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Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.

Gilead Sciences
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.

Genomics Institute of The Novartis Research Foundation
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase

Genomics Institute of The Novartis Research Foundation
Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor.

The National Center For Drug Screening
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.

TBA
A nonpeptidic agonist of glucagon-like peptide 1 receptors with efficacy in diabetic db/db mice.

National Center For Drug Screening
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

Genomics Institute of The Novartis Research Foundation
Bioactive compounds from Peperomia pellucida.

Chinese Academy of Sciences
Discovery of Sovleplenib, a Selective Inhibitor of Syk in Clinical Development for Autoimmune Diseases and Cancers.

HUTCHMED Limited
Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.

Sichuan University
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.

Merck & Co.
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors.

West China Hospital of Sichuan University
Annual review of PROTAC degraders as anticancer agents in 2022.

Zhengzhou University
Recent Progress and Prospects of Small Molecules for NLRP3 Inflammasome Inhibition.

Sichuan University
Discovery and Synthesis of a Naturally Derived Protein Kinase Inhibitor that Selectively Inhibits Distinct Classes of Serine/Threonine Kinases.

National Cancer Institute
Discovery of pyrimidine-5-carboxamide derivatives as novel salt-inducible kinases (SIKs) inhibitors for inflammatory bowel disease (IBD) treatment.

Sichuan University
Discovery of Triazinone Derivatives as Novel, Specific, and Direct NLRP3 Inflammasome Inhibitors for the Treatment of DSS-Induced Ulcerative Colitis.

Sichuan University
Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury.

Sichuan University
From lead to clinic: A review of the structural design of P2X7R antagonists.

Sichuan University
Isosteviol derivatives as protein tyrosine Phosphatase-1B inhibitors: Synthesis, biological evaluation and molecular docking.

Shanghai Ocean University
Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells.

Shenyang Pharmaceutical University
Discovery of Novel

Shenyang Pharmaceutical University
Hypouricemic Actions of the Pericarp of Mangosteen

Kunming Medical University
Synthesis and biological evaluation of aminobenzamides containing purine moiety as class I histone deacetylases inhibitors.

Nanchang University
Structure-Based Discovery of a Series of NSD2-PWWP1 Inhibitors.

Chinese Academy of Sciences
Development of Esterase-Resistant and Highly Active Ghrelin Analogs via Thiol-Ene Click Chemistry.

Tongji University
Development of MAO-A and 5-HT

China Pharmaceutical University
Optimization of Beclin 1-Targeting Stapled Peptides by Staple Scanning Leads to Enhanced Antiproliferative Potency in Cancer Cells.

Fudan University
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Na

Merck
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.

Merck
Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.

Lanzhou University
Discovery of a Bicyclic Peptidyl Pan-Ras Inhibitor.

The Ohio State University
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-

The Genomics Institute of The Novartis Research Foundation
Structure-Based Optimization of Multifunctional Agonists for Opioid and Neuropeptide FF Receptors with Potent Nontolerance Forming Analgesic Activities.

Lanzhou University
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.

Genomics Institute of The Novartis Research Foundation
Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis.

Bristol Myers Squibb
Synthesis and Biological Characterization of Cyclic Disulfide-Containing Peptide Analogs of the Multifunctional Opioid/Neuropeptide FF Receptor Agonists That Produce Long-Lasting and Nontolerant Antinociception.

Lanzhou University
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.

Merck
Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches.

Bristol Myers Squibb
Efficacy and Tolerability of Pyrazolo[1,5-

The Genomics Institute of The Novartis Research Foundation
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.

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

Xi'An Jiaotong University
Synthesis, structure elucidation, and biochemical evaluation of 7 alpha- and 7 beta-arylaliphatic-substituted androst-4-ene-3,17-diones as inhibitors of aromatase.

Ohio State University
Synthesis of C-4-modified zanamivir analogs as neuraminidase inhibitors and their anti-AIV activities.

Chinese Academy of Sciences
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.

Wuxi Apptec (Shanghai) Co.
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.

Chinese Academy of Sciences
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.

Chinese Academy of Sciences
INHIBITORS OF CHYMASE FOR USE IN THE SELECTIVE RESOLUTION OF THROMBI IN THROMBOTIC OR THROMBOEMBOLIC DISORDERS

Socpra Sciences Sante Et Humaines S.E.C.
IDURONIDASE STABILIZERS AND USES THEREOF

Academia Sinica
SUBSTITUTED FUSED RING COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR AND USES THEREOF

Suzhou Yabao Pharmaceutical R&D
SUBSTITUTED N-CYANOPYRROLIDINES WITH ACTIVITY AS USP30 INHIBITORS

Mission Therapeutics
Compounds of formulas (VII), (VIII), (IX), (XI), (XII), (XIII), and (XIV) as muscarinic receptor 4(M4) antagonists for treating neurological diseases

Neurocrine Biosciences
Wee-1 inhibiting pyrazolopyrimidinone compounds

Almac Discovery
Toll-like receptor 7 (TLR7) agonists having heteroatom-linked aromatic moieties, conjugates thereof, and methods and uses therefor

Bristol-Myers Squibb