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Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5675-5696 (2020)
Pliant Therapeutics
Congenetic Hybrids Derived from Dearomatized Isoprenylated Acylphloroglucinol with Opposite Effects on Ca![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1709-1716 (2020)
Chinese Academy of Sciences
Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1544-1563 (2020)
Guangxi Normal University
VEGFR-2 inhibiting effect and molecular modeling of newly synthesized coumarin derivatives as anti-breast cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National Research Centre
A panoramic review of IL-6: Structure, pathophysiological roles and inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Punjabi University
Discovery of novel cyclin-dependent kinase (CDK) and histone deacetylase (HDAC) dual inhibitors with potent in vitro and in vivo anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Key Laboratory of Biomedical Materials of Natural Macromolecules (Beijing University of Chemical Technology)
Celastrol: Progresses in structure-modifications, structure-activity relationships, pharmacology and toxicology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Zhejiang University
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1684-1698 (2020)
Universit£T Bonn
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1660-1670 (2020)
TBA
Optimisation of estrogen receptor subtype-selectivity of a 4-Aryl-4H-chromene scaffold previously identified by virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Trinity College
1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Mansoura University
Structure and Activity Studies of Disulfide-Deficient Analogues of ?O-Conotoxin GeXIVA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1564-1575 (2020)
Hainan University
Aromatic-Amine Pendants Produce Highly Potent and Efficacious Mixed Efficacy ?-Opioid Receptor (MOR)/?-Opioid Receptor (DOR) Peptidomimetics with Enhanced Metabolic Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1671-1683 (2020)
University of Michigan
Design, synthesis and biological evaluation of novel pyrazole sulfonamide derivatives as dual COX-2/5-LOX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Cairo University
Identification of a 2,4-diaminopyrimidine scaffold targeting Trypanosoma brucei pteridine reductase 1 from the LIBRA compound library screening campaign.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
University of Modena and Reggio Emilia
Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Fudan University
Substituted pteridinones as p90 ribosomal S6 protein kinase (RSK) inhibitors: A structure-activity study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Colorado Anschutz Medical Campus
Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Lilly China Research and Development Center (Lcrdc)
Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Chinese Academy of Sciences
Phosphine boranes as less hydrophobic building blocks than alkanes and silanes: Structure-property relationship and estrogen-receptor-modulating potency of 4-phosphinophenol derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The University of Tokyo
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Takeda Pharmaceutical
Inhibitors of the Zika virus protease NS2B-NS3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Australian National University
Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
University of Michigan Medical School
Nostotrebin 6 Related Cyclopentenediones and ?-Lactones with Broad Activity Spectrum Isolated from the Cultivation Medium of the Cyanobacterium ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 392-400 (2020)
University of Halle-Wittenberg
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 497-504 (2020)
The University of Queensland
Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Egyptian Russian University
Synthesis, biological evaluation and in silico modeling of novel integrase strand transfer inhibitors (INSTIs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Chemical Diversity Research Institute
Natural heat shock protein 90 inhibitors in cancer and inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Oswaldo Cruz Foundation
1,3-Dipolar Cycloaddition, HPLC Enantioseparation, and Docking Studies of Saccharin/Isoxazole and Saccharin/Isoxazoline Derivatives as Selective Carbonic Anhydrase IX and XII Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2470-2488 (2020)
Sapienza University of Rome
Benzenesulfonamide Derivatives as Calcium/Calmodulin-Dependent Protein Kinase Inhibitors and Antiviral Agents against Dengue and Zika Virus Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1313-1327 (2020)
National Taiwan Normal University
?-Helix-Mimicking Sulfono-?-AApeptide Inhibitors for p53-MDM2/MDMX Protein-Protein Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 975-986 (2020)
University of South Florida
Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2489-2510 (2020)
National Institute of Chemistry
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1612-1623 (2020)
Forma Therapeutics
Isocadiolides A-H: Polybrominated Aromatics from a ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 429-437 (2020)
Seoul National University
Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1415-1433 (2020)
St. Jude Children'S Research Hospital
Unique Sulfur-Aromatic Interactions Contribute to the Binding of Potent Imidazothiazole Indoleamine 2,3-Dioxygenase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1642-1659 (2020)
National Health Research Institutes
Kinase-Inhibitory Nucleoside Derivatives from the Pacific Bryozoan ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 547-551 (2020)
Victoria University of Wellington
Design and synthesis of (E)-1,2-diphenylethene-based EZH2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sichuan University and Collaborative Innovation Center
Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1068-1083 (2020)
Novartis Institutes For Biomedical Research
Synthesis and biological evaluation of FICZ analogues as agonists of aryl hydrocarbon receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Wisconsin-Madison
Discovery of a novel unsymmetrical structural class of HCV NS5A inhibitors with low picomolar antiviral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Japan Tobacco
Synthesis and biological evaluation of bis-N![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Rhodes University
Potent non-hydroxamate inhibitors of histone deacetylase-8: Role and scope of an isoindolin-2-yl linker with an ?-amino amide as the zinc-binding unit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University College London
Discovery of a lead series of potent benzodiazepine 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Arena Pharmaceuticals
Discovery and Structure-Activity Relationships of Nociceptin Receptor Partial Agonists That Afford Symptom Ablation in Parkinson's Disease Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2688-2704 (2020)
Astraea Therapeutics
Identification of potent pyrazole based APELIN receptor (APJ) agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Rti International
Total synthesis, chemical modification and structure-activity relationship of bufadienolides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Nanjing University of Chinese Medicine
Design and synthesis of ?-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 189: (2020)
Hunan Agricultural University
A perspective review on fatty acid amide hydrolase (FAAH) inhibitors as potential therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Assam University (A Central University)
Artemisinin-derived hybrids and their anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Qilu University of Technology (Shandong Academy of Sciences)
Discovery of Potent, Selective, and Direct Acid Sphingomyelinase Inhibitors with Antidepressant Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 961-974 (2020)
China Pharmaceutical University
Stilbenes with Potent Protein Tyrosine Phosphatase-1B Inhibitory Activity from the Roots of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 323-332 (2020)
Kyungpook National University
Multi-target dopamine D3 receptor modulators: Actionable knowledge for drug design from molecular dynamics and machine learning.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Consiglio Nazionale Delle Ricerche (Icrm-Cnr)
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3868-3880 (2020)
Genomics Institute of The Novartis Research Foundation (Gnf)
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 56-64 (2020)
University of Toronto Mississauga
Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 40-44 (2020)
Second Military Medical University
Epimers Switch Galectin-9 Domain Selectivity: 3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 34-39 (2020)
Lund University
Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 29-33 (2020)
Vanderbilt University
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 16-22 (2020)
University of Regensburg
Novel Pyrazolyl-dihydroisoquinolines as Positive Allosteric Modulator of the Dopamine D1 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: (2020)
Arrival Discovery
Novel Methyl-aza-quinazolines as Inhibitors of the RAS-SOS Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 11: 2-3 (2020)
Arrival Discovery
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1298-1312 (2020)
Shandong University
Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1281-1297 (2020)
China Pharmaceutical University
Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1624-1641 (2020)
Harvard Medical School
Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1397-1414 (2020)
Chinese Academy of Sciences
1-(2'-Bromobenzyl)-6,7-dihydroxy-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 127-133 (2020)
Universidad De Santiago De Compostela
Identification of novel GPR81 agonist lead series for target biology evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb
Suitable fusion of N-terminal heptad repeats to achieve covalently stabilized potent N-peptide inhibitors of HIV-1 infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Nankai University
Dual-target kinase drug design: Current strategies and future directions in cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Sichuan University
A review of currently identified small molecule modulators of microRNA function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Western Michigan University
Design, synthesis and biological evaluation of novel TR? selective agonists sustained by ADME-toxicity analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
University of Pisa
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5031-5073 (2020)
Terns Pharmaceuticals
Benzopyrimidodiazepinone inhibitors of TNK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Harvard Medical School
A Series of Compounds Bearing a Dipyrido-Pyrimidine Scaffold Acting as Novel Human and Insect Pest Chitinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 987-1001 (2020)
Dalian University of Technology
Discovery of novel pyrido-pyrrolidine hybrid compounds as alpha-glucosidase inhibitors and alternative agent for control of type 1 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Shiv Nadar University
One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
King Khalid University
Emerging small-molecule therapeutic approaches for amyotrophic lateral sclerosis and frontotemporal dementia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Astrazeneca
The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Chinese Academy of Medical Sciences&Peking Union Medical College
Thiazole-containing compounds as therapeutic targets for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Kurukshetra University
Synthesis and biological evaluation of 2-quinolineacrylamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kaohsiung Medical University
Spirobiflavonoid stereoisomers from the endangered conifer Glyptostrobus pensilis and their protein tyrosine phosphatase 1B inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Fudan University
Development of novel NLRP3-XOD dual inhibitors for the treatment of gout.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Soochow University
Molecular design, synthesis, and biological evaluation of bisamide derivatives as cyclophilin A inhibitors for HCV treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Chonnam National University
Diarylamides in anticancer drug discovery: A review of pre-clinical and clinical investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
University of Sharjah
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Shenyang Pharmaceutical University
Developing Inhibitors of the p47phox-p22phox Protein-Protein Interaction by Fragment-Based Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1156-1177 (2020)
University of Copenhagen
Impact of the structure-activity relationship of AHL analogues on quorum sensing in Gram-negative bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Larkin University
Stereoselective Activity of 1-Propargyl-4-styrylpiperidine-like Analogues That Can Discriminate between Monoamine Oxidase Isoforms A and B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1361-1387 (2020)
University of Ljubljana
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5119-5138 (2020)
University of Florida
Fragment-to-Lead Medicinal Chemistry Publications in 2018.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4430-4444 (2020)
Frontier Medicines
Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 4445-4467 (2020)
University of Zambia
Discovery of 6'-chloro-N-methyl-5'-(phenylsulfonamido)-[3,3'-bipyridine]-5-carboxamide (CHMFL-PI4K-127) as a novel Plasmodium falciparum PI(4)K inhibitor with potent antimalarial activity against both blood and liver stages of Plasmodium.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Chinese Academy of Sciences
Current progress in antimalarial pharmacotherapy and multi-target drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
International Medical University
Development of Novel ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1051-1067 (2020)
East China University of Science and Technology
Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1337-1360 (2020)
Chinese Academy of Sciences
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 529-541 (2020)
TBA
Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 621-637 (2020)
A*Star
Synthesis and Structure-Activity Relationship Studies of C2-Modified Analogs of the Antimycobacterial Natural Product Pyridomycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1105-1131 (2020)
Eth Zurich
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 714-746 (2020)
Gsk
Luciferase-based HMG-CoA reductase degradation assay for activity and selectivity profiling of oxy(lano)sterols.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
The University of Tokyo
Novel mouse GABA uptake inhibitors with enhanced inhibitory activity toward mGAT3/4 and their effect on pain threshold in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Jagiellonian University Medical College
N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides bearing heteroaromatic rings as novel antibacterial agents: Design, synthesis, biological evaluation and target identification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Chinese Academy of Medical Sciences&Peking Union Medical College
Pyrrolo and pyrrolopyrimidine sulfonamides act as cytotoxic agents in hypoxia via inhibition of transmembrane carbonic anhydrases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Cairo University
Design, synthesis and anti-Alzheimer's disease activity study of xanthone derivatives based on multi-target strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tianjin University of Traditional Chinese Medicine
Selective acetylcholinesterase inhibitors derived from muscle relaxant dantrolene.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo University of Pharmacy and Life Sciences
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Biogen
Design and biological evaluation of tetrahydropyridine derivatives as novel human GPR119 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sichuan University
?-Glucosidase and Protein Tyrosine Phosphatase 1B Inhibitors from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 675-683 (2020)
University of North Carolina Greensboro
Synthesis and Biological Evaluation of B-Cell Lymphoma 6 Inhibitors of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 676-695 (2020)
East China Normal University and Shanghai Fengxian District Central Hospital Joint Center For Translational Medicine
Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1216-1232 (2020)
Icahn School of Medicine At Mount Sinai
Discovery of a Small Side Cavity in Sphingosine Kinase 2 that Enhances Inhibitor Potency and Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1178-1198 (2020)
Virginia Tech
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1084-1104 (2020)
Takeda Pharmaceutical
Systematic Investigation of Lipophilicity Modulation by Aliphatic Fluorination Motifs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1002-1031 (2020)
University of Southampton
Thiazolidine-2,4-dione-based irreversible allosteric IKK-? kinase inhibitors: Optimization into in vivo active anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Korea Institute of Science & Technology (Kist)
Isolation of a High-Affinity Cannabinoid for the Human CB1 Receptor from a Medicinal ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 88-98 (2020)
University of Modena and Reggio Emilia
Evaluation of anti-depressant effects of phthalazinone-based triple-acting small molecules against 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Korea Institute of Science and Technology
Addressing hERG activity while maintaining favorable potency, selectivity and pharmacokinetic properties of PPAR? modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Mitobridge
Synthesis and cytotoxic evaluation of halogenated ?-exo-methylene-lactones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Jinan University
Design, synthesis characterization and biological evaluation of novel multi-isoform ALDH inhibitors as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
The Pennsylvania State University College of Medicine
A 18?-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Shenyang Pharmaceutical University
Synthesis of novel 5-substituted-2-aminotetralin analogs: 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Northeastern University
Discovery of 5-(pyridin-3-yl)-1H-indole-4,7-diones as indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Fudan University
Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Sanford Burnham Prebys Medical Discovery Institute
Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Jinan-Shandong Academy of Medical Sciences
Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 188: (2020)
Chinese Academy of Medical Sciences&Peking Union Medical College
[1,2,3]Triazolo[4,5-d]pyrimidine derivatives incorporating (thio)urea moiety as a novel scaffold for LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Henan University of Chinese Medicine
Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor ?t inverse agonists for the treatment of autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Fudan University
Modification of 7-piperazinylquinolone antibacterials to promising anticancer lead compounds: Synthesis and in vitro studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Mazandaran University of Medical Sciences
Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 696-713 (2020)
Second Military Medical University
Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Yale University
Identification of human lactate dehydrogenase A inhibitors with anti-osteosarcoma activity through cell-based phenotypic screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Jilin University China-Japan Union Hospital
Essential structure of orexin 1 receptor antagonist YNT-707, part V: Structure-activity relationship study of the substituents on the 17-amino group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Tsukuba
Variegatic acid from the edible mushroom Tylopilus ballouii inhibits TNF-? production and PKC?1 activity in leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo University of Agriculture
Recent advances in the discovery and development of glyoxalase I inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chengdu University
Bisphenol AF: Halogen bonding effect is a major driving force for the dual ER?-agonist and ER?-antagonist activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Kyushu University
Structural insights into the active site of poly(ADP-ribose) glycohydrolase using docking modes of 6-hydroxy-3H-xanthen-3-one derivative inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Tokyo University of Science
Inhibition of vertebrate aldehyde oxidase as a therapeutic treatment for cancer, obesity, aging and amyotrophic lateral sclerosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Shanghai Jiao Tong University
Recent developments of chalcones as potential antibacterial agents in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Weifang Medical University
Design, synthesis and evaluation of protein disulfide isomerase inhibitors with nitric oxide releasing activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Northwestern Polytechnical University (Npu)
Discovery of a follistatin-derived myostatin inhibitory peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Tokyo University of Pharmacy and Life Sciences
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
"A. Moro" University of Bari
Imidazolidine-2,4,5- and pirimidine-2,4,6-triones - New primary pharmacophore for soluble epoxide hydrolase inhibitors with enhanced water solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of California Davis
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Southern Medical University
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Dalian Medical University
Novel linked butanolide dimer compounds increase adiponectin production during adipogenesis in human mesenchymal stem cells through peroxisome proliferator-activated receptor ? modulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Seoul National University
Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Nanyang Normal University
Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Northwest A&F University
Synthesis and immunostimulatory activity of sugar-conjugated TLR7 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kagoshima University
Discovery of indane propanamides as potent and selective TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Seoul National University
Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Universidade De Lisboa
Synthesis of novel 2-pyrrolidinone and pyrrolidine derivatives and study of their inhibitory activity against autotaxin enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
National and Kapodistrian University of Athens
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University College London
Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Lanzhou University
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Astrazeneca
Structure-Activity Relationship in Pyrazolo[4,3-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 847-879 (2020)
Technische Universit£T M£Nchen
Phloroglucinol Benzophenones and Xanthones from the Leaves of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 83: 164-168 (2020)
University of Wollongong
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1528-1543 (2020)
Sosei Heptares
Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 827-846 (2020)
University of Tennessee Health Science Center
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 601-612 (2020)
Bayer
Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Northwest A&F University
Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Peking University
Synthesis and biological evaluation of Vinpocetine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Peking University
Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 656-675 (2020)
Frederick National Laboratory For Cancer Research
Pharmacokinetics-Driven Optimization of 7-Methylimidazo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1680-1685 (2019)
China Pharmaceutical University
Discovery of Novel Neuraminidase Inhibitors by Structure-Based Virtual Screening, Structural Optimization, and Bioassay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1667-1673 (2019)
Shanghai Institute of Technology
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1661-1666 (2019)
Goethe-University Frankfurt
New Potent DOT1L Inhibitors for ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1655-1660 (2019)
Novartis Institutes For Biomedical Research
Evaluating the Advantages of Using 3D-Enriched Fragments for Targeting BET Bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1648-1654 (2019)
University of Minnesota
Discovery of Axelopran (TD-1211): A Peripherally Restricted ?-Opioid Receptor Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1641-1647 (2019)
Theravance Biopharma Us
Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1635-1640 (2019)
University of Helsinki
Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1628-1634 (2019)
University of Michigan
In Silico Discovery of JMJD6 Inhibitors for Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1609-1613 (2019)
Xiamen University
Modulation of Tropomyosin Receptor Kinase for the Treatment of Neurotrophin Diseases: Alzheimer's, Huntington's and Parkinson's.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1590-1591 (2019)
Usona Institute
Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 804-815 (2020)
Chinese Academy of Sciences
Discovery and Characterization of 1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 569-590 (2020)
East China Normal University
Optimization of Orally Bioavailable PI3K? Inhibitors and Identification of Vps34 as a Key Selectivity Target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 638-655 (2020)
Glaxosmithkline
Binding Loop Substitutions in the Cyclic Peptide SFTI-1 Generate Potent and Selective Chymase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 816-826 (2020)
The University of Queensland
The Discovery of 7-Methyl-2-[(7-methyl[1,2,4]triazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3461-3471 (2020)
Astrazeneca
Engineering a Potent, Long-Acting, and Periphery-Restricted Oxytocin Receptor Agonist with Anorexigenic and Body Weight Reducing Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 382-390 (2020)
Calibr At The Scripps Research Institute
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Wenzhou Medical University
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Sichuan University and Collaborative Innovation Center of Biotherapy
