482 articles for thisTarget
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Article Title
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Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors.
Univ. Lille
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Novartis Institutes For Biomedical Research
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
University of Oxford
Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis.
Hoffmann-La Roche
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Pfizer
Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Kyowa Hakko Kogyo
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-
TBA
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation
TBA
Phenylamino-pyrimidine (PAP) — derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors
TBA
Competitive Kinase Enrichment Proteomics Reveals that Abemaciclib Inhibits GSK3β and Activates WNT Signaling.
University of North Carolina at Chapel Hill
Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Center for Lymphoid Malignancies
Small molecule inhibitor screen identifies synergistic activity of the bromodomain inhibitor CPI203 and bortezomib in drug resistant myeloma.
Knight Cancer Institute
Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor.
Westfalian Wilhelms University Muenster (WWU)
Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia.
S*BIO Pte Ltd.
Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.
Bayer HealthCare AG
Selective Itk inhibitors block T-cell activation and murine lung inflammation.
Bristol-Myers Squibb Pharmaceutical Research Institute
In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine).
Cyclacel, Ltd.
A homogeneous bioluminescent immunoassay to probe cellular signaling pathway regulation.
Promega Corporation
Limitations of current in vitro models for testing the clinical potential of epigenetic inhibitors for treatment of pediatric ependymoma.
University of Nottingham
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494).
AbbVie Bioresearch Center
A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.
Johns Hopkins University
PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.
Pfizer
Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase.
University of Dundee
Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.
Nerviano Medical Sciences
GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models.
GlaxoSmithKline
CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients.
Mayo Clinic
The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
ARIAD Pharmaceuticals, Inc.
Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor.
University of Tubingen
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
University of Cambridge
Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.
Wyeth Research
Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
Bayer AG
Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine.
Eli Lilly and Company
Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Galapagos NV
Human target validation of phosphoinositide 3-kinase (PI3K)β: effects on platelets and insulin sensitivity, using AZD6482 a novel PI3Kβ inhibitor.
AstraZeneca
NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.
Nerviano Medical Sciences Srl
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.
Genentech, Inc and Exelixis
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.
Tufts Medical Center
Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth.
Pfizer
A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation.
Pfizer
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Bristol-Myers Squibb
Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C-induced HIV latency reversal.
Tokyo Medical and Dental University
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
Bayer AG
The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice.
Astellas Pharma Inc.
Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor.
Pfizer
Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor.
OSI Pharmaceuticals, Inc.
Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
The Scripps Research Institute
Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor, CP-690,550, in rat adjuvant-induced arthritis.
Pfizer
PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Harvard Medical School
BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Boehringer Ingelheim Austria GmbH
In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1.
GlaxoSmithKline R & D
Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
Wyeth Research
Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4.
Novartis Pharma
Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.
GlaxoSmithKline
HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity.
University of Groningen
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
The Institute of Cancer Research
Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.
Bayer HealthCare AG
Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1.
GlaxoSmithKline
SNS-032 is a potent and selective CDK 2, 7 and 9 inhibitor that drives target modulation in patient samples.
Sunesis Pharmaceuticals Inc
In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase.
Novartis Institutes for BioMedical Research
CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer.
Ann Arbor Laboratories
Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model.
University of California Irvine (UCI)
NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family.
Johann Wolfgang Goethe University
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
AbbVie
Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain.
New York University Medical Center
Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Daiichi Sankyo Co., Ltd
Structural modification of tanshinone IIA and their α-glucosidase inhibitory activity.
Chulalongkorn University
Synthesis, biological evaluation and action mechanism of 7H-[1,2,4] triazolo [3,4-b] [1,3,4] thiadiazine-phenylhydrazone derivatives as α-glucosidase inhibitors.
The Affiliated Hospital of Guizhou Medical University
Design, synthesis, and biological evaluation of novel 4,4'-bipyridine derivatives acting as CDK9-Cyclin T1 protein-protein interaction inhibitors against triple-negative breast cancer.
Xiamen University
Synthesis and application of small molecules approved for the treatment of lymphoma.
