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Decoding the Papain Inhibitor from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2983-2995 (2020)
University of Applied Sciences of Darmstadt
Study of triaryl-based sulfamic acid derivatives as HPTP? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Engineering Research Center For The Emergency Strategic Drug
Studies on fragment-based design of allosteric inhibitors of human factor XIa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Virginia Commonwealth University
Design, synthesis and biological evaluation of vortioxetine derivatives as new COX-1/2 inhibitors in human monocytes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Piemonte Orientale
COVID-19 therapy: What weapons do we bring into battle?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universidade De Pernambuco
Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Qilu University of Technology (Shandong Academy of Sciences)
Discovery and Optimization of Non-bile Acid FXR Agonists as Preclinical Candidates for the Treatment of Nonalcoholic Steatohepatitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12748-12772 (2020)
Chinese Academy of Sciences
Rapid Solid-Phase Construction of Serine Hydrolase Probes Results in Selective Activity-Based Probes for Acyl Protein Thioesterases-1/2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11845-11853 (2020)
Ku Leuven
Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2950-2959 (2020)
Sichuan University
Discovery of novel quinazoline derivatives as potent PI3K? inhibitors with high selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
China Pharmaceutical University
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Shanghai Jiao Tong University
Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Cadila Healthcare
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
A guanidinium-based inhibitor of a type I isopentenyl diphosphate isomerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of British Columbia
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11045-11053 (2020)
Philipps-University
Synthesis, biological evaluation, in silico modeling and crystallization of novel small monocationic molecules with potent antiproliferative activity by dual mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Campus Cartuja S/N. University of Granada
Synthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sumitomo Dainippon Pharma.
Natural and Semisynthetic Chalcones as Dual FLT3 and Microtubule Polymerization Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 3111-3121 (2020)
Lahore University of Management Sciences
Targeting the aryl hydrocarbon receptor with a novel set of triarylmethanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Universitat De Val£Ncia. Av. Vicente Andr£S Estell£S
An electrophilic warhead library for mapping the reactivity and accessibility of tractable cysteines in protein kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Research Centre For Natural Sciences
Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Groningen
Discovery of novel VX-809 hybrid derivatives as F508del-CFTR correctors by molecular modeling, chemical synthesis and biological assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Genoa
Potent and Selective Human Prostaglandin F (FP) Receptor Antagonist (BAY-6672) for the Treatment of Idiopathic Pulmonary Fibrosis (IPF).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11639-11662 (2020)
Bayer
Research progress of mTOR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Jilin University
Cyclic tailor-made amino acids in the design of modern pharmaceuticals.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Nanjing Forestry University
Discovery of novel liver X receptor inverse agonists as lipogenesis inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Sun Yat-Sen University
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Korea Institute of Science & Technology (Kist)
Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Southern Medical University
Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Shenyang Pharmaceutical University
Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11854-11881 (2020)
Bayer
Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Nodthera
Discovery of Small-Molecule Inhibitors of Receptor Activator of Nuclear Factor-?B Ligand with a Superior Therapeutic Index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12043-12059 (2020)
Agricultural University of Athens
Bioactivity-Guided Discovery of Human Carboxylesterase Inhibitors from the Roots of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2940-2949 (2020)
Chinese Academy of Medical Sciences and Peking Union Medical College
Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
China Pharmaceutical University
Combined MD/QTAIM techniques to evaluate ligand-receptor interactions. Scope and limitations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Universidad Nacional De San Luis
A dual-acting 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Jagiellonian University Medical College
Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Chinese Academy of Sciences
The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Southern Medical University
Design, synthesis and biological evaluation of novel heptamethine cyanine dye-erlotinib conjugates as antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
National Institute On Drug Abuse - Intramural Research Program
Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Cairo University
Advances of CCR5 antagonists: From small molecules to macromolecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Chengdu University
First Structure-Activity Relationship Study of Potent BLT2 Agonists as Potential Wound-Healing Promoters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11548-11572 (2020)
Fraunhofer Ime
Identification, Structure-Activity Relationship, and Biological Characterization of 2,3,4,5-Tetrahydro-1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11169-11194 (2020)
D3-Pharmachemistry
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1678-1687 (2020)
Convergence Pharmaceuticals
Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1773-1779 (2020)
Vanderbilt University
Quinoline-Pyrazole Scaffold as a Novel Ligand of Galectin-3 and Suppressor of TREM2 Signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1759-1765 (2020)
Stanford University School of Medicine
Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1751-1758 (2020)
Princ
Facile Synthesis of Aminomethyl Phosphinate Esters as Serine Protease Inhibitors with Primed Site Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1739-1744 (2020)
Ku Leuven
Insights into the Molecular Determinants Involved in Urocontrin and Urocontrin A Action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1717-1722 (2020)
Universit£
A Phosphoramidate Strategy Enables Membrane Permeability of a Non-nucleotide Inhibitor of the Prolyl Isomerase Pin1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1704-1710 (2020)
University of California San Francisco
Identification of Novel Rho-Kinase-II Inhibitors with Vasodilatory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1694-1703 (2020)
Banasthali Vidyapith
Allosteric Modulation of Protein Arginine Methyltransferase 5 (PRMT5).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1688-1693 (2020)
Merck
Novel 4-Heteroarylcarbonyl-N-(phenyl or heteroaryl) Piperidine-1-carboxamides as Tankyrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1676-1677 (2020)
Lauren Mccallister
Novel Heteroaromatic Compounds as Vanin Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1674-1675 (2020)
Lauren Mccallister
Novel Cyclic Tetramer Compounds as PCSK9 Inhibitors for Treating Metabolic Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1671-1673 (2020)
Lauren Mccallister
2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Korea Institute of Science & Technology (Kist)
Design, synthesis and molecular docking study of ?-triazolylsialosides as non-hydrolyzable and potent CD22 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Academia Sinica
A comprehensive review of monoamine oxidase inhibitors as Anti-Alzheimer's disease agents: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Jamia Millia Islamia
The components and activities analysis of a novel anticoagulant candidate dHG-5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
University of Chinese Academy of Sciences
Discovery of methoxy-naphthyl linked N-(1-benzylpiperidine) benzamide as a blood-brain permeable dual inhibitor of acetylcholinesterase and butyrylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Csir-India
The synthesis and anti-tumour properties of novel 4-substituted phthalazinones as Aurora B kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Lanzhou University
Lycosquarrines A-R, ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2831-2843 (2020)
China Pharmaceutical University
7-Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11920-11933 (2020)
University of Groningen
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12116-12127 (2020)
The University of Sydney
Understanding and Improving the Membrane Permeability of VH032-Based PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1732-1738 (2020)
University of California Santa Cruz
4-Amino-1,2,4-triazole-3-thione-derived Schiff bases as metallo-?-lactamase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Universit£
Di-bromo-Based Small-Molecule Inhibitors of the PD-1/PD-L1 Immune Checkpoint.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11271-11285 (2020)
Jagiellonian University
Discovery of a Novel Inhibitor of Coronavirus 3CL Protease as a Clinical Candidate for the Potential Treatment of COVID-19.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
bioRxiv (2020)
Pfizer
Mycophenolic anilides as broad specificity inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Houston
Structural basis for producing selective MAP2K7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Osaka Prefecture University
Discovery of 1-(1H-indazol-4-yl)-3-((1-phenyl-1H-pyrazol-5-yl)methyl) ureas as potent and thermoneutral TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Seoul National University
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11725-11755 (2020)
Tu Dortmund University
Tranylcypromine Based Lysine-Specific Demethylase 1 Inhibitor: Summary and Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14197-14215 (2020)
Key Laboratory of Henan Provinc
Aryloxy Diester Phosphonamidate Prodrugs of Phosphoantigens (ProPAgens) as Potent Activators of V?9/V?2 T-Cell Immune Responses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11258-11270 (2020)
Cardiff University
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12542-12573 (2020)
Novartis Institutes For Biomedical Research
Therapeutic potential of uracil and its derivatives in countering pathogenic and physiological disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Pondicherry University
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Peking Union Medical College and Chinese Academy of Medical Sciences
Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Directing Drugs to Bugs: Antibiotic-Carbohydrate Conjugates Targeting Biofilm-Associated Lectins of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11707-11724 (2020)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11012-11033 (2020)
West China Hospital of Sichuan University
Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Sapienza University of Rome
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Faculty of Science and The University of Sydney
Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Chinese Academy of Medical Sciences & Peking Union Medical College
Structure-activity relationships of GPX4 inhibitor warheads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Institute of Mit and Harvard
Structure-activity relationship study of tryptophan-based butyrylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Ljubljana
Structure-activity relationship studies and bioactivity evaluation of 1,2,3-triazole containing analogues as a selective sphingosine kinase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Washington University School of Medicine
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Recent developments of small molecules with anti-inflammatory activities for the treatment of acute lung injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Zhejiang University
Bioactive pyrrole-based compounds with target selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Palermo
Design, synthesis and evaluation of novel indirubin-based N-hydroxybenzamides, N-hydroxypropenamides and N-hydroxyheptanamides as histone deacetylase inhibitors and antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Hanoi University of Pharmacy
Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14357-14381 (2020)
Genentech
Repurposing of Drugs-The Ketamine Story.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13514-13525 (2020)
University of Houston
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14228-14242 (2020)
University of Toyama
New cannabinoid receptor antagonists as pharmacological tool.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Instituto De Qu£Mica M£Dica (Csic)
Synthesis and evaluation of 17?-triazolyl and 9?-cyano derivatives of estradiol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Marquette University
Design, synthesis and biological evaluation of 4-aryl-5-aminoalkyl-thiazole-2-amines derivatives as ROCK II inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Yantai University
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jiangxi Science & Technology Normal University
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Zhejiang University
SAR study of bisamides as cyclophilin a inhibitors for the development of host-targeting therapy for hepatitis C virus infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chonnam National University
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Takeda Pharmaceuticals International
New drug approvals for 2019: Synthesis and clinical applications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Zhengzhou University
Discovery of AZD9833, a Potent and Orally Bioavailable Selective Estrogen Receptor Degrader and Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14530-14559 (2020)
Astrazeneca
Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13578-13594 (2020)
TBA
Discovery of PF-06835919: A Potent Inhibitor of Ketohexokinase (KHK) for the Treatment of Metabolic Disorders Driven by the Overconsumption of Fructose.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13546-13560 (2020)
Pfizer
Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11972-11989 (2020)
Max Planck Institute of Molecular Physiology
Anti-glioma effects of 2-aminothiophene-3-carboxamide derivatives, ANO1 channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Korea University
Discovery of 9-Cyclopropylethynyl-2-((![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13526-13545 (2020)
Galapagos
Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11149-11168 (2020)
China Pharmaceutical University
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10984-11011 (2020)
National Institutes of Health
Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12929-12941 (2020)
Vrije Universiteit Brussel
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1-13)-NH![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10782-10795 (2020)
University of Ferrara
Design and Identification of a GPR40 Full Agonist (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10352-10379 (2020)
Takeda Pharmaceutical
Current development of CFTR potentiators in the last decade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
University of Palermo
Structure-activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Central China Normal University
Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Soochow University
2-substituted benzothiazoles as antiproliferative agents: Novel insights on structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
"G. D'Annunzio" University of Chieti-Pescara
Covalent inhibitors of GAPDH: From unspecific warheads to selective compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Universit£
Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jiangnan University
Discovery of ONO-8590580: A novel, potent and selective GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Charles River Discovery Research Services
Fragment-based lead discovery of a novel class of small molecule antagonists of neuropeptide B/W receptor subtype 1 (GPR7).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3K? and mTOR Kinases for the Treatment of Solid Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11121-11130 (2020)
Sphaera Pharma
Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10829-10854 (2020)
Shandong University
Synthesis and Evaluation of 4-Hydroxycoumarin Imines as Inhibitors of Class II Myosins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11131-11148 (2020)
University of Nevada
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sichuan University
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb
Synthesis and SAR of a series of mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Structure-based amelioration of PXR transactivation in a novel series of macrocyclic allosteric inhibitors of HIV-1 integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb Research and Development
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11085-11099 (2020)
University of Illinois At Chicago
DPAGT1 Inhibitors of Capuramycin Analogues and Their Antimigratory Activities of Solid Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10855-10878 (2020)
University of Tennessee Health Science Center
Catch and Anchor Approach To Combat Both Toxicity and Longevity of Botulinum Toxin A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11100-11120 (2020)
Boston University School of Medicine
Photohormones Enable Optical Control of the Peroxisome Proliferator-Activated Receptor ? (PPAR?).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10908-10920 (2020)
New York University
Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Lanzhou University
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Sapienza Universit£
Factor XII/XIIa inhibitors: Their discovery, development, and potential indications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Namur
Targeting histone demethylase KDM5B for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Zhengzhou University
Synthesis of biphenyl oxazole derivatives via Suzuki coupling and biological evaluations as nucleotide pyrophosphatase/phosphodiesterase-1 and -3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Quaid-I-Azam University