Selectivity and Physicochemical Optimization of Repurposed Pyrazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 756-783 (2020)
Northeastern University
Docking Finds GPCR Ligands in Dark Chemical Matter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 613-620 (2020)
Uppsala University
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 122-139 (2020)
TBA
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of Melanocortin-5 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2194-2208 (2020)
University of Minnesota
Small molecules targeting HIF-1? pathway for cancer therapy in recent years.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shandong University
Modification of the lead molecule: Tryptophan and piperidine appended triazines reversing inflammation and hyeperalgesia in rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Guru Nanak Dev University
Thiophene bioisosteres of GluN2B selective NMDA receptor antagonists: Synthesis and pharmacological evaluation of [7]annuleno[b]thiophen-6-amines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Westf£Lische Wilhelms-Universit£T M£Nster
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Chia Tai Tianqing Pharmaceutical Group
Identification of 6'-?-fluoro-homoaristeromycin as a potent inhibitor of chikungunya virus replication.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Seoul National University
Prodrugs for nitroreductase-based cancer therapy-3: Antitumor activity of the novel dinitroaniline prodrugs/Ssap-NtrB enzyme suicide gene system: Synthesis, in vitro and in silico evaluation in prostate cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Balikesir University
Structure-Activity Relationships of Novel Thiazole-Based Modafinil Analogues Acting at Monoamine Transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 391-417 (2020)
University of Vienna
Heterotrimeric G Proteins as Therapeutic Targets in Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 5013-5030 (2020)
Sun Yat-Sen University
Discovery of Selective Inhibitors of Endoplasmic Reticulum Aminopeptidase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 103-121 (2020)
Kansas University Specialized Chemistry Center
Discovery of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 425-432 (2020)
Christian-Albrechts-University Kiel
Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Daegu-Gyeongbuk Medical Innovation Foundation (Dgmif)
Selective Blockade of Neuronal BK (? + ?4) Channels Preventing Epileptic Seizure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 216-230 (2020)
Chinese Academy of Sciences
Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Taipei Medical University
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Shanghai Institute of Technology
Licochalcone A suppresses the proliferation of sarcoma HT-1080 cells, as a selective R132C mutant IDH1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Guizhou Medcial University
Discovery of novel 1,2,3-triazole oseltamivir derivatives as potent influenza neuraminidase inhibitors targeting the 430-cavity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Shandong University
Therapeutic significance of ?-glucuronidase activity and its inhibitors: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
University of Kwazulu-Natal
Potent, Efficacious, and Stable Cyclic Opioid Peptides with Long Lasting Antinociceptive Effect after Peripheral Administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2673-2687 (2020)
Universit£
Investigation of the Adrenergic and Opioid Binding Affinities, Metabolic Stability, Plasma Protein Binding Properties, and Functional Effects of Selected Indole-Based Kratom Alkaloids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 433-439 (2020)
University of Florida
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 784-803 (2020)
Bristol-Myers Squibb
Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Brigham Young University
Identification of novel inhibitors for the tyrosyl-DNA-phosphodiesterase 1 (Tdp1) mutant SCAN1 using virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Siberian Branch of Russian Academy of Sciences
Tetrahydroquinoline units in flexible heteroarotinoids (Flex-Hets) convey anti-cancer properties in A2780 ovarian cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Oklahoma State University
Recent advances in steroid amino acid conjugates: Old scaffolds with new dimensions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Panjab University
Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Peking University
Synthesis and structure-activity relationship studies of ?-naphthoflavone derivatives as CYP1B1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Shanghai Jiao Tong University
Benzothiazole-Based LRRK2 Inhibitors as Wnt Enhancers and Promoters of Oligodendrocytic Fate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2638-2655 (2020)
Csic
Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor ?t (ROR?t) Inverse Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 241-259 (2020)
Technische Universiteit Eindhoven
Design, Synthesis, and Biological Evaluation of Amidobenzimidazole Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 260-282 (2020)
Peking Union Medical College and Chinese Academy of Medical Sciences
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3817-3833 (2020)
Univ. Lille
Targeting Stimulator of Interferon Genes (STING): A Medicinal Chemistry Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3785-3816 (2020)
China Pharmaceutical University
Development of Novel Oxotriazinoindole Inhibitors of Aldose Reductase: Isosteric Sulfur/Oxygen Replacement in the Thioxotriazinoindole Cemtirestat Markedly Improved Inhibition Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 369-381 (2020)
Comenius University In Bratislava
Exploring structure-promiscuity relationships using dual-site promiscuity cliffs and corresponding single-site analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Rheinische Friedrich-Wilhelms-Universit£T
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Array Biopharma
Identification of small-molecule urea derivatives as novel NAMPT inhibitors via pharmacophore-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Gazi University
Discovery of coumarin-based selective aldehyde dehydrogenase 1A1 inhibitors with glucose metabolism improving activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
China Pharmaceutical University
Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 163-185 (2020)
University Federico Ii of Naples
Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Jagiellonian University Medical College
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Government Arts College
Synthesis of certain benzothieno[3,2-d]pyrimidine derivatives as a selective SIRT2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Cairo University
Variations in the C-unit of bedaquiline provides analogues with improved biology and pharmacology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Auckland
Tyrosinase inhibitors as potential antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
The University of Queensland
Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Sun Yat-Sen University
Discovery of novel phosphatidylcholine-specific phospholipase C drug-like inhibitors as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
University of Auckland
Synthesis and evaluation of the HIF-1? inhibitory activity of 3(5)-substituted-4-(quinolin-4-yl)- and 4-(2-phenylpyridin-4-yl)pyrazoles as inhibitors of ALK5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Yanbian University
Scaffold Simplification Strategy Leads to a Novel Generation of Dual Human Immunodeficiency Virus and Enterovirus-A71 Entry Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 349-368 (2020)
Instituto De Qu£Mica M£Dica (Iqm-Csic)
Synthesis and PTP Inhibitory Activity of Illudalic Acid and Its Methyl Ether, with Insights into Selectivity for LAR PTP over Other Tyrosine Phosphatases under Physiologically Relevant Conditions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3386-3393 (2019)
University of Utah
Structural optimization of aminopyrimidine-based CXCR4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Soochow University
Optimization and evaluation of novel tetrahydropyrido[4,3-d]pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Shenyang Pharmaceutical University
Pyridin-2(1H)one derivatives: A possible new class of therapeutics for mechanical allodynia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 187: (2020)
Universit£
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Seoul National University
Optimization of LpxC Inhibitor Lead Compounds Focusing on Efficacy and Formulation for High Dose Intravenous Administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 88-102 (2020)
Idorsia Pharmaceuticals
Peptide-?-lactam Inhibitors of Dengue and West Nile Virus NS2B-NS3 Protease Display Two Distinct Binding Modes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 140-156 (2020)
Heidelberg University
Design, Synthesis, and Biological Evaluation of MEK PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 157-162 (2020)
Pharmaron Beijing
Synthesis and Characterization of an A6-A11 Methylene Thioacetal Human Insulin Analogue with Enhanced Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11437-11443 (2019)
University of Utah
Glucoconjugated Monoterpene Indole Alkaloids from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3288-3301 (2019)
Peking University Health Science Center
Novel Cell-Penetrating Peptide Conjugated Proteasome Inhibitors: Anticancer and Antifungal Investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 334-348 (2020)
University of Auckland
A Novel Decalin-Based Bicyclic Scaffold for FKBP51-Selective Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 231-240 (2020)
Max Planck Institute of Psychiatry
Polypropionate Derivatives with ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3440-3449 (2019)
Guangdong Institute of Microbiology
"A Sweet Combination": Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 321-333 (2020)
University of Florence
Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 295-308 (2020)
University of Pennsylvania
Isolation of three new meroterpenoids and seven known compounds from Albatrellus yasudae and their A?-aggregation inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Meiji Pharmaceutical University
A Novel Agonist of the Type 1 Lysophosphatidic Acid Receptor (LPA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2372-2390 (2020)
Universidad Complutense De Madrid
Uncarialins A-I, Monoterpenoid Indole Alkaloids from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3302-3310 (2019)
Dalian Medical University
Urea Derivatives in Modern Drug Discovery and Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2751-2788 (2020)
Purdue University
Discovery of Benzo[![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11080-11107 (2019)
China Pharmaceutical University
Discovery of structurally distinct tricyclic M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in chemoresistant cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Heinrich-Heine-Universit£T D£Sseldorf
Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Edinburgh
Tuning isoform selectivity and bortezomib sensitivity with a new class of alkenyl indene PDI inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Medical University of South Carolina
Discovery of novel 9-heterocyclyl substituted 9H-purines as L858R/T790M/C797S mutant EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Xi'An Jiaotong University
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Eli Lilly
Structure-based virtual screening and biological evaluation of novel non-bisphosphonate farnesyl pyrophosphate synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Jiangsu Institute of Nuclear Medicine
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Vanderbilt University
Design, synthesis, and enzymatic characterization of quinazoline-based CYP1A2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Florida
Development and structure-activity relationship study of SHP2 inhibitor containing 3,4,6-trihydroxy-5-oxo-5H-benzo[7]annulene.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Chungnam University
Further exploration of the structure-activity relationship of imidazoquinolines; identification of potent C7-substituted imidazoquinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Kansas
Rational design, synthesis and biological profiling of new KDM4C inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Fidelta
NO-releasing STAT3 inhibitors suppress BRAF-mutant melanoma growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
The University of Texas At Austin
Sulfonamide/sulfamate switch with a series of piperazinylureido derivatives: Synthesis, kinetic and in silico evaluation as carbonic anhydrase isoforms I, II, IV, and IX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Firenze
Application of Bivalent Bioisostere Concept on Design and Discovery of Potent Opioid Receptor Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11399-11415 (2019)
Virginia Commonwealth University
Synthesis, biological evaluation and SAR studies of ursolic acid 3?-ester derivatives as novel CETP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Nanjing Medical University
Substituted 4-phenylthiazoles: Development of potent and selective A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Bonn
Discovery of dihydropyrazino-benzimidazole derivatives as metabotropic glutamate receptor-2 (mGluR2) positive allosteric modulators (PAMs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Gedeon Richter
Discovery of a potent and selective adenylyl cyclase type 8 agonist by docking-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kunming Medical University
The Druggability of Solute Carriers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3834-3867 (2020)
The Scripps Research Institute
Structure-Activity Relationships of Pentacyclic Triterpenoids as Inhibitors of Cyclooxygenase and Lipoxygenase Enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3311-3320 (2019)
Osaka University
Synthesis of a novel and potent small-molecule antagonist of PAC1 receptor for the treatment of neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Toyama
Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Chinese Academy of Medical Science and Peking Union Medical College
Proline-Based Allosteric Inhibitors of Zika and Dengue Virus NS2B/NS3 Proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11359-11382 (2019)
Johannes Gutenberg University Mainz
The architecture of hydrogen and sulfur ?-hole interactions explain differences in the inhibitory potency of C-?-d-glucopyranosyl thiazoles, imidazoles and an N-?-d glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Thessaly
Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Discovery of N-ethylpyridine-2-carboxamide derivatives as a novel scaffold for orally active ?-secretase modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Astellas Pharma
Structure-activity relationships for binding of 4-substituted triazole-phenols to macrophage migration inhibitory factor (MIF).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Groningen
Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11260-11279 (2019)
Heinrich-Heine-Universit£T D£Sseldorf
Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Northeastern University
Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Bristol-Myers Squibb Research & Development
Recent advance in the development of novel, selective and potent FGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
China Pharmaceutical University
Synthesis and bioevaluation of 1-phenylimidazole-4-carboxylic acid derivatives as novel xanthine oxidoreductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
South China University of Technology
Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
China Pharmaceutical University
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Northwest University
Optimization of cyclic sulfamide derivatives as 11?-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Korea Research Institute of Chemical Technology
A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Electronic Science and Technology of China
Synthesis and characterization of quinoline-carbaldehyde derivatives as novel inhibitors for leishmanial methionine aminopeptidase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Hyderabad
Structure-activity relationship study of the pyridine moiety of isothiazolo[4,3-b]pyridines as antiviral agents targeting cyclin G-associated kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Ku Leuven
Generation of highly potent DYRK1A-dependent inducers of human ?-Cell replication via Multi-Dimensional compound optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Stanford University
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Temple University
Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Merck
Synthesis of novel 3-halo-3-nitroflavanones and their activities as DNA methyltransferase inhibitors in cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Cnrs Fre3600
Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Shenyang Pharmaceutical University
Synthesis, bioconversion, pharmacokinetic and pharmacodynamic evaluation of N-isopropyl-oxy-carbonyloxymethyl prodrugs of CZh-226, a potent and selective PAK4 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Shenyang Pharmaceutical University
Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 542-568 (2020)
Northeastern University
Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of ?7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 944-960 (2020)
Lupin
Design, synthesis and biological evaluation of imidazole and oxazole fragments as HIV-1 integrase-LEDGF/p75 disruptors and inhibitors of microbial pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of The Witwatersrand
Pan-specific and partially selective dye-labeled peptidic inhibitors of the polycomb paralog proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
University of Victoria
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shenyang Pharmaceutical University
Design, synthesis and cholinesterase inhibitory activity of novel spiropyrrolidine tethered imidazole heterocyclic hybrids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
King Saud University
Effect of Modifier Structure on the Activation of Leukotriene A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10605-10616 (2019)
George Mason University
Discovery of a Potent and Selective TRPC5 Inhibitor, Efficacious in a Focal Segmental Glomerulosclerosis Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1579-1585 (2019)
Goldfinch Bio
Synthesis and ?-Opioid Activity of the Primary Metabolites of Carfentanil.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1568-1572 (2019)
United States Army Ccdc Chemical Biological Center
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1561-1567 (2019)
Nestl�
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3K?).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1554-1560 (2019)
Incyte
Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1549-1553 (2019)
Dana-Farber Cancer Institute
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1543-1548 (2019)
Abbvie
Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1537-1542 (2019)
Broad Institute of Mit and Harvard
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1530-1536 (2019)
Merck
Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1524-1529 (2019)
Novartis Institute For Biomedical Research
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1518-1523 (2019)
Glaxosmithkline
Structure-Based Discovery of SD-36 as a Potent, Selective, and Efficacious PROTAC Degrader of STAT3 Protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11280-11300 (2019)
TBA
Discovery of Highly Polar ?-Homophenylalanine Derivatives as Nonsystemic Intestine-Targeted Dipeptidyl Peptidase IV Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10919-10925 (2019)
University of Chinese Academy of Sciences
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11301-11323 (2019)
University of Illinois At Chicago
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11194-11217 (2019)
Bayer
Discovery of novel nonpeptide small-molecule NRP1 antagonists: Virtual screening, molecular simulation and structural modification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
China Pharmaceutical University
Synthesis, in vitro and in vivo biological evaluation of novel graveolinine derivatives as potential anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Henan University
Design, synthesis and biological evaluation of substituted flavones and aurones as potential anti-influenza agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Prin. K.M. Kundnani College of Pharmacy
Identification of antimalarial leads with dual falcipain-2 and falcipain-3 inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Shoolini University of Biotechnology and Management Sciences
Early identification of promiscuous attributes of aldose reductase inhibitors using a DMSO-perturbation assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Kyushu University
Design, synthesis and biological evaluation of mogrol derivatives as a novel class of AMPK?2?1?1 activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Nanjing University of Chinese Medicine
4-Aryl-1-oxa-4,9-diazaspiro[5.5]undecane Derivatives as Dual ?-Opioid Receptor Agonists and ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2434-2454 (2020)
Esteve Pharmaceuticals
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11035-11053 (2019)
Leiden University
Discovery of 1,2,4-triazine-based derivatives as novel neddylation inhibitors and anticancer activity studies against gastric cancer MGC-803 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Zhengzhou University
PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Inner Mongolia Medical University
Virtual screening to identify potent sepiapterin reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Amgen
Design, synthesis, and evaluation of indeno[2,1-c]pyrazolones for use as inhibitors against hypoxia-inducible factor (HIF)-1 transcriptional activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Tokyo Institute of Innovative Research
Synthesis of natural product-like polyprenylated phenols and quinones: Evaluation of their neuroprotective activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 28: (2020)
Josai University
Battle tactics against MMP-9; discovery of novel non-hydroxamate MMP-9 inhibitors endowed with PI3K/AKT signaling attenuation and caspase 3/7 activation via Ugi bis-amide synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Alexandria University
Halogenated and di-substituted benzenesulfonamides as selective inhibitors of carbonic anhydrase isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Vilnius University
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Universit£
Design, synthesis, in-vitro, in-vivo and in-silico studies of pyrrolidine-2,5-dione derivatives as multitarget anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Malakand
Discovery of a Highly Selective and Potent ? Opioid Receptor Agonist from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11054-11070 (2019)
Fudan University
Subtype Selective ?-Aminobutyric Acid Type A Receptor (GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 3425-3446 (2020)
University of Sussex
Psiguadiols A-J, Rearranged Meroterpenoids as Potent PTP1B Inhibitors from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3267-3278 (2019)
China Pharmaceutical University
Structure-Based Optimization of Coumarin hA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2577-2587 (2020)
University of Porto
Alkaloids from the Branches and Leaves of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3221-3226 (2019)
Nanjing University of Science and Technology
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an ?-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10258-10271 (2019)
TBA
Reasonably activating Nrf2: A long-term, effective and controllable strategy for neurodegenerative diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
China Pharmaceutical University
Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Fudan University
Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Chinese Academy of Medical Science and Peking Union Medical College
Virtual screening-driven discovery of dual 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Polish Academy of Sciences
Discovery of the programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing an indoline scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
Shenyang Pharmaceutical University
Hydroxyl substituted benzoic acid/cinnamic acid derivatives: Tyrosinase inhibitory kinetics, anti-melanogenic activity and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
The University of Queensland (Uq)
Identification of neomacrophorins isolated from Trichoderma sp. 1212-03 as proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Iwate University
Discovery of covalent prolyl oligopeptidase boronic ester inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Mcgill University
Discovery of candesartan cilexetic as a novel neddylation inhibitor for suppressing tumor growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Shanghai University of Traditional Chinese Medicine
Targeting CXCR1/2: The medicinal potential as cancer immunotherapy agents, antagonists research highlights and challenges ahead.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Hangzhou Institute of Innovative Medicine
Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
"G. D'Annunzio" University
Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10897-10911 (2019)
Icahn School of Medicine At Mount Sinai
Multitarget CFTR Modulators Endowed with Multiple Beneficial Side Effects for Cystic Fibrosis Patients: Toward a Simplified Therapeutic Approach ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10833-10847 (2019)
Universit£
Structure-Based and Property-Driven Optimization of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10816-10832 (2019)
Global Discovery Chemistry
Indole-based melatonin analogues: Synthetic approaches and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Nantong University
Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
University of Perugia
Design, synthesis and biological evaluation of suramin-derived dual antagonists of the proinflammatory G protein-coupled receptors P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 186: (2020)
University of Bonn
Synthesis and elaboration of N-methylpyrrolidone as an acetamide fragment substitute in bromodomain inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Monash University (Parkville Campus)
