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Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3215-30 (2016)
East China University of Science and Technology
Synthesis, anti-inflammatory, analgesic and COX-1/2 inhibition activities of anilides based on 5,5-diphenylimidazolidine-2,4-dione scaffold: Molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 121-31 (2016)
King Saud University
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2318-23 (2016)
Astrazeneca
Synthesis of azepino[4,5-b]indol-4-ones via MCR/free radical cyclization and in vitro-in silico studies as 5-Ht?R ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2333-8 (2016)
Universidad De Guanajuato
Identification of new quinic acid derivatives as histone deacetylase inhibitors by fluorescence-based cellular assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2365-9 (2016)
Sungkyunkwan University
Piperidine derivatives as nonprostanoid IP receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2360-4 (2016)
Toray Industries
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2370-4 (2016)
The University of Tokyo
2-Phenylbenzofuran derivatives as butyrylcholinesterase inhibitors: Synthesis, biological activity and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2308-13 (2016)
University of Cagliari
Design, synthesis and structure activity relationship of potent pan-PIM kinase inhibitors derived from the pyridyl carboxamide scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2328-32 (2016)
Novartis Institutes For Biomedical Research
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 94-108 (2016)
Peking University
Identification of leads for antiproliferative activity on MDA-MB-435 human breast cancer cells through pharmacophore and CYP1A1-mediated metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 82-93 (2016)
National Institute of Pharmaceutical Education and Research (NIPER)
Applying the designed multiple ligands approach to inhibit dihydrofolate reductase and thioredoxin reductase for anti-proliferative activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 63-74 (2016)
National University of Singapore
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 53-62 (2016)
Shandong University
An integrated overview on pyrrolizines as potential anti-inflammatory, analgesic and antipyretic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 257-92 (2016)
Beni-Suef University
Thiadiazole derivatives as New Class ofß-glucuronidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1909-18 (2016)
University of Karachi
Discovery of novel N,N-3-phenyl-3-benzylaminopropionanilides as potent inhibitors of cholesteryl ester transfer protein in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1811-8 (2016)
Shenyang Pharmaceutical University
2,8-Diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine potent CCR4 antagonists capable of inducing receptor endocytosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 115: 14-25 (2016)
Glaxosmithkline Medicines Research Centre
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3264-71 (2016)
Vitae Pharmaceuticals
Design and evaluation of novel glutaminase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1819-39 (2016)
University of Pittsburgh
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1793-810 (2016)
Jagiellonian University Medical College
N-Alkylpyrido[1',2':1,5]pyrazolo-[4,3-d]pyrimidin-4-amines: A new series of negative allosteric modulators of mGlu1/5 with CNS exposure in rodents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1894-900 (2016)
Vanderbilt University Medical Center
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2105-14 (2016)
Astrazeneca
Pharmacophore elucidation of phosphoiodyn A - Potent and selective peroxisome proliferator-activated receptorß/d agonists with neuroprotective activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1889-93 (2016)
Texas Tech University Health Sciences Center
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1869-72 (2016)
Vanderbilt University Medical Center
Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1901-4 (2016)
Glaxosmithkline
A New Series of Orally Bioavailable Chemokine Receptor 9 (CCR9) Antagonists; Possible Agents for the Treatment of Inflammatory Bowel Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3098-111 (2016)
Norgine
Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide-2 (GLP-2) Analogues with Low Systemic Clearance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3129-39 (2016)
Ferring Research Institute
Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2962-72 (2016)
Universit£
Double Methotrexate-Modified Neuropeptide Y Analogues Express Increased Toxicity and Overcome Drug Resistance in Breast Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3409-17 (2016)
Universitat Leipzig
Structure-based design of N-substituted 1-hydroxy-4-sulfamoyl-2-naphthoates as selective inhibitors of the Mcl-1 oncoprotein.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 273-92 (2016)
University of Maryland
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 335-9 (2016)
Shanghai Institute of Materia Medica
Discovery of Novel 3,3-Disubstituted Piperidines as Orally Bioavailable, Potent, and Efficacious HDM2-p53 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 324-9 (2016)
Merck Research Laboratories
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 312-7 (2016)
Merck Research Laboratories
Discovery of G Protein-Biased EP2 Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 306-11 (2016)
Ono Pharmaceutical
Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 300-5 (2016)
Astrazeneca
Identification of a Small Molecule Cyclophilin D Inhibitor for Rescuing Aß-Mediated Mitochondrial Dysfunction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 294-9 (2016)
University of Kansas
Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 289-93 (2016)
Bristol-Myers Squibb Research & Development
Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 283-8 (2016)
Bristol-Myers Squibb
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 277-82 (2016)
Xenon Pharmaceuticals
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 271-6 (2016)
Bristol-Myers Squibb
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 266-70 (2016)
University of Notre Dame
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 261-5 (2016)
Merck Research Laboratories
Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 250-5 (2016)
Whitman College
Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 245-9 (2016)
Shandong University
Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 229-34 (2016)
Virginia Tech
Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 223-8 (2016)
Genentech
Potential Use of Inhibitors of Tankyrases and PARP-1 as Treatment for Cancer and Other Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 209-10 (2016)
Therachem Research Medilab (India)
Glutaminase GLS1 Inhibitors as Potential Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 207-8 (2016)
Therachem Research Medilab (India)
MALT1 Inhibitors May Potentially Treat Lymphomas and Autoimmune Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 205-6 (2016)
Therachem Research Medilab (India)
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 217-22 (2016)
Glaxosmithkline
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 211-6 (2016)
University of Bonn
Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 198-203 (2016)
Merck Research Laboratories
Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 192-7 (2016)
Roche Innovation Center Basel
New Colchicine-Derived Triazoles and Their Influence on Cytotoxicity and Microtubule Morphology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 188-91 (2016)
University of Cologne
Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 182-7 (2016)
University of Pittsburgh
Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 177-81 (2016)
Southern Research
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 162-6 (2016)
Epizyme
Characterizing the Covalent Targets of a Small Molecule Inhibitor of the Lysine Acetyltransferase P300.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 151-5 (2016)
National Cancer Institute
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 145-50 (2016)
Constellation Pharmaceuticals
Selective Inhibition of CBX6: A Methyllysine Reader Protein in the Polycomb Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 139-44 (2016)
University of Victoria
Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 134-8 (2016)
Epizyme
Aminotriazole and Aminotetrazole Inhibitors of LSD1 as Epigenetic Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 132-3 (2016)
Dart Neuroscience
Dihydropteridinone Inhibitors of BRD4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 131-131 (2016)
Dart Neuroscience
Inhibition of Histone Demethylases Offers a Novel and Promising Approach for the Treatment of Cancer and Other Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 128-30 (2016)
Therachem Research Medilab (India)
The"Gatekeeper" Residue Influences the Mode of Binding of Acetyl Indoles to Bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3087-97 (2016)
University of Z£Rich
Discovery of a 9-mer Cationic Peptide (LTX-315) as a Potential First in Class Oncolytic Peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2918-27 (2016)
Lytix Biopharma
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like ?-Helical Mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3152-62 (2016)
Dalian University of Technology
5-((3-Amidobenzyl)oxy)nicotinamides as Sirtuin 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2928-41 (2016)
University of Minnesota
Synthesis and Structure-Activity Relationships of N-Dihydrocoptisine-8-ylidene Aromatic Amines and N-Dihydrocoptisine-8-ylidene Aliphatic Amides as Antiulcerative Colitis Agents Targeting XBP1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 775-83 (2016)
Chinese Academy of Medical Sciences and Peking Union Medical College
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kd Selective Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3532-48 (2016)
Gilead Sciences
Synthesis and biological evaluation of quinoline derivatives as potential anti-prostate cancer agents and Pim-1 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1889-97 (2016)
Shenyang Pharmaceutical University
Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1910-8 (2016)
Beijing Pearl Biotech
Rational modification of the lead molecule: Enhancement in the anticancer and dihydrofolate reductase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1936-40 (2016)
Guru Nanak Dev University
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3732-49 (2016)
Amgen
Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 134-40 (2016)
Sun Yat-Sen University
Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1947-53 (2016)
Vanderbilt University School of Medicine
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1954-7 (2016)
Kbp Biosciences
Fragment-based discovery of inhibitor scaffolds targeting the metallo-ß-lactamases NDM-1 and VIM-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1973-7 (2016)
Uit The Arctic University of Norway
Synthesis, in vitro evaluation, and molecular modeling investigation of benzenesulfonimide peroxisome proliferator-activated receptorsa antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 191-200 (2016)
Universit£&Quot;G. D'Annunzio&Quot
Sulfatase inhibitors for recidivist breast cancer treatment: A chemical review.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 170-90 (2016)
Punjabi University
Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 162-9 (2016)
Qatar University
Discovery of non-peptide small molecular CXCR4 antagonists as anti-HIV agents: Recent advances and future opportunities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 65-78 (2016)
Shandong University
Chroman-4-one and chromone based somatostatinß-turn mimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 114: 59-64 (2016)
University of Gothenburg
Design and synthesis of thiourea derivatives with sulfur-containing heterocyclic scaffolds as potential tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1866-71 (2016)
East China University of Science and Technology
Comparison of the sulfonamide inhibition profiles of thea-,ß- and¿-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1941-6 (2016)
Universit£
Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1683-95 (2016)
National and Kapodistrian University of Athens
Design, synthesis of phenstatin/isocombretastatin-oxindole conjugates as antimitotic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1729-40 (2016)
Csir-Indian Institute of Chemical Technology
Recent progress on third generation covalent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1861-8 (2016)
Pfizer
Sclerotiamide: The First Non-Peptide-Based Natural Product Activator of Bacterial Caseinolytic Protease P.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 1193-7 (2016)
University of Oklahoma Cobre In Structural Biology
Identification of a Human Toll-Like Receptor (TLR) 8-Specific Agonist and a Functional Pan-TLR Inhibitor in 2-Aminoimidazoles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3311-30 (2016)
University of Kansas
Design, synthesis and docking studies of novel dipeptidyl boronic acid proteasome inhibitors constructed fromaa- andaß-amino acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1958-62 (2016)
China Pharmaceutical University
Novel Imbricatolic acid derivatives as protein tyrosine phosphatase-1B inhibitors: Design, synthesis, biological evaluation and molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1988-92 (2016)
University of Lucknow
7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2000-4 (2016)
Cardiff University
D-Amino acid oxidase inhibitors based on the 5-hydroxy-1,2,4-triazin-6(1H)-one scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2088-91 (2016)
Johns Hopkins University
Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2023-9 (2016)
Astrazeneca
Synthesis, and docking studies of phenylpyrimidine-carboxamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1749-56 (2016)
Jiangxi Science & Technology Normal University
Antiretroviral (HIV-1) activity of azulene derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1653-7 (2016)
University of Tartu
Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one: Design, synthesis, model and use as hMAO-B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1741-8 (2016)
Anhui Medical University
Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as a-glucosidase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 167-74 (2016)
Jishou University
Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3340-52 (2016)
Universit£
Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 1767-1772 (2016)
Imperial College
Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 1761-1766 (2016)
Imperial College
In vitro and in silico PTP-1B inhibition and in vivo antidiabetic activity of semisynthetic moronic acid derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2018-22 (2016)
Universidad Aut£Noma Del Estado De Morelos
Identification of PTP1B and ?-Glucosidase Inhibitory Serrulatanes from Eremophila spp. by Combined use of Dual High-Resolution PTP1B and ?-Glucosidase Inhibition Profiling and HPLC-HRMS-SPE-NMR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 1063-72 (2016)
University of Copenhagen
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3112-28 (2016)
University of Minnesota
Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2478-96 (2016)
Ontario Institute For Cancer Research
Discovery of 5-Chloro-1-(5-chloro-2-(methylsulfonyl)benzyl)-2-imino-1,2-dihydropyridine-3-carboxamide (TAK-259) as a Novel, Selective, and Orally Activea1D Adrenoceptor Antagonist with Antiurinary Frequency Effects: Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2989-3002 (2016)
Takeda Pharmaceutical
Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2410-22 (2016)
Max Planck Institute of Psychiatry
1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1619-36 (2016)
Aptuit
Isatin analogs as novel inhibitors of Candida spp.ß-carbonic anhydrase enzymes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1648-52 (2016)
Bezmialem Vakif University
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2057-64 (2016)
Novartis Institutes For Biomedical Research
Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2065-7 (2016)
Novartis Institutes For Biomedical Research
Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 146-58 (2016)
Tianjin University of Science and Technology
Small Molecule Inhibitors of Cyclophilin D To Protect Mitochondrial Function as a Potential Treatment for Acute Pancreatitis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2596-611 (2016)
University of Liverpool
The discovery of a novel antibiotic for the treatment of Clostridium difficile infections: a story of an effective academic-industrial partnership.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 1420-1426 (2016)
University College London
Identification of novel GLUT inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1732-7 (2016)
Bayer Pharma
Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1560-72 (2016)
University of Pardubice
Synthesis and biological evaluation of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine and 5,6,7,8-tetrahydroquinazoline derivatives as sigma-1 (s1) receptor antagonists for the treatment of pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2051-6 (2016)
Renmin Hospital of Wuhan University
Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-ß-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 2035-9 (2016)
Sichuan University
Inhibition of HIV-1 Reverse Transcriptase Dimerization by Small Molecules.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 17: 683-8 (2016)
University of Siena
Amyloid cascade in Alzheimer's disease: Recent advances in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 258-72 (2016)
University of Waterloo
Design, synthesis and Structure-activity relationship studies of new thiazole-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 246-57 (2016)
China Pharmaceutical University
Synthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 214-27 (2016)
University of Bordeaux
Synthesis, biological evaluation and structural analysis of novel peripherally active morphiceptin analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1582-8 (2016)
Medical University of Lodz
Synthesis of tetracyclic iminosugars fused benzo[e][1,3]thiazin-4-one and their HIV-RT inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1738-41 (2016)
Hebei University
Target ?-catenin/CD44/Nanog axis in colon cancer cells by certain N'-(2-oxoindolin-3-ylidene)-2-(benzyloxy)benzohydrazides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1664-70 (2016)
King Saud University
Synthesis and antiproliferative activity of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing the 2-oxo-4-chloro-1,2-dihydroquinoline-3-carboxamide moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1794-8 (2016)
Jiangxi Science and Technology Normal University
Discovery of Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2512-22 (2016)
The University of Michigan Medical School
Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 137-45 (2016)
Chulabhorn Research Institute
Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3018-33 (2016)
University of Bonn
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2794-809 (2016)
Amgen
Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2452-67 (2016)
Glaxosmithkline
Exploiting the Chromone Scaffold for the Development of Inhibitors of Corticosteroid Biosynthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2468-77 (2016)
University of Bologna
Structure-Based Design and Synthesis of Novel Inhibitors Targeting HDAC8 from Schistosoma mansoni for the Treatment of Schistosomiasis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2423-35 (2016)
Martin-Luther University of Halle-Wittenberg
Discovery of a New Inhibitor of Myeloid Differentiation 2 from Cinnamamide Derivatives with Anti-Inflammatory Activity in Sepsis and Acute Lung Injury.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2436-51 (2016)
Wenzhou Medical University
Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3231-48 (2016)
Merck Research Laboratories
Limonoids and Triterpenoids as 11?-HSD1 Inhibitors from Walsura robusta.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 899-906 (2016)
Chinese Academy of Sciences
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1573-81 (2016)
Mercachem
Emerging targets and new small molecule therapies in Parkinson's disease treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1419-30 (2016)
School of Medicine of University of Electronic Science and Technology of China
The Synthesis of 1,3,5-triazine Derivatives and JNJ7777120 Analogues with Histamine H4 Receptor Affinity and Their Interaction with PTEN Promoter.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 88: 254-63 (2016)
Jagiellonian University Medical College
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2841-6 (2016)
University of Southern Denmark
3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2648-59 (2016)
University of Minnesota
Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Inhibitors as a Potential Therapy for Diabetic Macular Edema.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2674-87 (2016)
Chinese Academy of Sciences
Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 367-72 (2016)
Shanghai Institute of Materia Medica
Structure-based design and development of (benz)imidazole pyridones as JAK1-selective kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1803-8 (2016)
Merck
Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase : synthesis, structure-activity relationship studies and antiviral activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 1666-1672 (2016)
Ku Leuven
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2820-40 (2016)
Bristol-Myers Squibb Research and Development
MutT Homolog 1 (MTH1): The Silencing of a Target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2343-5 (2016)
Nerviano Medical Sciences
Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1720-5 (2016)
Chungbuk National University
Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 1,2,3-triazole moiety as c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1680-4 (2016)
Jiangxi Science and Technology Normal University
Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 102-33 (2016)
RhôNe-Poulenc Rorer
Increasing the binding affinity of VEGFR-2 inhibitors by extending their hydrophobic interaction with the active site: Design, synthesis and biological evaluation of 1-substituted-4-(4-methoxybenzyl)phthalazine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 50-62 (2016)
Egyptian Russian University
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 11-27 (2016)
Universit£
4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 113: 1-10 (2016)
Gazi University
Sulfonamide inhibition studies of theß-carbonic anhydrase from the newly discovered bacterium Enterobacter sp. B13.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1821-6 (2016)
Recep Tayyip Erdogan University
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2760-79 (2016)
Pharmaron-Beijing
Humudifucol and Bioactive Prenylated Polyphenols from Hops (Humulus lupulus cv."Cascade").![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 590-7 (2016)
University of Naples Federico Ii
Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2579-95 (2016)
The University of Montana
Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1455-68 (2016)
Bristol-Myers Squibb
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1528-39 (2016)
China Pharmaceutical University
Design, synthesis, and analysis of antagonists of GPR55: Piperidine-substituted 1,3,4-oxadiazol-2-ones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1827-30 (2016)
University of North Carolina At Greensboro
A Novel Inhibitor of the Obesity-Related Protein FTO.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 55: 1516-22 (2016)
Basic Medical College of Zhengzhou University
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4462-75 (2016)
Boehringer Ingelheim Rcv
Chemical Space of DNA-Encoded Libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 6629-44 (2016)
University of Utah
Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 88: 241-53 (2016)
Shandong University
Galanthamine, Plicamine, and Secoplicamine Alkaloids from Zephyranthes candida and Their Anti-acetylcholinesterase and Anti-inflammatory Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 760-6 (2016)
Huazhong University of Science and Technology
Structure-guided design of new indoles as negative allosteric modulators (NAMs) of N-methyl-D-aspartate receptor (NMDAR) containing GluN2B subunit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1513-9 (2016)
Farmaceutiche Ed Ambientali (Chibiofaram) Universit£
Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrinaIIbß3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1839-43 (2016)
A.V. Bogatsky Physico-Chemical Institute of The National Academy of Sciences of Ukraine
Isoquinoline-1,3-diones as Selective Inhibitors of Tyrosyl DNA Phosphodiesterase II (TDP2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2734-46 (2016)
University of Minnesota
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 7029-65 (2016)
Vrije Universiteit Amsterdam
Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1446-54 (2016)
Shandong University
Three stories on Eph kinase inhibitors: From in silico discovery to in vivo validation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 347-66 (2016)
University of Z£Rich
Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 298-346 (2016)
Guru Nanak Dev University
Inhibition of human DNA topoisomerase IIa by two novel ellipticine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1809-12 (2016)
Vanderbilt University School of Medicine
Synthesis and biological evaluation of new fluorinated and chlorinated indenoisoquinoline topoisomerase I poisons.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1469-79 (2016)
Purdue University
Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1495-503 (2016)
Jiangxi Science & Technology Normal University
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1817-20 (2016)
The University of Tokyo
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1844-8 (2016)
Kyung Hee University
Plumbagin, Juglone, and Boropinal as Novel TRPA1 Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 697-703 (2016)
Universit£T Leipzig
Design and Synthesis of Benzimidazoles As Novel Corticotropin-Releasing Factor 1 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2551-66 (2016)
Takeda Pharmaceutical
Feeling Nature's PAINS: Natural Products, Natural Product Drugs, and Pan Assay Interference Compounds (PAINS).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 616-28 (2016)
Monash University (Parkville Campus)
Inhibition of Chikungunya Virus-Induced Cell Death by Salicylate-Derived Bryostatin Analogues Provides Additional Evidence for a PKC-Independent Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 680-4 (2016)
Stanford University
Design, synthesis, and structure-activity relationship study of glycyrrhetinic acid derivatives as potent and selective inhibitors against human carboxylesterase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 280-8 (2016)
Dalian Institute of Chemical Physics
Rational design in search for 5-phenylhydantoin selective 5-HT7R antagonists. Molecular modeling, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 258-69 (2016)
Jagiellonian University Medical College
New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 252-7 (2016)
University of Ljubljana
