PMID
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Data
Article Title
Organization
24
N

Seoul National University
4
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism.

Kyung Hee University
8
4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies.

Peking University Health Science Center
12
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.

Lanzhou University
17
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatic and antitumor agents.

Duquesne University
26
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.

AstraZeneca
16
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).

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

TBA
7
Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease.

Sun Yat-Sen University
4
An approach for differentiating isozymes. Construction of libraries containing short aromatic peptides as part of a method to design selective inhibitors against lipases.

Seoul National University
28
Novel benzothiophene H1-antihistamines for the treatment of insomnia.

Neurocrine Biosciences
3
Curcumin is a potent DNA hypomethylation agent.

The Ohio State University
28
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Merck Research Laboratories
21
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Merck Research Laboratories
8
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents.

Duquesne University
9
Development of potent non-carbohydrate imidazole-based small molecule selectin inhibitors with antiinflammatory activity.

Ontogen
9
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.

Duquesne University
21
Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia.

Neurocrine Biosciences
12
Potent and novel 11ß-HSD1 inhibitors identified from shape and docking based virtual screening.

Shanghai Pharmaceutical Holding
5
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.

Neurocrine Biosciences
3
Selectivea-glucosidase substrates and inhibitors containing short aromatic peptidyl moieties.

Seoul National University
27
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.

Neurocrine Biosciences
27
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.

Neurocrine Biosciences
15
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.

Institute of Science & Technology
25
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.

Neurocrine Biosciences
8
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.

Neurocrine Biosciences
37
Design, synthesis, and structure-affinity relationships of novel series of sialosides as CD22-specific inhibitors.

Gifu University
21
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.

Duquesne University
22
Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.

Graduate School of The Chinese Academy of Sciences
15
Discovery of novel transforming growth factor β type 1 receptor inhibitors through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation in hepatocellular carcinoma.

Tianjin Medical University
36
Harnessing the Magic Methyl Effect: Discovery of CLPP-2068 as a Novel HsClpP Activator for the Treatment of Diffuse Large B-Cell Lymphoma.

Shanghai Institute of Materia Medica
14
Selective Inhibition of Rat α7 Nicotinic Acetylcholine Receptors by LvID, a Newly Characterized α4/7-Conotoxin from Conus lividus.

Zhejiang University
3
New anti-ovarian cancer quinolone derivatives acting by modulating microRNA processing machinery.

University of Perugia
5
Scaffold hopping-driven optimization for the identification of NLRP3 inhibitors as potential gout therapeutics.

Peking University
36
Discovery of an Orally Bioavailable STING Inhibitor with In Vivo Anti-Inflammatory Activity in Mice with STING-Mediated Inflammation.

China Pharmaceutical University
4
Hit to lead optimization of the 4-trifluoromethylquinoline derivatives as novel SGK1 inhibitors with potent anti-prostate cancer activity.

Guizhou Medical University
24
Design, Synthesis, and biological evaluation of 7H-Pyrrolo[2,3-d]pyrimidines as potent HPK1 kinase inhibitors.

University of Chinese Academy of Sciences
5
PRMT7 in cancer: Structure, effects, and therapeutic potentials.

Ningbo University
8
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy.

Insilico Medicine Shanghai Ltd
55
Design, Synthesis, and Antitumor Activity Evaluation of 2-Phenylthiazole-5-Carboxylic Acid Derivatives Targeting Transactivation Response RNA-Binding Protein 2.

Chengdu Institute of Biology
4
Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy.

China Pharmaceutical University
8
Structure-based virtual screening discovers novel PKMYT1 inhibitors.

Shenyang Pharmaceutical University
1
Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents.

Sun Yat-sen University
36
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.

Shanghai Institute of Materia Medica
14
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.

Guizhou Medical University
31
Design and Synthesis of 7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylic Acid Derivatives as PP5 Inhibitors To Reverse Temozolomide Resistance in Glioblastoma Multiforme.

China Pharmaceutical University
5
Rational design of small-sized peptidomimetic inhibitors disrupting protein-protein interaction.

Ningxia Medical University
3
Allosteric Activation of Protein Phosphatase 5 with Small Molecules.

China Pharmaceutical University
29
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.

