PMID
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Article Title
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Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
Novel Bivalent Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine D

National Institute On Drug Abuse-Intramural Research Program
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).

Takeda California
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.

Columbia University College of Physicians and Surgeons
Design, synthesis and biological evaluation of N-phenylquinazolin-4-amine hybrids as dual inhibitors of VEGFR-2 and HDAC.

China Pharmaceutical University
Hybrids from 4-anilinoquinazoline and hydroxamic acid as dual inhibitors of vascular endothelial growth factor receptor-2 and histone deacetylase.

China Pharmaceutical University
Discovery of quinazolin-4-amines bearing benzimidazole fragments as dual inhibitors of c-Met and VEGFR-2.

China Pharmaceutical University
Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors.

China Pharmaceutical University
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.

National Institute On Drug Abuse-Intramural Research Program
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.

Takeda California
Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy.

Takeda California
Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.

Takeda California
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.

Abbott Laboratories
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.

Takeda California
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

Abbott Laboratories
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.

Abbott Laboratories
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.

Takeda California
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Takeda California
Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors.

Nanjing University
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.

Abbott Laboratories
Design, synthesis and biological evaluation of quinoline amide derivatives as novel VEGFR-2 inhibitors.

Nanjing University
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Abbott Laboratories
Synthesis and structure-activity relationships of N-benzyl-N-(X-2-hydroxybenzyl)-N'-phenylureas and thioureas as antitumor agents.

Nanjing University
Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors.

Nanjing University
Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.

Amgen
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.

Chinese Academy of Sciences
Oleanolic acid and its derivatives: new inhibitor of protein tyrosine phosphatase 1B with cellular activities.

Chinese Academy of Sciences
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.

Abbott Laboratories
Asymmetric Dirhodium-Catalyzed Modification of Immunomodulatory Imide Drugs and Their Biological Assessment.

Emory University
Machine learning-based QSAR and LB-PaCS-MD guided design of SARS-CoV-2 main protease inhibitors.

Chulalongkorn University
Modifications to 1-(4-(2-Bis(4-fluorophenyl)methyl)sulfinyl)alkyl Alicyclic Amines That Improve Metabolic Stability and Retain an Atypical DAT Inhibitor Profile.

National Institute on Drug Abuse - Intramural Research Program
Recent advances in the development of deubiquitinases inhibitors as antitumor agents.

China Pharmaceutical University
Identification of Small Molecule Inhibitors and Ligand Directed Degraders of Calcium/Calmodulin Dependent Protein Kinase Kinase 1 and 2 (CaMKK1/2).

Bristol Myers Squibb
Design and Synthesis of Novel Cereblon Binders for Use in Targeted Protein Degradation.

Bristol Myers Squibb
PROTACS: A technology with a gold rush-like atmosphere.

China Pharmaceutical University
Structure-based discovery of potent USP28 inhibitors derived from Vismodegib.

Anhui University of Chinese Medicine
Design, synthesis, and anticancer evaluation of arylurea derivatives as potent and selective type II irreversible covalent FGFR4 inhibitors.

China Pharmaceutical University
Discovery of Selective Pituitary Adenylate Cyclase 1 Receptor (PAC1R) Antagonist Peptides Potent in a Maxadilan/PACAP38-Induced Increase in Blood Flow Pharmacodynamic Model.

Amgen
Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma.

Peking University
Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.

Research Institute of Tsinghua University
Structure Activity Relationships for a Series of Eticlopride-Based Dopamine D

National Institute On Drug Abuse - Intramural Research Program
Discovery of novel VEGFR-2 inhibitors embedding 6,7-dimethoxyquinazoline and diarylamide fragments.

China Pharmaceutical University
Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1).

Fount Therapeutics
Novel tertiary sulfonamide derivatives containing benzimidazole moiety as potent anti-gastric cancer agents: Design, synthesis and SAR studies.

Zhengzhou University
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.

Roche Innovation Center Shanghai
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D

National Institute of Neurological Disorders and Stroke
Design, synthesis, biological evaluation of benzoyl amide derivatives containing nitrogen heterocyclic ring as potential VEGFR-2 inhibitors.

Zhengzhou Children'S Hospital
Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines.

Affymax Research Institute
Rational discovery of a highly novel and selective mTOR inhibitor.

Takeda California
The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.

Wyeth-Ayerst Research
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.

Affymax Research Institute
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.

Affymax Research Institute
Discovery of an Orally Available Janus Kinase 3 Selective Covalent Inhibitor.

Peking University
Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors.

Celgene
Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.

Abbvie
Discovery of 1,2,4-triazine-based derivatives as novel neddylation inhibitors and anticancer activity studies against gastric cancer MGC-803 cells.

Zhengzhou University
Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.

National Institute On Drug Abuse-Intramural Research Program
Sulphonamide 1,4-dithia-7-azaspiro[4,4]nonane derivatives as gelatinase A inhibitors.

Shandong University
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.

Abbott Laboratories
Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics.

Nanjing University
Synthesis, molecular docking and biological evaluation of metronidazole derivatives as potent Helicobacter pylori urease inhibitors.

Nanjing University
Sesquiterpenes from the Hainan Sponge Dysidea septosa.

Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors.

Celgene Quanticel Research
Structure-based design and discovery of potent and selective KDM5 inhibitors.

Celgene
Design, synthesis, and biological evaluation of pyrazole derivatives containing acetamide bond as potential BRAF

Nanjing University
Discovery of Novel Small-Molecule Inhibitors of NF-κB Signaling with Antiinflammatory and Anticancer Properties.

University of Colorado
Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models.

Celgene Quanticel Research
Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D

National Institute On Drug Abuse
Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D

National Institute On Drug Abuse-Intramural Research Program
Discovery of 2H-Chromen-2-one Derivatives as G Protein-Coupled Receptor-35 Agonists.

Dalian Institute of Chemical Physics
Structure-Activity Relationship Studies on a Series of 3α-[Bis(4-fluorophenyl)methoxy]tropanes and 3α-[Bis(4-fluorophenyl)methylamino]tropanes As Novel Atypical Dopamine Transporter (DAT) Inhibitors for the Treatment of Cocaine Use Disorders.

National Institute On Drug Abuse-Intramural Research Program
TGF-B INHIBITOR COMPOUND AND USE THEREOF

Medinno Pharmaceutical Technology (Zhuhai) Co.
Arginase inhibitors as therapeutics

Mars
Cyclohexylamine derivatives having β2 adrenergic agonist and M3 muscarinic antagonist activities

Almirall
Lipoamide channel-binding sulfonamides selectively inhibit mycobacterial lipoamide dehydrogenase.

Weill Cornell Medical College