PMID
Cmpds
Data
Article Title
Organization
16
Discovery of Spirocyclic Aldosterone Synthase Inhibitors as Potential Treatments for Resistant Hypertension.

Merck Research Laboratories
5
Enantiomeric 3-deaza-1',6'-isoneplanocin and its 3-bromo analogue: Synthesis by the Ullmann reaction and their antiviral properties.

Auburn University
22
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Merck Research Laboratories
13
Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1 F receptor agonists: Evolution from bicyclic to monocyclic cores.

Eli Lilly
37
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.

Merck Research Laboratories
3
A review on recent developments of indole-containing antiviral agents.

Central China Normal University
31
Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors.

Second Military Medical University
25
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.

Merck Research Laboratories
22
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.

Merck Research Laboratories
9
Design and application of a rigid quinazolone scaffold based on two-face Bima-helix mimicking.

Dalian University of Technology
34
Synthesis and acrosin inhibitory activities of 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives.

Second Military Medical University
21
Design and synthesis of novel benzoheterocyclic derivatives as human acrosin inhibitors by scaffold hopping.

Second Military Medical University
25
Identification of a novel family of BRAF(V600E) inhibitors.

University of Pennsylvania
18
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.

Central China Normal University
28
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 -Hydroxysteroid Dehydrogenase Type 1 Inhibitors.

TBA
1
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.

Merck Research Laboratories
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
26
Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives.

Second Military Medical University
38
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
24
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
26
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.

Merck Research Laboratories
46
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
26
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Merck Research Laboratories
1
A series of alpha-heterocyclic carboxaldehyde thiosemicarbazones inhibit topoisomerase IIalpha catalytic activity.

Chinese Academy of Sciences
11
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Merck Research Laboratories
29
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Merck Research Laboratories
3
Structure-Activity Relationship Studies of DNA Methyltransferase 1 Monovalent Degraders.

Icahn School of Medicine at Mount Sinai
22
Deep-Learning-Driven Discovery of SN3-1, a Potent NLRP3 Inhibitor with Therapeutic Potential for Inflammatory Diseases.

Peking University
44
Discovery of Potent STING Inhibitors Bearing a Difluorobenzodioxol Structural Motif as Potent Anti-Inflammatory Agents.

Shanghai Jiao Tong University
37
Design, Synthesis, Evaluation, and SAR of 5-Phenylisoindoline Derivatives, a Potent Class of Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (PD-1/PD-L1) Interaction.

Capital Medical University
28
Discovery of AMG 193, an MTA-Cooperative PRMT5 Inhibitor for the Treatment of MTAP-Deleted Cancers.

Amgen
37
Discovery of Potent and Balanced Dual RIPK2 and 3 Inhibitors as a New Strategy for the Treatment of Inflammatory Bowel Diseases.

Anhui Medical University
2
Anti-inflammatory agents design via the fragment hybrid strategy in the discovery of compound c1 for treating ALI and UC.

Wenzhou Medical University
5
Design, synthesis and optimization of Apcin analogues as Cdc20 inhibitors for triple-negative breast cancer therapy.

Central South University
3
A Prostate-Specific Membrane Antigen-Targeting Small Molecule-Drug Conjugate Strategy to Overcome the Hematological Toxicity of Olaparib.

Zhejiang University
41
Design, synthesis, and pharmacological characterization of sulfonylurea-based NLRP3 inhibitors: Towards an effective therapeutic strategy for Alzheimer's disease.

Peking University
2
Discovery of SZJK-0421: A Novel Potent, Low Toxicity, Selective Second Generation of CRM1 Inhibitor for the Treatment of Both Hematological and Solid Tumors.

Nanjing Normal University
6
Discovery of Novel MyD88 Inhibitor A5S to Alleviate Acute Lung Injury with Favorable Drug-like Properties.

Wenzhou Medical University
1
Discovery of pyridine-based derivatives as FLT3 inhibitors for the treatment of acute myeloid leukemia.

Guizhou Medical University
5
Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration.

Xiamen University
9
Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases.

Shanghai Institute of Pharmaceutical Industry Co., Ltd.
1
Discovery of highly potent and selective VEGFR2 kinase inhibitors for the treatment of rheumatoid arthritis.

Anhui Medical University
4
Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers.

Huanghuai University
49
Re-Evaluating PIN1 as a Therapeutic Target in Oncology Using Neutral Inhibitors and PROTACs.

Sichuan Kelun-Biotech Biopharmaceutical
34
Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma.

Zhejiang Sci-Tech University
22
Discovery and Optimization of Novel

Sichuan University
44
Optimized M24B Aminopeptidase Inhibitors for CARD8 Inflammasome Activation.

Memorial Sloan Kettering Cancer Center
18
Design, synthesis, and biological evaluation of novel 8-substituted quercetin derivatives targeting the β‑catenin/B-cell lymphoma 9 interaction.

Tongji University
17
Discovery of potent human dihydroorotate dehydrogenase inhibitors based on a benzophenone scaffold.

