxin Mr1.1 at the Human ?9?10 Nicotinic Acetylcholine Receptor.EBI
J Med Chem 65: 16204-16217 (2022)
Ocean University Of China
Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes.EBI
J Med Chem 65: 13264-13287 (2022)
Johann Wolfgang Goethe-University
Design, synthesis and biological evaluations of novel farnesoid X receptor (FXR) agonists.EBI
Bioorg Med Chem Lett 76: (2022)
Shandong University
Design, synthesis and biological evaluation of pteridine-7(8H)-one derivatives as potent and selective CDK4/6 inhibitors.EBI
Bioorg Med Chem Lett 76: (2022)
East China University Of Science & Technology
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.EBI
J Med Chem 65: 12895-12924 (2022)
Rapt Therapeutics
Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy.EBI
J Med Chem 65: 13216-13239 (2022)
Anhui Medical University
Identification of EBI
J Med Chem 65: 13198-13215 (2022)
Repare Therapeutics
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.EBI
J Nat Prod 85: 2424-2432 (2022)
Chinese Academy Of Sciences
Development of Hydrogen Sulfide-Releasing Carbonic Anhydrases IX- and XII-Selective Inhibitors with Enhanced Antihyperalgesic Action in a Rat Model of Arthritis.EBI
J Med Chem 65: 13143-13157 (2022)
University Of Firenze
Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4.EBI
J Med Chem 65: 12725-12746 (2022)
Lunenfeld-Tanenbaum Research Institute
Discovery of a potent MEBI
Bioorg Med Chem Lett 76: (2022)
Vanderbilt University
A simplified analog of debromoaplysiatoxin lacking the B-ring of spiroketal moiety retains protein kinase C-binding and antiproliferative activities.EBI
Bioorg Med Chem 73: (2022)
Kagawa University
Discovery of Novel Pyrazole-Based KDM5B Inhibitor EBI
J Med Chem 65: 12979-13000 (2022)
Zhengzhou University
Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of ?-Coronaviruses.EBI
J Med Chem 65: 12860-12882 (2022)
University Of North Carolina At Chapel Hill
Inhibiting Sodium Taurocholate Cotransporting Polypeptide in HBV-Related Diseases: From Biological Function to Therapeutic Potential.EBI
J Med Chem 65: 12546-12561 (2022)
Southwest Jiaotong University
Fragment Ligands of the mEBI
ACS Med Chem Lett 13: 1500-1509 (2022)
University Of Zurich
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.EBI
J Med Chem 65: 13343-13364 (2022)
Shandong University
Discovery of Betulinic Acid Derivatives as Potent Intestinal Farnesoid X Receptor Antagonists to Ameliorate Nonalcoholic Steatohepatitis.EBI
J Med Chem 65: 13452-13472 (2022)
Chinese Academy Of Sciences
Novel Coronavirus Main Protease Di- and Tripeptide Inhibitors for Treating COVID-19.EBI
ACS Med Chem Lett 13: 1388-1389 (2022)
Experimental Drug Development Centre
Stereoisomers of an Aryl Pyrazole Glucocorticoid Receptor Agonist Scaffold Elicit Differing Anti-inflammatory Responses.EBI
ACS Med Chem Lett 13: 1493-1499 (2022)
University Of Tennessee
Oral Nonpeptidic, Noncovalent Triazine Coronavirus Main Protease Inhibitors for Treating COVID-19.EBI
ACS Med Chem Lett 13: 1394-1396 (2022)
Experimental Drug Development Centre
Substituted 6,7-Dihydro-5EBI
ACS Med Chem Lett 13: 1392-1393 (2022)
Smith, Gambrell & Russell
2-Amino-1,3,4-thiadiazoles as Glutaminyl Cyclases Inhibitors Increase Phagocytosis through Modification of CD47-SIRP? Checkpoint.EBI
ACS Med Chem Lett 13: 1459-1467 (2022)
Ewha Womans University
Identification of a BAZ2A-Bromodomain Hit Compound by Fragment Growing.EBI
ACS Med Chem Lett 13: 1434-1443 (2022)
University Of Trento
Restoration of Motor Function Post-Neurological Injury Using Serotonergic Agonist.EBI
ACS Med Chem Lett 13: 1397-1399 (2022)
Usona Institute
Orexin Receptor Agonists as Possible Treatment for Narcolepsy and Idiopathic Hypersomnia.EBI
ACS Med Chem Lett 13: 1411-1412 (2022)
Therachem Research Medilab
Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction.EBI
ACS Med Chem Lett 13: 1510-1516 (2022)
University Of Texas Southwestern Medical Center
Multicomponent Macrocyclic IL-17a Modifier.EBI
ACS Med Chem Lett 13: 1468-1471 (2022)
University Of Groningen
Biological Effects of Modifications of the Englerin A Glycolate.EBI
ACS Med Chem Lett 13: 1472-1476 (2022)
National Cancer Institute
Novel 3-Aminopyrrolidine and Piperidine Macrocyclic Orexin Receptor Agonists for Treating Sleep Disorders.EBI
ACS Med Chem Lett 13: 1390-1391 (2022)
Smith, Gambrell & Russell
Structure-Activity Relationship and EBI
ACS Med Chem Lett 13: 1485-1492 (2022)
Riken Center For Biosystems Dynamics Research
Discovery of a Novel Potent STAT3 Inhibitor HP590 with Dual p-TyrEBI
J Med Chem 65: 12650-12674 (2022)
East China Normal University
X-ray Screening of an Electrophilic Fragment Library and Application toward the Development of a Novel ERK 1/2 Covalent Inhibitor.EBI
J Med Chem 65: 12319-12333 (2022)
Astex Pharmaceuticals
Discovery of ?-Arrestin-Biased 25CN-NBOH-Derived 5-HTEBI
J Med Chem 65: 12031-12043 (2022)
University Of Copenhagen
The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the ?EBI
