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141 articles for thisTarget


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

PMID
Data
Article Title
Organization
Development of 4,5-dihydro-benzodiazepinone derivatives as a new chemical series of BRD4 inhibitors.EBI
Zhejiang University
6-Oxooxazolidine-quinazolines as noncovalent inhibitors with the potential to target mutant forms of EGFR.EBI
Zhejiang University
Design, synthesis and biological evaluation of pyrazol-furan carboxamide analogues as novel Akt kinase inhibitors.EBI
Zhejiang University
Synthesis and biological evaluation of 3-([1,2,4]triazolo[4,3-a]pyridin-3-yl)-4-(indol-3-yl)-maleimides as potent, selective GSK-3ß inhibitors and neuroprotective agents.EBI
Zhejiang University
Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.EBI
Zhejiang University
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.EBI
Zhejiang University
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.EBI
Zhejiang University
Synthesis and biological evaluations of novel endomorphin analogues containinga-hydroxy-ß-phenylalanine (AHPBA) displaying mixedµ/d opioid receptor agonist andd opioid receptor antagonist activities.EBI
Zhejiang University
Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold.EBI
Zhejiang University
Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.EBI
Zhejiang University
Design, synthesis and biological evaluation of thienopyridinones as Chk1 inhibitors.EBI
Zhejiang University
Design, synthesis and biological evaluation of 6-(nitroimidazole-1H-alkyloxyl)-4-anilinoquinazolines as efficient EGFR inhibitors exerting cytotoxic effects both under normoxia and hypoxia.EBI
Zhejiang University
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI
Zhejiang University
Biotransformation of huperzine A by a fungal endophyte of Huperzia serrata furnished sesquiterpenoid-alkaloid hybrids.EBI
Zhejiang University
Design, synthesis and biological evaluation of novel tripeptidyl epoxyketone derivatives constructed fromß-amino acid as proteasome inhibitors.EBI
Zhejiang University
Discovery of novel inhibitors targeting the macrophage migration inhibitory factor via structure-based virtual screening and bioassays.EBI
Zhejiang University
Integrating docking scores, interaction profiles and molecular descriptors to improve the accuracy of molecular docking: toward the discovery of novel Akt1 inhibitors.EBI
Zhejiang University
Structure-based design, synthesis and biological evaluation of diphenylmethylamine derivatives as novel Akt1 inhibitors.EBI
Zhejiang University
Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors.EBI
Zhejiang University
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3ß (GSK-3ß) inhibitors.EBI
Zhejiang University
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.EBI
Zhejiang University
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.EBI
Zhejiang University
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinasea (PI3Ka) inhibitors.EBI
Zhejiang University
Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities.EBI
Zhejiang University
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.EBI
Zhejiang University
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.EBI
Zhejiang University
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.EBI
Zhejiang University
3D-QSAR studies on 4-hydroxyphenylpyruvate dioxygenase inhibitors by comparative molecular field analysis (CoMFA).EBI
Zhejiang University
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.EBI
Zhejiang University
Investigation of the diastereomerism of dihydrobenzoxathiin SERMs for ER alpha by molecular modeling.EBI
Zhejiang University
Pharmacophore identification, virtual screening and biological evaluation of prenylated flavonoids derivatives as PKB/Akt1 inhibitors.EBI
Zhejiang University
Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents.EBI
Zhejiang University
Synthesis and biological evaluation of novel 2-arylamino-3-(arylsulfonyl)quinoxalines as PI3Ka inhibitors.EBI
Zhejiang University
Angiotensin-I-converting enzyme inhibitory peptides: Chemical feature based pharmacophore generation.EBI
Zhejiang University
'Click' assembly of selective inhibitors for MAO-A.EBI
Zhejiang University
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.EBI
Zhejiang University
Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.EBI
Zhejiang University
QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine.EBI
Zhejiang University
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.EBI
Zhejiang University
Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.EBI
Zhejiang University
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.EBI
Zhejiang University
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.EBI
Zhejiang University
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.EBI
Zhejiang University
Complex sesquiterpenoids with tyrosinase inhibitory activity from the leaves of Chloranthus tianmushanensis.EBI
Zhejiang University
2,3-Disubstituted 8-arylamino-3H-imidazo[4,5-g]quinazolines: a novel class of antitumor agents.EBI
Zhejiang University
Design, Synthesis, and Biological Evaluation of an Orally Bioavailable, Potent, and Selective ROCK2 Inhibitor for Psoriasis Treatment.EBI
Zhejiang University
Design, synthesis and biological evaluation of 2-aminopyrimidine derivatives as potent FLT3 inhibitors.EBI