FabI (enoyl acyl carrier protein reductase) - A potential broad spectrum therapeutic target and its inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
National Institute of Pharmaceutical Education and Research (NIPER)
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
Goethe University Frankfurt
Discovery of Novel pERK1/2- or ?-Arrestin-Preferring 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10946-10971 (2020)
Jagiellonian University Medical College
Discovery of 4-methyl-N-(4-((4-methylpiperazin- 1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-oxy)benzamide as a potent inhibitor of RET and its gatekeeper mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Xiamen University
Rational design of new multitarget histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Jagiellonian University Medical College
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as ?7 nicotinic receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Peking University
7-Azaindolequinuclidinones (7-AIQD): A novel class of cannabinoid 1 (CB1) and cannabinoid 2 (CB2) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Arkansas For Medical Sciences
Tricyclic sulfones as potent, selective and efficacious ROR?t inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Structure-based drug optimization and biological evaluation of tetrahydroquinolin derivatives as selective and potent CBP bromodomain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Chinese Academy of Sciences
Development of Nonpeptidic Inverse Agonists of the Ghrelin Receptor (GHSR) Based on the 1,2,4-Triazole Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10796-10815 (2020)
Univ Montpellier
Bifunctional and Unusual Amino Acid ?- or ?-Ester Prodrugs of Nucleoside Analogues for Improved Affinity to ATB![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10816-10828 (2020)
Jiangxi University of Traditional Chinese Medicine
Highly Selective Sub-Nanomolar Cathepsin S Inhibitors by Merging Fragment Binders with Nitrile Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11801-11808 (2020)
Grunenthal
Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2727-2736 (2020)
University of Naples Federico Ii
Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11054-11084 (2020)
Albany College of Pharmacy and Health Sciences
Isoquinolinone derivatives as potent CNS multi-receptor D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Jiangsu Ocean University
3-Methylthiazolo[3,2-a]benzimidazole-benzenesulfonamide conjugates as novel carbonic anhydrase inhibitors endowed with anticancer activity: Design, synthesis, biological and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Jouf University
Insights of tankyrases: A novel target for drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Srinath College of Pharmacy
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Discovery of an Inhibitor for the TREK-1 Channel Targeting an Intermediate Transition State of Channel Gating.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10972-10983 (2020)
Shanghai Institute of Materia Medica
N-terminal modified cyclopeptidic mimetics of Apollo![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127401 (2020)
China Pharmaceutical University
Recent advances in epigenetic proteolysis targeting chimeras (Epi-PROTACs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
"Sapienza" University of Rome
Aldose reductase and protein tyrosine phosphatase 1B inhibitors as a promising therapeutic approach for diabetes mellitus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Aristotle University of Thessaloniki
Current advances in Vibrio harveyi quorum sensing as drug discovery targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Zhejiang University
Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and trytophan 2,3-dioxygenase (TDO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Sichuan University
Computational methods-guided design of modulators targeting protein-protein interactions (PPIs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Shanghai Jiao Tong University
N-Substituted piperazine derivatives as potential multitarget agents acting on histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Pharmacological Analysis of the Anti-inflammatory and Antiallodynic Effects of Zinagrandinolide E from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 84: 713-723 (2021)
Universidad Nacional Aut£Noma De M£Xico
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 14243-14275 (2020)
Endotherm
Anti-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13330-13354 (2020)
Commonwealth Scientific and Industrial Research Organization
Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
China Pharmaceutical University
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13228-13257 (2020)
China Pharmaceutical University
Bioinspired Hybrid Fluorescent Ligands for the FK1 Domain of FKBP52.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10330-10338 (2020)
Universit£
Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10433-10459 (2020)
Oric Pharmaceuticals
Discovery of Potent and Selective PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11235-11257 (2020)
Arcus Biosciences
Discovery of the first potent and selective ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 208: (2020)
University of Strathclyde
Neuroprotective effects of prenylated flavanones isolated from Dalea species, in vitro and in silico studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Ciudad Universitaria
PROTACs: New method to degrade transcription regulating proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 207: (2020)
Shenyang Pharmaceutical University
Identification of the subtype-selective Sirt5 inhibitor balsalazide through systematic SAR analysis and rationalization via theoretical investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Ludwig-Maximilians University
Half-life extension of peptidic APJ agonists by N-terminal lipid conjugation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127499 (2020)
Amgen
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9856-9875 (2020)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127508 (2020)
Chinese Academy of Medical Sciences and Peking Union Medical College
Structure activity relationship exploration of 5-hydroxy-2-(3-phenylpropyl)chromones as a unique 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127511 (2020)
Kalamazoo College
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Med Res Rev (2020)
University of Bonn
Development of Novel AKR1C3 Inhibitors as New Potential Treatment for Castration-Resistant Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10396-10411 (2020)
Gifu Pharmaceutical University
Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
China Pharmaceutical University
Modulation of the Innate Immune Response by Targeting Toll-like Receptors: A Perspective on Their Agonists and Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13466-13513 (2020)
University of Siena
Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13205-13227 (2020)
South China Agricultural University
Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9660-9671 (2020)
The Scripps Research Institute
Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11286-11301 (2020)
Sun Yat-Sen University
Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Ku Leuven
Novel Blocker of Onco SK3 Channels Derived from Scorpion Toxin Tamapin and Active against Migration of Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1627-1633 (2020)
Universidad Nacional Aut£Noma De M£Xico
Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1620-1626 (2020)
University of Sussex
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1588-1597 (2020)
Genentech
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1581-1587 (2020)
Glaxosmithkline Medicines Research Centre
Hitting a Moving Target: Simulation and Crystallography Study of ATAD2 Bromodomain Blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1573-1580 (2020)
University of Zurich
Identification and Development of 1,4-Diaryl-1,2,3-triazolo-Based Ureas as Novel FLT3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1567-1572 (2020)
Jinan University
Virtual Screening for Ligand Discovery at the ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1555-1561 (2020)
Harvard Medical School
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1548-1554 (2020)
Merck
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1535-1538 (2020)
The University of Notre Dame
Elucidation of Mechanism for Ligand Efficacy at Leukotriene B![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1529-1534 (2020)
Incerebro
Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10263-10286 (2020)
University of Michigan
Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
University of Michigan
Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jiangsu Ocean University
Biological evaluation and SAR analysis of novel covalent inhibitors against fructose-1,6-bisphosphatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Anhui University of Technology
Synthesis and activity of isoleucine sulfonamide derivatives as novel botulinum neurotoxin serotype A light chain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
California State University
Boronic acid-based arginase inhibitors in cancer immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Oncoarendi Therapeutics
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Research Centre
The neuronal calcium ion channel activity of constrained analogues of MONIRO-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The University of Queensland
Identification of the first noncompetitive SARM1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Umass Medical School
Suramin derivatives play an important role in blocking the interaction between FGF1 and FGFRD2 to inhibit cell proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
National Tsing Hua University
Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of RET: Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
University of Arkansas For Medical Sciences
From methylene bridged diindole to carbonyl linked benzimidazoleindole: Development of potent and metabolically stable PCSK9 modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
University of Wisconsin-Madison
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Nankai University
Synthesis and in vitro evaluation of vanillin derivatives as multi-target therapeutics for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127505 (2020)
Robert Gordon University
Discovery of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10307-10329 (2020)
Chinese Academy of Medical Sciences and Peking Union Medical College
The role of imidazole and benzimidazole heterocycles in Chagas disease: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Universidad De Navarra
Isolation, reactivity, pharmacological activities and total synthesis of hispanolone and structurally related diterpenes from Labiatae plants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Csic
Synthesis and Anti-HCV Activity of Sugar-Modified Guanosine Analogues: Discovery of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10380-10395 (2020)
Janssen Biopharma
Rational Design of Suprastat: A Novel Selective Histone Deacetylase 6 Inhibitor with the Ability to Potentiate Immunotherapy in Melanoma Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10246-10262 (2020)
The George Washington University
Design, Synthesis, and Pharmacological Characterization of Heterobivalent Ligands for the Putative 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9928-9949 (2020)
University of Copenhagen
Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 206: (2020)
Xiamen University
Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
University of Milan
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10879-10896 (2020)
Pfizer
Rational Design and Synthesis of Methyl-?-d-galactomalonyl Phenyl Esters as Potent Galectin-8![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11573-11584 (2020)
Griffith University
Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127496 (2020)
Crinetics Pharmaceuticals
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127474 (2020)
Bristol Myers Squibb
Opportunities for Tapping into Three-Dimensional Chemical Space through a Quaternary Carbon.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13291-13315 (2020)
St. John'S University
The Essential Medicinal Chemistry of Cannabidiol (CBD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12137-12155 (2020)
University of Minnesota
Discovery of Proteolysis-Targeting Chimera Molecules that Selectively Degrade the IRAK3 Pseudokinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10460-10473 (2020)
Astrazeneca
Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10339-10351 (2020)
Leipzig University
Identification of SARS-CoV-2 3CL Protease Inhibitors by a Quantitative High-throughput Screening.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
bioRxiv (2020)
National Institutes of Health
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Concept Life Sciences
Synthesis, crystal structure and biological activity of novel analogues of tricyclic drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127493 (2020)
Polish Academy of Sciences
Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127495 (2020)
Bristol Myers Squibb
Recent advancements in the development of bioactive pyrazoline derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Isf College of Pharmacy
Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9154-9167 (2020)
Guangxi Normal University
Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9828-9837 (2020)
Sun Yat-Sen University
Hydroxamic acid hybrids as the potential anticancer agents: An Overview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Huaihe Hospital of Henan University
Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Shenzhen Technology University
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9020-9044 (2020)
Gsk
Discovery of Clinical Candidate (5-(3-(4-Chlorophenoxy)prop-1-yn-1-yl)-3-hydroxypicolinoyl)glycine, an Orally Bioavailable Prolyl Hydroxylase Inhibitor for the Treatment of Anemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10045-10060 (2020)
China Pharmaceutical University
MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9695-9704 (2020)
Stanford University School of Medicine
Exploration of Alternative Scaffolds for P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9563-9589 (2020)
National Institute of Diabetes and Digestive and Kidney Diseases
Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9540-9562 (2020)
Purdue University
Structure-Activity Relationship Studies of ?-Ketoamides as Inhibitors of the Phospholipase A and Acyltransferase Enzyme Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9340-9359 (2020)
Leiden University & Oncode Institute
Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10030-10044 (2020)
China Pharmaceutical University
Non-naturally Occurring Regio Isomer of Lysophosphatidylserine Exhibits Potent Agonistic Activity toward G Protein-Coupled Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9990-10029 (2020)
The University of Tokyo
Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9888-9911 (2020)
University of Texas Md Anderson Cancer Center
Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9672-9694 (2020)
University of Salerno
Screening of a Custom-Designed Acid Fragment Library Identifies 1-Phenylpyrroles and 1-Phenylpyrrolidines as Inhibitors of Notum Carboxylesterase Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9464-9483 (2020)
University College London
Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9181-9196 (2020)
Janssen Research & Development
Advances in the Design of Genuine Human Tyrosinase Inhibitors for Targeting Melanogenesis and Related Pigmentations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13428-13443 (2020)
Universit£
Superior Pyrimidine Derivatives as Selective ABCG2 Inhibitors and Broad-Spectrum ABCB1, ABCC1, and ABCG2 Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10412-10432 (2020)
Rheinische Friedrich-Wilhelms-University Bonn
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13561-13577 (2020)
Pfizer
Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9773-9786 (2020)
Ut Southwestern Medical Center
Structural Analysis of VDR Complex with ZK168281 Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9457-9463 (2020)
Institut De G£N£Tique Et De Biologie Mol£Culaire Et Cellulaire (Igbmc)
Highly Potent and Selective ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9212-9227 (2020)
Purdue University
2-Oxaadamant-1-yl Ureas as Soluble Epoxide Hydrolase Inhibitors: ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9237-9257 (2020)
Universitat De Barcelona
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10061-10085 (2020)
Ontario Institute For Cancer Research
Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9977-9989 (2020)
Icahn School of Medicine At Mount Sinai
Rational Design and Evaluation of 6-(Pyrimidin-2-ylamino)-3,4-dihydroquinoxalin-2(1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9787-9802 (2020)
Chinese Academy of Sciences
Discovery of Potent Small-Molecule SIRT6 Activators: Structure-Activity Relationship and Anti-Pancreatic Ductal Adenocarcinoma Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10474-10495 (2020)
Sichuan University
DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10224-10234 (2020)
Goethe-University Frankfurt
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9705-9730 (2020)
Astrazeneca
Usnic Acid Conjugates with Monoterpenoids as Potent Tyrosyl-DNA Phosphodiesterase 1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2320-2329 (2020)
TBA
Allicin, a Potent New Ornithine Decarboxylase Inhibitor in Neuroblastoma Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2518-2527 (2020)
Michigan State University
Targeting Protein Folding: A Novel Approach for the Treatment of Pathogenic Bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13355-13388 (2020)
University of W£Rzburg
Targeting Metabolism of Extracellular Nucleotides via Inhibition of Ectonucleotidases CD73 and CD39.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13444-13465 (2020)
Arcus Biosciences
Generation of Leads for ?-Secretase Modulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8216-8230 (2020)
Merck
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8276-8295 (2020)
Genomics Institute of The Novartis Research Foundation
Design, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Southwest Jiaotong University
Heteroarylureas with fused bicyclic diamine cores as inhibitors of fatty acid amide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Pharmaceutical Companies of Johnson & Johnson