Dihydropyrazole derivatives as telomerase inhibitors: Structure-based design, synthesis, SAR and anticancer evaluation in vitro and in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 231-51 (2016)
Anhui Medical University
A potent and selective inhibitor targeting human and murine 12/15-LOX.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1183-90 (2016)
University of California
SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1529-35 (2016)
Merck Research Laboratories
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2747-59 (2016)
Universit£
Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based¿-secretase modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1554-7 (2016)
Bristol-Myers Squibb
Identification of potent and selective MTH1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1503-7 (2016)
Md Anderson Cancer Center
Design and synthesis of [(125)I]Pyricoxib: A novel (125)I-labeled cyclooxygenase-2 (COX-2) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1516-20 (2016)
University of Alberta
Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1525-8 (2016)
Lexicon Pharmaceuticals
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1331-45 (2016)
Shenyang Pharmaceutical University
Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1384-91 (2016)
Vitae Pharmaceuticals
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 209-16 (2016)
Saarland University
Design and synthesis of novel tamoxifen analogues that avoid CYP2D6 metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 171-9 (2016)
German University In Cairo
The natural diterpene tonantzitlolone A and its synthetic enantiomer inhibit cell proliferation and kinesin-5 function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 164-70 (2016)
Hannover Medical School (Mhh)
A new GLP-1 analogue with prolonged glucose-lowering activity in vivo via backbone-based modification at the N-terminus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1163-70 (2016)
Peking University
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 11: 1296-304 (2016)
Stony Brook University
Synthesis, a-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 100-9 (2016)
Universiti Teknologi Mara (Uitm), Puncak Alam Campus
Preparation and Evaluation of Radiolabeled Antibody Recruiting Small Molecules That Target Prostate-Specific Membrane Antigen for Combined Radiotherapy and Immunotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2660-73 (2016)
Mcmaster University
Discovery of New Monocarbonyl Ligustrazine-Curcumin Hybrids for Intervention of Drug-Sensitive and Drug-Resistant Lung Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1747-60 (2016)
China Pharmaceutical University
Single Residue Substitutions That Confer Voltage-Gated Sodium Ion Channel Subtype Selectivity in the NaV1.7 Inhibitory Peptide GpTx-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2704-17 (2016)
Amgen
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3249-63 (2016)
National Institute of Diabetes and Digestive and Kidney Diseases
Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 114-29 (2016)
Mendeleyev University of Chemical Technology
Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 99-105 (2016)
University of Milan
Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 81-90 (2016)
Shanghai Institute of Materia Medica
Tricyclic pyrazoles. Part 8. Synthesis, biological evaluation and modelling of tricyclic pyrazole carboxamides as potential CB2 receptor ligands with antagonist/inverse agonist properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 66-80 (2016)
Universit£
Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2612-32 (2016)
University of Siena
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2067-82 (2016)
Universit£T W£Rzburg
Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIß.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1830-9 (2016)
University of California
Identification of human telomerase inhibitors having the core of N-acyl-4,5-dihydropyrazole with anticancer effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1508-11 (2016)
Hefei University of Technology
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 6580-94 (2016)
Dalian Medical University
De Novo Design at the Edge of Chaos.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4077-86 (2016)
Swiss Federal Institute of Technology (Eth)
An NMR Biochemical Assay for Fragment-Based Drug Discovery: Evaluation of an Inhibitor Activity on Spermidine Synthase of Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2261-6 (2016)
National Institute of Advanced Industrial Science and Technology (Aist)
Application of PEG-400 as a green biodegradable polymeric medium for the catalyst-free synthesis of spiro-dihydropyridines and their use as acetyl and butyrylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1408-17 (2016)
Persian Gulf University
Functionalized imidazolium and benzimidazolium salts as paraoxonase 1 inhibitors: Synthesis, characterization and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1392-401 (2016)
In£N£
Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1241-54 (2016)
Yamagata University
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1571-5 (2016)
Beijing University of Technology
Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2346-61 (2016)
Astrazeneca
A Real-World Perspective on Molecular Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4087-102 (2016)
F. Hoffmann-La Roche
Nociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 7011-28 (2016)
Astraea Therapeutics
Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2054-66 (2016)
Vanderbilt University School of Medicine
Recent Progress on Bile Acid Receptor Modulators for Treatment of Metabolic Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 6553-79 (2016)
Eli Lilly
Linker Modification Strategies To Control the Prostate-Specific Membrane Antigen (PSMA)-Targeting and Pharmacokinetic Properties of DOTA-Conjugated PSMA Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1761-75 (2016)
German Cancer Research Center
An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
J Med Chem 59: 6595-628 (2016)
University of Bonn
Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1605-11 (2016)
Abbott Healthcare Products
Development of 3-(4-aminosulphonyl)-phenyl-2-mercapto-3H-quinazolin-4-ones as inhibitors of carbonic anhydrase isoforms involved in tumorigenesis and glaucoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1402-7 (2016)
Dais
Synthesis, biological evaluation and molecular modeling of pseudo-peptides based statine as inhibitors for human tissue kallikrein 5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 39-47 (2016)
Universidade Federal Fluminense
The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 20-32 (2016)
University of Manchester
Simple N(e)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1612-7 (2016)
Jiangsu University
Dihydropyrano [2,3-c] pyrazole: Novel in vitro inhibitors of yeast a-glucosidase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 61-72 (2016)
King Abdulaziz University
Scouting new sigma receptor ligands: Synthesis, pharmacological evaluation and molecular modeling of 1,3-dioxolane-based structures and derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 112: 1-19 (2016)
Universit£
Some Anticancer Agents Act on Human Serum Paraoxonase-1 to Reduce Its Activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 88: 188-96 (2016)
Ahi Evran University
Definitive Metabolite Identification Coupled with Automated Ligand Identification System (ALIS) Technology: A Novel Approach to Uncover Structure-Activity Relationships and Guide Drug Design in a Factor IXa Inhibitor Program.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1818-29 (2016)
Merck Research Laboratories
Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 111: 193-201 (2016)
San Raffaele Scientific Institute
A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1365-70 (2016)
Mitsubishi Tanabe Pharma
In silico to in vitro screening of hydroxypyridinones as acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1624-8 (2016)
University of British Columbia
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1298-307 (2016)
Birla Institute of Technology
Potenta-amino-ß-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure-activity relationship (SAR) studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 111: 138-59 (2016)
Italian Institute of Technology
Discovery of Novel Allosteric Eg5 Inhibitors Through Structure-Based Virtual Screening.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 88: 178-87 (2016)
Southern Research Institute
Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 11: 1245-54 (2016)
Technical University of Munich
Tweaking Subtype Selectivity and Agonist Efficacy at (S)-2-Amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propionic acid (AMPA) Receptors in a Small Series of BnTetAMPA Analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2244-54 (2016)
University of Copenhagen
Discovery and Characterization of Biased Allosteric Agonists of the Chemokine Receptor CXCR3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2222-43 (2016)
Friedrich-Alexander University
2-Sulfonamidopyridine C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1231-40 (2016)
Seoul National University
Synthesis of benzofuran derivatives as selective inhibitors of tissue-nonspecific alkaline phosphatase: effects on cell toxicity and osteoblast-induced mineralization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1457-9 (2016)
Universit£
Conopeptide-Derived ?-Opioid Agonists (Conorphins): Potent, Selective, and Metabolic Stable Dynorphin A Mimetics with Antinociceptive Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2381-95 (2016)
Xenome
Synthesis of 6-chloro-2-Aryl-1H-imidazo[4,5-b]pyridine derivatives: Antidiabetic, antioxidant, ß-glucuronidase inhibiton and their molecular docking studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 48-56 (2016)
Universiti Teknologi Mara (Uitm), Puncak Alam Campus
DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2163-78 (2016)
Glaxosmithkline
Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 326-39 (2016)
La Trobe University
Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 111: 72-83 (2016)
National Institute of Pharmaceutical Education and Research
Non-symmetrical furan-amidines as novel leads for the treatment of cancer and malaria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 111: 33-45 (2016)
University of Manchester
Anion inhibition studies of theß-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1406-10 (2016)
Universit£
Natural Products as Sources of New Drugs from 1981 to 2014.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 629-61 (2016)
Nih Special Volunteer
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1443-51 (2016)
Merck
Design, synthesis, and biological evaluation of water-soluble amino acid prodrug conjugates derived from combretastatin, dihydronaphthalene, and benzosuberene-based parent vascular disrupting agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 938-56 (2016)
Baylor University
Novel N-acyl-carbazole derivatives as 5-HT7R antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 302-10 (2016)
Yonsei University
2-Oxo-1,2-dihydropyridinyl-3-yl amide-based GPa inhibitors: Design, synthesis and structure-activity relationship study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 111: 1-14 (2016)
Griffith University
One-pot synthesis of tetrazole-1,2,5,6-tetrahydronicotinonitriles and cholinesterase inhibition: Probing the plausible reaction mechanism via computational studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 38-47 (2016)
University of Karachi
Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 65: 26-37 (2016)
Panjab University
5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 291-301 (2016)
Palack£
Sulfonamide inhibition studies of theß-carbonic anhydrase from the pathogenic bacterium Vibrio cholerae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1115-20 (2016)
Universit£
Structure-activity relationship study of 4-(thiazol-5-yl)benzoic acid derivatives as potent protein kinase CK2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1136-41 (2016)
Kyoto University
Anti-inflammatory and antioxidant properties of a novel resveratrol-salicylate hybrid analog.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1411-5 (2016)
University of Alberta
Arylboronic acids as dual-action FAAH and TRPV1 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1401-5 (2016)
Sapienza University of Rome
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1475-9 (2016)
Merck Research Laboratories
The natural flavone fukugetin as a mixed-type inhibitor for human tissue kallikreins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1485-9 (2016)
Campus
Design and optimization of tricyclic gamma-secretase modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1498-502 (2016)
Bristol-Myers Squibb Research and Development
Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2179-91 (2016)
University of Salerno
Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5563-86 (2016)
Chinese Academy of Sciences
Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 5: 1507-1514 (2014)
The University of Arizona
Bioactive Constituents of Glycyrrhiza uralensis (Licorice): Discovery of the Effective Components of a Traditional Herbal Medicine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 281-92 (2016)
Peking University
Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 259-66 (2016)
Egyptian Russian University
New quinoline derivatives as nicotinic receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 246-58 (2016)
University of Florence
Design, synthesis and biological evaluation of 3'-benzylated analogs of 3'-epi-neoponkoranol as potenta-glucosidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 224-36 (2016)
China Pharmaceutical University
Synthesis of C-5a-chain extended derivatives of 4-epi-isofagomine: Powerfulß-galactosidase inhibitors and low concentration activators of GM1-gangliosidosis-related human lysosomalß-galactosidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1438-42 (2016)
Graz University of Technology
Optimization by Molecular Fine Tuning of Dihydro-ß-agarofuran Sesquiterpenoids as Reversers of P-Glycoprotein-Mediated Multidrug Resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1880-90 (2016)
Instituto Universitario De Bio-Org£Nica&Quot;Antonio Gonz£Lez&Quot
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 88: 43-53 (2016)
Yogi Vemana University
Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1229-32 (2016)
Bristol-Myers Squibb Discovery
Sulfonamide inhibition studies of the¿-carbonic anhydrase from the Antarctic bacterium Colwellia psychrerythraea.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1253-9 (2016)
Universit£
Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 195-203 (2016)
Dalian Medical University
Synthesis, evaluation and structure-activity relationship of new 3-carboxamide coumarins as FXIIa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 181-94 (2016)
University of Namur
Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1050-62 (2016)
Institute of Physiologically Active Compounds Russian Academy of Sciences
Pyrazole antagonists of the CB1 receptor with reduced brain penetration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1063-70 (2016)
Rti International
Pyridoxine hydroxamic acids as novel HIV-integrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1233-6 (2016)
Ambrilia Biopharma
Identification and characterization of potent, selective and metabolically stable IKKß inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1120-3 (2016)
The Catholic University of Korea
Design and discovery of 4-anilinoquinazoline-acylamino derivatives as EGFR and VEGFR-2 dual TK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 371-9 (2016)
China Pharmaceutical University
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1967-83 (2016)
Uppsala University
Mimicking of Arginine by Functionalized N(¿)-Carbamoylated Arginine As a New Broadly Applicable Approach to Labeled Bioactive Peptides: High Affinity Angiotensin, Neuropeptide Y, Neuropeptide FF, and Neurotensin Receptor Ligands As Examples.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1925-45 (2016)
University of Regensburg
Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2118-25 (2016)
The University of Queensland
Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1176-83 (2016)
University of Toronto
N-Acyl Dehydrotyrosines, Tyrosinase Inhibitors from the Marine Bacterium Thalassotalea sp. PP2-459.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 447-50 (2016)
University of Rhode Island
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1023-31 (2016)
Nas of Ukraine
Symmetric 4,4'-(piperidin-4-ylidenemethylene)bisphenol derivatives as novel tunable estrogen receptor (ER) modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1089-94 (2016)
Tohoku Pharmaceutical University
Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1124-9 (2016)
Karos Pharmaceuticals
4H-Thieno[3,2-c]chromene based inhibitors of Notum Pectinacetylesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1184-7 (2016)
Lexicon Pharmaceuticals
Inhibition of monoamine oxidase by benzoxathiolone analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1200-4 (2016)
North-West University
The Halicylindramides, Farnesoid X Receptor Antagonizing Depsipeptides from a Petrosia sp. Marine Sponge Collected in Korea.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 499-506 (2016)
Daegu-Gyeongbuk Medical Innovation Foundation
Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1232-8 (2016)
University of Gothenburg
Synthesis, in vitro and in vivo pharmacological evaluation of serotoninergic ligands containing an isonicotinic nucleus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 133-50 (2016)
Dipartimento Di Farmacia Universit£
Synthesis and evaluation of colletoic acid core derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 126-32 (2016)
St. Jude Children'S Research Hospital
Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 360-70 (2016)
Universit£
Potent Small Agonists of Protease Activated Receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 105-10 (2016)
The University of Queensland
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 100-4 (2016)
Genentech
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 94-9 (2016)
Astrazeneca
Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 83-8 (2016)
Glaxosmithkline
Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 72-6 (2016)
Novartis Institutes For Biomedical Research
Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 56-61 (2016)
Birla Institute of Technology
Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 51-5 (2016)
Zydus Research Centre
Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 40-5 (2016)
Bristol-Myers Squibb Research and Development
Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 34-9 (2016)
Biofocus
SAR Exploration Guided by LE and Fsp(3): Discovery of a Selective and Orally Efficacious ROR¿ Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 23-7 (2016)
Central Pharmaceutical Research Institute
Sulfonamide Derivatives and Pharmaceutical Applications Thereof.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 12-4 (2016)
Temple University
Cyclopropanamine Compounds and Use Thereof.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 7: 10-1 (2016)
Temple University
Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 957-66 (2016)
Second Military Medical University
Discovery of novel phenoxazinone derivatives as DKK1/LRP6 interaction inhibitors: Synthesis, biological evaluation and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1014-22 (2016)
Aristotle University of Thessaloniki
Insight to the binding mode of triazole RGD-peptidomimetics to integrin-rich cancer cells by NMR and molecular modeling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 989-94 (2016)
University of Milano
ß-Hydroxyacyl-acyl Carrier Protein Dehydratase (FabZ) from Francisella tularensis and Yersinia pestis: Structure Determination, Enzymatic Characterization, and Cross-Inhibition Studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 55: 1091-9 (2016)
Brookhaven National Laboratory
Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1330-9 (2016)
Constellation Pharmaceuticals
Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 350-9 (2016)
Shenyang Pharmaceutical University
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 914-24 (2016)
University of Copenhagen
Oxaspirol B with p97 Inhibitory Activity and Other Oxaspirols from Lecythophora sp. FL1375 and FL1031, Endolichenic Fungi Inhabiting Parmotrema tinctorum and Cladonia evansii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 340-52 (2016)
University of Arizona
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2328-42 (2016)
Amgen
Kinetic and X-ray crystallographic investigations on carbonic anhydrase isoforms I, II, IX and XII of a thioureido analog of SLC-0111.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 976-81 (2016)
University of Florida College of Medicine
Design, synthesis, and docking studies of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety as c-Met inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 812-9 (2016)
Jiangxi Science & Technology Normal University
Fluorinated matrix metalloproteinases inhibitors--Phosphonate based potential probes for positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 902-9 (2016)
Westf£Lische Wilhelms-Universit£T
A novel library of saccharin and acesulfame derivatives as potent and selective inhibitors of carbonic anhydrase IX and XII isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 1095-105 (2016)
University of Chieti-Pescara
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1260-4 (2016)
Merck Research Laboratories
Structural determinants of subtype selectivity and functional activity of angiotensin II receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1355-9 (2016)
Uppsala University
Identification of new SUMO activating enzyme 1 inhibitors using virtual screening and scaffold hopping.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1218-23 (2016)
Riken
Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1282-6 (2016)
Dongguk University-Seoul
Discovery of highly selective CRAF inhibitors, 3-carboxamido-2H-indazole-6-arylamide: In silico FBLD design, synthesis and evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1188-92 (2016)
Hanyang University
A Dual Non-ATP Analogue Inhibitor of Aurora Kinases A and B, Derived from Resorcinol with a Mixed Mode of Inhibition.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 958-67 (2016)
Jawaharlal Nehru Centre For Advanced Scientific Research
Discovery of Dual Inhibitors for Wild Type and D816V Mutant of c-KIT Kinase through Virtual and Biochemical Screening of Natural Products.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 293-9 (2016)
Sejong University
Pyrrole: An emerging scaffold for construction of valuable therapeutic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 110: 13-31 (2016)
Padmashri Vikhe Patil College
Kinetically Selective Inhibitors of Human Carbonic Anhydrase Isozymes I, II, VII, IX, XII, and XIII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2083-93 (2016)
Uppsala University
Novel Strategies for the Treatment of Pseudomonas aeruginosa Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5929-69 (2016)
Helmholtz Institute For Pharmaceutical Research Saarland (HIPS)
Synthesis of Novel Oxazolo[4,5-b]pyridine-2-one based 1,2,3-triazoles as Glycogen Synthase Kinase-3ß Inhibitors with Anti-inflammatory Potential.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 918-26 (2016)
Hamdard University (Jamia Hamdard)
Dissecting structure-activity-relationships of crebinostat: Brain penetrant HDAC inhibitors for neuroepigenetic regulation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1265-71 (2016)
Massachusetts General Hospital
Discovery of diamide compounds as diacylglycerol acyltransferase 1 (DGAT1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1245-8 (2016)
Novartis Institutes For Biomedical Research
Design and synthesis of substituted pyrido[3,2-d]-1,2,3-triazines as potential Pim-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1224-8 (2016)
Shenyang Pharmaceutical University
Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1156-60 (2016)
Takeda Pharmaceutical
Pyridazinone substituted benzenesulfonamides as potent carbonic anhydrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1337-41 (2016)
Jamia Hamdard (Hamdard University)
Synthesis of 4-sulfamoylphenyl-benzylamine derivatives with inhibitory activity against human carbonic anhydrase isoforms I, II, IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 982-8 (2016)
Harran University
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 294-304 (2016)
Shandong University
Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1727-46 (2016)
Sygnature Discovery
Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5172-208 (2016)
Purdue University
Sulfonamides incorporating heteropolycyclic scaffolds show potent inhibitory action against carbonic anhydrase isoforms I, II, IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 921-7 (2016)
Universit£
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1078-101 (2016)
The Institute of Cancer Research
Investigation ofa-conotoxin unbinding using umbrella sampling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1296-300 (2016)
Ocean University of China
Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 886-93 (2016)
Southeast University
Sulfamide derivatives with selective carbonic anhydrase VII inhibitory action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 894-901 (2016)
National University of La Plata
Design, synthesis and biological evaluation of novel analgesic agents targeting both cyclooxygenase and TRPV1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 849-57 (2016)
Henan University
Structural features underlying raloxifene's biophysical interaction with bone matrix.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 759-67 (2016)
Lilly Research Laboratories
Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1209-13 (2016)
Ono Pharmaceutical
Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1193-5 (2016)
Waseda University
A new chromanone derivative isolated from Hypericum lissophloeus (Hypericaceae) potentiates GABAA receptor currents in a subunit specific fashion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 681-5 (2016)
University of Graz
Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5970-86 (2016)
University Jena
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1149-64 (2016)
Intra-Cellular Therapies
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1984-2004 (2016)
High Magnetic Field Laboratory
Potentµ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1239-45 (2016)
Torrey Pines Institute For Molecular Studies
Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1840-53 (2016)
Instituto De Qu£Mica M£Dica
Characterization of Multisubstituted Corticotropin Releasing Factor (CRF) Peptide Antagonists (Astressins).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 854-66 (2016)
Salk Institute
Turmeric Sesquiterpenoids: Expeditious Resolution, Comparative Bioactivity, and a New Bicyclic Turmeronoid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 267-73 (2016)
Universit£
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 877-85 (2016)
Institute of Technology & Science-Pilani
Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of GyrB.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1314-8 (2016)
Cubist Pharmaceuticals
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1329-32 (2016)
Aptuit
Identification of six new lupane-type triterpenoids from Acanthopanax koreanum leaves and their tyrosinase inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1061-7 (2016)
