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153 articles for J Yu


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Cmpds
Data
Article Title
Organization
24
NEBI
Seoul National University
4
Identification of novel estrogen receptor (ER) agonists that have additional and complementary anti-cancer activities via ER-independent mechanism.EBI
Kyung Hee University
8
4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies.EBI
Peking University Health Science Center
12
Design, synthesis, and pharmacological characterization of novel endomorphin-1 analogues as extremely potentµ-opioid agonists.EBI
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.EBI
Duquesne University
26
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.EBI
AstraZeneca
16
A new class of highly potent and selective endomorphin-1 analogues containinga-methylene-ß-aminopropanoic acids (map).EBI
Lanzhou University
28
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11 -Hydroxysteroid Dehydrogenase Type 1 Inhibitors.EBI
TBA
7
Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease.EBI
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.EBI
Seoul National University
28
Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
3
Curcumin is a potent DNA hypomethylation agent.EBI
The Ohio State University
28
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.EBI
Merck Research Laboratories
21
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.EBI
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.EBI
Duquesne University
9
Development of potent non-carbohydrate imidazole-based small molecule selectin inhibitors with antiinflammatory activity.EBI
Ontogen
9
Design, synthesis, and X-ray crystal structure of a potent dual inhibitor of thymidylate synthase and dihydrofolate reductase as an antitumor agent.EBI
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.EBI
Neurocrine Biosciences
12
Potent and novel 11ß-HSD1 inhibitors identified from shape and docking based virtual screening.EBI
Shanghai Pharmaceutical Holding
5
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.EBI
Neurocrine Biosciences
3
Selectivea-glucosidase substrates and inhibitors containing short aromatic peptidyl moieties.EBI
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.EBI
Neurocrine Biosciences
27
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
15
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.EBI
Institute of Science & Technology
25
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI
Neurocrine Biosciences
8
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI
Neurocrine Biosciences
37
Design, synthesis, and structure-affinity relationships of novel series of sialosides as CD22-specific inhibitors.EBI
Gifu University
21
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.EBI
Duquesne University
22
Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.EBI
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.EBI
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.EBI
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.EBI
Zhejiang University
3
New anti-ovarian cancer quinolone derivatives acting by modulating microRNA processing machinery.EBI
University of Perugia
5
Scaffold hopping-driven optimization for the identification of NLRP3 inhibitors as potential gout therapeutics.EBI
Peking University
36
Discovery of an Orally Bioavailable STING Inhibitor with In Vivo Anti-Inflammatory Activity in Mice with STING-Mediated Inflammation.EBI
China Pharmaceutical University
4
Hit to lead optimization of the 4-trifluoromethylquinoline derivatives as novel SGK1 inhibitors with potent anti-prostate cancer activity.EBI
Guizhou Medical University
24
Design, Synthesis, and biological evaluation of 7H-Pyrrolo[2,3-d]pyrimidines as potent HPK1 kinase inhibitors.EBI
University of Chinese Academy of Sciences
5
PRMT7 in cancer: Structure, effects, and therapeutic potentials.EBI
Ningbo University
8
Discovery of a Novel Macrocyclic Noncovalent CDK7 Inhibitor for Cancer Therapy.EBI
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.EBI
Chengdu Institute of Biology
4
Modulating Phosphorylation by Proximity-Inducing Modalities for Cancer Therapy.EBI
China Pharmaceutical University
8
Structure-based virtual screening discovers novel PKMYT1 inhibitors.EBI
Shenyang Pharmaceutical University
1
Design, synthesis, and biological evaluation of a series of new anthraquinone derivatives as anti-ZIKV agents.EBI
Sun Yat-sen University
36
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.EBI
Shanghai Institute of Materia Medica
14
Advances in dual-targeting inhibitors of HDAC6 for cancer treatment.EBI
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.EBI
China Pharmaceutical University
5
Rational design of small-sized peptidomimetic inhibitors disrupting protein-protein interaction.EBI
Ningxia Medical University
3