J Med Chem 65: 12367-12385 (2022)
Monash University (Parkville Campus)
Naturally Occurring Partially Reduced Perylenequinones from Fungi.EBI
J Nat Prod 85: 2236-2250 (2022)
Universidade Federal Da Bahia
Highly Potent and Selective Dopamine DEBI
J Med Chem 65: 12124-12139 (2022)
The Natural Products Withaferin A and Withanone from the Medicinal Herb EBI
J Nat Prod 85: 2340-2350 (2022)
Shiv Nadar University
Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.EBI
J Med Chem 65: 12445-12459 (2022)
Charles River Laboratories
Bisubstrate Inhibitors of Severe Acute Respiratory Syndrome Coronavirus-2 Nsp14 Methyltransferase.EBI
ACS Med Chem Lett 13: 1477-1484 (2022)
University Of Minnesota
Discovery of Novel Src Homology-2 Domain-Containing Phosphatase 2 and Histone Deacetylase Dual Inhibitors with Potent Antitumor Efficacy and Enhanced Antitumor Immunity.EBI
J Med Chem 65: 12200-12218 (2022)
Shandong University
Spiroisoxazoline Inhibitors of Acetylcholinesterase from EBI
J Nat Prod 85: 2207-2216 (2022)
University Of Riau
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia.EBI
J Med Chem 65: 12014-12030 (2022)
Newcastle University
Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.EBI
RSC Med Chem 13: 944-954 (2022)
Julius Maximilian University Of W�Rzburg
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.EBI
RSC Med Chem 13: 963-969 (2022)
University Of Maryland
Development of tumor-targeting aza-vesamicol derivatives with high affinity for sigma receptors for cancer theranostics.EBI
RSC Med Chem 13: 986-997 (2022)
Kanazawa University
Design and Characterization of a Natural Arf-GEFs Inhibitor Prodrug EBI
J Med Chem 65: 11970-11984 (2022)
Ocean University Of China
Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.EBI
J Med Chem 65: 12292-12318 (2022)
Yeditepe University
Development of Inhibitors Targeting the V-Domain Ig Suppressor of T Cell Activation Signal Pathway.EBI
J Med Chem 65: 11900-11912 (2022)
China Pharmaceutical University
Cyclic Peptide Screening Methods for Preclinical Drug Discovery.EBI
J Med Chem 65: 11913-11926 (2022)
University Of Washington
Design, Synthesis, and Biological Evaluation of Dual-Target COX-2/CYP51 Inhibitors for the Treatment of Fungal Infectious Diseases.EBI
J Med Chem 65: 12219-12239 (2022)
Liaocheng University
Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner.EBI
J Med Chem 65: 12334-12345 (2022)
Purdue University
First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation.EBI
J Med Chem 65: 12140-12162 (2022)
Ocean University Of China
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.EBI
J Med Chem 65: 11840-11853 (2022)
Chinese Academy Of Sciences
Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.EBI
J Med Chem 65: 12460-12481 (2022)
Shanghai Institute Of Materia Medica
Discovery of Selenium-Containing STING Agonists as Orally Available Antitumor Agents.EBI
J Med Chem 65: 15048-15065 (2022)
China Pharmaceutical University
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors.EBI
J Med Chem 65: 12386-12402 (2022)
Novartis Institutes For Biomedical Research
Discovery of the Novel 1EBI
J Med Chem 65: 12095-12123 (2022)
Anhui Medical University
Discovery of Cyclic Peptide Inhibitors Targeting PD-L1 for Cancer Immunotherapy.EBI
J Med Chem 65: 12002-12013 (2022)
University Of Missouri-Kansas City
Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.EBI
J Med Chem 65: 12427-12444 (2022)
Chugai Pharmaceutical
Discovery of a Novel Oral Proteasome Inhibitor to Block NLRP3 Inflammasome Activation with Anti-inflammation Activity.EBI
J Med Chem 65: 11985-12001 (2022)
Guangzhou Medical University
From a Cone Snail Toxin to a Competitive MC4R Antagonist.EBI
J Med Chem 65: 12084-12094 (2022)
Discovery of Novel Imidazo[4,5-EBI
J Med Chem 65: 11949-11969 (2022)
Chinese Academy Of Sciences
Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer.EBI
J Med Chem 65: 12346-12366 (2022)
Sun Yat-Sen University
Zamamiphidins B and C, Manzamine-Related Alkaloids from an EBI
J Nat Prod 85: 2226-2231 (2022)
Showa Pharmaceutical University
J Med Chem 65: 12256-12272 (2022)
Universidad Complutense De Madrid
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.EBI
J Med Chem 65: 11927-11948 (2022)
Bristol Myers Squibb Research And Early Development
Discovery of IHMT-MST1-58 as a Novel, Potent, and Selective MST1 Inhibitor for the Treatment of Type 1/2 Diabetes.EBI
J Med Chem 65: 11818-11839 (2022)
Chinese Academy Of Sciences
Discovery of Potent and Selective Transient Receptor Potential Vanilloid 1 (TRPV1) Agonists with Analgesic Effects EBI
J Med Chem 65: 11658-11678 (2022)
Fudan University
Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities.EBI
J Med Chem 65: 11745-11758 (2022)
Sun Yat-Sen University
Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction.EBI
J Med Chem 65: 11485-11496 (2022)
Semisynthetic Transformations on (+)-Boldine Reveal a 5-HTEBI
J Nat Prod 85: 2149-2158 (2022)
City University Of New York

BDB Curated by BindingDB
EBI Curated by ChEMBL