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Discovery of New Imidazo[2,1-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6877-6901 (2021)
National Research Centre (Nrc)
Novel Mixed NOP/Opioid Receptor Peptide Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6656-6669 (2021)
University of Ferrara
Pyrimidine-based EGFR TK inhibitors in targeted cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Tehran University of Medical Sciences
Natural products and analogs as preventive agents for metabolic syndrome via peroxisome proliferator-activated receptors: An overview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
University Clinic Hospital of Valencia
Design, synthesis and biological evaluation of 3, 4-disubstituted-imidazolidine-2, 5-dione derivatives as HDAC6 selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Shandong University
Computer-aided design of 1,4-naphthoquinone-based inhibitors targeting cruzain and rhodesain cysteine proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 41: (2021)
Federal University of Alagoas
A novel GSK-3 inhibitor binds to GSK-3? via a reversible, time and Cys-199-dependent mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Ohio University
Nitrile-based peptoids as cysteine protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 41: (2021)
University of S£O Paulo
Green synthesis of therapeutically active 1,3,4-oxadiazoles as antioxidants, selective COX-2 inhibitors and their in silico studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Karnatak University
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 47: (2021)
Glaxosmithkline
Discovery of a new class of JMJD6 inhibitors and structure-activity relationship study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 44: (2021)
Nankai University
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 44: (2021)
Merck
Development of BET inhibitors as potential treatments for cancer: A search for structural diversity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 44: (2021)
Bristol Myers Squibb Research and Development
Synthesis and Evaluation of PPAR? Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6996-7032 (2021)
University of Toledo College of Pharmacy and Pharmaceutical Sciences
Synthesis, Structure-Activity Relationships, and In Vivo Evaluation of Novel Tetrahydropyran-Based Thiodisaccharide Mimics as Galectin-3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6634-6655 (2021)
Bristol Myers Squibb
Dual-target compounds for Alzheimer's disease: Natural and synthetic AChE and BACE-1 dual-inhibitors and their structure-activity relationship (SAR).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
University of Aveiro
Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 44: (2021)
Roche Innovation Center Shanghai
Promising anti-SARS-CoV-2 drugs by effective dual targeting against the viral and host proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Bristol University
Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
University Hospital Hradec Kralove
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 10682-10710 (2021)
Goethe University Frankfurt Am Main
Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Agri Ibrahim Cecen University
Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Shandong University
Dual-Targeting Antiproliferation Hybrids Derived from 1-Deoxynojirimycin and Kaempferol Induce MCF-7 Cell Apoptosis through the Mitochondria-Mediated Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1534-1543 (2021)
Jiangsu University of Science and Technology
Structure-Guided Discovery of Potent and Selective DYRK1A Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6745-6764 (2021)
Servier Research Institute of Medicinal Chemistry
Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
University of Pisa
Structure-Guided Design of the First Noncovalent Small-Molecule Inhibitor of CRM1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6596-6607 (2021)
Sichuan University and Collaborative Innovation Centre of Biotherapy
Development of Selective FXIa Inhibitors Based on Cyclic Peptides and Their Application for Safe Anticoagulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6802-6813 (2021)
Ecole Polytechnique F�D�Rale De Lausanne (Epfl)
Design and Synthesis of Highly Selective Brain Penetrant p38? Mitogen-Activated Protein Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 1225-1242 (2022)
Eberhard Karls Universit£T T£Bingen
Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6856-6876 (2021)
China Pharmaceutical University
Design, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
China Pharmaceutical University
Exploiting the HSP60/10 chaperonin system as a chemotherapeutic target for colorectal cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Indiana University School of Medicine
Discovery of novel tripeptide propylene oxide proteasome inhibitors for the treatment of multiple myeloma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Nanjing Normal University
Kinase Inhibitors as Underexplored Antiviral Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 935-954 (2022)
Centro De Investigaciones Biol�Gicas Margarita Salas (Csic)
Adamantane derivatives as potential inhibitors of p37 major envelope protein and poxvirus reproduction. Design, synthesis and antiviral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Samara State Technical University
Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Egyptian Russian University
Novel hybrid conjugates with dual estrogen receptor ? degradation and histone deacetylase inhibitory activities for breast cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Wuhan University
Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Shanghai University of Traditional Chinese Medicine
Using conformational constraints at position 6 of Angiotensin II to generate compounds with enhanced AT2R selectivity and proteolytic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Vrije Universiteit Brussel
Design, synthesis and evaluation of novel 9-arylalkyl-10-methylacridinium derivatives as highly potent FtsZ-targeting antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Shandong University
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Ningxia Medical University
Folate-targeted verrucarin A reduces the number of activated macrophages in a mouse model of acute peritonitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
Indian Institute of Technology Indore
1,2,4-Triazolo[1,5-a]pyrimidines: Efficient one-step synthesis and functionalization as influenza polymerase PA-PB1 interaction disruptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
University of Perugia
Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
South Valley University
Halting the Spread of Herpes Simplex Virus-1: The Discovery of an Effective Dual ?v?6/?v?8 Integrin Ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6972-6984 (2021)
Universit£
Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
University of Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Xinxiang Medical University
Cryptic Biosynthesis of the Berkeleypenostatins from Coculture of Extremophilic ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1656-1665 (2021)
TBA
Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1? Axis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1563-1572 (2021)
University of Rhode Island
Discovery of Novel, Potent Inhibitors of Hydroxy Acid Oxidase 1 (HAO1) Using DNA-Encoded Chemical Library Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6730-6744 (2021)
X-Chem
Design and evaluation of 1,2,3-dithiazoles and fused 1,2,4-dithiazines as anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
University of North Carolina At Chapel Hill
Neuroactive Type-A ?-Aminobutyric Acid Receptor Allosteric Modulator Steroids from the Hypobranchial Gland of Marine Mollusk, ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 7033-7043 (2021)
University of Utah
Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5667-5688 (2021)
Sorbonne Universit£
Macrocyclic Peptides that Selectively Inhibit the ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6262-6272 (2021)
Weill Cornell Medicine
Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Shenyang Pharmaceutical University
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 221: (2021)
Harvard Medical School
Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5850-5862 (2021)
University of Kentucky
Efficient Dimerization Disruption of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6137-6160 (2021)
Instituto De Qu£Mica M£Dica (Iqm-Csic)
From the Design to the ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5429-5446 (2021)
Unitat Associada Al Csic
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6358-6380 (2021)
Biogen
X-ray Crystal Structure-Guided Design and Optimization of 7![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6985-6995 (2021)
Yonsei University
Discovery of cytotoxic natural products from Red Sea sponges: Structure and synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Csir-National Institute of Oceanography
Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Sichuan University
Synthesis, biological, and photophysical studies of molecular rotor-based fluorescent inhibitors of the trypanosome alternative oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Instituto De Qu£Mica M£Dica
Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6037-6058 (2021)
Galapagos
Discovery of Potent Coumarin-Based Kinetic Stabilizers of Amyloidogenic Immunoglobulin Light Chains Using Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6273-6299 (2021)
The Scripps Research Institute
Pharmacological Targeting of Executioner Proteins: Controlling Life and Death.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5276-5290 (2021)
University of Toronto
Structure-Based Discovery of Pyrimidine Aminobenzene Derivatives as Potent Oral Reversal Agents against P-gp- and BCRP-Mediated Multidrug Resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6179-6197 (2021)
China Pharmaceutical University
Discovery of 4-Arylindolines Containing a Thiazole Moiety as Potential Antitumor Agents Inhibiting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5519-5534 (2021)
Shenyang Pharmaceutical University
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Taipei Medical University
Design and biological evaluation of cinnamic and phenylpropionic amide derivatives as novel dual inhibitors of HIV-1 protease and reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Chinese Academy of Medical Science and Peking Union Medical College
A ?-lactam siderophore antibiotic effective against multidrug-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae, and Acinetobacter spp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Louis Stokes Cleveland Department of Veterans Affairs Medical Center
Rational modification, synthesis and biological evaluation of N-substituted phthalazinone derivatives designed to target interleukine-15 protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
Universit£
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 40: (2021)
Emd Serono Research & Development Institute
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Bristol-Myers Squibb
Discovery of a potent and selective Axl inhibitor in preclinical model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
Eisai
Design, synthesis of novel celastrol derivatives and study on their antitumor growth through HIF-1? pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Yanbian University
Overview of piperlongumine analogues and their therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Nantong University
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5816-5837 (2021)
Shanghai Institute of Materia Medica
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6329-6357 (2021)
Novartis Institutes For Biomedical Research
Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Karlsruhe Institute of Technology (Kit)
Discovery of Orally Bioavailable Purine-Based Inhibitors of the Low-Molecular-Weight Protein Tyrosine Phosphatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5645-5653 (2021)
University of California
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5730-5745 (2021)
Csic
Design of Dimeric Bile Acid Derivatives as Potent and Selective Human NTCP Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5973-6007 (2021)
National Institute of Biological Sciences
Design and evaluation of novel piperidine HIV-1 protease inhibitors with potency against DRV-resistant variants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Chinese Academy of Medical Science and Peking Union Medical College
Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
China Pharmaceutical University
A novel Hsp70 inhibitor specifically targeting the cancer-related Hsp70-Bim protein-protein interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Dalian University of Technology
Developments of small molecules as inhibitors for carbonic anhydrase isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
Georgia State University
Covalent Small Molecule Immunomodulators Targeting the Protease Active Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5291-5322 (2021)
National Cancer Institute
Heterodimeric GW7604 Derivatives: Modification of the Pharmacological Profile by Additional Interactions at the Coactivator Binding Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5766-5786 (2021)
University of Innsbruck
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5905-5930 (2021)
University of Dundee
Discovery of 2-(3-(3-Carbamoylpiperidin-1-yl)phenoxy)acetic Acid Derivatives as Novel Small-Molecule Inhibitors of the ?-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5886-5904 (2021)
H. Lee Moffitt Cancer Center and Research Institute
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human ?7 Nicotinic Acetylcholine Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5620-5631 (2021)
Hainan University
Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
India
Fused-azepinones: Emerging scaffolds of medicinal importance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Beyond direct Nrf2 activation; reinvestigating 1,2,4-oxadiazole scaffold as a master key unlocking the antioxidant cellular machinery for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Alexandria University
Chemoenzymatic synthesis of 2,6-disubstituted tetrahydropyrans with high ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Westf£Lische Wilhelms-Universit£T M£Nster
Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
University of Auckland
Discovery of boronic acid-based potent activators of tumor pyruvate kinase M2 and development of gastroretentive nanoformulation for oral dosing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
National Institute of Pharmaceutical Education and Research-Ahmedabad
Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5956-5972 (2021)
Northeastern University
Fragment-Based Design of a Potent MAT2a Inhibitor and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6814-6826 (2021)
Astrazeneca
Discovery of a Vitamin D Receptor-Silent Vitamin D Derivative That Impairs Sterol Regulatory Element-Binding Protein In Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5689-5709 (2021)
Teikyo University
Using NMR to identify binding regions for N and C-terminal Hsp90 inhibitors using Hsp90 domains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 12: 410-415 (2021)
University of New South Wales
Overview of all-trans-retinoic acid (ATRA) and its analogues: Structures, activities, and mechanisms in acute promyelocytic leukaemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Shaanxi University of Science & Technology
Aminopyrazole based CDK9 PROTAC sensitizes pancreatic cancer cells to venetoclax.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
University of Nebraska Medical Center
Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Hibercell
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 220: (2021)
Shenyang Pharmaceutical University
Discovery of selective fragment-sized immunoproteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Hungarian Academy of Sciences
SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
Taussig Cancer Institute
Design, synthesis and molecular docking studies of thymol based 1,2,3-triazole hybrids as thymidylate synthase inhibitors and apoptosis inducers against breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Albaha University
Progress in developing MNK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Ocean University of China and Laboratory For Marine Drugs and Bioproducts
A biphenyl inhibitor of eIF4E targeting an internal binding site enables the design of cell-permeable PROTAC-degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Dana-Farber Cancer Institute
Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
University Hospital Hradec Kralove
Novel 1,2,4-triazine-quinoline hybrids: The privileged scaffolds as potent multi-target inhibitors of LPS-induced inflammatory response via dual COX-2 and 15-LOX inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Zagazig University
Identification of an allosteric and Smad3-selective inhibitor of p38?MAPK using a substrate-based approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Carna Biosciences
Xanthine-Guanine-Hypoxanthine Phosphoribosyltransferase-A Putative Target for Drug Discovery against Gastrointestinal Tract Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5710-5729 (2021)
The University of Queensland
Expedited Approach toward the Rational Design of Noncovalent SARS-CoV-2 Main Protease Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 2848-2865 (2022)
The University of Arizona
From High-Throughput Screening to Target Validation: Benzo[![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5931-5955 (2021)
Aptuit, An Evotec
Synthesis, Molecular Pharmacology, and Structure-Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6381-6396 (2021)
West Virginia University
Discovery of Novel Pyrimidine-Based Capsid Assembly Modulators as Potent Anti-HBV Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5500-5518 (2021)
Gwangju Institute of Science and Technology (Gist)
Nucleotide analogues containing a pyrrolidine, piperidine or piperazine ring: Synthesis and evaluation of inhibition of plasmodial and human 6-oxopurine phosphoribosyltransferases and in vitro antimalarial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
The Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Hefei University of Technology
Investigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
The Institute of Cancer Research
Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Daiichi Sankyo
Positional Isomeric Effects on the Optical Properties, Multivalent Glycosidase Inhibition Effect, and Hypoglycemic Effect of Perylene Bisimide-deoxynojirimycin Conjugates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5863-5873 (2021)
Hebei University
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5577-5592 (2021)
University of Minnesota
New tetrahydroisoquinoline-based D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
City University of New York
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6085-6136 (2021)
Medicines For Malaria Venture
Design, Synthesis, and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 7331-7340 (2021)
TBA
Discovery of Dihydro-1,4-Benzoxazine Carboxamides as Potent and Highly Selective Inhibitors of Sirtuin-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5838-5849 (2021)
Max Planck Institute of Molecular Physiology
AAA ATPases as therapeutic targets: Structure, functions, and small-molecule inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
California Institute of Technology
Amphiphilic peptide-based MMP3 inhibitors for intra-articular treatment of knee OA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Fidia Farmaceutici
Development of Dimethylisoxazole-Attached Imidazo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5787-5801 (2021)
University of Massachusetts Boston
Taurultams incorporating arylsulfonamide: First in vitro inhibition studies of ?-, ?- and ?-class Carbonic Anhydrases from Vibrio cholerae and Burkholderia pseudomallei.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Ege University
Dipeptide inhibitors of the prostate specific membrane antigen (PSMA): A comparison of urea and thiourea derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
King'S College London
Discovery of a new series of PI3K-? inhibitors from Virtual Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
Merck