Catholic University of Daegu
Synthesis of 2-arylfuro[3,2-b]pyridines: Effect of the C2-aryl group on melatoninergic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 268-75 (2016)
Universit£
Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 276-86 (2016)
Medical University of Lodz
Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1217-31 (2016)
Catabasis Pharmaceuticals
Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 747-50 (2016)
Linyi People'S Hospital
Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1348-54 (2016)
Merck Research Laboratories
Synthesis and biological evaluation of 3-tetrazolo steroidal analogs: Novel class of 5a-reductase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 779-88 (2016)
University Institute of Pharmaceutical Sciences
From Sphingosine Kinase to Dihydroceramide Desaturase: A Structure-Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 965-84 (2016)
Monash University (Parkville Campus)
Synthesis of novel polybrominated benzimidazole derivatives-potential CK2 inhibitors with anticancer and proapoptotic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 735-41 (2016)
Warsaw University of Technology
New MKLP-2 inhibitors in the paprotrain series: Design, synthesis and biological evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 721-34 (2016)
Cnrs
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 751-6 (2016)
Vanderbilt University Medical Center
Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 757-60 (2016)
Reset Therapeutics
2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 820-6 (2016)
Universit£
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 721-5 (2016)
Chinese Academy of Sciences
Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 734-8 (2016)
North-West University
Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 238-46 (2016)
University of Wisconsin
Design, synthesis, and biological evaluation of crenatoside analogues as novel influenza neuraminidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 199-205 (2016)
Central South University
Potent multitarget FAAH-COX inhibitors: Design and structure-activity relationship studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 216-37 (2016)
Fondazione Istituto Italiano Di Tecnologia
Highly improved antiparasitic activity after introduction of an N-benzylimidazole moiety on protein farnesyltransferase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 173-86 (2016)
Cnrs Upr2301
Design, synthesis, and biological evaluation of novel thiazolidinediones as PPAR¿/FFAR1 dual agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 157-72 (2016)
Suez Canal University
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 742-6 (2016)
Novartis Institutes For Biomedical Research
4-Aryl-3-arylsulfonyl-quinolines as negative allosteric modulators of metabotropic GluR5 receptors: From HTS hit to development candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1249-52 (2016)
Gedeon Richter
Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 778-81 (2016)
Shanghai Institute of Materia Medica
Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 124-33 (2016)
University of Regensburg
Neuroprotective profile of pyridothiazepines with blocking activity of the mitochondrial Na(+)/Ca(2+) exchanger.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 114-23 (2016)
Universidad Aut£Noma De Madrid
Synthesis and biological evaluation of fluorinated 1,5-diarylpyrrole-3-alkoxyethyl ether derivatives as selective COX-2 inhibitors endowed with anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 99-106 (2016)
University of Siena
Synthesis and tyrosinase inhibition activity of trans-stilbene derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 97-102 (2016)
Indian Institute of Integrative Medicine
The Medicinal Chemistry of Dengue Virus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5622-49 (2016)
Heidelberg University
Discovery of Highly Potent Inhibitors Targeting the Predominant Drug-Resistant S31N Mutant of the Influenza A Virus M2 Proton Channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1207-16 (2016)
The University of Arizona
Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1140-8 (2016)
Karolinska Institutet
Recent developments of 2-aminothiazoles in medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 89-98 (2016)
Sree Chaitanya College
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1370-87 (2016)
Glaxosmithkline
Dihydropyrimidine based hydrazine dihydrochloride derivatives as potent urease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 85-96 (2016)
University of Karachi
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1357-69 (2016)
Glaxosmithkline
The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1556-64 (2016)
Epizyme
Discovery of potent aryl-substituted 3-[(3-methylpyridine-2-carbonyl) amino]-2,4-dimethyl-benzoic acid EP4 antagonists with improved pharmacokinetic profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 931-5 (2016)
Eli Lilly
Peptide-based inhibitors of protein-protein interactions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 707-13 (2016)
Wroclaw University of Technology
Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 578-87 (2016)
Northern Kentucky University
Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 521-44 (2016)
Icahn School of Medicine At Mount Sinai
Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 75-88 (2016)
Sungkyunkwan University
Indole Based Weapons to Fight Antibiotic Resistance: A Structure-Activity Relationship Study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 867-91 (2016)
University of Perugia
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 947-64 (2016)
University of Warwick
Targeting the Bacterial Division Protein FtsZ.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 6975-98 (2016)
University of Wisconsin-Madison
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2005-24 (2016)
Pfizer
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous Solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1052-67 (2016)
Universit£
Identification of benzothiophene amides as potent inhibitors of human nicotinamide phosphoribosyltransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 765-8 (2016)
Second Military Medical University
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 836-40 (2016)
University College of Pharmaceutical Sciences
One-pot green synthesis of 1,3,5-triarylpentane-1,5-dione and triarylmethane derivatives as a new class of tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 795-8 (2016)
Jiangnan University
Synthesis and biological evaluation of novel 5-hydroxylaminoisoxazole derivatives as lipoxygenase inhibitors and metabolism enhancing agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 712-20 (2016)
Lomonosov Moscow State University
Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 750-8 (2016)
The First Affiliated Hospital of Xi'An Jiaotong University
Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dualaVß3 anda5ß1 integrin ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 703-11 (2016)
University of Florence
Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 686-92 (2016)
University of Minnesota
Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 554-69 (2016)
Cnrs
Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 672-80 (2016)
Henan University
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1003-20 (2016)
Glaxosmithkline
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1041-51 (2016)
Bristol-Myers Squibb Research & Development
TRPA1 channels as targets for resveratrol and related stilbenoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 899-902 (2016)
Sapienza University of Rome
Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 889-93 (2016)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Amides of non-steroidal anti-inflammatory drugs with thiomorpholine can yield hypolipidemic agents with improved anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 910-3 (2016)
Aristotelian University of Thessaloniki
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1090-1096 (2016)
Genomics Institute of The Novartis Research Foundation
2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1044-7 (2016)
Vanderbilt University Medical Center
Enantiomeric 3-deaza-1',6'-isoneplanocin and its 3-bromo analogue: Synthesis by the Ullmann reaction and their antiviral properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 928-30 (2016)
Auburn University
The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 914-20 (2016)
Gedeon Richter
Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 936-40 (2016)
Bristol-Myers Squibb Pharmaceutical Research and Development
Arylpiperidines as a new class of oxidosqualene cyclase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 13-22 (2016)
Ludwig-Maximilians University
Development of Autotaxin Inhibitors: An Overview of the Patent and Primary Literature.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5604-21 (2016)
University of Strathclyde
Mechanism of the Flavoprotein l-Hydroxynicotine Oxidase: Kinetic Mechanism, Substrate Specificity, Reaction Product, and Roles of Active-Site Residues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 55: 697-703 (2016)
University of Texas At San Antonio
Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 892-913 (2016)
University of Michigan
The Rational Design of Selective Benzoxazepin Inhibitors of thea-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 985-1002 (2016)
Genentech
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 730-40 (2016)
The University of Sydney
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 701-19 (2016)
University of Tours
Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 109: 1-12 (2016)
China Pharmaceutical University
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1388-409 (2016)
The Institute of Cancer Research
Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2497-511 (2016)
Astrazeneca
4-Arylbenzenesulfonamides as Human Carbonic Anhydrase Inhibitors (hCAIs): Synthesis by Pd Nanocatalyst-Mediated Suzuki-Miyaura Reaction, Enzyme Inhibition, and X-ray Crystallographic Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 721-32 (2016)
Universit£
Illuminating the binding interactions of galactonoamidines during the inhibition ofß-galactosidase (E. coli).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 661-71 (2016)
University of Arkansas
Receptor binding profiles and quantitative structure-affinity relationships of some 5-substituted-N,N-diallyltryptamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 959-64 (2016)
The Alexander Shulgin Research Institute
Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 819-23 (2016)
Shanghai Hengrui Pharmaceutical
In vitro synergistic anticancer activity of the combination of T-type calcium channel blocker and chemotherapeutic agent in A549 cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1073-1079 (2016)
Kyung Hee University
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1116-39 (2016)
Takeda Pharmaceutical
Cardanol-derived AChE inhibitors: Towards the development of dual binding derivatives for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 687-700 (2016)
University of Bras£Lia
Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1634-41 (2016)
Centre National de la Recherche Scientifique/INSERM/ULP
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1165-75 (2016)
Pfizer
Synthesis and evaluation of a radioiodinated 4,6-diaryl-3-cyano-2-pyridinone derivative as a survivin targeting SPECT probe for tumor imaging.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 999-1004 (2016)
Nagasaki University
Identification of allosteric ERK2 inhibitors through in silico biased screening and competitive binding assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 955-8 (2016)
Osaka Prefecture University
Active site-directed plasmin inhibitors: Extension on the P2 residue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 545-53 (2016)
Kobe Gakuin University
4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1518-30 (2016)
Albert-Ludwigs-University of Freiburg
Discovery of Benzo[cd]indol-2(1H)-ones as Potent and Specific BET Bromodomain Inhibitors: Structure-Based Virtual Screening, Optimization, and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1565-79 (2016)
Guangzhou Institutes of Biomedicine and Health
Amorfrutin C Induces Apoptosis and Inhibits Proliferation in Colon Cancer Cells through Targeting Mitochondria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 79: 2-12 (2016)
Max Planck Institute For Molecular Genetics
Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 655-62 (2016)
Suven Life Sciences
Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 644-54 (2016)
Sun Yat-Sen University
Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1648-53 (2016)
University of Oxford
A FRET-Based Assay for the Identification and Characterization of Cereblon Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 770-4 (2016)
Max Planck Institute For Developmental Biology
Small Molecule Inhibitors of Ca(2+)-S100B Reveal Two Protein Conformations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 592-608 (2016)
University of Maryland
Discovery of highly potent dual EP(2) and EP(3) agonists with subtype selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1016-9 (2016)
Ono Pharmaceutical
Benzylamide antagonists of protease activated receptor 2 with anti-inflammatory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 986-91 (2016)
The University of Queensland
Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 623-43 (2016)
Semmelweis University
Improving selectivity of dopamine D3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 885-8 (2016)
Bioprojet-Biotech
Inhibition of guinea pig aldehyde oxidase activity by different flavonoid compounds: An in vitro study.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 74-84 (2016)
Kermanshah University of Medical Sciences
(E)-1,3-diphenyl-1H-pyrazole derivatives containing O-benzyl oxime moiety as potential immunosuppressive agents: Design, synthesis, molecular docking and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 586-93 (2016)
Anhui Agricultural University
Structural insights into mechanisms for inhibiting amyloidß42 aggregation by non-catechol-type flavonoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 304-13 (2016)
Kyoto University
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor-H1/H4-receptor selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 292-300 (2016)
Friedrich-Alexander-Universit£T Erlangen-N£Rnberg
Development of sigma-1 (s1) receptor fluorescent ligands as versatile tools to studys1 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 577-85 (2016)
Universit£
O-alkylhydroxylamines as rationally-designed mechanism-based inhibitors of indoleamine 2,3-dioxygenase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 564-76 (2016)
Bryn Mawr College
Drug design, synthesis, in vitro and in silico evaluation of selective monoaminoxidase B inhibitors based on 3-acetyl-2-dichlorophenyl-5-aryl-2,3-dihydro-1,3,4-oxadiazole chemical scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 542-52 (2016)
Universit£
5,7-Disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazines as pharmacological tools to explore the antagonist selectivity profiles toward adenosine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 529-41 (2016)
Universit£
Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 505-28 (2016)
St. Jude Children'S Research Hospital
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 495-504 (2016)
Shenyang Pharmaceutical University
Design, synthesis and in-vitro evaluation of novel tetrahydroquinoline carbamates as HIV-1 RT inhibitor and their antifungal activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 66-73 (2016)
Birla Institute of Technology
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1241-6 (2015)
Genentech
Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1236-40 (2015)
China Pharmaceutical University
Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1225-30 (2015)
University of Pittsburgh
4(5)-Aryl-2-C-glucopyranosyl-imidazoles as New Nanomolar Glucose Analogue Inhibitors of Glycogen Phosphorylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1215-9 (2015)
University of Debrecen
Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1209-14 (2015)
Vrije Universiteit Brussel
Rapid Synthesis of Boc-2',6'-dimethyl-l-tyrosine and Derivatives and Incorporation into Opioid Peptidomimetics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1199-203 (2015)
University of Michigan
Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1195-8 (2015)
University of Iowa
Discovery of Novel and Orally Bioavailable Inhibitors of PI3 Kinase Based on Indazole Substituted Morpholino-Triazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1190-4 (2015)
Sphaera Pharma
Inhibitors of the Antiapoptotic Myeloid Cell Leukemia-1 (Mcl-1) May Provide Effective Treatment for Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1171-3 (2015)
Therachem Research Medilab (India)
Sulfonamide Compounds as Voltage Gated Sodium Channel Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1168-70 (2015)
Temple University
Design synthesis and structure-activity relationship of 5-substituted (tetrahydronaphthalen-2yl)methyl with N-phenyl-N-(piperidin-2-yl)propionamide derivatives as opioid ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 85-91 (2016)
University of Arizona
9-Benzoyl 9-deazaguanines as potent xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 226-31 (2016)
Universidade Estadual De Campinas
Discovery of novel tetrahydroisoquinoline-containing pyrimidines as ALK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 207-19 (2016)
Korea Research Institute of Chemical Technology
Diarylthiophenes as inhibitors of the pore-forming protein perforin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 355-60 (2016)
University of Auckland
Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 310-4 (2016)
Korea University
A dimeric urea of the bisabolene sesquiterpene from the Okinawan marine sponge Axinyssa sp. inhibits protein tyrosine phosphatase 1B activity in Huh-7 human hepatoma cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 315-7 (2016)
Tohoku Pharmaceutical University
Recent Progress in Histone Demethylase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1308-29 (2016)
University of Oxford
Discovery of Vibegron: A Potent and Selectiveß3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 609-23 (2016)
Merck Research Laboratories
Exploring the role of chloro and methyl substitutions in 2-phenylthiomethyl-benzoindole derivatives for 5-LOX enzyme inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 466-75 (2016)
Second University of Naples
Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 455-65 (2016)
Instituto De Tecnologia Em F£Rmacos
Glucose-derived spiro-isoxazolines are anti-hyperglycemic agents against type 2 diabetes through glycogen phosphorylase inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 444-54 (2016)
Universit£
Inhibitory effect of phenothiazine- and phenoxazine-derived chloroacetamides on Leishmania major growth and Trypanosoma brucei trypanothione reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 436-43 (2016)
University of Wuerzburg
Design and synthesis of novel Y-shaped barbituric acid derivatives as PPAR¿ activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 423-35 (2016)
National Institute of Pharmaceutical Education and Research (NIPER)
Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARß/d antagonists: Effects on the affinity and selectivity towards PPARß/d.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 247-60 (2016)
University of Oslo
Design, synthesis and evaluation of bitopic arylpiperazinephenyl-1,2,4-oxadiazoles as preferential dopamine D3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 191-200 (2016)
Chonnam National University
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 257-61 (2016)
Janssen Research and Development
Characterization of isobutylhydroxyamides with NGF-potentiating activity from Zanthoxylum bungeanum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 338-42 (2016)
Northwest A & F University
Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 415-22 (2016)
Egyptian Russian University
Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 392-405 (2016)
Universit£
Synthesis and pharmacological evaluation of dehydroabietic acid thiourea derivatives containing bisphosphonate moiety as an inducer of apoptosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 381-91 (2016)
Southeast University
Straightforward and effective synthesis of¿-aminobutyric acid transporter subtype 2-selective acyl-substituted azaspiro[4.5]decanes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 417-23 (2016)
Universit£
Development and structural analysis of adenosine site binding tankyrase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 328-33 (2016)
University of Oulu
7TM X-ray structures for class C GPCRs as new drug-discovery tools. 1. mGluR5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 484-94 (2016)
Shenyang Pharmaceutical University
a-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 495-8 (2016)
Genentech
Novel thiol-based histone deacetylase inhibitors bearing 3-phenyl-1H-pyrazole-5-carboxamide scaffold as surface recognition motif: Design, synthesis and SAR study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 375-9 (2016)
Shenyang Pharmaceutical University
8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 160-78 (2016)
New York University Abu Dhabi
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 179-90 (2016)
Xi'An Jiaotong University
Highly potent tyrosinase inhibitor, neorauflavane from Campylotropis hirtella and inhibitory mechanism with molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 153-9 (2016)
Gyeongsang National University
N-Alkylated arylsulfonamides of (aryloxy)ethyl piperidines: 5-HT(7) receptor selectivity versus multireceptor profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 130-9 (2016)
Jagiellonian University Medical College
Design, Synthesis, and Pharmacological Evaluation of Novel N-Acylhydrazone Derivatives as Potent Histone Deacetylase 6/8 Dual Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 655-70 (2016)
Universidade Federal De Alfenas
Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 578-91 (2016)
University of Illinois At Chicago
Synthesis of Triphenylethylene Bisphenols as Aromatase Inhibitors That Also Modulate Estrogen Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 157-70 (2016)
Purdue University
Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 277-82 (2016)
Shanghai Hengrui Pharmaceutical
Novel phenylalanine derived diamides as Factor XIa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 472-8 (2016)
Bristol-Myers Squibb
Novel compounds reducing IRS-1 serine phosphorylation for treatment of diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 424-8 (2016)
Semmelweis University
Fragment-based drug discovery of potent and selective MKK3/6 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1086-9 (2016)
Takeda California
Novel chromenedione derivatives displaying inhibition of protein tyrosine phosphatase 1B (PTP1B) from Flemingia philippinensis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 318-21 (2016)
Qiqihar University
Discovery of a Novel Inhibitor of Histone Lysine-Specific Demethylase 1A (KDM1A/LSD1) as Orally Active Antitumor Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1501-17 (2016)
European Institute of Oncology
Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Sci Adv 1: (2015)
University of Oxford
Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 55: 608-17 (2016)
University College London
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 733-49 (2016)
Takeda Pharmaceutical
KATching-Up on Small Molecule Modulators of Lysine Acetyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1249-70 (2016)
University of Freiburg
Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 707-20 (2016)
National Institute of Biological Sciences, Beijing
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 671-86 (2016)
Ariad Pharmaceuticals
Kinetic and Structural Insights into the Mechanism of Binding of Sulfonamides to Human Carbonic Anhydrase by Computational and Experimental Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4245-56 (2016)
Istituto Italiano Di Tecnologia
Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1531-44 (2016)
Kyoto Prefectural University of Medicine
Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1580-98 (2016)
University of Oxford
Towards new 5-HT7 antagonists among arylsulfonamide derivatives of (aryloxy)ethyl-alkyl amines: Multiobjective based design, synthesis, and antidepressant and anxiolytic properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 334-46 (2016)
Jagiellonian University Medical College
Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 322-33 (2016)
Chinese Academy of Sciences
Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1599-612 (2016)
Albert-Ludwigs-University of Freiburg
Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3ß Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 531-44 (2016)
Alma Mater Studiorum-University of Bologna
SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1184-1189 (2015)
University of Washington
The indole alkaloid meleagrin, from the olive tree endophytic fungus Penicillium chrysogenum, as a novel lead for the control of c-Met-dependent breast cancer proliferation, migration and invasion.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 113-22 (2016)
University of Louisiana At Monroe
Sulfonamide inhibition studies of thea-carbonic anhydrase from the gammaproteobacterium Thiomicrospira crunogena XCL-2, TcruCA.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 401-5 (2016)
Universit£
Novel PTP1B inhibitors identified by DNA display of fragment pairs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 1080-1085 (2016)
University of Geneva
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,3,5-triarylpyrazoline and 1,5-diarylpyrazole derivatives as selective COX-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 406-12 (2016)
Beni-Suef University
Identifying New Drug Targets for Potent Phospholipase D Inhibitors: Combining Sequence Alignment, Molecular Docking, and Enzyme Activity/Binding Assays.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 714-29 (2016)
Roxbury Community College
Chlorophenoxy aminoalkyl derivatives as histamine H(3)R ligands and antiseizure agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 53-72 (2016)
Jagiellonian University Medical College
Molecular modeling studies, synthesis and biological evaluation of dabigatran analogues as thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 73-84 (2016)
Shanghai Institute of Technology
Recent Progress in the Discovery of Next Generation Inhibitors of Aromatase from the Structure-Function Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5131-48 (2016)
State University of New York Upstate Medical University
Orally available stilbene derivatives as potent HDAC inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 274-86 (2016)
Orchid Chemicals & Pharmaceuticals
Thioxocoumarins Show an Alternative Carbonic Anhydrase Inhibition Mechanism Compared to Coumarins.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 462-73 (2016)
Universit£
Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 466-71 (2016)
Boehringer Ingelheim Pharmaceuticals
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 11: 1001-11 (2016)
German Cancer Research Center (Dkfz)
Specific Inhibitors of HIV Capsid Assembly Binding to the C-Terminal Domain of the Capsid Protein: Evaluation of 2-Arylquinazolines as Potential Antiviral Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 545-58 (2016)