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10867-10896 (2019)
Tsinghua University
Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11383-11398 (2019)
The Institute of Cancer Research
Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11119-11134 (2019)
Merck Healthcare
Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11232-11259 (2019)
Vanderbilt University
Biphenyl Acid Derivatives as APJ Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10456-10465 (2019)
Bristol-Myers Squibb
New Dual Small Molecules for Alzheimer's Disease Therapy Combining Histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11416-11422 (2019)
Universit£
Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10783-10797 (2019)
TBA
An Agonist Radioligand for the Proinflammatory Lipid-Activated G Protein-Coupled Receptor GPR84 Providing Structural Insights.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2391-2410 (2020)
University of Bonn
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11135-11150 (2019)
National Health Research Institutes
Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 512-528 (2020)
Sanofi
Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Egyptian Russian University
Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3065-3073 (2019)
Soochow University
Enzymatic Preparation of 2'-5',3'-5'-Cyclic Dinucleotides, Their Binding Properties to Stimulator of Interferon Genes Adaptor Protein, and Structure/Activity Correlations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10676-10690 (2019)
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences and Gilead Sciences Research Centre At Iocb
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11430-11436 (2019)
Fudan University
Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1261-1280 (2020)
Universit£
Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10617-10629 (2019)
University of Messina
Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6251-6275 (2020)
Astrazeneca
Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
University of Porto
Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent ?-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Nanjing University of Chinese Medicine
Exploration of zinc-binding groups for the design of inhibitors for the oxytocinase subfamily of M1 aminopeptidases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
National Centre For Scientific Research "Demokritos
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11004-11018 (2019)
Astrazeneca
Novel Benzohydroxamate-Based Potent and Selective Histone Deacetylase 6 (HDAC6) Inhibitors Bearing a Pentaheterocyclic Scaffold: Design, Synthesis, and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10711-10739 (2019)
Preclinical R&D
Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10563-10582 (2019)
Lupin
Rational Design and Optimization of a Novel Class of Macrocyclic Apoptosis Signal-Regulating Kinase 1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10740-10756 (2019)
TBA
Discovery of potent and selective butyrylcholinesterase inhibitors through the use of pharmacophore-based screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Kentucky
Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Qingdao University of Science and Technology
Design, synthesis and biological evaluation of oseltamivir derivatives containing pyridyl group as potent inhibitors of neuraminidase for influenza A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Wuyi University
A new chemotype with promise against Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
University of Nebraska Medical Center
Selective apoptosis-inducing activity of synthetic hydrocarbon-stapled SOS1 helix with d-amino acids in H358 cancer cells expressing KRAS![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
China Pharmaceutical University
Design, synthesis, and evaluation of compounds capable of reducing Pseudomonas aeruginosa virulence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Texas Tech University Health Sciences Center
Discovery of small-molecule candidates against inflammatory bowel disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Zhejiang University
Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 418-424 (2020)
Seoul National University
Optimizing Targeted Inhibitors of P-Glycoprotein Using Computational and Structure-Guided Approaches.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10645-10663 (2019)
TBA
Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10757-10782 (2019)
Johann Wolfgang Goethe-University
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Peking Union Medical College and Chinese Academy of Medical Sciences
An isoform-selective inhibitor of tropomyosin receptor kinase A behaves as molecular glue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 30: (2020)
Osaka Prefecture University
Synthesis and antidepressant-like activity of novel alkoxy-piperidine derivatives targeting SSRI/5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
China Pharmaceutical University
Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Iowa
Development of small molecule inhibitors targeting NLRP3 inflammasome pathway for inflammatory diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Shandong University
Direct and straightforward access to substituted alkyl selenols as novel carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
University of Florence
Development of Robust 17(![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10124-10143 (2019)
University of Texas Southwestern
A New Approach of Mitigating CYP3A4 Induction Led to the Discovery of Potent Hepatitis B Virus (HBV) Capsid Inhibitor with Optimal ADMET Profiles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10352-10361 (2019)
TBA
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10272-10293 (2019)
Boehringer Ingelheim Rcv
Discovery of Novel Small Molecule Dual Inhibitors Targeting Toll-Like Receptors ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10221-10244 (2019)
University of Colorado Boulder
6-Hydrophobic aromatic substituent pyrimethamine analogues as potential antimalarials for pyrimethamine-resistant Plasmodium falciparum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
National Science and Technology Development Agency
Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Jiangxi Science & Technology Normal University
Nitrothiadiazolo[3,2-a]pyrimidines as promising antiglycating agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Ural Federal University Named After The First President of Russia B.N. Eltsin
Isoquinoline Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-like 2 (KEAP1-NRF2) Inhibitors with High Metabolic Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6547-6560 (2020)
TBA
Advances in Discovering Deubiquitinating Enzyme (DUB) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2731-2750 (2020)
Dana-Farber Cancer Institute
Discovery of amide-bridged pyrrolo[2,3-d]pyrimidines as tumor targeted classical antifolates with selective uptake by folate receptor ? and inhibition of de novo purine nucleotide biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Duquesne University
Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
China Pharmaceutical University
6-Substituted amiloride derivatives as inhibitors of the urokinase-type plasminogen activator for use in metastatic disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Wollongong
Identification of a new small molecule chemotype of Melanin Concentrating Hormone Receptor-1 antagonists using pharmacophore-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Science and Technology
Discovery and optimization of a series of small-molecule allosteric inhibitors of MALT1 protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Janssen Research & Development
Synthesis and biological evaluation of new MET inhibitors with 1,6-naphthyridinone scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Central China Normal University
Discovery of a novel bicyclic compound, DS54360155, as an orally potent analgesic without mu-opioid receptor agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Daiichi Sankyo
Multigram scale synthesis of polycyclic lactones and evaluation of antitumor and other biological properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Universitat De Barcelona
6-Methyluracil derivatives as peripheral site ligand-hydroxamic acid conjugates: Reactivation for paraoxon-inhibited acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Kazan Scientific Center of The Russian Academy of Sciences
Drug Design Targeting T-Cell Factor-Driven Epithelial-Mesenchymal Transition as a Therapeutic Strategy for Colorectal Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10182-10203 (2019)
Colorado State University
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10848-10866 (2019)
Vrije Universiteit Amsterdam
Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for ?7 nAChRs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10376-10390 (2019)
University of California-San Diego
Flavipesines A and B and Asperchalasines E-H: Cytochalasans and Merocytochalasans from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2994-3001 (2019)
Huazhong University of Science and Technology
The identification and pharmacological evaluation of potent, selective and orally available ACC1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Takeda Pharmaceutical
The Immunoproteasome: An Emerging Target in Cancer and Autoimmune and Neurological Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1841-1858 (2020)
Purdue University
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10305-10320 (2019)
West China Hospital of Sichuan University
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10321-10341 (2019)
Bayer
Could Dissecting the Molecular Framework of ?-Lactam Integrin Ligands Enhance Selectivity?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10156-10166 (2019)
University of Bologna
A novel chalcone derivative as Nrf2 activator attenuates learning and memory impairment in a scopolamine-induced mouse model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Korea Institute of Science & Technology (Kist)
Search for new multi-target compounds against Alzheimer's disease among histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Jagiellonian University Medical College
Discovery of arylamide-5-anilinoquinazoline-8-nitro derivatives as VEGFR-2 kinase inhibitors: Synthesis, in vitro biological evaluation and molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Yunnan University
An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Marquette University
Glechomanamides A-C, Germacrane Sesquiterpenoids with an Unusual ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3056-3064 (2019)
Seoul National University
Discovery of Small Molecule Antagonists of the USP5 Zinc Finger Ubiquitin-Binding Domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10144-10155 (2019)
University of Toronto
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1798-1822 (2020)
China Pharmaceutical University
?-Lactamase Inhibitors To Restore the Efficacy of Antibiotics against Superbugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1859-1881 (2020)
Universidade De Santiago De Compostela
Validation of Human Sterol 14?-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10391-10401 (2019)
Vanderbilt University School of Medicine
Structure-Activity Relationships for a Series of (Bis(4-fluorophenyl)methyl)sulfinyl Alkyl Alicyclic Amines at the Dopamine Transporter: Functionalizing the Terminal Nitrogen Affects Affinity, Selectivity, and Metabolic Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2343-2357 (2020)
National Institute On Drug Abuse-Intramural Research Program
Fibrinolysis Inhibitors: Potential Drugs for the Treatment and Prevention of Bleeding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1445-1472 (2020)
Philipps University Marburg
Structure-Activity Relationship Studies of Small Molecule Modulators of the Staphylococcal Accessory Gene Regulator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2705-2730 (2020)
Veterans Affairs Eastern Colorado Health Care System
Enhancing the Cell Permeability of Stapled Peptides with a Cyclic Cell-Penetrating Peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10098-10107 (2019)
The Ohio State University
N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-? induced PD-L1 expression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Taipei Medical University
Optimization of pyrrolizine-based Schiff bases with 4-thiazolidinone motif: Design, synthesis and investigation of cytotoxicity and anti-inflammatory potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
Umm Al-Qura University
From bench to counter: Discovery and validation of a peony extract as tyrosinase inhibiting cosmeceutical.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
University of Innsbruck
Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Nanjing University
Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Design, synthesis, and bioactivity of dihydropyrimidine derivatives as kinesin spindle protein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Tanta University
Overcoming imatinib resistance in chronic myelogenous leukemia cells using non-cytotoxic cell death modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 185: (2020)
University of Innsbruck
Free-Wilson Analysis of Comprehensive Data on Phosphoinositide-3-kinase (PI3K) Inhibitors Reveals Importance of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10402-10422 (2019)
University of Nottingham
Kinase Chemodiversity from the Arctic: The Breitfussins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10167-10181 (2019)
Uit - The Arctic University of Norway
Differentiating the Pharmacodynamics and Toxicology of Macrolide and Ketolide Antibiotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6462-6473 (2020)
Ponce De Leon Health
Synthesis of 2-arylhydrazinylidene-3-oxo-4,4,4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Ural Branch of Russian Academy of Sciences
Development and Therapeutic Potential of Selenazo Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1473-1489 (2020)
Universidad De Navarra
Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with in Vivo Antitumor Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10204-10220 (2019)
Daiichi Sankyo
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9931-9946 (2019)
Bristol-Myers Squibb
Discovery of novel Cyclophilin D inhibitors starting from three dimensional fragments with millimolar potencies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Merck Healthcare
Strategies for Late-Stage Optimization: Profiling Thermodynamics by Preorganization and Salt Bridge Shielding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9753-9771 (2019)
Philipps-Universit£T Marburg
Engineering Fluorine into Verticillins (Epipolythiodioxopiperazine Alkaloids) via Precursor-Directed Biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3104-3110 (2019)
University of North Carolina At Greensboro
One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Koneru Lakshmaiah Education Foundation
Optimization of the chromone scaffold through QSAR and docking studies: Identification of potent inhibitors of ABCG2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Univ. Grenoble Alpes
Synthesis and structure activity relationship of 1, 3-benzo-thiazine-2-thiones as selective HDAC8 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
University of Applied Sciences
Synthetic strategy and SAR studies of C-glucoside heteroaryls as SGLT2 inhibitor: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Jamia Hamdard
Novel berberine-based derivatives with potent hypoglycemic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Guizhou Medical University
Design, synthesis, and biological evaluation of 4-phenoxyquinoline derivatives as potent c-Met kinase inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Shenyang Pharmaceutical University
Piperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Northeastern University
3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Egyptian Russian University
Benzo[b]thiophene-thiazoles as potent anti-Toxoplasma gondii agents: Design, synthesis, tyrosinase/tyrosine hydroxylase inhibitors, molecular docking study, and antioxidant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Nicolaus Copernicus University
Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Hefei University of Technology
Synthesis and antidepressant effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
China State Institute of Pharmaceutical Industry
Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Shenyang Pharmaceutical University
Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
National University of Singapore
Structure-Guided Enhancement of Selectivity of Chemical Probe Inhibitors Targeting Bacterial Seryl-tRNA Synthetase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9703-9717 (2019)
University of Warwick
Discovery of Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9718-9731 (2019)
TBA
Synthesis, Purification, and Selective ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2986-2993 (2019)
Shandong University
Trivirensols: Selectively Bacteriostatic Sesquiterpene Trimers from the Australian Termite Nest-Derived Fungus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 3165-3175 (2019)
The University of Queensland
Synthesis and biological evaluation of 3-acyl-2-phenylamino-1,4-dihydroquinolin-4(1H)-one derivatives as potential MERS-CoV inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Korea Research Institute of Chemical Technology
Developing new hybrid scaffold for urease inhibition based on carbazole-chalcone conjugates: Synthesis, assessment of therapeutic potential and computational docking analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Quaid-I-Azam University
Development of a novel class of peroxisome proliferator-activated receptor (PPAR) gamma ligands as an anticancer agent with a unique binding mode based on a non-thiazolidinedione scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Hokkaido University
Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Shanghai Institute of Materia Medica
Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9918-9930 (2019)
Astrazeneca
Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1490-1510 (2020)
Fudan University
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1492-1497 (2019)
Astrazeneca
Discovery of Pyridazinone and Pyrazolo[1,5-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1486-1491 (2019)
Bristol-Myers Squibb
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1480-1485 (2019)
Astrazeneca
Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl-Pyrimidine Moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1473-1479 (2019)
University of Basel
Design of Potent and Selective Covalent Inhibitors of Bruton's Tyrosine Kinase Targeting an Inactive Conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1467-1472 (2019)
Novartis Institutes For Biomedical Research
Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1443-1449 (2019)
Dana Farber Cancer Institute
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1436-1442 (2019)
University of Minnesota Twin Cities
Novel Pyrazole-Containing Compounds Active against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1423-1429 (2019)
Sapienza University of Rome
Chalcone-Thiazole Hybrids: Rational Design, Synthesis, and Lead Identification against 5-Lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1415-1422 (2019)
Indian Institute of Technology
Pyridinylimidazoles as GSK3? Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1407-1414 (2019)
Eberhard Karls Universit£T T£Bingen
Lysophosphatidic Acid Receptor 1 Antagonists for the Treatment of Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1378-1379 (2019)
Therachem Research Medilab
Inhibitors of KRAS May Potentially Provide Effective Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1376-1377 (2019)
Therachem Research Medilab
Second-Generation FGFR Inhibitors for the Treatment of Cancers Harboring Mutated FGFRs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1374-1375 (2019)
Therachem Research Medilab
PROTAC-Mediated Degradation of Estrogen Receptor in the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1367-1369 (2019)
Usona Institute
Structure-Activity Relationships of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9792-9805 (2019)
University of Melbourne
Protein Tyrosine Phosphatase 1B Inhibitory Iridoids from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2916-2924 (2019)
University of Illinois At Chicago
Garcinol and Related Polyisoprenylated Benzophenones as Topoisomerase II Inhibitors: Biochemical and Molecular Modeling Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2768-2779 (2019)
European Biomedical Research Institute of Salerno (Ebris)
Structure-Activity Relationships of Fish Oil Derivatives with Antiallergic Activity in Vitro and in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9576-9592 (2019)
Ehime University
In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6477-6488 (2020)
Case Western Reserve University
Oleanolic Acid Derivatives as Potential Inhibitors of HIV-1 Protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2886-2896 (2019)
TBA
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Vichem Chemie Research
Benzyl Phenylsemicarbazides: A Chemistry-Driven Approach Leading to G Protein-Biased Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9658-9679 (2019)
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Lead identification and characterization of hTrkA type 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Zoetis
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
South China Agricultural University
Structure-activity relationship study of NPP1 inhibitors based on uracil-N1-(methoxy)ethyl-?-phosphate scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Bar-Ilan University
Effective Virtual Screening Strategy toward heme-containing proteins: Identification of novel IDO1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
China Pharmaceutical University
Design, synthesis, and biological evaluation of 1-substituted -2-aryl imidazoles targeting tubulin polymerization as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Southern Medical University
Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9045-9060 (2019)
TBA
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9078-9102 (2019)
Julius Maximilian University of W£Rzburg
Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer's Disease Mouse Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9116-9140 (2019)
Julius Maximilian University W£Rzburg
Discovery and optimization of covalent Bcl-xL antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Astrazeneca
Anti-hepatitis-C virus activity and QSAR study of certain thiazolidinone and thiazolotriazine derivatives as potential NS5B polymerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
Cairo University
Development and Characterization of a Fluorescent Probe for GLS1 and the Application for High-Throughput Screening of Allosteric Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9642-9657 (2019)
China Pharmaceutical University
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2547-2556 (2020)
University of Oxford
Opioids as Substrates and Inhibitors of the Genetically Highly Variable Organic Cation Transporter OCT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9890-9905 (2019)
University Medicine Greifswald
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9806-9823 (2019)
Research Triangle Institute
Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2292-2307 (2020)
Sanofi-Aventis Deutschland
Design, synthesis, and evaluation of potent novel peroxisome proliferator-activated receptor ? indole partial agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
The University of Oklahoma Health Science Center
Discovery of novel allosteric site and covalent inhibitors of FBPase with potent hypoglycemic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 184: (2019)
International Cooperation Base of Pesticide and Green Synthesis (Hubei)
High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9837-9873 (2019)
Biokin
Protein Stability Effects in Aggregate-Based Enzyme Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9593-9599 (2019)
University of California
Discovery of AM-6494: A Potent and Orally Efficacious ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2263-2281 (2020)
TBA
Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Medical University of Warsaw
Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Jinan University
Phosphatidylinositol 3 kinase (PI3K) inhibitors as new weapon to combat cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Ain Shams University
The discovery of a potent and selective third-generation EGFR kinase inhibitor as a therapy for EGFR L858R/T790M double mutant non-small cell lung cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Sun Yat-Sen University
Structure-activity relationships of serotonin 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Normandie Univ
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Chinese Academy of Sciences
Hot-Spots of Mcl-1 Protein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 928-943 (2020)
Normandie Univiversit�
Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9488-9520 (2019)
University of Nottingham
-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9161-9174 (2019)
Fudan University
Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9874-9889 (2019)
Pharmaxis
Novel tertiary sulfonamide derivatives containing benzimidazole moiety as potent anti-gastric cancer agents: Design, synthesis and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Zhengzhou University
Chirality-Driven Mode of Binding of ?-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9691-9702 (2019)
Mcgill University
Recent Developments in Therapeutic Peptides for the Glucagon-like Peptide 1 and 2 Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 905-927 (2020)
Sosei Heptares
Bipolaricins A-I, Ophiobolin-Type Tetracyclic Sesterterpenes from a Phytopathogenic ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2897-2906 (2019)
Huazhong University of Science and Technology
Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Zhejiang University
Development of Chemical Entities Endowed with Potent Fast-Killing Properties against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9217-9235 (2019)
Glaxosmithkline
Divalent cannabinoid-1 receptor ligands: A linker attachment point survey of SR141716A for development of high-affinity CB1R molecular probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Auckland
Discovery of novel, potent, isosteviol-based antithrombotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Peking University
Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Montana State University
Ellagic acid a multi-target bioactive compound for drug discovery in CNS? A narrative review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Genoa
Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Universidade De S£O Paulo
Recent advances in class IIa histone deacetylases research.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Heinrich-Heine-Universit£T D£Sseldorf
Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Chinese Academy of Sciences
Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Indian Institute of Technology (Banaras Hindu University)
Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9471-9487 (2019)
TBA
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10108-10123 (2019)
National Health Research Institutes
Selective Phenylimidazole-Based Inhibitors of the ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9246-9253 (2019)
Weill Cornell Medicine
Dihydroorotate dehydrogenase inhibitors in anti-infective drug research.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Turin (Unito)
Design, synthesis and biological evaluation of N-(3-(1H-tetrazol-1-yl)phenyl)isonicotinamide derivatives as novel xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
China Medical University
Insights on the synthesis of asymmetric curcumin derivatives and their biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Universiti Kuala Lumpur
Trifluorinated Pyrimidine-Based A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9315-9330 (2019)
Uppsala University
Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1? Signaling Inhibitors with Potent Activities of Anticancer Metastasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9299-9314 (2019)
Anhui Medical University
Anti-biofilm Agents against ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9201-9216 (2019)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Progress in the development of more effective and safer analgesics for pain management.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Catania
Heme Oxygenase-2 (HO-2) as a therapeutic target: Activators and inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Catania
Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Shenyang Pharmaceutical University
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9008-9025 (2019)
University of Oxford
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9188-9200 (2019)
TBA
The Exploration of Chirality for Improved Druggability within the Human Kinome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 441-469 (2020)
University of Arkansas For Medical Sciences
p97: An Emerging Target for Cancer, Neurodegenerative Diseases, and Viral Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 1892-1907 (2020)
TBA
Discovery of an Extremely Potent Thiazine-Based ?-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9331-9337 (2019)
TBA
Drugs for the Treatment of Zika Virus Infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 470-489 (2020)
University of North Carolina At Chapel Hill
Structure optimization of a new class of PPAR? antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Fraunhofer Institute For Molecular Biology and Applied Ecology Ime
Design, synthesis and biological evaluation of novel serotonin and dopamine receptor ligands being 6-bromohexyl saccharine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Cracow University of Technology
1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Guizhou University of Traditional Chinese Medicine
Rational discovery of a highly novel and selective mTOR inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Takeda California
Synthesis of coumarin-sulfonamide derivatives and determination of their cytotoxicity, carbonic anhydrase inhibitory and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Bezmialem Vakif University
Discovery of a benzothiophene-flavonol halting miltefosine and antimonial drug resistance in Leishmania parasites through the application of medicinal chemistry, screening and genomics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Modena and Reggio Emilia
Design and synthesis of (2-(phenylamino)thieno[3,2-d]pyrimidin-4-yl)(3,4,5-trimethoxyphenyl)methanone analogues as potent anti-tubulin polymerization agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Peking University
Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Shandong University
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic ?-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Northwest University
New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Cairo University
Continued exploration and tail approach synthesis of benzenesulfonamides containing triazole and dual triazole moieties as carbonic anhydrase I, II, IV and IX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Kurukshetra University
Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9026-9044 (2019)
The University of Jordan
Design, synthesis and evaluation of activity and pharmacokinetic profile of new derivatives of xanthone and piperazine in the central nervous system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Jagiellonian University Medical College
Discovery of a novel 3,4-dimethylcinnoline carboxamide M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Vanderbilt University
1,3,4-Oxadiazol-2-ylbenzenesulfonamides as privileged structures for the inhibition of monoamine oxidase B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Ushinsky Yaroslavl State Pedagogical University
Indole: A privileged scaffold for the design of anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Hunan University of Science and Technology
Structure activity relationship towards design of cryptosporidium specific thymidylate synthase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Yale University
Sulfide, sulfoxide and sulfone bridged acyclic nucleoside phosphonates as inhibitors of the Plasmodium falciparum and human 6-oxopurine phosphoribosyltransferases: Synthesis and evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
The Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Potent combretastatin A-4 analogs containing 1,2,4-triazole: Synthesis, antiproliferative, anti-tubulin activity, and docking study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Minia University
SAR Exploration of Tight-Binding Inhibitors of Influenza Virus PA Endonuclease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9438-9449 (2019)
University of California
Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9270-9280 (2019)
Glaxosmithkline
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8711-8732 (2019)
Amri
Development of High-Throughput Fluorescent-Based Screens to Accelerate Discovery of P2X Inhibitors from Animal Venoms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2559-2567 (2019)
University of East Anglia
Cinerols, Nitrogenous Meroterpenoids from the Marine Sponge ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2586-2593 (2019)
Shanghai Jiao Tong University
?-Fluorofentanyls Are pH-Sensitive Mu Opioid Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1353-1356 (2019)
Marquette University
A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1346-1352 (2019)
Goethe-University Frankfurt
Photoswitchable Inhibitor of the Calcium Channel TRPV6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1341-1345 (2019)
University of Bern
Fluorinated Analogues of the Histone Deacetylase Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere, BITE.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1336-1340 (2019)
University of Munster
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1322-1327 (2019)
Astrazeneca
Systematically Mitigating the p38? Activity of Triazole-based BET Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1296-1301 (2019)
University of Minnesota Twin Cities
Synthesis and Bioactivity of the Alanyl Phosphonamidate Stereoisomers Derived from a Butyrophilin Ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1284-1289 (2019)
University of Iowa
Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1266-1271 (2019)
Universidade Estadual De Campinas (Unicamp)
Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1260-1265 (2019)
Genentech
PROTAC Degradation of IRAK4 for the Treatment of Neurodegenerative and Cardiovascular Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1251-1252 (2019)
Usona Institute
Triazolo Pyridines Useful as Inhibitors of ?-Secretase and Their Methods of Use.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1249-1250 (2019)
Temple University
Sodium Channel Modulators and Their Method of Use.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1247-1248 (2019)
Temple University
Modulators of KEAP-1 Activity as Potential Therapies for the Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1245-1246 (2019)
Temple University
Triazolo-azepine Inhibitors of ?-Secretase and Their Methods of Use.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1243-1244 (2019)
Temple University
[1]Benzothieno[3,2-d]pyrimidine derivatives as ligands for the serotonergic 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Universit£
Structure-based rational design of staurosporine-based fluorescent probe with broad-ranging kinase affinity for kinase panel application.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Takeda Pharmaceutical
Investigation of Novel Primary and Secondary Pharmacophores and 3-Substitution in the Linking Chain of a Series of Highly Selective and Bitopic Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9061-9077 (2019)
National Institute On Drug Abuse-Intramural Research Program
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9618-9641 (2019)
Xenon Pharmaceuticals
Inhibition of the Cytolytic Protein Perforin Prevents Rejection of Transplanted Bone Marrow Stem Cells in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2229-2239 (2020)
University of Auckland
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2074-2094 (2020)
Universit£
Inhibition Mechanisms of Indoleamine 2,3-Dioxygenase 1 (IDO1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8784-8795 (2019)
Sib Swiss Institute of Bioinformatics
Antibacterial activity of 2-amino-4-hydroxypyrimidine-5-carboxylates and binding to Burkholderia pseudomallei 2-C-methyl-d-erythritol-2,4-cyclodiphosphate synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Northern Illinois University
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Glaxosmithkline
The discovery and optimization of a series of 2-aminobenzoxazole derivatives as ChemR23 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Kyowa Kirin
Synthesis and biological evaluation of calycanthaceous alkaloid analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Jiangsu University of Science and Technology
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Hangzhou Xixi Hospital
Discovery of a potent p38?/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Sharjah
C-terminal modulators of heat shock protein of 90?kDa (HSP90): State of development and modes of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Heinrich Heine University D£Sseldorf
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Janssen Research & Development
Benzothiazole-based compounds as potent endothelial lipase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Bristol-Myers Squibb
Development of novel multipotent compounds modulating endocannabinoid and dopaminergic systems.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Siena
The Rise of Molecules Able To Regenerate the Central Nervous System.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 490-511 (2020)
Universit£
Synthesis and exploration of 2-morpholino-4-phenylthiazol-5-yl acrylamide derivatives for their effects against carbonic anhydrase I, II, IX and XII isoforms as a non-sulfonamide class of inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
National Institute of Pharmaceutical Education and Research (NIPER)
Highly hydrophilic 1,3-oxazol-5-yl benzenesulfonamide inhibitors of carbonic anhydrase II for reduction of glaucoma-related intraocular pressure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Saint Petersburg State University
Recent advances in the development of cyclin-dependent kinase 7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
Tianjin University of Science and Technology
Synthesis of benzotriazoles derivatives and their dual potential as ?-amylase and ?-glucosidase inhibitors in vitro: Structure-activity relationship, molecular docking, and kinetic studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 183: (2019)
University of Karachi
Activity of 2,6,9-trisubstituted purines as potent PDGFR? kinase inhibitors with antileukaemic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Palack£
Discovery of potent 4-aminoquinoline hydrazone inhibitors of NRH:quinoneoxidoreductase-2 (NQO2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Manchester
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9141-9160 (2019)
Korea University
Design and Biological Evaluation of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8773-8783 (2019)
Shenyang Pharmaceutical University
Targeting the ?-Aminobutyric Acid Type B (GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8819-8830 (2019)
University of Copenhagen
Potential Tools for Eradicating HIV Reservoirs in the Brain: Development of Trojan Horse Prodrugs for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2131-2138 (2020)
Purdue University
Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Yantai University
Structural Characterization of Agonist Binding to an A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8831-8846 (2019)
National and Kapodistrian University of Athens
Recent advances in the targeting of human DNA ligase I as a potential new strategy for cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Allahabad
Design, synthesis, and biological evaluation of novel benzodiazepine derivatives as anticancer agents through inhibition of tubulin polymerization in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
The Second Affiliated Hospital of Guangzhou University of Chinese Medicine
14- and 15-membered lactone macrolides and their analogues and hybrids: structure, molecular mechanism of action and biological activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Adam Mickiewicz University
Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8631-8641 (2019)
Eisai
Designing around Structural Alerts in Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 6276-6302 (2020)
Pfizer
Discovery of an Orally Bioavailable Pan ?v Integrin Inhibitor for Idiopathic Pulmonary Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8796-8808 (2019)
Glaxosmithkline Medicines Research Centre
Structure-Reactivity Relationships on Substrates and Inhibitors of the Lysine Deacylase Sirtuin 2 from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8733-8759 (2019)
University of Freiburg
In vitro cytotoxicity screening to identify novel anti-osteosarcoma therapeutics targeting pyruvate dehydrogenase kinase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Capital Medical University
Natural products as important tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Southwest Jiaotong University
Natural dimers of coumarin, chalcones, and resveratrol and the link between structure and pharmacology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Nagasaki International University
Highly potent non-steroidal FXR agonists protostane-type triterpenoids: Structure-activity relationship and mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Dalian Medical University
Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Florence
Identification and characterization of benzo[d]oxazol-2(3H)-one derivatives as the first potent and selective small-molecule inhibitors of chromodomain protein CDYL.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Peking University
Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Luoyang Normal University
Recent advancements in mechanistic studies and structure activity relationship of F![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Kurukshetra University
Novel N-Substituted oseltamivir derivatives as potent influenza neuraminidase inhibitors: Design, synthesis, biological evaluation, ADME prediction and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
The Hong Kong Polytechnic University
Design, synthesis and biological evaluation of a new series of thiazolyl-pyrazolines as dual EGFR and HER2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Anadolu University
Synthesis, biological activities, and docking studies of d-pantolactone derivatives as novel FAS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Third Institute of Oceanography
An exploration of solvent-front region high affinity moiety leading to novel potent ALK & ROS1 dual inhibitors with mutant-combating effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Shenyang Pharmaceutical University
Discovery of novel steroidal histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Chemical Works of Gedeon Richter
Structure-Based Discovery and Development of a Series of Potent and Selective Bromodomain and Extra-Terminal Protein Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8642-8663 (2019)
University of Chinese Academy of Sciences
Novel promising 4-anilinoquinazoline-based derivatives as multi-target RTKs inhibitors: Design, molecular docking, synthesis, and antitumor activities in vitro and vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Beijing Normal University
Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Universitat De Barcelona
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10062-10097 (2019)
Merck
Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for Retinoid X Receptor Ligand Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8809-8818 (2019)
Okayama University Graduate School of Medicine
Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Cairo University
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015-2019).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Eli Lilly
From random to rational: A discovery approach to selective subnanomolar inhibitors of human carbonic anhydrase IV based on the Castagnoli-Cushman multicomponent reaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Saint Petersburg State University
GAC inhibitors with a 4-hydroxypiperidine spacer: Requirements for potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Pittsburgh
?-Hydroxy isoprenoid bisphosphonates as linkable GGDPS inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
University of Iowa
Discovery of dual-acting opioid ligand and TRPV1 antagonists as novel therapeutic agents for pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Seoul National University
Structure-activity relationship with pyrazoline-based aromatic sulfamates as carbonic anhydrase isoforms I, II, IX and XII inhibitors: Synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Cagliari
Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Lifearc
Novel lipid side chain modified exenatide analogs emerged prolonged glucoregulatory activity and potential body weight management properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
China Pharmaceutical University
Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
University of Texas-Arlington
Identification of Novel Resorcinol Amide Derivatives as Potent and Specific Pyruvate Dehydrogenase Kinase (PDHK) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8461-8479 (2019)
Korea University
Indole-Diterpenoids with Protein Tyrosine Phosphatase Inhibitory Activities from the Marine-Derived Fungus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2638-2644 (2019)
Hebei University
Optimization and anti-inflammatory evaluation of methyl gallate derivatives as a myeloid differentiation protein 2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Wenzhou Medical University
Design, synthesis, and biological evaluation of 4-((6,7-dimethoxyquinoline-4-yl)oxy)aniline derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Shenyang Pharmaceutical University
Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8578-8608 (2019)
Hong Kong Polytechnic University
Myxochelin- and Pseudochelin-Derived Lipoxygenase Inhibitors from a Genetically Engineered ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2544-2549 (2019)
Institute For Natural Product Research and Infection Biology
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8609-8630 (2019)
University of Basel
Discovery, structural insight, and bioactivities of BY27 as a selective inhibitor of the second bromodomains of BET proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Chinese Academy of Sciences
Myrmenaphthol A, Isolated from a Hawaiian Sponge of the Genus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2668-2671 (2019)
University of Hawaii At Manoa
Bicyclic Boronate VNRX-5133 Inhibits Metallo- and Serine-?-Lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8544-8556 (2019)
University of Oxford
Antioxidant-Conjugated 1,2,4-Triazolo[4,3-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8511-8531 (2019)
Universit£
Glycocluster Tetrahydroxamic Acids Exhibiting Unprecedented Inhibition of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7722-7738 (2019)
Cnrs-Universit£
A rational search for discovering potential neutraligands of human complement fragment 5a (![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Indian Institute of Technology Bhubaneswar
Structural tuning of acridones for developing anticancer agents targeting dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Guru Nanak Dev University
Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates bearing sulfonylpiperazine as antitumor inhibitors targeting PI3K?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
School of Traditional Chinese Pharmacy
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Bristol-Myers Squibb
Synthesis and characterization of novel isoform-selective IP6K1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Johns Hopkins University School of Medicine
Discovery of potent p38? MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Perugia
Cyclic enaminone as new chemotype for selective cyclooxygenase-2 inhibitory, anti-inflammatory, and analgesic activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
National Institute of Pharmaceutical Education and Research (NIPER)
Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Illinois At Chicago
Discovery of phosphonamidate IDO1 inhibitors for the treatment of non-small cell lung cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Nanjing Medical University
Synthesis, evaluation and structural investigations of potent purple acid phosphatase inhibitors as drug leads for osteoporosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
The University of Queensland
Pyrazolo-benzothiazole hybrids: Synthesis, anticancer properties and evaluation of antiangiogenic activity using in vitro VEGFR-2 kinase and in vivo transgenic zebrafish model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Academy of Scientific and Innovative Research (Acsir)
Type 2 inhibitor leads of human tropomyosin receptor kinase (hTrkA).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Zoetis
The development of 2-acetylphenol-donepezil hybrids as multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Guizhou Medical University
Discovery of novel functionalized 1,2,4-triazoles as PARP-1 inhibitors in breast cancer: Design, synthesis and antitumor activity evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Suez Canal University
Chromenone derivatives as a versatile scaffold with dual mode of inhibition of HIV-1 reverse transcriptase-associated Ribonuclease H function and integrase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Cagliari
Thienopyrimidinone Derivatives That Inhibit Bacterial tRNA (Guanine37-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7788-7805 (2019)
Singapore-Mit Alliance For Research and Technology
Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Southwest Jiaotong University
Discovery of novel series of 2-substituted benzo[d]oxazol-5-amine 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 182: (2019)
Indian Institute of Technology (Banaras Hindu University)
Structure Kinetics Relationships and Molecular Dynamics Show Crucial Role for Heterocycle Leaving Group in Irreversible Diacylglycerol Lipase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7910-7922 (2019)
Leiden University
Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8443-8460 (2019)
Goethe-University Frankfurt
Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Xi'An Jiaotong University
Discovery of fused heterocyclic carboxamide derivatives as novel ?7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Peking University
Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Instituto Oswaldo Cruz
Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Shandong University
Cholinesterase Inhibitory Arisugacins L-Q from a ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2627-2637 (2019)
Institute For Natural Products Applications and Research Technologies
Correlation of indoleamine-2,3-dioxigenase 1 inhibitory activity of 4,6-disubstituted indazole derivatives and their heme binding affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Osaka University
Novel ?,?-unsaturated hydroxamic acid derivatives overcome cisplatin resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Heinrich-Heine-University D£Sseldorf
Dehydroabietylamine Ureas and Thioureas as Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Enhance the Antitumor Effect of Temozolomide on Glioblastoma Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2443-2450 (2019)
Siberian Branch of The Russian Academy of Sciences
2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2308-2324 (2020)
University of Manchester
Labdanes, Withanolides, and Other Constituents from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2489-2500 (2019)
Universidad Nacional Aut£Noma De M£Xico
Lead Optimization Yields High Affinity Frizzled 7-Targeting Peptides That Modulate ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7739-7750 (2019)
TBA
Synthesis, biological evaluation and molecular modeling of novel selective COX-2 inhibitors: sulfide, sulfoxide, and sulfone derivatives of 1,5-diarylpyrrol-3-substituted scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Universit£
Discovery of aryl-substituted indole and indoline derivatives as ROR?t agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Fudan University
How To Design Selective Ligands for Highly Conserved Binding Sites: A Case Study Using ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2095-2113 (2020)
Johannes Gutenberg-Universit£T Mainz
Galloyl esters of trans-stilbenes are inhibitors of FASN with anticancer activity on non-small cell lung cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
