PMID
Data
Article Title
Organization
Discovery of benzofuran-3(2H)-one derivatives as novel DRAK2 inhibitors that protect isletβ-cells from apoptosis.

East China Normal University
Novel ferulic amide derivatives with tertiary amine side chain as acetylcholinesterase and butyrylcholinesterase inhibitors: The influence of carbon spacer length, alkylamine and aromatic group.

Hu'Nan University
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.

Wuhan University School of Pharmaceutical Sciences
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.

Gilead Sciences
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.

Gilead Sciences
Synthesis and biological activities of indolizine derivatives as alpha-7 nAChR agonists.

Peking University
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.

Purdue University
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.

Glaxosmithkline
Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.

East China Normal University
Structure-Based Design of Potent and Selective CK1¿ Inhibitors.

TBA
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.

Purdue University
Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potentß-secretase inhibitors.

Purdue University
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Glaxosmithkline
Discovery of novel dual functional agent as PPARgamma agonist and 11beta-HSD1 inhibitor for the treatment of diabetes.

Chinese Academy of Sciences
Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.

Glaxosmithkline
Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.

Glaxosmithkline
Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.

Amgen
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.

Amgen
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.

Amgen
Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.

East China Normal University
Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.

Purdue University
Structure-based screening, optimization and biological evaluation of novel chrysin-based derivatives as selective PPARγ modulators for the treatment of T2DM and hepatic steatosis.

Guangzhou Medical University
Design, synthesis and evaluation of novel UDCA-aminopyrimidine hybrids as ATX inhibitors for the treatment of hepatic and pulmonary fibrosis.

Chinese Academy of Medical Sciences and Peking Union Medical College
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.

Shenyang Pharmaceutical University
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.

Ningxia Medical University
Overview of the development of selective androgen receptor modulators (SARMs) as pharmacological treatment for osteoporosis (1998-2021).

China Pharmaceutical University
Structure-Based Optimization of Coumestan Derivatives as Polyketide Synthase 13-Thioesterase(Pks13-TE) Inhibitors with Improved hERG Profiles for

East China Normal University
A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing.

China Pharmaceutical University
Identification of Small Molecule Inhibitors of RNase L by Fragment-Based Drug Discovery.

Peking University Shenzhen Graduate School
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.

Astrazeneca
3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.

University of Minnesota
3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.

University of Minnesota
Development of Novel Alkoxyisoxazoles as Sigma-1 Receptor Antagonists with Antinociceptive Efficacy.

East China Normal University
Pharmacophore-based design of novel 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H: Tolerance of a nonflexible linker.

University of Minnesota
Discovery of a Potent and Selective Oral Inhibitor of ERK1/2 (AZD0364) That Is Efficacious in Both Monotherapy and Combination Therapy in Models of Nonsmall Cell Lung Cancer (NSCLC).

Astrazeneca
Design and Synthesis of Novel Positive Allosteric Modulators of α7 Nicotinic Acetylcholine Receptors with the Ability To Rescue Auditory Gating Deficit in Mice.

Peking University
6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase.

University of Minnesota
N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase.

University of Minnesota
Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase.

University of Minnesota
6-Biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibited HIV reverse transcriptase-associated RNase H.

University of Minnesota
6-Arylthio-3-hydroxypyrimidine-2,4-diones potently inhibited HIV reverse transcriptase-associated RNase H with antiviral activity.

University of Minnesota
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.

Purdue University
Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors.

East China Normal University
Structure-Guided Discovery of Potent and Selective Inhibitors of ERK1/2 from a Modestly Active and Promiscuous Chemical Start Point.

Astrazeneca
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis.

East China Normal University
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.

Purdue University
IDURONIDASE STABILIZERS AND USES THEREOF

Academia Sinica
PYRAZOLOPYRIMIDINE DERIVATIVE AND ANTICANCER PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT

Korea Research Institute of Chemical Technology
COMPOUNDS CONTAINING A GEM-DIFLUORIDE GROUP AND PREPARATION METHOD AND USE THEREOF

Cgenetech (Suzhou, China) Co.
DEVELOPMENT AND OPTIMIZATION OF THIOCHROMENOTHIAZOLE-BASED MSUT2 INHIBITORS AS CANDIDATES FOR THE TREATMENT OF TAUOPATHY

Department of Veterans Affairs
COMPOUND AS ADENOSINE A2a RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

Chong Kun Dang Pharmaceutical
N-methyl, n-(6-(methoxy)pyridazin-3-yl) amine derivatives as autotaxin (ATX) modulators

Boehringer Ingelheim International
Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors

Neurolixis
JAK kinase inhibitor compounds for treatment of respiratory disease

Theravance Biopharma R&D Ip
Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases

Zhejiang Dtrm Biopharma
Substituted benzene compounds

Epizyme
Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as HIV integrase inhibitor

Japan Tobacco
Pyrazolo[3,4-d]pyrimidine compounds, their preparation and use as sigma ligands

Laboratorios Del Dr. Esteve
Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists

Bayer Intellectual Property
Piperazine compound capable of inhibiting prostaglandin D synthase

Taiho Pharmaceutical
Venlafaxine: discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites.

Mcgill University
Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.

Abbott Laboratories
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bristol-Myers Squibb
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.

Merck Research Laboratories
The vnd/NK-2 homeodomain: thermodynamics of reversible unfolding and DNA binding for wild-type and with residue replacements H52R and H52R/T56W in helix III.

National Institutes of Health