Synthesis and biological evaluation of thiazole derivatives on basic defects underlying cystic fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127473 (2020)
Rccs Istituto Giannina Gaslini
Discovery of noscapine derivatives as potential ?-tubulin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127489 (2020)
Shahid Beheshti University
New coumarin-benzotriazole based hybrid molecules as inhibitors of acetylcholinesterase and amyloid aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Guru Nanak Dev University
Discovery of USP7 small-molecule allosteric inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Medivir
Discovery of novel histone lysine methyltransferase G9a/GLP (EHMT2/1) inhibitors: Design, synthesis, and structure-activity relationships of 2,4-diamino-6-methylpyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Daiichi Sankyo
Modification of imidazothiazole derivatives gives promising activity in B-Raf kinase enzyme inhibition; synthesis, in vitro studies and molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Science & Technology (Ust)
The design of a novel near-infrared fluorescent HDAC inhibitor and image of tumor cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
East China Normal University
An investigative study of antitumor properties of a novel thiazolo[4,5-d]pyrimidine small molecule revealing superior antitumor activity with CDK1 selectivity and potent pro-apoptotic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Egyptian Russian University
The design, synthesis and evaluation of 2-aminobenzoxazole analogues as potent and orally efficacious ChemR23 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kyowa Kirin
An insight on medicinal attributes of 1,2,4-triazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Kurukshetra University
Potential treatment methods targeting 2019-nCoV infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Southern Medical University
Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Soochow University
Discovery of a d-pro-lys peptidomimetic inhibitor of MMP9: Addressing the gelatinase selectivity beyond S1' subsite.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127467 (2020)
University of Florence
Integrating DNA-encoded chemical libraries with virtual combinatorial library screening: Optimizing a PARP10 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Mcdaniel College
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Bonn
Discovery of novel urea-diarylpyrazole hybrids as dual COX-2/sEH inhibitors with improved anti-inflammatory activity and highly reduced cardiovascular risks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Beni-Suef University
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (ROR?/RORc) inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
An orally available inverse agonist of estrogen-related receptor gamma showed expanded efficacy for the radioiodine therapy of poorly differentiated thyroid cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Daegu-Gyeongbuk Medical Innovation Foundation
Research advances on selective phosphatidylinositol 3 kinase ? (PI3K?) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Xi'An Jiaotong University
Identification of free fatty acid receptor 2 agonists using virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: 127460 (2020)
TBA
Structure activity study of S-trityl-cysteamine dimethylaminopyridine derivatives as SIRT2 inhibitors: Improvement of SIRT2 binding and inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Science Farm
Design, synthesis and biological evaluation of 3,5-diaryl isoxazole derivatives as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Atat£Rk University
Discovery of novel anti-angiogenesis agents. Part 11: Development of PROTACs based on active molecules with potency of promoting vascular normalization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
The First Affiliated Hospital of Xi'An Jiaotong University
Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sci Transl Med 12: (2020)
Wichita State University
Novel quinazoline-based EGFR kinase inhibitors: A review focussing on SAR and molecular docking studies (2015-2019).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
School of Pharmaceutical Education and Research
A cell-penetrant lactam-stapled peptide for targeting eIF4E protein-protein interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
University of Michigan
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Dana-Farber Cancer Institute
Synthesis and biological evaluation of parthenolide derivatives with reduced toxicity as potential inhibitors of the NLRP3 inflammasome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Guangzhou Medical University
Structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo Medical and Dental University (Tmdu)
The transcriptional repressor REV-ERB as a novel target for disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Imperial College London
5,5-Difluoro- and 5-Fluoro-5-methyl-hexose-based C-Glucosides as potent and orally bioavailable SGLT1 and SGLT2 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Structure-guided optimization of a novel class of ASK1 inhibitors with increased sp![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Takeda Research In California
Design, synthesis and biological evaluation of 2-indolinone derivatives as PAK1 inhibitors in MDA-MB-231 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Harbin Medical University
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Genomics Institute of The Novartis Research Foundation
Orally bioavailable HCV NS5A inhibitors of unsymmetrical structural class.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Japan Tobacco
Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Topical 'dual-soft' glucocorticoid receptor agonist for dermatology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Leo Pharma
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel ROR?t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Synthesis and evaluations of selective COX-2 inhibitory effects: Benzo[d]thiazol analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Zhejiang Ocean University
Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Shenyang Pharmaceutical University
Synthesis, inhibitory activity and in silico docking of dual COX/5-LOX inhibitors with quinone and resorcinol core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Institute of Experimental Botany of The Czech Academy of Sciences
Medicinal chemistry strategies for the development of protein tyrosine phosphatase SHP2 inhibitors and PROTAC degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Zhengzhou University
Design, synthesis and in vitro cell-free/cell-based biological evaluations of novel ERCC1-XPF inhibitors targeting DNA repair pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
University of Alberta
Synthesis and biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 205: (2020)
Shanghai Jiao Tong University
Bioisosteric substitution of adamantane with bicyclic lipophilic groups improves water solubility of human soluble epoxide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of California Davis
New V1a receptor antagonist. Part 1. Synthesis and SAR development of urea derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Gedeon Richter
Discovery of 2,6-difluorobenzyl ether series of phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfones as surprisingly potent, selective and orally bioavailable ROR?t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Development of SKI-349, a dual-targeted inhibitor of sphingosine kinase and microtubule polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Pennsylvania State University College of Medicine
Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Palack£
Recent developments of gallic acid derivatives and their hybrids in medicinal chemistry: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
King Abdulaziz University
Design, synthesis and biological activities of novel pleuromutilin derivatives with a substituted triazole moiety as potent antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
South China Agricultural University
Identification of benzofused five-membered sultams, potent dual NOD1/NOD2 antagonists in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Chinese Academy of Medical Sciences & Peking Union Medical College
Identification of novel quinoline analogues bearing thiazolidinones as potent kinase inhibitors for the treatment of colorectal cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Zhuhai Campus of Zunyi Medical University
New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Gedeon Richter
Exploiting binding-site arginines in drug design: Recent examples.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Prelude Therapeutics
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Design and synthesis of peptidic partial agonists of human neuromedin U receptor 1 with enhanced serum stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo University of Pharmacy and Life Sciences
Thienochromene derivatives inhibit pSTAT1 and pSTAT5 signaling induced by cytokines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Rijeka
The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38? MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Development of chiral fluorinated alkyl derivatives of emixustat as drug candidates for the treatment of retinal degenerative diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bar-Ilan University
Synthesis and biological evaluation of novel quinazoline-triazole hybrid compounds with potential use in Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Viet Nam
Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
University of Arkansas For Medical Sciences
The ups and downs of Poly(ADP-ribose) Polymerase-1 inhibitors in cancer therapy-Current progress and future direction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Central South University
Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Xiamen University
Benzothiophene-2-carboxamide derivatives as SENPs inhibitors with selectivity within SENPs family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Shanghai Jiao Tong University
An exhaustive perspective on structural insights of SGLT2 inhibitors: A novel class of antidiabetic agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Dr. Harisingh Gour University (A Central University)
Designing an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Sichuan University
Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Universidade Federal Do Rio De Janeiro
Design, synthesis and bioevaluation of novel substituted triazines as potential dual PI3K/mTOR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Guizhou Medical University
Synthesis and matched molecular pair analysis of covalent reversible inhibitors of the cysteine protease CPB.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
S£O Carlos Institute of Chemistry-University of S£O Paulo (Iqsc-Usp)
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Sichuan University
Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Alma Mater Studiorum-Universit£
Automated design and optimization of multitarget schizophrenia drug candidates by deep learning.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Shanghai Institute of Materia Medica
Recent research progress on natural small molecule bibenzyls and its derivatives in Dendrobium species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 204: (2020)
Chengdu University
Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Universit£
Development of disulfide-derived fructose-1,6-bisphosphatase (FBPase) covalent inhibitors for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
East China University of Science and Technology
A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Mizoram University
Stepwise Design of ?-Secretase Modulators with an Advanced Profile by Judicious Coordinated Structural Replacements and an Unconventional Phenyl Ring Bioisostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8534-8553 (2020)
F. Hoffmann-La Roche
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9360-9390 (2020)
University of Barcelona (Ub)
Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Jinan University
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9093-9126 (2020)
Glaxosmithkline
Advances in research of spirodienone and its derivatives: Biological activities and synthesis methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Sichuan University
PROTAC: A promising technology for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
China Pharmaceutical University
Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Taisho Pharmaceutical
Discovery of carboxyl-containing biaryl ureas as potent ROR?t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Fudan University
Design, Synthesis, and Evaluation of New Quinazolinone Derivatives that Inhibit Bloom Syndrome Protein (BLM) Helicase, Trigger DNA Damage at the Telomere Region, and Synergize with PARP Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9752-9772 (2020)
Sun Yat-Sen University
Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12526-12541 (2020)
Biogen
Discovery and Characterization of Pure RhlR Antagonists against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8388-8407 (2020)
Korea University
Chlorine substituents and linker topology as factors of 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Jagiellonian University
Recent researches for dual Aurora target inhibitors in antitumor field.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Chengdu University
Lung Protection by Cathepsin C Inhibition: A New Hope for COVID-19 and ARDS?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 13258-13265 (2020)
Centre D'Etude Des Pathologies Respiratoires and Universit£
Recent Progress in the Discovery of Antifungal Agents Targeting the Cell Wall.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12429-12459 (2020)
Shaanxi University of Science and Technology
Design and Synthesis of a Highly Selective and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9070-9092 (2020)
Glaxosmithkline
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9045-9069 (2020)
Glaxosmithkline
Design, synthesis and biological evaluation of novel glyoxalase I inhibitors possessing diazenylbenzenesulfonamide moiety as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jordan University of Science and Technology
Synthesis of 2-guanidinyl pyridines and their trypsin inhibition and docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University College Dublin
Structure-activity relationship studies for the development of inhibitors of murine adipose triglyceride lipase (ATGL).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Graz University of Technology
Modulation of TRPV4 and BKCa for treatment of brain diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kunming University of Science and Technology
Design and biological evaluation of novel HIV-1 protease inhibitors with isopropanol as P1' ligand to enhance binding with S1' subsite.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chinese Academy of Medical Science and Peking Union Medical College
An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shandong University
Amides as bioisosteres of triazole-based geranylgeranyl diphosphate synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Iowa
Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Southern Medical University
Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9512-9522 (2020)
Virginia Commonwealth University
Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
University of Defense
Development of dual inhibitors targeting pyruvate dehydrogenase kinases and human lactate dehydrogenase A: High-throughput virtual screening, synthesis and biological validation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Chongqing University
Structure-activity relationships of Wee1 inhibitors: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Sichuan University
The importance of indole and azaindole scaffold in the development of antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Qingdao University of Science and Technology
Design and Structural Optimization of Dual FXR/PPAR? Activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8369-8379 (2020)
Goethe University Frankfurt
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12290-12358 (2020)
University of Nebraska Medical Center
Photoswitchable Antagonists for a Precise Spatiotemporal Control of ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8458-8470 (2020)
Institute For Advanced Chemistry of Catalonia (Iqac-Csic)
Fluoropyrimidin-2,4-dihydroxy-5-isopropylbenzamides as antitumor agents against CRC and NSCLC cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Taipei Medical University
Design of G-protein-coupled bile acid receptor 1 (GPBAR1, TGR5) soft drugs with reduced gallbladder-filling effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Chinese Academy of Sciences
A novel long-acting oxyntomodulin analogue eliminates diabetes and obesity in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Beijing University of Chinese Medicine
Development of a metabolically stable topoisomerase I poison as anticancer agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Csir-Indian Institute of Chemical Biology
Amphiphilic aminoglycosides with increased selectivity for inhibition of connexin 43 (Cx43) hemichannels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Utah State University
PFKFB3 inhibitors as potential anticancer agents: Mechanisms of action, current developments, and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Liaocheng University
Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Jiangxi Science & Technology Normal University
Structure-based design, synthesis and bioactivity evaluation of macrocyclic inhibitors of mutant isocitrate dehydrogenase 2 (IDH2) displaying activity in acute myeloid leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 203: (2020)
Hangzhou Institute of Innovative Medicine
Nonclassical Phenyl Bioisosteres as Effective Replacements in a Series of Novel Open-Source Antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11585-11601 (2020)
The University of Sydney
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1484-1489 (2020)
University of Texas Md Anderson Cancer Center
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1476-1483 (2020)
Merck
Antiglioma Activity of Aryl and Amido-Aryl Acetamidine Derivatives Targeting iNOS: Synthesis and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1470-1475 (2020)
University "G. D'Annunzio" of Chieti-Pescara
Discovery of 3-Quinazolin-4(3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1463-1469 (2020)
Luoxin Pharmaceutical (Shanghai) Co.
Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1429-1434 (2020)
National Center For Scientific Research Demokritos
Designing Dihydrofolate Reductase Inhibitors as X-ray Radiosensitizers to Reverse Radioresistance of Cervical Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1421-1428 (2020)
Jinan University
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1402-1409 (2020)
Biocon Bristol Myers Squibb Research Center
Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1386-1391 (2020)
Gsk Medicines Research Centre
Novel anilide and benzylamide derivatives of arylpiperazinylalkanoic acids as 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Jagiellonian University Medical College
Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8325-8337 (2020)
Vanderbilt University School of Medicine
Neuropeptide FF and Its Receptors: Therapeutic Applications and Ligand Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12387-12402 (2020)
Research Triangle Institute
Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8296-8313 (2020)
University of Massachusetts Medical School
Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8634-8648 (2020)
University of Toronto Mississauga
Modulating microRNA Processing: Enoxacin, the Progenitor of a New Class of Drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12275-12289 (2020)
University of Perugia
Recent progress in Keap1-Nrf2 protein-protein interaction inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Taizhou University
Structure-based design, semi-synthesis and anti-inflammatory activity of tocotrienolic amides as 5-lipoxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Univ Angers
Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8338-8358 (2020)
Southern Medical University
Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8584-8607 (2020)
Rapt Therapeutics
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10773-10781 (2020)
Genomics Institute of The Novartis Research Foundation (Gnf)
Discovery of an Orally Active Small-Molecule Tumor Necrosis Factor-? Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8146-8156 (2020)
Huazhong University of Science and Technology
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9316-9339 (2020)
Peking Union Medical College and Chinese Academy of Medical Sciences
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9523-9539 (2020)
University of Dundee
Discovery of first-in-class multi-target adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Universit£
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Universit£
Small-Molecule Fms-like Tyrosine Kinase 3 Inhibitors: An Attractive and Efficient Method for the Treatment of Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12403-12428 (2020)
Nanjing University of Chinese Medicine
The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8314-8324 (2020)
University of Tennessee
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8567-8583 (2020)
Tsinghua University
Chromones bearing amino acid residues: Easily accessible and potent inhibitors of the breast cancer resistance protein ABCG2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Cnrs
Recent advances in chemistry and bioactivity of marine cyanobacteria Moorea species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Ningbo University
Kojic acid-natural product conjugates as mushroom tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Mazandaran University of Medical Sciences
Natural and nature-inspired stilbenoids as antiviral agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Universita Degli Studi di Milano
Anticancer fungal natural products: Mechanisms of action and biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Sun Yat-Sen University
Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-? aggregation against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Affiated Tumor Hospital of Guangxi Medical University
Synthesis of the Major Mammalian Metabolites of THCV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2060-2065 (2020)
National Research Council of Italy
Tideglusib and Its Analogues As Inhibitors of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8442-8457 (2020)
Guizhou University
Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Bharati Vidyapeeth'S College of Pharmacy
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7773-7816 (2020)
Novartis Institutes For Biomedical Research
Design synthesis and evaluation of novel aldose reductase inhibitors: The case of indolyl-sulfonyl-phenols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
251 General Air Force Hospital
Design, synthesis and biological activity of novel substituted 3-benzoic acid derivatives as MtDHFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University Hospital T£Bingen
Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Tetrazoles as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Central University of Punjab
Structural studies of triazole inhibitors with promising inhibitor effects against antibiotic resistance metallo-?-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Uit The Arctic University of Norway
Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Federal University of S£O Carlos
Amide derivatives of Gallic acid: Design, synthesis and evaluation of inhibitory activities against in vitro ?-synuclein aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Zhengzhou University
New coumarin/sulfocoumarin linked phenylacrylamides as selective transmembrane carbonic anhydrase inhibitors: Synthesis and in-vitro biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Institute of Pharmaceutical Education and Research (NIPER)
Phenyltriazole-functionalized sulfamate inhibitors targeting tyrosyl- or isoleucyl-tRNA synthetase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Ku Leuven
Structural manipulation of aporphines via C10 nitrogenation leads to the identification of new 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
City University of New York
Synthesis and biological evaluation of thioadatanserin and its dialkylated products as partial 5-HTR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Dominican College
Improving NK1R-targeted gene delivery of stearyl-antimicrobial peptide CAMEL by conjugating it with substance P.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Lanzhou University
A chalcone derivative binds a putative allosteric site of YopH: Inhibition of a virulence factor of Yersinia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Universidade Federal De Santa Catarina
SAR of non-hydrolysable analogs of pyridoxal 5'-phosphate against low molecular weight protein tyrosine phosphatase isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Saint John'S University
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-? (TGF-?) type I receptor inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Cairo University
Design, synthesis and biological evaluation of novel pteridinone derivatives possessing a hydrazone moiety as potent PLK1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of 2-methyl-(1,1'-biphenyl)-pyrimidine conjugates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Zhejiang University
Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
East China University of Science & Technology
Anticonvulsant and analgesic in neuropathic pain activity in a group of new aminoalkanol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Synthesis and dopamine receptor pharmacological evaluations on ring C ortho halogenated 1-phenylbenzazepines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
City University of New York
Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ?FosB homodimers and ?FosB/JunD heterodimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Texas Medical Branch
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
M. V. Lomonosov Moscow State University
Development of a new class of liver receptor homolog-1 (LRH-1) agonists by photoredox conjugate addition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Emory University
Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sabila Biosciences
C2-substituted quinazolinone derivatives exhibit A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
North-West University
Discovery of 5-(4-methylpiperazin-1-yl)-2-nitroaniline derivatives as a new class of SIRT6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sichuan University
A novel pipeline of 2-(benzenesulfonamide)-N-(4-hydroxyphenyl) acetamide analgesics that lack hepatotoxicity and retain antipyresis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Ochsner Clinic
Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 202: (2020)
Xuzhou Medical University
Design, synthesis and evaluation of carbamate-linked uridyl-based inhibitors of human ST6Gal I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Wollongong
Bisphosphonate esters interact with HMG-CoA reductase membrane domain to induce its degradation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The University of Tokyo
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Florida
2?-3,4-Unsaturated sialic acid derivatives: Synthesis optimization, and biological evaluation as Newcastle disease virus hemagglutinin-neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Milan
PTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
University of Toronto Mississauga
Discovery of AB680: A Potent and Selective Inhibitor of CD73.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11448-11468 (2020)
Arcus Biosciences
Oligopeptides as Neuropeptide Y Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8198-8215 (2020)
University of Regensburg
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12460-12484 (2020)
University of East Anglia
Amino Acids Bearing Aromatic or Heteroaromatic Substituents as a New Class of Ligands for the Lysosomal Sialic Acid Transporter Sialin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8231-8249 (2020)
Universit£
A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8179-8197 (2020)
Heidelberg University
Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8419-8431 (2020)
Purdue University
Rational modification, synthesis and biological evaluation of 3,4-dihydroquinoxalin-2(1H)-one derivatives as potent and selective c-Jun N-terminal kinase 3 (JNK3) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Peking University
Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Shanghai University of Traditional Chinese Medicine
Medicinal chemistry insights into novel CDC25 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Shandong University
Discovery of Novel PDE? Degraders for the Treatment of KRAS Mutant Colorectal Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7892-7905 (2020)
Second Military Medical University
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7867-7879 (2020)
Sun Yat-Sen University
A Venomics Approach Coupled to High-Throughput Toxin Production Strategies Identifies the First Venom-Derived Melanocortin Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8250-8264 (2020)
Universit£
Pyrido[2,3-b][1,5]benzoxazepin-5(6H)-one derivatives as CDK8 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Spanish National Cancer Research Centre (Cnio)
Rosuvastatin based novel 3-substituted isocoumarins / 3-alkylidenephthalides: Ultrasound assisted synthesis and identification of new anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
University of Hyderabad Campus
Hydroxy-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2212-2220 (2020)
Universidad Nacional Aut£Noma De M£Xico
Development of Conformationally Constrained ?-RgIA Analogues as Stable Peptide Antagonists of Human ?9?10 Nicotinic Acetylcholine Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8380-8387 (2020)
University of Utah
?-Lactams as promising anticancer agents: Molecular hybrids, structure activity relationships and potential targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Beijing University of Chinese Medicine
Structural and Mechanistic Basis of the Inhibitory Potency of Selected 2-Aminothiazole Compounds on Protein Kinase CK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7766-7772 (2020)
Universit£T Zu K£Ln
Characterization of Inhibition Reveals Distinctive Properties for Human and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7545-7558 (2020)
Georg-August-University G£Ttingen
Dehydrohispanolone Derivatives Attenuate the Inflammatory Response through the Modulation of Inflammasome Activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2155-2164 (2020)
Universidad Complutense De Madrid (Ucm)
Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7840-7856 (2020)
X-Chem
EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7252-7267 (2020)
University of Michigan
Novel Thienopyrimidine Inhibitors of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7740-7765 (2020)
Imperial College London
Development of small-molecule inhibitors of fatty acyl-AMP and fatty acyl-CoA ligases in Mycobacterium tuberculosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
University of Minnesota
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7721-7739 (2020)
Uppsala University
Dual Targeting of Norepinephrine Transporter (NET) Function and Thyrointegrin ?v?3 Receptors in the Treatment of Neuroblastoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7653-7662 (2020)
Albany College of Pharmacy and Health Sciences
Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
China Medical University
The structure-based optimization of ?-sultone-fused pyrazoles as selective BuChE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Anhui Medical University
Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7529-7544 (2020)
University of Texas Medical Branch
Fight against novel coronavirus: A perspective of medicinal chemists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Jadavpur University
Synthesis of adenine dinucleosides SAM analogs as specific inhibitors of SARS-CoV nsp14 RNA cap guanine-N7-methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
University of Montpellier
Single and dual target inhibitors based on Bcl-2: Promising anti-tumor agents for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Shandong First Medical University & Shandong Academy of Medical Sciences
Structure-Based Drug Discovery of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7906-7920 (2020)
Sosei Heptares
Synthesis and Anticancer Activity of Novel Actinonin Derivatives as HsPDF Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6959-6978 (2020)
Sun Yat-Sen University
Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ? Inhibitors with Fragment-Merging Strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7143-7162 (2020)
Asahi Kasei Pharma
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8088-8113 (2020)
Novartis Institutes For Biomedical Research
Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1342-1347 (2020)
Genentech
ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1335-1341 (2020)
Ono Pharmaceutical
Discovery of Diphenylacetamides as CXCR7 Inhibitors with Novel ?-Arrestin Antagonist Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1330-1334 (2020)
Pfizer
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1324-1329 (2020)
Constellation Pharmaceuticals
Discovery of Novel Nonpeptidic PAR2 Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1316-1323 (2020)
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)
Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1305-1309 (2020)
H3 Biomedicine
P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1281-1286 (2020)
Saint Louis University School of Medicine
Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1269-1273 (2020)
Dana-Farber Cancer Institute
Discovery of RO7185876, a Highly Potent ?-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1257-1268 (2020)
F. Hoffmann-La Roche
Development of Selective Steroid Inhibitors for the Glucose-6-phosphate Dehydrogenase from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1250-1256 (2020)
Brazilian Biosciences National Laboratory
Computer-Aided Fragment Growing Strategies to Design Dual Inhibitors of Soluble Epoxide Hydrolase and LTA4 Hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1244-1249 (2020)
Goethe-University
Discovery of an Atropisomeric PI3K? Selective Inhibitor through Optimization of the Hinge Binding Motif.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1236-1243 (2020)
Gilead Sciences
Benzoxazepine-Derived Selective, Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1228-1235 (2020)
Oncoarendi Therapeutics
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1221-1227 (2020)
Bristol Myers Squibb
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1213-1220 (2020)
Constellation Pharmaceuticals
Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1205-1212 (2020)
Constellation Pharmaceuticals
Novel HIV-1 Protease Inhibitors with Morpholine as the P2 Ligand to Enhance Activity against DRV-Resistant Variants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1196-1204 (2020)
Chinese Academy of Medical Science and Peking Union Medical College
Scaffold Repurposing of in-House Chemical Library toward the Identification of New Casein Kinase 1 ? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1168-1174 (2020)
University of Padova
Discovery of a Potent Dual Inhibitor of Wild-Type and Mutant Respiratory Syncytial Virus Fusion Proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1145-1151 (2020)
Taisho Pharmaceutical
Identification of Inhibitors of Thrombospondin 1 Activation of TGF-?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1130-1136 (2020)
Southern Research Institute
Design and Synthesis of Tetrazole- and Pyridine-Containing Itraconazole Analogs as Potent Angiogenesis Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1111-1117 (2020)
Johns Hopkins School of Medicine
Ligand Design for Cereblon Based Immunomodulatory Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1088-1089 (2020)
Usona Institute
Cancer Immunotherapy through the Inhibition of Diacylglycerol Kinases Alpha and Zeta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1083-1085 (2020)
Therachem Research Medilab
Potential Cancer Treatment by Agonists of the Stimulator of Interferon Genes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1081-1082 (2020)
Therachem Research Medilab
Inhibitors of Hypoxia-Inducible Factors as Treatment for Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1079-1080 (2020)
Therachem Research Medilab
Discovery of novel potent GPR40 agonists containing imidazo[1,2-a]pyridine core as antidiabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
A critical update on the strategies towards modulators targeting androgen receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Mining the PDB for Tractable Cases Where X-ray Crystallography Combined with Fragment Screens Can Be Used to Systematically Design Protein-Protein Inhibitors: Two Test Cases Illustrated by IL1?-IL1R and p38?-TAB1 Complexes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7559-7568 (2020)
King'S College London
Fragment Linking Strategies for Structure-Based Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11420-11435 (2020)
Universit£
Inhibitors of SARS-CoV-2 Entry: Current and Future Opportunities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12256-12274 (2020)
Shandong University
Targeting Peroxisome Proliferator-Activated Receptor Delta (PPAR?): A Medicinal Chemistry Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10109-10134 (2020)
Daegu-Gyeongbuk Medical Innovation Foundation
Discovery of Dihydropyrrolo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7569-7600 (2020)
Emory University
Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Shenyang Pharmaceutical University
Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6876-6897 (2020)
TBA
Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7817-7826 (2020)
Harvard Medical School
Synthesis and Structure-Activity Relationships of 5'-Aryl-14-alkoxypyridomorphinans: Identification of a ? Opioid Receptor Agonist/? Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7663-7694 (2020)
University of Alabama At Birmingham
Rapid Elaboration of Fragments into Leads by X-ray Crystallographic Screening of Parallel Chemical Libraries (REFiL![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6863-6875 (2020)
Monash University (Parkville Campus)
Discovery of quinoline-based irreversible BTK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Acerta Pharma
A cell-based fluorescent assay for FAP inhibitor discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Peking University First Hospital
Design, synthesis and evaluation of pyrazolopyrimidinone derivatives as novel PDE9A inhibitors for treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sun Yat-Sen University
Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Prof John Barnabas Post Graduate School of Biological Studies
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Amgen
Discovery of triazolo [1,5-a] pyridine derivatives as novel JAK1/2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shenyang Pharmaceutical University
Azetidine-based selective glycine transporter-1 (GlyT1) inhibitors with memory enhancing properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Dart Neuroscience
Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bengbu Medical College
Quinazoline Based HSP90 Inhibitors: Synthesis, Modeling Study and ADME Calculations Towards Breast Cancer Targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Mansoura University
Discovery of hydroxy pyrimidine Factor IXa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Chiba University
Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
University of Perugia
Epoxide containing molecules: A good or a bad drug design approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 201: (2020)
Univ Coimbra.
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8857-8866 (2020)
Google Research Applied Science, Mountain View, California 94043, United States.