Charles University
Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 687-706 (2016)
Servier Research Institute of Medicinal Chemistry
Rapid Identification of Novel Inhibitors of the Human Aquaporin-1 Water Channel.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 794-805 (2016)
Novartis Institutes of Biomedical Research Institute
Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 429-34 (2016)
Janssen Pharmaceutica
Evaluation of Natural and Synthetic 1,4-naphthoquinones as Inhibitors of Monoamine Oxidase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 737-46 (2016)
North-West University
2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 750-5 (2016)
Eli Lilly
Fluorescent sulfonamide carbonic anhydrase inhibitors incorporating 1,2,3-triazole moieties: Kinetic and X-ray crystallographic studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 104-12 (2016)
Universit£
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 5: 1879-1886 (2014)
University of Oxford
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 4: 140-144 (2013)
University of Oxford
Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 454-9 (2016)
Sanofi Research Center
Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1613-33 (2016)
Washington University
Selective Human Estrogen Receptor Partial Agonists (ShERPAs) for Tamoxifen-Resistant Breast Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 219-37 (2016)
University of Illinois At Chicago
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 42-52 (2016)
Birla Institute of Technology & Science-Pilani
Inhibition of carbonic anhydrase isoforms I, II, IV, VII and XII with carboxylates and sulfonamides incorporating phthalimide/phthalic anhydride scaffolds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 24: 20-5 (2016)
King Saud University
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 575-9 (2016)
Genentech
Design of High-Affinity Stapled Peptides To Target the Repressor Activator Protein 1 (RAP1)/Telomeric Repeat-Binding Factor 2 (TRF2) Protein-Protein Interaction in the Shelterin Complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 328-34 (2016)
University of Michigan
Synthesis, in vitro antitumor activity, dihydrofolate reductase inhibition, DNA intercalation and structure-activity relationship studies of 1,3,5-triazine analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 518-23 (2016)
Thapar University
Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 374-87 (2016)
Latvian Institute of Organic Synthesis
Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 22: 1588-96 (2015)
Pfizer
Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 694-703 (2016)
East China University of Science & Technology
Multitarget opioid ligands in pain relief: New players in an old game.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 211-28 (2016)
University of Catania
Targeting quorum sensing by designing azoline derivatives to inhibit the N-hexanoyl homoserine lactone-receptor CviR: Synthesis as well as biological and theoretical evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7565-77 (2015)
Instituto Polit£Cnico Nacional (Ipn)
Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9562-77 (2015)
Mayo Clinic
Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 448-61 (2016)
University of Copenhagen
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 313-27 (2016)
Pfizer
Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 413-6 (2016)
Queen'S University Belfast
Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (HDAC6) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1545-55 (2016)
Albert-Ludwigs-University of Freiburg
Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 194-205 (2016)
Eli Lilly
Phenyl Benzenesulfonylhydrazides Exhibit Selective Indoleamine 2,3-Dioxygenase Inhibition with Potent in Vivo Pharmacodynamic Activity and Antitumor Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 419-30 (2016)
National Health Research Institutes
Synthesis and antitumor activity evaluation of PI3K inhibitors containing 3-substituted quinazolin-4(3H)-one moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7765-76 (2015)
Xi'An Jiaotong University
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 358-73 (2016)
Korea Institute of Science & Technology (Kist)
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 335-57 (2016)
Biomarin Pharmaceutical
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3K? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 431-47 (2016)
Amgen
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 677-83 (2016)
Nanjing University
3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 253-63 (2016)
Baylor College of Medicine
Synthesis and Mechanism Studies of 1,3-Benzoazolyl Substituted Pyrrolo[2,3-b]pyrazine Derivatives as Nonintercalative Topoisomerase II Catalytic Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 238-52 (2016)
Sun Yat-Sen University
1,2,3-Triazolyl-4-oxoquinolines: A feasible beginning for promising chemical structures to inhibit oseltamivir-resistant influenza A and B viruses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7777-84 (2015)
Universidade Federal Fluminense
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as ?1A/1D-AR subselective antagonists for BPH.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7735-42 (2015)
Jinan University
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-?-D-ribose 2'-oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7694-710 (2015)
Astrazeneca
Synthesis of 4-[2-(3,4-dimethoxybenzyl)cyclopentyl]-1,2-dimethoxybenzene Derivatives and Evaluations of Their Carbonic Anhydrase Isoenzymes Inhibitory Effects.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 594-607 (2016)
Atat£Rk University
Synthesis of a new inhibitor of breast cancer resistance protein with significantly improved pharmacokinetic profiles.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 551-555 (2016)
Takeda Pharmaceuticals International
Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 282-93 (2016)
National Health Research Institutes
Azaphilones from an Acid Mine Extremophile Strain of a Pleurostomophora sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2917-23 (2015)
Memorial Sloan-Kettering Cancer Center
Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 480-5 (2016)
Texas State University
Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 264-81 (2016)
University of Belgrade
An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in ß-Cell Protection.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 11: 363-74 (2016)
Broad Institute of Harvard and Mit
Synthesis and biological activity of diisothiocyanate-derived mercapturic acids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 667-71 (2016)
Wroclaw University of Technology
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 534-9 (2016)
Genentech
Synthesis, experimental evaluation and molecular modelling of hydroxamate derivatives as zinc metalloproteinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 141-53 (2016)
Uit The Arctic University of Norway
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 117-33 (2016)
Universit£
Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 89-103 (2016)
China Pharmaceutical University
Benzimidazole derivatives as new a-glucosidase inhibitors and in silico studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 29-36 (2016)
Universiti Teknologi Mara (Uitm)
Synthesis and Characterization of 4,11-Diaminoanthra[2,3-b]furan-5,10-diones: Tumor Cell Apoptosis through tNOX-Modulated NAD(+)/NADH Ratio and SIRT1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9522-34 (2015)
Gause Institute of New Antibiotics
Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 559-77 (2016)
Duke University School of Medicine
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting theµ-Opioid Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9754-67 (2015)
University of Nottingham
Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 114-31 (2016)
China Pharmaceutical University
Synthesis and activity of novel 16-dehydropregnenolone acetate derivatives as inhibitors of type 1 5a-reductase and on cancer cell line SK-LU-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7535-42 (2015)
Universidad Nacional Aut£Noma De M£Xico
Discovery of 2-aryloxy-4-amino-quinazoline derivatives as novel protease-activated receptor 2 (PAR2) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7717-27 (2015)
Yonsei University
Phenolic group on A-ring is key for dracoflavan B as a selective noncompetitive inhibitor of ?-amylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7641-9 (2015)
National University of Singapore
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 662-6 (2016)
Bristol-Myers Squibb
Design and optimization of selective azaindole amide M1 positive allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 650-5 (2016)
Pfizer
Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9625-38 (2015)
Chinese Academy of Sciences
A Methylene Group on C-2 of 24,24-Difluoro-19-nor-1a,25-dihydroxyvitamin D3 Markedly Increases Bone Calcium Mobilization in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9731-41 (2015)
University of Wisconsin-Madison
Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 53-67 (2016)
European Institute of Oncology
Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 39-52 (2016)
Universit£
Synthesis and evaluation of gallocyanine dyes as potential agents for the treatment of Alzheimer's disease and related neurodegenerative tauopathies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 28-38 (2016)
Aristotle University of Thessaloniki
Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 108: 21-7 (2016)
Fudan University
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 132-46 (2016)
Novartis Institutes For Biomedical Research
Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 25-32 (2016)
Sanofi-Aventis R&D
Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7685-93 (2015)
Shandong University
Discovery of the imidazole-derived GPR40 agonist AM-3189.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 15-20 (2015)
Amgen
3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4221-34 (2016)
Mcgill University
Avertoxins A-D, Prenyl Asteltoxin Derivatives from Aspergillus versicolor Y10, an Endophytic Fungus of Huperzia serrata.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 3067-70 (2015)
Fujian Normal University
Design and Synthesis of a Focused Library of Diamino Triazines as Potential Mycobacterium tuberculosis DHFR Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1140-4 (2015)
Institute of Chemical Technology
Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1128-33 (2015)
Pfizer
Identification of dual PPAR?/? agonists and their effects on lipid metabolism.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7676-84 (2015)
The University of Sydney
Addressing cytotoxicity of 1,4-biphenyl amide derivatives: Discovery of new potent and selective 17?-hydroxysteroid dehydrogenase type 2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 21-4 (2016)
Saarland University
Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 33-7 (2015)
Birla Institute of Technology
Identification of azabenzimidazoles as potent JAK1 selective inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 60-7 (2015)
Astrazeneca
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7597-606 (2015)
Mcgill University
Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7650-60 (2015)
Chugai Pharmaceutical
Synthesis, Biological Activities, and X-ray Crystal Structural Analysis of 25-Hydroxy-25(or 26)-adamantyl-17-[20(22),23-diynyl]-21-norvitamin D Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9510-21 (2015)
Rikkyo University
Structure-Based Discovery of Novel Cyclophilin A Inhibitors for the Treatment of Hepatitis C Virus Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9546-61 (2015)
Chonnam National University
Optimization of allosteric MEK inhibitors. Part 2: Taming the sulfamide group balances compound distribution properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 186-93 (2015)
Bayer Healthcare
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 154-9 (2016)
University of Geneva
Enkephalin analogues with N-phenyl-N-(piperidin-2-ylmethyl)propionamide derivatives: Synthesis and biological evaluations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 222-7 (2016)
University of Arizona
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 105-9 (2016)
Eli Lilly
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 51-4 (2015)
Korea University of Science and Technology
Identification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extension.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 87-93 (2016)
Chungnam National University
Hit-to-lead optimization of phenylsulfonyl hydrazides for a potent suppressor of PGE2 production: Synthesis, biological activity, and molecular docking study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 94-9 (2015)
Kyung Hee University
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 126-32 (2016)
Merck Research Laboratories
Synthesis and evaluation of bis-thiazole derivatives as new anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 288-94 (2016)
Anadolu University
Extended structure-activity study of thienopyrimidine-based EGFR inhibitors with evaluation of drug-like properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 255-74 (2015)
Norwegian University of Science and Technology
Identification of Noncompetitive Inhibitors of Cytosolic 5'-Nucleotidase II Using a Fragment-Based Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9680-96 (2015)
Universit£
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9773-8 (2015)
Universit£
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 11: 772-81 (2016)
University of Toronto
Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 140-4 (2016)
Korea Institute of Science & Technology (Kist)
Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 100-4 (2015)
Dalhousie University
Identification of a potent inhibitor targeting human lactate dehydrogenase A and its metabolic modulation for cancer cell line.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 72-5 (2016)
Chongqing University
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 197-202 (2016)
Astrazeneca
Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11?-HSD1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7607-17 (2015)
Universitat De Barcelona
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7585-96 (2015)
Zhejiang University
N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor¿ Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 61-81 (2016)
Goethe-University Frankfurt
Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 13-20 (2016)
Government College University
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9578-90 (2015)
Stockholm University
1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 165-79 (2016)
Cairo University
Discovery of benzamides as potent human ?3 adrenergic receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 26: 55-9 (2016)
Merck And
Can Small Chemical Modifications of Natural Pan-inhibitors Modulate the Biological Selectivity? The Case of Curcumin Prenylated Derivatives Acting as HDAC or mPGES-1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2867-79 (2015)
Mashhad University of Medical Sciences
Structure-Activity Relationships of Novel Tryptamine-Based Inhibitors of Bacterial Transglycosylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9712-21 (2015)
University of Ljubljana
Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 219-32 (2016)
Yogi Vemana University
New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 204-18 (2016)
Glsynthesis
Perspectives on the Two-Pore Domain Potassium Channel TREK-1 (TWIK-Related K(+) Channel 1). A Novel Therapeutic Target?![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 5149-57 (2016)
Universit£
Synthesis and comparison of the biological activity of monocyclic phosphonate, difluorophosphonate and phosphate analogs of the natural AChE inhibitor cyclophostin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7529-34 (2015)
University of Missouri-St. Louis
A structure-activity relationship of non-peptide macrocyclic histone deacetylase inhibitors and their anti-proliferative and anti-inflammatory activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7543-64 (2015)
Georgia Institute of Technology
2,30-Bis(10H-indole) heterocycles: New p53/MDM2/MDMX antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5661-6 (2015)
University of Groningen
Comprehensive Analysis of Structure-Activity Relationships of ?-Ketoheterocycles as sn-1-Diacylglycerol Lipase ? Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9742-53 (2015)
Leiden University
1,9-seco-Bicyclic Polyprenylated Acylphloroglucinols from Hypericum uralum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 3075-9 (2015)
Chinese Academy of Sciences
Design of ?7 nicotinic acetylcholine receptor ligands using the (het)Aryl-1,2,3-triazole core: Synthesis, in vitro evaluation and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 153-64 (2016)
Universite Orleans
An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9309-33 (2015)
University of Sheffield
Development of 2-(Substituted Benzylamino)-4-Methyl-1, 3-Thiazole-5-Carboxylic Acid Derivatives as Xanthine Oxidase Inhibitors and Free Radical Scavengers.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 508-16 (2016)
Jamia Hamdard
Potent and selective N-(4-sulfamoylphenyl)thiourea-based GPR55 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 119-32 (2016)
University of Eastern Finland
Arthroamide, a Cyclic Depsipeptide with Quorum Sensing Inhibitory Activity from Arthrobacter sp.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2827-31 (2015)
Toyama Prefectural University
Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9238-57 (2015)
University of Antwerp (Ua)
Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1271-98 (2016)
Genentech
Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9273-86 (2015)
Novartis Institutes For Biomedical Research
Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9296-9308 (2015)
Dana-Farber Cancer Institute
Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9768-72 (2015)
Eli Lilly
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9287-95 (2015)
Janssen Pharmaceutica
Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9480-97 (2015)
Cleave Biosciences
Efficient stereoselective synthesis of 2-acetamido-1,2-dideoxyallonojirimycin (DAJNAc) and sp(2)-iminosugar conjugates: Novel hexosaminidase inhibitors with discrimination capabilities between the mature and precursor forms of the enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 121: 926-938 (2016)
The Barcelona Institute of Science and Technology
Identification, synthesis and pharmacological evaluation of novel anti-EV71 agents via cyclophilin A inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5682-6 (2015)
East China University of Science and Technology
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 97-108 (2015)
Institute of Radiopharmaceutical Cancer Research
Pivotal role of glycogen synthase kinase-3: A therapeutic target for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 63-81 (2015)
Central University
Novel nonsecosteroidal VDR ligands with phenyl-pyrrolyl pentane skeleton for cancer therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 48-62 (2016)
China Pharmaceutical University
Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9228-37 (2015)
University of Southern California
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9345-53 (2015)
Merck
Design, synthesis and biological screening of new 4-thiazolidinone derivatives with promising COX-2 selectivity, anti-inflammatory activity and gastric safety profile.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 64: 1-12 (2016)
Beni-Suef University
Novel Hits in the Correction of ?F508-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Protein: Synthesis, Pharmacological, and ADME Evaluation of Tetrahydropyrido[4,3-d]pyrimidines for the Potential Treatment of Cystic Fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9697-711 (2015)
Siena Biotech
Benzoxazolone Carboxamides as Potent Acid Ceramidase Inhibitors: Synthesis and Structure-Activity Relationship (SAR) Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9258-72 (2015)
Fondazione Istituto Italiano Di Tecnologia
Discovery of a marine-derived bis-indole alkaloid fascaplysin, as a new class of potent P-glycoprotein inducer and establishment of its structure-activity relationship.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 107: 1-11 (2016)
Csir-Indian Institute of Integrative Medicine
Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7359-65 (2015)
Shandong University
Microwave-assisted solid-phase synthesis of side-chain to side-chain lactam-bridge cyclic peptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5708-11 (2015)
University of Minnesota
Novel ?-Carboline/Hydroxamic Acid Hybrids Targeting Both Histone Deacetylase and DNA Display High Anticancer Activity via Regulation of the p53 Signaling Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9214-27 (2015)
China Pharmaceutical University
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3593-608 (2016)
University of Edinburgh
Development of a Highly Potent D2/D3 Agonist and a Partial Agonist from Structure-Activity Relationship Study of N(6)-(2-(4-(1H-Indol-5-yl)piperazin-1-yl)ethyl)-N(6)-propyl-4,5,6,7-tetrahydrobenzo[d]thiazole-2,6-diamine Analogues: Implication in the Treatment of Parkinson's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9179-95 (2015)
Wayne State University
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Cancer Res 75: 5106-5119 (2015)
University of Oxford
Meroterpenoids from a Tropical Dysidea sp. Sponge.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2814-21 (2015)
Seoul National University
Triazole double-headed ribonucleosides as inhibitors of eosinophil derived neurotoxin.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 152-65 (2015)
University of Thessaly
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N ? S (nN ? ?*S-X) Interaction for Conformational Constraint.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9663-79 (2015)
Amgen
Structural design, synthesis and pharmacological evaluation of 4-thiazolidinones against Trypanosoma cruzi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7478-86 (2015)
Universidade Federal De Pernambuco
Design and synthesis of an in vivo-efficacious PIM3 kinase inhibitor as a candidate anti-pancreatic cancer agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5687-93 (2015)
The University of Tokyo
2-Arylquinazolin-4(3H)-ones: A novel class of thymidine phosphorylase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 142-51 (2015)
University of Karachi
Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 180-93 (2015)
Gwangju Institute of Science and Technology (Gist)
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of novel triarylpyrazoline derivatives as selective COX-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5787-91 (2015)
Beni-Suef University
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5743-7 (2015)
Astrazeneca
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5767-71 (2015)
Merck Research Laboratories
Identification and activity of inhibitors of the essential nematode-specific metalloprotease DPY-31.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5752-5 (2015)
University of Glasgow
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5720-5 (2015)
Corcept Therapeutics
Discovery of bis-aryl urea derivatives as potent and selective Limk inhibitors: Exploring Limk1 activity and Limk1/ROCK2 selectivity through a combined computational study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7464-77 (2015)
Shanghai Institute of Technology
Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 157-66 (2015)
Kyungpook National University
Structure activity relationships of 4-hydroxy-2-pyridones: A novel class of antituberculosis agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 144-56 (2015)
Novartis Institute For Tropical Diseases
Novel orally active inhibitors of ?-1,3-glucan synthesis derived from enfumafungin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5813-8 (2015)
Merck Research Laboratories
Synthesis, biological activity evaluation and molecular docking studies of novel coumarin substituted thiazolyl-3-aryl-pyrazole-4-carbaldehydes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5797-803 (2015)
National Institute of Technology
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9382-94 (2015)
Novartis Institutes For Biomedical Research
Resveratrol-Related Polymethoxystilbene Glycosides: Synthesis, Antiproliferative Activity, and Glycosidase Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2675-83 (2015)
Universit£
Design, synthesis and antithrombotic evaluation of novel dabigatran etexilate analogs, a new series of non-peptides thrombin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7405-16 (2015)
China Pharmaceutical University
Synthesis and biological evaluation of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 120-31 (2015)
Kuwait University
Design of Specific Serine Protease Inhibitors Based on a Versatile Peptide Scaffold: Conversion of a Urokinase Inhibitor to a Plasma Kallikrein Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8868-76 (2015)
Aarhus University
Small Molecule CXCR3 Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2894-917 (2016)
Heptares Therapeutics
Carbonic anhydrase inhibitors: Design, synthesis, kinetic, docking and molecular dynamics analysis of novel glycine and phenylalanine sulfonamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7353-8 (2015)
Gebze Technical University
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5792-6 (2015)
Eisai
Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5748-51 (2015)
University Munster
Flavones Inhibit the Activity of AKR1B10, a Promising Therapeutic Target for Cancer Treatment.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2666-74 (2015)
University of Hradec Kralove
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 44-60 (2016)
Dalhousie University
Synthesis and activities of new indolopyrrolobenzodiazepine derivatives toward acute myeloid leukemia cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7313-23 (2015)
Universit£
Synthesis of novel benzohydrazone-oxadiazole hybrids asß-glucuronidase inhibitors and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7394-404 (2015)
Universiti Teknologi Mara (Uitm)
Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7340-7 (2015)
Univ. Lille
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7332-9 (2015)
Southern Medical University
Discovery of potent, selective, and orally bioavailable inhibitors of interleukin-1 receptor-associate kinase-4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5546-50 (2015)
Amgen
Inhibitory kinetics of novel 2,3-dihydro-1H-inden-1-one chalcone-like derivatives on mushroom tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5495-9 (2015)
University of Technology Sydney
A novel class of negative allosteric modulators of NMDA receptor function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5583-8 (2015)
Emory University
A selective delta opioid receptor antagonist based on a stilbene core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5532-5 (2015)
The University of Iowa
Anion and sulfonamide inhibition studies of an ?-carbonic anhydrase from the Antarctic hemoglobinless fish Chionodraco hamatus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5485-9 (2015)
Universit£
