115 articles for P Li
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locke
Bristol-Myers Squibb Research and Development
Exploitation of a Novel Binding Pocket in Human Lipoprotein-Associated Phospholipase A2 (Lp-PLA2) Discovered through X-ray Fragment Screening.
Astex Pharmaceuticals
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
Intra-Cellular Therapies
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Bristol-Myers Squibb R & D
Discovery of 4-(dihydropyridinon-3-yl)amino-5-methylthieno[2,3-d]pyrimidine derivatives as potent Mnk inhibitors: synthesis, structure-activity relationship analysis and biological evaluation.
University of South Australia
Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: design, synthesis and 3D-QSAR studies.
Xi'An Jiaotong University
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Zhejiang University
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
Peking Union Medical College
Discovery of (E)-3-((styrylsulfonyl)methyl)pyridine and (E)-2-((styrylsulfonyl)methyl)pyridine derivatives as anticancer agents: synthesis, structure-activity relationships, and biological activities.
University of South Australia
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Intra-Cellular Therapies
Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors.
Shenyang Pharmaceutical University
Design, synthesis and SAR of piperidyl-oxadiazoles as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Chinese Academy of Sciences
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11ß-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.
TBA
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
University of Michigan Comprehensive Cancer Center
Potent and novel 11ß-HSD1 inhibitors identified from shape and docking based virtual screening.
Shanghai Pharmaceutical Holding
Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore.
University of Athens
Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.
Wyeth Research
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Glaxosmithkline
A Tiny Pocket Packs a Punch: Leveraging Pyridones for the Discovery of CNS-Penetrant Aza-indazole IRAK4 Inhibitors.
Biogen
Development of chalcone-like derivatives and their biological and mechanistic investigations as novel influenza nuclear export inhibitors.
Shandong University
Discovery of novel substituted pyridine carboxamide derivatives as potent allosteric SHP2 inhibitors.
China Pharmaceutical University
Identification of naphthalimide-derivatives as novel PBD-targeted polo-like kinase 1 inhibitors with efficacy in drug-resistant lung cancer cells.
Guangxi Normal University
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
Shanghai Institute of Materia Medica
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
Biogen
Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders.
Intra-Cellular Therapies, Inc.
Discovery of BIO-8169─A Highly Potent, Selective, and Brain-Penetrant IRAK4 Inhibitor for the Treatment of Neuroinflammation.
Biogen Inc.
Discovery and Development of NLRP3 Inhibitors Targeting the LRR Domain to Disrupt NLRP3-NEK7 Interaction for the Treatment of Rheumatoid Arthritis.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 1,2,4-Oxadiazole Derivatives Containing an Aryl Carboxylic Acid Moiety as Potent Sarbecovirus Papain-like Protease Inhibitors.
Peking Union Medical College and Chinese Academy of Medical Sciences
Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.
Erasca
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bristol-Myers Squibb
Ligand-Directed Photodegradation of Interacting Proteins: Oxidative HER2/HER3 Heterodimer Degradation with a Lapatinib-Derived Photosensitizer.
Shandong University
Discovery and pharmacological characterization of a novel benzimidazole TRPV4 antagonist with cyanocyclobutyl moiety.
Beijing Institute of Pharmacology and Toxicology
Development, validation, and evaluation of a deep learning model to screen cyclin-dependent kinase 12 inhibitors in cancers.
Peking Union Medical College
Discovery of novel bicyclic[3.3.0]proline peptidyl α-ketoamides as potent 3CL-protease inhibitors for SARS-CoV-2.
Sun Yat-Sen University
Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates.
Vertex Pharmaceuticals
Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1.
Kansas State University
Research progress of indole compounds with potential antidiabetic activity.
Xi'An Jiaotong University
Recent advances in the development of ubiquitin-specific-processing protease 7 (USP7) inhibitors.
Zhengzhou University
Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome.
China Pharmaceutical University
Slow-binding human serine racemase inhibitors from high-throughput screening of combinatorial libraries.
University of California
Synthesis and pharmacological validation of fluorescent diarylsulfonylurea analogues as NLRP3 inhibitors and imaging probes.
Shanghaitech University
The Discovery of GSK3640254, a Next-Generation Inhibitor of HIV-1 Maturation.
Bristol Myers Squibb Research and Early Development
A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.
Texas A&M University
A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.