Antiproliferative Flavanoid Dimers Isolated from Brazilian Red Propolis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1784-1793 (2020)
Universidade De S£O Paulo
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6924-6940 (2020)
Ocean University of China
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7422-7444 (2020)
University of Firenze
New Broad-Spectrum Antibiotics Containing a Pyrrolobenzodiazepine Ring with Activity against Multidrug-Resistant Gram-Negative Bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6941-6958 (2020)
King'S College London
Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7369-7391 (2020)
University of Siena
On the Promise of Photopharmacology Using Photoswitches: A Medicinal Chemist's Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11436-11447 (2020)
Imperial College London
Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11397-11419 (2020)
Norman Drug Discovery Training and Consulting
Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6834-6846 (2020)
University of Oslo
Discovery of a Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7163-7185 (2020)
Japan Tobacco
Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7033-7051 (2020)
The First Affiliated Hospital of Xi'An Jiao Tong University
Receptor-interacting protein kinase 2 (RIPK2) and nucleotide-binding oligomerization domain (NOD) cell signaling inhibitors based on a 3,5-diphenyl-2-aminopyridine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
University of Houston
Design, synthesis and biological evaluation of novel N-sulfonylamidine-based derivatives as c-Met inhibitors via Cu-catalyzed three-component reaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Harbin Institute of Technology
Cytosolic delivery of peptidic STAT3 SH2 domain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Tufts University
Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Zhejiang University
Synthesis of novel 3,5,6-trisubstituted 2-pyridone derivatives and evaluation for their anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universidade Estadual De Maring£
The synthesis and biological evaluation of nucleobases/tetrazole hybrid compounds: A new class of phosphodiesterase type 3 (PDE3) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shiraz University
Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of novel pyrrolo[2,3-d]pyrimidine as tumor-targeting agents with selectivity for tumor uptake by high affinity folate receptors over the reduced folate carrier.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Duquesne University
Factor XIIIa inhibitors as potential novel drugs for venous thromboembolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Xavier University of Louisiana
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
China Pharmaceutical University
1,4-Benzodioxane, an evergreen, versatile scaffold in medicinal chemistry: A review of its recent applications in drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Universit£
Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6708-6726 (2020)
Harvard Medical School
Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7293-7325 (2020)
Bayer
N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Pyrimidine: A promising scaffold for optimization to develop the inhibitors of ABC transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Key Laboratory of Technology of Drug Preparation (Zhengzhou University)
Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Martin-Luther University of Halle-Wittenberg
Structural Revision of Garcinielliptin Oxide and Garcinielliptone E.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 2041-2044 (2020)
University of Kentucky
Design, synthesis, and biological characterization of a new class of symmetrical polyamine-based small molecule CXCR4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Tsinghua University
Inhibiting Matrix Metalloproteinase-2 Activation by Perturbing Protein-Protein Interactions Using a Cyclic Peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6979-6990 (2020)
University of California
Discovery and Structural Optimization of 4-(Aminomethyl)benzamides as Potent Entry Inhibitors of Ebola and Marburg Virus Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7211-7225 (2020)
University of Illinois At Chicago
Iodoquinazolinones bearing benzenesulfonamide as human carbonic anhydrase I, II, IX and XII inhibitors: Synthesis, biological evaluation and radiosensitizing activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
National Center For Radiation Research and Technology (Ncrrt)
Recent advancements in the development of heterocyclic anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Isf College of Pharmacy
Expanding the anticancer potential of 1,2,3-triazoles via simultaneously targeting Cyclooxygenase-2, 15-lipoxygenase and tumor-associated carbonic anhydrases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Alexandria University
Resveratrol - A comprehensive review of recent advances in anticancer drug design and development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Mazandaran University of Medical Sciences
Design and Synthesis of a Trifunctional Molecular System "Programmed" to Block Epidermal Growth Factor Receptor Tyrosine Kinase, Induce High Levels of DNA Damage, and Inhibit the DNA Repair Enzyme (Poly(ADP-ribose) Polymerase) in Prostate Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5752-5762 (2020)
The Research Institute of The Mcgill University Health Center/Glen Hospital
Discovery of ORN0829, a potent dual orexin 1/2 receptor antagonist for the treatment of insomnia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Taisho Pharmaceutical
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10533-10593 (2020)
Taipei Medical University
Substituted benzothiophene and benzofuran derivatives as a novel class of bone morphogenetic Protein-2 upregulators: Synthesis, anti-osteoporosis efficacies in ovariectomized rats and a zebrafish model, and ADME properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Chinese Academy of Medical Sciences & Peking Union Medical College
Discovery of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7326-7346 (2020)
Shenyang Pharmaceutical University
Identification of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6748-6773 (2020)
China Pharmaceutical University
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5879-5955 (2020)
Inception Therapeutics
-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8359-8368 (2020)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips) - Helmholtz Centre For Infection Research (Hzi
Precursor-Directed Biosynthesis and Fluorescence Labeling of Clickable Microcystins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1960-1970 (2020)
University of Halle-Wittenberg
Progress toward a Glycoprotein VI Modulator for the Treatment of Thrombosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 12213-12242 (2020)
University of Leeds
Overview of AKR1C3: Inhibitor Achievements and Disease Insights.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11305-11329 (2020)
China Pharmaceutical University
Azidothymidine "Clicked" into 1,2,3-Triazoles: First Report on Carbonic Anhydrase-Telomerase Dual-Hybrid Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7392-7409 (2020)
Universit£
Fragment-Based Discovery of Pyrazolopyridones as JAK1 Inhibitors with Excellent Subtype Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7008-7032 (2020)
Gvk Biosciences
Bioisosteric Replacement of Arylamide-Linked Spine Residues with ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7347-7354 (2020)
Federal University of Rio De Janeiro (Ufrj)
Late-Stage Lead Diversification Coupled with Quantitative Nuclear Magnetic Resonance Spectroscopy to Identify New Structure-Activity Relationship Vectors at Nanomole-Scale Synthesis: Application to Loratadine, a Human Histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7268-7292 (2020)
Pfizer
Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 11368-11396 (2020)
China Pharmaceutical University
Development of oxathiino[6,5-b]pyridine 2,2-dioxide derivatives as selective inhibitors of tumor-related carbonic anhydrases IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Latvian Institute of Organic Synthesis
Recent advances in DNA gyrase-targeted antimicrobial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Queensland University of Technology
Matrix Metalloproteinases as New Targets in Alzheimer's Disease: Opportunities and Challenges.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10705-10725 (2020)
Normandie Univ
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7226-7242 (2020)
Bristol Myers Squibb
Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Northwest A&F University
Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7186-7210 (2020)
University of Illinois At Chicago
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7108-7126 (2020)
Haisco Pharmaceutical Group
Optical control of muscular nicotinic channels with azocuroniums, photoswitchable azobenzenes bearing two N-methyl-N-carbocyclic quaternary ammonium groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Consejo Superior De Investigaciones Cient�Ficas (Iqm-Csic)
Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
China Pharmaceutical University
DDX3X inhibitors, an effective way to overcome HIV-1 resistance targeting host proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
Universit£
Penicillin binding protein 2a: An overview and a medicinal chemistry perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Ain Shams University
Privileged scaffold-based design to identify a novel drug-like 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Universit£
Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7510-7528 (2020)
TBA
Factor H-Inspired Design of Peptide Biomarkers of the Complement C3d Protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1054-1059 (2020)
University of California Riverside
HOPPI-NMR: Hot-Peptide-Based Screening Assay for Inhibitors of Protein-Protein Interactions by NMR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1047-1053 (2020)
University of Naples "Federico Ii
Discovery of Small-Molecule Stabilizers of 14-3-3 Protein-Protein Interactions via Dynamic Combinatorial Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1041-1046 (2020)
University of Groningen
Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1028-1034 (2020)
University of Modena and Reggio Emilia
Benzofuran-Based Carboxylic Acids as Carbonic Anhydrase Inhibitors and Antiproliferative Agents against Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1022-1027 (2020)
Kafrelsheikh University
Phenolic Compounds from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1006-1013 (2020)
Centre of Experimental Medicine
Looking toward the Rim of the Active Site Cavity of Druggable Human Carbonic Anhydrase Isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 1000-1005 (2020)
Universit£
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 977-983 (2020)
Sapienza University of Rome
Structure-Guided Identification of DNMT3B Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 971-976 (2020)
Yale University
Progress in the Field of Aldehyde Dehydrogenase Inhibitors: Novel Imidazo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 963-970 (2020)
University of Pisa
Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 956-962 (2020)
Universit£
Sigma Receptor Ligands Carrying a Nitric Oxide Donor Nitrate Moiety: Synthesis, In Silico, and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 889-894 (2020)
University of Catania
Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 869-876 (2020)
University of Bari Aldo Moro
From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 862-868 (2020)
University of Naples
New Dihydrothiazole Benzensulfonamides: Looking for Selectivity toward Carbonic Anhydrase Isoforms I, II, IX, and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 852-856 (2020)
University of Cagliari
Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 825-831 (2020)
Angelini Pharma
GPBAR1 Activation by C6-Substituted Hyodeoxycholane Analogues Protect against Colitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 818-824 (2020)
University of Naples "Federico Ii
Peptides Mimicking the ?7/?8 Loop of HIV-1 Reverse Transcriptase p51 as "Hotspot-Targeted" Dimerization Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 811-817 (2020)
Instituto De Qu£Mica M£Dica (Iqm, Csic)
Drug Synergism: Studies of Combination of RK-52 and Curcumin against Rhodesain of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 806-810 (2020)
University of Messina
Pyrrolyl Pyrazoles as Non-Diketo Acid Inhibitors of the HIV-1 Ribonuclease H Function of Reverse Transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 798-805 (2020)
"Sapienza" Universit£
Targeting mPGES-1 by a Combinatorial Approach: Identification of the Aminobenzothiazole Scaffold to Suppress PGE![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 783-789 (2020)
University of Salerno
5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 766-772 (2020)
Irbm
Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 754-759 (2020)
European Institute of Oncology Irccs
Combined Peptide and Small-Molecule Approach toward Nonacidic THIQ Inhibitors of the KEAP1/NRF2 Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 740-746 (2020)
Irbm
Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 732-739 (2020)
Alma Mater Studiorum-University of Bologna
Glycomimetic Based Approach toward Selective Carbonic Anhydrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 727-731 (2020)
Universit£
Developing Cyclic Opioid Analogues: Fluorescently Labeled Bioconjugates of Biphalin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 720-726 (2020)
Universit£
New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 713-719 (2020)
Universidad San Pablo-Ceu
Structural and in Vivo Characterization of Tubastatin A, a Widely Used Histone Deacetylase 6 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 706-712 (2020)
University of Illinois At Chicago
Development of Pyrazolo[3,4-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 657-663 (2020)
University of Genoa
Synthesis, Cytotoxicity Evaluation, and Computational Insights of Novel 1,4-Diazepane-Based Sigma Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 651-656 (2020)
University of Trieste
Discovery of New 1,1'-Biphenyl-4-sulfonamides as Selective Subnanomolar Human Carbonic Anhydrase II Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 633-637 (2020)
Sapienza University of Rome
Sulfonimide and Amide Derivatives as Novel PPAR? Antagonists: Synthesis, Antiproliferative Activity, and Docking Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 624-632 (2020)
"G. D'Annunzio" University of Chieti-Pescara
Chimeric Peptidomimetics of SOCS 3 Able to Interact with JAK2 as Anti-inflammatory Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 615-623 (2020)
University of Naples "Federico Ii
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6784-6801 (2020)
University of Nottingham
High-Throughput Screening for the Discovery of Enzyme Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10742-10772 (2020)
University of Bath
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10726-10741 (2020)
Jinan University
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5783-5796 (2020)
China Pharmaceutical University
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Central South University
Characterization and Noncovalent Inhibition of the Deubiquitinase and deISGylase Activity of SARS-CoV-2 Papain-Like Protease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Infect Dis 6: 2099-2109 (2020)
University of Georgia
Discovery of indoximod prodrugs and characterization of clinical candidate NLG802.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Newlink Genetics
Exploration of carbamide derived pyrimidine-thioindole conjugates as potential VEGFR-2 inhibitors with anti-angiogenesis effect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 200: (2020)
National Institute of Pharmaceutical Education and Research (NIPER)
Hybrid Screening Approach for Very Small Fragments: X-ray and Computational Screening on FKBP51.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5856-5864 (2020)
Boehringer Ingelheim Pharma
UR-DEBa242: A Py-5-Labeled Fluorescent Multipurpose Probe for Investigations on the Histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5297-5311 (2020)
University of Regensburg
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6144-6163 (2020)
Washington University School of Medicine
A ?-Lactam Siderophore Antibiotic Effective against Multidrug-Resistant Gram-Negative Bacilli.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5990-6002 (2020)
Louis Stokes Cleveland Department of Veterans Affairs Medical Center
Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Erciyes University
Targeting mTOR for fighting diseases: A revisited review of mTOR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Sichuan University
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5816-5840 (2020)
Glaxosmithkline R&D
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8046-8058 (2020)
Janssen Pharmaceutical Companies of Johnson & Johnson
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10188-10203 (2020)
Gilead Sciences
Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 9003-9019 (2020)
Kyorin Pharmaceutical
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Zhengzhou University
Identification of a new series of flavopiridol-like structures as kinase inhibitors with high cytotoxic potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
University Paris-Saclay
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Novel bacterial topoisomerase inhibitors derived from isomannide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
The Ohio State University
Discovery of DS-1971a, a Potent, Selective Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10204-10220 (2020)
Daiichi Sankyo
-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5734-5751 (2020)
Universidad De Granada
Structure-Activity Relationship Study Enables the Discovery of a Novel ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5841-5855 (2020)
Xiamen University
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5865-5878 (2020)
Ocean University of China
Non-'classical' MEKs: A review of MEK3-7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Northwestern University
Design, synthesis and SAR study of bridged tricyclic pyrimidinone carboxamides as HIV-1 integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Bristol Myers Squibb
Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Southern Medical University
Monocarboxylate transporter 1 and 4 inhibitors as potential therapeutics for treating solid tumours: A review with structure-activity relationship insights.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management
Discovery of bazedoxifene analogues targeting glycoprotein 130.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 199: (2020)
China Pharmaceutical University
Rational design and biological evaluation of gemfibrozil modified Xenopus GLP-1 derivatives as long-acting hypoglycemic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Jiangnan University
Synthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Universidad De Chile
Synthesis, characterization and carbonic anhydrase I and II inhibitory evaluation of new sulfonamide derivatives bearing dithiocarbamate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Anadolu University
Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-? type 1 receptor inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
China Pharmaceutical University
Design, synthesis and biological evaluation of N-hydroxy-aminobenzyloxyarylamide analogues as novel selective ? opioid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Achiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5956-5971 (2020)
The University of Queensland
Synthesis, biochemical evaluation, and molecular modeling of organophosphate-coumarin hybrids as potent and selective butyrylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
California State University
New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Sapienza University of Rome
N-alkylpiperidine carbamates as potential anti-Alzheimer's agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 197: (2020)
University of Ljubljana
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6225-6237 (2020)
Westf£Lische Wilhelms-Universit£T M£Nster
Identification of the New Covalent Allosteric Binding Site of Fructose-1,6-bisphosphatase with Disulfiram Derivatives toward Glucose Reduction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6238-6247 (2020)
Central China Normal University
Design, synthesis and biological activity of novel 2,3,4,5-tetra-substituted thiophene derivatives as PI3K? inhibitors with potent antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 197: (2020)
Guizhou Medical University
Design, synthesis and biological evaluation of novel naturally-inspired multifunctional molecules for the management of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Indian Institute of Technology (Banaras Hindu University)
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5763-5782 (2020)
Universit£
Therapeutic potential of targeting ?/?-Hydrolase domain-containing 6 (ABHD6).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Sichuan University
Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jouf University
Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sungkyunkwan University
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4978-4996 (2020)
University of Toronto
Discovery of Potent, Selective, and State-Dependent Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6107-6133 (2020)
Lupin
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5477-5487 (2020)
Icahn School of Medicine At Mount Sinai
Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Antimicrob Agents Chemother 64: (2020)
Institut Pasteur Korea
Learning Molecular Representations for Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8705-8722 (2020)
University of California
Heterodimeric Analogues of the Potent Y1R Antagonist 1229U91, Lacking One of the Pharmacophoric C-Terminal Structures, Retain Potent Y1R Affinity and Show Improved Selectivity over Y4R.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5274-5286 (2020)
Monash University (Parkville Campus)
Structural Specificity of Flavonoids in the Inhibition of Human Fructose 1,6-Bisphosphatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1541-1552 (2020)
University of Porto
