PMID
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Article Title
Organization
25
Discovery of new Syk inhibitors through structure-based virtual screening.

Second Military Medical University
6
Synthesis and in vitro biological evaluation of novel quinazoline derivatives.

Key Laboratory of The Ministry of Education For Medicinal Resources and Natural Pharmaceutical Chemistry
36
Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.

Merck Research Laboratories
9
Investigation of piperazine benzamides as human

Merck
3
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.

Abbvie
19
Design, Synthesis, and Pharmacological Evaluation of Fused -Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.

Chinese Academy of Sciences
4
Separation and peroxisome proliferator-activated receptor- agonist activity evaluation of synthetic racemic bavachinin enantiomers.

Shanghai University of Traditional Chinese Medicine
36
Rapid development of two factor IXa inhibitors from hit to lead.

Merck Research Laboratories
25
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.

Zhejiang University
8
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.

Alcon Laboratories
6
Hit-to-lead optimization and kinase selectivity of imidazo[1,2-a]quinoxalin-4-amine derived JNK1 inhibitors.

Activx Biosciences
37
Design and synthesis of diazatricyclodecane agonists of the G-protein-coupled receptor 119.

Pfizer
5
Identification of unique VLA-4 antagonists from a combinatorial library.

Merck Research Laboratories
21
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.

Merck Research Laboratories
38
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.

Abbott Laboratories
30
Coumarin-based inhibitors of Bacillus anthracis and Staphylococcus aureus replicative DNA helicase: chemical optimization, biological evaluation, and antibacterial activities.

Microbiotix
2
An efficient synthesis of 3-OBn-6ß,14-epoxy-bridged opiates from naltrexone and identification of a related dual MOR inverse agonist/KOR agonist.

University of New England
35
Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors.

Microbiotix
2
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.

Abbott Laboratories
6
Discovery of azetidinyl ketolides for the treatment of susceptible and multidrug resistant community-acquired respiratory tract infections.

Pfizer
18
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.

Sichuan University
13
Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.

Neurocrine Biosciences
3
Synthesis and inhibitory activity of oligosaccharide thiazolines as a class of mechanism-based inhibitors for endo-beta-N-acetylglucosaminidases.

University of Maryland
11
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.

Georgetown University Medical Center
24
A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization

TBA
17
6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3ß: discovery of nitrile derivatives with picomolar potency.

Activx Biosciences
30
Time-dependent botulinum neurotoxin serotype A metalloprotease inhibitors.

Microbiotix
34
Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3ß.

Activx Biosciences
12
Strategies to lower the Pgp efflux liability in a series of potent indole azetidine MCHR1 antagonists.

Lundbeck Research Usa
5
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

Pfizer
14
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.

Chinese Academy of Sciences
26
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.

Abbott Laboratories
25
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

Neurocrine Biosciences
23
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.

Abbott Bioresearch Center
22
Novel Carbamate-Based o-aminobenzamide Derivatives as Potent Antigastric Carcinoma Agents via Disrupting NAD+ Salvage Synthesis.

University of South China
17
Insights into NEK2 inhibitors as antitumor agents: From mechanisms to potential therapeutics.

Institute of Respiratory Healthand
24
Discovery of 4,5-dihydro-benzo[g]indazole-based hydroxamic acids as HDAC3/BRD4 dual inhibitors and anti-tumor agents.

Shenyang Pharmaceutical University
1
Synthesis and Antiosteoporotic Characterization of Diselenyl Maleimides: Discovery of a Potent Agent for the Treatment of Osteoporosis by Targeting RANKL.

Wenzhou Medical University
7
Nucleoside antiviral agents with atypical structures and new targets.

Shandong University
9
Discovery of Novel 2,4,5-Trisubstituted Pyrimidine Derivatives as Potent and Selective FGFR Inhibitors against Gatekeeper Mutants for the Treatment of NSCLC.

Wenzhou Medical University
32
One stone two birds: Introducing piperazine into a series of nucleoside derivatives as potent and selective PRMT5 inhibitors.

Ocean University of China
11
Rational design of a high-affinity fluorescent probe for visualizing monitoring the amyloid β clearance effect of anti-Alzheimer's disease drug candidates.

East China University of Science and Technology
31
Inhibitors targeting the PWWP domain-containing proteins.

Central China Normal University
3
Design, synthesis, and biological evaluation of novel penindolone derivatives as potential inhibitors of hemagglutinin-mediated membrane fusion.

Ocean University of China
40
Discovery of a Highly Potent and Selective Inhibitor Targeting Protein Lysine Methyltransferase NSD2.