Magnolol, a natural aldehyde dehydrogenase-2 agonist, inhibits the proliferation and collagen synthesis of cardiac fibroblasts.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 43: (2021)
Southern Medical University
Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
School of Traditional Chinese Pharmacy
Azetidinimines as a novel series of non-covalent broad-spectrum inhibitors of ?-lactamases with submicromolar activities against carbapenemases KPC-2 (class A), NDM-1 (class B) and OXA-48 (class D).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Universit£
Identification and optimization of 3-bromo-N'-(4-hydroxybenzylidene)-4-methylbenzohydrazide derivatives as mTOR inhibitors that induce autophagic cell death and apoptosis in triple-negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Sichuan University-Oxford University Huaxi Gastrointestinal Cancer Centre
Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
University of Wisconsin-Madison
Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
University of New South Wales (Unsw)
Dipyridyl-substituted thiosemicarbazone as a potent broad-spectrum inhibitor of metallo-?-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Northwest University
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 39: (2021)
China Pharmaceutical University
Discovery of New Potent Positive Allosteric Modulators of Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6209-6220 (2021)
University of Porto
First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 9875-9890 (2021)
Takeda California
Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship, ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6008-6020 (2021)
Northeastern University
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 653-661 (2021)
Merck
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 647-652 (2021)
Jinan University
A Set of Highly Sensitive Sirtuin Fluorescence Probes for Screening Small-Molecular Sirtuin Defatty-Acylase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 617-624 (2021)
Nagoya City University
Discovery of the First Orally Available, Selective K![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 593-602 (2021)
Praxis Precision Medicines
Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 572-578 (2021)
The University of Tennessee Health Science Center
Novel Pyrimidine-5-carboxamide Compounds as NNMT Inhibitors for Treating Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 538-539 (2021)
Smith, Gambrell & Russell
Heterocyclic Compounds as Monoacylglycerol Lipase (MAGL) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 536-537 (2021)
Smith, Gambrell & Russell
Thienopyridinyl and Thiazolopyridinyl Compounds as IRAK4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 532-533 (2021)
Smith, Gambrell & Russell
Novel N-Heteroaryl Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 530-531 (2021)
Smith, Gambrell & Russell
Novel Pyridazines as Autotaxin Inhibitors for Treating Inflammatory Airway or Fibrotic Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 528-529 (2021)
Smith, Gambrell & Russell
Novel Azaquinolones as PARP1 Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 524-525 (2021)
Smith, Gambrell & Russell
Design, synthesis and biological evaluation of novel pleuromutilin derivatives as potent anti-MRSA agents targeting the 50S ribosome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
South China Agricultural University
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Sichuan University
Development of Potent NEDD8-Activating Enzyme Inhibitors Bearing a Pyrimidotriazole Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6161-6178 (2021)
Shanghai Institute of Materia Medica (Simm)
Covalent Occlusion of the ROR?t Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 631-639 (2021)
Technische Universiteit Eindhoven
Synthesis, Inhibitory Activity, and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 610-616 (2021)
Czech Academy of Sciences
Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 540-547 (2021)
Merck
Defining Target Engagement Required for Efficacy ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5470-5484 (2021)
Lilly Research Laboratories
Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6241-6261 (2021)
Peking Union Medical College and Chinese Academy of Medical Sciences
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4567-4587 (2021)
Heidelberg University
Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5067-5081 (2021)
Fudan University
An affinity prediction approach for the ligand of E3 ligase Cbl-b and an insight into substrate binding pattern.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
China Pharmaceutical University
An insight into the medicinal attributes of berberine derivatives: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Isf College of Pharmacy
Identification of 2,2-Dimethylbutanoic Acid (HST5040), a Clinical Development Candidate for the Treatment of Propionic Acidemia and Methylmalonic Acidemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5037-5048 (2021)
Hemoshear Therapeutics
Structural Determinants for the Mode of Action of Imidazopyridine DS2 at ?-Containing ?-Aminobutyric Acid Type A Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4730-4743 (2021)
University of Copenhagen
Discovery of a potent, selective, and covalent ZAP-70 kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
University of Chinese Academy of Science
Further lead optimization on Bax activators: Design, synthesis and pharmacological evaluation of 2-fluoro-fluorene derivatives for the treatment of breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
University of Texas Medical Branch (Utmb)
Synthesis and biological evaluation of phenothiazine derivative-containing hydroxamic acids as potent class II histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Taipei Medical University
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 219: (2021)
Guangzhou Medical University
Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4333-4358 (2021)
University of Maryland
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5404-5428 (2021)
University of Turin
Bispecific Estrogen Receptor ? Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5049-5066 (2021)
X-Chem
Synthesis of the Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor NB-360.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4677-4696 (2021)
TBA
GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4312-4332 (2021)
University of Siena
Radioligand and computational insight in structure - Activity relationship of saccharin derivatives being ipsapirone and revospirone analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
Cracow University of Technology
Design and identification of a new farnesoid X receptor (FXR) partial agonist by computational structure-activity relationship analysis: Ligand-induced H8 helix fluctuation in the ligand-binding domain of FXR may lead to partial agonism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Computer-Aided Molecular Modeling Research Center
Design, synthesis and in-vitro evaluation of fluorinated triazoles as multi-target directed ligands for Alzheimer disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenylpyrimidine derivatives with 4-amino or 4-hydroxy as a pharmacophore element binding with xanthine oxidase active site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Shenyang Pharmaceutical University
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and ?-aminobutyric acid transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Jagiellonian University Medical College
Discovery of effective phosphodiesterase 2 inhibitors with antioxidant activities for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Sun Yat-Sen University
Prodrugs of a 1'-CN-4-Aza-7,9-dideazaadenosine ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5001-5017 (2021)
Gilead Sciences
Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4762-4786 (2021)
Southern Research
Discovery of 5-(3-Chlorophenylamino)benzo[![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5082-5098 (2021)
Southeast University
Discovery of novel potent migrastatic Thiazolo[5,4-b]pyridines targeting Lysyl-tRNA synthetase (KRS) for treatment of Cancer metastasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Cha University
Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1,3-dione scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Institute of Physiologically Active Compounds Russian Academy of Sciences
Identification of novel 1,3-diaryl-1,2,4-triazole-capped histone deacetylase 6 inhibitors with potential anti-gastric cancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Zhengzhou University
Discovery of novel pyrimidine molecules containing boronic acid as VCP/p97 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 38: (2021)
Nanjing Normal University
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
National Institute of Diabetes and Digestive and Kidney Diseases
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4810-4840 (2021)
University of Illinois At Chicago
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4430-4449 (2021)
Agios Pharmaceuticals
Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4972-4990 (2021)
Alma Mater Studiorum - University of Bologna
Tricyclic Triazoles as ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5157-5170 (2021)
Esteve Pharmaceuticals
Discovery of new pyrimidopyrrolizine/indolizine-based derivatives as P-glycoprotein inhibitors: Design, synthesis, cytotoxicity, and MDR reversal activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Umm Al-Qura University
An insight in anti-malarial potential of indole scaffold: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Amity University
Discovery of a potent, highly selective, and orally bioavailable inhibitor of CDK8 through a structure-based optimisation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
University of South Australia
Small-Molecule Inhibitors Targeting the Canonical WNT Signaling Pathway for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4257-4288 (2021)
Ocean University of China
Discovery and Optimization of 2![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4913-4946 (2021)
National Center For Advancing Translational Sciences
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4891-4902 (2021)
Lundbeck Research Usa
Synthesis and Biological Evaluation of PSMA Ligands with Aromatic Residues and Fluorescent Conjugates Based on Them.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4532-4552 (2021)
Lomonosov Moscow State University
Optimization of Truncated Glucagon Peptides to Achieve Selective, High Potency, Full Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4697-4708 (2021)
Indiana University
Structure-Based Design of Selective LONP1 Inhibitors for Probing ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4857-4869 (2021)
Genomics Institute of The Novartis Research Foundation
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4623-4661 (2021)
University of Copenhagen
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
China Pharmaceutical University
Small molecule and macrocyclic pyrazole derived inhibitors of myeloperoxidase (MPO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 42: (2021)
Bristol-Myers Squibb
Discovery of novel Staphylococcus aureus penicillin binding protein 2a inhibitors by multistep virtual screening and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
The First Affiliated Hospital of Anhui Medical University
Systematic evaluation of structure-property relationships and pharmacokinetics in 6-(hetero)aryl-substituted matched pair analogs of amiloride and 5-(N,N-hexamethylene)amiloride.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 37: (2021)
University of Wollongong
Design, synthesis and biological evaluation of brain penetrant benzazepine-based histone deacetylase 6 inhibitors for alleviating stroke-induced brain infarction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Shanghai Institute of Pharmaceutical Industry
Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Sanford Burnham Prebys Medical Discovery Institute
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4709-4729 (2021)
Merck
Design, Synthesis, and Structural Characterization of Lysine Covalent BH3 Peptides Targeting Mcl-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4903-4912 (2021)
University of California Riverside
Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3K? Immunomodulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5137-5156 (2021)
Merck
Discovery of a Potent and Selective FLT3 Inhibitor (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4870-4890 (2021)
Nanjing University of Chinese Medicine
Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) - A promising target for liver regeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Eberhard Karls Universit£T
Oxaprozin Analogues as Selective RXR Agonists with Superior Properties and Pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5123-5136 (2021)
Goethe-University Frankfurt
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4462-4477 (2021)
German University In Cairo
Structure-Enabled Discovery of Novel Macrocyclic Inhibitors Targeting Glutaminase 1 Allosteric Binding Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4588-4611 (2021)
China Pharmaceutical University
Structure-Activity Relationship of Heterocyclic P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5099-5122 (2021)
National Institute of Diabetes and Digestive and Kidney Diseases
Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
China Pharmaceutical University
Mechanistic selectivity investigation and 2D-QSAR study of some new antiproliferative pyrazoles and pyrazolopyridines as potential CDK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Cairo University
Selective Discovery of GPCR Ligands within DNA-Encoded Chemical Libraries Derived from Natural Products: A Case Study on Antagonists of Angiotensin II Type I Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4196-4205 (2021)
Northwest University
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3976-3996 (2021)
Peking University
Structure-Based Exploration of Selectivity for ATM Inhibitors in Huntington's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5018-5036 (2021)
Charles River
Carboxylesterase Notum Is a Druggable Target to Modulate Wnt Signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4289-4311 (2021)
University College London
Synthetic Approaches to the New Drugs Approved during 2019.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3604-3657 (2021)
Takeda Pharmaceuticals
Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Chinese Academy of Sciences
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3940-3955 (2021)
Genentech
Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Zhengzhou University
Structure-activity relationship studies of 3-substituted pyrazoles as novel allosteric inhibitors of MALT1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Toray Industries
Discovery of N-amido-phenylsulfonamide derivatives as novel microsomal prostaglandin E![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Kyung Hee University
Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
The First Affiliated Hospital of Wenzhou Medical University
Insertion of metal carbenes into the anilinic N-H bond of unprotected aminobenzenesulfonamides delivers low nanomolar inhibitors of human carbonic anhydrase IX and XII isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Saint Petersburg State University
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 37: (2021)
Wayne State University School of Medicine
If small molecules immunotherapy comes, can the prime be far behind?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Zhejiang University
Identification of N-phenyl-2-(phenylsulfonyl)acetamides/propanamides as new SLC-0111 analogues: Synthesis and evaluation of the carbonic anhydrase inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 218: (2021)
Kafrelsheikh University
FFAR1/GPR40: One target, different binding sites, many agonists, no drugs, but a continuous and unprofitable tug-of-war between ligand lipophilicity, activity, and toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
University of Siena
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Misr International University
Optimization of ether and aniline based inhibitors of lactate dehydrogenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Vanderbilt University
Design, synthesis, and structure-activity relationship of programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing a benzo[d]isothiazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Chinese Academy of Medical Sciences & Peking Union Medical College
Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4130-4149 (2021)
Sungkyunkwan University
Melatonin- and Ferulic Acid-Based HDAC6 Selective Inhibitors Exhibit Pronounced Immunomodulatory Effects ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3794-3812 (2021)
Julius Maximilian University of W£Rzburg
Demonstrating Ligandability of the LC3A and LC3B Adapter Interface.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3720-3746 (2021)
Goethe-University Frankfurt
Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Nanchang University
Exploring naltrexamine derivatives featuring azaindole moiety via nitrogen-walk approach to investigate their in vitro pharmacological profiles at the mu opioid receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Virginia Commonwealth University
The dual inhibition against the activity and expression of tyrosine phosphatase PRL-3 from a rhodanine derivative.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Shanxi University
Synthesis, biological evaluation, and correlation of cytotoxicity versus redox potential of 1,4-naphthoquinone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
National Research Institute of Chinese Medicine
Rationally designed TNF-? inhibitors: Identification of promising cytotoxic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Guru Nanak Dev University
Recent progress in agents targeting polo-like kinases: Promising therapeutic strategies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Shandong First Medical University & Shandong Academy of Medical Sciences
Balancing potency and basicity by incorporating fluoropyridine moieties: Discovery of a 1-amino-3,4-dihydro-2,6-naphthyridine BACE1 inhibitor that affords robust and sustained central A? reduction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Shionogi
Designed ?-Hairpins Inhibit LDH5 Oligomerization and Enzymatic Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3767-3779 (2021)
Queensland University of Technology
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3827-3842 (2021)
Leiden University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3508-3545 (2021)
Niddk
Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3897-3910 (2021)
Institut De Recherches Servier
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3870-3884 (2021)
The Scripps Research Institute
Allosteric Modulation: Dynamics is Double-"E"dged.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3694-3696 (2021)
Chinese Academy of Sciences
Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4150-4162 (2021)
The University of Melbourne
Discovery and antitumor activity of Benzo[d]imidazol-containing 2,4-diarylaminopyrimidine analogues as ALK inhibitors with mutation-combating effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 37: (2021)
Cancer Hospital of China Medical University
Development of phenyltriazole thiol-based derivatives as highly potent inhibitors of DCN1-UBC12 interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Zhengzhou University
A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Shanghai University of Traditional Chinese Medicine
Scaffold repurposing of fendiline: Identification of potent KRAS plasma membrane localization inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
University of Texas Medical Branch
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3911-3939 (2021)
Merck
Structure-Based Identification of Potent Lysine-Specific Demethylase 1 Inhibitor Peptides and Temporary Cyclization to Enhance Proteolytic Stability and Cell Growth-Inhibitory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3707-3719 (2021)
Nagoya City University
Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Chiesi Farmaceutici
An insight on medicinal aspects of novel HIV-1 capsid protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Shandong University
