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

Roche Innovation Center Shanghai
Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Bristol-Myers Squibb
Hybrids of phenylsulfonylfuroxan and coumarin as potent antitumor agents.

Fudan University
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).

Forma Therapeutics
The discovery of BMS-457, a potent and selective CCR1 antagonist.

Bristol-Myers Squibb
Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.

Bristol-Myers Squibb
Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.

Bristol-Myers Squibb
Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.

TBA
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.

Bristol-Myers Squibb
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).

Bristol-Myers Squibb Research and Development
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Novel sulfone-containing di- and trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Discovery of trisubstituted cyclohexanes as potent CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.

Bristol-Myers Squibb
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.

Bristol-Myers Squibb
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

Incyte
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Incyte
Discovery of a novel class of reversible monoacylglycerol lipase inhibitors for potential treatment of depression.

China Pharmaceutical University
Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action.

China Pharmaceutical University
Design, synthesis and evaluation of a pyrazolo[3,4-d]pyrimidine derivative as a novel and potent TGFβ1R1 inhibitor.

Nankai University
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.

Tanabe Research Laboratories Usa
Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).

Bristol-Myers Squibb
Hybrids of selective COX-2 inhibitors and active derivatives of edaravone as COX-2 selective NSAIDs with free radical scavenging activity: Design, synthesis and biological activities.

China Pharmaceutical University
Design and synthesis of a novel class of PDE4 inhibitors with antioxidant properties as bifunctional agents for the potential treatment of COPD.

China Pharmaceutical University
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.

Nankai University
Discovery of Pyxinol Amide Derivatives Bearing Amino Acid Residues as Nonsubstrate Allosteric Inhibitors of P-Glycoprotein-Mediated Multidrug Resistance.

Yantai University
Bisindole natural products: A vital source for the development of new anticancer drugs.

Hubei University of Science and Technology
Design and discovery of new selective and potent VEGF receptor 2 tyrosine kinase inhibitors.

Nankai University
Discovery, Synthesis, and Evaluation of Novel Dual Inhibitors of a Vascular Endothelial Growth Factor Receptor and Poly(ADP-Ribose) Polymerase for BRCA Wild-Type Breast Cancer Therapy.

Sichuan University
Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection.

China Innovation Center of Roche
Structure optimization and discovery of novel compound for the treatment of insertion mutations within exon 20 of EGFR and HER2.

Nankai University
Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery.

West China Hospital of Sichuan University
Discovery of potent and orally available malonyl-CoA decarboxylase inhibitors as cardioprotective agents.

Chugai Pharma Usa
Targeting Atg4B for cancer therapy: Chemical mediators.

Sichuan University
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.

West China Hospital of Sichuan University
Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors.

Chugai Pharma
Targeting Bromodomain-Selective Inhibitors of BET Proteins in Drug Discovery and Development.

Sichuan University
Discovery of SHR5133, a Highly Potent and Novel HBV Capsid Assembly Modulator.

Shanghai Hengrui Pharmaceutical
Structure-Activity Relationship Study of Subtype-Selective Positive Modulators of K

Chapman University School of Pharmacy
Discovery and Optimization of a Novel 2

Nankai University
Discovery, Synthesis, and Evaluation of Highly Selective Vascular Endothelial Growth Factor Receptor 3 (VEGFR3) Inhibitor for the Potential Treatment of Metastatic Triple-Negative Breast Cancer.

West China Hospital of Sichuan University
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.

Chinese Academy of Sciences
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer.

Nankai University
Pyxinol bearing amino acid residues: Easily achievable and promising modulators of P-glycoprotein-mediated multidrug resistance.

Universities of Shandong
First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo.

Nankai University
Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma.

Dana-Farber Cancer Institute
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.

Bristol-Myers Squibb Pharmaceuticals
Designing an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells.

Sichuan University
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.

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

Roche Innovation Center Shanghai
A New Approach of Mitigating CYP3A4 Induction Led to the Discovery of Potent Hepatitis B Virus (HBV) Capsid Inhibitor with Optimal ADMET Profiles.

TBA
Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.

Universities of Shandong
Synthesis, nitric oxide release, and dipeptidyl peptidase-4 inhibition of sitagliptin derivatives as new multifunctional antidiabetic agents.

Xi'An Jiaotong University
Pyridine-derived γ-secretase modulators.

Glaxosmithkline Pharmaceuticals
Pyridazine-derived γ-secretase modulators.

Glaxosmithkline Pharmaceuticals
Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profile.

Yale University
Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphate.

Yale University
Stereo-controlled synthesis of novel photoreactive gamma-secretase inhibitors.

Memorial Sloan-Kettering Cancer Center
Ribemansides A and B, TRPC6 Inhibitors from Ribes manshuricum That Suppress TGF-β1-Induced Fibrogenesis in HK-2 Cells.

China Pharmaceutical University
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.

Wuxi Apptec (Shanghai)
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.

Wuxi Apptec (Shanghai)
COMPOSITION AND METHOD FOR TREATMENT OF GRAM NEGATIVE BACTERIAL INFECTION

The State University of New York
Psychedelics and the human receptorome.

University of Oklahoma
PREPARATION AND APPLICATION METHOD OF HETEROCYCLIC COMPOUNDS AS KRAS INHIBITOR

Shanghai Kechow Pharma
TRUXILLIC ACID MONOESTER-DERIVATIVES AS SELECTIVE FABP5 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

The State University of New York
2-beta-naphthyl-acetic acid analogs as AKR1C3 inhibitors and methods of using same

The Trustees of The University of Pennsylvania
Substituted pyrazoles as LRRK2 inhibitors

Oscotec
Imidazopyrazine inhibitors of Bruton's tyrosine kinase

Acerta Pharma
Quinazolinones and azaquinazolinones as ubiquitin-specific protease 7 inhibitors

Valo Early Discovery
6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-B][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity

University of Pittsburgh
Compounds, compositions, and methods

Denali Therapautics
Substituted tetrahydrocarbazole and carbazole carboxamide compounds

Bristol-Myers Squibb
Inhibitors of lysine specific demethylase-1

Celgene Quanticel Research
Salt form of a human histone methyltransferase EZH2 inhibitor

Epizyme
Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase.

University of Regensburg
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.

Glaxosmithkline