PMID
Cmpds
Data
Article Title
Organization
7
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
9
Structure-based discovery of novel 4,5,6-trisubstituted pyrimidines as potent covalent Bruton's tyrosine kinase inhibitors.

China Pharmaceutical University
19
Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one: Design, synthesis, model and use as hMAO-B inhibitors.

Anhui Medical University
16
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

Pfizer
6
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

Merck Research Laboratories
10
Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Pfizer
15
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists.

National Center For Advancing Translational Sciences
2
Creation of an HDAC-based yeast screening method for evaluation of marine-derived actinomycetes: discovery of streptosetin A.

San Francisco State University
22
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.

Pfizer
14
Discovery of a novel noniminosugar acida glucosidase chaperone series.

National Center For Advancing Translational Sciences
23
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.

Merck Research Laboratories
37
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Merck Research Laboratories
29
Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Merck Research Laboratories
47
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

Merck
7
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.

Institute of Pharmacology & Toxicology
9
Discovery, synthesis, and biological evaluation of novel SMN protein modulators.

National Human Genome Research Institute
18
Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.

Pfizer
2
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
52
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

Merck Research Laboratories
27
Design, Synthesis, and Biological Evaluation of Selective STING Synergists That Enhance cGAMP-STING Pathway Activation without Inherent Agonist Activity.

Beijing Institute of Pharmacology & Toxicology
2
Discovery of 2,4-quinazolinedione derivatives as LC3B recruiters in the facilitation of protein complex degradations.

Hangzhou Institute for Advanced Study
10
Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease.

Texas A&M University
16
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
32
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.

Wenzhou Medical University Lishui Hospital
1
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
30
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.

Pfizer
33
A Systematic Survey of Reversibly Covalent Dipeptidyl Inhibitors of the SARS-CoV-2 Main Protease.

Texas A&M University
45
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.

Pfizer
18
Design and synthesis of functionalized 4-aryl-Catechol derivatives as new antiinflammtory agents with in vivo efficacy.

University of Sannio
2
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
19
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines.

Shanghai Institute of Materia Medica
1
Artemisinin-derived hybrids and their anticancer activity.

Qilu University of Technology (Shandong Academy of Sciences)
21
A systematic exploration of boceprevir-based main protease inhibitors as SARS-CoV-2 antivirals.

Texas A&M University
25
A multi-pronged evaluation of aldehyde-based tripeptidyl main protease inhibitors as SARS-CoV-2 antivirals.

Texas A&M University
12
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
1
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)
16
PF-07059013: A Noncovalent Modulator of Hemoglobin for Treatment of Sickle Cell Disease.

Pfizer
2
Chemical Proteomic Characterization of a Covalent KRASG12C Inhibitor.

Lilly Research Laboratories
10
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
37
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
19
Quinolone hybrids and their anti-cancer activities: An overview.

Qilu University of Technology (Shandong Academy of Sciences)
53
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Merck
5
Discovery of two novel branched peptidomimetics containing endomorphin-2 and RF9 pharmacophores: Synthesis and neuropharmacological evaluation.

Lanzhou University
23
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.

University of South China
13
Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9.

Pfizer
6
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

Merck
2
Antitumor Activity of Lankacidin Group Antibiotics Is Due to Microtubule Stabilization via a Paclitaxel-like Mechanism.

University of Alberta
5
Non-iminosugar glucocerebrosidase small molecule chaperones.

National Human Genome Research Institute
3
Structures of Ebola Virus Glycoprotein Complexes with Tricyclic Antidepressant and Antipsychotic Drugs.

University of Oxford
14
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
50
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
15
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.

Pfizer
17
Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.

Pfizer
1
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
14
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Pfizer
9
Steroids and protein-conjugates thereof

Regeneron Pharmaceuticals
30
Synthesis, structure-activity relationships studies of benzoxazinone derivatives as a-chymotrypsin inhibitors.

University of Karachi
5
Tryptophan-Rich Sensory Protein/Translocator Protein (TSPO) from Cyanobacterium Fremyella diplosiphon Binds a Broad Range of Functionally Relevant Tetrapyrroles.

Michigan State University
6
Novel Diketopiperazine Dihydroorotate Dehydrogenase Inhibitors Purified from Traditional Tibetan Animal Medicine Osteon Myospalacem Baileyi.

Chinese Academy of Sciences
2
Treatment of cerebral cavernous malformations and cerebral aneurysms with Rho kinase inhibitors

Bioaxone Biosciences