Shanghai Institute of Materia Medica
15
Discovery of a Novel ASM Direct Inhibitor with a 1,5-Diphenyl-pyrazole Scaffold and Its Antidepressant Mechanism of Action.

China Pharmaceutical University
33
Structural Modification and Biological Evaluation of 2,8-Disubstituted Adenine and Its Nucleosides as A2A Adenosine Receptor Antagonists: Exploring the Roles of Ribose at Adenosine Receptors.

Seoul National University
5
Discovery of LC-MI-3: A Potent and Orally Bioavailable Degrader of Interleukin-1 Receptor-Associated Kinase 4 for the Treatment of Inflammatory Diseases.

Hangzhou Medical College
14
Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal

Rigel Pharmaceuticals
36
Transformation of a Dopamine D

Shanghaitech University
24
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.

Insilico Medicine Shanghai
21
Discovery of Novel

China Pharmaceutical University
4
Novel Strategy To Inhibit Transthyretin Amyloidosis via the Synergetic Effect of Chemoselective Acylation and Noncovalent Inhibitor Release.

Chungnam National University
22
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A

Seoul National University
21
Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis.

Shanghai Institute of Materia Medica
38
Discovery of a potent and selective allosteric inhibitor targeting the SHP2 tunnel site for RTK-driven cancer treatment.

Hangzhou Medical College
8
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.

Zhejiang University
7
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.

Ningxia Medical University
44
Discovery of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.

Shanghai Institute of Materia Medica
10
Structure-Based Design of Novel Alkynyl Thio-Benzoxazepinone Receptor-Interacting Protein Kinase-1 Inhibitors: Extending the Chemical Space from the Allosteric to ATP Binding Pockets.

Ningxia Medical University
7
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.

Guangxi University
29
Structure-Based Design of the Indole-Substituted Triazolopyrimidines as New EED-H3K27me3 Inhibitors for the Treatment of Lymphoma.

Zhengzhou University
2
Design, synthesis, and biological evaluation of novel 2'-methyl-2'-fluoro-6-methyl-7-alkynyl-7-deazapurine nucleoside analogs as anti-Zika virus agents.

Guangzhou Institutes of Biomedicine and Health
8
Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances.

Shandong University
13
Interaction of A

National Cancer Institute (Ba, Mm, Sl, Sva)
16
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis.

Southern Medical University Biomedical Research Center
8
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.

Ningxia Medical University
9
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.

Chinese Academy of Sciences
9
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.

Shenyang Pharmaceutical University
1
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A

University of Southern California
17
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HT

Hec Pharm Group
20
Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HT

Hec Research and Development Center
20
Design, synthesis and activity evaluation of isopropylsulfonyl-substituted 2,4- diarylaminopyrimidine derivatives as FAK inhibitors for the potential treatment of pancreatic cancer.

Dalian Medical University
8
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.

China Pharmaceutical University
19
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human α7 Nicotinic Acetylcholine Receptors.

Hainan University
22
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.

Neurocrine Biosciences
2
Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.

University of South Florida
51
2-Phenylcyclopropylmethylamine Derivatives as Dopamine D

Shanghaitech University
45
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous

Agios Pharmaceuticals
24
Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.

Ningxia Medical University
7
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.

Ningxia Medical University
26
Discovery of a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.

Shanghai Pharmaceuticals Holding
29
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.

Northwestern University
2
An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators.

Shandong University
23
Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors.

China Pharmaceutical University
15
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.

Seoul National University
17
High Selectivity of an α-Conotoxin LvIA Analogue for α3β2 Nicotinic Acetylcholine Receptors Is Mediated by β2 Functionally Important Residues.

Guangxi University
5
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.

Cullgen (Shanghai)
28
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ-Lyase.

Shanghai Jiao Tong University
36
Exploration of Alternative Scaffolds for P2Y

National Institute of Diabetes and Digestive and Kidney Diseases
8
P2Y

Saint Louis University School of Medicine
7
Selenium bioisosteric replacement of adenosine derivatives promoting adiponectin secretion increases the binding affinity to peroxisome proliferator-activated receptor δ.

Seoul National University
1
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.

Sichuan University and Collaborative Innovation Center of Biotherapy
84
Discovery and optimization of a series of imidazo[4,5-b]pyrazine derivatives as highly potent and exquisitely selective inhibitors of the mesenchymal-epithelial transition factor (c-Met) protein kinase.