Using porphyrins as albumin-binding molecules to enhance antitumor efficacies and reduce systemic toxicities of antimicrobial peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Fuzhou University
Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Shanghaitech University
Structure-Activity Relationship Study of Dexrazoxane Analogues Reveals ICRF-193 as the Most Potent Bisdioxopiperazine against Anthracycline Toxicity to Cardiomyocytes Due to Its Strong Topoisomerase II? Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3997-4019 (2021)
Charles University
Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3843-3869 (2021)
Genentech
Structure-Based Design of a Selective Class I Histone Deacetylase (HDAC) Near-Infrared (NIR) Probe for Epigenetic Regulation Detection in Triple-Negative Breast Cancer (TNBC).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4020-4033 (2021)
China Pharmaceutical University
Pragmatic recruitment of memantine as the capping group for the design of HDAC inhibitors: A preliminary attempt to unravel the enigma of glioblastoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Taipei Medical University
Novel dual-mode antitumor chlorin-based derivatives as potent photosensitizers and histone deacetylase inhibitors for photodynamic therapy and chemotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Second Military Medical University
Synthesis, biological evaluation, and docking studies of novel pyrrolo[2,3-b]pyridine derivatives as both ectonucleotide pyrophosphatase/phosphodiesterase inhibitors and antiproliferative agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Comsats University Islamabad
Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Ataturk University
Discovery of antiproliferative and anti-FAK inhibitory activity of 1,2,4-triazole derivatives containing acetamido carboxylic acid skeleton.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Deraya University
Discovery of 3-aryl substituted benzoxaboroles as broad-spectrum inhibitors of serine- and metallo-?-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Sichuan University
Development of new disulfiram analogues as ALDH1a1-selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Umm Al-Qura University
Discovery of 5-(N-hydroxycarbamimidoyl) benzofuran derivatives as novel indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Seoul National University
Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Pla Strategic Support Force Medical Center
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
China Pharmaceutical University
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 494-501 (2021)
Bristol Myers Squibb Research and Development
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 485-493 (2021)
Purdue University
Identification of Potent Reverse Indazole Inhibitors for HPK1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 459-466 (2021)
Merck
Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 451-458 (2021)
Janssen Research & Development
Discovery of Orally Active and Nonsteroidal Farnesoid X Receptor (FXR) Antagonist with Propensity for Accumulation and Responsiveness in Ileum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 420-425 (2021)
Hiroshima International University
Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 397-403 (2021)
Chinese Academy of Sciences
Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 380-388 (2021)
Charles River Discovery
Biological Evaluation of 5'-(![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 373-379 (2021)
National Institute of Diabetes and Digestive and Kidney Diseases
Design and Structure-Activity Relationship of a Potent Furin Inhibitor Derived from Influenza Hemagglutinin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 365-372 (2021)
University of Gda?Sk
Novel Potent Selective Orally Active S1P5 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 351-355 (2021)
Biogen
Synthesis of HDAC Inhibitor Libraries via Microscale Workflow.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 337-342 (2021)
Merck
Myeloid Cell Leukemia-1 Inhibitors as Emerging Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 334-336 (2021)
Therachem Research Medilab
Targeting Stimulator of Interferon Genes (STING) for the Potential Treatment of Cancer and Infectious Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 328-330 (2021)
Usona Institute
Tumor-Targeted Bivalent Protein Degradation for Application in Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 326-327 (2021)
Usona Institute
Novel Bicyclic Heterocycles as FGFR Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 320-321 (2021)
Smith, Gambrell & Russell
Novel Benzimidazole Derivatives as Transient Receptor Potential Channel 6 (TRPC6) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 314-315 (2021)
Smith, Gambrell & Russell
Novel Oxazine Monoacylglycerol Lipase (MAGL) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 312-313 (2021)
Smith, Gambrell & Russell
1-Pyrazolyl-5,6-Disubstituted Indazole Derivatives as LRRK2 Inhibitors for Treating Parkinson's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 310-311 (2021)
Smith, Gambrell & Russell
Withanolides from dietary tomatillo suppress HT1080 cancer cell growth by targeting mutant IDH1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 36: (2021)
Shenyang Pharmaceutical University
2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4239-4256 (2021)
Shandong University
Structure-Activity Relationship Studies on Oxazolo[3,4-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 4089-4108 (2021)
University of Ferrara
Discovery of a Pyrimidinedione Derivative as a Potent and Orally Bioavailable Axl Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3956-3975 (2021)
Chinese Academy of Sciences
Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 443-450 (2021)
Bristol Myers Squibb
The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 426-432 (2021)
Philipps University
Ring closure strategy leads to potent RIPK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Soochow University
Recent advances in development of hetero-bivalent kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Cha University
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3677-3693 (2021)
Athenex
Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3658-3676 (2021)
Reviral
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Zhejiang University
One-step modification to identify dual-inhibitors targeting both pancreatic triglyceride lipase and Niemann-Pick C1-like 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
The Affiliated Hospital of Qingdao University
Design, synthesis, and biological evaluation of nitroisoxazole-containing spiro[pyrrolidin-oxindole] derivatives as novel glutathione peroxidase 4/mouse double minute 2 dual inhibitors that inhibit breast adenocarcinoma cell proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 217: (2021)
Chengdu University of Traditional Chinese Medicine
Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3813-3826 (2021)
University of East Anglia
C@PA: Computer-Aided Pattern Analysis to Predict Multitarget ABC Transporter Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3350-3366 (2021)
University of Bonn
Alkyne-Bridged ?-Conotoxin Vc1.1 Potently Reverses Mechanical Allodynia in Neuropathic Pain Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3222-3233 (2021)
Monash University
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6670-6695 (2021)
Monash University
Developing novel classes of protein kinase CK1? inhibitors by fusing [1,2,4]triazole with different bicyclic heteroaromatic systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Universit£
Structural insights of oxindole based kinase inhibitors as anticancer agents: Recent advances.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery of Potent Carbonic Anhydrase Inhibitors as Effective Anticonvulsant Agents: Drug Design, Synthesis, and In Vitro and In Vivo Investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3100-3114 (2021)
Sookmyung Women'S University
Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3439-3448 (2021)
Lilly Research Laboratories
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2937-2952 (2021)
Galapagos
FLT3 Inhibitors in Acute Myeloid Leukemia: Challenges and Recent Developments in Overcoming Resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2878-2900 (2021)
China Pharmaceutical University
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective ?-Secretase (BACE1) Inhibitors over BACE2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3075-3085 (2021)
Shionogi
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 6569-6580 (2021)
Boehringer Ingelheim Rcv
Discovery of Selective Pituitary Adenylate Cyclase 1 Receptor (PAC1R) Antagonist Peptides Potent in a Maxadilan/PACAP38-Induced Increase in Blood Flow Pharmacodynamic Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3427-3438 (2021)
Amgen
Design, Synthesis, and Evaluation of Small Molecule G?q/11 Protein Inhibitors for the Treatment of Uveal Melanoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3131-3152 (2021)
Sun Yat-Sen University
Histone deacetylase 2: A potential therapeutic target for cancer and neurodegenerative disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Nirma University
Imidazo[1,2-c]pyrimidin-5(6H)-one inhibitors of CDK2: Synthesis, kinase inhibition and co-crystal structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Institute For Organic Syntheses (Vuos)
IDO1 and TDO inhibitory evaluation of analogues of the marine pyrroloiminoquinone alkaloids: Wakayin and Tsitsikammamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Universit£
Addition of hydrophobic side chains improve the apoptosis inducibility of the human glyoxalase I inhibitor, TLSC702.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Tokyo University of Science
Folic Acid-Peptide Conjugates Combine Selective Cancer Cell Internalization with Thymidylate Synthase Dimer Interface Targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3204-3221 (2021)
University of Modena and Reggio Emilia
Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Universities of Shandong
The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Beijing University of Technology
Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Huazhong University of Science and Technology
A novel class of selective non-nucleoside inhibitors of human DNA methyltransferase 3A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
University of California
Cyclic Analogues of the Chemerin C-Terminus Mimic a Loop Conformation Essential for Activating the Chemokine-like Receptor 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3048-3058 (2021)
Leipzig University
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3234-3248 (2021)
Peking Union Medical College and Chinese Academy of Medical Sciences
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3006-3025 (2021)
Rti International
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Sumitomo Dainippon Pharma.
Discovery of potent colony-stimulating factor 1 receptor inhibitors by replacement of hinge-binder moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Chung-Ang University
Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Fudan University
One pot synthesis, in silico study and evaluation of some novel flavonoids as potent topoisomerase II inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Dr. Babasaheb Ambedkar Marathwada University
Discovery and characterization of a novel glucose-6-phosphate dehydrogenase (G6PD) inhibitor via high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Nanjing University of Chinese Medicine
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3086-3099 (2021)
Bristol Myers Squibb
Conformational Constraint between Aromatic Residue Side Chains in the "Message" Sequence of the Peptide Arodyn Using Ring Closing Metathesis Results in a Potent and Selective Kappa Opioid Receptor Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3153-3164 (2021)
The University of Kansas
Current status in the discovery of dual BET/HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
The First Affiliated Hospital of Zhengzhou University
Design, synthesis, biological evaluation and structure-activity relationship study of quinazolin-4(3H)-one derivatives as novel USP7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Zhengzhou University
Novel monocyclic amide-linked phenol derivatives without mitochondrial toxicity have potent uric acid-lowering activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Fuji Yakuhin
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 39: (2021)
Astrazeneca
Heparan Sulfate Mimetics Differentially Affect Homologous Chemokines and Attenuate Cancer Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3367-3380 (2021)
Indian Institute of Science Education and Research
Dihydro-?-agarofuran-Type Sesquiterpenoids from the Seeds of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 588-600 (2021)
Chinese Academy of Sciences
Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3165-3184 (2021)
Astrazeneca
DYRK1A Inhibitors as Potential Therapeutics for ?-Cell Regeneration for Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2901-2922 (2021)
Icahn School of Medicine At Mount Sinai
Discovery of a Potent and Orally Bioavailable Melatonin Receptor Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3059-3074 (2021)
Takeda Pharmaceutical
Discovery of deoxyceramide analogs as highly selective ACER3 inhibitors in live cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Institute For Advanced Chemistry of Catalonia (Iqac-Csic)
Synthesis and evaluation of the epithelial-to- mesenchymal inhibitory activity of indazole-derived imidazoles as dual ALK5/p38? MAP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Yanbian University
Structure-activity relationship and mechanistic studies for a series of cinnamyl hydroxamate histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
University of S£O Paulo
Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 36: (2021)
Southeast University
A grafted peptidomimetic for EGFR heterodimerization inhibition: Implications in NSCLC models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
University of Louisiana At Monroe
Development of novel benzofuran-based SLC-0111 analogs as selective cancer-associated carbonic anhydrase isoform IX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Kafrelsheikh University
Design, synthesis and evaluation of novel dimethylamino chalcone-O-alkylamines derivatives as potential multifunctional agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Nanyang Normal University
Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
China Pharmaceutical University
Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3299-3319 (2021)
University of Sheffield
Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3320-3349 (2021)
Technical University Darmstadt
3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3035-3047 (2021)
Heinrich Heine University D£Sseldorf
A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Indian Institute of Technology (Banaras Hindu University)
Discovery of 3,6-disubstutited-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 41: (2021)
Sichuan University
Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Cyclerion Therapeutics
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3249-3281 (2021)
Glaxosmithkline
Freshwater Fungi as a Source of Chemical Diversity: A Review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 898-916 (2021)
Jordan University of Science and Technology
Design and Synthesis of Novel Epigenetic Inhibitors Targeting Histone Deacetylases, DNA Methyltransferase 1, and Lysine Methyltransferase G9a with ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3392-3426 (2021)
University of Navarra
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2851-2877 (2021)
Sichuan University
Discovery of pyrazolo-thieno[3,2-d]pyrimidinylamino-phenyl acetamides as type-II pan-tropomyosin receptor kinase (TRK) inhibitors: Design, synthesis, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
University of Arkansas For Medical Sciences
Small-Molecule Drug Discovery in Triple Negative Breast Cancer: Current Situation and Future Directions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2382-2418 (2021)
Sichuan University
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
Duquesne University
Design, synthesis, and evaluation of a novel prodrug, a S-trityl-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
University of Shizuoka
Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
Guizhou Medical University
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 216: (2021)
Southeast University
Synthesis and biological evaluation of novel 4,7-disubstituted coumarins as selective tumor-associated carbonic anhydrase IX and XII inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 39: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
A new class of ?-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Tsinghua University
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Masaryk University
Medulloblastoma drugs in development: Current leads, trials and drawbacks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
University of Connecticut
Oxa-adamantyl cannabinoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
University of Hawaii At Manoa
Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
Arena Pharmaceuticals
Structure based design and synthesis of novel Toll-like Receptor 2 (TLR 2) lipid antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 40: (2021)
Neuropore Therapies
Exploring the Chemistry of Alkaloids from Malaysian ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1034-1043 (2021)
Universiti Sains Malaysia
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2501-2520 (2021)
Millennium Pharmaceuticals, A Wholly Owned Subsidiary of Takeda Pharmaceuticals
Structure-Activity Relationship Studies of Coumarin-like Diacid Derivatives as Human G Protein-Coupled Receptor-35 (hGPR35) Agonists and a Consequent New Design Principle.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2634-2647 (2021)
Chinese Academy of Sciences
Fragment-like Chloroquinolineamines Activate the Orphan Nuclear Receptor Nurr1 and Elucidate Activation Mechanisms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2659-2668 (2021)
Goethe University
Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2669-2677 (2021)
Taiho Pharmaceutical
Pharmacokinetics of Eleven Kratom Alkaloids Following an Oral Dose of Either Traditional or Commercial Kratom Products in Rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1104-1112 (2021)
University of Florida
Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPAR? Modulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2815-2828 (2021)
Goethe University
Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2466-2488 (2021)
Zhengzhou University
Design, synthesis, and biological evaluation of indazole derivatives as selective and potent FGFR4 inhibitors for the treatment of FGF19-driven hepatocellular cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Wenzhou Medical University
Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2419-2435 (2021)
West China Hospital of Sichuan University
Design, synthesis, and biological evaluation of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives as potent CDK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Shanghaitech University
Molecular modeling-guided optimization of acetylcholinesterase reactivators: A proof for reactivation of covalently inhibited targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Fourth Military Medical University
Discovery of a novel potent cytochrome P450 CYP4Z1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Freie Universit£T Berlin
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
M. S. University of Baroda
Synthetic and medicinal perspective of quinolines as antiviral agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Indo-Soviet Friendship College of Pharmacy (ISFCP)
3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 37: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Discovery of novel Hsp90 C-terminal domain inhibitors that disrupt co-chaperone binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
University of Auckland
Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
Roche Innovation Center Shanghai
Novel bicyclic pyrazoles as potent ALK2 (R206H) inhibitors for the treatment of fibrodysplasia ossificans progressiva.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
Riken Center For Sustainable Resource Science