The First Affiliated Hospital of Zhengzhou University
Inhibition of Son of Sevenless Homologue 1 (SOS1): Promising therapeutic treatment for KRAS-mutant cancers.
China Pharmaceutical University
Galantamine-memantine hybrids for Alzheimer's disease: The influence of linker rigidity in biological activity and pharmacokinetic properties.
Alma Mater Studiorum - University of Bologna
Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety.
Kazan (Volga region) Federal University
Identification of 1,3,4-oxadiazolyl-containing β-carboline derivatives as novel α-glucosidase inhibitors with antidiabetic activity.
Wuyi University
Hydrophobicity modulation via the substituents at positions 2 and 4 of 1,3,5-triazine to enhance therapeutic ability against Alzheimer's disease for potent serotonin 5-HT6R agents.
Jagiellonian University
A review: FDA-approved fluorine-containing small molecules from 2015 to 2022.
Iran University of Medical Sciences
Micafungin: A promising inhibitor of UBE2M in cancer cell growth suppression.
Zhengzhou University
Design and optimization of selective and potent CDK9 inhibitors with flavonoid scaffold for the treatment of acute myeloid leukemia.
China Pharmaceutical University
Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways.
Tianjin University of Science & Technology
An overview of phosphodiesterase 9 inhibitors: Insights from skeletal structure, pharmacophores, and therapeutic potential.
Southern Medical University
Design, synthesis, and evaluation of dual EGFR/AURKB inhibitors as anticancer agents for non-small cell lung cancer.
Ferris State University
Discovery of potent pyrrolo-pyrimidine and purine HDAC inhibitors for the treatment of advanced prostate cancer.
University of Modena and Reggio Emilia
Targeting autophagy with small-molecule activators for potential therapeutic purposes.
Sichuan University
A review of progress in o-aminobenzamide-based HDAC inhibitors with dual targeting capabilities for cancer therapy.
Zhengzhou University
Are inhibitors of histone deacetylase 8 (HDAC8) effective in hematological cancers especially acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL)?
Jadavpur University
Synthesis and evaluation of dihydrofuro[2,3-b]pyridine derivatives as potent IRAK4 inhibitors.
Soochow University
Development of novel PEX5-PEX14 protein-protein interaction (PPI) inhibitors based on an oxopiperazine template.
Medical University of Warsaw
Orally bioavailable styryl derivative of rohitukine-N-oxide inhibits CDK9/T1 and the growth of pancreatic cancer cells.
CSIR-Indian Institute of Integrative Medicine
Advances in the development of phosphodiesterase 7 inhibitors.
Southern Medical University
Side Chain Investigation of Imidazopyridazine as a Hinge Binder for Targeting Actionable Mutations of RET Kinase.
Gachon University
Design, synthesis, and optimization of novel PD-L1 inhibitors and the identification of a highly potent and orally bioavailable PD-L1 inhibitor.
Chulalongkorn University
Discovery of novel N2-indazole derivatives as phosphodiesterase 4 inhibitors for the treatment of inflammatory bowel disease.
Southern Medical University
Novel carbazole-oxadiazole derivatives as anti-α-glucosidase and anti-α-amylase agents: Design, synthesis, molecular docking, and biological evaluation.
Guizhou Medical University
Quinazolines annelated at the N(3)-C(4) bond: Synthesis and biological activity.
Ural Federal University
Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potency.
Shandong University
Discovery of Benzo[d]oxazoles as Novel Dual Small-Molecule Inhibitors Targeting PD-1/PD-L1 and VISTA Pathway.
China Pharmaceutical University
An Adenosine Analogue Library Reveals Insights into Active Sites of Protein Arginine Methyltransferases and Enables the Discovery of a Selective PRMT4 Inhibitor.
Purdue University
Nicotinic Acid Derivatives As Novel Noncompetitive α-Amylase and α-Glucosidase Inhibitors for Type 2 Diabetes Treatment.
University of Milan
Virtual Screening and Molecular Docking: Discovering Novel METTL3 Inhibitors.