National University of Singapore
Synthesis and in vitro evaluation of piperazinyl-ureido sulfamates as steroid sulfatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Cagliari
Design, synthesis and biological evaluation of 3,5-dimethylisoxazole and pyridone derivatives as BRD4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Sichuan University
Rasagiline derivatives combined with histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Heinrich Heine University D£Sseldorf
Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Fudan University
Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Groningen
Discovery of small molecule inhibitors of human uridine-cytidine kinase 2 by high-throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2559-2564 (2019)
Stanford University
Fluorescent analogs of peptoid-based HDAC inhibitors: Synthesis, biological activity and cellular uptake kinetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Leipzig University
Identification of new dual FABP4/5 inhibitors based on a naphthalene-1-sulfonamide FABP4 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Fudan University
Discovery and development of substituted thiadiazoles as inhibitors of Staphylococcus aureus Sortase A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
University of Gothenburg
STING modulators: Predictive significance in drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Zhejiang Normal University
Carbonic anhydrase inhibitors based on sorafenib scaffold: Design, synthesis, crystallographic investigation and effects on primary breast cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
University of Florence
Novel multi target-directed ligands targeting 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 182: (2019)
Normandie Univ
Development of the First Low Nanomolar Liver Receptor Homolog-1 Agonist through Structure-guided Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 11022-11034 (2019)
Emory University School of Medicine
First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8235-8248 (2019)
Macquarie University
Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10927-10954 (2019)
Zhejiang University
Synthesis and Evaluation of Novel TLR2 Agonists as Potential Adjuvants for Cancer Vaccines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2282-2291 (2020)
University of Auckland
Lowering Lipophilicity by Adding Carbon: AzaSpiroHeptanes, a log![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1198-1204 (2019)
Astrazeneca
Discovery of Selective, Orally Bioavailable Pyrazolopyridine Inhibitors of Protein Kinase C? (PKC?) That Ameliorate Symptoms of Experimental Autoimmune Encephalomyelitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1134-1139 (2019)
Vertex Pharmaceuticals
Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Kyushu Institute of Technology1-1 Sensuicho
Synthesis, molecular docking, and QSAR study of bis-sulfonamide derivatives as potential aromatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Srinakharinwirot University
Design and evaluation of pyrazolopyrimidines as KCNQ channel modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: (2019)
Abbvie
Potent HIV-1 protease inhibitors incorporating squaramide-derived P2 ligands: Design, synthesis, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2565-2570 (2019)
Purdue University
Design of selective PI3K? inhibitors using an iterative scaffold-hopping workflow.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2575-2580 (2019)
Merck
Discovery of ?-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Anhui Medical University
Design, synthesis and preliminary bioactivity evaluations of 8-hydroxyquinoline derivatives as matrix metalloproteinase (MMP) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Shandong University
Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7769-7787 (2019)
Orexo
Old but Gold: Tracking the New Guise of Histone Deacetylase 6 (HDAC6) Enzyme as a Biomarker and Therapeutic Target in Rare Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 23-39 (2020)
University of Naples Federico Ii
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7669-7683 (2019)
Pfizer
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8557-8577 (2019)
University of Illinois At Chicago
Iterative Optimization of the Cyclic Peptide SFTI-1 Yields Potent Inhibitors of Neutrophil Proteinase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1234-1239 (2019)
The University of Queensland
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1228-1233 (2019)
Glaxosmithkline
DPP1 Inhibitors: Exploring the Role of Water in the S2 Pocket of DPP1 with Substituted Pyrrolidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1222-1227 (2019)
Astrazeneca
Identification of CB1 Receptor Allosteric Sites Using Force-Biased MMC Simulated Annealing and Validation by Structure-Activity Relationship Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1216-1221 (2019)
University of North Carolina At Greensboro
Bis-benzoxaboroles: Design, Synthesis, and Biological Evaluation as Carbonic Anhydrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1205-1210 (2019)
Universit£
Design of a Long-Acting and Selective MEG-Fatty Acid Stapled Prolactin-Releasing Peptide Analog.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1166-1172 (2019)
Calibr At Scripps Research
Evaluation of a Series of ?-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1159-1165 (2019)
Janssen Research & Development
Malabaricone C as Natural Sphingomyelin Synthase Inhibitor against Diet-Induced Obesity and Its Lipid Metabolism in Mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1154-1158 (2019)
Hokkaido University
Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1128-1133 (2019)
Novartis Institutes For Biomedical Research
Design, Synthesis, and Biological Evaluation of 2,4-Imidazolinedione Derivatives as HDAC6 Isoform-Selective Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1122-1127 (2019)
Shandong University
Prodrug Activation by a Viral Protease: Evaluating Combretastatin Peptide Hybrids To Selectively Target Infected Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1115-1121 (2019)
Heidelberg University
Inhibition of ACSS2 for Treatment of Cancer and Neuropsychiatric Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1100-1101 (2019)
Usona Institute
In Praise of Remarkably Powerful Centamolecular Therapeutic Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1094-1097 (2019)
Bristol-Myers Squibb Research and Development
Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8011-8027 (2019)
Seoul National University
A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8028-8052 (2019)
University of Copenhagen
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Shenyang Pharmaceutical University
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Chinese Academy of Medical Sciences and Peking Union Medical College
Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9983-9989 (2019)
Shanghaitech University
Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor ? Type I Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7961-7975 (2019)
Sun Yat-Sen University
New Approaches to Cancer Therapy: Combining Fatty Acid Amide Hydrolase (FAAH) Inhibition with Peroxisome Proliferator-Activated Receptors (PPARs) Activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10995-11003 (2019)
Universit£
Coumarin-containing hybrids and their anticancer activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Tsinghua University
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Palack£
Development of novel theranostic agents for in vivo amyloid imaging and protective effects on human neuroblastoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Guangdong University of Technology
Homotrimerization Approach in the Design of Thrombospondin-1 Mimetic Peptides with Improved Potency in Triggering Regulated Cell Death of Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7656-7668 (2019)
Sorbonne Universit£
Synthetic routes and structure-activity relationships (SAR) of anti-HIV agents: A key review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Wuhan University of Technology
Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
University of Florence
Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Charles University
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 690-706 (2019)
Julius Maximilian University of W£Rzburg
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3979-3997 (2019)
Y. B. Chavan College of Pharmacy
Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2595-2603 (2019)
Sichuan University
Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2638-2645 (2019)
Qingdao University
Exploring hydroxamic acid inhibitors of HDAC1 and HDAC2 using small molecule tools and molecular or homology modelling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2581-2586 (2019)
The University of Sydney
Small molecule modulators targeting protein kinase CK1 and CK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
China Pharmaceutical University
Identification of potent triazolylpyridine nicotinamide phosphoribosyltransferase (NAMPT) inhibitors bearing a 1,2,3-triazole tail group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Universit£
Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
University of Belgrade
Design, synthesis and biological evaluation of novel vicinal diaryl-substituted 1H-Pyrazole analogues of combretastatin A-4 as highly potent tubulin polymerization inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Universit£
Identification of a new family of pyrazolo[3,4-d]pyrimidine derivatives as multitarget Fyn-Blk-Lyn inhibitors active on B- and T-lymphoma cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
University of Siena
Discovery of benzimidazole analogs as a novel interleukin-5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Chungnam National University
A Qualified Success: Discovery of a New Series of ATAD2 Bromodomain Inhibitors with a Novel Binding Mode Using High-Throughput Screening and Hit Qualification.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7506-7525 (2019)
Cellzome
Structure-activity analysis of peptidic Chlamydia HtrA inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4185-4199 (2019)
University of Otago
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4124-4142 (2019)
Peking University Health Science Center
New anthranilic acid-incorporating N-benzenesulfonamidophthalimides as potent inhibitors of carbonic anhydrases I, II, IX, and XII: Synthesis, in vitro testing, and in silico assessment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
King Saud University
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7874-7884 (2019)
Mcgill University
Bioactivatable Pseudotripeptidization of Cyclic Dipeptides To Increase the Affinity toward Oligopeptide Transporter 1 for Enhanced Oral Absorption: An Application to Cyclo(l-Hyp-l-Ser) (JBP485).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7708-7721 (2019)
Dalian Medical University
Non-covalent albumin-binding ligands for extending the circulating half-life of small biotherapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 10: 1068-1081 (2019)
Swiss Federal Institute of Technology Lausanne
Discovery of ?-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8357-8363 (2019)
Sanford Burnham Prebys Medical Discovery Institute
Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8152-8163 (2019)
TBA
4,8-Dimethylcoumarin Inhibitors of Intestinal Anion Exchanger slc26a3 (Downregulated in Adenoma) for Anti-Absorptive Therapy of Constipation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8330-8337 (2019)
TBA
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2690-2694 (2019)
Temple University
Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Peking Union Medical College & Chinese Academy of Medical Sciences
A computer-assisted discovery of novel potential anti-obesity compounds as selective carbonic anhydrase VA inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
"Magna Gr£Cia" University of Catanzaro
HIV-1 Protease Inhibitors Incorporating Stereochemically Defined P2' Ligands To Optimize Hydrogen Bonding in the Substrate Envelope.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8062-8079 (2019)
University of Massachusetts Medical School
Synthesis and SAR Study of Carbamoyl Pyridone Bicycle Derivatives as Potent Inhibitors of Influenza Cap-dependent Endonuclease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8101-8114 (2019)
Shionogi
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10526-10562 (2019)
The Walter and Eliza Hall Institute of Medical Research
11-Aminostrychnine and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2332-2336 (2019)
The German University In Cairo
Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4151-4162 (2019)
Nanjing Forestry University
Novel multitarget 5-arylidenehydantoins with arylpiperazinealkyl fragment: Pharmacological evaluation and investigation of cytotoxicity and metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4163-4173 (2019)
Jagiellonian University Medical College
Incorporation of a chiral gem-disubstituted nitrogen heterocycle yields an oxazolidinone antibiotic with reduced mitochondrial toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2686-2689 (2019)
California Institute of Technology
Discovery of novel PTHR1 antagonists: Design, synthesis, and structure activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2613-2616 (2019)
Daiichi Sankyo
Novel dual inhibitors targeting CDK4 and VEGFR2 synergistically suppressed cancer progression and angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Nankai University
Novel reverse thia-analogs of fosmidomycin: Synthesis and antiplasmodial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Heinrich Heine University D£Sseldorf
Synthesis, biological evaluation, and docking studies of new raloxifene sulfonate or sulfamate derivatives as inhibitors of nucleotide pyrophosphatase/phosphodiesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
University of Sharjah
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7897-7909 (2019)
Merck Healthcare
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7923-7940 (2019)
TBA
Profile of a Highly Selective Quaternized Pyrrolidine Betaine ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7543-7556 (2019)
Glaxosmithkline Medicines Research Centre
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7697-7707 (2019)
Chengdu University
Microwave-Assisted Organic Synthesis, structure-activity relationship, kinetics and molecular docking studies of non-cytotoxic benzamide derivatives as selective butyrylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4030-4040 (2019)
University of Karachi
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4013-4029 (2019)
Vrije Universiteit Amsterdam
Applications of amide isosteres in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2535-2550 (2019)
Xenon Pharmaceuticals
Targeting the subpocket in xanthine oxidase: Design, synthesis, and biological evaluation of 2-[4-alkoxy-3-(1H-tetrazol-1-yl) phenyl]-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Shenyang Pharmaceutical University
Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Nankai University
Cinnamamide: An insight into the pharmacological advances and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
National Institute of Pharmaceutical Education and Research (NIPER)
Design, synthesis and anti-inflammatory evaluation of 3-amide benzoic acid derivatives as novel P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
China Pharmaceutical University
Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Universidad De Sevilla
Essential structure of orexin 1 receptor antagonist YNT-707, Part IV: The role of D-ring in 4,5-epoxymorphinan on the orexin 1 receptor antagonistic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2655-2658 (2019)
University of Tsukuba
Incorporation of privileged structures into 3-O-?-chacotriosyl ursolic acid can enhance inhibiting the entry of the H5N1 virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2675-2680 (2019)
South China Agricultural University
Design, synthesis and biological evaluation of 2-(4-alkoxy-3-cyano)phenyl-6-oxo-1,6-dihydropyrimidine-5-carboxylic acid derivatives as novel xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 181: (2019)
Shenyang Pharmaceutical University
Targeting DNA Repair in Tumor Cells via Inhibition of ERCC1-XPF.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7684-7696 (2019)
University of Alberta
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7643-7655 (2019)
Merck
Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7976-7997 (2019)
Boehringer Ingelheim Rcv
Ophiobolin-Type Sesterterpenoids from the Mangrove Endophytic Fungus ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2268-2278 (2019)
Sun Yat-Sen University
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2632-2634 (2019)
Second Military Medical University
A fragment-like approach to PYCR1 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2626-2631 (2019)
University of Strathclyde
Synthesis and evaluation of 2'H-spiro[cyclohexane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione derivatives as Mnk inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2650-2654 (2019)
University of South Australia
Discovery and optimization of pyridyl-cycloalkyl-carboxylic acids as inhibitors of microsomal prostaglandin E synthase-1 for the treatment of endometriosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2700-2705 (2019)
Bayer
Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9418-9437 (2019)
Astrazeneca
Can Cysteine Protease Cross-Class Inhibitors Achieve Selectivity?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10497-10525 (2019)
University of S£O Paulo
Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2670-2674 (2019)
Vanderbilt University
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2448-2451 (2019)
Shenyang Pharmaceutical University
Towards multi-target antidiabetic agents: Discovery of biphenyl-benzimidazole conjugates as AMPK activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2443-2447 (2019)
Volgograd State Medical University
Identification of new aryl hydrocarbon receptor (AhR) antagonists using a zebrafish model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Gwangju Institute of Science and Technology
Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 673-689 (2019)
Medical University of Lublin
Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 656-672 (2019)
Wuhan Institute of Technology
Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 648-655 (2019)
Medical School of Nanjing University
Peptide derivatives as inhibitors of NS2B-NS3 protease from Dengue, West Nile, and Zika flaviviruses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3963-3978 (2019)
Federal University of Alagoas
Molecular modelling, synthesis, and biological evaluations of a 3,5-disubstituted isoxazole fatty acid analogue as a PPAR?-selective agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4059-4068 (2019)
University of Oslo
Symmetry-based ligand design and evaluation of small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2464-2467 (2019)
Japan Tobacco
Protective effect of piceatannol and bioactive stilbene derivatives against hypoxia-induced toxicity in H9c2 cardiomyocytes and structural elucidation as 5-LOX inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 637-647 (2019)
University of Campania "L. Vanvitelli
Expedient assembly of Oligo-LacNAcs by a sugar nucleotide regeneration system: Finding the role of tandem LacNAc and sialic acid position towards siglec binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 627-636 (2019)
National Tsing-Hua University
A novel class of multitarget anti-Alzheimer benzohomoadamantane?chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 613-626 (2019)
University of Barcelona
Structure-aided optimization of 3-O-?-chacotriosyl ursolic acid as novel H5N1 entry inhibitors with high selective index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 4048-4058 (2019)
South China Agricultural University
Comparative analysis of stilbene and benzofuran neolignan derivatives as acetylcholinesterase inhibitors with neuroprotective and anti-inflammatory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2475-2479 (2019)
Gifu University
Novel SAR for quinazoline inhibitors of EHMT1 and EHMT2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2516-2524 (2019)
Mercachem
Sulfonate and sulfamate derivatives possessing benzofuran or benzothiophene nucleus as potent carbonic anhydrase II/IX/XII inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3889-3901 (2019)
University of Sharjah
COX-1/COX-2 inhibition activities and molecular docking study of newly designed and synthesized pyrrolo[3,4-c]pyrrole Mannich bases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3918-3928 (2019)
Wroclaw Medical University
Rational modification of Mannich base-type derivatives as novel antichagasic compounds: Synthesis, in vitro and in vivo evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3902-3917 (2019)
Universidad De Navarra
Discovery of human lactate dehydrogenase 5 inhibitors (hLDH5) with anti-lung cancer activity through an in silico method and biological validation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2459-2463 (2019)
The 5Th Affiliated Hospital of Shenzhen University Health Science Center
An insight into the medicinal perspective of synthetic analogs of indole: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 562-612 (2019)
Isf College of Pharmacy
Cell-active carbazole derivatives as inhibitors of the zika virus protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 536-545 (2019)
University of Patras
Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6958-6971 (2019)
Toho University
Design, Synthesis, and Biological Characterization of Orally Active 17?-Hydroxysteroid Dehydrogenase Type 2 Inhibitors Targeting the Prevention of Osteoporosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7289-7301 (2019)
Elexopharm
Identification of ?-Mangostin as a Potential Inhibitor of Microtubule Affinity Regulating Kinase 4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2252-2261 (2019)
Jamia Millia Islamia University
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6913-6924 (2019)
Servier Research Institute of Medicinal Chemistry
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 509-523 (2019)
Guangxi Medical University
Discovery and Development of a Series of Pyrazolo[3,4-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7473-7488 (2019)
Shanghai University
Discovery of 4-Methylquinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8873-8879 (2019)
TBA
5-Lipoxygenase as a drug target: A review on trends in inhibitors structural design, SAR and mechanism based approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3745-3759 (2019)
School of Advanced Sciences
Role of sulphur-heterocycles in medicinal chemistry: An update.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 486-508 (2019)
Maharaja Ranjit Singh Punjab Technical University
Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 449-456 (2019)
Purdue University
Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3813-3824 (2019)
Zhengzhou Children'S Hospital
Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3775-3787 (2019)
Astellas Pharma
Identification and characterization of the first fragment hits for SETDB1 Tudor domain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3866-3878 (2019)
University of Toronto
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3998-4012 (2019)
Vrije Universiteit Amsterdam
Inhibition of 3-phosphoglycerate dehydrogenase (PHGDH) by indole amides abrogates de novo serine synthesis in cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2503-2510 (2019)
Meyer Cancer Center
An overview on chemical structures as ?F508-CFTR correctors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 430-448 (2019)
University of Palermo
Urea moiety as amide bond mimetic in peptide-like inhibitors of VEGF-A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2493-2497 (2019)
University of Warsaw
Design, synthesis and biological evaluation of 6-deoxy O-spiroketal C-arylglucosides as novel renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 398-416 (2019)
Chinese Academy of Sciences
Synthesis of new 5,6,7,8-tetrahydropyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 383-397 (2019)
Medical University of Warsaw
Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 367-382 (2019)
Zhejiang University
Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 350-366 (2019)
East China University of Science and Technology
Total synthesis of dryocrassin ABBA and its analogues with potential inhibitory activity against drug-resistant neuraminidases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3846-3852 (2019)
Chinese Academy of Sciences
Design, synthesis and biological evaluation of 3-hydroxyquinazoline-2,4(1H,3H)-diones as dual inhibitors of HIV-1 reverse transcriptase-associated RNase H and integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3836-3845 (2019)
Shandong University
Design and synthesis of biotinylated Hexylselen as a probe to identify KGA allosteric inhibitors by a convenient biomolecular interaction assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2498-2502 (2019)
Zhejiang University
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3788-3796 (2019)
Marquette University
Structural development of 1H-pyrazolo-[3,4-b]pyridine-4-carboxylic acid derivatives as human peroxisome proliferator-activated receptor alpha (PPAR?)-selective agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2124-2128 (2019)
Okayama University
Strategies to develop selective CB![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 291-309 (2019)
The University of Sydney
Discovery of new potent dual sigma receptor/GluN2b ligands with antioxidant property as neuroprotective agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 268-282 (2019)
University of Trieste
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8973-8995 (2019)
TBA
Naturally Occurring Lumazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 2054-2065 (2019)
University of Auckland
Synthesis and Biological Activity of Peptide ?-Ketoamide Derivatives as Proteasome Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1086-1092 (2019)
University of Ferrara
Targeting IRAK4 for Degradation with PROTACs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1081-1085 (2019)
Glaxosmithkline Medicines Research Centre
Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1074-1080 (2019)
University of Southern California
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor ?/? Agonist for the Treatment of Primary Biliary Cirrhosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1068-1073 (2019)
Wuxi Apptec (Shanghai) Co.