Texas A&M University
Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Bristol Myers Squibb
Modulation of Naturally Occurring Linear Dipeptide Chirality to Reduce the Affinity for Oligopeptide Transporter 1 and Increase Intestinal Stability for an Enhanced Colon-Targeting Effect in the Treatment of Inflammatory Bowel Disease: An Application of
Shenyang Pharmaceutical University
Discovery of highly potent and selective EGFR
Beijing Institute of Pharmacology and Toxicology
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1.
Vertex Pharmaceuticals
Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.
Hong Kong Polytechnic University
Synthesis and biological evaluation of imidazole-based small molecule antagonists of the melanocortin 4 receptor (MC4-R).
Millennium Pharmaceuticals
Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.
China Pharmaceutical University
Design, synthesis and biological evaluation of macrocyclic derivatives as TRK inhibitors.
China Pharmaceutical University
Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model.
Millennium Pharmaceuticals
Design, synthesis, biological evaluation and structure-activity relationship study of quinazolin-4(3H)-one derivatives as novel USP7 inhibitors.
Zhengzhou University
Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT).
Gsk
Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
Peking Union Medical College
Potent Grb2-SH2 domain antagonists not relying on phosphotyrosine mimics.
National Cancer Institute-Frederick
The optimization and characterization of functionalized sulfonamides derived from sulfaphenazole against Mycobacterium tuberculosis with reduced CYP 2C9 inhibition.
Beijing University of Technology
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.
Shandong University
Structure-based design of thioether-bridged cyclic phosphopeptides binding to Grb2-SH2 domain.
National Cancer Institute-Frederick
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P
Bristol-Myers Squibb
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors.
Vertex Pharmaceuticals
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.
Bristol Myers Squibb
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Bristol Myers Squibb
Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P
Bristol-Myers Squibb
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Bristol Myers Squibb Research
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
National Cancer Institute-Frederick
Discovery of Novel Thiophene-Based, Thumb Pocket 2 Allosteric Inhibitors of the Hepatitis C NS5B Polymerase with Improved Potency and Physicochemical Profiles.
Vertex Pharmaceuticals
Optimization of 4-Aminopiperidines as Inhibitors of Influenza A Viral Entry That Are Synergistic with Oseltamivir.
University of Illinois At Chicago
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
TBA
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
Peking Union Medical College
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Development of hydroxamate-based histone deacetylase inhibitors containing 1,2,4-oxadiazole moiety core with antitumor activities.
University of Jinan
Second-generation antibacterial benzimidazole ureas: discovery of a preclinical candidate with reduced metabolic liability.
Vertex Pharmaceuticals
Development of novel ferulic acid derivatives as potent histone deacetylase inhibitors.
Xi'An Jiaotong University
Design, synthesis and biological activity of bicyclic carboxamide derivatives as TRK inhibitors.
China Pharmaceutical University
CH...O and CH...N hydrogen bonds in ligand design: a novel quinazolin-4-ylthiazol-2-ylamine protein kinase inhibitor.
Vertex Pharmaceuticals
Exploring Halogen Bonds in 5-Hydroxytryptamine 2B Receptor-Ligand Interactions.
National Institute of Biological Sciences
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.
Wuxi Apptec (Shanghai)
Synthesis and Biological Evaluation of a Series of Bile Acid Derivatives as FXR Agonists for Treatment of NASH.
Wuxi Apptec (Shanghai)
Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia.
University of South Australia
Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy.
Crystal Pharmatech
MIXED LINEAGE KINASE INHIBITORS AND METHODS OF USE
Department of Health And Human Services
MULTI-TARGET INHIBITOR TARGETING HDAC AND NAD SYNTHESIS AND USE OF MULTI-TARGET INHIBITOR
Ocean University of China
Substituted pyridines, pyridazines, pyrimidines, and 1,2,3-triazines as bruton's tyrosine kinase inhibitors
Hutchison Medipharma
CDK6/DYRK2 DUAL-TARGET INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF
Jiangsu Tasly Diyi Pharmaceutical
Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases
Janssen Sciences Ireland
EGFR proteolysis targeting chimeric molecules and associated methods of use
Arvinas Operations
Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
Boehringer Ingelheim International
Benzimidazole derivates useful as inhibitors of mammalian histone deacetylase activity
Kancera
Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain.
Oncology Innovative Medicines Unit
1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
University of Michigan
Competitive inhibition of human poly(A)-specific ribonuclease (PARN) by synthetic fluoro-pyranosyl nucleosides.
University of Thessaly
2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.
Universita Degli Studi Di Milano