Phenyl(thio)phosphon(amid)ate Benzenesulfonamides as Potent and Selective Inhibitors of Human Carbonic Anhydrases II and VII Counteract Allodynia in a Mouse Model of Oxaliplatin-Induced Neuropathy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5185-5200 (2020)
University of Florence
Exploring tryptamine conjugates as pronucleotides of phosphate-modified 7-methylguanine nucleotides targeting cap-dependent translation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Warsaw
Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
National Research Centre
Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 198: (2020)
Beijing University of Chemical Technology
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6727-6740 (2020)
Goethe-University Frankfurt
Design and synthesis of 1,3-benzothiazinone derivatives as potential anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Lanzhou University
Synthesis of morpholine derivatives using the Castagnoli-Cushman reaction as BACE1 inhibitors: Unexpected binding activity of cyclic thioamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Florence
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Nature 583: 459-468 (2020)
Qbi Covid-19 Research Group (Qcrg)
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5421-5441 (2020)
East China Normal University
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4867-4879 (2020)
Purdue University
Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1461-1472 (2020)
Taipei Chang Gung Memorial Hospital
Discovery of Novel Fungal Lanosterol 14?-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5341-5359 (2020)
Second Military Medical University
Discovery of novel, potent, and orally bioavailable pyrido[2,3-d][1]benzazepin-6-one antagonists for parathyroid hormone receptor 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Daiichi Sankyo
Secondary metabolites from Isodon ternifolius (D. Don) Kudo and their anticancer activity as DNA topoisomerase IB and Tyrosyl-DNA phosphodiesterase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Sun Yat-Sen University
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6164-6178 (2020)
University of Bonn
Discovery of novel TNNI3K inhibitor suppresses pyroptosis and apoptosis in murine myocardial infarction injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 197: (2020)
Sichuan University and Collaborative Innovation Center
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-?-d-Ribose Oxidase (DprE1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5367-5386 (2020)
University of Antwerp
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5526-5567 (2020)
National Institute of Neurological Disorders and Stroke
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universit£
Design and synthesis of novel pyrrolo[2,3-b]pyridine derivatives targeting ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Research Centre (Nrc Id: 60014618)
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Synthesis and Biochemical Evaluation of Noncyclic Nucleotide Exchange Proteins Directly Activated by cAMP 1 (EPAC1) Regulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5159-5184 (2020)
University of Texas Medical Branch
Emerging targets and potential therapeutic agents in non-alcoholic fatty liver disease treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 197: (2020)
Sichuan University
Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4997-5010 (2020)
TBA
Treating Cancer by Spindle Assembly Checkpoint Abrogation: Discovery of Two Clinical Candidates, BAY 1161909 and BAY 1217389, Targeting MPS1 Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8025-8042 (2020)
Bayer
Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5488-5500 (2020)
University of Bath
Cytotoxicity of 4-substituted quinoline derivatives: Anticancer and antileishmanial potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Universidade De Mogi Das Cruzes (Umc)
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Phenex Pharmaceuticals
The discovery of diazetidinyl diamides as potent and reversible inhibitors of monoacylglycerol lipase (MAGL).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Phenex Pharmaceuticals
Substituted benzyloxytricyclic compounds as retinoic acid-related orphan receptor gamma t (ROR?t) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol Myers Squibb
Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 197: (2020)
University of Colorado Anschutz Medical Campus
Monovalent protein-degraders - Insights and future perspectives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Cedilla Therapeutics
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Recent developments of small molecules targeting RNA m![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 196: (2020)
China Pharmaceutical University
Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4957-4977 (2020)
Firmenich
Positional Analogue Scanning: An Effective Strategy for Multiparameter Optimization in Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8956-8976 (2020)
TBA
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a Diaminotriazole Core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5324-5340 (2020)
Yale University
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5458-5476 (2020)
Chinese Academy of Medical Sciences & Peking Union Medical College
An aza-nucleoside, fragment-like inhibitor of the DNA repair enzyme alkyladenine glycosylase (AAG).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Surrey
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidines as atypical protein kinase C inhibitors to control retinal vascular permeability and cytokine-induced edema.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Michigan
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kyung Hee University
Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Latvian Institute of Organic Synthesis
Purine/purine isoster based scaffolds as new derivatives of benzamide class of HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 196: (2020)
Taipei Medical University
p62/SQSTM1, a Central but Unexploited Target: Advances in Its Physiological/Pathogenic Functions and Small Molecular Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10135-10157 (2020)
China Pharmaceutical University
Structure-based design of antiviral drug candidates targeting the SARS-CoV-2 main protease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Science 368: 1331-1335 (2020)
Shanghai Institute of Materia Medica
Design of Hydrazide-Bearing HDACIs Based on Panobinostat and Their p53 and FLT3-ITD Dependency in Antileukemia Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5501-5525 (2020)
Ocean University of China
Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5212-5241 (2020)
University of Strathclyde
Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8977-9002 (2020)
Shandong First Medical University & Shandong Academy of Medical Sciences
Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Central South University
Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5139-5158 (2020)
Dongguk University-Seoul
The Oxidation of Phytocannabinoids to Cannabinoquinoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1711-1715 (2020)
Universit£
Discovery, Structure-Activity Relationship, and Biological Activity of Histone-Competitive Inhibitors of Histone Acetyltransferases P300/CBP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4716-4731 (2020)
Avera Institute For Human Genetics
Aromatic Esters of the Crinane Amaryllidaceae Alkaloid Ambelline as Selective Inhibitors of Butyrylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1359-1367 (2020)
University of Defence
Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for ?-secretase modulators with oral efficacy against cognitive deficits in Alzheimer's disease model mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Astellas Pharma
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Discovery of novel heat shock protein (Hsp90) inhibitors based on luminespib with potent antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Seoul National University
Design and discovery of boronic acid drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Mcgill University
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5398-5420 (2020)
Rapt Therapeutics
Triazolo-Peptidomimetics: Novel Radiolabeled Minigastrin Analogs for Improved Tumor Targeting.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4484-4495 (2020)
Eth Zurich
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4824-4836 (2020)
University of Washington
First Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4528-4554 (2020)
Northwestern University
A Chemical Switch for Transforming a Purine Agonist for Toll-like Receptor 7 to a Clinically Relevant Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4776-4789 (2020)
Csir-Indian Institute of Chemical Biology
Evaluation of nitrocatechol chalcone and pyrazoline derivatives as inhibitors of catechol-O-methyltransferase and monoamine oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
North-West University
Discovery of ? opioid receptor full agonists lacking a basic nitrogen atom and their antidepressant-like effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kitasato University
Induction of enantio-selective apoptosis in human leukemia HL-60 cells by (S)-erypoegin K, an isoflavone isolated from Erythrina poeppigiana.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Meijo University
Dihydrofolate reductase inhibitors for use as antimicrobial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Sichuan University
Novel Human Neutral Sphingomyelinase 2 Inhibitors as Potential Therapeutics for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6028-6056 (2020)
Czech Academy of Sciences
Naphthacemycins from a ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1394-1399 (2020)
Hebei Medical University
Discovery and Structure-Activity Relationship Study of (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4880-4895 (2020)
Dana-Farber Cancer Institute
Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4506-4516 (2020)
Universit£
Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4790-4810 (2020)
Shandong University
Structure-Activity Relationship of SPOP Inhibitors against Kidney Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4849-4866 (2020)
Chinese Academy of Sciences
Mechanism of Action of an EPAC1-Selective Competitive Partial Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4762-4775 (2020)
University of Texas Medical Branch
Flexible diaminodihydrotriazine inhibitors of Plasmodium falciparum dihydrofolate reductase: Binding strengths, modes of binding and their antimalarial activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
National Center For Genetic Engineering and Biotechnology (Biotec)
Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4837-4848 (2020)
Shandong University
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 582-588 (2020)
Merck
Efficacy and Tolerability of Pyrazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 558-565 (2020)
The Genomics Institute of The Novartis Research Foundation
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 550-557 (2020)
Merck
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 541-549 (2020)
Genentech
Quantitative Proteomics Reveals Cellular Off-Targets of a DDR1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 535-540 (2020)
Jinan University
Discovery of [1,2,4]Triazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 528-534 (2020)
Teijin Pharma
Synthesis and Evaluation of Noncovalent Naphthalene-Based KEAP1-NRF2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 521-527 (2020)
University of Illinois At Chicago
Catching a Moving Target: Comparative Modeling of Flaviviral NS2B-NS3 Reveals Small Molecule Zika Protease Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 514-520 (2020)
Freie Universit£T Berlin
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 506-513 (2020)
Gilead Sciences
Discovery and Optimization of wt-RET/KDR-Selective Inhibitors of RET![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 497-505 (2020)
University of Manchester
Accelerated Discovery of Novel Ponatinib Analogs with Improved Properties for the Treatment of Parkinson's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 491-496 (2020)
University of Oxford
Discovery of CNS-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 485-490 (2020)
Biogen
Discovery and Pharmacokinetics of Sulfamides and Guanidines as Potent Human Arginase 1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 433-438 (2020)
Oncoarendi Therapeutics
Ahp-Cyclodepsipeptide Inhibitors of Elastase: Lyngbyastatin 7 Stability, Scalable Synthesis, and Focused Library Analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 419-425 (2020)
University of Florida
Selective Estrogen Receptor Degraders for the Potential Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 412-413 (2020)
Usona Institute
Bifunctional Pyrimidines as Modulators of Focal Adhesion Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 409-411 (2020)
Usona Institute
Cereblon Based Immunomodulatory Therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 407-408 (2020)
Usona Institute
Discovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4685-4700 (2020)
Central South University
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Shanghai Institute of Materia Medica
Both d- and l-Glucose Polyphosphates Mimic d-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5442-5457 (2020)
University of Oxford
Design, Synthesis, and Biological Evaluation of New Peripheral 5HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4171-4182 (2020)
Gwangju Institute of Science and Technology
Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
North-West University
A medicinal chemistry perspective of drug repositioning: Recent advances and challenges in drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
University of Bonn
Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor ? (ER?) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Wuhan University
A novel class of selective CK2 inhibitors targeting its open hinge conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
University of Trento
hERG toxicity assessment: Useful guidelines for drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Normandie Univ
Ene-yne Hydroquinones from a Marine-derived Strain of the Fungus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1258-1264 (2020)
Chinese Academy of Sciences
Discovery and Optimization of Glucose Uptake Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5201-5211 (2020)
Kadmon
Design and Synthesis of Bitopic 2-Phenylcyclopropylmethylamine (PCPMA) Derivatives as Selective Dopamine D3 Receptor Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4579-4602 (2020)
Shanghaitech University
Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Astellas Pharma
Screening of chalcone analogs with anti-depressant, anti-inflammatory, analgesic, and COX-2-inhibiting effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
China-Japan Union Hospital of Jilin University
Chalcones bearing a 3,4,5-trimethoxyphenyl motif are capable of selectively inhibiting oncogenic K-Ras signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Wright State University
MymA Bioactivated Thioalkylbenzoxazole Prodrug Family Active against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4732-4748 (2020)
Glaxosmithkline
Synthesis and biological evaluation of heterocyclic bis-aryl amides as novel Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jiangnan University
Ansamycin derivatives from the marine-derived Streptomyces sp. SCSGAA 0027 and their cytotoxic and antiviral activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
South China Sea Institute of Oceanology
Influence of side-chain changes on histone deacetylase inhibitory and cytotoxicity activities of curcuminoid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Khon Kaen University
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors ![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nature 582: 289-293 (2020)
Shanghaitech University
Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPAR? activation and on growth of imatinib-resistant chronic myelogenous leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
University of Innsbruck
Discovery of orally active indirubin-3'-oxime derivatives as potent type 1 FLT3 inhibitors for acute myeloid leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 195: (2020)
Gwangju Institute of Science and Technology
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4334-4348 (2020)
Medical College of Wisconsin
A Selective Modulator of Peroxisome Proliferator-Activated Receptor ? with an Unprecedented Binding Mode.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4555-4561 (2020)
Goethe-University Frankfurt
Discovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4701-4715 (2020)
Shandong University
Molecule Property Analyses of Active Compounds for ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 8917-8955 (2020)
Russian Academy of Science
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5242-5256 (2020)
University of Texas Medical Branch
PTP1B-Inhibiting Branched-Chain Fatty Acid Dimers from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1598-1610 (2020)
University of Copenhagen
Advances in the Development of Phosphodiesterase-4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 10594-10617 (2020)
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Sci Transl Med 12: 1-15 (2020)
University of North Carolina At Chapel Hill
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Pfizer
Identification of the Clinical Development Candidate ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6679-6693 (2020)
Array Biopharma
Interrogating the Lactate Dehydrogenase Tetramerization Site Using (Stapled) Peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4628-4643 (2020)
Universit£
S1P![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Peking Union Medical College and Chinese Academy of Medical Sciences
Identification of a new class of non-electrophilic TRPA1 agonists by a structure-based virtual screening approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kyoto University
In silico and in vitro studies on interaction of novel non-imidazole histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jagiellonian University Medical College
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4929-4956 (2020)
University of Washington
Discovery of new LXR? agonists as glioblastoma inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Sun Yat-Sen University
Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Annamalai University
Chemical puzzles in the search for new, flexible derivatives of lurasidone as antipsychotic drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Cracow University of Technology
A chemically stable peptide agonist to neuromedin U receptor type 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Tokyo University of Pharmacy and Life Sciences
Finding the mechanism of esterase D activation by a small molecule.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shandong University
Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tongji University
Environment-sensitive fluorescent inhibitors of histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shandong University
A potent photoreactive general anesthetic with novel binding site selectivity for GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
University of Illinois At Chicago
New CDK8 inhibitors as potential anti-leukemic agents - Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Nord University
Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4293-4305 (2020)
Dana-Farber Cancer Institute
New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Universit£
Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Nanyang Normal University
Fragment-Based Design of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4749-4761 (2020)
University of Cambridge
Furofuranone Lignans from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1424-1431 (2020)
Universidad Aut£Noma Del Estado De Morelos
Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Iowa
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4133-4154 (2020)
University of Regensburg
Rationally Designed Small-Molecule Inhibitors Targeting an Unconventional Pocket on the TLR8 Protein-Protein Interface.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4117-4132 (2020)
The University of Tokyo
Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Shenyang Pharmaceutical University
Use of Non-Natural Amino Acids for the Design and Synthesis of a Selective, Cell-Permeable MALT1 Activity-Based Probe.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3996-4004 (2020)
Ku Leuven
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1092-1098 (2020)
University of Mississippi
Design, synthesis and biological evaluation of novel N-[4-(2-fluorophenoxy)pyridin-2-yl]cyclopropanecarboxamide derivatives as potential c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
College of Pharmacy of Liaoning University
Matrix metalloproteinase-9 (MMP-9) and its inhibitors in cancer: A minireview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Jadavpur University
Multistep Binding of the Non-Steroidal Inhibitors Orteronel and Seviteronel to Human Cytochrome P450 17A1 and Relevance to Inhibition of Enzyme Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6513-6522 (2020)
Vanderbilt University School of Medicine
Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4315-4333 (2020)
Vanderbilt University
Discovery of Selective Small Molecule Degraders of BRAF-V600E.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4069-4080 (2020)
Cullgen
Small-Molecule Antagonist Targeting Exportin-1 via Rational Structure-Based Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3881-3895 (2020)
Dalian University of Technology
Tellurides Bearing Sulfonamides as Novel Inhibitors of Leishmanial Carbonic Anhydrase with Potent Antileishmanial Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4306-4314 (2020)
University of Florence
Design, synthesis and biological evaluation of 1H-pyrazolo [3,4-d]pyrimidine derivatives as PAK1 inhibitors that trigger apoptosis, ER stress and anti-migration effect in MDA-MB-231 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Sichuan University
Antitumor activity and structure-activity relationship of heparanase inhibitors: Recent advances.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Guangzhou University of Chinese Medicine
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Fujian Medical University (Fmu)
N-benzyl 4,4-disubstituted piperidines as a potent class of influenza H1N1 virus inhibitors showing a novel mechanism of hemagglutinin fusion peptide interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Instituto De Qu£Mica M£Dica (C.S.I.C.)