Allosteric Activation of Protein Phosphatase 5 with Small Molecules.EBI
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.EBI
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.EBI
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.EBI
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.EBI
Hangzhou Medical College
14
Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal EBI
Rigel Pharmaceuticals
36
Transformation of a Dopamine DEBI
Shanghaitech University
24
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of Cancer.EBI
Insilico Medicine Shanghai
21
Discovery of Novel EBI
China Pharmaceutical University
4
Novel Strategy To Inhibit Transthyretin Amyloidosis via the Synergetic Effect of Chemoselective Acylation and Noncovalent Inhibitor Release.EBI
Chungnam National University
22
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual AEBI
Seoul National University
21
Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis.EBI
Shanghai Institute of Materia Medica
38
Discovery of a potent and selective allosteric inhibitor targeting the SHP2 tunnel site for RTK-driven cancer treatment.EBI
Hangzhou Medical College
8
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.EBI
Zhejiang University
7
Scaffold hopping derived novel benzoxazepinone RIPK1 inhibitors as anti-necroptosis agents.EBI
Ningxia Medical University
44
Discovery of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.EBI
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.EBI
Ningxia Medical University
7
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.EBI
Guangxi University
29
Structure-Based Design of the Indole-Substituted Triazolopyrimidines as New EED-H3K27me3 Inhibitors for the Treatment of Lymphoma.EBI
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.EBI
Guangzhou Institutes of Biomedicine and Health
8
Pan- and isoform-specific inhibition of Hsp90: Design strategy and recent advances.EBI
Shandong University
13
Interaction of AEBI
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.EBI
Southern Medical University Biomedical Research Center
8
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors.EBI
Ningxia Medical University
9
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.EBI
Chinese Academy of Sciences
9
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.EBI
Shenyang Pharmaceutical University
1
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the AEBI
University of Southern California
17
Novel difluoromethyl-containing 1-((4-methoxy-3-(piperazin-1-yl)phenyl)sulfonyl)-1H-indole scaffold as potent 5-HTEBI
Hec Pharm Group
20
Novel difluoromethylated 1-(phenylsulfonyl)-4-(piperazin-1-yl)-1H-indole derivatives as potent 5-HTEBI
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.EBI
Dalian Medical University
8
Discovery of a Trifluoromethoxy Cyclopentanone Benzothiazole Receptor-Interacting Protein Kinase 1 Inhibitor as the Treatment for Alzheimer's Disease.EBI
China Pharmaceutical University
19
Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human α7 Nicotinic Acetylcholine Receptors.EBI
Hainan University
22
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.EBI
Neurocrine Biosciences
2
Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.EBI
University of South Florida
51
2-Phenylcyclopropylmethylamine Derivatives as Dopamine DEBI
Shanghaitech University
45
Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous EBI
Agios Pharmaceuticals
24
Structure-based molecular hybridization design of Keap1-Nrf2 inhibitors as novel protective agents of acute lung injury.EBI
Ningxia Medical University
7
Enantiomeric profiling of a chiral benzothiazole necroptosis inhibitor.EBI
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.EBI
Shanghai Pharmaceuticals Holding
29
Small Molecule Approaches for Targeting the Polycomb Repressive Complex 2 (PRC2) in Cancer.EBI
Northwestern University
2
An in silico mechanistic insight into HDAC8 activation facilitates the discovery of new small-molecule activators.EBI
Shandong University
23
Design, synthesis, and biological evaluation of 1,3,6,7-tetrahydroxyxanthone derivatives as phosphoglycerate mutase 1 inhibitors.EBI
China Pharmaceutical University
15
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.EBI
Seoul National University
17
High Selectivity of an α-Conotoxin LvIA Analogue for α3β2 Nicotinic Acetylcholine Receptors Is Mediated by β2 Functionally Important Residues.EBI
Guangxi University
5
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.EBI
Cullgen (Shanghai)
28
Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ-Lyase.EBI
Shanghai Jiao Tong University
36
Exploration of Alternative Scaffolds for P2YEBI
National Institute of Diabetes and Digestive and Kidney Diseases
8
P2YEBI
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.EBI
Seoul National University
1
Development of selective mono or dual PROTAC degrader probe of CDK isoforms.EBI