Further Optimization and Evaluation of Bioavailable, Mixed-Efficacyµ-Opioid Receptor (MOR) Agonists/d-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8952-69 (2015)
University of Michigan
Development of a potent and selective cell penetrant Legumain inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5642-5 (2015)
Queen'S University Belfast
Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5555-60 (2015)
Novartis Institutes For Biomedical Research
Potent complement C3a receptor agonists derived from oxazole amino acids: Structure-activity relationships.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5604-8 (2015)
The University of Queensland
The use of porcupine inhibitors to target Wnt-driven cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5472-6 (2015)
Experimental Therapeutics Centre
Interactions of a potent cyclic peptide inhibitor with the light chain of botulinum neurotoxin A: Insights from X-ray crystallography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7264-73 (2015)
Brookhaven National Laboratory
Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 123-31 (2015)
Hazara University
Interaction of carbonic anhydrase isozymes I, II, and IX with some pyridine and phenol hydrazinecarbothioamide derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5636-41 (2015)
Balikesir University
1,3-Disubstituted and 1,3,3-trisubstituted adamantyl-ureas with isoxazole as soluble epoxide hydrolase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5514-9 (2015)
University of California Davis
Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 50-9 (2015)
Leiden University
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 444-54 (2016)
Peking University
Spiroindole Alkaloids and Spiroditerpenoids from Aspergillus duricaulis and Their Potential Neuroprotective Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2572-9 (2015)
Korea University
Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8938-51 (2015)
University of Copenhagen
Fine tuning of agonistic/antagonistic activity for vitamin D receptor by 22-alkyl chain length of ligands: 22S-Hexyl compound unexpectedly restored agonistic activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7274-81 (2015)
Showa Pharmaceutical University
Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5576-82 (2015)
Ataturk University
Highly functionalized tetrahydropyridines are cytotoxic and selective inhibitors of human puromycin sensitive aminopeptidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 26-33 (2015)
Csir-Indian Institute of Chemical Technology
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 106: 15-25 (2015)
Universit£
G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3579-92 (2016)
Sanofi-Aventis Deutschland
Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5609-12 (2015)
Lehigh University
Pharmacological Targeting of AMP-Activated Protein Kinase and Opportunities for Computer-Aided Drug Design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2879-93 (2016)
Maastricht University
Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2849-78 (2016)
Shandong University
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9154-70 (2015)
Abbvie Bioresearch Center
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8513-28 (2015)
Pfizer
Synthesis of natural phaeosphaeride A derivatives and an in vitro evaluation of their anti-cancer potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5566-9 (2015)
Research Institute of Hygiene
Discovery ofa-mangostin as a novel competitive inhibitor against mutant isocitrate dehydrogenase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5625-31 (2015)
Dongguk University
Peptidyl prolyl isomerase Pin1-inhibitory activity of D-glutamic and D-aspartic acid derivatives bearing a cyclic aliphatic amine moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5619-24 (2015)
Nagoya City University
Synthesis of potent urease inhibitors based on disulfide scaffold and their molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7211-8 (2015)
Universiti Teknologi Mara (Uitm)
Structure-activity relationships of amide-phosphonate derivatives as inhibitors of the human soluble epoxide hydrolase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7199-210 (2015)
Ehime University
Targeting the Src Homology 2 (SH2) Domain of Signal Transducer and Activator of Transcription 6 (STAT6) with Cell-Permeable, Phosphatase-Stable Phosphopeptide Mimics Potently Inhibits Tyr641 Phosphorylation and Transcriptional Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8970-84 (2015)
Rice University
Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8373-86 (2015)
Novartis Institutes For Biomedical Research
Enzyme kinetics and inhibition of histone acetyltransferase KAT8.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 289-96 (2015)
University of Groningen
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8985-9003 (2015)
University Hospital Hradec Kralove
A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8713-22 (2015)
University of Cape Town
Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 3609-34 (2016)
Universit£
Structural Elucidation of a Small Molecule Inhibitor of Protein Disulfide Isomerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 966-971 (2015)
Columbia University
Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 274-88 (2015)
University of Pisa
Inhibition of mammalian carbonic anhydrase isoforms I-XIV with a series of phenolic acid esters.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7181-8 (2015)
Universit£
New natural product carbonic anhydrase inhibitors incorporating phenol moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7219-25 (2015)
Aristotle University of Thessaloniki
Macrocyclic prolinyl acyl guanidines as inhibitors ofß-secretase (BACE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5040-7 (2015)
Bristol-Myers Squibb
Discovery of 1,1'-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8564-72 (2015)
Sapienza University of Rome
Iminothiazoline-Sulfonamide Hybrids as Jack Bean Urease Inhibitors; Synthesis, Kinetic Mechanism and Computational Molecular Modeling.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 434-43 (2016)
Quaid-I-Azam University
Development of hydroxylated naphthylchalcones as polyphenol oxidase inhibitors: Synthesis, biochemistry and molecular docking studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 116-22 (2015)
University of Technology Sydney
Evaluation of Improved Glycogen Synthase Kinase-3a Inhibitors in Models of Acute Myeloid Leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8907-19 (2015)
Technische Universit£T Darmstadt
Identification ofß-Lapachone Analogs as Novel MALT1 Inhibitors To Treat an Aggressive Subtype of Diffuse Large B-Cell Lymphoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8491-502 (2015)
Institute of Basic Science (Ibs)
Discovery of a Novel, Potent Spirocyclic Series of¿-Secretase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8806-17 (2015)
Merck Research Laboratories
Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7138-49 (2015)
Takeda Pharmaceutical
Muscarinic acetylcholine receptor binding affinities of pethidine analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5032-5 (2015)
University of Kentucky
Probing the S2' Subsite of the Anthrax Toxin Lethal Factor Using Novel N-Alkylated Hydroxamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8723-33 (2015)
University of Minnesota
Novel 5-carboxy-8-HQ based histone demethylase JMJD2A inhibitors: introduction of an additional carboxyl group at the C-2 position of quinoline.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 145-55 (2015)
China Pharmaceutical University
Structure-Activity Relationships of the Peptide Kappa Opioid Receptor Antagonist Zyklophin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8783-95 (2015)
The University of Kansas
Identification of Non-nucleoside Human Ribonucleotide Reductase Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9498-509 (2015)
Case Western Reserve University
Synthesis and Evaluation of Novel Erlotinib-NSAID Conjugates as More Comprehensive Anticancer Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1086-90 (2015)
Guangzhou Institutes of Biomedicine and Health
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1080-5 (2015)
Cubist Pharmaceuticals
Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1075-9 (2015)
Yale University
Design, Synthesis, and Biological Evaluation of 1,2-Dihydroisoquinolines as HIV-1 Integrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1065-70 (2015)
University of Delhi
Thioxo-dihydroquinazolin-one Compounds as Novel Inhibitors of Myeloperoxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1047-52 (2015)
Emory University
5-Aryl-1-imino-1-oxo-[1,2,4]thiadiazines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1031-4 (2015)
Temple University
Hit Optimization of 5-Substituted-N-(piperidin-4-ylmethyl)-1H-indazole-3-carboxamides: Potent Glycogen Synthase Kinase-3 (GSK-3) Inhibitors with in Vivo Activity in Model of Mood Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8920-37 (2015)
Angelini
Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 2269-300 (2016)
Amakem Therapeutics
Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5299-305 (2015)
Huazhong University of Science and Technology
Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-ß type I receptor kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5228-31 (2015)
Ewha Womans University
Chemical conjugation of 2-hexadecynoic acid to C5-curcumin enhances its antibacterial activity against multi-drug resistant bacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5067-71 (2015)
Inter American University of Puerto Rico
Constituents of the seeds of Cassia tora with inhibitory activity on soluble expoxide hydrolease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5097-101 (2015)
Chungnam National University
Design, synthesis and biological activity of phenoxyacetic acid derivatives as novel free fatty acid receptor 1 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7158-64 (2015)
China Pharmaceutical University
New macrocyclic analogs of the natural histone deacetylase inhibitor FK228; design, synthesis and preliminary biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6785-93 (2015)
Ronzoni Institute For Chemical and Biochem. Research
Novel, potent, selective and cellular active ABC type PTP1B inhibitors containing (methanesulfonyl-phenyl-amino)-acetic acid methyl ester phosphotyrosine mimetic.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7079-88 (2015)
Qilu University of Technology
Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6993-9 (2015)
University of North Carolina At Greensboro
Discovery of a Novel Series of Imidazo[1,2-a]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8529-41 (2015)
Chinese Academy of Sciences
Multicomponent reaction-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 120-37 (2015)
Universitat De Barcelona
Development of new highly potent imidazo[1,2-b]pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 80-105 (2015)
Universit£
Discovery of Novel Inhibitor Scaffolds against the Metallo-ß-lactamase VIM-2 by Surface Plasmon Resonance (SPR) Based Fragment Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8671-82 (2015)
Uit The Arctic University of Norway
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5107-10 (2015)
Vanderbilt University Medical Center
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 39-56 (2015)
Chinese Academy of Sciences
Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5115-20 (2015)
Vanderbilt University Medical Center
Targeting EGFR/HER2 tyrosine kinases with a new potent series of 6-substituted 4-anilinoquinazoline hybrids: Design, synthesis, kinase assay, cell-based assay, and molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5147-54 (2015)
Korea University of Science and Technology (Ust)
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5137-41 (2015)
China Pharmaceutical University
Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5102-6 (2015)
City University of New York
Synthetic, structural mimetics of the ?-hairpin flap of HIV-1 protease inhibit enzyme function.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7095-109 (2015)
University of Maryland
Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6844-54 (2015)
Seoul National University
Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8616-37 (2015)
Sun Yat-Sen University
Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 121: 864-879 (2016)
Okayama University
Molecular hybridization yields triazole bronchodilators for the treatment of COPD.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5121-6 (2015)
Pfizer
Design and synthesis of aloe-emodin derivatives as potent anti-tyrosinase, antibacterial and anti-inflammatory agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5142-6 (2015)
Shaoyang University
Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 105: 1-38 (2015)
The M. S. University of Baroda
Antibacterial Prenylated Acylphloroglucinols from Psorothamnus fremontii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2748-53 (2015)
China Pharmaceutical University
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2884-90 (2015)
University of Leipzig
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8683-93 (2015)
University of Glasgow
Phenyl Ether- and Aniline-Containing 2-Aminoquinolines as Potent and Selective Inhibitors of Neuronal Nitric Oxide Synthase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8694-712 (2015)
Northwestern University
N(?)-Carbamoylation of the Argininamide Moiety: An Avenue to Insurmountable NPY Y1 Receptor Antagonists and a Radiolabeled Selective High-Affinity Molecular Tool ([(3)H]UR-MK299) with Extended Residence Time.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8834-49 (2015)
Cnrs/Ipbs (Institut De Pharmacologie Et Biologie Structurale)
Discovery of Novel Multifunctional Ligands with ?/? Opioid Agonist/Neurokinin-1 (NK1) Antagonist Activities for the Treatment of Pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8573-83 (2015)
University of Arizona
Computational Tools To Model Halogen Bonds in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1655-70 (2016)
Colorado State University
Influence of polar side chains modifications on the dual enkephalinase inhibitory activity and conformation of human opiorphin, a pain perception related peptide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5190-3 (2015)
Institute of Advanced Chemistry of Catalonia (Iqac-Csic)
Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5172-7 (2015)
Astrazeneca
2-Aminopyrimidines as dual adenosine A1/A2A antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 177-88 (2015)
North-West University
Synthesis of novel compounds containing morpholine and 5(4H)-oxazolone rings as potent tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7089-94 (2015)
Payame Noor University (Pnu)
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6974-92 (2015)
Baylor University
First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8743-9 (2015)
University of New South Wales
Novel Series of Dihydropyridinone P2X7 Receptor Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8413-26 (2015)
Hoffmann-La Roche
Discovery of Azaindole Ureas as a Novel Class of Bacterial Gyrase B Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8503-12 (2015)
Cubist Pharmaceuticals
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5258-64 (2015)
Genentech
Cembranoids from the Gum Resin of Boswellia carterii as Potential Antiulcerative Colitis Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2322-31 (2015)
Chinese Academy of Medical Sciences and Peking Union Medical College
Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5111-4 (2015)
Emory University
Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 22: 1347-61 (2015)
Aston University
Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8877-95 (2015)
Argenta Discovery
Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6807-14 (2015)
Tohoku Pharmaceutical University
Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6855-68 (2015)
Soochow University
Crystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7000-6 (2015)
Glaxosmithkline
Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5212-6 (2015)
China Pharmaceutical University
Exploration of labeling by near infrared dyes of the polyproline linker for bivalent-type CXCR4 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6967-73 (2015)
Tokyo Medical and Dental University
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 139-47 (2015)
First Affiliated Hospital of Xi'An Jiaotong University
Synthesis of dihydropyrimidine ?,?-diketobutanoic acid derivatives targeting HIV integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 127-38 (2015)
Univ. Orl£Ans Et Cnrs
Novel hydrazone moiety-bearing aminopyrimidines as selective inhibitors of epidermal growth factor receptor T790M mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 115-26 (2015)
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast a-glucosidase, acetylcholinesterase and butyrylcholinesterase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 64-71 (2015)
Gc University
Optimization of on-resin palladium-catalyzed Sonogashira cross-coupling reaction for peptides and its use in a structure-activity relationship study of a class B GPCR ligand.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 106-14 (2015)
Universit£
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8427-43 (2015)
Bar-Ilan University
Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7024-34 (2015)
Universit£
Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1455-70 (2016)
Sichuan University
Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8285-91 (2015)
Bioinformatics Institute (Bii)
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5186-9 (2015)
Institute For Basic Science (Ibs)
Synthesis, cholinesterase inhibition and molecular modelling studies of coumarin linked thiourea derivatives.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 58-63 (2015)
Quaid-I-Azam University
New IDH1 mutant inhibitors for treatment of acute myeloid leukemia![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Chem Biol 11: 878-86 (2015)
Albert Einstein College of Medicine
Preliminary evaluation of fluoro-pegylated benzyloxybenzenes for quantification of ?-amyloid plaques by positron emission tomography.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 86-96 (2015)
Beijing Normal University
Mutational mapping of the transmembrane binding site of the G-protein coupled receptor TGR5 and binding mode prediction of TGR5 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 104: 57-72 (2015)
Heinrich Heine University
Antihyperlipidemic morpholine derivatives with antioxidant activity: An investigation of the aromatic substitution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7015-23 (2015)
University of Athens
Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5291-4 (2015)
Merck Research Laboratory
A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5306-8 (2015)
University of Minnesota
Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of a-glucosidases.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 36-44 (2015)
Universiti Teknologi Mara
Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7053-60 (2015)
University of Messina
Click-tailed coumarins with potent and selective inhibitory action against the tumor-associated carbonic anhydrases IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6955-66 (2015)
Universit£
5-Lipoxygenase inhibitors suppress RANKL-induced osteoclast formation via NFATc1 expression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7069-78 (2015)
Sookmyung Women'S University
Evaluation of small molecule SecA inhibitors against methicillin-resistant Staphylococcus aureus.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 7061-8 (2015)
Georgia State University
Monoamine oxidase inhibitory activities of heterocyclic chalcones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5270-6 (2015)
North-West University
Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5362-6 (2015)
National Institute of Health Sciences
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8182-99 (2015)
Wuxi Apptec
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists ors1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8601-15 (2015)
Universit£
Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8584-600 (2015)
Washington University
Identification of a molecular target of kurahyne, an apoptosis-inducing lipopeptide from marine cyanobacterial assemblages.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5295-8 (2015)
Keio University
Design, synthesis, and biological evaluation of oxindole derivatives as antidepressive agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5281-5 (2015)
Manipal College of Pharmaceutical Sciences
Discovery and structure-activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5449-53 (2015)
Sichuan University
Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5357-61 (2015)
Sumitomo Dainippon Pharma
Synthesis, Biological Evaluation, and Molecular Docking of (R)-2-((8-(3-aminopiperidin-1-yl)-3-methyl-7-(3-methylbut-2-en-1-yl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl)methyl)benzonitrile as Dipeptidyl Peptidase IV Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 290-5 (2016)
West China Hospital
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7959-71 (2015)
Vanderbilt University
Protostane Triterpenoids from the Rhizome of Alisma orientale Exhibit Inhibitory Effects on Human Carboxylesterase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2372-80 (2015)
Liaoning University of Traditional Chinese Medicine
Synthesis of novel acridine bis-sulfonamides with effective inhibitory activity against the carbonic anhydrase isoforms I, II, IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6573-80 (2015)
Dumlupinar University
Inhibiting the Inflammasome: A Chemical Perspective.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1691-710 (2016)
The University of Manchester
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5265-9 (2015)
Shandong University
Structure-guided discovery of 2-aryl/pyridin-2-yl-1H-indole derivatives as potent and selective hepsin inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5309-14 (2015)
Aurigene Discovery Technologies
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8292-308 (2015)
Glenmark Research Centre
Design, synthesis and structure-activity relationship studies of novel phenoxyacetamide-based free fatty acid receptor 1 agonists for the treatment of type 2 diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6666-72 (2015)
China Pharmaceutical University
Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7796-806 (2015)
Max Planck Institute of Psychiatry
Novel 3-Substituted 7-Phenylpyrrolo[3,2-f]quinolin-9(6H)-ones as Single Entities with Multitarget Antiproliferative Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7991-8010 (2015)
University of Padova
Harnessing Enzymatic Promiscuity in Myxochelin Biosynthesis for the Production of 5-Lipoxygenase Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 16: 2445-50 (2015)
Hans Knöll Institute
Ligand binding studies, preliminary structure-activity relationship and detailed mechanistic characterization of 1-phenyl-6,6-dimethyl-1,3,5-triazine-2,4-diamine derivatives as inhibitors of Escherichia coli dihydrofolate reductase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 600-14 (2015)
Georgia Institute of Technology
Discovery of spirocyclic-diamine inhibitors of mammalian acetyl CoA-carboxylase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5352-6 (2015)
Pfizer
Conformationally restricted¿-opioid receptor agonists: Synthesis and pharmacological evaluation of diastereoisomeric and enantiomeric decahydroquinoxalines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5326-30 (2015)
Mercachem
Nitrogenated honokiol derivatives allosterically modulate GABAA receptors and act as strong partial agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6757-62 (2015)
University of Graz
Isatin-pyrazole benzenesulfonamide hybrids potently inhibit tumor-associated carbonic anhydrase isoforms IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 583-93 (2015)
Egyptian Russian University
Diethylstilbestrol-scaffold-based pregnane X receptor modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 551-62 (2015)
University of Ljubljana
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 539-50 (2015)
University of South Australia
Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8128-40 (2015)
Astrazeneca
Highly Substituted Cyclopentane-CMP Conjugates as Potent Sialyltransferase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7972-90 (2015)
Peking University
Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5393-7 (2015)
Lanzhou University
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5384-8 (2015)
Merck Research Laboratories
Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5402-8 (2015)
Merck Research Laboratories
Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8054-65 (2015)
Roche Pharma Research and Early Development (Pred)
Evaluation of 2-indolcarbohydrazones as potent a-glucosidase inhibitors, in silico studies and DFT based stereochemical predictions.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 24-35 (2015)
Universiti Teknologi Mara (Uitm)
1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 63: 13-23 (2015)
Beni-Suef University
Discovery of novel, potent and low-toxicity angiotensin II receptor type 1 (AT1) blockers: Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazoles with a chiral center.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 473-87 (2015)
Beijing Institute of Technology
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1019-24 (2015)
Hoffmann-La Roche
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1015-8 (2015)
Janssen Research and Development
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 1004-9 (2015)
University of Shizuoka
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPAR? Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 998-1003 (2015)
The Scripps Research Institute
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 987-92 (2015)
Amgen
Identification of Bidentate Salicylic Acid Inhibitors of PTP1B.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 982-6 (2015)
University of Toronto Mississauga
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 961-5 (2015)
Novartis Institutes For Biomedical Research
RORc Modulators for the Treatment of Autoimmune Diseases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 958-60 (2015)
Therachem Research Medilab (India)
Nav1.7 Inhibitors: Potential Effective Therapy for the Treatment of Chronic Pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 956-7 (2015)
Therachem Research Medilab (India)
Kynurenine Monooxygenase (KMO) Inhibitors for the Treatment of Acute Pancreatitis and Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 954-5 (2015)
Therachem Research Medilab (India)
From carbohydrates to drug-like fragments: Rational development of novela-amylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6725-32 (2015)
Freie Universit£T Berlin
Mechanism of MenE inhibition by acyl-adenylate analogues and discovery of novel antibacterial agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 6514-24 (2015)
Argonne National Laboratory
Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1? Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7659-71 (2015)
Duke University
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide Library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8257-68 (2015)
Queensland University of Technology
Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8236-56 (2015)
Glaxosmithkline
1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6641-9 (2015)
