PMID
Data
Article Title
Organization
Discovery of Potent and Selective Leads against

Turing Pharmaceuticals
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.

Peking Union Medical College
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Constellation Pharmaceuticals
Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.

Sun Yat-Sen University
Suppression of Hepatocellular Carcinoma by Inhibition of Overexpressed Ornithine Aminotransferase.

Hebrew University-Hadassah Medical Center
2-Aminopyrimidin-4(1H)-one as the novel bioisostere of urea: discovery of novel and potent CXCR2 antagonists.

Glaxosmithkline
Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors.

Shanghai Hengrui Pharmaceutical
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: part 2. Pyridazine-based analogs.

Janssen Research and Development
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs.

Janssen Research and Development
Novel complex crystal structure of prolyl hydroxylase domain-containing protein 2 (PHD2): 2,8-Diazaspiro[4.5]decan-1-ones as potent, orally bioavailable PHD2 inhibitors.

Glaxosmithkline
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.

Merck Research Laboratories
Discovery of novel orally bioavailable GPR40 agonists.

Shanghai Hengrui Pharmaceutical
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.

University of Michigan
Indole-propionic acid derivatives as potent, S1P3-sparing and EAE efficacious sphingosine-1-phosphate 1 (S1P1) receptor agonists.

Glaxosmithkline
2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.

Shanghai Jiao Tong University
Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor.

The National Center For Drug Screening
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).

Glaxosmithkline
Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.

Glaxosmithkline
Design, synthesis, and biological activity of novel 1,4-disubstituted piperidine/piperazine derivatives as CCR5 antagonist-based HIV-1 entry inhibitors.

Beijing Institute of Biotechnology
Discovery of thiadiazole amides as potent, S1P3-sparing agonists of sphingosine-1-phosphate 1 (S1P1) receptor.

Glaxosmithkline
Discovery of a potent peptidic cyclophilin A inhibitor Trp-Gly-Pro.

Fudan University
Tetrahydroindolizinone NK1 antagonists.

Merck Research Laboratories
The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators.

The First Affiliated Hospital of China Medical University
Sticklac-Derived Natural Compounds Inhibiting RNase H Activity of HIV-1 Reverse Transcriptase.

Chiba University
Fluorinated conformationally restricted gamma-aminobutyric acid aminotransferase inhibitors.

Northwestern University
Discovery of aromatic 2-(3-(methylcarbamoyl) guanidino)-N-aylacetamides as highly potent chitinase inhibitors.

China Agricultural University
Optimization of NAMPT activators to achieve in vivo neuroprotective efficacy.

School of Pharmaceutical Sciences
(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Johnson & Johnson Pharmaceutical Research and Development
Discovery of Novel 7-Hydroxy-5-oxo-4,5-dihydrothieno[3,2-

Tongji University
Sortase A-mediated cyclization of novel polycyclic RGD peptides for α

Hefei Normal University
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity.

Soochow University
Identification of Novel Tricyclic Benzo[1,3]oxazinyloxazolidinones as Potent Antibacterial Agents with Excellent Pharmacokinetic Profiles against Drug-Resistant Pathogens.

Peking Union Medical College
Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer.

Guangxi University of Chinese Medicine
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.

Fujian Medical University
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.

Peking Union Medical College and Chinese Academy of Medical Sciences
Discovery of a novel 53BP1 inhibitor through AlphaScreen-based high-throughput screening.

Yantai University
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.

Bristol Myers Squibb
Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.

Bristol-Myers Squibb
Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.

Bristol-Myers Squibb
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.

Bristol-Myers Squibb Research & Development
Modification of the Thioglycosyl-Naphthalimides as Potent and Selective Human O-GlcNAcase Inhibitors.

China Agricultural University
Identification of Reversible Small Molecule Inhibitors of Endothelial Lipase (EL) That Demonstrate HDL-C Increase In Vivo.

TBA
Novel N-hydroxyfurylacrylamide-based histone deacetylase (HDAC) inhibitors with branched CAP group (Part 2).

China Pharmaceutical University
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.

Beijing Institute of Biotechnology
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.

Shandong University
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.

Gsk Pharmaceuticals R & D
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinaseδ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Bristol-Myers Squibb
MEMBRANE-ASSOCIATED TYROSINE- AND THREONINE-SPECIFIC CDC2-INHIBITORY KINASE (PKMYT1) INHIBITORS AND USES THEREOF

Insilico Medicine IP
Benzothiophene-based selective estrogen receptor downregulator compounds

University of Illinois
HETEROARYL CARBOXAMIDE COMPOUND

Astellas Pharma
Arginase inhibitors as therapeutics

Mars
Hydroxyindole carboxylic acid based inhibitors for oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2)

Indiana University Research and Technology
Modulators of calcium release-activated calcium channel

Rhizen Pharmaceuticals
New, potent P1/P2-morpholinone-based HIV-protease inhibitors.

Glaxosmithkline
In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine.

National Cancer Institute-Bethesda