Hangzhou Medical College
Development of a First-in-Class DNMT1/HDAC Inhibitor with Improved Therapeutic Potential and Potentiated Antitumor Immunity.
Shandong University
Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with In Vitro and In Vivo Activity in Neurodegenerative Diseases.
Institute of General Organic Chemistry (CSIC)
Development of narrow-spectrum topoisomerase-targeting antibacterials against mycobacteria.
University of Ljubljana
Design, synthesis and biological evaluation of a new series of imidazothiazole-hydrazone hybrids as dual EGFR and Akt inhibitors for NSCLC therapy.
Anadolu University
Design, synthesis, and evaluation of antitumor activity of 2-arylmethoxy-4-(2-fluoromethyl-biphenyl-3-ylmethoxy) benzylamine derivatives as PD-1/PD-l1 inhibitors.
Zhejiang University
Discovery of bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).
Stanford University
Design, synthesis and structure-activity relationships of novel non-ketolides: 9-Oxime clarithromycin featured with seven-to thirteen-atom-length diamine linkers at 3-OH.
Beijing Institute of Technology
Synthesis and evaluation of neuroactive steroids with novel pharmacophore at C-21 let identify a compound with advantageous PK profile and higher EC50 and Emax as PAM on GABAA receptor.
Yantai University
Opportunities and perspectives of small molecular phosphodiesterase inhibitors in neurodegenerative diseases.
Qingdao University
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death.
Shandong University
Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
Jinan University
Identification of an m6A Natural Inhibitor, Lobeline, That Reverses Lenvatinib Resistance in Hepatocellular Tumors.
The First Hospital of China Medical University
Rational design of small-sized peptidomimetic inhibitors disrupting protein-protein interaction.
Ningxia Medical University
N-methylmorpholine incorporation into the structure of biphenyl leads to the bioactive inhibitor of PD-1/PD-L1 interaction.
Jagiellonian University
Synthesis, biosimulation and pharmacological evaluation of benzimidazole derivatives with antihypertensive multitarget effect.
Universidad Autonoma del Estado de Morelos
Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance.
Southwest University
Small molecules that regulate the N6-methyladenosine RNA modification as potential anti-cancer agents.
University of Connecticut
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia.
Tyra Biosciences, Inc.
Structure-Activity Relationship Studies of Substituted 2-Phenyl-1,2,4-triazine-3,5(2H,4H)-dione Analogues: Development of Potent eEF2K Degraders against Triple-Negative Breast Cancer.
Soochow University
Development of Novel Bacterial Topoisomerase Inhibitors Assisted by Computational Screening.
Ohio State University
Design, synthesis, pharmacological evaluation, and computational study of benzo[d] isothiazol-based small molecule inhibitors targeting PD-1/PD-l1 interaction.
Shenyang Pharmaceutical University
The U.S. FDA approved cardiovascular drugs from 2011 to 2023: A medicinal chemistry perspective.
Sichuan University
Design and synthesis of 6-C-alkyl-DMDP type nanomolar inhibitors of β-galactosidase and β-glucosidase based on broussonetine S and related derivatives.
Beijing National Laboratory For Molecular Sciences
Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity.
Shenyang Pharmaceutical University
Non-kinase off-target inhibitory activities of clinically-relevant kinase inhibitors.
Purdue University
Re-exploration of tetrahydro-β-carboline scaffold: Discovery of selective histone deacetylase 6 inhibitors with neurite outgrowth-promoting and neuroprotective activities.
Yangling Vocational & Technical College
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.
AstraZeneca
Genomic Discovery and Structure-Activity Exploration of a Novel Family of Enzyme-Activated Covalent Cyclin-Dependent Kinase Inhibitors.
LifeMine Therapeutics
Discovery of Oxidized p-Terphenyls as Phosphodiesterase 4 Inhibitors from Marine-Derived Fungi.
Chinese Academy of Sciences
Bioisosteric heterocyclic analogues of natural bioactive flavonoids by scaffold-hopping approaches: State-of-the-art and perspectives in medicinal chemistry.
University of Palermo
Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy.
Gwangju Institute of Science and Technology
Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer's Disease.