North-West University
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2687-96 (2015)
Dana-Farber Cancer Institute
Discovery and Optimization of Novel, Selective Histone Methyltransferase SET7 Inhibitors by Pharmacophore- and Docking-Based Virtual Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8166-81 (2015)
Shanghai University
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 810-40 (2016)
University of Minnesota
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6632-40 (2015)
Shandong University
Rhododendrol glycosides as stereospecific tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6650-8 (2015)
Tokyo University of Agriculture and Technology
Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4412-8 (2015)
Bristol-Myers Squibb Research and Development
Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4405-11 (2015)
Virginia Tech
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6587-93 (2015)
Wuhan Institute of Technology
Design, synthesis and pharmacological evaluation of pyrimidobenzothiazole-3-carboxylate derivatives as selective L-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6689-713 (2015)
Rashtrasant Tukadoji Maharaj Nagpur University
Discovery of novel S1P2 antagonists. Part 2: Improving the profile of a series of 1,3-bis(aryloxy)benzene derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4387-92 (2015)
Ono Pharmaceutical
Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4441-6 (2015)
Kangwon National University
Converting maslinic acid into an effective inhibitor of acylcholinesterases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 438-45 (2015)
Martin-Luther-Universit£T Halle-Wittenberg
Design of novel 3,6-diazabicyclo[3.1.1]heptane derivatives with potent and selective affinities fora4ß2 neuronal nicotinic acetylcholine receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 429-37 (2015)
University of Sassari
Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7888-94 (2015)
Merck Research Laboratories
1,4-Oxazineß-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8216-35 (2015)
Janssen Pharmaceutica
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4457-60 (2015)
University of Milan
Quaternary Indolizidine and Indolizidone Iminosugars as Potential Immunostimulating and Glycosidase Inhibitory Agents: Synthesis, Conformational Analysis, Biological Activity, and Molecular Docking Study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7820-32 (2015)
Savitribai Phule Pune University (Formerly University of Pune)
Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4437-40 (2015)
Rwth Aachen University
Phenothiazine-based CaaX competitive inhibitors of human farnesyltransferase bearing a cysteine, methionine, serine or valine moiety as a new family of antitumoral compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4447-52 (2015)
Alexandru Ioan Cuza University
Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4428-33 (2015)
National Institute of Pharmaceutical Education and Research-Ahmedabad
Soluble epoxide hydrolase inhibitory activity of anthraquinone components from Aloe.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6659-65 (2015)
Chungnam National University
Reengineered tricyclic anti-cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6528-34 (2015)
Icahn School of Medicine At Mt. Sinai
Structure-Based Inhibitor Design for Evaluation of a CYP3A4 Pharmacophore Model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4210-20 (2016)
University of California Irvine
New Synthetic Routes to Triazolo-benzodiazepine Analogues: Expanding the Scope of the Bump-and-Hole Approach for Selective Bromo and Extra-Terminal (BET) Bromodomain Inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1492-500 (2016)
University of Dundee
New coumarin-based fluorescent melatonin ligands. Design, synthesis and pharmacological characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 370-3 (2015)
Iqm-Csic
Phenylalanine and Phenylglycine Analogues as Arginine Mimetics in Dengue Protease Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7719-33 (2015)
Heidelberg University
Design, Virtual Screening, and Synthesis of Antagonists ofaIIbß3 as Antiplatelet Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7681-94 (2015)
A.V. Bogatsky Physico-Chemical Institute of The National Academy of Sciences of Ukraine
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1a-Hydroxyl Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7881-7 (2015)
Veterans Affairs Medical Center
Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6763-73 (2015)
Shenyang Pharmaceutical University
Progress in the development of fatty acid synthase inhibitors as anticancer targets.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4363-9 (2015)
University of South Alabama
Structure and Inhibition of Microbiome ß-Glucuronidases Essential to the Alleviation of Cancer Drug Toxicity.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol 22: 1238-49 (2015)
University of North Carolina At Chapel Hill
Synthesis and structure-activity relationship study of benzofuran-based chalconoids bearing benzylpyridinium moiety as potent acetylcholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 361-9 (2015)
Alzahra University
Discovery of WQ-3810: Design, synthesis, and evaluation of 7-(3-alkylaminoazetidin-1-yl)fluoro-quinolones as orally active antibacterial agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 354-60 (2015)
Wakunaga Pharmaceutical
Synthesis and evaluation of 1-hydroxy/methoxy-4-methyl-2-phenyl-1H-imidazole-5-carboxylic acid derivatives as non-purine xanthine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 343-53 (2015)
Shenyang Pharmaceutical University
3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 325-34 (2015)
Northshore University Healthsystem
¿(5)-Cholenoyl-amino acids as selective and orally available antagonists of the Eph-ephrin system.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 312-24 (2015)
Universit£
New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 302-11 (2015)
1St Affiliated Hospital of Guangxi Medical University
Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 289-301 (2015)
Suven Life Sciences
Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 269-88 (2015)
China Pharmaceutical University
Probing the structural requirements of non-electrophilic naphthalene-based Nrf2 activators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 252-68 (2015)
University of Illinois At Chicago
Synthesis, In vitro and Docking Studies of New Flavone Ethers as a-Glucosidase Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 87: 361-73 (2016)
Universiti Teknologi Mara
Inhibitor versus chaperone behaviour of d-fagomine, DAB and LAB sp(2)-iminosugar conjugates against glycosidases: A structure-activity relationship study in Gaucher fibroblasts.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 121: 880-891 (2016)
University of Seville
(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 238-51 (2015)
Jagiellonian University Medical College
Cyclic Peptides Incorporating Phosphotyrosine Mimetics as Potent and Specific Inhibitors of the Grb7 Breast Cancer Target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7707-18 (2015)
The University of Sydney
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6246-9 (2015)
Hokkaido University
Neutrophil elastase inhibitors for the treatment of (cardio)pulmonary diseases: Into clinical testing with pre-adaptive pharmacophores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4370-81 (2015)
Bayer Healthcare
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5419-23 (2015)
Daiichi Sankyo
Oxidative Reactivities of 2-Furylquinolines: Ubiquitous Scaffolds in Common High-Throughput Screening Libraries.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7419-30 (2015)
University of Minnesota
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 788-809 (2016)
Georgia Institute of Technology
Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8309-13 (2015)
Cancer Research Technology
OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4171-88 (2016)
Harvard University
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7431-48 (2015)
Glaxosmithkline
Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 210-22 (2015)
Korea University of Science and Technology (Ust)
Structure-activity relationships for lipoprotein lipase agonists that lower plasma triglycerides in vivo.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 191-209 (2015)
Ume£
Novel 2H-chromen-2-one derivatives of resveratrol: Design, synthesis, modeling and use as human monoamine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 185-90 (2015)
Hefei University of Technology
Cyclic alpha-conotoxin peptidomimetic chimeras as potent GLP-1R agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 175-84 (2015)
The University of Queensland
Novel aminotetrazole derivatives as selective STAT3 non-peptide inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 163-74 (2015)
University of Franche-Comt£
Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7833-49 (2015)
University of Kansas
Benzimidazole Derivatives as Potent JAK1-Selective Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7596-602 (2015)
Konkuk University
Discovery and SAR of novel pyrazolo[1,5-a]pyrimidines as inhibitors of CDK9.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6280-96 (2015)
The University of Melbourne
Identification of Substituted Naphthotriazolediones as Novel Tryptophan 2,3-Dioxygenase (TDO) Inhibitors through Structure-Based Virtual Screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7807-19 (2015)
National Health Research Institutes
Design, Synthesis, and Evaluation of Triazole Derivatives That Induce Nrf2 Dependent Gene Products and Inhibit the Keap1-Nrf2 Protein-Protein Interaction.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7186-94 (2015)
University College London
Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7785-95 (2015)
University of Montpellier
Phosphate Chemical Probes Designed for Location Specific Inhibition of Intracellular Carbonic Anhydrases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7580-90 (2015)
Griffith University
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 5, novel pentacyclic propellane derivatives with a 6-amide side chain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6271-9 (2015)
University of Tsukuba
Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4664-71 (2015)
Nanjing University
Ynamide Click chemistry in development of triazole VEGFR2 TK modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 105-22 (2015)
University of Strasburg
Revisiting 1,3,4-Oxadiazol-2-ones: Utilization in the Development of ABHD6 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6335-45 (2015)
University of Eastern Finland
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6250-7 (2015)
Xi'An Jiaotong University
Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6467-76 (2015)
Northshore University Healthsystem
Synthesis, antiangiogenesis evaluation and molecular docking studies of 1-aryl-3-[(thieno[3,2-b]pyridin-7-ylthio)phenyl]ureas: Discovery of a new substitution pattern for type II VEGFR-2 Tyr kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6497-509 (2015)
Universidade Do Minho
New arylalkanones from Horsfieldia macrobotrys, effective antidiabetic agents concomitantly inhibitinga-glucosidase and free radicals.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4529-33 (2015)
Chulalongkorn University
Discovery of a potent enoyl-acyl carrier protein reductase (FabI) inhibitor suitable for antistaphylococcal agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4481-6 (2015)
The Catholic University of Korea
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4557-61 (2015)
China Pharmaceutical University
Discovery of 6-phenylimidazo[2,1-b]thiazole derivatives as a new type of FLT3 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4534-8 (2015)
Sichuan University
Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6379-88 (2015)
Research Triangle Institute
Synthesis, biological evaluation and 3D-QSAR studies of imidazolidine-2,4-dione derivatives as novel protein tyrosine phosphatase 1B inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 91-104 (2015)
Tianjin Medical University
Discovery of novel VEGFR-2 inhibitors. Part 5: Exploration of diverse hinge-binding fragments via core-refining approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 80-90 (2015)
The First Affiliated Hospital of Xi'An Jiaotong University
Recent Update on Human Lactate Dehydrogenase Enzyme 5 (hLDH5) Inhibitors: A Promising Approach for Cancer Chemotherapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 487-96 (2016)
National Cancer Institute-Cro
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4728-32 (2015)
Genentech
Discovery and SAR study of 3-(tert-butyl)-4-hydroxyphenyl benzoate and benzamide derivatives as novel farnesoid X receptor (FXR) antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6427-36 (2015)
East China University of Science and Technology
Synthesis of a series of unsaturated ketone derivatives as selective and reversible monoamine oxidase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6486-96 (2015)
Korea Institute of Science and Technology
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6418-26 (2015)
Chonnam National University
Multifunctional novel Diallyl disulfide (DADS) derivatives withß-amyloid-reducing, cholinergic, antioxidant and metal chelating properties for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6389-403 (2015)
University of Delhi
Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7485-500 (2015)
Vanderbilt University Medical Center
Highly Potent and Selective MT2 Melatonin Receptor Full Agonists from Conformational Analysis of 1-Benzyl-2-acylaminomethyl-tetrahydroquinolines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7512-25 (2015)
Universit£
Phenolic Compounds from the Leaves and Twigs of Osteomeles schwerinae That Inhibit Rat Lens Aldose Reductase and Vessel Dilation in Zebrafish Larvae.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 2249-54 (2015)
Institute of Oriental Medicine
Rational Development of a Potent 15-Lipoxygenase-1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7850-62 (2015)
University of Groningen
Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importina-2 Expression, and Induce Antitumor Effects against Human Glioma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7734-48 (2015)
University of Hawaii At Hilo
Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7672-80 (2015)
Guangzhou Institute of Biomedicine and Health
Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7763-74 (2015)
University of Alabama At Birmingham
Synthesis and biological evaluation of 2-alkyl-2-methoxymethyl-salvinorin ethers as selective¿-opioid receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4689-92 (2015)
Harvard Medical School
Design and synthesis of novel bivalent ligands (MOR and DOR) by conjugation of enkephalin analogues with 4-anilidopiperidine derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4683-8 (2015)
University of Arizona
Towards the evaluation in an animal disease model: Fluorinated 17ß-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 56-68 (2015)
Saarland University
Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7572-9 (2015)
University of Cape Town
Characterization of 2,4-Diamino-6-oxo-1,6-dihydropyrimidin-5-yl Ureido Based Inhibitors of Trypanosoma brucei FolD and Testing for Antiparasitic Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7938-48 (2015)
University of Dundee
Identification of Novel D-Aspartate Oxidase Inhibitors by in Silico Screening and Their Functional and Structural Characterization in Vitro.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7328-40 (2015)
Kitasato University
Inhibition and Allosteric Regulation of Monomeric Phosphoenolpyruvate Carboxykinase by 3-Mercaptopicolinic Acid.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 5878-87 (2015)
The University of Kansas Medical Center
Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7400-8 (2015)
University of Toyama
Synthesis and anticancer effects evaluation of 1-alkyl-3-(6-(2-methoxy-3-sulfonylaminopyridin-5-yl)benzo[d]thiazol-2-yl)urea as anticancer agents with low toxicity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6477-85 (2015)
Xi'An Jiaotong University
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4109-13 (2015)
Genentech
N-Hydroxyimides and hydroxypyrimidinones as inhibitors of the DNA repair complex ERCC1-XPF.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4104-8 (2015)
Mrc Technology
Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7557-71 (2015)
Chinese Academy of Medical Sciences and Peking Union Medical College
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4642-7 (2015)
Novartis Institutes For Biomedical Research
Novel bivalent inhibitors with sub-nanomolar affinities towards human glyoxalase I.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4724-7 (2015)
Chengdu University
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4610-4 (2015)
South China Agricultural University
Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4265-9 (2015)
Bristol-Myers Squibb Pharmaceutical Research Institute
Cyclodextrin complexation highly enhances efficacy of arylsulfonylureido benzenesulfonamide carbonic anhydrase inhibitors as a topical antiglaucoma agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6223-7 (2015)
Universit£
Design and discovery of 2-(4-(1H-tetrazol-5-yl)-1H-pyrazol-1-yl)-4-(4-phenyl)thiazole derivatives as cardiotonic agents via inhibition of PDE3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6111-7 (2015)
Daqing Oil Field General Hospital
Development of a novel tricyclic class of potent and selective FIXa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 5437-43 (2015)
Merck Research Laboratories
Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4287-92 (2015)
Trinity College
Integrated kinetic studies and computational analysis on naphthyl chalcones as mushroom tyrosinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4085-91 (2015)
University of Technology Sydney
Catechols and 3-hydroxypyridones as inhibitors of the DNA repair complex ERCC1-XPF.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4097-103 (2015)
Mrc Technology
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 600-10 (2015)
Hanyang University
Investigation of new 2-aryl substituted Benzothiopyrano[4,3-d]pyrimidines as kinase inhibitors targeting vascular endothelial growth factor receptor 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 29-43 (2015)
Universit£
4-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 103: 1-16 (2015)
Birla Institute of Technology
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 504-30 (2016)
Merck Research Laboratories
6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptora and the Proton-Coupled Folate Transporter in Human Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6938-59 (2015)
Duquesne University
Design, synthesis and biological evaluation of multifunctional ligands targeting opioid and bradykinin 2 receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4148-52 (2015)
University of Arizona
Dicarabrol, a new dimeric sesquiterpene from Carpesium abrotanoides L.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4082-4 (2015)
Hunan University of Chinese Medicine
Discovery of novel nonpeptide allosteric inhibitors interrupting the interaction of CDK2/cyclin A3 by virtual screening and bioassays.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4069-73 (2015)
Dalian Medical University
Discovery, synthesis and biological evaluation of 2-(4-(N-phenethylsulfamoyl)phenoxy)acetamides (SAPAs) as novel sphingomyelin synthase 1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6173-84 (2015)
Fudan University
Imidazopyridines as a source of biological activity and their pharmacological potentials-Infrared and Raman spectroscopic evidence of their content in pharmaceuticals and plant materials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6087-99 (2015)
Wroclaw University of Economics
Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7341-8 (2015)
Zhengzhou University
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7526-48 (2015)
Eli Lilly
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8200-15 (2015)
Astrazeneca
Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 552-73 (2015)
Xinjiang Technical Institute of Physics and Chemistry
Design, synthesis and evaluation of thiohydantoin derivatives as potent topoisomerase I (Top1) inhibitors with anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 540-51 (2015)
Shiv Nadar University
Quinazolinedione SIRT6 inhibitors sensitize cancer cells to chemotherapeutics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 530-9 (2015)
University of Genoa
Synthesis and inhibitory effects of novel pyrimido-pyrrolo-quinoxalinedione analogues targeting nucleoproteins of influenza A virus H1N1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 477-86 (2015)
Genomics Research Center
Discovery of indole-based tetraarylimidazoles as potent inhibitors of urease with low antilipoxygenase activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 464-70 (2015)
University of The Punjab
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 445-63 (2015)
Qilu Pharmaceutical
6-Hydroxy-1,2,4-triazine-3,5(2H,4H)-dione Derivatives as Novel D-Amino Acid Oxidase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7258-72 (2015)
Johns Hopkins University
Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7370-80 (2015)
Novo Nordisk
Novel 11ß-HSD1 inhibitors: C-1 versus C-2 substitution and effect of the introduction of an oxygen atom in the adamantane scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4250-3 (2015)
Universitat De Barcelona
Design of HIV-1 Protease Inhibitors with Amino-bis-tetrahydrofuran Derivatives as P2-Ligands to Enhance Backbone-Binding Interactions: Synthesis, Biological Evaluation, and Protein-Ligand X-ray Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6994-7006 (2015)
Purdue University
Discovery of Potent 17ß-Hydroxywithanolides for Castration-Resistant Prostate Cancer by High-Throughput Screening of a Natural Products Library for Androgen-Induced Gene Expression Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6984-93 (2015)
University of Arizona
A novel series of indazole-/indole-based glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4143-7 (2015)
Merck Research Laboratories
Exploration of the molecular architecture of the orthosteric binding site in thea4ß2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 425-44 (2015)
University of Copenhagen
Recent developments in steroidal and nonsteroidal aromatase inhibitors for the chemoprevention of estrogen-dependent breast cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 375-86 (2015)
American University of Ras Al Khaimah
Discovery of 5-substituted tetrahydronaphthalen-2yl-methyl with N-phenyl-N-(piperidin-4-yl)propionamide derivatives as potent opioid receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6185-94 (2015)
University of Arizona
1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6195-209 (2015)
Friedrich-Alexander University
Targeting Mycobacterium tuberculosis Biotin Protein Ligase (MtBPL) with Nucleoside-Based Bisubstrate Adenylation Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7349-69 (2015)
University of Minnesota
Discovery, synthesis and biochemical profiling of purine-2,6-dione derivatives as inhibitors of the human poly(A)-selective ribonuclease Caf1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4219-24 (2015)
University of Nottingham
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4158-63 (2015)
Eli Lilly
Optimization of a small molecule probe that restores e-cadherin expression.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4260-4 (2015)
Vanderbilt University Medical Center
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4136-42 (2015)
Amgen
Recent progress on MAP kinase pathway inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4047-56 (2015)
Ontario Institute For Cancer Research
Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4164-8 (2015)
Xi'An Jiaotong University
Design, synthesis of novel tryptophan derivatives for antiplatelet aggregation activity based on tripeptide pENW (pGlu-Asn-Trp).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 363-74 (2015)
China Pharmaceutical University
Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 352-62 (2015)
Iqm-Csic
Substrate-guided optimization of the syringolins yields potent proteasome inhibitors with activity against leukemia cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6218-22 (2015)
Brown University
3-Benzamides and 3,4,5-trimethoxyphenyl amines as calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6166-72 (2015)
Ewha Womans University
Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 310-9 (2015)
Ochanomizu University
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7057-75 (2015)
Astrazeneca
Discovery of Novel 15-Lipoxygenase Activators To Shift the Human Arachidonic Acid Metabolic Network toward Inflammation Resolution.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4202-9 (2016)
University of California San Diego
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 942-7 (2015)
Merck Research Laboratories
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 936-41 (2015)
Merck Research Laboratories
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 919-24 (2015)
Glaxosmithkline
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 913-8 (2015)
Genentech
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 908-12 (2015)
Bristol-Myers Squibb Research and Development
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 902-7 (2015)
The University of Tokyo
Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 894-7 (2015)
Virginia Commonwealth University
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 888-93 (2015)
Glaxosmithkline
Virtual Screening and Biological Validation of Novel Influenza Virus PA Endonuclease Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 866-71 (2015)
Universit£
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 861-5 (2015)
Merck Research Laboratories
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 850-5 (2015)
Bristol-Myers Squibb R & D
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 845-9 (2015)
Bristol-Myers Squibb Research & Development
Suppression of Hepatocellular Carcinoma by Inhibition of Overexpressed Ornithine Aminotransferase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 840-4 (2015)
Hebrew University-Hadassah Medical Center
Fatty Acid Synthase (FASN) Inhibitors as Potential Treatment for Cancer, Obesity, and Liver Related Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 838-9 (2015)
Therachem Research Medilab (India)
Fused Morphlinopyrimidines and Methods of Use Thereof.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 836-7 (2015)
Temple University
Inhibitors of the Renal Outer Medullary Potassium Channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 831-3 (2015)
Temple University
Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6747-52 (2015)
Novartis Institutes For Biomedical Research
Medicinal Chemistry Approaches to Heart Regeneration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9451-79 (2015)
Tu Dortmund University
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 882-7 (2015)
Universit Degli Studi Di Milano
Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6784-802 (2015)
Amgen
Rational Design of Orthogonal Multipolar Interactions with Fluorine in Protein-Ligand Complexes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7465-74 (2015)
University of Michigan