Study on chemical modification and analgesic activity of N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl) piperazine-1-carboxamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 194: (2020)
Henan University
Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
China Pharmaceutical University
Modulating Heparanase Activity: Tuning Sulfation Pattern and Glycosidic Linkage of Oligosaccharides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4227-4255 (2020)
Wayne State University
Discovery of a Potent and Selective NF-?B-Inducing Kinase (NIK) Inhibitor That Has Anti-inflammatory Effects in Vitro and in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4388-4407 (2020)
Chinese Academy of Sciences
Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3935-3955 (2020)
Arcus Biosciences
Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4256-4292 (2020)
National Center For Advancing Translational Sciences
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3915-3934 (2020)
Karolinska Institutet
Design, synthesis & biological evaluation of ferulic acid-based small molecule inhibitors against tumor-associated carbonic anhydrase IX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jamia Millia Islamia
The signal peptide as a new target for drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Nevada
Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Andhra University
2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3908-3914 (2020)
Cha University
CN128: A New Orally Active Hydroxypyridinone Iron Chelator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4215-4226 (2020)
Zhejiang University
Discovery of 8-Methyl-pyrrolo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3956-3975 (2020)
Chinese Academy of Sciences
Structure-activity relationships of triazole-benzodioxine inhibitors of cathepsin X.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
University of Ljubljana
Small molecule inhibitors of I?B kinase ?: A chip-based screening and molecular docking simulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kangwon National University
Anti-inflammatory effect and inhibition of nitric oxide production by targeting COXs and iNOS enzymes with the 1,2-diphenylbenzimidazole pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Instituto Polit£Cnico Nacional
Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Universit£
Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Shenyang Pharmaceutical University
Tail approach synthesis of novel benzenesulfonamides incorporating 1,3,4-oxadiazole hybrids as potent inhibitor of carbonic anhydrase I, II, IX, and XII isoenzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Kurukshetra University
Development of potent inhibitors of the human microsomal epoxide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
University of California Davis
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4183-4204 (2020)
Japanese Foundation For Cancer Research
GSK2818713, a Novel Biphenylene Scaffold-Based Hepatitis C NS5A Replication Complex Inhibitor with Broad Genotype Coverage.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4155-4170 (2020)
Glaxosmithkline
Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4107-4116 (2020)
Bicycletx
Exploration of Fragment Binding Poses Leading to Efficient Discovery of Highly Potent and Orally Effective Inhibitors of FABP4 for Anti-inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4090-4106 (2020)
Chinese Academy of Sciences
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4349-4369 (2020)
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
High throughput in vivo phenotypic screening for drug repurposing: Discovery of MLR-1023 a novel insulin sensitizer and novel Lyn kinase activator with clinical proof of concept.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Melior Discovery
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Liaocheng University
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Shanghai Pharmaceuticals Holding
Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Beijing Institute of Technology
Structure-based discovery of novel 4-(2-fluorophenoxy)quinoline derivatives as c-Met inhibitors using isocyanide-involved multicomponent reactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Harbin Institute of Technology
Discovery of novel pyrrole derivatives as potent agonists for the niacin receptor GPR109A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Daiichi Sankyo
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Tennessee Health Science Center
Design, synthesis, and biological activity of new endomorphin analogs with multi-site modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Lanzhou University
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
University of Regensburg
Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved ?-ketoamide inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Science 368: 409-412 (2020)
University of Lubeck
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Messina
Prenylated Phenolic Compounds from the Aerial Parts of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 814-824 (2020)
Peking University
Design, Synthesis, Dynamic Docking, Biochemical Characterization, and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3508-3521 (2020)
Istituto Italiano Di Tecnologia
Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3485-3507 (2020)
University of Antwerp
p62 as a therapeutic target for tumor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
China Pharmaceutical University
Discovery of cyclic guanidine-linked sulfonamides as inhibitors of LMTK3 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
San Diego State University
Novel quinolin-4(1H)-one derivatives as multi-effective aldose reductase inhibitors for treatment of diabetic complications: Synthesis, biological evaluation, and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Institute of Technology
-Acylethanolamine Acid Amidase (NAAA): Structure, Function, and Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7475-7490 (2020)
University of California
LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3763-3783 (2020)
University of Kentucky
Structure-Functional-Selectivity Relationship Studies of Novel Apomorphine Analogs to Develop D1R/D2R Biased Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 385-392 (2020)
Duke University
Design and Optimization of 3'-(Imidazo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 379-384 (2020)
Jinan University
Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 371-378 (2020)
University of Pennsylvania
Development of a Versatile and Sensitive Direct Ligand Binding Assay for Human NR5A Nuclear Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 365-370 (2020)
Emory University
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 358-364 (2020)
Gilead Sciences
Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 346-352 (2020)
Dana-Farber Cancer Institute
SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 340-345 (2020)
University of North Carolina At Chapel Hill (Unc-Ch)
An Alkyne-functionalized Arginine for Solid-Phase Synthesis Enabling "Bioorthogonal" Peptide Conjugation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 334-339 (2020)
University of Regensburg
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 327-333 (2020)
Genentech
Regioisomeric Family of Novel Fluorescent Substrates for SHIP2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 309-315 (2020)
School of Biological Sciences, Uea
Spiro-oxindole Piperidines and 3-(Azetidin-3-yl)-1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 303-308 (2020)
Division of Janssen-Cilag
Design of Dual Inhibitors of Soluble Epoxide Hydrolase and LTA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 298-302 (2020)
Goethe University Frankfurt
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 272-277 (2020)
University of Minnesota
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 266-271 (2020)
Bristol-Myers Squibb Research & Development
Selective CDK6 degradation mediated by cereblon, VHL, and novel IAP-recruiting PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Fudan University
Design, synthesis and bioactivity study of N-salicyloyl tryptamine derivatives as multifunctional agents for the treatment of neuroinflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Lanzhou University
Metabolic and Pharmaceutical Aspects of Fluorinated Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6315-6386 (2020)
Bristol Myers Squibb
Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 193: (2020)
Shanghaitech University
Synthesis and pharmacokinetic study of a ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Harvard Medical School
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3634-3664 (2020)
University of Illinois At Chicago
Discovery of 4-arylquinoline-2-carboxamides, highly potent and selective class of mGluR2 negative allosteric modulators: From HTS to activity in animal models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Lead discovery, chemical optimization, and biological evaluation studies of novel histone methyltransferase SET7 small-molecule inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Chinese Academy of Sciences
Design, synthesis and biological evaluation of 4-(pyridin-4-yloxy)benzamide derivatives bearing a 5-methylpyridazin-3(2H)-one fragment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jiangxi Science & Technology Normal University
A new series of aryl sulfamate derivatives: Design, synthesis, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Sharjah
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Changzhou University
Design and synthesis of selective degraders of EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Jinan University
Design, synthesis, and evaluation of N-phenyl-4-(2-phenylsulfonamido)-benzamides as microtubule-targeting agents in drug-resistant cancer cells, displaying HDAC inhibitory response.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Taipei Medical University
Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
China Pharmaceutical University
Development of bivalent triarylalkene- and cyclofenil-derived dual estrogen receptor antagonists and downregulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
University of Innsbruck
Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of The Western Cape
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Universit£
Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Jadavpur University
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Xihua University
Antiausterity Activity of Secondary Metabolites from the Roots of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1099-1106 (2020)
University of Innsbruck
Anti-inflammatory Metabolites from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 881-887 (2020)
Korea University
TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3665-3677 (2020)
East China Normal University
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3701-3712 (2020)
University of Perugia
Investigation of Inactive-State ? Opioid Receptor Homodimerization via Single-Molecule Microscopy Using New Antagonistic Fluorescent Probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3596-3609 (2020)
Julius Maximilian University of W£Rzburg
Discovery of pyrazole derivatives as cellular active inhibitors of histone lysine specific demethylase 5B (KDM5B/JARID1B).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Zhengzhou University
Discovery of Thieno[2,3-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3678-3700 (2020)
Sichuan University and Collaborative Innovation Center of Biotherapy
Synthesis and biological evaluation of acridine-based histone deacetylase inhibitors as multitarget agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Taipei Medical University
Design, synthesis and biological evaluation of novel indazole-based derivatives as potent HDAC inhibitors via fragment-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Jiangsu Key Laboratory For Functional Substance of Chinese Medicine
Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3047-3065 (2020)
Universit£
Bicyclic ?-Iminophosphonates as High Affinity Imidazoline I![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3610-3633 (2020)
University of Barcelona
Bioactive Azepine-Indole Alkaloids from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 852-863 (2020)
Universidade Federal Do Rio Grande Do Sul-Ufrgs
Discovery of Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-?-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7491-7507 (2020)
Qpex Biopharma
CDK7 Inhibitors in Cancer Therapy: The Sweet Smell of Success?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7458-7474 (2020)
Lebanese American University
Synthesis of multimeric pyrrolidine iminosugar inhibitors of human ?-glucocerebrosidase and ?-galactosidase A: First example of a multivalent enzyme activity enhancer for Fabry disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Universidad De Sevilla
Design and synthesis of tripeptidyl furylketones as selective inhibitors against the ?5 subunit of human 20S proteasome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Peking University Health Science Center
Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Guizhou Medical University
Comparative analysis of the dual EGFR-DNA targeting and growth inhibitory properties of 6-mono-alkylamino- and 6,6-dialkylaminoquinazoline-based type II combi-molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
The Research Institute of The Mcgill University Health Center/Glen Hospital
Design and synthesis of novel 2-arylbenzimidazoles as selective mutant isocitrate dehydrogenase 2 R140Q inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shandong Provincial Hospital Affiliated To Shandong University
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3215-3226 (2020)
Takeda Pharmaceutical
Medicinal Chemistry of Inhibiting RING-Type E3 Ubiquitin Ligases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 7957-7985 (2020)
Genentech
Distribution of Bibenzyls, Prenyl Bibenzyls, Bis-bibenzyls, and Terpenoids in the Liverwort Genus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 756-769 (2020)
Tokushima Bunri University
Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3577-3595 (2020)
University of Copenhagen
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jiangsu Aosaikang Pharmaceutical
Identification of Potent ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3188-3204 (2020)
The University of Tokyo
Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2915-2929 (2020)
Janssen Research and Development
Discovery and Development of Small-Molecule Inhibitors of Glycogen Synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3538-3551 (2020)
Indiana University School of Medicine
The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Nanyang Normal University
Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6648-6676 (2020)
Celgene
Discovery and SARs of 5-Chloro-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3327-3347 (2020)
Anhui Medical University
Novel class of benzimidazole-thiazole hybrids: The privileged scaffolds of potent anti-inflammatory activity with dual inhibition of cyclooxygenase and 15-lipoxygenase enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Assiut University
Repurposed drug candidates for antituberculosis therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Sichuan University
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3298-3316 (2020)
Texas A&M University
Calorimetric Studies of Binary and Ternary Molecular Interactions between Transthyretin, A? Peptides, and Small-Molecule Chaperones toward an Alternative Strategy for Alzheimer's Disease Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3205-3214 (2020)
Institut De Qu??Mica Avan£Ada De Catalunya (I.Q.A.C.-C.S.I.C.)