Sichuan University
1
PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism.

Nanjing University
1
Modified Podophyllotoxin Phenoxyacetamide Phenylacetate Derivatives: Tubulin/AKT1 Dual-Targeting and Potential Anticancer Agents for Human NSCLC.

Changzhou University
46
Discovery of Novel 3-Phenylpiperidine Derivatives Targeting the β-Catenin/B-Cell Lymphoma 9 Interaction as a Single Agent and in Combination with the Anti-PD-1 Antibody for the Treatment of Colorectal Cancer.

Fudan University
20
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders.

China Pharmaceutical University
8
Novel strategies to improve tumour therapy by targeting the proteins MCT1, MCT4 and LAT1.

Guang Xi University of Chinese Medicine
11
Design and synthesis of highly TRAIL expression HDAC inhibitors based on ONC201 to promote apoptosis of colorectal cancer.

China Pharmaceutical University
32
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.

Sichuan University
4
From lab to clinic: The discovery and optimization journey of PI3K inhibitors.

China Medical University
8
Structure-activity relationship of the novel bivalent and C-terminal modified analogues of endomorphin-2.

Lanzhou University
6
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.

TBA
5
Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor.

Lilly Research Laboratories
19
Design, Synthesis, and Biological Evaluation of a Novel Series of Teriflunomide Derivatives as Potent Human Dihydroorotate Dehydrogenase Inhibitors for Malignancy Treatment.

Sichuan University
25
Design and synthesis of dual inhibitors targeting snail and histone deacetylase for the treatment of solid tumour cancer.

China Pharmaceutical University
78
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

Merck
28
Design, synthesis and biological evaluation of 1H-indazole derivatives as novel ASK1 inhibitors.

China Pharmaceutical University
55
Discovery of a potent and selective inhibitor of histone lysine demethylase KDM4D.

Nankai University
27
Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis.

China Pharmaceutical University
31
Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.

University of Michigan
32
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).

Lilly Research Laboratories
1
Single-step fluorescent probes to detect decrotonylation activity of HDACs through intramolecular reactions.

City University of Hong Kong
20
Characterization of Specific

Pfizer
61
Bifunctional Naphtho[2,3-

Sichuan University
21
Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.

The First Affiliated Hospital of Xi'An Jiaotong University
22
Discovery of Macrocyclic Inhibitors of Apurinic/Apyrimidinic Endonuclease 1.

Boston University
19
Structure-Based Design of Selective, Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors.

University of Michigan
18
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.

Merck
35
Structure-Based Development of (1-(3'-Mercaptopropanamido)methyl)boronic Acid Derived Broad-Spectrum, Dual-Action Inhibitors of Metallo- and Serine-β-lactamases.

Sichuan University
2
Structural Basis for ( S)-3,4-Dicarboxyphenylglycine (DCPG) As a Potent and Subtype Selective Agonist of the mGlu

TBA
56
Discovery and Development of S6821 and S7958 as Potent TAS2R8 Antagonists.

Firmenich
3
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1

AMRI
13
Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.

Chinese Academy of Sciences
16
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.

Merck
21
Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human β-N-Acetyl-d-hexosaminidase.

East China University of Science and Technology
23
Syntheses and herbicidal activity of new triazolopyrimidine-2-sulfonamides as acetohydroxyacid synthase inhibitor.

Central China Normal University
37
Design, synthesis, and 3D-QSAR analysis of novel 1,3,4-oxadiazol-2(3H)-ones as protoporphyrinogen oxidase inhibitors.

Central China Normal University
7
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.

The University of Texas M.D. Anderson Cancer Center
42
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.

Chinese Academy of Sciences
1
6'-Fluoro-3-deazaneplanocin: Synthesis and antiviral properties, including Ebola.

Auburn University
7
Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor.

Soochow University
44
Identification of highly potent N-acylethanolamine acid amidase (NAAA) inhibitors: Optimization of the terminal phenyl moiety of oxazolidone derivatives.

Chinese Academy of Sciences
40
X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells.

West China School of Pharmacy
20
Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs.

Merck
5
Synthesis and anti-tumor activity of EF24 analogues as IKKβ inhibitors.

The First Affiliated Hospital of Wenzhou Medical University
8
Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.

University of Pisa
31
Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.

Merck Research Laboratories
20
Synthesis and Pharmacological Characterization of C4

TBA
9
INHIBITOR OF RECEPTOR-INTERACTING PROTEIN KINASE 1, AND PREPARATION METHOD AND USE THEREFOR

China Pharmaceutical University
157
Dihydrobenzimidazolones for medical treatment

C4 Therapeutics
46
Glucosylceramide synthase inhibitors for the treatment of diseases

Biomarin Pharmaceutical
27
Pyrazolyl-substituted heteroaryls and their use as medicaments

Boehringer Ingelheim International
4
Methods of treatment using modulators of SIRT2

Cornell University
5
Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties

Research Triangle Institute
88
Heterocyclic oxime compounds

Novartis
44
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.

Pfizer