Shenyang Pharmaceutical University
A Comprehensive In Vitro Characterization of a New Class of Indole-Based Compounds Developed as Selective Haspin Inhibitors.
University of Salerno
Exploring the interaction of N-(benzothiazol-2-yl)pyrrolamide DNA gyrase inhibitors with the GyrB ATP-binding site lipophilic floor: A medicinal chemistry and QTAIM study.
University of Ljubljana
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor.
WuXi AppTec
Discovery of novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors.
Tianjin University
Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines.
Universite Clermont Auvergne
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.
Tango Therapeutics
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.
Tianjin University
Recent Discovery and Development of Inhibitors that Target CDK9 and Their Therapeutic Indications.
Sichuan University
Design, synthesis, and biological characterization of proteolysis targeting chimera (PROTACs) for the ataxia telangiectasia and RAD3-related (ATR) kinase.
Martin-Luther-University of Halle-Wittenberg
3,5-Disubstituted-thiazolidine-2,4-dione hybrids as antidiabetic agents: Design, synthesis, in-vitro and In vivo evaluation.
IK Gujral Punjab Technical University
Phenoxytacrine derivatives: Low-toxicity neuroprotectants exerting affinity to ifenprodil-binding site and cholinesterase inhibition.
Charles University in Prague
Technologies of targeting histone deacetylase in drug discovery: Current progress and emerging prospects.
Sichuan University
Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research.
Bristol-Myers Squibb
Dual Antagonism of α9α10 nAChR and GABAB Receptor-Coupled CaV2.2 Channels by an Analgesic αO-Conotoxin Analogue.
Ocean University of China
Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo.
East China University of Science and Technology
Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development.
Japan Tobacco
Advances in targeting Phosphodiesterase 1: From mechanisms to potential therapeutics.
Sichuan University
Discovery of triazole tethered thymol/carvacrol-coumarin hybrids as new class of α-glucosidase inhibitors with potent in vivo antihyperglycemic activities.
Guru Nanak Dev University
Synthetic approaches and application of clinically approved small-molecule drugs to treat hepatitis.
Children's Hospital Affiliated to Zhengzhou University
Lead Identification of Novel Naphthyridine Derivatives as Potent SOS1 Inhibitors.
Haihe Biopharma Co., Ltd.
Nonsymmetrically Substituted 1,1'-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction.
Jagiellonian University
Metabolomic Analysis and Antiviral Screening of a Marine Algae Library Yield Jobosic Acid (2,5-Dimethyltetradecanoic Acid) as a Selective Inhibitor of SARS-CoV-2.
University of Puerto Rico-Medical Sciences Campus
Synthesis of α3β4 Nicotinic Acetylcholine Receptor Modulators Derived from Aristoquinoline That Reduce Reinstatement of Cocaine-Seeking Behavior.
University of Illinois Chicago
Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.
Tianjin University
Dual inhibitors of HDAC and other epigenetic regulators: A novel strategy for cancer treatment.
Guru Ghasidas University
HDAC specificity and kinase off-targeting by purine-benzohydroxamate anti-hematological tumor agents.
University of Sao Paulo
Targeting protein kinases for the treatment of Alzheimer's disease: Recent progress and future perspectives.
Southwest Jiaotong University
MNK, mTOR or eIF4E-selecting the best anti-tumor target for blocking translation initiation.
Shandong University
Design, Synthesis, and Biological Evaluation of Pierardine Derivatives as Novel Brain-Penetrant and In Vivo Potent NMDAR-GluN2B Antagonists for Ischemic Stroke Treatment.
Anhui University of Chinese Medicine
Discovery of Highly Potent Small-Molecule PD-1/PD-L1 Inhibitors with a Novel Scaffold for Cancer Immunotherapy.
China Pharmaceutical University
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.
Incyte
Discovery of Novel PROTAC Degraders of p300/CBP as Potential Therapeutics for Hepatocellular Carcinoma.
Fudan University
Design, Synthesis, and Biological Evaluation for First GPX4 and CDK Dual Inhibitors.