Antioxidant, Anti-inflammatory, and Neuroprotective Effects of Novel Vinyl Sulfonate Compounds as Nrf2 Activator.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1061-1067 (2019)
Korea Institute of Science & Technology (Kist)
Development of Highly Selective Pyrimidine-Based Aldosterone Synthase (CYP11B2) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1056-1060 (2019)
Selenity Therapeutics
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1039-1044 (2019)
University of Maryland
Discovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1033-1038 (2019)
Prelude Therapeutics
Treatment of Cancers by Inhibition of Isoprenylcysteine Carboxyl Methyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 1024-1025 (2019)
Usona Institute
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2090-2093 (2019)
Genentech
Phenylhydrazides as inhibitors of Leishmania amazonensis arginase and antileishmanial activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3853-3859 (2019)
Universidade Federal Do Rio De Janeiro
Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 238-252 (2019)
Nanyang Normal University
Tapping the therapeutic potential of protein tyrosine phosphatase 4A with small molecule inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2008-2015 (2019)
University of Pittsburgh
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2294-2301 (2019)
Genentech
Identification of a potent small-molecule inhibitor of bacterial DNA repair that potentiates quinolone antibiotic activity in methicillin-resistant Staphylococcus aureus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Imperial College London
2-(phenylthio)ethylidene derivatives as anti-Trypanosoma cruzi compounds: Structural design, synthesis and antiparasitic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 191-203 (2019)
Universidade De Pernambuco
Design, synthesis, and biological evaluation of a new class of histone acetyltransferase p300 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 171-190 (2019)
Fudan University
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 916-935 (2019)
Fuzhou University
Optimization and Mechanistic Characterization of Pyridopyrimidine Inhibitors of Bacterial Biotin Carboxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7489-7505 (2019)
Achaogen
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7417-7430 (2019)
Bielefeld University
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6894-6912 (2019)
Universit£
Synthesis and biological evaluation of novel benzo[c][1,2,5]thiadiazol-5-yl and thieno[3,2-c]- pyridin-2-yl imidazole derivatives as ALK5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2070-2075 (2019)
Yanbian University
Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 154-170 (2019)
German University In Cairo
Functionalized 6-(piperidin-1-yl)-8,9-diphenyl purines as inverse agonists of the CB1 receptor - SAR efforts towards selectivity and peripheralization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3632-3649 (2019)
Rti International
Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3692-3706 (2019)
Astellas Pharma
Synthesis, pharmacological evaluation, and mechanistic study of adefovir mixed phosphonate derivatives bearing cholic acid and l-amino acid moieties for the treatment of HBV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3707-3721 (2019)
Guizhou Medical University
Synthesis of peptidomimetics and chemo-biological tools for CD95/PLC?1 interaction analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2094-2099 (2019)
Univ Rennes 1
Discovery, synthesis, and in vitro evaluation of a novel bioactive peptide for ACE and DPP-IV inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 99-110 (2019)
University of Mysore
Design of balanced COX inhibitors based on anti-inflammatory and/or COX-2 inhibitory ascidian metabolites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 86-98 (2019)
Pusan National University
Discovery of pyrazole-thiophene derivatives as highly Potent, orally active Akt inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 72-85 (2019)
Hangzhou Institute of Innovative Medicine
Merging memantine and ferulic acid to probe connections between NMDA receptors, oxidative stress and amyloid-? peptide in Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 111-120 (2019)
Alma Mater Studiorum - University of Bologna
A new approach to procyanidins synthesis with potent anti-adipogenic effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2079-2084 (2019)
Daegu University
1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3511-3531 (2019)
Chinese Academy of Sciences
Development of novel lithocholic acid derivatives as vitamin D receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3674-3681 (2019)
Tokyo Medical and Dental University
Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 51-61 (2019)
Universit£
Design, synthesis, biological evaluation and docking study of novel indole-2-amide as anti-inflammatory agents with dual inhibition of COX and 5-LOX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 41-50 (2019)
Anhui University of Chinese Medicine
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 15-27 (2019)
Yanbian University
Probing the Existence of a Metastable Binding Site at the ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7806-7839 (2019)
University of Copenhagen
Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7264-7288 (2019)
Chinese Academy of Sciences
Design, Synthesis, Evaluation, and Structural Studies of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7250-7263 (2019)
Jagiellonian University
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7302-7308 (2019)
Jinan University
Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7557-7574 (2019)
Icahn School of Medicine At Mount Sinai
Exploring the Natural Piericidins as Anti-Renal Cell Carcinoma Agents Targeting Peroxiredoxin 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7058-7069 (2019)
Chinese Academy of Sciences
Synthesis and biological evaluation of 1-alkylaminomethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3663-3673 (2019)
Universidad De Buenos Aires
Oxadiazole scaffolds in anti-tuberculosis drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1999-2007 (2019)
Institute of Chemical Technology
Discovery of Novel Naphthylphenylketone and Naphthylphenylamine Derivatives as Cell Division Cycle 25B (CDC25B) Phosphatase Inhibitors: Design, Synthesis, Inhibition Mechanism, and in Vitro Efficacy against Melanoma Cell Lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7089-7110 (2019)
University of Naples Federico Ii
Mechanistic Insight on the Mode of Action of Colletoic Acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6925-6940 (2019)
The University of Tennessee Health Science Center
Development of Dual Chitinase Inhibitors as Potential New Treatment for Respiratory System Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7126-7145 (2019)
Oncoarendi Therapeutics
Design, synthesis, and evaluation of novel N-(4-phenoxybenzyl)aniline derivatives targeting acetylcholinesterase, ?-amyloid aggregation and oxidative stress to treat Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3650-3662 (2019)
Indian Institute of Technology (Banaras Hindu University)
Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2100-2106 (2019)
Japan Tobacco
A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 180: 1-14 (2019)
Cardiff University
Boron in drug design: Recent advances in the development of new therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 791-804 (2019)
S£O Paulo State University
Antifungal activity, mode of action variability, and subcellular distribution of coumarin-based antifungal azoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 779-790 (2019)
Tel Aviv University
Synthesis and Evaluation of Carbonic Anhydrase Inhibitors with Carbon Monoxide Releasing Properties for the Management of Rheumatoid Arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7233-7249 (2019)
Universit£
Biological evaluation of molecules of the azaBINOL class as antiviral agents: Inhibition of HIV-1 RNase H activity by 7-isopropoxy-8-(naphth-1-yl)quinoline.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3595-3604 (2019)
Oregon State University
Discovery and characterization of trypanocidal cysteine protease inhibitors from the 'malaria box'.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 765-778 (2019)
Universidade Federal De Minas Gerais
Identification and characterization of a novel chemotype for human TLR8 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 744-752 (2019)
Freie Universit£T Berlin
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 707-722 (2019)
National Research Centre
Discovery of a Potent Kelch-Like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitor with Natural Proline Structure as a Cytoprotective Agent against Acetaminophen-Induced Hepatotoxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6796-6813 (2019)
China Pharmaceutical University
Discovery of 3-Oxabicyclo[4.1.0]heptane, a Non-nitrogen Containing Morpholine Isostere, and Its Application in Novel Inhibitors of the PI3K-AKT-mTOR Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6972-6984 (2019)
Glaxosmithkline R&D
Novel and Selective TLR7 Antagonists among the Imidazo[1,2-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7015-7031 (2019)
Universit£
Linear and Rationally Designed Stapled Peptides Abrogate TLR4 Pathway and Relieve Inflammatory Symptoms in Rheumatoid Arthritis Rat Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6495-6511 (2019)
Ajou University
Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2182-2188 (2019)
Yale University
Synthesis and evaluation of tetrahydropyrazolopyridine inhibitors of anion exchange protein SLC26A4 (pendrin).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2119-2123 (2019)
University of California
Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2150-2152 (2019)
Sun Yat-Sen University
2-Aryladenine derivatives as a potent scaffold for A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3551-3558 (2019)
Universidade Do Minho
Novel N-benzylpiperidine carboxamide derivatives as potential cholinesterase inhibitors for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 680-693 (2019)
University of Pretoria
Design, synthesis, and in vitro bioactivity evaluation of fluorine-containing analogues for sphingosine-1-phosphate 2 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3619-3631 (2019)
Washington University
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 608-622 (2019)
China Pharmaceutical University
Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 576-590 (2019)
Medical University of Gdansk
Styryl quinazolinones and its ethynyl derivatives induce myeloid differentiation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2286-2289 (2019)
National University of Singapore
Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 557-566 (2019)
Univ. Lille
Application of hydrazino and hydrazido linkers to connect benzenesulfonamides with hydrophilic/phobic tails for targeting the middle region of human carbonic anhydrases active site: Selective inhibitors of hCA IX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 547-556 (2019)
Cairo University
Recent progress in histone methyltransferase (G9a) inhibitors as anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 537-546 (2019)
Southern Medical University
Endomorphin-2 analogs containing modified tyrosines: Biological and theoretical investigation of the influence on conformation and pharmacological profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 527-536 (2019)
Medical University of Lodz
Novel phenanthridin-6(5H)-one derivatives as potent and selective BET bromodomain inhibitors: Rational design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 502-514 (2019)
Henan University of Traditional Chinese Medicine
Alkaloids Purified from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1953-1960 (2019)
American University of Health Sciences
Monosaccharide Analogues of Anticancer Peptide R-Lycosin-I: Role of Monosaccharide Conjugation in Complexation and the Potential of Lung Cancer Targeting and Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7857-7873 (2019)
TBA
Virtual Screening Approach and Investigation of Structure-Activity Relationships To Discover Novel Bacterial Topoisomerase Inhibitors Targeting Gram-Positive and Gram-Negative Pathogens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7445-7472 (2019)
Angelini
Kinase Atlas: Druggability Analysis of Potential Allosteric Sites in Kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6512-6524 (2019)
University of California
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6751-6764 (2019)
Oric Pharmaceuticals
Route to Prolonged Residence Time at the Histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6630-6644 (2019)
Vu University Amsterdam
Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3574-3586 (2019)
Affiliated To Sardar Patel University
Melanogenic inhibitory effects of Triangularin in B16F0 melanoma cells, in vitro and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3722-3728 (2019)
Universidad Nacional De C£Rdoba
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2208-2217 (2019)
Advinus Therapeutics
Discovery of novel 9H-purin derivatives as dual inhibitors of HDAC1 and CDK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2136-2140 (2019)
Chongqing Medical University
Sulfonamide derivatives as multi-target agents for complex diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2042-2050 (2019)
University of Massachusetts Boston
Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 483-492 (2019)
The Czech Academy of Sciences
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 470-482 (2019)
Chinese Academy of Sciences
Bis(het)aryl-1,2,3-triazole quinuclidines as ?7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 449-469 (2019)
Universit£
Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7042-7057 (2019)
Institute of Biotechnology of The Czech Academy of Sciences
Homoharringtonine stabilizes secondary structure of guanine-rich sequence existing in the 5'-untranslated region of Nrf2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2189-2196 (2019)
Dongguk University
Structure-Based Development of (1-(3'-Mercaptopropanamido)methyl)boronic Acid Derived Broad-Spectrum, Dual-Action Inhibitors of Metallo- and Serine-?-lactamases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7160-7184 (2019)
Sichuan University
Prenylated Stilbenoids Affect Inflammation by Inhibiting the NF-?B/AP-1 Signaling Pathway and Cyclooxygenases and Lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1839-1848 (2019)
Czech Academy of Sciences
Probing the Ligand-Binding Pocket of BTN3A1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6814-6823 (2019)
Western Michigan University
Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2051-2073 (2020)
University of Nebraska Medical Center
7-Methylation of Chenodeoxycholic Acid Derivatives Yields a Substantial Increase in TGR5 Receptor Potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6824-6830 (2019)
University of Minnesota
A- and D-Ring Structural Modifications of an Androsterone Derivative Inhibiting 17?-Hydroxysteroid Dehydrogenase Type 3: Chemical Synthesis and Structure-Activity Relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7070-7088 (2019)
Chu De Queb£C-Research Center
Multistage Screening Reveals 3-Substituted Indolin-2-one Derivatives as Novel and Isoform-Selective c-Jun N-terminal Kinase 3 (JNK3) Inhibitors: Implications to Drug Discovery for Potential Treatment of Neurodegenerative Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6645-6664 (2019)
Peking University
Polycerasoidol, a Natural Prenylated Benzopyran with a Dual PPAR?/PPAR? Agonist Activity and Anti-inflammatory Effect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1802-1812 (2019)
University of Valencia
Small-molecule agents for the treatment of inflammatory bowel disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2034-2041 (2019)
Gilead Sciences
Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 404-422 (2019)
Ntz Lab
Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6482-6494 (2019)
Glaxosmithkline
Bisubstrate Inhibitors of Nicotinamide ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6597-6614 (2019)
Leiden University
Discovery of Clinical Candidate (1![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6705-6733 (2019)
Newlink Genetics
Design, synthesis and biological evaluations of 2-amino-4-(1-piperidine) pyridine derivatives as novel anti crizotinib-resistant ALK/ROS1 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 358-375 (2019)
Southern Medical University
Discovery of a novel 2,5-dihydroxycinnamic acid-based 5-lipoxygenase inhibitor that induces apoptosis and may impair autophagic flux in RCC4 renal cancer cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 347-357 (2019)
Universit£
TASK Channels Pharmacology: New Challenges in Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10044-10058 (2019)
Universidad De Talca
Chivosazole A Modulates Protein-Protein Interactions of Actin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1961-1970 (2019)
Ludwig-Maximilians-University
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8996-9007 (2019)
Icahn School of Medicine At Mount Sinai
Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6561-6574 (2019)
Tsinghua University
Discovery of a Potent and Selective CCR4 Antagonist That Inhibits T![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6190-6213 (2019)
Rapt Therapeutics
The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6287-6314 (2019)
National Institute On Drug Abuse-Intramural Research Program
Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure-Activity Relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6063-6082 (2019)
Korea University
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2265-2269 (2019)
Bristol-Myers Squibb
Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2016-2024 (2019)
Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2168-2172 (2019)
Southeast University
New insights into the binding mode of pyridine-3-carboxamide inhibitors of E. coli DNA gyrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3546-3550 (2019)
University of Leeds
Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7146-7159 (2019)
Cancer Therapeutics Crc
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 310-324 (2019)
National Engineering Research Center For The Emergency Drug
Human disorders associated with inflammation and the evolving role of natural products to overcome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 272-309 (2019)
University of Delhi
Sulfamates in drug design and discovery: Pre-clinical and clinical investigations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 257-271 (2019)
University of Sharjah
Structure-activity relationship study and biological evaluation of SAC-Garlic acid conjugates as novel anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 233-245 (2019)
Southern Medical University
Rational approaches, design strategies, structure activity relationship and mechanistic insights for therapeutic coumarin hybrids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3477-3510 (2019)
Guru Nanak Dev University
Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3559-3567 (2019)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Design, synthesis and activity of novel 2,6-disubstituted purine derivatives, potential small molecule inhibitors of signal transducer and activator of transcription 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 218-232 (2019)
Wenzhou Medical University
Discovery of novel pyrimidine-based benzothiazole derivatives as potent cyclin-dependent kinase 2 inhibitors with anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 196-207 (2019)
Southern Medical University
Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3396-3407 (2019)
Cracow University of Technology
Discovery of BR102375, a new class of non-TZD PPAR? full agonist for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2275-2282 (2019)
Boryung Pharmaceuticals
New dual ligands for the D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2236-2242 (2019)
Cracow University of Technology
Inhibition of neutral lipid synthesis by avarols from a marine sponge.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2283-2285 (2019)
Kitasato University
Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 147-165 (2019)
Yunnan University
Light-controlled inhibition of BRAFV600E kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 133-146 (2019)
University Medical Center Groningen
Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7185-7209 (2019)
Monash University
De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6615-6629 (2019)
Max Planck Institute For Developmental Biology
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6083-6101 (2019)
Chinese Academy of Sciences
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2224-2228 (2019)
Vanderbilt University
Synthesis and biological evaluation of PSMA-targeting paclitaxel conjugates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2229-2235 (2019)
Lomonosov Moscow State University
l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2254-2258 (2019)
University of Nebraska At Kearney
Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 84-99 (2019)
University of Maryland
Selective Toll-like receptor 7 agonists with novel chromeno[3,4-d]imidazol-4(1H)-one and 2-(trifluoromethyl)quinoline/ quinazoline-4-amine scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 109-122 (2019)
University of Ljubljana
Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7400-7416 (2019)
Bristol-Myers Squibb Research & Development
Molecular Networking Reveals the Chemical Diversity of Selaginellin Derivatives, Natural Phosphodiesterase-4 Inhibitors from ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1820-1830 (2019)
Seoul National University
Meroterpenoids with BACE1 Inhibitory Activity from the Fruiting Body of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1797-1801 (2019)
Meiji Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-? Motif Kinase (ZAK) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2114-2130 (2020)
Jinan University
Design, Synthesis, and Anti-RNA Virus Activity of 6'-Fluorinated-Aristeromycin Analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6346-6362 (2019)
Seoul National University
Structure-Based Discovery of M-89 as a Highly Potent Inhibitor of the Menin-Mixed Lineage Leukemia (Menin-MLL) Protein-Protein Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6015-6034 (2019)
TBA
Philanthotoxin Analogues That Selectively Inhibit Ganglionic Nicotinic Acetylcholine Receptors with Exceptional Potency.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6214-6222 (2019)
University of Nottingham
Engineered Substrate for Cyclooxygenase-2: A Pentapeptide Isoconformational to Arachidonic Acid for Managing Inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6363-6376 (2019)
TBA
Photoactivatable Prolyl Hydroxylase 2 Inhibitors for Stabilizing the Hypoxia-Inducible Factor with Light.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 7583-7588 (2019)
China Pharmaceutical University
Fragment-Based Discovery of Novel Potent Sepiapterin Reductase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6391-6397 (2019)
Gr�Nenthal
Design of wogonin-inspired selective cyclin-dependent kinase 9 (CDK9) inhibitors with potent in vitro and in vivo antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 782-801 (2019)