Zhejiang University
Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit.EBI
Zhejiang University
Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis.EBI
Zhejiang University
Novel Benzo Five-Membered Heterocycle Derivatives as P-Glycoprotein Inhibitors: Design, Synthesis, Molecular Docking, and Anti-Multidrug Resistance Activity.EBI
Zhejiang University
Scaffold Hybrid of the Natural Product Tanshinone I with Piperidine for the Discovery of a Potent NLRP3 Inflammasome Inhibitor.EBI
Zhejiang University
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.EBI
Zhejiang University
Insight from Linker Investigations: Discovery of a Novel Phenylbenzothiazole Necroptosis Inhibitor Targeting Receptor-Interacting Protein Kinase 1 (RIPK1) from a Phenoxybenzothiazole Compound with Dual RIPK1/3 Targeting Activity.EBI
Zhejiang University
Discovery of Novel Oxazepine Derivatives as Akt/ROCK Inhibitors for Growth Arrest and Differentiation Induction in Neuroblastoma Treatment.EBI
Zhejiang University
Discovery of Highly Selective and Orally Bioavailable PI3Kδ Inhibitors with Anti-Inflammatory Activity for Treatment of Acute Lung Injury.EBI
Zhejiang University
Design, Synthesis, and Antitumor Activity Evaluation of 2-Arylmethoxy-4-(2,2'-dihalogen-substituted biphenyl-3-ylmethoxy) Benzylamine Derivatives as Potent PD-1/PD-L1 Inhibitors.EBI
Zhejiang University
PepScaf: Harnessing Machine Learning with In Vitro Selection toward De Novo Macrocyclic Peptides against IL-17C/IL-17RE Interaction.EBI
Zhejiang University
Diselenide Covalent Allosteric Inhibitors of Glutaminase with Strong EBI
Zhejiang University
Discovery of novel non-nucleoside inhibitors with high potency and selectivity for DNA methyltransferase 3A.EBI
Zhejiang University
Exploring gabosine and chlorogentisyl alcohol derivatives from a marine-derived fungus as EcGUS inhibitors with informatic assisted approaches.EBI
Zhejiang University
Discovery of Novel 1,2,3,4-Tetrahydrobenzofuro[2,3-EBI
Zhejiang University
Carbohydrate Strengthens the Immunotherapeutic Effect of Small-Molecule PD-L1 Inhibitors.EBI
Zhejiang University
Structure-guided design of novel HEPT analogs with enhanced potency and safety: From Isopropyl-HEPTs to Cyclopropyl-HEPTs.EBI
Zhejiang University
Recent advances in the development of EGFR degraders: PROTACs and LYTACs.EBI
Zhejiang University
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.EBI
Zhejiang University
Current advances in Vibrio harveyi quorum sensing as drug discovery targets.EBI
Zhejiang University
Discovery of pyrido[4,3-d]pyrimidinone derivatives as novel Wee1 inhibitors.EBI
Zhejiang University
Discovery of 4-oxo-4,5-dihydropyrazolo[1,5-a]quinoxaline-7-carboxamide derivatives as PI3Kα inhibitors via virtual screening and docking-based structure optimization.EBI
Zhejiang University
Synthesis and Anti-Inflammatory Activity of the Natural Cyclooxygenase-2 Inhibitor Axinelline A and Its Analogues.EBI
Zhejiang University
If small molecules immunotherapy comes, can the prime be far behind?EBI
Zhejiang University
Discovery and Optimization of EBI
Zhejiang University
Therapeutic potential of targeting SHP2 in human developmental disorders and cancers.EBI
Zhejiang University
Celastrol: Progresses in structure-modifications, structure-activity relationships, pharmacology and toxicology.EBI
Zhejiang University
Recent developments of small molecules with anti-inflammatory activities for the treatment of acute lung injury.EBI
Zhejiang University
Discovery of natural anti-inflammatory alkaloids: Potential leads for the drug discovery for the treatment of inflammation.EBI
Zhejiang University
Synthesis of Novel Kidney-Type Glutaminase Allosteric Inhibitors Targeting the Critical Lys-320 Residue.EBI
Zhejiang University
Design, synthesis, and evaluation of pyrido.[3,4-b]pyrazin-2(1H)-one derivatives as potent FLT3 inhibitors.EBI
Zhejiang University
Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.EBI
Zhejiang University
Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma.EBI
Zhejiang University
: A Prolific Source of Bioactive Secondary Metabolites with Therapeutic Potential.EBI
Zhejiang University
Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton's Tyrosine Kinase for the Treatment of Lymphoma.EBI
Zhejiang University
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.EBI
Zhejiang University
Discovery of novel non-steroidal selective glucocorticoid receptor modulators by structure- and IGN-based virtual screening, structural optimization, and biological evaluation.EBI
Zhejiang University
Protein Lysine Methyltransferase SMYD2: A Promising Small Molecule Target for Cancer Therapy.EBI
Zhejiang University
An overview on Estrogen receptors signaling and its ligands in breast cancer.EBI
Zhejiang University
Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents.EBI
Zhejiang University
Discovery of 2-(1-(3-Chloro-4-cyanophenyl)-1EBI
Zhejiang University
Recent advance of peptide-based molecules and nonpeptidic small-molecules modulating PD-1/PD-L1 protein-protein interaction or targeting PD-L1 protein degradation.EBI
Zhejiang University
Discovery of a Novel Androgen Receptor Antagonist Manifesting Evidence to Disrupt the Dimerization of the Ligand-Binding Domain via Attenuating the Hydrogen-Bonding Network Between the Two Monomers.EBI
Zhejiang University
Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT.EBI