Sun Yat-Sen University
1
Design, synthesis and biological evaluation of N-salicyloyl tryptamine derivatives as multifunctional neuroprotectants for the treatment of ischemic stroke.

University of South China
7
Design, synthesis, and biological evaluation of novel 1-amido-2-one-4-thio-deoxypyranose as potential antitumor agents for multiple myeloma.

Chinese Academy of Sciences
4
Research progress on GPX4 targeted compounds.

Peking University
31
Discovery of a Highly Potent Lysine Methyltransferases G9a/NSD2 Dual Inhibitor to Treat Solid Tumors.

Sun Yat-Sen University
36
Design, synthesis and structure-activity relationship of 1,8-naphthalimide derivatives as highly potent hCYP1B1 inhibitors.

Nanjing University of Chinese Medicine
1
Design, Synthesis, and Biological Evaluation of β-Trifluoroethoxydimethyl Selenides as Potent Antiosteoporosis Agents.

Wenzhou Medical University
16
Discovery of HC-7366: An Orally Bioavailable and Efficacious GCN2 Kinase Activator.

Pharmaron UK Ltd.
34
Discovery of Potent and Selective Covalent Inhibitors of HER2WT and HER2YVMA.

Pfizer
25
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.

Lundbeck Research Usa
23
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.

Lundbeck Research Usa
18
Rational design of 4-((6-phenoxypyrimidin-4-yl)amino)-N-(4-(piperazin-1-yl)phenyl)-1H-pyrazole-3-carboxamide (LT-540-717) as orally bioavailable FLT3 inhibitor.

Henan University of Chinese Medicine
3
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.

Shanghai Institute of Materia Medica
11
Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.

Sun Yat-Sen University
14
Discovery of benzoheterocyclic-substituted amide derivatives as apoptosis signal-regulating kinase 1 (ASK1) inhibitors.

South China University
11
Tuning the Metabolic Stability of Visual Cycle Modulators through Modification of an RPE65 Recognition Motif.

University of California - Irvine
17
Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.

Sun Yat-Sen University
2
Discovery of

Ocean University of China
55
Discovery of quinazoline HPK1 inhibitors with high cellular potency.

Emd Serono Research & Development Institute
33
Design, synthesis and biological evaluation of salicylanilides as novel allosteric inhibitors of human pancreatic lipase.

Shanghai University of Traditional Chinese Medicine
1
Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells.

Peking University
27
Discovery of thienopyridines as Src-family selective Lck inhibitors.

Abbott Bioresearch Center
3
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.

Tufts University School of Medicine
41
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.

Merck Research Laboratories
23
Discovery of pyrrolo[2,3-d]pyrimidine-based molecules as a Wee1 inhibitor template.

Capital Medical University
22
Discovery and development of selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors.

China Pharmaceutical University
18
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

Abbott Bioresearch Center
16
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.

Activx Biosciences
1
Chemo- and Site-Selective Lysine Modification of Peptides and Proteins under Native Conditions Using the Water-Soluble Zolinium.

Chinese Academy of Sciences
7
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.

Abbott Bioresearch Center
36
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.

University of North Carolina at Chapel Hill
25
Discovery of High-Affinity Inhibitors of the BPTF Bromodomain.

Fujian Medical University
29
Optimization of 4,6-Disubstituted Pyrido[3,2-

Shenyang Pharmaceutical University
1
Structure-based discovery of potent and selective small-molecule inhibitors targeting signal transducer and activator of transcription 3 (STAT3).

Sun Yat-Sen University
9
Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity.

China Pharmaceutical University
2
Discovery of chiral N-2'-aryletheryl-1'-alkoxy-ethyl substituted arylisoquinolones with anti-inflammatory activity from the nucleophilic addition reactions of the thiophenols and oxazolinium.

Chinese Academy of Sciences
7
Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y

China Pharmaceutical University
2
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.

Nankai University
1
Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators.

Xiamen University
5
Development of novel benzimidazole-derived neddylation inhibitors for suppressing tumor growth invitro and invivo.

East China University of Science and Technology
5
Macrocyclization in the design of Grb2 SH2 domain-binding ligands exhibiting high potency in whole-cell systems.

National Cancer Institute-Frederick
29
Novel Potent Selective Orally Active S1P5 Receptor Antagonists.

Biogen
3
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.

National Institutes of Health
15
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.

Moffitt Cancer Center
13
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.

Merck Research Laboratories
22
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.

Merck Research Laboratories
12
Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma.

University of Paris
24
Discovery of small molecule FLT3 inhibitors that are able to overcome drug-resistant mutations.