China Pharmaceutical University
Structure-activity relationship study of thiazolyl-hydroxamate derivatives as selective histone deacetylase 6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3408-3420 (2019)
Sungkyunkwan University
Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3440-3450 (2019)
Mitsubishi Tanabe Pharma
Structure-based design of potent linear peptide inhibitors of the YAP-TEAD protein-protein interaction derived from the YAP omega-loop sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2316-2319 (2019)
Novartis Institutes For Biomedical Research
The discovery of novel 3-aryl-indazole derivatives as peripherally restricted pan-Trk inhibitors for the treatment of pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2320-2326 (2019)
Asahi Kasei Pharma
Discovery of novel biaryl sulfonamide based Mcl-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2375-2382 (2019)
Forma Therapeutics
Discovery and structure-activity relationship of novel diphenylthiazole derivatives as BTK inhibitor with potent activity against B cell lymphoma cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 767-781 (2019)
Nankai University
Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 38-55 (2019)
Shanghai Institute of Materia Medica (Simm)
Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2415-2427 (2019)
Gilead Sciences
2-Aminoimidazole-based antagonists of the 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 179: 1-15 (2019)
Polish Academy of Sciences
Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 740-751 (2019)
Jagiellonian University
Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 726-739 (2019)
Nanyang Normal University
2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 705-714 (2019)
Central China Normal University
Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3358-3363 (2019)
Kanazawa University
Medicinal prospects of antioxidants: A review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 687-704 (2019)
Jamia Hamdard (Deemed To Be University)
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 667-686 (2019)
West China Hospital of Sichuan University
Inhibition of polypeptide N-acetyl-?-galactosaminyltransferases is an underlying mechanism of dietary polyphenols preventing colorectal tumorigenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3372-3382 (2019)
Shanghai Jiao Tong University
Discovery of novel N-methyl carbazole tethered rhodanine derivatives as direct inhibitors of Mycobacterium tuberculosis InhA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2338-2344 (2019)
University of Kwazulu-Natal (Ukzn)
SAR studies in the sulfonyl carboxamide class of HBV capsid assembly modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2405-2409 (2019)
Novira Therapeutics
Discovery of 2,3'-diindolylmethanes as a novel class of PCSK9 modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2345-2348 (2019)
University of Wisconsin
Identification of benzo[cd]indol-2(1H)-ones as novel Atg4B inhibitors via a structure-based virtual screening and a novel AlphaScreen assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 648-666 (2019)
Institute of Advanced Chemistry of Catalonia
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 996-1001 (2019)
Shanghai Hengrui Pharmaceutical
Chain-Shortened Myostatin Inhibitory Peptides Improve Grip Strength in Mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 985-990 (2019)
Tokyo University of Pharmacy and Life Sciences
Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 978-984 (2019)
Experimental Drug Development Centre
Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 972-977 (2019)
Astrazeneca
4-Aryl Pyrrolidines as Novel Orally Efficacious Antimalarial Agents. Part 2: 2-Aryl-![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 966-971 (2019)
Saint Louis University
Modifications at Arg and Ile Give Neurotensin(8-13) Derivatives with High Stability and Retained NTS![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 960-965 (2019)
University of Regensburg
Discovery of Imidazoisoindole Derivatives as Highly Potent and Orally Active Indoleamine-2,3-dioxygenase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 949-953 (2019)
Shanghai Hengrui Pharmaceutical
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 941-948 (2019)
Pfizer
Synthesis and Optimization of K![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 929-935 (2019)
University of Pittsburgh
DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 923-928 (2019)
Kyushu University
Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 911-916 (2019)
Bristol-Myers Squibb
Discovery of GlyT2 Inhibitors Using Structure-Based Pharmacophore Screening and Selectivity Studies by FEP+ Calculations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 904-910 (2019)
The University of Texas At El Paso
Computer-Aided Selective Optimization of Side Activities of Talinolol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 899-903 (2019)
Goethe-University of Frankfurt
Structure-Based Design and Synthesis of an Isozyme-Selective MTHFD2 Inhibitor with a Tricyclic Coumarin Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 893-898 (2019)
Daiichi Sankyo
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 887-892 (2019)
Novartis Institutes For Biomedical Research
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 869-873 (2019)
East China University of Science and Technology
Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 863-868 (2019)
Umr Cnrs 7285
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 857-862 (2019)
Glaxosmithkline
LRRK2 Kinase Inhibitors as Possible Therapy for Parkinson's Disease and Other Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 846-847 (2019)
Therachem Research Medilab
Rapalogs Potential as Practical Alternatives to Rapamycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 843-845 (2019)
Therachem Research Medilab
Potential of ROCK Inhibitors as Treatment for Cardiovascular Diseases, Cancer, and More.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 841-842 (2019)
Therachem Research Medilab
Discovery and Biological evaluation of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione derivatives as potent Bruton's tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3390-3395 (2019)
East China University of Science & Technology
Synthesis and molecular modeling of novel non-sulfonylureas as hypoglycemic agents and selective ALR2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3383-3389 (2019)
Suez Canal University
Identification and characterization of potent and selective inhibitors targeting protein tyrosine phosphatase 1B (PTP1B).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2358-2363 (2019)
Zhejiang Sci-Tech University
Structure-activity relationship studies on Bax activator SMBA1 for the treatment of ER-positive and triple-negative breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 589-605 (2019)
University of Texas Medical Branch
Preparation of bivalent agonists for targeting the mu opioid and cannabinoid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 571-588 (2019)
Biological Research Centre of The Hungarian Academy of Sciences
Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38? and BRD4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 530-543 (2019)
Newcastle University
Discovery of DC_H31 as potential mutant IDH1 inhibitor through NADPH-based high throughput screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3229-3236 (2019)
Huazhong Agricultural University
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 468-483 (2019)
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Polybenzyls from Gastrodia elata, their agonistic effects on melatonin receptors and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3299-3306 (2019)
Chinese Academy of Sciences
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3339-3346 (2019)
National Institute of Advanced Industrial Science and Technology (Aist)
Switching on the activity of 1,5-diaryl-pyrrole derivatives against drug-resistant ESKAPE bacteria: Structure-activity relationships and mode of action studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 500-514 (2019)
Sapienza University of Rome
Identify liver X receptor ? modulator building blocks by developing a fluorescence polarization-based competition assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 458-467 (2019)
Sun Yat-Sen University
Design, synthesis and biological evaluation of novel 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole triazole derivatives as potent TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 433-445 (2019)
Henan University
Exploiting the 1-(4-fluorobenzyl)piperazine fragment for the development of novel tyrosinase inhibitors as anti-melanogenic agents: Design, synthesis, structural insights and biological profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 380-389 (2019)
Polo Universitario Ss. Annunziata
Synthesis of N'-propylhydrazide analogs of hydroxamic inhibitors of histone deacetylases (HDACs) and evaluation of their impact on activities of HDACs and replication of hepatitis C virus (HCV).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2369-2374 (2019)
Russian Academy of Sciences
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 352-364 (2019)
Shanghai Pharmaceuticals Holding
Tetrazole hybrids with potential anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 341-351 (2019)
Henan University of Chinese Medicine
Targeting dihydrofolate reductase: Design, synthesis and biological evaluation of novel 6-substituted pyrrolo[2,3-d]pyrimidines as nonclassical antifolates and as potential antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 329-340 (2019)
Hebei Medical University
Discovery of a Thiadiazole-Pyridazine-Based Allosteric Glutaminase 1 Inhibitor Series That Demonstrates Oral Bioavailability and Activity in Tumor Xenograft Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6540-6560 (2019)
Astrazeneca
Isolation of Sesquiterpene-Amino Acid Conjugates, Onopornoids A-D, and a Flavonoid Glucoside from Onopordum alexandrinum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1471-1477 (2019)
Hiroshima University
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6575-6596 (2019)
Forma Therapeutics
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against ?-synuclein aggregation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3089-3096 (2019)
Zhengzhou University
Synthesis of oxadiazole-coupled-thiadiazole derivatives as a potent ?-glucuronidase inhibitors and their molecular docking study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3145-3155 (2019)
Imam Abdulrahman Bin Faisal University
Evaluating the effects of fluorine on biological properties and metabolic stability of some antitubulin 3-substituted 7-phenyl-pyrroloquinolinones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 297-314 (2019)
University of Padova
Histone acetyltransferase inhibitors: An overview in synthesis, structure-activity relationship and molecular mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 259-286 (2019)
Sichuan University
PeIA-5466: A Novel Peptide Antagonist Containing Non-natural Amino Acids That Selectively Targets ?3?2 Nicotinic Acetylcholine Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6262-6275 (2019)
Veterans Affairs Medical Center
Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6003-6014 (2019)
Roche Pharma Research and Early Development
Why Some Targets Benefit from beyond Rule of Five Drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 10005-10025 (2019)
Boston University
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6175-6189 (2019)
Universidad Nacional De Colombia
De Novo Design of Boron-Based Peptidomimetics as Potent Inhibitors of Human ClpP in the Presence of Human ClpX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6377-6390 (2019)
University of Toronto
Defined concatenated ?6?1?3?2 GABA![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3167-3178 (2019)
Medical University of Vienna
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 243-258 (2019)
Alma Mater Studiorum-University of Bologna
Discovery of novel Bcr-Abl![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 232-242 (2019)
Xi'An Jiaotong University
Design, synthesis, antitumor activities and biological studies of novel diaryl substituted fused heterocycles as dual ligands targeting tubulin and katanin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 177-194 (2019)
Fudan University
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6330-6345 (2019)
Rti International
A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6035-6046 (2019)
Universidad Complutense De Madrid
Inhibitory selectivity among class I HDACs has a major impact on inflammatory gene expression in macrophages.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 457-466 (2019)
University of Groningen
Synthesis of N-hydroxycinnamoyl amide derivatives and evaluation of their anti-oxidative and anti-tyrosinase activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Beijing Technology and Business University
Design, synthesis and biological evaluation of novel aryl-acrylic derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3135-3144 (2019)
Shenyang Pharmaceutical University
Improvement of Asparagine Ethylenediamines as Anti-malarial ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6137-6145 (2019)
Weill Cornell Medicine
Synthesis and anti-tumor efficacy of novel 2, 4-diarylaminopyrimidine derivatives bearing N-(3-pyridinylmethyl) urea moiety as anaplastic lymphoma kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 141-153 (2019)
Peking University Health Science Center
Discovery of 1,2,4-oxadiazole-Containing hydroxamic acid derivatives as histone deacetylase inhibitors potential application in cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 116-130 (2019)
Sichuan University and Collaborative Innovation Center of Biotherapy
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1918-1921 (2019)
Bristol-Myers Squibb
Development of substituted pyrido[3,2-d]pyrimidines as potent and selective dihydrofolate reductase inhibitors for pneumocystis pneumonia infection.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1874-1880 (2019)
Duquesne University
Backbone modifications in peptidic inhibitors of flaviviral proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1913-1917 (2019)
Heidelberg University
Naphthalene-triazolopyrimidine hybrid compounds as potential multifunctional anti-Alzheimer's agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3156-3166 (2019)
Jamia Millia Islamia (Central University)
Nature-inspired pyrrolo[2,3-d]pyrimidines targeting the histamine H![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3194-3200 (2019)
Heinrich Heine University D£Sseldorf
Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: (2019)
Xi'An Jiaotong University
New pyrazolopyrimidine derivatives as Leishmania amazonensis arginase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 3061-3069 (2019)
Instituto De Tecnologia Em Farmacos
Development of potential preclinical candidates with promising in vitro ADME profile for the inhibition of type 1 and type 2 17?-Hydroxysteroid dehydrogenases: Design, synthesis, and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 93-107 (2019)
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Design, synthesis and biological evaluation of "Multi-Site"-binding influenza virus neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 64-80 (2019)
Shandong University
Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1985-1993 (2019)
Harvard Medical School
1-Phenyl-dihydrobenzoindazoles as novel colchicine site inhibitors: Structural basis and antitumor efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 448-456 (2019)
Second Military Medical University
An overview on the synthetic and medicinal perspectives of indenopyrazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 178: 1-12 (2019)
Csir-Indian Institute of Chemical Technology
Chalcone derivatives bearing chromen or benzo[f]chromen moieties: Design, synthesis, and evaluations of anti-inflammatory, analgesic, selective COX-2 inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1909-1912 (2019)
Zhejiang Ocean University
Discovery of piperazic acid peptide deformylase inhibitors with in vivo activity for respiratory tract and skin infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 2410-2414 (2019)
Glaxosmithkline
3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1891-1894 (2019)
Okayama University Graduate School of Medicine
Design, synthesis and biological evaluation of 2-H pyrazole derivatives containing morpholine moieties as highly potent small molecule inhibitors of APC-Asef interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 425-447 (2019)
Nanjing University
Investigating 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole as scaffold of butyrylcholinesterase-selective inhibitors with additional neuroprotective activities for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 414-424 (2019)
University of Bari Aldo Moro
Enhanced tumor retention of NTSR1-targeted agents by employing a hydrophilic cysteine cathepsin inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 386-400 (2019)
University of Nebraska Medical Center
Design and synthesis of novel xanthone-triazole derivatives as potential antidiabetic agents: ?-Glucosidase inhibition and glucose uptake promotion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 362-373 (2019)
Sun Yat-Sen University
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 316-337 (2019)
Institute of Cancer Research
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 269-290 (2019)
Universit£
Caffeic acid phenethyl ester (CAPE)-derivatives act as selective inhibitors of acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 259-268 (2019)
Martin-Luther-University Halle-Wittenberg
Development of the "hidden" multifunctional agents for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 247-258 (2019)
Zhejiang Academy of Medical Sciences
Potent 5-Cyano-6-phenyl-pyrimidin-Based Derivatives Targeting DCN1-UBE2M Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5382-5403 (2019)
Zhengzhou University
Discovery of naphthacemycins as a novel class of PARP1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1904-1908 (2019)
North China Pharmaceutical Group
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1962-1967 (2019)
Astrazeneca
Chemical conversion of nicotinamide into type I positive allosteric modulator of ?7 nAChRs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1928-1933 (2019)
Peking University
Development of covalent antagonists for ?1- and ?2-adrenergic receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2959-2971 (2019)
Friedrich-Alexander Universit£T Erlangen-N£Rnberg
Andrographolide: A natural product template for the generation of structurally and biologically diverse diterpenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 513-533 (2019)
Institute of Higher Learning
Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 221-234 (2019)
Central University of Punjab
A novel indirubin derivative that increases somatic cell plasticity and inhibits tumorigenicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2923-2934 (2019)
Gwangju Institute of Science and Technology
Discovery of conolidine derivative DS39201083 as a potent novel analgesic without mu opioid agonist activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1938-1942 (2019)
Daiichi Sankyo
Determining the necessity of phenyl ring ?-character in warfarin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1954-1956 (2019)
University of Queensland
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5901-5919 (2019)
National Institute of Biological Sciences (Nibs)
Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5844-5862 (2019)
Kyoto Prefectural University of Medicine
Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1974-1980 (2019)
Janssen Research & Development
Naturally occurring biflavonoids with amyloid ? aggregation inhibitory activity for development of anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1994-1997 (2019)
Meiji Pharmaceutical University
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2905-2913 (2019)
Biogen
Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 198-211 (2019)
Anhui Medical University
Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 188-197 (2019)
University of Florence
Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5810-5831 (2019)
Ku Leuven
Discovery of ABT-957: 1-Benzyl-5-oxopyrrolidine-2-carboxamides as selective calpain inhibitors with enhanced metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1968-1973 (2019)
Abbvie Deutschland
SAR study of celastrol analogs targeting Nur77-mediated inflammatory pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 171-187 (2019)
Xiamen University
Developments in the anticancer activity of structurally modified curcumin: An up-to-date review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 76-104 (2019)
Manipal Academy of Higher Education
The chemical biology of apoptosis: Revisited after 17 years.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 63-75 (2019)
Tsinghua University
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and ?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 47-62 (2019)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Universit£T M£Nster
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 32-46 (2019)
Peking University Health Science Center
Estrogen signaling: An emanating therapeutic target for breast cancer treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 116-143 (2019)
Indian Institute of Technology (Bhu)
Development of novel human lactate dehydrogenase A inhibitors: High-throughput screening, synthesis, and biological evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 177: 105-115 (2019)
Hubei University of Medicine
Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1727-1731 (2019)
University of North Carolina At Chapel Hill
A high throughput substrate binding assay reveals hexachlorophene as an inhibitor of the ER-resident HSP70 chaperone GRP78.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1689-1693 (2019)
University of Arizona
Quinoline and thiazolopyridine allosteric inhibitors of MALT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1694-1698 (2019)
Harvard Medical School
Investigation of flexibility of neuraminidase 150-loop using tamiflu derivatives in influenza A viruses H1N1 and H5N1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2935-2947 (2019)
Charles University
2-Phenyl-8-(1-phenylallyl)-chromenone compounds have a pan-PPAR modulator pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2948-2958 (2019)
Seoul National University
Design, synthesis, and biological evaluation of novel 4-oxobenzo[d]1,2,3-triazin-benzylpyridinum derivatives as potent anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2914-2922 (2019)
University of Zanjan
Development of selective small molecule MDM2 degraders based on nutlin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 476-491 (2019)
University of Wisconsin-Madison
Recent update on anti-dengue drug discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 431-455 (2019)
Queensland University of Technology
Highly tunable thiosulfonates as a novel class of cysteine protease inhibitors with anti-parasitic activity against Schistosoma mansoni.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2857-2870 (2019)