Design and synthesis of dansyl-labeled inhibitors of steroid sulfatase for optical imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chu De Qu£Bec - Research Center
Discovery and optimization of 2-aminopyridine derivatives as novel and selective JAK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
East China University of Science & Technology
Design and synthesis of potent PAR-1 antagonists based on vorapaxar.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Hebei University of Technology
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Chinese Academy of Sciences
Substituted 1-methyl-4-phenylpyrrolidin-2-ones - Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Monash University (Parkville Campus)
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
China Pharmaceutical University
Discovery of Acylsulfonohydrazide-Derived Inhibitors of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-Inducing Anti-Cancer Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4655-4684 (2020)
Monash University (Parkville Campus)
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3370-3380 (2020)
Guangzhou University of Chinese Medicine
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Zhejiang University
Discovery of sulfonamides and 9-oxo-2,8-diazaspiro[5,5]undecane-2-carboxamides as human kynurenine aminotransferase 2 (KAT2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Orion Pharma
Discovery of 4-((1-(1H-imidazol-2-yl)alkoxy)methyl)pyridines as a new class of Trypanosoma cruzi growth inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Irbm
Discovery of 1,6-naphthyridinone-based MET kinase inhibitor bearing quinoline moiety as promising antitumor drug candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
China Pharmaceutical University
Activity-based protein profiling: Recent advances in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Sichuan University
Overview of cannabidiol (CBD) and its analogues: Structures, biological activities, and neuroprotective mechanisms in epilepsy and Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 192: (2020)
Shaanxi University of Science & Technology
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3348-3358 (2020)
Glaxosmithkline
Identification of C10 nitrogen-containing aporphines with dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
City University of New York
The discovery, design and synthesis of potent agonists of adenylyl cyclase type 2 by virtual screening combining biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Chinese Academy of Sciences
Novel pyrrolidinone derivative lacks claimed histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Heinrich Heine University D£Sseldorf
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Jagiellonian University Medical College
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
University of Regensburg
Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2894-2914 (2020)
Monash University
Substituent Position of Iminocyclitols Determines the Potency and Selectivity for Gut Microbial Xenobiotic-Reactivating Enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4617-4627 (2020)
Academia Sinica
Dimerization of ?-Conotoxins as a Strategy to Enhance the Inhibition of the Human ?7 and ?9?10 Nicotinic Acetylcholine Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2974-2985 (2020)
Ocean University of China
Diterpenoids from the Root Bark of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 1229-1237 (2020)
Chinese Academy of Sciences
One-pot synthesis of thioxo-tetrahydropyrimidine derivatives as potent ?-glucuronidase inhibitor, biological evaluation, molecular docking and molecular dynamics studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shiraz University of Medical Sciences
Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
China Pharmaceutical University
Novel ?- and ?-Amino Acid-Derived Inhibitors of Prostate-Specific Membrane Antigen.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3261-3273 (2020)
Korea University
Effective Application of Metabolite Profiling in Drug Design and Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6387-6406 (2020)
Pfizer
Evolution of a 4-Benzyloxy-benzylamino Chemotype to Provide Efficacious, Potent, and Isoform Selective PPAR? Agonists as Leads for Retinal Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2854-2876 (2020)
University of Oklahoma
Novel cilengitide-based cyclic RGD peptides as ?v?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Division of Organic Chemistry Csir-National Chemical Laboratory (Ncl)
Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
University of Szeged
Development of small molecule inhibitors targeting TGF-? ligand and receptor: Structures, mechanism, preclinical studies and clinical usage.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Minzu University of China
Recent advances in the development of ubiquitin-specific-processing protease 7 (USP7) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Zhengzhou University
Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3227-3237 (2020)
Moffitt Cancer Center
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Janssen Research & Development
DNA sequence-specific ligands. XVIII. Synthesis, physico-chemical properties; genetic, virological, and biochemical studies of fluorescent dimeric bisbenzimidazoles DBPA(n).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Russian Academy of Sciences
Design, synthesis and evaluation of flurbiprofen-clioquinol hybrids as multitarget-directed ligands against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Guizhou Medical University
Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Southwest Jiaotong University
Design, synthesis and biological evaluation of 2,3-dihydro-5,6-dimethoxy-1H-inden-1-one and piperazinium salt hybrid derivatives as hAChE and hBuChE enzyme inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
University of Tabriz
Progress in 11?-HSD1 inhibitors for the treatment of metabolic diseases: A comprehensive guide to their chemical structure diversity in drug development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Hong Kong Baptist University
Design, synthesis and anticancer activities of novel dual poly(ADP-ribose) polymerase-1/histone deacetylase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Hefei University of Technology
Discovery of novel hydroxyamidine derivatives as indoleamine 2,3-dioxygenase 1 inhibitors with in vivo anti-tumor efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Fudan University
Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Takeda Pharmaceutical
Computational discovery and biological evaluation of novel inhibitors targeting histone-lysine N-methyltransferase SET7.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Piperidine propionamide as a scaffold for potent sigma-1 receptor antagonists and mu opioid receptor agonists for treating neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Huazhong University of Science and Technology
Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
University of Belgrade
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Sussex
Synthesis, biological evaluation and molecular modeling study of [1,2,4]-Triazolo[4,3-c]quinazolines: New class of EGFR-TK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Mansoura University
Discovery of 4,6-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2877-2893 (2020)
Hubei University of Technology
Isolation and Structural Characterization of Specific Bacterial ?-Glucuronidase Inhibitors from Noni (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 825-833 (2020)
Wayne State University
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5102-5118 (2020)
TBA
Design, synthesis and identification of N, N-dibenzylcinnamamide (DBC) derivatives as novel ligands for ?-synuclein fibrils by SPR evaluation system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Fudan University
Discovery and Optimization of Novel Pyrazolopyrimidines as Potent and Orally Bioavailable Allosteric HIV-1 Integrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2620-2637 (2020)
Bristol-Myers Squibb Research and Development
Structurally novel PI3K?/? dual inhibitors characterized by a seven-membered spirocyclic spacer: The SARs investigation and PK evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 191: (2020)
Anhui University of Chinese Medicine
Inhibition of striatal-enriched protein tyrosine phosphatase by targeting computationally revealed cryptic pockets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Shandong University
Targeting different binding sites in the CFTR structures allows to synergistically potentiate channel activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Universit£
Synthesis and Biological Evaluation of Tryptamines Found in Hallucinogenic Mushrooms: Norbaeocystin, Baeocystin, Norpsilocin, and Aeruginascin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 461-467 (2020)
Usona Institute
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2958-2973 (2020)
Genomics Institute of The Novartis Research Foundation (Gnf)
Discovery of 4-((2 S,4 S)-4-Ethoxy-1-((5-methoxy-7-methyl-1 H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5697-5722 (2020)
Novartis Institutes For Biomedical Research
DNA-Encoded Library Technology-Based Discovery, Lead Optimization, and Prodrug Strategy toward Structurally Unique Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3552-3562 (2020)
Glaxosmithkline
Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 188-194 (2020)
Novartis Institutes For Biomedical Research
Discovery of Hydroxyamidine Based Inhibitors of IDO1 for Cancer Immunotherapy with Reduced Potential for Glucuronidation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 179-187 (2020)
Phenex Pharmaceuticals
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 172-178 (2020)
Bristol-Myers Squibb Research & Development
Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 166-171 (2020)
Korea Research Institute of Chemical Technology
Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 141-146 (2020)
Baylor University
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 133-140 (2020)
Glaxosmithkline
Discovery of 4-Piperazine Isoquinoline Derivatives as Potent and Brain-Permeable Tau Prion Inhibitors with CDK8 Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 127-132 (2020)
University of California
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as ROR??t Allosteric Inhibitors for Autoimmune Diseases![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 114-119 (2020)
Merck
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 101-107 (2020)
Agios Pharmaceuticals
Negative allosteric modulators of the GluN2B NMDA receptor with phenylethylamine structure embedded in ring-expanded and ring-contracted scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Serendipitous Discovery of Leucine and Methionine Depletion Agents during the Search for Polyamine Transport Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2814-2832 (2020)
University of Central Florida
Design, Synthesis, and Biological Evaluation of Imidazo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3028-3046 (2020)
East China Normal University
Optimization of 4-Aminopiperidines as Inhibitors of Influenza A Viral Entry That Are Synergistic with Oseltamivir.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3120-3130 (2020)
University of Illinois At Chicago
Dual Binding to Orthosteric and Allosteric Sites Enhances the Anticancer Activity of a TRAP1-Targeting Drug.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2930-2940 (2020)
Ulsan National Institutes of Science and Technology (Unist)
A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring N![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Fudan University
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Pennsylvania
The cell division protein FtsZ as a cellular target to hit cystic fibrosis pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
University of Pavia
Allosteric inhibitors of the STAT3 signaling pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
West China Second University Hospital
Discovery and development of plasma kallikrein inhibitors for multiple diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Hefei University of Technology
Design, synthesis and evaluation of unnatural peptides as T1R2/T1R3 PAMs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Ajinomoto
Recent advances in TRPV4 agonists and antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Glaxosmithkline
Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Zhejiang University
Multi-step parallel synthesis enabled optimization of benzofuran derivatives as pan-genotypic non-nucleoside inhibitors of HCV NS5B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Unexpected small molecules as novel SIRT2 suicide inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Engineering Research Center For The Development and Application of Ethnic Medicine and Tcm (Ministry of Education)
Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Georgia Institute of Technology
Yanhusanines A-F, Isoquinoline-Derived Alkaloid Enantiomers from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 489-496 (2020)
Chinese Academy of Medical Sciences and Peking Union Medical College
Blocking the CGRP Pathway for Acute and Preventive Treatment of Migraine: The Evolution of Success.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6600-6623 (2020)
Biohaven Pharmaceuticals
Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
The Key Laboratory of Chemistry For Natural Products of Guizhou Province and Chinese Academy of Sciences
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Taipei Medical University
Design, synthesis and biological activity of N![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Peking University
Discovery and optimization of 4-oxo-2-thioxo-thiazolidinones as NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Xiamen University
Design, synthesis and biological evaluation of HIV-1 protease inhibitors with morpholine derivatives as P2 ligands in combination with cyclopropyl as P1' ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jinzhou Medical University
Novel, Self-Assembling Dimeric Inhibitors of Human ? Tryptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3004-3027 (2020)
Weill Cornell Medicine
A small molecule inhibitor of PCSK9 that antagonizes LDL receptor binding via interaction with a cryptic PCSK9 binding groove.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Nyrada
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3252-3260 (2020)
University of Oxford
The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6624-6647 (2020)
University of Perugia
Discovery of disubstituted xylylene derivatives as small molecule direct inhibitors of Keap1-Nrf2 protein-protein interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The State University of New Jersey
Discovery and structure-activity relationships of spiroindolines as novel inducers of oligodendrocyte progenitor cell differentiation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Asubio Pharma
Discovery of 2-aminoisobutyric acid ethyl ester (AIBEE) phosphoramidate prodrugs for delivering nucleoside HCV NS5B polymerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Abbvie
2-Substituted ?,?-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2941-2957 (2020)
University of Bonn
Inclusion of a 5-fluorouracil moiety in nitrogenous bases derivatives as human carbonic anhydrase IX and XII inhibitors produced a targeted action against MDA-MB-231 and T47D breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
University of Florence
STAT3 inhibitory activity of naphthoquinones isolated from Tabebuia avellanedae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kindai University
An increase in side-group hydrophobicity largely improves the potency of ritonavir-like inhibitors of CYP3A4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of California
DNA-Encoded Library Screening as Core Platform Technology in Drug Discovery: Its Synthetic Method Development and Applications in DEL Synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6578-6599 (2020)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Synthesis and Evaluation of Bicyclic Hydroxypyridones as Inhibitors of Catechol ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1573-1578 (2019)
Lieber Institute For Brain Development
Synthetic Lethality in Pancreatic Cancer: Discovery of a New RAD51-BRCA2 Small Molecule Disruptor That Inhibits Homologous Recombination and Synergizes with Olaparib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2588-2619 (2020)
Istituto Italiano Di Tecnologia
Synthesis, biological evaluation and molecular modeling study of 2-amino-3,5-disubstituted-pyrazines as Aurora kinases inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Lanzhou University
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Universit£
Inhibition of cholesteryl ester synthesis by polyacetylenes from Atractylodes rhizome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kitasato University
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb Research and Development
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1724-1749 (2020)
Lindsley F. Kimball Research Institute
Discovery of Novel Peptidomimetic Boronate ClpP Inhibitors with Noncanonical Enzyme Mechanism as Potent Virulence Blockers ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3104-3119 (2020)
Sichuan University
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3317-3326 (2020)
University of Wollongong
Antimycobacterial Rufomycin Analogues from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 657-667 (2020)
University of Illinois At Chicago
Acetylene Group, Friend or Foe in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5625-5663 (2020)
St. John'S University
The Other Angiotensin II Receptor: AT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1978-1995 (2020)
Centre Hospitalier Universitaire Vaudois (Chuv) and University of Lausanne (Unil
Sarco/Endoplasmic Reticulum Calcium ATPase Inhibitors: Beyond Anticancer Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1937-1963 (2020)
University of Chemistry and Technology Prague
Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5664-5674 (2020)
National Institute of Chemistry
Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine ?4?2 Receptor Antagonist for the Treatment of Depression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2833-2853 (2020)
Suven Life Sciences
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4468-4483 (2020)
Astrazeneca
Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5089-5099 (2020)
Chugai Pharmaceutical
BET proteins: Investigating BRDT as a potential target for male contraception.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Minnesota
Tuning melatonin receptor subtype selectivity in oxadiazolone-based analogues: Discovery of QR2 ligands and NRF2 activators with neurogenic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Consejo Superior De Investigaciones Cient�Ficas (Iqm-Csic)
Structural features and functional activities of benzimidazoles as NOD2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
University of Ljubljana
Design and synthesis of Imidazo[1,2-b]pyridazine IRAK4 inhibitors for the treatment of mutant MYD88 L265P diffuse large B-cell lymphoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
China Pharmaceutical University
Design, synthesis and biological evaluation of 1-alkyl-5/6-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-1H-indole-3-carbonitriles as novel xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 190: (2020)
Shenyang Pharmaceutical University
Protein-Induced Change in Ligand Protonation during Trypsin and Thrombin Binding: Hint on Differences in Selectivity Determinants of Both Proteins?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3274-3289 (2020)
Philipps-University Marburg
Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Hebei University
Anti-diabetic drugs recent approaches and advancements.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Mizoram University
Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jinan University
Discovery of novel akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Sichuan University
Dammarane-type leads panaxadiol and protopanaxadiol for drug discovery: Biological activity and structural modification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Shenyang Pharmaceutical University
New thiopyrimidine-benzenesulfonamide conjugates as selective carbonic anhydrase II inhibitors: synthesis, in vitro biological evaluation, and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Research Centre
A novel series of cysteine-dependent, allosteric inverse agonists of the nuclear receptor ROR?t.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Reata Pharmaceuticals
Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer
Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1576-1596 (2020)
Czech Academy of Sciences
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human ?-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2986-3003 (2020)
Icahn School of Medicine At Mount Sinai
Discovery of thieno[2,3-d]pyrimidin-4(3H)-one derivatives as a new class of ROCK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sichuan University
Optimization of 8-oxoadenines with toll-like-receptor 7 and 8 activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Montana
Synthesis and evaluation of novel radioiodinated PSMA targeting ligands for potential radiotherapy of prostate cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Beijing Normal University
Hi-JAK-ing the ubiquitin system: The design and physicochemical optimisation of JAK PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Strathclyde
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)