Design, synthesis and bioactivity evaluation of novel pyrazole linked phenylthiazole derivatives in context of antibacterial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 39: (2021)
Griffith University
Pyridones in drug discovery: Recent advances.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 38: (2021)
Astrazeneca
Design and synthesis of a monocyclic derivative as a selective ACC1 inhibitor by chemical modification of biphenyl ACC1/2 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
Takeda Pharmaceutical
Synthesis and evaluation of cyclopentane-based muraymycin analogs targeting MraY.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Duke University
Design and Synthesis of EZH2-Based PROTACs to Degrade the PRC2 Complex for Targeting the Noncatalytic Activity of EZH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2829-2848 (2021)
Sichuan University
Fragment-Based Discovery of Novel Allosteric MEK1 Binders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 302-308 (2021)
Astrazeneca
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 288-294 (2021)
Bristol Myers Squibb Research and Development
A New FXR Ligand Chemotype with Agonist/Antagonist Switch.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 267-274 (2021)
Goethe-University Frankfurt
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 249-255 (2021)
Yale University
Sulfamoylbenzamide-based Capsid Assembly Modulators for Selective Inhibition of Hepatitis B Viral Replication.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 242-248 (2021)
Korea Research Institute of Chemical Technology
Development of a Hematopoietic Prostaglandin D Synthase-Degradation Inducer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 236-241 (2021)
National Institute of Health Sciences
Virtual Screening Approach to Identifying a Novel and Tractable Series of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 217-227 (2021)
Antabio
Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 211-216 (2021)
Kogakuin University
Investigation on the Anticancer Activity of Symmetric and Unsymmetric Cyclic Sulfamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 202-210 (2021)
National Institutes of Health (Nih) National Center of Excellence For Computational Drug Abuse Research
Discovery of Hydroxyamidine Derivatives as Highly Potent, Selective Indoleamine-2,3-dioxygenase 1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 195-201 (2021)
Shanghai Hengrui Pharmaceutical
Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 182-184 (2021)
Therachem Research Medilab
Methionine Adenosyltransferase Inhibitors for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 180-181 (2021)
Usona Institute
Sigma-1 and Sigma-2 Receptor Modulators as Potential Therapeutics for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 178-179 (2021)
Usona Institute
Novel Galectin-3 Inhibitors for Treating Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 174-175 (2021)
Smith, Gambrell & Russell
Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 170-171 (2021)
Smith, Gambrell & Russell
SARS-CoV-2 Mpro inhibitors with antiviral activity in a transgenic mouse model![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Science (2021)
Sichuan University
Anticancer potential of spirocompounds in medicinal chemistry: A pentennial expedition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Synthesis and biological evaluation of benzhydryl-based antiplasmodial agents possessing Plasmodium falciparum chloroquine resistance transporter (PfCRT) inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
University of Siena
Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Korea Institute of Science & Technology (Kist)
Design of pyrido[2,3-d]pyrimidin-7-one inhibitors of receptor interacting protein kinase-2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
University of Houston
Synthesis of Yakuchinone B-Inspired Inhibitors against Islet Amyloid Polypeptide Aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1096-1103 (2021)
Taipei Medical University
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2608-2621 (2021)
Leiden Academic Centre For Drug Research
C-2-Linked Dimeric Strychnine Analogues as Bivalent Ligands Targeting Glycine Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 382-394 (2021)
The German University In Cairo
Synthesis, Structure-Activity Relationships, and Antiviral Activity of Allosteric Inhibitors of Flavivirus NS2B-NS3 Protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2777-2800 (2021)
Baylor College of Medicine
Discovery of 3-(4-(2-((1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1966-1988 (2021)
West China Hospital of Sichuan University
Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1889-1903 (2021)
TBA
Inhibitors of Eukaryotic Translational Machinery as Therapeutic Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2436-2465 (2021)
Merck
CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1835-1843 (2021)
Bristol Myers Squibb
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 3697-3706 (2021)
Icahn School of Medicine At Mount Sinai
Tricyclic-Carbocyclic ROR?t Inverse Agonists-Discovery of BMS-986313.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2714-2724 (2021)
Bristol Myers Squibb
Bicyclic Diazepinones as Dual Ligands of the ?2?-1 Subunit of Voltage-Gated Calcium Channels and the Norepinephrine Transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2167-2185 (2021)
Esteve Pharmaceuticals
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based ?-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1873-1888 (2021)
Janssen Research & Development
Application of marine natural products in drug research.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 35: (2021)
Weihai Marine Organism & Medical Technology Research Institute
Discovery and structural optimization of 3-O-?-chacotriosyl oleanane-type triterpenoids as potent entry inhibitors of SARS-CoV-2 virus infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
South China Agricultural University
Antitubercular properties of thiazolidin-4-ones - A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Medical University of Lublin
CAP rigidification of MS-275 and chidamide leads to enhanced antiproliferative effects mediated through HDAC1, 2 and tubulin polymerization inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Taipei Medical University
Multifunctional agents based on benzoxazolone as promising therapeutic drugs for diabetic nephropathy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Beijing Institute of Technology
Discovery of Novel Pyrrolo[2,3-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 1243-1264 (2022)
Chinese Academy of Sciences
Discovery of new phenyl sulfonyl-pyrimidine carboxylate derivatives as the potential multi-target drugs with effective anti-Alzheimer's action: Design, synthesis, crystal structure and in-vitro biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Jamia Millia Islamia
Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 215: (2021)
Palack£
New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Florida A&M University
Targeting SHP2 as a therapeutic strategy for inflammatory diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Shenyang Pharmaceutical University
Annual review of LSD1/KDM1A inhibitors in 2020.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Beijing University of Chinese Medicine
Medicinal chemistry strategies for the development of phosphodiesterase 10A (PDE10A) inhibitors - An update of recent progress.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Nirma University
Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Shenyang Pharmaceutical University
Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Florence
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Nottingham
Discovery of remogliflozin etabonate: A potent and highly selective SGLT2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
Toho University
Unique Molecular Interaction with the Histone Deacetylase 6 Catalytic Tunnel: Crystallographic and Biological Characterization of a Model Chemotype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2691-2704 (2021)
University of Toronto Mississauga
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2291-2309 (2021)
University of Cape Town
Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
University of Regensburg
Discovery of a novel 53BP1 inhibitor through AlphaScreen-based high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
Yantai University
Synthesis and preliminary anticancer evaluation of new triazole bisphosphonate-based isoprenoid biosynthesis inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Universit£
Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of South Australia
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 37: (2021)
Sungkyunkwan University
Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1844-1855 (2021)
Chinese Academy of Sciences
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2228-2241 (2021)
Moffitt Cancer Center
HDAC7 Inhibition by Phenacetyl and Phenylbenzoyl Hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2186-2204 (2021)
The University of Queensland
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Shandong University
Structural optimization towards promising ?-methyl-4-acrylamido quinoline derivatives as PI3K/mTOR dual inhibitors for anti-cancer therapy: The in vitro and in vivo biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Jiaxing University
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2272-2290 (2021)
Universidad Aut£Noma De Madrid
Axial Chiral Binaphthoquinone and Perylenequinones from the Stromata of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 436-443 (2021)
Chinese Academy of Sciences
Azole-Based Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2205-2227 (2021)
Sib Swiss Institute of Bioinformatics
Synthesis and evaluation of azalamellarin N and its A-ring-modified analogues as non-covalent inhibitors of the EGFR T790M/L858R mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
Nagasaki University
Recent advances of dual FGFR inhibitors as a novel therapy for cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Southwest Jiaotong University
Discovery and optimization of a novel CNS penetrant series of mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 37: (2021)
Vanderbilt University
Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2139-2150 (2021)
Sanofi R&D
Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1856-1872 (2021)
Eicosis Human Health
Tetrahydroindazole inhibitors of CDK2/cyclin complexes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Minnesota
Synthesis, biological evaluation and structure-activity relationship of novel dichloroacetophenones targeting pyruvate dehydrogenase kinases with potent anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Chongqing University
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 33: (2021)
University of Tennessee Health Science Center
Chemical validation of a druggable site on Hsp27/HSPB1 using in silico solvent mapping and biophysical methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
University of California At San Francisco
Discovery of benzo[f]pyrido[4,3-b][1,4]oxazepin-10-one derivatives as orally available bromodomain and extra-terminal domain (BET) inhibitors with efficacy in an in vivo psoriatic animal model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
Kyorin Pharmaceutical
Discovery of a novel series of indolinylpyrimidine-based GPR119 agonists: Elimination of ether-a-go-go-related gene liability using a hydrogen bond acceptor-focused approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 34: (2021)
Takeda Pharmaceutical
Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Regensburg
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Cologne
Amyloid-? and tau aggregation dual-inhibitors: A synthetic and structure-activity relationship focused review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
University of Aveiro
Synthesis and evaluation of novel cyclopentane urea FPR2 agonists and their potential application in the treatment of cardiovascular inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Queen Mary University of London
Pyrazolo[3,4-d]pyrimidine-based dual EGFR T790M/HER2 inhibitors: Design, synthesis, structure-activity relationship and biological activity as potential antitumor and anticonvulsant agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Beni-Suef University
Discovering High Potent Hsp90 Inhibitors as Antinasopharyngeal Carcinoma Agents through Fragment Assembling Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2010-2023 (2021)
Sun Yat-Sen University
Discovery of Novel ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2254-2271 (2021)
East China University of Science and Technology
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Zhengzhou University
Discovery of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor: Scaffold hopping approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 214: (2021)
Gedeon Richter
HIV latency reversal agents: A potential path for functional cure?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
S£O Paulo State University (Unesp)
Dioxotriazine derivatives as a new class of P2X![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 37: (2021)
Shionogi
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 893-921 (2022)
Csir-Indian Institute of Integrative Medicine
Design, Structural Optimization, and Characterization of the First Selective Macrocyclic Neurotensin Receptor Type 2 Non-opioid Analgesic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2110-2124 (2021)
Universit£
Chemical Highlights Supporting the Role of Lipid A in Efficient Biological Adaptation of Gram-Negative Bacteria to External Stresses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1816-1834 (2021)
Aix Marseille Universit£
Metalloaminopeptidases of the Protozoan Parasite ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1763-1785 (2021)
University of Leeds
New 2-Pyrazoline and Hydrazone Derivatives as Potent and Selective Monoamine Oxidase A Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1989-2009 (2021)
Hacettepe University
Design and Characterization of a Pyridone-Containing EZH2 Inhibitor Phosphate Prodrug.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1725-1732 (2021)
TBA
Discovery of 6-(7-Nitro-2,1,3-benzoxadiazol-4-ylthio)hexanol Derivatives as Glutathione Transferase Inhibitors with Favorable Selectivity and Tolerated Toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1701-1712 (2021)
Southeast University
?-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1392-1422 (2021)
Univ. Grenoble Alpes
New dual ATP-competitive inhibitors of bacterial DNA gyrase and topoisomerase IV active against ESKAPE pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
University of Ljubljana
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 5345-5364 (2021)
Universit£
Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1685-1700 (2021)
Veterans Affairs Medical Center
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1362-1391 (2021)
Zhengzhou University
Inhibition of Carbonic Anhydrase Using SLC-149: Support for a Noncatalytic Function of CAIX in Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1713-1724 (2021)
University of Florida
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1584-1592 (2021)
University of Toronto
Bisphosphonates, Old Friends of Bones and New Trends in Clinics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1260-1282 (2021)
University of Aveiro
Insights into non-peptide small-molecule inhibitors of the PD-1/PD-L1 interaction: Development and perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 33: (2021)
Shenyang Pharmaceutical University
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
University of South Australia
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Anhui Medical University
Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 36: (2021)
China Pharmaceutical University
Discovery of a Napabucasin PROTAC as an Effective Degrader of the E3 Ligase ZFP91.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1626-1648 (2021)
University of Michigan
A High-Affinity Peptide Ligand Targeting Syntenin Inhibits Glioblastoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1423-1434 (2021)
University of Copenhagen
Structure-Based Design of Potent Selective Nanomolar Type-II Inhibitors of Glycogen Synthase Kinase-3?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1497-1509 (2021)
University of Central Lancashire
Discovery of 3-phenyl- and 3-N-piperidinyl-isothiazolo[4,3-b]pyridines as highly potent inhibitors of cyclin G-associated kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Ku Leuven
Building a Chemical Toolbox for Human Pregnane X Receptor Research: Discovery of Agonists, Inverse Agonists, and Antagonists Among Analogs Based on the Unique Chemical Scaffold of SPA70.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1733-1761 (2021)
St. Jude Children'S Research Hospital
Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1481-1496 (2021)
Tokyo Medical and Dental University (Tmdu)
Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Tsinghua University
Design, synthesis and biological evaluation of novel 2-(4-(1H-indazol-6-yl)-1H-pyrazol-1-yl)acetamide derivatives as potent VEGFR-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Lanzhou University
Discovery of a novel family of FKBP12 "reshapers" and their use as calcium modulators in skeletal muscle under nitro-oxidative stress.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Universidad Del Pa£S Vasco Upv/Ehu
4-Oxoquinolines and monoamine oxidase: When tautomerism matters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Universit£"Magna Gr£Cia" Di Catanzaro
Discovery of 6-Oxo-4-phenyl-hexanoic acid derivatives as ROR?t inverse agonists showing favorable ADME profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 36: (2021)
Teijin Pharma
Bicyclic Ligand-Biased Agonists of S1P![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1454-1480 (2021)
Bristol Myers Squibb Research & Early Development
Copper(I)-Catalyzed Nitrile-Addition/![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1435-1453 (2021)
National Chiayi University
Secondary Metabolites from the Leather Coral-Derived Fungal Strain ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 466-473 (2021)
University of Hawai'I At Hilo
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 162-167 (2021)
Astrazeneca
Discovery of PIPE-359, a Brain-Penetrant, Selective M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 155-161 (2021)
Pipeline Therapeutics
Discovery of a Series of Pyrazinone ROR? Antagonists and Identification of the Clinical Candidate BI 730357.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 143-154 (2021)
Boehringer Ingelheim Pharmaceuticals
Synthesis and Metabolism of BTN3A1 Ligands: Studies on Modifications of the Allylic Alcohol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 136-142 (2021)
University of Iowa
Discovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 129-135 (2021)
Vertex Pharmaceuticals
Multiresidue Tetrapeptide Substitutions Yield a 140-fold Selective Melanocortin-3 over Melanocortin-4 Receptor Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 115-120 (2021)
University of Minnesota
Solution Conformations Shed Light on PROTAC Cell Permeability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 107-114 (2021)
Uppsala University
Discovery of an Anion-Dependent Farnesyltransferase Inhibitor from a Phenotypic Screen.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 99-106 (2021)
Merck
Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 93-98 (2021)
H3 Biomedicine
Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 82-87 (2021)
Chinese Academy of Sciences
Sweet and Blind Spots in E3 Ligase Ligand Space Revealed by a Thermophoresis-Based Assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 74-81 (2021)
Max Planck Institute For Developmental Biology
Design and Synthesis of Fragment Derivatives with a Unique Inhibition Mechanism of the uPAR·uPA Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 60-66 (2021)
Indiana University School of Medicine
Studying Histone Deacetylase Inhibition and Apoptosis Induction of Psammaplin A Monomers with Modified Thiol Group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 39-47 (2021)
Shenyang Pharmaceutical University
Discovery of a Pyrimidothiazolodiazepinone as a Potent and Selective Focal Adhesion Kinase (FAK) Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 30-38 (2021)
Dana-Farber Cancer Institute