Lanostane Triterpenes from the Tibetan Medicinal Mushroom Ganoderma leucocontextum and Their Inhibitory Effects on HMG-CoA Reductase anda-Glucosidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1977-89 (2015)
Chinese Academy of Sciences
Potent and Selective Inhibitors of Histone Deacetylase-3 Containing Chiral Oxazoline Capping Groups and a N-(2-Aminophenyl)-benzamide Binding Unit.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6803-18 (2015)
University College London
Prokineticin Receptor Modulators May Potentially Treat Psychiatric and Neurological Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 834-5 (2015)
Therachem Research Medilab (India)
Identification of inhibitors that target dual-specificity phosphatase 5 provide new insights into the binding requirements for the two phosphate pockets.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
BMC Biochem 16: 19 (2015)
Texas Wesleyan University
Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 898-901 (2015)
University of Michigan
Expanding the chemical space of human serine racemase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4297-303 (2015)
University of Parma
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6928-37 (2015)
National Institute of Chemistry
Inhibition of Cancer-Associated Mutant Isocitrate Dehydrogenases by 2-Thiohydantoin Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6899-908 (2015)
Baylor College of Medicine
Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6710-5 (2015)
University of Jena
Synthesis and evaluation of arylpiperazine-reverse amides as biased dopamine D3 receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5264-72 (2015)
Chonnam National University
Design, chemical synthesis and biological evaluation of 3-spiromorpholinone/3-spirocarbamate androsterone derivatives as inhibitors of 17ß-hydroxysteroid dehydrogenase type 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5433-51 (2015)
Chu De Qu£Bec-Research Center (Chul)
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6059-68 (2015)
China Pharmaceutical University
Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent ROR¿t inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5293-302 (2015)
Fudan University
Carbonic anhydrase inhibitors: Design, synthesis and structural characterization of new heteroaryl-N-carbonylbenzenesulfonamides targeting druggable human carbonic anhydrase isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 223-32 (2015)
Universit£
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 215-22 (2015)
Fudan University
Synthesis, biological evaluation, and docking studies of novel thiourea derivatives of bisindolylmethane as carbonic anhydrase II inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 62: 83-93 (2015)
Universiti Teknologi Mara (Uitm)
Discovery and structure of a new inhibitor scaffold of the autophagy initiating kinase ULK1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5483-8 (2015)
University of California
Synthesis and biological evaluation of (3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5390-401 (2015)
University of Tennessee Health Science Center
Antimalarial activity of prodrugs of N-branched acyclic nucleoside phosphonate inhibitors of 6-oxopurine phosphoribosyltransferases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5502-10 (2015)
Academy of Sciences of The Czech Republic
Computer-aided identification, synthesis, and biological evaluation of novel inhibitors for botulinum neurotoxin serotype A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5489-95 (2015)
Stony Brook University
Total Synthesis of Hispidulin and the Structural Basis for Its Inhibition of Proto-oncogene Kinase Pim-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1969-76 (2015)
Taiwan Academia Sinica
Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6844-63 (2015)
Tu Dortmund University
Recent progress in the development of small-molecule glucagon receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4057-64 (2015)
Pfizer
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4337-41 (2015)
Eli Lilly
Synthesis and Characterization of 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC) and Its Analogues as Non-nitrogenous 5-HT2B Ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1859-67 (2015)
Virginia Commonwealth University
Fragment Binding Can Be Either More Enthalpy-Driven or Entropy-Driven: Crystal Structures and Residual Hydration Patterns Suggest Why.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6960-71 (2015)
Philipps University Marburg
Discovery of Potent and Selective RSK Inhibitors as Biological Probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6766-83 (2015)
Novartis Institutes For Biomedical Research
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7021-56 (2015)
Glaxosmithkline
Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7931-7 (2015)
Kitasato University
Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5626-40 (2015)
Kyoto Pharmaceutical University
Phosphate-modified analogues of m(7)GTP and m(7)Gppppm(7)G-Synthesis and biochemical properties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5369-81 (2015)
University of Warsaw
Exploring new Probenecid-based carbonic anhydrase inhibitors: Synthesis, biological evaluation and docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5311-8 (2015)
University of Chieti-Pescara
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4320-4 (2015)
University of Minnesota
Structure-Activity Relationship Study on Isothiocyanates: Comparison of TRPA1-Activating Ability between Allyl Isothiocyanate and Specific Flavor Components of Wasabi, Horseradish, and White Mustard.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1937-41 (2015)
University of Shizuoka
N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7224-40 (2015)
Universit£
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Proc Natl Acad Sci U S A 112: 10768-73 (2015)
University of Oxford
Tight binding enantiomers of pre-clinical drug candidates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5326-33 (2015)
Victoria University of Wellington
Galantamine derivatives with indole moiety: Docking, design, synthesis and acetylcholinesterase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5382-9 (2015)
Medical University of Sofia
Structure-based de novo design and synthesis of aminothiazole-based p38 MAP kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3784-7 (2015)
Sejong University
Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3788-92 (2015)
Novartis Institutes For Biomedical Research
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7164-72 (2015)
Pfizer
Development of Selective Covalent Janus Kinase 3 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6589-606 (2015)
Harvard Medical School
Structure-Activity and Structure-Property Relationship and Exploratory in Vivo Evaluation of the Nanomolar Keap1-Nrf2 Protein-Protein Interaction Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6410-21 (2015)
China Pharmaceutical University
The N-Terminal T-T Motif of a Third-Generation HIV-1 Fusion Inhibitor Is Not Required for Binding Affinity and Antiviral Activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6378-88 (2015)
Chinese Academy of Medical Sciences & Peking Union Medical College
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 115-31 (2015)
Jazan University
Strongylophorines, new protein tyrosine phosphatase 1B inhibitors, from the marine sponge Strongylophora strongilata collected at Iriomote Island.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3900-2 (2015)
Tohoku Pharmaceutical University
Novel diazabicycloalkane delta opioid agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5527-38 (2015)
Istituto Di Farmacologia Traslazionale
Structural and computational study on inhibitory compounds for endonuclease activity of influenza virus polymerase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5466-75 (2015)
Chiba University
Synergistic activation of quorum sensing in Vibrio harveyi.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3966-9 (2015)
National Institute For Biotechnology In The Negev
Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3793-7 (2015)
Syntrix Biosystems
Synthesis and molecular modelling studies of novel sulphonamide derivatives as dengue virus 2 protease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 62: 74-82 (2015)
Birla Institute of Technology
Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 80-92 (2015)
Bezmialem Vakif University
Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3810-5 (2015)
Laboratoires Chemrf Inc/Chemrf Laboratories
Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5610-8 (2015)
Jagiellonian University Medical College
Modulation of disulfide dual ENKephalinase inhibitors (DENKIs) activity by a transient N-protection for pain alleviation by oral route.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 58-67 (2015)
Pharmaleads
Triazine as a promising scaffold for its versatile biological behavior.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 39-57 (2015)
Thapar University
Synthesis, estrogenic activity, and anti-osteoporosis effects in ovariectomized rats of resveratrol oligomer derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 102: 26-38 (2015)
Fudan University
N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6549-58 (2015)
Taipei Medical University
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3914-20 (2015)
Daiichi Sankyo Rd Novare
Indolylpiperidine derivatives as potent and selectivea1B adrenoceptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3921-3 (2015)
Toray Industries
2-Phenoxy-1,4-naphthoquinones: From a Multitarget Antitrypanosomal to a Potential Antitumor Profile.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6422-34 (2015)
Alma Mater Studiorum-University of Bologna
Kinetic and Structural Characterization of the Interaction of 6-Methylidene Penem 2 with the ß-Lactamase from Mycobacterium tuberculosis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 5657-64 (2015)
Indian Institute of Technology
Structure-Based Design, Synthesis by Click Chemistry and ![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 555-563
National Institute of Diabetes and Digestive and Kidney Diseases
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4011-5 (2015)
Renovis
Design, synthesis, and in vivo activity of novel inhibitors of delta-5 desaturase for the treatment of metabolic syndrome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3836-9 (2015)
Lexicon Pharmaceuticals
Synthesis and evaluation of novel 2,4-diaminopyrimidines bearing bicyclic aminobenzazepines for anaplastic lymphoma kinase (ALK) inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3992-8 (2015)
Korea Research Institute of Chemical Technology
Synthesis and biological evaluation of 9-N-oxamyl sialosides as Siglec-7 ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5915-21 (2015)
G3-Biotec
Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5546-65 (2015)
Daiichi Sankyo
Synthesis and structure-activity relationship of uracil nucleotide derivatives towards the identification of human P2Y6 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5764-73 (2015)
Bar-Ilan University
Synthesis, nicotinic acetylcholine receptor binding, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5693-701 (2015)
Research Triangle Institute
Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5574-9 (2015)
Virginia Commonwealth University
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5566-73 (2015)
Ocean University of China
Synthesis and carbonic anhydrase I, II, IX and XII inhibitory activity of sulfamates incorporating piperazinyl-ureido moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5619-25 (2015)
University of Cagliari
Dual inhibitors of the dengue and West Nile virus NS2B-NS3 proteases: Synthesis, biological evaluation and docking studies of novel peptide-hybrids.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5748-55 (2015)
Heidelberg University
Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3850-3 (2015)
University of Cagliari
Design, synthesis and biological characterization of selective LIMK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4005-10 (2015)
Amakem Therapeutics
Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3941-6 (2015)
Actelion Pharmaceuticals
Structure-activity relationship study of syringolin A as a potential anticancer agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4872-7 (2015)
Hokkaido University
Discovery of Tyk2 inhibitors via the virtual site-directed fragment-based drug design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3947-52 (2015)
Chungnam National University
Selective inhibition of PARP10 using a chemical genetics strategy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4770-3 (2015)
Oregon Health & Science University
Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4787-92 (2015)
Columbia University
Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3956-60 (2015)
Massachusetts General Hospital
Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 818-35 (2015)
Universidade Federal De Pernambuco
Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 780-9 (2015)
Xi'An Jiaotong University
Polyketides witha-Glucosidase Inhibitory Activity from a Mangrove Endophytic Fungus, Penicillium sp. HN29-3B1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1816-22 (2015)
Hebei University
New Frontiers in Druggability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 9063-88 (2015)
Stony Brook University
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6151-78 (2015)
Glaxosmithkline
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3924-7 (2015)
Beijing Institute of Technology
Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3970-4 (2015)
Fudan University
Benzylated and prenylated flavonoids from the root barks of Cudrania tricuspidata with pancreatic lipase inhibitory activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3455-7 (2015)
Chungbuk National University
C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3451-4 (2015)
City University of New York
Novel Oxazolidinone-Based Peroxisome Proliferator Activated Receptor Agonists: Molecular Modeling, Synthesis, and Biological Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6639-52 (2015)
Iqm-Csic
Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5930-41 (2015)
University of Texas Southwestern Medical Center
Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed asa4ß2-Nicotinic Acetylcholine Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6665-77 (2015)
Universit£
Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6653-64 (2015)
Heptares Therapeutics
Inhibitory Effects of Highly Oxygenated Lanostane Derivatives from the Fungus Ganoderma lucidum on P-Glycoprotein anda-Glucosidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1868-76 (2015)
Chinese Academy of Sciences
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6448-55 (2015)
Glaxosmithkline
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6875-98 (2015)
Nerviano Medical Sciences
A Ligand-Based Drug Design. Discovery of 4-Trifluoromethyl-7,8-pyranocoumarin as a Selective Inhibitor of Human Cytochrome P450 1A2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6481-93 (2015)
Xavier University of Louisiana
Design and synthesis of new non nucleoside inhibitors of DNMT3A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5946-53 (2015)
Unit£
Human SIRT3 tripeptidic inhibitors containing N(?)-thioacetyl-lysine.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3481-7 (2015)
Jiangsu University
Inhibitor Fingerprinting of Rhomboid Proteases by Activity-Based Protein Profiling Reveals Inhibitor Selectivity and Rhomboid Autoprocessing.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2325-33 (2015)
Technische Universität München
Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 736-45 (2015)
Institute of Biomedical Imaging (I2Bm)
Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 716-35 (2015)
Korea Research Institute of Chemical Technology
Small Molecule Inhibitors of 8-Oxoguanine DNA Glycosylase-1 (OGG1).![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2334-43 (2015)
Oregon Health & Science University
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6359-67 (2015)
University of Arizona
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6607-18 (2015)
Eli Lilly
Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6574-88 (2015)
Astex Pharmaceuticals
Imine/amide-imidazole conjugates derived from 5-amino-4-cyano-N1-substituted benzyl imidazole: Microwave-assisted synthesis and anticancer activity via selective topoisomerase-II-a inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5654-61 (2015)
Central University of Punjab
Design, synthesis and biological evaluation of saccharin-based N-hydroxybenzamides as histone deacetylases (HDACs) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5774-81 (2015)
Shandong University
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5641-53 (2015)
National Institute of Pharmaceutical Education and Research
Virtual Screening for UDP-Galactopyranose Mutase Ligands Identifies a New Class of Antimycobacterial Agents.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2209-18 (2015)
University of Wisconsin-Madison
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6507-15 (2015)
Ume£
The amylase inhibitor montbretin A reveals a new glycosidase inhibition motif.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Nat Chem Biol 11: 691-6 (2015)
University of British Columbia
Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3442-6 (2015)
Nanjing University of Chinese Medicine
Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3488-94 (2015)
Merck Research Laboratories Boston
Discovery of tripeptide-derived multifunctional ligands possessing delta/mu opioid receptor agonist and neurokinin 1 receptor antagonist activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3716-20 (2015)
University of Arizona
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5881-90 (2015)
The Walter and Eliza Hall Institute of Medical Research
A-ring substituted 17ß-arylsulfonamides of 17ß-aminoestra-1,3,5(10)-trien-3-ol as highly potent reversible inhibitors of steroid sulfatase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5681-92 (2015)
University of Waterloo
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 681-91 (2015)
Leiden University
Modification of N-(6-(2-methoxy-3-(4-fluorophenylsulfonamido)pyridin-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)acetamide as PI3Ks inhibitor by replacement of the acetamide group with alkylurea.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5662-71 (2015)
Xi'An Jiaotong University
Identification of 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide (29) as an orally available MGAT2 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5922-31 (2015)
Taisho Pharmaceutical
Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 651-67 (2015)
Universit£
Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8762-82 (2015)
Colorado College
Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3569-74 (2015)
Novartis Institutes For Biomedical Research
Novel 9-Alkyl- and 9-Alkylidene-Substituted 1a,25-Dihydroxyvitamin D3 Analogues: Synthesis and Biological Examinations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6237-47 (2015)
University of Warsaw
Synthesis, kinetic mechanism and docking studies of vanillin derivatives as inhibitors of mushroom tyrosinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5870-80 (2015)
Kongju National University
4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 627-39 (2015)
Ghent University
Small lipidated anti-obesity compounds derived from neuromedin U.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 616-26 (2015)
University of California At Los Angeles
Mapping Selective Inhibition of the Cancer-Related Carbonic Anhydrase IX Using Structure-Activity Relationships of Glucosyl-Based Sulfamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6630-8 (2015)
University of Florida
High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6195-213 (2015)
National Institute On Drug Abuse-Intramural Research Program
Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5979-88 (2015)
University of Auckland
Applications of Fluorine in Medicinal Chemistry.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8315-59 (2015)
Bristol-Myers Squibb Research and Development
Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6093-113 (2015)
Setsunan University
Design, Synthesis, and Evaluation of Polyamine Deacetylase Inhibitors, and High-Resolution Crystal Structures of Their Complexes with Acetylpolyamine Amidohydrolase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 4692-703 (2015)
University of Pennsylvania
Novel inhibitor against Malassezia globosa LIP1 (SMG1), a potential anti-dandruff target.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3464-7 (2015)
South China University of Technology
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3520-5 (2015)
Merck Research Laboratories
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3575-81 (2015)
Novartis Institutes For Biomedical Research
Design, synthesis and evaluation of semi-synthetic triazole-containing caffeic acid analogues as 5-lipoxygenase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 573-83 (2015)
University of Ferrara
Synthesis of new 4-phenylpyrimidine-2(1H)-thiones and their potency to inhibit COX-1 and COX-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 552-9 (2015)
University of Graz
A Selective, Cell-Permeable Nonphosphorylated Bicyclic Peptidyl Inhibitor against Peptidyl-Prolyl Isomerase Pin1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6306-12 (2015)
The Ohio State University
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3458-63 (2015)
Guangzhou Institutes of Biomedicine and Health
SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5808-24 (2015)
Florida Atlantic University
Discovery, synthesis and structure-activity analysis of symmetrical 2,7-disubstituted fluorenones as urea transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 1278-1284 (2015)
University of California
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 822-6 (2015)
Vertex Pharmaceuticals
Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 819-21 (2015)
Institute of Biomolecules Max Mousseron (Ibmm)
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 804-8 (2015)
National Institute of Diabetes and Digestive and Kidney Diseases
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 798-803 (2015)
Astex Pharmaceuticals
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant ROR¿t Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 787-92 (2015)
Fudan University
Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 782-6 (2015)
Indiana University School of Medicine
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 776-81 (2015)
Novartis Institutes For Biomedical Research
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 770-5 (2015)
Bristol-Myers Squibb Research
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 764-9 (2015)
University of Maryland
Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 753-7 (2015)
Emory University
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 747-52 (2015)
Merck Research Laboratories
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 741-6 (2015)
Astrazeneca
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 736-40 (2015)
Euroscreen
Inhibitors of the Epidermal Growth Factor Receptor (EGFR) May Provide Effective Treatment for Lung Adenocarcinoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 732-3 (2015)
Therachem Research Medilab (India)
Novel Pyrazine Amide Compounds.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 729-31 (2015)
Temple University
Pyrrolopyridine or Pyrazolopyridine Derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 726-8 (2015)
Temple University
Vinyl sulfone analogs of lysophosphatidylcholine irreversibly inhibit autotaxin and prevent angiogenesis in melanoma.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5999-6013 (2015)
The University of Georgia
Chemical synthesis of tetracyclic terpenes and evaluation of antagonistic activity on endothelin-A receptors and voltage-gated calcium channels.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5985-98 (2015)
Kansas State University
Discovery, design, and synthesis of indole-based EZH2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3644-9 (2015)
Constellation Pharmaceuticals
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6014-24 (2015)
University of The Punjab
Development of fluorinated methoxylated chalcones as selective monoamine oxidase-B inhibitors: Synthesis, biochemistry and molecular docking studies.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 62: 22-29 (2015)
Grace College of Pharmacy
Coumarins as anticancer agents: a review on synthetic strategies, mechanism of action and SAR studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 476-95 (2015)
Central University of Punjab
Chalcone scaffolds as anti-infective agents: structural and molecular target perspectives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 496-524 (2015)
Guru Ghasidas Vishwavidyalaya (A Central University)
Design, synthesis and biological activities of novel oxazolo[4,5-g]quinazolin-2(1H)-one derivatives as EGFR inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 462-75 (2015)
China Pharmaceutical University
Discovery of 11ß-hydroxysteroid dehydrogenase type 1 inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3501-6 (2015)
Incheon National University
Multistage virtual screening and identification of novel HIV-1 protease inhibitors by integrating SVM, shape, pharmacophore and docking methods.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 409-18 (2015)
Nankai University
4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIa targeting the ATP binding site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4218-29 (2015)
National Institute of Chemistry
Structural development of stabilized helical peptides as inhibitors of estrogen receptor (ER)-mediated transcription.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4132-8 (2015)
National Institute of Health Sciences
Discovery of potent and selective nonplanar tankyrase inhibiting nicotinamide mimics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4139-49 (2015)
University of Oulu
Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3515-9 (2015)
Vanderbilt University Medical Center
Design, Synthesis, and Biological Evaluation of a Series of Anthracene-9,10-dione Dioximeß-Catenin Pathway Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5854-62 (2015)
University of Utah
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6348-58 (2015)
Novartis Institutes For Biomedical Research
Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5863-88 (2015)
Columbia University Medical Center
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6081-92 (2015)
Universit£
Design, Synthesis, and Characterization of 3-(Benzylidene)indolin-2-one Derivatives as Ligands fora-Synuclein Fibrils.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6002-17 (2015)
Washington University
Sulfonamide inhibition studies of the¿-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3550-5 (2015)
Universit£
Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chembiochem 16: 1771-81 (2015)
The Johns Hopkins University School of Medicine
Analysis of the Resistance Mechanism of a Benzoxaborole Inhibitor Reveals Insight into the Leucyl-tRNA Synthetase Editing Mechanism.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2277-85 (2015)
Ujf-Embl-Cnrs
A New Class of Potent N-Methyl-D-Aspartate Receptor Inhibitors: Sulfated Neuroactive Steroids with Lipophilic D-Ring Modifications.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5950-66 (2015)
Academy of Sciences of The Czech Republic V.V.I.
Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4344-53 (2015)
China Pharmaceutical University
Design and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives bearing an imidazolone moiety as c-Met kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4410-22 (2015)
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Bifunctional compounds targeting both D2 and non-a7 nACh receptors: design, synthesis and pharmacological characterization.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 367-83 (2015)
Universit£
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Ka inhibitor with high PI3K isoform selectivity and potent cellular activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3582-4 (2015)
Novartis Institutes For Biomedical Research
Regulating the master regulator: Controlling heat shock factor 1 as a chemotherapy approach.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3409-14 (2015)
University of New South Wales
Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 358-66 (2015)
Gdansk University of Technology
Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of a-glucosidase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 62: 15-21 (2015)
Hazara University
4-(N-Phenyl-N'-substituted benzenesulfonyl)-6-(4-hydroxyphenyl)quinolines as inhibitors of mammalian target of rapamycin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4237-47 (2015)
India Academy of Scientific & Innovative Research (Acsir)
Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4248-4255 (2015)
Fudan University
4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 4: 1156-1165 (2013)
National Institute of Diabetes and Digestive and Kidney Diseases
Probing the 'bipolar' nature of the carbonic anhydrase active site: aromatic sulfonamides containing 1,3-oxazol-5-yl moiety as picomolar inhibitors of cytosolic CA I and CA II isoforms.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 334-47 (2015)
Saint Petersburg State University
Antimitotic and antivascular activity of heteroaroyl-2-hydroxy-3,4,5-trimethoxybenzenes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4230-6 (2015)
Taipei Medical University
A computational view on the significance of E-ring in binding of (+)-arisugacin A to acetylcholinesterase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4848-53 (2015)
Alchemical Research
Type II Inhibitors Targeting CDK2.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
ACS Chem Biol 10: 2116-25 (2015)
University of Oxford
Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5649-73 (2015)
Glaxosmithkline
Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5609-19 (2015)
National Institute On Drug Abuse
Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3630-5 (2015)
Merck Research Laboratories
Structure-Activity Relationship Studies of Substituted 2-(Isoxazol-3-yl)-2-oxo-N'-phenyl-acetohydrazonoyl Cyanide Analogues: Identification of Potent Exchange Proteins Directly Activated by cAMP (EPAC) Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6033-47 (2015)
University of Texas Medical Branch
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5751-69 (2015)
Zhejiang University
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6225-36 (2015)
TBA
Discovery of N-aryl-naphthylamines as in vitro inhibitors of the interaction between HIV integrase and the cofactor LEDGF/p75.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 288-94 (2015)
"Sapienza" Universit£
Tyrosyl-DNA Phosphodiesterase I Inhibitors from the Australian Plant Macropteranthes leichhardtii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1756-60 (2015)
Griffith University
Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1671-82 (2015)
University of California Berkeley
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4364-4374 (2015)
Shandong University
Inhibition studies of bacterial, fungal and protozoanß-class carbonic anhydrases with Schiff bases incorporating sulfonamide moieties.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4181-7 (2015)
Universit£
Cloning, characterization and anion inhibition studies of a new¿-carbonic anhydrase from the Antarctic bacterium Pseudoalteromonas haloplanktis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4405-9 (2015)
Istituto Di Bioscienze E Biorisorse
Stereoselective synthesis and pharmacological evaluation of [4.3.3]propellan-8-amines as analogs of adamantanamines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4277-85 (2015)
Institut F£R Pharmazeutische Und Medizinische Chemie Der Westf£Lischen Wilhelms-Universit£T M£Nster
Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4428-33 (2015)
China Pharmaceutical University
Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4834-7 (2015)
University of California
Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3626-9 (2015)
Novartis Institutes For Biomedical Research
Potent benzoazepinone¿-secretase modulators with improved bioavailability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3495-500 (2015)
Merck Research Laboratories
Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 274-87 (2015)
Cnrs Umr 7311
The twin drug approach for novel nicotinic acetylcholine receptor ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4375-89 (2015)
University of Hawaii At Hilo
Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 185-204 (2015)
Universit£
Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3636-43 (2015)
Merck Research Laboratories
Design, synthesis and antiproliferative activities of novel benzamides derivatives as HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 100: 270-6 (2015)
Academy of Military Medical Sciences
Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4699-709 (2015)
Washington University
Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBß and Autophagy.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5900-15 (2015)
Fondazione Istituto Italiano Di Tecnologia
Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 163-78 (2015)
Seoul National University
Design, synthesis, pharmacological evaluation and molecular dynamics ofß-amino acids morphan-derivatives as novel ligands for opioid receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 150-62 (2015)
Universidad De Salamanca
Identification and Co-complex Structure of a New S. pyogenes SpeB Small Molecule Inhibitor.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 4365-73 (2015)
The Scripps Research Institute
Structure-Based Development of a Protein-Protein Interaction Inhibitor Targeting Tumor Necrosis Factor Receptor-Associated Factor 6.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5674-83 (2015)
Eisai
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3738-43 (2015)
Beijing Pearl Biotech
DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 4152-70 (2016)
University of Kansas
Discovery of CREBBP Bromodomain Inhibitors by High-Throughput Docking and Hit Optimization Guided by Molecular Dynamics.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1340-9 (2016)
University of Z£Rich
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Humanß3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 6048-57 (2015)
Asahi Kasei Pharma
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5916-29 (2015)
Leiden University
Structural Requirements for CNS Active Opioid Glycopeptides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5728-41 (2015)
The University of Arizona
Development of Safe and Effective Botanical Dietary Supplements.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 8360-72 (2015)
University of Illinois College of Pharmacy
Synthesis and biological evaluation of novel myrtucommulones and structural analogues that target mPGES-1 and 5-lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 133-49 (2015)
University of Jena
The interaction of 4-thiazolidinone derivatives containing indolin-2-one moiety with P-glycoprotein studied using K562 cell lines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 126-32 (2015)
The First Affiliated Hospital of Dalian Medical University
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 58-65 (2015)
Gwangju Institute of Science and Technology
Synthesis and biological evaluation of novel histone deacetylases inhibitors with nitric oxide releasing activity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4481-4488 (2015)
Shandong University
¿-Benzylidene digoxin derivatives synthesis and molecular modeling: Evaluation of anticancer and the Na,K-ATPase activity effect.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4397-404 (2015)
Universidade Federal De S£O Jo£O Del Rei
Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3676-80 (2015)
Tokyo University of Pharmacy and Life Sciences
Discovery of Highly Isoform Selective Thiazolopiperidine Inhibitors of Phosphoinositide 3-Kinase¿.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5684-8 (2015)
Vertex Pharmaceuticals
2-Aminopyridines with a Truncated Side Chain To Improve Human Neuronal Nitric Oxide Synthase Inhibitory Potency and Selectivity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5548-60 (2015)
Northwestern University
Synthesis, biological evaluation and molecular docking of N-phenyl thiosemicarbazones as urease inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 51-7 (2015)
University of Karachi
Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3665-70 (2015)
Soochow University
Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole as potential anti-inflammatory and analgesic agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 81-95 (2015)
Indian Institute of Technology (Banaras Hindu University)
Crystal structures of the apo form and a complex of human LMW-PTP with a phosphonic acid provide new evidence of a secondary site potentially related to the anchorage of natural substrates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4462-71 (2015)
University of Campinas
Biarylsulfonamide CCR9 inhibitors for inflammatory bowel disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3661-4 (2015)
Cubist Pharmaceuticals
Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4442-52 (2015)
University of Ljubljana
Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5247-63 (2015)
Institute of Experimental Botany Ascr & Palack£
Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4878-80 (2015)
University of East Anglia
Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3203-7 (2015)
Merck Research Laboratories
Cyclin dependent kinase (CDK) inhibitors as anticancer drugs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3420-35 (2015)
Eli Lilly
Verruculides A and B, two new protein tyrosine phosphatase 1B inhibitors from an Indonesian ascidian-derived Penicillium verruculosum.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3087-90 (2015)
Tohoku Pharmaceutical University
Identification of N-acylhydrazone derivatives as novel lactate dehydrogenase A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 63-70 (2015)
University of Bologna
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 101: 41-51 (2015)
Southeast University
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4453-61 (2015)
University of Copenhagen
Synthesis and evaluation of N-analogs of 1,2-diarylethane as Helicobacter pylori urease inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4508-4513 (2015)
Jishou University
Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3168-71 (2015)
Mercer University
Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3706-10 (2015)
Laboratoires Chemrf Inc/Chemrf Laboratories
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part I: Optimization of HTS hits towards an in vivo efficacious tool compound BI 414.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3264-9 (2015)
Boehringer Ingelheim Pharma
Synthesis and biological evaluation of 3,5-disubstituted-4-alkynylisoxozales as a novel class of HSP90 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3129-34 (2015)
Chengdu University of Tcm
Identification of alpha-substituted acylamines as novel, potent, and orally active mGluR5 negative allosteric modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3135-41 (2015)
Toray Industries
Synthesis and evaluation of pyrrolotriazine based molecules as PI3 kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3142-6 (2015)
Sphaera Pharma
Discovery and Optimization of a Porcupine Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5889-99 (2015)
Experimental Therapeutics Centre
Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5561-78 (2015)
Universit£
Structure-based design of potent HIV-1 protease inhibitors with modified P1-biphenyl ligands: synthesis, biological evaluation, and enzyme-inhibitor X-ray structural studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5334-43 (2015)
Purdue University
In vitro evaluation and in silico screening of synthetic acetylcholinesterase inhibitors bearing functionalized piperidine pharmacophores.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4567-75 (2015)
Visva-Bharati (A Central University)
Sulfonamide bearing pyrazolylpyrazolines as potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3208-12 (2015)
Kurukshetra University
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3275-80 (2015)
Boehringer Ingelheim Pharma
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5599-608 (2015)
Celgene
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 711-5 (2015)
Genentech
Dehydro-?-proline Containing ?4?1 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 701-6 (2015)
University of Bologna
Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 695-700 (2015)
Abbvie
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 683-8 (2015)
Merck
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 677-82 (2015)
Merck Research Laboratories
Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 665-70 (2015)
Kyoto Prefectural University of Medicine
Amino Acid Thioester Derivatives: A Highly Promising Scaffold for the Development of Metallo-ß-lactamase L1 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 660-4 (2015)
North-West University
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 655-9 (2015)
Epizyme
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 650-4 (2015)
Pfizer
Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 641-4 (2015)
Abbvie
Selective Acetamidine-Based Nitric Oxide Synthase Inhibitors: Synthesis, Docking, and Biological Studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 635-40 (2015)
University of Chieti&Quot;G. D'Annunzio&Quot
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 630-4 (2015)
Takeda Pharmaceutical
Prostaglandin EP3 Receptor Antagonists May Provide Novel Treatment for Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 626-7 (2015)
Therachem Research Medilab (India)
Pyridinonaphthyridinone Inhibitors of Type 2 Methionine Aminopeptidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 622-3 (2015)
Dart Neuroscience
Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4891-8 (2015)
Qilu University of Technology
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4792-803 (2015)
Asubio Pharma
Design, synthesis and preliminary biological evaluation of indoline-2,3-dione derivatives as novel HDAC inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4728-36 (2015)
Shandong University
3,5-Diarylpyrazole Derivatives Obtained by Ammonolysis of the Total Flavonoids from Chrysanthemum indicum Extract Show Potential for the Treatment of Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1593-9 (2015)
Sun Yat-Sen University
Molecular modeling based approach, synthesis, and cytotoxic activity of novel benzoin derivatives targeting phosphoinostide 3-kinase (PI3Ka).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3120-4 (2015)
Al-Zaytoonah University of Jordan
Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3164-7 (2015)
University of Leeds
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3157-63 (2015)
Janssen Research and Development
Therapeutic Potential of 5-HT6 Receptor Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7901-12 (2015)
Universit£
Discovery of 4,5,6,7-Tetrahydrobenzo[1,2-d]thiazoles as Novel DNA Gyrase Inhibitors Targeting the ATP-Binding Site.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5501-21 (2015)
University of Ljubljana
Virtual High-Throughput Screening To Identify Novel Activin Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5637-48 (2015)
Northwestern University
Exploration on natural product anibamine side chain modification toward development of novel CCR5 antagonists and potential anti-prostate cancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3721-5 (2015)
Virginia Commonwealth University
Phenoxymethyl 1,3-oxazoles and 1,2,4-oxadiazoles as potent and selective agonists of free fatty acid receptor 1 (GPR40).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3105-11 (2015)
Enamine
Structure-based design, synthesis, X-ray studies, and biological evaluation of novel HIV-1 protease inhibitors containing isophthalamide-derived P2-ligands.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4903-4909 (2015)
Purdue University
An oxidative coupling product of luteolin with cysteine ester and its enhanced inhibitory activity for xanthine oxidase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3117-9 (2015)
Osaka City University
Discovery and characterization of a potent and selective EP4 receptor antagonist.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3176-8 (2015)
Eli Lilly
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7140-63 (2015)
Glaxosmithkline
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4669-80 (2015)
University of Malaya
Discovery of novel, non-acidic mPGES-1 inhibitors by virtual screening with a multistep protocol.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4839-45 (2015)
University of Innsbruck
5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4649-59 (2015)
University of Belgrade
Discovery of potent, selective small molecule inhibitors ofa-subtype of type III phosphatidylinositol-4-kinase (PI4KIIIa).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3189-93 (2015)
Astrazeneca
Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammaliana7 nicotinic acetylcholine receptor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3184-8 (2015)
Universit£
Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5437-44 (2015)
Takeda California
Thiosemicarbazones as Aedes aegypti larvicidal.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 100: 162-75 (2015)
Universidade Federal De Pernambuco
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5620-36 (2015)
TBA
Strategies for the Discovery of Target-Specific or Isoform-Selective Modulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 7611-33 (2015)
Shandong University
Structures and Biological Evaluations of Agelasines Isolated from the Okinawan Marine Sponge Agelas nakamurai.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1428-33 (2015)
Tohoku Pharmaceutical University
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5323-33 (2015)
Celgene
Design and synthesis of new barbituric- and thiobarbituric acid derivatives as potent urease inhibitors: Structure activity relationship and molecular modeling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 6049-58 (2015)
The Islamia University of Bahawalpur
Novel inhibitors of RANKL-induced osteoclastogenesis: Design, synthesis, and biological evaluation of 6-(2,4-difluorophenyl)-3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-diones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4522-32 (2015)
Taipei Medical University
Arylpiperazine agonists of the serotonin 5-HT1A receptor preferentially activate cAMP signaling versus recruitment ofß-arrestin-2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4824-30 (2015)
Karolinska Institute and Karolinska University Hospital
Novel thiourea-based sirtuin inhibitory warheads.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3319-24 (2015)
Jiangsu University
Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3295-300 (2015)
Technische Universitat Dresden
Identification of a potent 5-phenyl-thiazol-2-ylamine-based inhibitor of FLT3 with activity against drug resistance-conferring point mutations.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 100: 151-61 (2015)
National Health Research Institutes
Structure-Based Design of¿-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 4927-39 (2015)
University of Michigan
Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5579-98 (2015)
Institut Pasteur
NO-donor thiacarbocyanines as multifunctional agents for Alzheimer's disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4688-98 (2015)
Universit£
Discovery of an 8-methoxytetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain without CYP inhibition liability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4638-48 (2015)
Astellas Pharma
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 86: 1425-32 (2015)
Tehran University of Medical Sciences
Fluorescent photoaffinity probes for mitotic protein kinase Aurora A.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3290-4 (2015)
University of Tartu
Synthesis of novel derivatives of oxindole, their urease inhibition and molecular docking studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3285-9 (2015)
Universiti Teknologi Mara Puncak Alam Campus
Anti-influenza activities of polyphenols from the medicinal mushroom Phellinus baumii.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3256-60 (2015)
Chonbuk National University
Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3270-4 (2015)
Boehringer Ingelheim Pharma
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4893-8 (2015)
Merck Research Laboratories
Synthesis of benzimidazole derivatives as potent ß-glucuronidase inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 36-44 (2015)
Universiti Teknologi Mara (Uitm)
New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3281-4 (2015)
University of Cagliari
Synthesis and carbonic anhydrase inhibitory properties of novel uracil derivatives.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3261-3 (2015)
Agriibrahim£E£En University
Indoline ureas as potential anti-hepatocellular carcinoma agents targeting VEGFR-2: Synthesis, in vitro biological evaluation and molecular docking.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 100: 89-97 (2015)
Egyptian Russian University
New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 100: 50-67 (2015)
Institute of Radiopharmaceutical Cancer Research
Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4871-83 (2015)
Astellas Pharma
Discovery of a 1-isopropyltetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4624-37 (2015)
Astellas Pharma
Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 99: 125-37 (2015)
Nanjing University
Structure and inhibition studies of a type II beta-carbonic anhydrase psCA3 from Pseudomonas aeruginosa.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4831-8 (2015)
University of Florida
Inhibitor Bound Crystal Structures of Bacterial Nitric Oxide Synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Biochemistry 54: 4075-82 (2015)
University of California Irvine
Synthesis, Biological Evaluation, and Docking of Dihydropyrazole Sulfonamide Containing 2-hydroxyphenyl Moiety: A Series of Novel MMP-2 Inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 86: 1405-10 (2015)
Nanjing University
Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1440-54 (2016)
The University of Texas M.D. Anderson Cancer Center
A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5256-73 (2015)
Amgen
Peptidomimeticß-Secretase Inhibitors Comprising a Sequence of Amyloid-ß Peptide for Alzheimer's Disease.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5408-18 (2015)
Instituto De Biologia Experimental E Tecnol£Gica
Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5143-9 (2015)
Philochem
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4846-59 (2015)
Astellas Pharma
Structure-based design of benzo[e]isoindole-1,3-dione derivatives as selective GSK-3ß inhibitors to activate Wnt/ß-catenin pathway.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 21-7 (2015)
Peking University
Modular synthesis and biological activity of pyridyl-based analogs of the potent Class I Histone Deacetylase Inhibitor Largazole.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5061-74 (2015)
Colorado State University
Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5274-86 (2015)
Jagiellonian University Medical College
New monomeric and dimeric uridinyl derivatives as inhibitors of chitin synthase.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 13-20 (2015)
Silesian University of Technology
Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 5000-14 (2015)
Takeda Pharmaceutical
Discovery of biaryl carboxylamides as potent ROR¿ inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2991-7 (2015)
Biogen Idec
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2958-62 (2015)
Merck Research Laboratories
Discovery of substituted 1,4-dihydroquinolines as novel promising class of P-glycoprotein inhibitors: First structure-activity relationships and bioanalytical studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3005-8 (2015)
Martin-Luther-University Halle-Wittenberg
Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3039-43 (2015)
Bristol-Myers Squibb
Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen asd opioid receptor inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2927-30 (2015)
Kitasato University
Investigation on the sucrose binding pocket of HIV-1 Integrase by molecular dynamics and synergy experiments.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3013-6 (2015)
Universit£
Synthesis and characterization of novel oxazines and demonstration that they specifically target cyclooxygenase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2931-6 (2015)
Bangalore University
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2907-12 (2015)
Genentech
Identification of 3,5,6-substituted indolin-2-one's inhibitors of Aurora B by development of a luminescent kinase assay.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2937-42 (2015)
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3034-8 (2015)
Arena Pharmaceuticals
Discovery of novel pyrazole-containing benzamides as potent ROR¿ inverse agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2985-90 (2015)
Biogen
Meridianin derivatives as potent Dyrk1A inhibitors and neuroprotective agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2948-52 (2015)
India Academy of Scientific & Innovative Research (Acsir)
Synthesis, molecular docking and biological evaluation of 3-arylfuran-2(5H)-ones as anti-gastric ulcer agent.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4860-4865 (2015)
Jishou University
Design and synthesis of benzothiazole-6-sulfonamides acting as highly potent inhibitors of carbonic anhydrase isoforms I, II, IX and XII.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4989-99 (2015)
Jazan University
One-pot reaction to obtain N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold as human A3 adenosine receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5355-60 (2015)
Universit£
Design, synthesis and biological evaluation of novel 5-oxo-2-thioxoimidazolidine derivatives as potent androgen receptor antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 99: 51-66 (2015)
Alla Chem
Recent trends in orexin research--2010 to 2015.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2875-87 (2015)
Actelion Pharmaceuticals
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4899-910 (2015)
Defence Research & Development Establishment (Drde)
Fragment-Based Design of Selective Nanomolar Ligands of the CREBBP Bromodomain.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 59: 1350-6 (2016)
University of Z£Rich
Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 7-12 (2015)
The M. S. University of Baroda
Development of novel adenosine receptor ligands based on the 3-amidocoumarin scaffold.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Bioorg Chem 61: 1-6 (2015)
Universidade Do Porto
Development of novel CXC chemokine receptor 7 (CXCR7) ligands: selectivity switch from CXCR4 antagonists with a cyclic pentapeptide scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5218-25 (2015)
Kyoto University
Synthesis and structure-activity relationship of aminoarylthiazole derivatives as correctors of the chloride transport defect in cystic fibrosis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 99: 14-35 (2015)
Istituto Giannina Gaslini
Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5028-37 (2015)
Vertex Pharmaceuticals
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Ka inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 99: 1-13 (2015)
Cairo University
Discovery and structural analyses of S-adenosyl-L-homocysteine hydrolase inhibitors based on non-adenosine analogs.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 4952-69 (2015)
Mitsubishi Tanabe Pharma
3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3024-9 (2015)
Uppsala University
N-Substituted pyrazole-3-carboxamides as inhibitors of human 15-lipoxygenase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 3017-23 (2015)
Uppsala University
Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1461-5 (2015)
University of Mississippi
Natural Product Primary Sulfonamides and Primary Sulfamates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1470-7 (2015)
Griffith University
Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 86: 1323-9 (2015)
Nanjing University
Novel 4-heteroaryl-antipyrines as DPP-IV inhibitors.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 86: 1292-303 (2015)
Cairo University
In Vitro Inhibitory Effects of 8-O-Demethylmaritidine and Undulatine on Acetylcholinesterase and Their Predicted Penetration across the Blood-Brain Barrier.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Nat Prod 78: 1189-92 (2015)
Charles University
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5121-36 (2015)
Shanghai Chempartner
Creation of Customized Bioactivity within a 14-Membered Macrolide Scaffold: Design, Synthesis, and Biological Evaluation Using a Family-18 Chitinase.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 4984-97 (2015)
Kitasato University
Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3013-32 (2015)
University of Bath
New indole-isoxazolone derivatives: Synthesis, characterisation and in vitro SIRT1 inhibition studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2768-72 (2015)
National Institute of Technology Karnataka
Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 4998-5014 (2015)
Iqm-Csic
Discovery of xanthine oxidase inhibitors and/ora-glucosidase inhibitors by carboxyalkyl derivatization based on the flavonoid of apigenin.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2778-81 (2015)
Beijing Institute of Pharmacology & Toxicology
Discovery of a new chemical series of BRD4(1) inhibitors using protein-ligand docking and structure-guided design.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2818-23 (2015)
Amri
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2793-9 (2015)
Bristol-Myers Squibb Research and Development
Design, synthesis, and biological activity of phenyl-pyrazole derivatives as BCR-ABL kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3147-52 (2015)
Beijing University of Technology
Selective inhibition of prolyl 4-hydroxylases by bipyridinedicarboxylates.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3081-90 (2015)
University of Wisconsin-Madison
Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 2982-8 (2015)
The University of Tokyo
Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3040-58 (2015)
University of Modena and Reggio Emilia
Structure-Activity Relationships of (+)-Naltrexone-Inspired Toll-like Receptor 4 (TLR4) Antagonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5038-52 (2015)
National Institute of Health
Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5096-107 (2015)
University of Pisa
Structure-Activity Relationships of Neplanocin A Analogues as S-Adenosylhomocysteine Hydrolase Inhibitors and Their Antiviral and Antitumor Activities.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5108-20 (2015)
Seoul National University
Substituted Bis-THF Protease Inhibitors with Improved Potency against Highly Resistant Mature HIV-1 Protease PR20.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
J Med Chem 58: 5088-95 (2015)
Georgia State University
Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.![BDB](/images/logo_bindingdb.png)
![BDB](/images/logo_bindingdb.png)
Chem Biol Drug Des 86: 1215-20 (2015)
Tehran University of Medical Sciences
A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2800-3 (2015)
Purdue University
New amide derivatives of Probenecid as selective inhibitors of carbonic anhydrase IX and XII: biological evaluation and molecular modelling studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 2975-81 (2015)
University of Chieti-Pescara
Discovery of a new class of histone deacetylase inhibitors with a novel zinc binding group.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Medchemcomm 6: 613-618 (2015)
Medical University of South Carolina
Design and Evaluation of 3-(Benzylthio)benzamide Derivatives as Potent and Selective SIRT2 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 607-11 (2015)
Northwestern University
Design, Synthesis, and Pharmacological Evaluation of Fusedß-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 602-6 (2015)
Chinese Academy of Sciences
Design of Pyridopyrazine-1,6-dione¿-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 596-601 (2015)
Pfizer
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 590-5 (2015)
Bristol-Myers Squibb
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 579-83 (2015)
Medical University of Lodz
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 573-8 (2015)
Merck Research Laboratories
Synthesis and Pharmacology ofa/ß(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 568-72 (2015)
University of Minnesota
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 562-7 (2015)
Genomics Institute of The Novartis Research Foundation
Monocarboxylate transporter 1 inhibitors as potential anticancer agents.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 558-61 (2015)
Medical School Duluth
Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 548-52 (2015)
University of Cambridge
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 543-7 (2015)
Guangzhou Institutes of Biomedicine and Health
Discovery of a Potent Class of PI3Ka Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 531-6 (2015)
Glaxosmithkline
Design and Validation of FRESH, a Drug Discovery Paradigm Resting on Robust Chemical Synthesis.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 518-22 (2015)
Emory University
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 513-7 (2015)
Merck Research Laboratories
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 507-12 (2015)
Shanghai Institute of Materia Medica
Discovery of Quinazoline-Based Fluorescent Probes toa1-Adrenergic Receptors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 502-6 (2015)
Shandong University
Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 496-501 (2015)
University of Camerino
Inhibitors of the PD-1/PD-L1 Pathway Can Mobilize the Immune System: An Innovative Potential Therapy for Cancer and Chronic Infections.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 489-90 (2015)
Therachem Research Medilab (India)
Inhibitors of the PAR-2 Signaling Pathway May Treat Pain and Inflammation.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
ACS Med Chem Lett 6: 487-8 (2015)
Therachem Research Medilab (India)
Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 98: 127-38 (2015)
Quaid-I-Azam University
Discovery of novel non-covalent inhibitors selective to theß5-subunit of the human 20S proteasome.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 98: 61-8 (2015)
Chinese Academy of Medical Sciences and Peking Union Medical College
(±) cis-Bisamido epoxides: A novel series of potent FXIII-A inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 98: 49-53 (2015)
University of Leeds
An unprecedented dual antagonist and agonist of human Transglutaminase 2.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 4922-6 (2015)
Stanford University
Recent advances for FLAP inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2607-12 (2015)
Astrazeneca
Isolation of cholinesterase andß-secretase 1 inhibiting compounds from Lycopodiella cernua.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3126-34 (2015)
Catholic University of Daegu
Synthesis and evaluation of tamoxifen derivatives with a long alkyl side chain as selective estrogen receptor down-regulators.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3091-6 (2015)
National Institute of Health Sciences
Combination of 4-anilinoquinazoline and rhodanine as novel epidermal growth factor receptor tyrosine kinase inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3221-7 (2015)
Soochow University
From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem Lett 25: 2804-8 (2015)
University of Bologna
Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Eur J Med Chem 97: 289-305 (2015)
Universit£
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3260-8 (2015)
Eli Lilly
Novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone: a new class ofß-glucuronidase inhibitors and in silico studies.![EBI](/images/logo_chembl.png)
![EBI](/images/logo_chembl.png)
Bioorg Med Chem 23: 3119-25 (2015)
Universiti Teknologi Mara
![BDB](/images/logo_bindingdb.png)
![EBI](/images/logo_chembl.png)