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Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.

Pfizer
Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.

China Pharmaceutical University
Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one: Design, synthesis, model and use as hMAO-B inhibitors.

Anhui Medical University
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

Pfizer
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Pfizer
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.

National Center For Advancing Translational Sciences
Creation of an HDAC-based yeast screening method for evaluation of marine-derived actinomycetes: discovery of streptosetin A.

San Francisco State University
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.

Pfizer
Discovery of a novel noniminosugar acida glucosidase chaperone series.

National Center For Advancing Translational Sciences
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.

Merck Research Laboratories
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Merck Research Laboratories
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Merck Research Laboratories
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Merck
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.

Institute of Pharmacology & Toxicology
Discovery, synthesis, and biological evaluation of novel SMN protein modulators.

National Human Genome Research Institute
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.

Pfizer
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).

Institute of Pharmacology and Toxicology
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Merck Research Laboratories
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.

Texas A&M University
Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy.

The Sixth Affiliated Hospital of Wenzhou Medical University
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.

Wenzhou Medical University Lishui Hospital
Degradation of Cyclin-Dependent Kinase 9/Cyclin T1 by Optimized Microtubule-Associated Protein 1 Light Chain 3 Beta-Recruiting Coumarin Analogs.

Shanghai Institute of Materia Medica
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.

Pfizer
A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease.

Texas A&M University
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.

Pfizer
Design and synthesis of functionalized 4-aryl-Catechol derivatives as new antiinflammtory agents with in vivo efficacy.

University of Sannio
Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment.

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

Shanghai Institute of Materia Medica
Artemisinin-derived hybrids and their anticancer activity.

Qilu University of Technology (Shandong Academy of Sciences)
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
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
Recent advances of podophyllotoxin/epipodophyllotoxin hybrids in anticancer activity, mode of action, and structure-activity relationship: An update (2010-2020).

Qilu University of Technology (Shandong Academy of Sciences)
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.

Pfizer
Chemical Proteomic Characterization of a Covalent KRASG12C Inhibitor.

Lilly Research Laboratories
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
Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo.

National Engineering Research Center For The Emergency Drug
Quinolone hybrids and their anti-cancer activities: An overview.

Qilu University of Technology (Shandong Academy of Sciences)
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Merck
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.

Lanzhou University
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.

University of South China
Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.

Pfizer
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

Merck
Antitumor Activity of Lankacidin Group Antibiotics Is Due to Microtubule Stabilization via a Paclitaxel-like Mechanism.

University of Alberta
Non-iminosugar glucocerebrosidase small molecule chaperones.

National Human Genome Research Institute
Structures of Ebola Virus Glycoprotein Complexes with Tricyclic Antidepressant and Antipsychotic Drugs.

University of Oxford
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.

Shanghai Jiao Tong University
Optimization of the first small-molecule relaxin/insulin-like family peptide receptor (RXFP1) agonists: Activation results in an antifibrotic gene expression profile.

National Center For Advancing Translational Sciences
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.

Pfizer
Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

Pfizer
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle.

National Institute of Diabetes and Digestive and Kidney Diseases
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Pfizer
Steroids and protein-conjugates thereof

Regeneron Pharmaceuticals
Synthesis, structure-activity relationships studies of benzoxazinone derivatives as a-chymotrypsin inhibitors.

University of Karachi
Tryptophan-Rich Sensory Protein/Translocator Protein (TSPO) from Cyanobacterium Fremyella diplosiphon Binds a Broad Range of Functionally Relevant Tetrapyrroles.

Michigan State University
Novel Diketopiperazine Dihydroorotate Dehydrogenase Inhibitors Purified from Traditional Tibetan Animal Medicine Osteon Myospalacem Baileyi.

Chinese Academy of Sciences
Treatment of cerebral cavernous malformations and cerebral aneurysms with Rho kinase inhibitors

Bioaxone Biosciences