Thiophene-Pyrazolourea Derivatives as Potent, Orally Bioavailable, and Isoform-Selective JNK3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 24-29 (2021)
Reaction Biology
Cyclin-Dependent Kinase Inhibitors in Cancer Therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 11-12 (2021)
Usona Institute
Novel Pyrimidinones as SHP2 Antagonists for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 12: 3-4 (2021)
Smith, Gambrell & Russell
The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
American University of Ras Al Khaimah
Recent advances in the design and development of formyl peptide receptor 2 (FPR2/ALX) agonists as pro-resolving agents with diverse therapeutic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Queen Mary University of London
Synthesis and structure-activity relationships of pyrimidine derivatives as potent and orally active FGFR3 inhibitors with both increased systemic exposure and enhanced in vitro potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 33: (2021)
Astellas Pharma
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
China Pharmaceutical University
A theranostic probe of indoleamine 2,3-dioxygenase 1 (IDO1) for small molecule cancer immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Second Military Medical University
Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1283-1345 (2021)
Hefei University of Technology
Novel 1,3,4-thiadiazole compounds as potential MAO-A inhibitors - design, synthesis, biological evaluation and molecular modelling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1063-1074 (2020)
Anadolu University
Fenretinide binding to the lysosomal protein saposin D alters ceramide solubilization and hydrolysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1048-1052 (2020)
Syracuse University
Natural product inspired optimization of a selective TRPV6 calcium channel inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1032-1040 (2020)
University of Bern
Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1023-1031 (2020)
University of Bern
Recent developments of small molecule ?-secretase modulators for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1003-1022 (2020)
Memorial Sloan-Kettering Cancer Center
Histone lysine specific demethylase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 969-981 (2020)
Taipei Medical University
Synthesis and initial pharmacology of dual-targeting ligands for putative complexes of integrin ?V?3 and PAR2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 940-949 (2020)
Marquette University
Anticancer potential of some imidazole and fused imidazole derivatives: exploring the mechanism ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 923-939 (2020)
Central University of Punjab
G-Protein biased opioid agonists: 3-hydroxy-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 896-904 (2020)
National Institute On Drug Abuse
Structure-guided discovery of selective methionyl-tRNA synthetase inhibitors with potent activity against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 885-895 (2020)
University of Washington
Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 823-832 (2020)
University of Regensburg
2-Arylamino-6-ethynylpurines are cysteine-targeting irreversible inhibitors of Nek2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 707-731 (2020)
Newcastle University
Understanding the mechanism of action of pyrrolo[3,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 665-675 (2020)
University of Zurich
Online informatics resources to facilitate cancer target and chemical probe discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 611-624 (2020)
Emory University School of Medicine
Computer-aided discovery of phenylpyrazole based amides as potent S6K1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 583-590 (2020)
Shanghai Institute of Technology
Discovery, SAR study and ADME properties of methyl 4-amino-3-cyano-1-(2-benzyloxyphenyl)-1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 577-582 (2020)
Universit£
Synthesis, evaluation and molecular modelling of piceatannol analogues as arginase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 559-568 (2020)
Univ. Bourgogne Franche-Comt�
Discovery of a novel kinase hinge binder fragment by dynamic undocking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 552-558 (2020)
Universitat De Barcelona
Arylsulfonyl histamine derivatives as powerful and selective ?-glucosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 518-527 (2020)
Universidad Nacional De Rosario
Reversing binding sensitivity to A147T translocator protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 511-517 (2020)
The University of Sydney
Chemotherapy for human schistosomiasis: how far have we come? What's new? Where do we go from here?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 455-490 (2020)
University of Cape Town
Synthesis and evaluation of anticancer activity of new 9-acridinyl amino acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 378-386 (2020)
University of Belgrade
Synthetic inhibitor leads of human tropomyosin receptor kinase A (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 370-377 (2020)
Zoetis
Structure-activity relationships of sulfonamides derived from carvacrol and their potential for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 307-316 (2020)
School of Health Sciences/Graduate Program In Pharmaceutical Sciences
Argininamide-type neuropeptide Y Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 274-282 (2020)
University of Regensburg
Development of potent CPP6-gemcitabine conjugates against human prostate cancer cell line (PC-3).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 268-273 (2020)
University of Porto
Macrocyclic peptidomimetics as inhibitors of insulin-regulated aminopeptidase (IRAP).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 234-244 (2020)
Uppsala University
Chromone and donepezil hybrids as new multipotent cholinesterase and monoamine oxidase inhibitors for the potential treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 225-233 (2020)
China Pharmaceutical University
An epigrammatic status of the '![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 184-211 (2020)
Uttaranchal University
Identification of 6-amino-1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1168-1177 (2020)
University of Dundee
Recent progress in the discovery of ghrelin ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1136-1144 (2020)
National Institute On Alcohol Abuse and Alcoholism
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 1112-1135 (2020)
University of Edinburgh
Design and synthesis of a bivalent probe targeting the putative mu opioid receptor and chemokine receptor CXCR4 heterodimer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
RSC Med Chem 11: 125-131 (2020)
Virginia Commonwealth University
Design, synthesis and biological evaluation of novel indanone containing spiroisoxazoline derivatives with selective COX-2 inhibition as anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Qom University of Medical Sciences
A covalent p97/VCP ATPase inhibitor can overcome resistance to CB-5083 and NMS-873 in colorectal cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
California Institute of Technology
Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Jiangxi University of Traditional Chinese Medicine
In silico drug repositioning on F508del-CFTR: A proof-of-concept study on the AIFA library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
National Research Council (Itb-Cnr)
Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1558-1569 (2021)
West China Hospital of Sichuan University
How a Fragment Draws Attention to Selectivity Discriminating Features between the Related Proteases Trypsin and Thrombin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1611-1625 (2021)
Philipps-Universit£T Marburg
Structure-Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1649-1669 (2021)
Chinese Academy of Sciences
Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 909-924 (2021)
Janssen Research and Development
Design, synthesis, and antiviral activity of a series of CD4-mimetic small-molecule HIV-1 entry inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Lindsley F. Kimball Research Institute
Targeting MYC: From understanding its biology to drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Institut De Recherches Cliniques De Montreal (IRCM)
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 36: (2021)
China Pharmaceutical University
Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 925-937 (2021)
Zhengzhou University
Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Zhejiang University
Rational design of SphK inhibitors using crystal structures aided by computer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Shandong First Medical University & Shandong Academy of Medical Sciences
Discovery of natural anti-inflammatory alkaloids: Potential leads for the drug discovery for the treatment of inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Zhejiang University
Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Rheinische Friedrich-Wilhelms-University of Bonn
A novel [5.2.1]bicyclic amine is a potent analgesic without µ opioid activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 36: (2021)
Daiichi Sankyo
Discovery of a PROTAC targeting ALK with in vivo activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
West China Hospital of Sichuan University
Discovery of a true bivalent dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Changzhou University
Design and Evaluation of Peptide Dual-Agonists of GLP-1 and NPY2 Receptors for Glucoregulation and Weight Loss with Mitigated Nausea and Emesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1127-1138 (2021)
Syracuse University
Probing the substitution pattern of indole-based scaffold reveals potent and selective sphingosine kinase 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Virginia Tech
A perspective on medicinal chemistry approaches towards adenomatous polyposis coli and Wnt signal based colorectal cancer inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Gitam (Deemed To Be University)
The subgroup of 2'-hydroxy-flavonoids: Molecular diversity, mechanism of action, and anticancer properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Oncowitan
Berberine Directly Targets the NEK7 Protein to Block the NEK7-NLRP3 Interaction and Exert Anti-inflammatory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 768-781 (2021)
Chinese Academy of Medical Sciences and Peking Union Medical College
Design, synthesis and evaluation of 1-benzyl-1H-imidazole-5-carboxamide derivatives as potent TGR5 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Henan University
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Charles University
Discovery of novel 1,3,5-triazine derivatives as potent inhibitor of cervical cancer via dual inhibition of PI3K/mTOR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
Maternal and Child Health Hospital of Hubei Province
Novel arylcarbamate-N-acylhydrazones derivatives as promising BuChE inhibitors: Design, synthesis, molecular modeling and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 32: (2021)
State University of Maring£
Structure-Activity Relationship and Biological Investigation of SR18292 (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 980-990 (2021)
The Scripps Research Institute
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Sun Yat-Sen University
Discovery and Biological Evaluation of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 958-979 (2021)
Ewha Womans University
The Development of Hsp90?-Selective Inhibitors to Overcome Detriments Associated with ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1545-1557 (2021)
The University of Notre Dame
Ifenprodil Stereoisomers: Synthesis, Absolute Configuration, and Correlation with Biological Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1170-1179 (2021)
Westf£Lische Wilhelms-Universit£T M£Nster
Evolution in non-peptide ?-helix mimetics on the road to effective protein-protein interaction modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
IQM-CSIC
Tetrazanbigen Derivatives as Peroxisome Proliferator-Activated Receptor Gamma (PPAR?) Partial Agonists:?Design, Synthesis, Structure-Activity Relationship, and Anticancer Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1018-1036 (2021)
Chongqing Medical University
Design of novel Xenopus GLP-1-based dual glucagon-like peptide 1 (GLP-1)/glucagon receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Affiliated Tumor Hospital of Guangxi Medical University
Recent findings leading to the discovery of selective dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
University of Camerino
Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
City University of Hong Kong
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Istanbul Medipol University
Design, synthesis and anti-inflammatory activity of imidazol-5-yl pyridine derivatives as p38?/MAPK14 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 31: (2021)
University of Science & Technology (Ust)
Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 31: (2021)
Chemveda Life Sciences India
Anti-inflammatory activity of naturally occuring diarylheptanoids - A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 31: (2021)
Universita Paul Sabatier
Substituted diaryl ether compounds as retinoic acid-related orphan Receptor-?t (ROR?t) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 35: (2021)
Bristol Myers Squibb
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University of Coimbra
Peripheral Selective Oxadiazolylphenyl Alanine Derivatives as Tryptophan Hydroxylase 1 Inhibitors for Obesity and Fatty Liver Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1037-1053 (2021)
Gwangju Institute of Science and Technology
The long and winding road of designing phosphodiesterase inhibitors for the treatment of heart failure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Rural Federal University of Rio De Janeiro
Discovery of a Novel and Brain-Penetrant ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1103-1115 (2021)
Takeda Pharmaceutical
Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 343-353 (2021)
Galapagos
Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 845-860 (2021)
Arcus Biosciences
Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Gazi University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Zhejiang University
Small Molecule Inhibitors Targeting Biosynthesis of Ceramide, the Central Hub of the Sphingolipid Network.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 279-297 (2021)
TBA
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 719-740 (2021)
University of Cape Town
Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 566-585 (2021)
University of Michigan
Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 1-10 (2021)
The Chinese University of Hong Kong (Shenzhen)
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 31: (2021)
Shanghai Institute of Materia Medica
Synthesis, anticancer and antimicrobial evaluation of new benzofuran based derivatives: PI3K inhibition, quorum sensing and molecular modeling study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 31: (2021)
Mansoura University
Development and optimization of halogenated vinyl sulfones as Nrf2 activators for the treatment of Parkinson's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Korea Institute of Science & Technology (Kist)
Lipophilic tail modifications of 2-(hydroxymethyl)pyrrolidine scaffold reveal dual sphingosine kinase 1 and 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Virginia Tech
Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Taisho Pharmaceutical
Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 370-384 (2021)
Seoul National University
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Second Military Medical University
Novel amide and imidazole compounds as potent hematopoietic prostaglandin D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Cayman Chemical
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 385-403 (2021)
East China Normal University
Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 481-515 (2021)
Leiden University and Oncode Institute
Spirocyclic Scaffolds in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 150-183 (2021)
Goethe University
Novel Nonsecosteroidal Vitamin D Receptor Modulator Combined with Gemcitabine Enhances Pancreatic Cancer Therapy through Remodeling of the Tumor Microenvironment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 629-643 (2021)
China Pharmaceutical University
Convenient Retinoid X Receptor Binding Assay Based on Fluorescence Change of the Antagonist NEt-C343.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 861-870 (2021)
Okayama University Graduate School of Medicine
Development of Orally Efficacious Allosteric Inhibitors of TNF? via Fragment-Based Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 417-429 (2021)
Abbvie
3,4-Dihydropyrimidin-2(1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 458-480 (2021)
Universidade De Santiago De Compostela
Novel Sigma 1 Receptor Antagonists as Potential Therapeutics for Pain Management.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 890-904 (2021)
The State University of New Jersey
Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 527-542 (2021)
Academia Sinica
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 677-694 (2021)
Bristol-Myers Squibb Research & Development
Diflunisal Derivatives as Modulators of ACMS Decarboxylase Targeting the Tryptophan-Kynurenine Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 797-811 (2021)
University of Texas At San Antonio
Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 516-526 (2021)
Ochanomizu University
Potent and Specific Inhibition of NTCP-Mediated HBV/HDV Infection and Substrate Transporting by a Novel, Oral-Available Cyclosporine A Analogue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 543-565 (2021)
National Institute of Biological Sciences
Variously substituted 2-oxopyridine derivatives: Extending the structure-activity relationships for allosteric modulation of the cannabinoid CB2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University of Pisa
Omipalisib inspired macrocycles as dual PI3K/mTOR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Spanish National Cancer Research Centre (Cnio)
Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Leipzig University
2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University Hospital Hradec Kralove
STING, a promising target for small molecular immune modulator: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Yantai University
Design, synthesis and biological evaluation of imidazole and triazole-based carbamates as novel aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
"G. D'Annunzio" University
Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Design, synthesis and evaluation of PD-L1 peptide antagonists as new anticancer agents for immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Ferdowsi University of Mashhad
Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Heinrich-Heine-Universit£T D£Sseldorf
Design, synthesis, and biological studies of novel 3-benzamidobenzoic acid derivatives as farnesoid X receptor partial agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Guangdong Pharmaceutical University
MCC950, a NLRP3 inhibitor, ameliorates lipopolysaccharide-induced lung inflammation in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Zhejiang Chinese Medical University
Synthetic approaches to unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles and their MAO-B inhibitory activity. A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Medical University-Sofia
Modulators of hERAP2 discovered by high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Institut Pasteur De Lille
Discovery of natural product ellagic acid as a potent CD73 and CD39 dual inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Ningxia Medical University
Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Jubilant Therapeutics India
Characterization of ibrutinib as a non-covalent inhibitor of SRC-family kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Central South University
Novel BuChE-IDO1 inhibitors from sertaconazole: Virtual screening, chemical optimization and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Southwest University
N-(6-phenylpyridazin-3-yl)benzenesulfonamides as highly potent, brain-permeable, and orally active kynurenine monooxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Sumitomo Dainippon Pharma.
Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 812-839 (2021)
University of Barcelona
Discovery of Venturicidin Congeners and Identification of the Biosynthetic Gene Cluster from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 110-119 (2021)
Second Military Medical University
Novel Carboline Fungal Histone Deacetylase (HDAC) Inhibitors for Combinational Treatment of Azole-Resistant Candidiasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1116-1126 (2021)
Second Military Medical University
Tuning the Biological Activity of RGD Peptides with Halotryptophans?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 586-601 (2021)
Bielefeld University
Phytocannabinoid Pharmacology: Medicinal Properties of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 142-160 (2021)
Scientus Pharma
Discovery of a "Gatekeeper" Antagonist that Blocks Entry Pathway to Retinoid X Receptors (RXRs) without Allosteric Ligand Inhibition in Permissive RXR Heterodimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 430-439 (2021)
Okayama University Graduate School of Medicine
Structure-Based Drug Design and Synthesis of PI3K?-Selective Inhibitor (PF-06843195).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 644-661 (2021)
Pfizer
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 326-342 (2021)
Pfizer
Development and Therapeutic Potential of NUAKs Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2-25 (2021)
University of Science and Technology (Ust)
Bioactive Cyclization Optimizes the Affinity of a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Peptide Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 2523-2533 (2021)
The University of Queensland
Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 298-325 (2021)
China Pharmaceutical University
Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Shandong University
Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 695-710 (2021)
University of Hawaii Cancer Center
Natural Products with Potential to Treat RNA Virus Pathogens Including SARS-CoV-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 161-182 (2021)
University of California San Diego
Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 602-615 (2021)
Universit£
Evaluation of pyrrolidine-based analog of jaspine B as potential SphK1 inhibitors against rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Shandong First Medical University & Shandong Academy of Medical Sciences
Elongation of the side chain by linear alkyl groups increases the potency of salacinol, a potent ?-glucosidase inhibitor from the Ayurvedic traditional medicine "Salacia," against human intestinal maltase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Kindai University
Glycogen Synthase Kinase 3?: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 26-41 (2021)
University of Turin
TLR2 Agonistic Small Molecules: Detailed Structure-Activity Relationship, Applications, and Future Prospects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 233-278 (2021)
Panjab University
Diverse chemical space of indoleamine-2,3-dioxygenase 1 (Ido1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Panjab University
Development of 2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of aldehyde dehydrogenase 1A (ALDH1A) as potential adjuncts to ovarian cancer chemotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University of Michigan
Synthesis and evaluation of tiaprofenic acid-derived UCHL5 deubiquitinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Wayne State University
In vitro and in vivo effects of inhibitors on actin and myosin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Tu Dresden
Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
China Pharmaceutical University
Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Shandong University
Does targeting Arg98 of FimH lead to high affinity antagonists?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University of Ljubljana
1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Palack£
Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
China Medical University
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Shanghai Institute of Materia Medica
A study of the structure-affinity relationship in SYA16263; is a D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Florida A&M University
Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
China Pharmaceutical University
Mining Natural Products for Macrocycles to Drug Difficult Targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 1054-1072 (2021)
Uppsala University
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2519-2525 (2020)
Astrazeneca
Novel Tricyclic Pyroglutamide Derivatives as Potent ROR?t Inverse Agonists Identified using a Virtual Screening Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2510-2518 (2020)
Bristol Myers Squibb
Discovery of PEGylated 6-Benzhydryl-4-amino-quinazolines as Peripherally Restricted CB![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2504-2509 (2020)
Janssen Research & Development
Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2476-2483 (2020)
Merck
Optimization of Versatile Oxindoles as Selective PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2461-2469 (2020)
Merck
Human Insulin-like Peptide 5 (INSL5). Identification of a Simplified Version of Two-Chain Analog A13.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2455-2460 (2020)
The University of Melbourne
Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2446-2454 (2020)
The Ohio State University
Decreasing HepG2 Cytotoxicity by Lowering the Lipophilicity of Benzo[d]oxazolephosphinate Ester Utrophin Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2421-2427 (2020)
University of Oxford
Synthesis, Characterization, and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2397-2405 (2020)
Bahauddin Zakariya University
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1? Inhibitory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2389-2396 (2020)
Paraza Pharma
Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2374-2381 (2020)
Aurigene Discovery Technologies
Novel Compounds as STING Modulators for Treating Hepatitis B Virus Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2372-2373 (2020)
Smith, Gambrell & Russell
Novel Arginase Inhibitors for Treating Cancer and Respiratory Inflammatory Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2370-2371 (2020)
Smith, Gambrell & Russell
Novel KIF18A Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2368-2369 (2020)
Smith, Gambrell & Russell
Carboxamides as Modulators of Sodium Channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2364-2365 (2020)
Temple University
Estrogen Receptor Degrading PROTACS for the Treatment of Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2361-2363 (2020)
Usona Institute
Novel Potassium Channel Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2357-2358 (2020)
Temple University
2-Amino-N-heteroaryl-nicotimamides as Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2354-2356 (2020)
Temple University
Novel APOL1 Inhibitors for Treating Kidney Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2352-2353 (2020)
Smith, Gambrell & Russell
Novel CDK2 Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2346-2347 (2020)
Smith, Gambrell & Russell
Novel Pyrido-pyrimidinones and Pteridinones as Endoribonuclease Inositol Requiring Enzyme 1 (IRE1?) Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2344-2345 (2020)
Smith, Gambrell & Russell
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Universidade Federal De S£O Paulo
Identification of N-acyl-N-indanyl-?-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 30: (2021)
Kissei Pharmaceutical
Development of Mcl-1 inhibitors for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
National University of Ireland Galway
Discovery and optimization of substituted oxalamides as novel heme-displacing IDO1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Phenex Pharmaceuticals
Discovery of BAZ1A bromodomain inhibitors with the aid of virtual screening and activity evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Sichuan Provincial People'S Hospital
Development of Novel Tetrahydroquinoline Inhibitors of NLRP3 Inflammasome for Potential Treatment of DSS-Induced Mouse Colitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 871-889 (2021)
China Pharmaceutical University
Exploring the Chemical Space of Benzothiazole-Based DNA Gyrase B Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2433-2440 (2020)
University of Ljubljana
Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Perugia
Rationally designed N-phenylsulfonylindoles as a tool for the analysis of the non-basic 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Polish Academy of Sciences
Discovery and development of selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Isolation and Pharmacological Characterization of Six Opioidergic ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 71-80 (2021)
University of Illinois At Chicago
Modifications at C(5) of 2-(2-Pyrrolidinyl)-Substituted 1,4-Benzodioxane Elicit Potent ?4?2 Nicotinic Acetylcholine Receptor Partial Agonism with High Selectivity over the ?3?4 Subtype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15668-15692 (2020)
Universit£
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPAR?/? Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 16012-16027 (2020)
Seoul National University
The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
The University of Sydney
-Benzyl-linoleamide, a Constituent of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3689-3697 (2020)
University of California Davis
Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
University of Sharjah
Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: Towards adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Sun Yat-Sen University
Discovery of a novel small-molecule inhibitor of Fam20C that induces apoptosis and inhibits migration in triple negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Southwest Jiaotong University
Design, synthesis and biological evaluation of novel 4-(pyrrolo[2,3-d]pyrimidine-4-yloxy)benzamide derivatives as potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Wenzhou Medical University
Design, synthesis, and biological evaluation of 2,6,7-substituted pyrrolo[2,3-d]pyrimidines as cyclin dependent kinase inhibitor in pancreatic cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Chinese Academy of Medical Sciences and Peking Union Medical College
Molecular docking and synthesis of caffeic acid analogous and its anti-inflammatory, analgesic and ulcerogenic studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
University of Mysore
Discovery of highly potent heme-displacing IDO1 inhibitors based on a spirofused bicyclic scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Phenex Pharmaceuticals
Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15864-15882 (2020)
Idorsia Pharmaceuticals
Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15153-15186 (2020)
Shanghai Institute of Materia Medica
Cyclic Peptidyl Inhibitors against CAL/CFTR Interaction for Treatment of Cystic Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15773-15784 (2020)
The Ohio State University
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15906-15945 (2020)
Texas A&M University
The 3-D conformational shape of N-naphthyl-cyclopenta[d]pyrimidines affects their potency as microtubule targeting agents and their antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Duquesne University
Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
University of Sharjah
Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Universidad Complutense
Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Normandie Univ
Research progress in biological activities of isochroman derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Shaanxi University of Chinese Medicine
Synergistic effects of curcumin and its analogs with other bioactive compounds: A comprehensive review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Texas Southern University
Xanthenes in Medicinal Chemistry - Synthetic strategies and biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Ciimar
N-(Methyloxycarbonyl)thiophene sulfonamides as high affinity AT2 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Uppsala University
Discovery of novel PARP/PI3K dual inhibitors with high efficiency against BRCA-proficient triple negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
China Pharmaceutical University
Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRAS![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Shanghai Institute of Materia Medica (Simm)
4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: A promising scaffold towards bioactive molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Universita Degli Studi di Palermo
Switching a Xanthine Oxidase Inhibitor to a Dual-Target Antagonist of P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15752-15772 (2020)
Shenyang Pharmaceutical University
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15564-15590 (2020)
Astrazeneca
Non-hydroxamate inhibitors of 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR): A critical review and future perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Birla Institute of Technology and Science-Pilani
Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Ege University
Discovery of indazole-pyridinone derivatives as a novel class of potent and selective MNK1/2 kinase inhibitors that protecting against endotoxin-induced septic shock.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Ryvu Therapeutics
Discovery of a Potent and Selective PI3K? Inhibitor (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14700-14723 (2020)
Lupin
Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15852-15863 (2020)
Sun Yat-Sen University
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 16028-16042 (2020)
Huazhong University of Science & Technology
Soluble Guanylate Cyclase Inhibitors Discovered among Natural Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3642-3651 (2020)
Inserm U1182 - Cnrs Umr7645
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15821-15851 (2020)
Fondazione Istituto Italiano Di Tecnologia
Development of Potential Antitumor Agents from the Scaffolds of Plant-Derived Terpenoid Lactones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15410-15448 (2020)
The Ohio State University
Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15639-15654 (2020)
The Scripps Research Institute
Synthesis and biological evaluation of all possible inosine-mixed cyclic dinucleotides that activate different hSTING variants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Nankai University
Discovery of new thieno[2,3-d]pyrimidine and thiazolo[5,4-d]pyrimidine derivatives as orally active phosphoinositide 3-kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of a benzimidazole series as the first highly potent and selective ACSL1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Shionogi
Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15883-15905 (2020)
Icahn School of Medicine At Mount Sinai
A Quick Route to Multiple Highly Potent SARS-CoV-2 Main Protease Inhibitors![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ChemMedChem (2020)
Texas A&M University
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15344-15370 (2020)
Northwestern University
Discovery of novel CA-4 analogs as dual inhibitors of tubulin polymerization and PD-1/PD-L1 interaction for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Southern Medical University
Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15979-15996 (2020)
Zhengzhou University
Optimization of novel oxidative DIMs as Nur77 modulators of the Nur77-Bcl-2 apoptotic pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Xiamen University
Outline of gelatinase inhibitors as anti-cancer agents: A patent mini-review for 2010-present.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Jadavpur University
Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Shandong University
A review: Biologically active 3,4-heterocycle-fused coumarins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Tehran University of Medical Sciences
Synthesis and in vitro evaluation of novel spiroketopyrazoles as acetyl-CoA carboxylase inhibitors and potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Xuzhou Medical University
4-Acyl Pyrroles as Dual BET-BRD7/9 Bromodomain Inhibitors Address BETi Insensitive Human Cancer Cell Lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15603-15620 (2020)
Albert-Ludwigs-Universit£T Freiburg
Design, synthesis, evaluation, and SAR of 4-phenylindoline derivatives, a novel class of small-molecule inhibitors of the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of tetrahydroquinolines and benzomorpholines as novel potent ROR?t agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Fudan University
Recent Advances in the Development of PD-L1 Modulators: Degraders, Downregulators, and Covalent Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15389-15398 (2020)
Southern Medical University
Recent advances on synthesis and biological activities of aurones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Northwest A&F University
Identification and structure-activity relationship studies of small molecule inhibitors of the human cathepsin D.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Aten Porus Lifesciences
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15709-15725 (2020)
Lanzhou University
Heteroaryl ether analogues of an antileishmanial 7-substituted 2-nitroimidazooxazine lead afford attenuated hERG risk: In vitro and in vivo appraisal.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Auckland
Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15399-15409 (2020)
Chinese Academy of Sciences
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15541-15563 (2020)
TBA
Discovery of Novel and Highly Potent Resorcinol Dibenzyl Ether-Based PD-1/PD-L1 Inhibitors with Improved Drug-like and Pharmacokinetic Properties for Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15946-15959 (2020)
Southern Medical University
Structural modifications in the distal, regulatory region of histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Jagiellonian University Medical College
Synthesis and anticancer activity evaluation of naphthalene-substituted triazole spirodienones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Sichuan University
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNF? Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15050-15071 (2020)
Bristol Myers Squibb
ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 33: (2021)
Vertex Pharmaceuticals
Synthesis and Structure-Activity Relationship of Tetra-Substituted Cyclohexyl Diol Inhibitors of Proviral Insertion of Moloney Virus (PIM) Kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14885-14904 (2020)
Novartis Institutes For Biomedical Research
Paracetamol analogues conjugated by FAAH induce TRPV1-mediated antinociception without causing acute liver toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Lund University
Engagement of phytoestrogens in breast cancer suppression: Structural classification and mechanistic approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Central University of Punjab
Angel or Devil ? - CDK8 as the new drug target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 213: (2021)
Hefei Technology College
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Nankai University
-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14921-14936 (2020)
West China Hospital of Sichuan University
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
University of S£O Paulo
Lead optimization of the VU0486321 series of mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 32: (2021)
Vanderbilt University
Interdiction at a protein-protein interface: MCL-1 inhibitors for oncology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 32: (2021)
Amgen
Store-Operated Calcium Entry as a Therapeutic Target in Acute Pancreatitis: Discovery and Development of Drug-Like SOCE Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14761-14779 (2020)
Universit£
In Vivo Biological Evaluation of a Synthetic Royleanone Derivative as a Promising Fast-Acting Trypanocidal Agent by Inducing Mitochondrial-Dependent Necrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3571-3583 (2020)
Hospitales Universitarios De Granada/University of Granada
Discovery of Potent, Highly Selective, and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14576-14593 (2020)
Novartis Institutes For Biomedical Research
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Guangzhou Institutes of Biomedicine and Health
Synthesis and structure-activity studies of novel anhydrohexitol-based Leucyl-tRNA synthetase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Ku Leuven
Ligand-based optimization to identify novel 2-aminobenzo[d]thiazole derivatives as potent sEH inhibitors with anti-inflammatory effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of 4-amino-1H-pyrazolo[3,4-d]pyrimidin derivatives as novel discoidin domain receptor 1 (DDR1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Pyrazolo[1,5-a]pyrimidine based Trk inhibitors: Design, synthesis, biological activity evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Jiangnan University
Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Central South University
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Panjab University
The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Jiangxi Science & Technology Normal University
Xanthones for melanogenesis inhibition: Molecular docking and QSAR studies to understand their anti-tyrosinase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Universidade Dos A£Ores
Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Zhejiang Hisun Pharmaceutical
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
China Pharmaceutical University
EST64454: a Highly Soluble ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14979-14988 (2020)
Esteve Pharmaceuticals
Metronidazole-conjugates: A comprehensive review of recent developments towards synthesis and medicinal perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
North-West University
Design and development of FGF-23 antagonists: Definition of the pharmacophore and initial structure-activity relationships probed by synthetic analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Tennessee Technological University
Current status in the discovery of dual BET/HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
The First Affiliated Hospital of Zhengzhou University
Synthesis and evaluation of a UMI-77-based fluorescent probe for selective detecting Mcl-1 protein and imaging in living cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Shandong University
Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Massachusetts College of Pharmacy and Health Sciences University
Structure guided development of potent piperazine-derived hydroxamic acid inhibitors targeting falcilysin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 32: (2021)
California State University
Peptide Ligands Specifically Targeting HER2 Receptor and the Role Played by a Synthetic Model System of the Receptor Extracellular Domain: Hypothesized Future Perspectives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15333-15343 (2020)
National Research Council
Stabilization Strategies for Linear Minigastrin Analogues: Further Improvements ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14668-14679 (2020)
Medical University of Innsbruck
Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14740-14760 (2020)
Bristol Myers Squibb Research and Early Development
Fragment-to-Lead Medicinal Chemistry Publications in 2019.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15494-15507 (2020)
Novartis Institutes For Biomedical Research
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14404-14424 (2020)
Jinan University
Optimization of piperidine constructed peptidyl derivatives as proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Hangzhou Xixi Hospital
Development of programmable gemcitabine-GnRH pro-drugs bearing linker controllable "click" oxime bond tethers and preclinical evaluation against prostate cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
University of Ioannina
Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Universit£
Development of pyrimidone D1 dopamine receptor positive allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
National Institutes of Health
Pyrrolo[2,3-b]pyridine-3-one derivatives as novel fibroblast growth factor receptor 4 inhibitors for the treatment of hepatocellular carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Nanjing University of Chinese Medicine
Synthesis and structure-activity relationship of coumarins as potent Mcl-1 inhibitors for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Dalian University of Technology
Exploration of nitrogen heterocycle scaffolds for the development of potent human neutrophil elastase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
University of Florence
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 211: (2021)
Chinese Academy of Sciences
Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14680-14699 (2020)
Goethe University Frankfurt
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14626-14646 (2020)
University of North Carolina At Chapel Hill
Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15115-15139 (2020)
China Pharmaceutical University
Effects of C-Terminal B-Chain Modifications in a Relaxin 3 Agonist Analogue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2336-2340 (2020)
The University of Melbourne
Bivalent Ligand Aiming Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Dimers in Opioid Enhanced HIV-1 Entry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2318-2324 (2020)
Virginia Commonwealth University
Simultaneous Inhibition of SIRT2 Deacetylase and Defatty-Acylase Activities via a PROTAC Strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2305-2311 (2020)
Cornell University
In Silico-Guided Identification of New Potent Inhibitors of Carbonic Anhydrases Expressed in ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2294-2299 (2020)
Universit£
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2285-2289 (2020)
University of Bayreuth
Benzoxaboroles: New Potent Inhibitors of the Carbonic Anhydrases of the Pathogenic Bacterium ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2277-2284 (2020)
University of Florence
Spiroindoline-Capped Selective HDAC6 Inhibitors: Design, Synthesis, Structural Analysis, and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2268-2276 (2020)
University of Siena
Fluorescent Probes for Ecto-5'-nucleotidase (CD73).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2253-2260 (2020)
University of Bonn
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2244-2252 (2020)
Arcus Biosciences
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2238-2243 (2020)
Dana-Farber Cancer Institute
A Chemical Probe for the Methyl Transferase PRMT5 with a Novel Binding Mode.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2227-2231 (2020)
Janssen Pharmaceutica
?-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2212-2220 (2020)
University of Copenhagen
Synthesis and Biological Evaluation of Pyrroloindolines as Positive Allosteric Modulators of the ?1?2?2 GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2204-2211 (2020)
California Institute of Technology
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2195-2203 (2020)
Bristol Myers Squibb Research
Hydrogen Peroxide Inducible JAK3 Covalent Inhibitor: Prodrug for the Treatment of RA with Enhanced Safety Profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2182-2189 (2020)
China Pharmaceutical University
Identification of 3,5-Dimethylisoxazole Derivatives as BRD4 Inhibitors for the Treatment of Colorectal Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2174-2181 (2020)
China Pharmaceutical University
Discovery and SAR of Novel Disubstituted Quinazolines as Dual PI3Kalpha/mTOR Inhibitors Targeting Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2156-2164 (2020)
Temple University
Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2151-2155 (2020)
Shanghai Hengrui Pharmaceutical
Biotransformation: Impact and Application of Metabolism in Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2087-2107 (2020)
Hypha Discovery
Novel 5-Alkyl Pyrrolidine Orexin Receptor Agonists for Treating Sleep Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2085-2086 (2020)
Smith, Gambrell & Russell
Novel KIF18A Inhibitors for Treating Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2079-2080 (2020)
Smith, Gambrell & Russell
Novel Bicyclic Heteroaryl Compounds as ?-Secretase Modulators for Treating Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2077-2078 (2020)
Smith, Gambrell & Russell
Therapeutic Potential of Autotaxin Inhibitors in Treatment of Interstitial Lung Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2075-2076 (2020)
Therachem Research Medilab
Use of Dihydroorotate Dehydrogenase Inhibitors for Treatment of Autoimmune Diseases and Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2072-2074 (2020)
Therachem Research Medilab
Modulation of Androgen Receptor for Therapeutic Application in Cancer and Viral Infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2068-2069 (2020)
Usona Institute
Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Kangwon National University
Design, synthesis, and anti-proliferative evaluation of new quinazolin-4(3H)-ones as potential VEGFR-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Al-Azhar University
Design, synthesis and biological evaluation of novel chalcone-like compounds as potent and reversible pancreatic lipase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Zhengzhou University
Recent Advances in ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15218-15242 (2020)
Shenyang Pharmaceutical University
From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14780-14804 (2020)
Leibniz-Forschungsinstitut F�R Molekulare Pharmakologie (Fmp)
Computational Fragment-Based Design Facilitates Discovery of Potent and Selective Monoamine Oxidase-B (MAO-B) Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15021-15036 (2020)
Sunshine Lake Pharma
Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14805-14820 (2020)
Taisho Pharmaceutical
Targeted Covalent Inhibition of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2131-2138 (2020)
Broad Institute of Mit and Harvard
Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15037-15049 (2020)
Yale University
Design, Synthesis, and Structure-Activity Relationship Studies of (4-Alkoxyphenyl)glycinamides and Bioisosteric 1,3,4-Oxadiazoles as GPR88 Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14989-15012 (2020)
Research Triangle Institute
Design and Optimization of an Acyclic Amine Series of TRPV4 Antagonists by Electronic Modulation of Hydrogen Bond Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14867-14884 (2020)
Glaxosmithkline
Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14609-14625 (2020)
Institute
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3K? inhibitors via docking-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Zhejiang University
The discovery of quinoline derivatives, as NF-?B inducing kinase (NIK) inhibitors with anti-inflammatory effects in vitro, low toxicities against T cell growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Celon Pharma
Novel quinolone-based potent and selective HDAC6 inhibitors: Synthesis, molecular modeling studies and biological investigation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
University of Siena
Water-soluble inhibitors of ABCG2 (BCRP) - A fragment-based and computational approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
University of Regensburg
From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Eberhard Karls Universit£T T£Bingen
Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13951-13972 (2020)
University of Texas Medical Branch
Targeting the Allosteric Pathway That Interconnects the Core-Functional Scaffold and the Distal Phosphorylation Sites for Specific Dephosphorylation of Bcl-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13733-13744 (2020)
Dalian University of Technology
Selective Inhibitors of G2019S-LRRK2 Kinase Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14821-14839 (2020)
Escape Bio
Diazaspirononane Nonsaccharide Inhibitors of O-GlcNAcase (OGA) for the Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14017-14044 (2020)
Janssen-Cilag
High Selectivity of an ?-Conotoxin LvIA Analogue for ?3?2 Nicotinic Acetylcholine Receptors Is Mediated by ?2 Functionally Important Residues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13656-13668 (2020)
Guangxi University
Design, synthesis and biological evaluation of imidazolopyridone derivatives as novel BRD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
China Pharmaceutical University
Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 29: (2021)
Jadavpur University
An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
University of Kwazulu-Natal (Westville)
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 357-369 (2021)
Vrije Universiteit Brussel
Discovery of a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins through the modulation of atropisomer interconversion properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Shanghai Institute of Pharmaceutical Industry
ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 212: (2021)
Southeast University
2-((1-Phenyl-1H-1,2,3-triazol-4-yl)methyl)-2-azabicyclo[3.2.1]octan-3-one derivatives: Simplification and modification of aconitine scaffold for the discovery of novel anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
China Medical University
Synthesis and characterization of new potent TLR7 antagonists based on analysis of the binding mode using biomolecular simulations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Csir-Indian Institute of Chemical Biology
PROTACs to address the challenges facing small molecule inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Oregon Health & Science University
Exploring the ability of dihydropyrimidine-5-carboxamide and 5-benzyl-2,4-diaminopyrimidine-based analogues for the selective inhibition of L. major dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Comsats University Islamabad
Chemical and pharmacological characterization of the TRPML calcium channel blockers ML-SI1 and ML-SI3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Ludwig-Maximilians University
Targeting SARS-CoV-2 Proteases and Polymerase for COVID-19 Treatment: State of the Art and Future Opportunities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 65: 2716-2746 (2022)
University of Naples "Federico Ii
Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13825-13850 (2020)
National Engineering Research Center For The Emergency Drug
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 64: 941-957 (2021)
Fudan University
Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13994-14016 (2020)
University of Michigan
Novel naphthylamide derivatives as dual-target antifungal inhibitors: Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Liaocheng University
Syntheses and anti-HIV and human cluster of differentiation 4 (CD4) down-modulating potencies of pyridine-fused cyclotriazadisulfonamide (CADA) compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Nevada
Discovery of (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13973-13993 (2020)
Hefei Institutes of Physical Science
Discovery and optimization of withangulatin A derivatives as novel glutaminase 1 inhibitors for the treatment of triple-negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Novel 2,7-Diazaspiro[4,4]nonane Derivatives to Inhibit Mouse and Human Osteoclast Activities and Prevent Bone Loss in Ovariectomized Mice without Affecting Bone Formation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13680-13694 (2020)
Universit£
Identification of a New Heterocyclic Scaffold for Inhibitors of the Polo-Box Domain of Polo-like Kinase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14087-14117 (2020)
National Cancer Institute
Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Janssen Research & Development
Synthesis and Pharmacology of a Novel ?-? Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13618-13637 (2020)
St Louis College of Pharmacy and Washington University
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13796-13824 (2020)
Merck
Therapeutic potential for coxibs-nitric oxide releasing hybrids in cystic fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Sapienza University of Rome
Discovery of novel pyrazolo[3,4-b]pyridine scaffold-based derivatives as potential PIM-1 kinase inhibitors in breast cancer MCF-7 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Suez Canal University
Design, synthesis and biological evaluation of new bivalent quinazoline analogues as IAP antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 34: (2021)
Chung-Ang University
4-(Difluoromethyl)-5-(4-((3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13595-13617 (2020)
University of Basel
Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 32: (2021)
Merck
Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Iranian Fisheries Science Research Institute
N-Hydroxyformamide LpxC inhibitors, their in vivo efficacy in a mouse Escherichia coli infection model, and their safety in a rat hemodynamic assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Entasis Therapeutics
Development of autotaxin inhibitors: A series of tetrazole cinnamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Novartis Institutes For Biomedical Research
Design, synthesis and screening of benzimidazole containing compounds with methoxylated aryl radicals as cytotoxic molecules on (HCT-116) colon cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Misr University For Science & Technology
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Shandong First Medical University & Shandong Academy of Medical Sciences
Synthesis and biological screening of thiosemicarbazones of substituted 3-acetylcoumarins having d-glucose moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Institute For Advanced Technology (Vietnam Academy of Military Science and Technology)
Recent research progress of Uncaria spp. based on alkaloids: phytochemistry, pharmacology and structural chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
China Pharmaceutical University
In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Universit£
2-Aminothiazole: A privileged scaffold for the discovery of anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Hunan University of Science and Technology
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13878-13898 (2020)
University of Kansas
Discovery of S64315, a Potent and Selective Mcl-1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13762-13795 (2020)
Servier Research Institute of Medicinal Chemistry
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
National Institute of Pharmaceutical Education and Research (NIPER)
Peptide Inhibitors of the ?-Cobratoxin-Nicotinic Acetylcholine Receptor Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13709-13718 (2020)
University of Bergen
Development of a Polo-like Kinase-1 Polo-Box Domain Inhibitor as a Tumor Growth Suppressor in Mice Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14905-14920 (2020)
Korea Basic Science Institute (Kbsi)
A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor ? Binding Properties and Biological Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13124-13139 (2020)
Aix Marseille University
Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13187-13196 (2020)
University of South Florida
Targeting nuclear protein TDP-43 by cell division cycle kinase 7 inhibitors: A new therapeutic approach for amyotrophic lateral sclerosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Centro De Investigaciones Biol�Gicas Margarita Salas-Csic
Di-aryl guanidinium derivatives: Towards improved ?2-Adrenergic affinity and antagonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Trinity College
Potent antiproliferative activity of bradykinin B2 receptor selective agonist FR-190997 and analogue structures thereof: A paradox resolved?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
University of Patras
Small molecule therapeutics for tauopathy in Alzheimer's disease: Walking on the path of most resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Karolinska Institutet
Selective Estrogen Receptor Degraders (SERDs): A Promising Strategy for Estrogen Receptor Positive Endocrine-Resistant Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15094-15114 (2020)
Nanjing University of Chinese Medicine
Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Xinyang Normal University
Discovery of a Remarkable Methyl Shift Effect in the Vanilloid Activity of Triterpene Amides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3476-3481 (2020)
National Research Council (Icb-Cnr)
Synthetic Lethality through the Lens of Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14151-14183 (2020)
Istituto Italiano Di Tecnologia
Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Xuzhou Medical University
The optimization of a novel selective antagonist for human M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shanghai Jiao Tong University School of Medicine
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shionogi
Sulfonamide antibiotics inhibit RNAi by binding to human Argonaute protein 2 PAZ.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Gifu University
An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
Jamia Millia Islamia (A Central University)
Synthesis and evaluation of HIF-1? inhibitory activities of novel panaxadiol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Yanbian University
Synthesis and biological activities of simplified aplysiatoxin analogs focused on the CH/? interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kyoto University
The food-grade antimicrobial xanthorrhizol targets the enoyl-ACP reductase (FabI) in Escherichia coli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Yonsei University
Design, synthesis, and computational validation of novel compounds selectively targeting HER2-expressing breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol University
Discovery of natural TRPA1 activators through pharmacophore-based virtual screening and a biological assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Kyoto University Shogoin-Kawaharacho
Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth invitro and invivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
East China University of Science and Technology
An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Bari "Aldo Moro
Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Key Laboratory of Technology of Drug Preparation (Zhengzhou University)
Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Oxford
Synthesis and evaluation of 3-(4-(phenoxymethyl)phenyl)propanoic acid and N-phenylbenzenesulfonamide derivatives as FFA4 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Dalian Institute of Chemical Physics
Structure-Activity Relationships for the Marine Natural Product Sintokamides: Androgen Receptor N-Terminus Antagonists of Interest for Treatment of Metastatic Castration-Resistant Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 797-813 (2021)
Bc Cancer
5-Phenyl-1,3,4-oxadiazol-2(3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12942-12956 (2020)
University College London
Recent advances in the medicinal chemistry of carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Isf College of Pharmacy
Pyridine alkaloids with activity in the central nervous system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Auckland
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Lupin
Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12707-12724 (2020)
Universit£
Proposed Allosteric Inhibitors Bind to the ATP Site of CK2?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12786-12798 (2020)
University of Cambridge
Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12957-12977 (2020)
The University of Texas Md Anderson Cancer Center
Discovery of a Beetroot Protease Inhibitor to Identify and Classify Plant-Derived Cystine Knot Peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3305-3314 (2020)
Medical University of Vienna
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15187-15217 (2020)
Soochow University
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Chinese Academy of Sciences
Design, synthesis and bioevaluation of inhibitors targeting HSP90-CDC37 protein-protein interaction based on a hydrophobic core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Design, synthesis, biological activity evaluation of 3-(4-phenyl-1H-imidazol-2-yl)-1H-pyrazole derivatives as potent JAK 2/3 and aurora A/B kinases multi-targeted inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Xuzhou Medical University
Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12574-12594 (2020)
Bayer
Therapeutic Targeting of MMP-12 for the Treatment of Chronic Obstructive Pulmonary Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12911-12920 (2020)
University of California Riverside
[1,2,4]Triazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12887-12910 (2020)
Janssen Pharmaceutica N. V.
Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13013-13030 (2020)
University of Cape Town
Identification, Structure-Activity Relationships of Marine-Derived Indolocarbazoles, and a Dual PKC?/? Inhibitor with Potent Antipancreatic Cancer Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12978-12991 (2020)
Zhejiang University
PROTACs suppression of GSK-3?, a crucial kinase in neurodegenerative diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 210: (2021)
China Pharmaceutical University
Synthesis and identification of a novel derivative of salidroside as a selective, competitive inhibitor of monoamine oxidase B with enhanced neuroprotective properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Fujian University of Traditional Chinese Medicine
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 31: (2021)
Bristol-Myers Squibb
Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sanofi
Pyrazol-1-yl-propanamides as SARD and Pan-Antagonists for the Treatment of Enzalutamide-Resistant Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12642-12665 (2020)
University of Tennessee Health Science Center
Structure-Activity Relationships of Noncovalent Immunoproteasome ?5i-Selective Dipeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13103-13123 (2020)
Weill Cornell Medicine
Cannabinoid Receptor Subtype 2 (CB2R) in a Multitarget Approach: Perspective of an Innovative Strategy in Cancer and Neurodegeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14448-14469 (2020)
Cnr-Institute of Crystallography
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Astrazeneca
Structural Basis of Nanomolar Inhibition of Tumor-Associated Carbonic Anhydrase IX: X-Ray Crystallographic and Inhibition Study of Lipophilic Inhibitors with Acetazolamide Backbone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13064-13075 (2020)
University of Florida
Structural Insights into the Recognition of Mono- and Diacetylated Histones by the ATAD2B Bromodomain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12799-12813 (2020)
Albany College of Pharmacy and Health Sciences
An update into the medicinal chemistry of translocator protein (TSPO) ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Pisa
Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II ? over ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12873-12886 (2020)
Istituto Italiano Di Tecnologia
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Shanghai Institute of Materia Medica
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Menoufia University
Targeting Atg4B for cancer therapy: Chemical mediators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Sichuan University
Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Institut Pasteur Korea
Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
The University of Tours
Design, synthesis and biological assessment of new selective COX-2 inhibitors including methyl sulfonyl moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Anadolu University
SP1-independent inhibition of FOXM1 by modified thiazolidinediones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Alberta
Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
A brief overview on recent advances in spiro[chromane-2,4'-piperidine]-4(3H)-one-functionalized compounds in medicinal chemistry research.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Kwazulu-Natal
Allosteric kidney-type glutaminase (GLS) inhibitors with a mercaptoethyl linker.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Johns Hopkins University
Pyrroformyl-containing 2,4-diaminopyrimidine derivatives as a new optimization strategy of ALK inhibitors combating mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Beijing Institute of Technology
Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Synthesis, biological evaluation and in silico modeling of novel pan-genotypic NS5A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chemical Diversity Research Institute
Rational design of cell-permeable cyclic peptides containing a d-Pro-l-Pro motif.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The Ohio State University
Small-molecule active pharmaceutical ingredients of approved cancer therapeutics inhibit human aspartate/asparagine-?-hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Oxford
Discovery of heterocycle-containing ?-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Shanghai Jiao Tong University
New series of isoxazole derivatives targeting EGFR-TK: Synthesis, molecular modeling and antitumor evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Mansoura University
Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Northeastern University
Next generation quorum sensing inhibitors: Accounts on structure activity relationship studies and biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Dnyanprassarak Mandal'S College and Research Centre
Optimization of linear and cyclic peptide inhibitors of KEAP1-NRF2 protein-protein interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Irbm
Design and synthesis of new disubstituted benzoxazolone derivatives that act as iNOS inhibitors with potent anti-inflammatory activity against LPS-induced acute lung injury (ALI).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shanxi Medical University
Discovery of DS34942424: An orally potent analgesic without mu opioid receptor agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Daiichi Sankyo
Structure-activity relationship studies of phenothiazine derivatives as a new class of ferroptosis inhibitors together with the therapeutic effect in an ischemic stroke model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Sichuan University
Discovery of EST73502, a Dual ?-Opioid Receptor Agonist and ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 15508-15526 (2020)
Esteve Pharmaceuticals
Backbone Cyclization Turns a Venom Peptide into a Stable and Equipotent Ligand at Both Muscle and Neuronal Nicotinic Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12682-12692 (2020)
Universit£
Discovery of Tricyclic Xanthines as Agonists of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2024-2031 (2020)
University of Bonn
Discovery of Dotinurad (FYU-981), a New Phenol Derivative with Highly Potent Uric Acid Lowering Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2017-2023 (2020)
Fuji Yakuhin
Brain Penetrable Inhibitors of Ceramide Galactosyltransferase for the Treatment of Lysosomal Storage Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2010-2016 (2020)
Sanofi R&D
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2002-2009 (2020)
Janssen Research & Development
De-risking Drug Discovery of Intracellular Targeting Peptides: Screening Strategies to Eliminate False-Positive Hits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1993-2001 (2020)
Msd
Discovery of a Cyclic Choline Analog That Inhibits Anaerobic Choline Metabolism by Human Gut Bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1980-1985 (2020)
Harvard University
Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1965-1972 (2020)
Purdue University
Exception That Proves the Rule: Investigation of Privileged Stereochemistry in Designing Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1956-1964 (2020)
National Institute On Drug Abuse-Intramural Research Program
Mechanism-Based Design of 3-Amino-4-Halocyclopentenecarboxylic Acids as Inactivators of GABA Aminotransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1949-1955 (2020)
Northwestern University
Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1935-1941 (2020)
National Institute of Diabetes and Digestive and Kidney Disease
Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1928-1934 (2020)
Rwth Aachen University
Gibberellin JRA-003: A Selective Inhibitor of Nuclear Translocation of IKK?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1913-1918 (2020)
University of Michigan
Discovery of Selective, Covalent FGFR4 Inhibitors with Antitumor Activity in Models of Hepatocellular Carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1899-1904 (2020)
Bristol Myers Squibb
Dethioacylation by Sirtuins 1-3: Considerations for Drug Design Using Mechanism-Based Sirtuin Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1886-1892 (2020)
University of Copenhagen
Harmaline Analogs as Substrate-Selective Cyclooxygenase-2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1881-1885 (2020)
Vanderbilt University School of Medicine
Discovery and Evaluation of Pyrazolo[3,4-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1863-1868 (2020)
Hubei Bio-Pharmaceutical Industrial Technological Institute
Synthesis and SAR Studies of 1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1848-1854 (2020)
University of Nebraska Medical Center
Inhibition of Macrophage Migration Inhibitory Factor by a Chimera of Two Allosteric Binders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1843-1847 (2020)
L2 Diagnostics
Targeted Detection of Cyclooxygenase-1 in Ovarian Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1837-1842 (2020)
Vanderbilt University School of Medicine
Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-X![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1829-1836 (2020)
Abbvie
The Resurrection of Phenotypic Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1820-1828 (2020)
Temple University
Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1810-1819 (2020)
Therapeutics
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1799-1809 (2020)
University of California, Los Angeles
Selective DYRK1A Inhibitor for the Treatment of Neurodegenerative Diseases: Alzheimer, Parkinson, Huntington, and Down Syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1795-1796 (2020)
Usona Institute
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Glaxosmithkline
Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Universit£
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14562-14575 (2020)
Cullgen (Shanghai)
Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14382-14403 (2020)
China Pharmaceutical University
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12725-12747 (2020)
Pfizer
Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14502-14521 (2020)
TBA
Design, Synthesis, and Pharmacological Evaluation of Analogues Derived from the PLEV Tetrapeptide as Protein-Protein Interaction Modulators of Voltage-Gated Sodium Channel 1.6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11522-11547 (2020)
TBA
Protease activated receptor 4 (PAR4) antagonists: Research progress on small molecules in the field of antiplatelet agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Synthesis, binding, and functional properties of tetrahydroisoquinolino-2-alkyl phenones as selective ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Guangdong Medical University
Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
China Pharmaceutical University
Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
University of Pisa
Current development of CBP/p300 inhibitors in the last decade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Zhengzhou University
Design, synthesis and biological evaluation of novel c-Met/HDAC dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5-Lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11498-11521 (2020)
Goethe-University of Frankfurt
Design, synthesis and biological evaluation of novel naphthoquinone-4-aminobenzensulfonamide/carboxamide derivatives as proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Ege University
Design, synthesis and structure-activity relationship study of novel urea compounds as FGFR1 inhibitors to treat metastatic triple-negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Texas Tech University Health Sciences Center
Rapid discovery of a selective butyrylcholinesterase inhibitor using structure-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
The University of Queensland
Novel 3-substituted coumarins as selective human carbonic anhydrase IX and XII inhibitors: Synthesis, biological and molecular dynamics analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Egyptian Russian University
The discovery of potent small molecule activators of human STING.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Curadev Pharma
Crystal structure of Leishmania mexicana cysteine protease B in complex with a high-affinity azadipeptide nitrile inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of S£O Paulo
hDM2 protein-binding peptides screened from stapled ?-helical peptide phage display libraries with different types of staple linkers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo Institute of Technology
Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Squaric acid analogues in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Palacky University Olomouc
Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Scripps Research
Selective targeting of the ?C and DFG-out pocket in p38 MAPK.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Johann Wolfgang Goethe University
Design, syntheses and evaluations of novel indole derivatives as orally selective estrogen receptor degraders (SERD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Luoxin Pharmaceutical (Shanghai) Co.
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14522-14529 (2020)
Fount Therapeutics
Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Meroterpenoids produced by fungi: Occurrence, structural diversity, biological activities, and their molecular targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Guangzhou University of Chinese Medicine
Structure activity relationship of novel antiviral nucleosides against Enterovirus A71.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
National Institute of Diabetes and Digestive and Kidney Disease
Development of a Potent and Specific FGFR4 Inhibitor for the Treatment of Hepatocellular Carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11484-11497 (2020)
University of Southern California
Biological Evaluation of Selected Flavonoids as Inhibitors of MNKs Targeting Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2967-2975 (2020)
The Chinese University of Hong Kong (Shenzhen)
Piperlonguminine and Piperine Analogues as TrxR Inhibitors that Promote ROS and Autophagy and Regulate p38 and Akt/mTOR Signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3041-3049 (2020)
Nantong University
Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14470-14501 (2020)
Zhejiang University
New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Palack£
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12083-12099 (2020)
Shandong University
Effective anti-aromatase therapy to battle against estrogen-mediated breast cancer: Comparative SAR/QSAR assessment on steroidal aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Jadavpur University
Design and synthesis of 3-(4-pyridyl)-5-(4-sulfamido-phenyl)-1,2,4-oxadiazole derivatives as novel GSK-3? inhibitors and evaluation of their potential as multifunctional anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Anhui Medical University
Automated Design of Macrocycles for Therapeutic Applications: From Small Molecules to Peptides and Proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12100-12115 (2020)
Schrodinger
Synthesis and structure-activity relationship studies of LLY-507 analogues as SMYD2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Key Laboratory of Molecule Synthesis and Function Discovery (Fujian Province University)
Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
University of Auckland
Modern trends in diuretics development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
National University of Pharmacy
Design, synthesis and biological evaluation of indanone-chalcone hybrids as potent and selective hCES2A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 209: (2021)
Shanghai University of Traditional Chinese Medicine
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Indian Institute of Technology (Banaras Hindu University)
Druggable targets from coronaviruses for designing new antiviral drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Federal University of Alagoas
N-phenyl ureidobenzenesulfonates, a novel class of promising human dihydroorotate dehydrogenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universit£
Design and synthesis of Coenzyme A analogues as Aurora kinase A inhibitors: An exploration of the roles of the pyrophosphate and pantetheine moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University College London
Preparation and evaluation of soluble epoxide hydrolase inhibitors with improved physical properties and potencies for treating diabetic neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Synthia
Design and synthesis of novel methoxypyridine-derived gamma-secretase modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of California
Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universit£T M£Nster
Discovery and structure activity relationships of 7-benzyl triazolopyridines as stable, selective, and reversible inhibitors of myeloperoxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Bristol Myers Squibb
Analogs of nitrofuran antibiotics are potent GroEL/ES inhibitor pro-drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Indiana University School of Medicine
Dual antagonists of ?5?1/?v?1 integrin for airway hyperresponsiveness.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of California San Francisco
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Pharmaceutical Research & Development
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
South China Agricultural University
The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Pisa
Ahp-Cyclodepsipeptides as tunable inhibitors of human neutrophil elastase and kallikrein 7: Total synthesis of tutuilamide A, serine protease selectivity profile and comparison with lyngbyastatin 7.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Florida
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)