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.EBI
Shanghai Pharmaceuticals Holding
12
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.EBI
Zhejiang University
32
Discovery of Potent, Selective, and Direct Acid Sphingomyelinase Inhibitors with Antidepressant Activity.EBI
China Pharmaceutical University
31
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.EBI
Zhejiang University
14
Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade.EBI
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
23
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.EBI
Hutchison Medipharma
7
Structure-based modification of carbonyl-diphenylpyrimidines (Car-DPPYs) as a novel focal adhesion kinase (FAK) inhibitor against various stubborn cancer cells.EBI
The First Affiliated Hospital of Dalian Medical University
4
Discovery and biological evaluation of novel androgen receptor antagonist for castration-resistant prostate cancer.EBI
Sichuan University and Collaborative Innovation Center For Biotherapy
31
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.EBI
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.EBI
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.EBI
Shanghai Pharmaceuticals Holding
15
Single Amino Acid Substitution in α-Conotoxin TxID Reveals a Specific α3β4 Nicotinic Acetylcholine Receptor Antagonist.EBI
Hainan University
22
Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.EBI
Wuxi Apptec (Shanghai)
44
Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI
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.EBI
Rigel Pharmaceuticals
15
Polypharmacology of NEBI
Sahmyook University
23
Amido-substituted heterocyclic compounds and methods of use thereof for the treatment of herpes virusesBDB
Merck Sharp & Dohme
216
TRIAZOLO WRN INHIBITORSBDB
Nimbus Wadjet
32
COMPOUND-LINKER CONSTRUCTS COMPRISING NOVEL COMPOUNDS USEFUL AS STING AGONISTS AND USES THEREOFBDB
Jacobio Pharmaceuticals
10
PHOSPHONATES AS INHIBITORS OF ENPP1 AND CDNPBDB
Stingray Therapeutics
34
3-HYDROXY-5-(ISOXAZOL-5-YL) PYRIDINE FORMYLGLYCINE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USEBDB
China Pharmaceutical University
53
HETEROAROMATIC COMPOUNDSBDB
AstraZeneca
10
LRRK2 inhibiting compounds and use thereof for treating neurodegenerative diseasesBDB
Consejo Superior De Investigaciones Cientificas
82
MK2 inhibitors and uses thereofBDB
Xinthera
6
Substituted piperazines as BTK inhibitorsBDB
Hutchison Medipharma
4
Heterocyclic compounds as immunomodulatorsBDB
Incyte
22
Phosphonate linkers and their use to facilitate cellular retention of compoundsBDB
Merck Sharp & Dohme
41
Small molecule activators of Parkin enzyme functionBDB
Mayo Foundation For Medical Education and Research
106
Galactoside inhibitor of galectinsBDB
Galecto Biotech
33
Apoptosis signal-regulating kinase 1 (ASK 1) inhibitor compoundsBDB
Pharmakea
34
Alpha-truxillic acid derivatives and pharmaceutical compositions thereofBDB
The State University of New York
143
5-heteroaryl substituted indazole-3-carboxamides and preparation and use thereofBDB
Samumed
119
Heterocyclic inhibitors of ATR kinaseBDB
University Of Texas
2
Matrix metalloproteinase inhibitors and methods for the treatment of pain and other diseasesBDB
TBA
67
Tricyclic pyrrolopyridine compound, and JAK inhibitorBDB
Nissan Chemical Industries
40
Protein kinase inhibitorsBDB
Orion
4
6-substituted demethyl-estradiol derivatives as selective ER-β agonistsBDB
Endece
14
Piperidine compound or salt thereofBDB
Taiho Pharmaceutical
4
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells.BDB
Genentech
117
Triazolyl PDE10 inhibitorsBDB
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.BDB
Birla Institute of Technology
118
Compounds and compositions for the inhibition of NAMPTBDB
Forma Tm
26
Synthesis, Biological Evaluation, and Docking of Dihydropyrazole Sulfonamide Containing 2-hydroxyphenyl Moiety: A Series of Novel MMP-2 Inhibitors.BDB
Nanjing University
181
Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their useBDB
Boehringer Ingelheim International
8
Targeting NAD biosynthesis in bacterial pathogensBDB
University of Maryland, Baltimore
10
8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositionsBDB
Boehringer Ingelheim International
2
Methyl Yellow: A Potential Drug Scaffold for Parkinson's Disease.BDB
Northeast Ohio Medial University
24
Pharmacology of delta2 glutamate receptors: effects of pentamidine and protons.BDB
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.BDB
Albert Einstein College of Medicine
6
A new series of S-adenosyl-L-methionine synthetase inhibitors.BDB
Laboratoire De Chimie Bioorganique
27
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.BDB
Glaxo Wellcome Research and Development
17
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.BDB
Neurogen
1
Inhibition of human caspases by peptide-based and macromolecular inhibitors.BDB
Merck Research Laboratories