University of Glasgow
Transformation of Santonin to a Naproxen Analogue with Anti-Inflammatory Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1710-1713 (2019)
Indian Institute of Integrative Medicine (Csir)
Design and synthesis of a novel series of cyanoindole derivatives as potent ?-secretase modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1737-1745 (2019)
Janssen Research & Development
Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 247-268 (2019)
Jilin University
Hydroxamic Acid Derivatives of ?-Carboline/Hydroxycinnamic Acid Hybrids Inducing Apoptosis and Autophagy through the PI3K/Akt/mTOR Pathways.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1442-1450 (2019)
Nantong University
Caspase-Dependent Apoptosis in Prostate Cancer Cells and Zebrafish by Corchorusoside C from Streptocaulon juventas.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1645-1655 (2019)
University of Illinois At Chicago
Isolation and Biological Activity of 8- Epitetrodotoxin and the Structure of a Possible Biosynthetic Shunt Product of Tetrodotoxin, Cep-226A, from the Newt Cynops ensicauda popei.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1656-1663 (2019)
Tohoku University
From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5522-5540 (2019)
University of Calgary
Design, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6992-7014 (2019)
TBA
Development of Peptide-Based Sirtuin Defatty-Acylase Inhibitors Identified by the Fluorescence Probe, SFP3, That Can Efficiently Measure Defatty-Acylase Activity of Sirtuin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5434-5452 (2019)
Nagoya City University
Design and Synthesis of Potent, Selective Inhibitors of Protein Arginine Methyltransferase 4 against Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5414-5433 (2019)
Chinese Academy of Sciences
Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at ?-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5797-5809 (2019)
University of Copenhagen
VU6005806/AZN-00016130, an advanced M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1714-1718 (2019)
Vanderbilt University School of Medicine
Synthetic heterocyclic candidates as promising ?-glucosidase inhibitors: An overview.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 343-377 (2019)
Babasaheb Bhimrao Ambedkar University (A Central University)
An update about the crucial role of stereochemistry on the effects of Peroxisome Proliferator-Activated Receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 326-342 (2019)
Universit£
1,3-Dioxane as a scaffold for potent and selective 5-HT![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 310-325 (2019)
Universit£
Multi-targeting protein-protein interaction inhibitors: Evolution of macrocyclic ligands with embedded carbohydrates (MECs) to improve selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 292-309 (2019)
National University of Ireland Galway
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1842-1848 (2019)
Merck
Synthesis and biological evaluation of novel xanthine derivatives as potential apoptotic antitumor agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 117-128 (2019)
Deraya University
Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1854-1858 (2019)
Merck
Capsaicin-like analogue induced selective apoptosis in A2058 melanoma cells: Design, synthesis and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2893-2904 (2019)
University of S£O Paulo
Natural products as multidrug resistance modulators in cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 268-291 (2019)
Central University of Punjab
Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 248-267 (2019)
China Pharmaceutical University
Multi-target design strategies for the improved treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 228-247 (2019)
China Pharmaceutical University
Thioether-based 2-aminobenzamide derivatives: Novel HDAC inhibitors with potent in vitro and in vivo antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 195-207 (2019)
Beijing University of Chemical Technology
Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 187-194 (2019)
Heidelberg University
Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1859-1863 (2019)
Shenyang Pharmaceutical University
Synthesis and biological evaluation of acylthiourea against DUSP1 inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1746-1748 (2019)
Anticancer Agent Research Center
Identification and immunological evaluation of novel TLR2 agonists through structure optimization of Pam![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2784-2800 (2019)
Fudan University
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active ROR? inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1799-1806 (2019)
Inventiva
Discovery of novel pyridazine derivatives as glucose transporter type 4 (GLUT4) translocation activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1785-1790 (2019)
Daiichi Sankyo
The past, present and future of potential small-molecule drugs targeting p53-MDM2/MDMX for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 92-104 (2019)
Sichuan University
Nitric Oxide-Releasing Selective Estrogen Receptor Modulators: A Bifunctional Approach to Improve the Therapeutic Index.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6525-6539 (2019)
Helmholtz-Zentrum Dresden-Rossendorf
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5579-5593 (2019)
Shanghai Institute of Materia Medica
Unnatural Tripeptides as Potent Positive Allosteric Modulators of T1R2/T1R3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 800-805 (2019)
Ajinomoto
Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 792-799 (2019)
University of Texas Medical Branch
Discovery of CDK5 Inhibitors through Structure-Guided Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 786-791 (2019)
University of South Australia
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 780-785 (2019)
Cellzome
Identification of New Small-Molecule Inducers of Estrogen-related Receptor ? (ERR?) Degradation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 767-772 (2019)
Jinan University
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of ?7 nAChRs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 754-760 (2019)
Bionomics
Discovery of Novel Pyrido-pyridazinone Derivatives as FER Tyrosine Kinase Inhibitors with Antitumor Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 10: 737-742 (2019)
Daiichi Sankyo
Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2729-2740 (2019)
Shenyang Pharmaceutical University
Application of the concept of oxime library screening by mass spectrometry (MS) binding assays to pyrrolidine-3-carboxylic acid derivatives as potential inhibitors of ?-aminobutyric acid transporter 1 (GAT1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2753-2763 (2019)
Ludwig Maximilians-Universit£T M£Nchen
Discovery and synthesis of novel indole derivatives-containing 3-methylenedihydrofuran-2(3H)-one as irreversible LSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 357-372 (2019)
Zhengzhou University
Discovery of Dioxino[2,3-f]quinazoline derivative VEGFR-2 inhibitors exerting significant antipro-liferative activity in HUVECs and mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 349-356 (2019)
Beijing University of Technology
Structure-guided optimization of 4,6-substituted-1,3,5-triazin-2(1H)-ones as catalytic inhibitors of human DNA topoisomerase II?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 330-348 (2019)
Slovenia
Pyridinylimidazoles as dual glycogen synthase kinase 3?/p38? mitogen-activated protein kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 309-329 (2019)
Eberhard Karls Universit£T T£Bingen
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor ?.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1558-1564 (2019)
Chinese Academy of Sciences
Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5616-5627 (2019)
TBA
-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6665-6681 (2019)
Ningxia Medical University
Assessment of quinazolinone derivatives as novel non-nucleoside hepatitis B virus inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 41-49 (2019)
Xuzhou Medical University
Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 176: 11-20 (2019)
Fudan University
Synthesis, biological evaluation, and molecular docking study of sulfonate derivatives as nucleotide pyrophosphatase/phosphodiesterase (NPP) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2741-2752 (2019)
University of Sharjah
Fasudil dichloroacetate (FDCA), an orally available agent with potent therapeutic efficiency on monocrotaline-induced pulmonary arterial hypertension rats.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1812-1818 (2019)
The First Affiliated Hospital of Nanjing Medical University
Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1825-1830 (2019)
Jouf University
Structural Tailoring of a Novel Fluorescent IRE-1 RNase Inhibitor to Precisely Control Its Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5404-5413 (2019)
The Wistar Institute
Hydroxyl Groups in Synthetic and Natural-Product-Derived Therapeutics: A Perspective on a Common Functional Group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8915-8930 (2019)
University of Basel
Structure-activity relationship and synthetic methodologies of ?-santonin derivatives with diverse bioactivities: A mini-review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 215-233 (2019)
Shanghai Ocean University
Design, synthesis and pharmacological evaluation of a novel mTOR-targeted anti-EV71 agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 172-186 (2019)
National Engineering Research Center For The Emergency Drug
Discovery of tropinone-thiazole derivatives as potent caspase 3/7 activators, and noncompetitive tyrosinase inhibitors with high antiproliferative activity: Rational design, one-pot tricomponent synthesis, and lipophilicity determination.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 162-171 (2019)
Nicolaus Copernicus University
Development of Small-Molecules Targeting Receptor Activator of Nuclear Factor-?B Ligand (RANKL)-Receptor Activator of Nuclear Factor-?B (RANK) Protein-Protein Interaction by Structure-Based Virtual Screening and Hit Optimization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5370-5381 (2019)
Shanghai Jiaotong University School of Medicine
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 6223-6240 (2019)
Genentech
Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8881-8914 (2019)
China Pharmaceutical University
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2801-2812 (2019)
School of Marine Science and Technology
Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2771-2783 (2019)
Shandong University
Design, Synthesis, and Preclinical Efficacy of Novel Nonretinoid Antagonists of Retinol-Binding Protein 4 in the Mouse Model of Hepatic Steatosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5470-5500 (2019)
Albany College of Pharmacy and Health Sciences
Structure based designing of triazolopyrimidone-based reversible inhibitors for kinases involved in NSCLC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1565-1571 (2019)
Punjabi University
A new lateral root growth inhibitor from the sponge-derived fungus Aspergillus sp. LS45.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1593-1596 (2019)
Ningbo University
Targeting tropomyosin receptor kinase for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 129-148 (2019)
China Pharmaceutical University
Ligand retargeting by binding site analogy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 107-113 (2019)
University of Zurich
Exploring the effect of chirality on the therapeutic potential of N-alkyl-deoxyiminosugars: anti-inflammatory response to Pseudomonas aeruginosa infections for application in CF lung disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 63-71 (2019)
University of Napoli Federico Ii
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR) Kinase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5547-5561 (2019)
Vertex Pharmaceuticals (Europe)
On the Process of Discovering Leads That Target the Heparin-Binding Site of Neutrophil Elastase in the Sputum of Cystic Fibrosis Patients.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5501-5511 (2019)
Virginia Commonwealth University
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5358-5369 (2019)
University of Regensburg
Mechanisms of Specific versus Nonspecific Interactions of Aggregation-Prone Inhibitors and Attenuators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5063-5079 (2019)
University Health Network
Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1601-1604 (2019)
Ono Pharmaceutical
5-Arylisothiazol-3(2H)-one-1,(1)-(di)oxides: A new class of selective tumor-associated carbonic anhydrases (hCA IX and XII) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 40-48 (2019)
Universit£
Recent progress on the discovery of P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 34-39 (2019)
China Pharmaceutical University
Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5863-5884 (2019)
The Institute of Cancer Research
Exploiting Structural Dynamics To Design Open-Flap Inhibitors of Malarial Aspartic Proteases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8931-8950 (2019)
Latvian Institute of Organic Synthesis
Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5562-5578 (2019)
The University of Sydney
Design and Discovery of ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 63: 2013-2027 (2020)
Novartis Institutes For Biomedical Research
Structure Guided Design, Synthesis, and Biological Evaluation of Novel Benzosuberene Analogues as Inhibitors of Tubulin Polymerization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5594-5615 (2019)
Baylor University
A multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 175: 2-19 (2019)
Jamia Millia Islamia (Central University)
1-Aryl-3-(4-methoxybenzyl)ureas as potentially irreversible glycogen synthase kinase 3 inhibitors: Synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1597-1600 (2019)
Stellenbosch University
Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1605-1608 (2019)
China Pharmaceutical University
The Trifluoromethyl Group as a Bioisosteric Replacement of the Aliphatic Nitro Group in CB![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5049-5062 (2019)
University of Aberdeen
Overview of Recent Strategic Advances in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 9375-9414 (2019)
Shandong University
Acylated sulfonamide adenosines as potent inhibitors of the adenylate-forming enzyme superfamily.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 252-264 (2019)
Ku Leuven
Design, synthesis and biological evaluation of novel antitumor spirodihydrothiopyran-oxindole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1636-1642 (2019)
Shaanxi University of Science & Technology
Dual-targeting GroEL/ES chaperonin and protein tyrosine phosphatase B (PtpB) inhibitors: A polypharmacology strategy for treating Mycobacterium tuberculosis infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1665-1672 (2019)
Indiana University School of Medicine
Discovery of ( E)- N![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5006-5024 (2019)
Chinese Academy of Sciences
Synthesis, in vitro and in vivo characterization of new benzoxazole and benzothiazole-based sigma receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 226-235 (2019)
University of Catania
Design and Synthesis of Poly(ADP-ribose) Polymerase Inhibitors: Impact of Adenosine Pocket-Binding Motif Appendage to the 3-Oxo-2,3-dihydrobenzofuran-7-carboxamide on Potency and Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5330-5357 (2019)
St. John'S University
Hybridization of ?-Adrenergic Agonists and Antagonists Confers G Protein Bias.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5111-5131 (2019)
Friedrich-Alexander University Erlangen-N£Rnberg (Fau)
Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5242-5248 (2019)
Monash University
Cytotoxic Components from Hypericum elodeoides Targeting RXR? and Inducing HeLa Cell Apoptosis through Caspase-8 Activation and PARP Cleavage.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1072-1080 (2019)
Xiamen University
Small molecule PROTACs in targeted therapy: An emerging strategy to induce protein degradation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 159-180 (2019)
Shaoxing University
Review of the molecular mechanisms of Ganoderma lucidum triterpenoids: Ganoderic acids A, C2, D, F, DM, X and Y.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 130-141 (2019)
Shaanxi University of Science & Technology
Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8682-8694 (2019)
University of Nebraska Medical Center
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3K?-PI3K? Dual Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4936-4948 (2019)
Hutchison Medipharma
Consideration of Binding Kinetics in the Design of Stapled Peptide Mimics of the Disordered Proteins Eukaryotic Translation Initiation Factor 4E-Binding Protein 1 and Eukaryotic Translation Initiation Factor 4G.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4967-4978 (2019)
University of Michigan
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1660-1664 (2019)
Emd Serono Research and Development Institute
Benzoic acid-derived nitrones: A new class of potential acetylcholinesterase inhibitors and neuroprotective agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 116-129 (2019)
University of Porto
Design, synthesis and biological evaluation of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing sulfonamido as potential PI3K? inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2261-2267 (2019)
School of Traditional Chinese Pharmacy
Identification of potent farnesoid X receptor (FXR) antagonist showing favorable PK profile and distribution toward target tissues: Comprehensive understanding of structure-activity relationship of FXR antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2220-2227 (2019)
Hiroshima International University
Discovery of 4,6-bis(benzyloxy)-3-phenylbenzofuran as a novel Pin1 inhibitor to suppress hepatocellular carcinoma via upregulating microRNA biogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2235-2244 (2019)
Sichuan University
A combinatorial approach for the discovery of drug-like inhibitors of 15-lipoxygenase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 45-55 (2019)
University of Groningen
Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4949-4966 (2019)
East China Normal University
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1435-1439 (2019)
Sabila Biosciences
Discovery of novel acylhydrazone neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 305-313 (2019)
Shanghai Institute of Technology
Discovery of Potent, Selective, and Short-Acting Peptidic V![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4991-5005 (2019)
Ferring Research Institute
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4979-4990 (2019)
Chinese Academy of Sciences
Structure-Based Design of Selective ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5080-5095 (2019)
TBA
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5132-5147 (2019)
University of Pennsylvania
Pharmacological Chaperones for the Treatment of ?-Mannosidosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5832-5843 (2019)
University of Sevilla
1,2,4-Triazole-quinoline/quinolone hybrids as potential anti-bacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 174: 1-8 (2019)
Henan University of Chinese Medicine
Synthesis and biological evaluation of new HIV-1 protease inhibitors with purine bases as P2-ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1541-1545 (2019)
Chinese Academy of Medical Science and Peking Union Medical College
Investigation of biaryl heterocycles as inhibitors of Wee1 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1481-1486 (2019)
Global Pharmaceutical Research and Development
Design, synthesis and biological evaluation of 4-aniline-thieno[2,3-d]pyrimidine derivatives as MNK1 inhibitors against renal cell carcinoma and nasopharyngeal carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2268-2279 (2019)
Chengdu Medical College
Discovery and Lead-Optimization of 4,5-Dihydropyrazoles as Mono-Kinase Selective, Orally Bioavailable and Efficacious Inhibitors of Receptor Interacting Protein 1 (RIP1) Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 5096-5110 (2019)
Glaxosmithkline
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4884-4901 (2019)
Tetra Discovery Partners
Strepantibins A-C: Hexokinase II Inhibitors from a Mud Dauber Wasp Associated Streptomyces sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 82: 1114-1119 (2019)
Shandong University At Weihai
Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform Na![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 8695-8710 (2019)
Siteone Therapeutics
3-Substituted Quinolines as ROR?t Inverse Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1463-1470 (2019)
Janssen Research and Development
Synthesis of novel andrographolide beckmann rearrangement derivatives and evaluation of their HK2-related anti-inflammatory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 282-293 (2019)
Shenyang Pharmaceutical University
Multitarget PPAR? agonists as innovative modulators of the metabolic syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 261-273 (2019)
University of Chieti "G. D.Annunzio
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 213-227 (2019)
Northwest University
Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4915-4935 (2019)
Takeda Pharmaceutical
Synthesis and evaluation of the HIF-1? inhibitory activities of novel ursolic acid tetrazole derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1440-1445 (2019)
Yanbian University College of Pharmacy
Identification and SAR exploration of a novel series of Legumain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1546-1548 (2019)
Queen'S University Belfast
Synthesis and in vitro biological evaluation of new P2X7R radioligands [![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1476-1480 (2019)
Indiana University School of Medicine
Design, synthesis of orally bioavailable novel anaplastic lymphoma kinase (ALK) inhibitor diphenylaminopyrimidine analogs and efficacy study on NCI-H2228 xenografts mice model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1514-1517 (2019)
Arromax Pharmatech
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 29: 1454-1458 (2019)
Glaxosmithkline R&D
Discovery of coumarin Mannich base derivatives as multifunctional agents against monoamine oxidase B and neuroinflammation for the treatment of Parkinson's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 203-212 (2019)
Institute of Materia Medica
Design, synthesis and biological evaluation of novel thioquinazolinone-based 2-aminobenzamide derivatives as potent histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 173: 185-202 (2019)
Beijing University of Chemical Technology
Structure-Guided Drug Design of 6-Substituted Adenosine Analogues as Potent Inhibitors of Mycobacterium tuberculosis Adenosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 62: 4483-4499 (2019)
Texas A&M University
Veratric acid derivatives containing benzylidene-hydrazine moieties as promising tyrosinase inhibitors and free radical scavengers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 27: 2644-2651 (2019)
Shiraz University of Medical Sciences
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