Zhejiang University
Discovery of EBI
Zhejiang University
Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor.EBI
Zhejiang University
Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury.EBI
Zhejiang University
Development of peptide epoxyketones as selective immunoproteasome inhibitors.EBI
Zhejiang University
Design, synthesis and biological evaluation of quinazoline derivatives as potent and selective FGFR4 inhibitors.EBI
Zhejiang University
Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile.EBI
Zhejiang University
Discovery of EBI
Zhejiang University
Discovery of phenyl-linked symmetric small molecules as inhibitors of the programmed cell death-1/programmed cell death-ligand 1 interaction.EBI
Zhejiang University
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.EBI
Zhejiang University
Design, synthesis and biological evaluation of 2-styryl-5-hydroxy-4-pyrone derivatives and analogues as multiple functional agents with the potential for the treatment of Alzheimer's disease.EBI
Zhejiang University
Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable HEBI
Zhejiang University
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFREBI
Zhejiang University
Discovery of 2-(5-(quinolin-6-yl)-1,3,4-oxadiazol-2-yl)acetamide derivatives as novel PI3Kα inhibitors via docking-based virtual screening.EBI
Zhejiang University
Discovery of 1,5-Dihydro-4EBI
Zhejiang University
Hydroxypyridinone-Based Iron Chelators with Broad-Ranging Biological Activities.EBI
Zhejiang University
Novel androgen receptor antagonist identified by structure-based virtual screening, structural optimization, and biological evaluation.EBI
Zhejiang University
Identification, Structure-Activity Relationships of Marine-Derived Indolocarbazoles, and a Dual PKCθ/δ Inhibitor with Potent Antipancreatic Cancer Efficacy.EBI
Zhejiang University
Design, synthesis and biological evaluation of 2-methyl-(1,1'-biphenyl)-pyrimidine conjugates.EBI
Zhejiang University
Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.EBI
Zhejiang University
Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.EBI
Zhejiang University
Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants.EBI
Zhejiang University
Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies.EBI
Zhejiang University
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.EBI
Zhejiang University
CN128: A New Orally Active Hydroxypyridinone Iron Chelator.EBI
Zhejiang University
Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK).EBI
Zhejiang University
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.EBI
Zhejiang University
Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors.EBI
Zhejiang University
Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity.EBI
Zhejiang University
Design, synthesis and biological evaluation of hydroxypyridinone-coumarin hybrids as multimodal monoamine oxidase B inhibitors and iron chelates against Alzheimer's disease.EBI
Zhejiang University
Design and synthesis of biotinylated Hexylselen as a probe to identify KGA allosteric inhibitors by a convenient biomolecular interaction assay.EBI
Zhejiang University
Synthesis and biological evaluation of 3-aryl-4-indolyl-maleimides as potent mutant isocitrate dehydrogenase-1 inhibitors.EBI
Zhejiang University
Design, synthesis, and biological evaluation of novel phenol ether derivatives as non-covalent proteasome inhibitors.EBI
Zhejiang University
Discovery of small-molecule candidates against inflammatory bowel disease.EBI
Zhejiang University
Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation.EBI
Zhejiang University
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.EBI
Zhejiang University
Design and synthesis of novel 3-substituted-indole derivatives as selective H3 receptor antagonists and potent free radical scavengers.EBI
Zhejiang University
Structure-based drug design using GPCR homology modeling: toward the discovery of novel selective CysLT2 antagonists.EBI
Zhejiang University
Molecular cloning and pharmacological characterisation of a tyramine receptor from the rice stem borer, Chilo suppressalis (Walker).EBI
Zhejiang University
Dibenzocyclooctadiene lignans: a class of novel inhibitors of multidrug resistance-associated protein 1.EBI
Zhejiang University
Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines.EBI
Zhejiang University
3D QSAR studies on GSK-3 inhibition by aloisines.EBI
Zhejiang University
Resveratrol-maltol hybrids as multi-target-directed agents for Alzheimer's disease.EBI
Zhejiang University
Bioactive Indolocarbazoles from the Marine-Derived Streptomyces sp. DT-A61.EBI
Zhejiang University
Medermycin-Type Naphthoquinones from the Marine-Derived Streptomyces sp. XMA39.EBI
Zhejiang University
Synthesis, Evaluation, and Structure-Activity Relationship Study of Lanosterol Derivatives To Reverse Mutant-Crystallin-Induced Protein Aggregation.EBI
Zhejiang University
Cyclizidine-Type Alkaloids from Streptomyces sp. HNA39.EBI
Zhejiang University
High-Affinity Peptidomimetic Inhibitors of the DCN1-UBC12 Protein-Protein Interaction.EBI
Zhejiang University
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies.EBI
Zhejiang University
Development of Quinazoline/Pyrimidine-2,4(1EBI
Zhejiang University
Constrained dansyl derivatives reveal bacterial specificity of highly conserved thymidylate synthases.BDB
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