Sichuan University
24
Discovery of a series of benzopyrimidodiazepinone TNK2 inhibitors via scaffold morphing.

Dana-Farber Cancer Institute
53
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.

Merck Research Laboratories
41
Substituted imidazoles as glucagon receptor antagonists.

Merck Research Laboratories
18
Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors.

China Pharmaceutical University
1
Enzymatic biosynthesis and biological evaluation of novel 17-AAG glucoside as potential anti-cancer agents.

Bengbu Medical College
19
Prenylated Phenolic Compounds from the Aerial Parts of

Peking University
37
Benzopyrimidodiazepinone inhibitors of TNK2.

Harvard Medical School
23
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.

Biogen
2
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase.

High Magnetic Field Laboratory
50
Potent, orally absorbed glucagon receptor antagonists.

Merck Research Laboratories
8
Design and synthesis of novel conformationally restricted HIV protease inhibitors.

Vertex Pharmaceuticals
32
Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.

Vertex Pharmaceuticals
54
Pyrroles and other heterocycles as inhibitors of p38 kinase.

Merck Research Laboratory
7
Design, synthesis and anti-inflammatory evaluation of 3-amide benzoic acid derivatives as novel P2Y

China Pharmaceutical University
37
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors.

Peking University
2
Harzianoic acids A and B, new natural scaffolds with inhibitory effects against hepatitis C virus.

Peking University
1
Discovery of candesartan cilexetic as a novel neddylation inhibitor for suppressing tumor growth.

Shanghai University of Traditional Chinese Medicine
2
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Northwest University
12
Discovery of benzamides as potent human β3 adrenergic receptor agonists.

Merck And
23
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.

Jinan University
3
Flavonoids from Matteuccia struthiopteris and Their Anti-influenza Virus (H1N1) Activity.

Shenyang Pharmaceutical University
6
Novel 3-arylfuran-2(5H)-one-fluoroquinolone hybrid: design, synthesis and evaluation as antibacterial agent.

Jishou University
25
Combining pharmacophore, docking and substructure search approaches to identify and optimize novel B-RafV600E inhibitors.

Chinese Academy of Sciences
26
Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PA

South China Agricultural University
33
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.

Unc Eshelman School of Pharmacy
23
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa

Xenon Pharmaceuticals
39
Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant

East China University of Science and Technology
7
Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design.

Shenyang Pharmaceutical University
3
Novel 4-arylaminoquinazoline derivatives with (E)-propen-1-yl moiety as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.

Shaanxi Normal University
18
Discovery of the selective and efficacious inhibitors of FLT3 mutations.

China Pharmaceutical University
2
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.

Lilly Research Laboratories
9
Tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one scaffold derivatives: Synthesis and biological evaluation as selective BuChE inhibitors.

Anhui Medical University
4
6,7-Dimorpholinoalkoxy quinazoline derivatives as potent EGFR inhibitors with enhanced antiproliferative activities against tumor cells.

Shaanxi Normal University
2
Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.

East China University of Science and Technology
34
Discovery of 4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide (FN-1501), an FLT3- and CDK-Kinase Inhibitor with Potentially High Efficiency against Acute Myelocytic Leukemia.

China Pharmaceutical University
6
Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR andα-glucosidase.

Key Laboratory of The Ministry of Education For Medicinal Resources and Natural Pharmaceutical Chemistry
109
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.

East China University of Science and Technology
94
Novel Inhibitors of Staphyloxanthin Virulence Factor in Comparison with Linezolid and Vancomycin versus Methicillin-Resistant, Linezolid-Resistant, and Vancomycin-Intermediate Staphylococcus aureus Infections in Vivo.

East China University of Science and Technology
46
CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME

Arvinas
42
Compound modulators of sting

Ctxt
24
PYRIDO[4,3-b]INDOLE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS

Ventus Therapeutics U.S.
78
PYRAZOLEAMIDE DERIVATIVES

Hoffmann-La Roche
23
Therapeutic compounds and uses thereof

Kala Pharmaceuticals
28
Btk inhibitors

Merck Sharp & Dohme
6
Substituted pyridines as sodium channel blockers

Purdue Pharma
48
Carboxamide derivatives

Novartis
30
Fluorescent antagonists of the A3 adenosine receptor

Department Of Health And Human Services
9
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.

Gwangju Institute of Science and Technology
10
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors

Leo Pharma
3
Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors

Merck Patent
9
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.

Merck Research Laboratories
5
Modulation of Anopheles gambiae Epsilon glutathione transferase activity by plant natural products in vitro.

University of Zimbabwe
3
Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.

University of Michigan At Ann Arbor