PMID
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Article Title
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Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT

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

Roche Innovation Center Shanghai
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved

Genentech
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.

Pharmaron-Beijing
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton's tyrosine kinase (BTK) inhibitors.

Xi'An Jiaotong University
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.

China Pharmaceutical University
Studies examining the relationship between the chemical structure of protoxin II and its activity on voltage gated sodium channels.

Purdue Pharma
Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.

Departments of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical and Translational Research, and Pharmaceutical Candi
Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.

Bristol-Myers Squibb
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.

Bristol-Myers Squibb Research and Development
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.

Dalian University of Technology
Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase.

China Pharmaceutical University
Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases.

China Pharmaceutical University
Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design.

Dalian University of Technology
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.

Dalian University of Technology
Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.

Bristol-Myers Squibb
Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.

The Chinese Academy of Sciences
Carboxyl-promoted enhancement of selectivity for the β
3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-β
3 binding selectivity

TBA
Aglycone exploration of C-arylglucoside inhibitors of renal sodium-dependent glucose transporter SGLT2.

Bristol Myers Squibb
Design, synthesis and biological evaluation of N-salicyloyl tryptamine derivatives as multifunctional neuroprotectants for the treatment of ischemic stroke.

University of South China
Discovery of potent HIV-1 NNRTIs by CuAAC click-chemistry-based miniaturized synthesis, rapid screening and structure optimization.

Shandong University
Design, synthesis and antibacterial activity evaluation of ebselen derivatives in NDM-1 producing bacteria.

Ocean University of China
pH regulators and their inhibitors in tumor microenvironment.

University of South China
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.

Zhejiang University
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

TBA
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.

Bristol-Myers Squibb Pharmaceutical Research Institute
Exploration and Biological Evaluation of 1,3-Diamino-7

Chinese Academy of Medical Sciences&Peking Union Medical College
Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.

Pharmaceutical Research Institute
Recent progress toward developing axial chirality bioactive compounds.

Shandong University
Discovery of conformationally constrained c-Abl inhibitors with potential neuroprotective effects against Parkinson's disease.

Southern Medical University
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines.

Shanghai Institute of Materia Medica
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.

China Innovation Center of Roche
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.

Zhejiang University
Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity.

Merck
Syntheses, Biological Evaluations, and Mechanistic Studies of Benzo[

China Pharmaceutical University
BMS-201620: a selective beta 3 agonist.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis.

Bristol-Myers Squibb
Discovery of macrocyclic HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Merck
BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor.

Bristol-Myers Squibb Pharmaceutical Research Institute
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.

Merck
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.

Merck
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.

Merck
Chemoreactive-Inspired Discovery of Influenza A Virus Dual Inhibitor to Block Hemagglutinin-Mediated Adsorption and Membrane Fusion.

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

Roche Innovation Center Shanghai
Highly Potent and Selective Plasmin Inhibitors Based on the Sunflower Trypsin Inhibitor-1 Scaffold Attenuate Fibrinolysis in Plasma.

The University of Queensland
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.

Shandong University
Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.

Genentech
Overview of Recent Strategic Advances in Medicinal Chemistry.

Shandong University
Identification of highly potent and selective Cdc25 protein phosphatases inhibitors from miniaturization click-chemistry-based combinatorial libraries.

Shandong University
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.

Bristol-Myers Squibb Research and Development
Discovery of phenylalanine derivatives as potent HIV-1 capsid inhibitors from click chemistry-based compound library.

Shandong University
Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.

Shandong University
Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.

Shandong University
Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.

Genentech
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).

Genentech
Discovery of Thiophene[3,2-

Shandong University
Design, synthesis and biological evaluation of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydroquinoxaline moiety as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Shandong University
Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Pharmaron-Beijing
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.

Second Military Medical University
QUINOLINE COMPOUND AND USE THEREOF

Shanghai Pharmaceuticals Holding Co.
Deuterated protease inhibitors

Kansas State University Research Foundation
ISOXAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERED RELATED THERETO

Arena Pharmaceuticals
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN

Poseidon Innovation 1
COMPOUND USED AS KINASE INHIBITOR AND USE THEREOF

Tyk Medicines
SARS-CoV-2 inhibitors for treating coronavirus infections

Insilico Medicine Ip
Combination therapy for treatment of hematological diseases

Incyte
Substituted pyridines as inhibitors of histone deacetylase

Alkermes
Selective NR2B antagonists

Bristol-Myers Squibb
Bipyrazole derivatives as JAK inhibitors

Incyte
Autotaxin inhibitors

Cancer Research Technology
[5,6]—fused bicyclic antidiabetic compounds

Merck Sharp & Dohme
Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists

Bristol-Myers Squibb
Imidazopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases

Bristol-Myers Squibb
Selective histone deactylase 6 inhibitors

H. Lee Moffitt Cancer Center and Research Institute
Disubstituted beta-lactones as inhibitors of N-acylethanolamine acid amidase (NAAA)

University of California
Aniline derivatives, their preparation and their therapeutic application

Fovea Pharmaceuticals
Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives

Reviva Pharmaceuticals
Selective NR2B antagonists

Bristol-Myers Squibb
Coumarin-thiazole and -oxadiazole derivatives: Synthesis, bioactivity and docking studies for aldose/aldehyde reductase inhibitors.

Comsats Institute of Information Technology
Sulfamide sodium channel inhibitors

Amgen
DiPOA ([8-(3,3-diphenyl-propyl)-4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]dec-3-yl]-acetic acid), a novel, systemically available, and peripherally restricted mu opioid agonist with antihyperalgesic activity: I. In vitro pharmacological characterization and pharmacokinetic properties.

Purdue Pharma Discovery Research
Pharmacology and functions of metabotropic glutamate receptors.

Emory University
Splicing factor SF3b as a target of the antitumor natural product pladienolide.

Eisai