Shanghai Pharmaceuticals Holding
12
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.

Zhejiang University
32
Discovery of Potent, Selective, and Direct Acid Sphingomyelinase Inhibitors with Antidepressant Activity.

China Pharmaceutical University
31
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.

Zhejiang University
14
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.

Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
23
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.

Hutchison Medipharma
7
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells.

The First Affiliated Hospital of Dalian Medical University
4
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.

Sichuan University and Collaborative Innovation Center For Biotherapy
31
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.

Zhejiang University
2
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.

Northwest University
22
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.

Shanghai Pharmaceuticals Holding
15
Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist.

Hainan University
22
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.

Wuxi Apptec (Shanghai)
44
Structure-Guided Modification of Heterocyclic Antagonists of the P2Y

National Institute of Diabetes and Digestive and Kidney Diseases
30
Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy.

Rigel Pharmaceuticals
15
Polypharmacology of N

Sahmyook University
23
Amido-substituted heterocyclic compounds and methods of use thereof for the treatment of herpes viruses

Merck Sharp & Dohme
216
TRIAZOLO WRN INHIBITORS

Nimbus Wadjet
32
COMPOUND-LINKER CONSTRUCTS COMPRISING NOVEL COMPOUNDS USEFUL AS STING AGONISTS AND USES THEREOF

Jacobio Pharmaceuticals
10
PHOSPHONATES AS INHIBITORS OF ENPP1 AND CDNP

Stingray Therapeutics
34
3-HYDROXY-5-(ISOXAZOL-5-YL) PYRIDINE FORMYLGLYCINE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE

China Pharmaceutical University
53
HETEROAROMATIC COMPOUNDS

AstraZeneca
10
LRRK2 inhibiting compounds and use thereof for treating neurodegenerative diseases

Consejo Superior De Investigaciones Cientificas
82
MK2 inhibitors and uses thereof

Xinthera
6
Substituted piperazines as BTK inhibitors

Hutchison Medipharma
4
Heterocyclic compounds as immunomodulators

Incyte
22
Phosphonate linkers and their use to facilitate cellular retention of compounds

Merck Sharp & Dohme
41
Small molecule activators of Parkin enzyme function

Mayo Foundation For Medical Education and Research
106
Galactoside inhibitor of galectins

Galecto Biotech
33
Apoptosis signal-regulating kinase 1 (ASK 1) inhibitor compounds

Pharmakea
34
Alpha-truxillic acid derivatives and pharmaceutical compositions thereof

The State University of New York
143
5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereof

Samumed
119
Heterocyclic inhibitors of ATR kinase

University Of Texas
2
Matrix metalloproteinase inhibitors and methods for the treatment of pain and other diseases

TBA
67
Tricyclic pyrrolopyridine compound, and JAK inhibitor

Nissan Chemical Industries
40
Protein kinase inhibitors

Orion
4
6-substituted demethyl-estradiol derivatives as selective ER-β agonists

Endece
14
Piperidine compound or salt thereof

Taiho Pharmaceutical
4
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.

Genentech
117
Triazolyl PDE10 inhibitors

Merck Sharp & Dohme
16
Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.

Birla Institute of Technology
118
Compounds and compositions for the inhibition of NAMPT

Forma Tm
26
Synthesis, Biological Evaluation, and Docking of Dihydropyrazole Sulfonamide Containing 2-hydroxyphenyl Moiety: A Series of Novel MMP-2 Inhibitors.

Nanjing University
181
Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use

Boehringer Ingelheim International
8
Targeting NAD biosynthesis in bacterial pathogens

University of Maryland, Baltimore
10
8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions

Boehringer Ingelheim International
2
Methyl Yellow: A Potential Drug Scaffold for Parkinson's Disease.

Northeast Ohio Medial University
24
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.

State University of New York
10
Synthetic modification of prostaglandin f(2alpha) indicates different structural determinants for binding to the prostaglandin F receptor versus the prostaglandin transporter.

Albert Einstein College of Medicine
6
A new series of S-adenosyl-L-methionine synthetase inhibitors.

Laboratoire De Chimie Bioorganique
27
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.

Glaxo Wellcome Research and Development
17
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.

Neurogen
1
Inhibition of human caspases by peptide-based and macromolecular inhibitors.

Merck Research Laboratories