China Pharmaceutical University
Synthesis and biological evaluation of indole derivatives containing thiazolidine-2,4-dione as α-glucosidase inhibitors with antidiabetic activity.
Wuyi University
Discovery of Novel Nonpeptidic and Noncovalent Small Molecule 3CLpro Inhibitors as anti-SARS-CoV-2 Drug Candidate.
University of Chinese Academy of Sciences
Discovery of Preclinical Candidate AD1058 as a Highly Potent, Selective, and Brain-Penetrant ATR Inhibitor for the Treatment of Advanced Malignancies.
Shanghai Institute of Materia Medica
New Class of Hsp90 C-Terminal Domain Inhibitors with Anti-tumor Properties against Triple-Negative Breast Cancer.
University of Ljubljana
Design, Synthesis, and Activity Evaluation of Novel Benzazole Bifunctional Antifungal Inhibitors with an LDH Carrier.
Liaocheng University
Preferential HDAC6 inhibitors derived from HPOB exhibit synergistic antileukemia activity in combination with decitabine.
Leipzig University
Akt Inhibitor Advancements: From Capivasertib Approval to Covalent-Allosteric Promises.
TU Dortmund University and Drug Discovery Hub Dortmund (DDHD)
Design, Synthesis, and Biological Evaluation of a Novel NIK Inhibitor with Anti-Inflammatory and Hepatoprotective Effects for Sepsis Treatment.
China Pharmaceutical University
Identification of Dihydrobenzofuran Neolignans as Novel PDE4 Inhibitors and Evaluation of Antiatopic Dermatitis Efficacy in DNCB-Induced Mice Model.
Shanghai University of Traditional Chinese Medicine
Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.
Shenyang Pharmaceutical University
The Discovery of 7-Isopropoxy-2-(1-methyl-2-oxabicyclo[2.1.1]hexan-4-yl)-N-(6-methylpyrazolo[1,5-a]pyrimidin-3-yl)imidazo[1,2-a]pyrimidine-6-carboxamide (BIO-7488), a Potent, Selective, and CNS-Penetrant IRAK4 Inhibitor for the Treatment of Ischemic Stroke.
Biogen
Discovery of Novel PD-L1 Small-Molecular Inhibitors with Potent In Vivo Anti-tumor Immune Activity.
China Pharmaceutical University
Design, Synthesis, and Structure-Activity Relationship of Novel Pyridazinone-Based PARP7/HDACs Dual Inhibitors for Elucidating the Relationship between Antitumor Immunity and HDACs Inhibition.
Hangzhou Normal University
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Merck & Co.
Dual-targeting compounds possessing enhanced anticancer activity via microtubule disruption and histone deacetylase inhibition.
National Taiwan University
Thiazole-based analogues as potential antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA) and their SAR elucidation.
Jiangxi Science & Technology Normal University
Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.
Pfizer
Design, Synthesis, and Structure-Activity Relationships of Novel Peptide Derivatives of the Severe Acute Respiratory Syndrome-Coronavirus-2 Spike-Protein that Potently Inhibit Nicotinic Acetylcholine Receptors.
University of Utah
Evaluation of novel 2-(quinoline-2-ylthio)acetamide derivatives linked to diphenyl-imidazole as α-glucosidase inhibitors: Insights from in silico, in vitro, and in vivo studies on their anti-diabetic properties.
Qom University of Technology
Current advances and development strategies of targeting son of sevenless 1 (SOS1) in drug discovery.
Sichuan University
Overview of the development of protein arginine methyltransferase modulators: Achievements and future directions.
China Pharmaceutical University
MYC the oncogene from hell: Novel opportunities for cancer therapy.
Biomedical Research Foundation of the Academy of Athens
HDAC-targeting epigenetic modulators for cancer immunotherapy.
Hubei Polytechnic University
Small molecules targeting selected histone methyltransferases (HMTs) for cancer treatment: Current progress and novel strategies.
First Affiliated Hospital of Gannan Medical University
Discovery of GLPG3667, a Selective ATP Competitive Tyrosine Kinase 2 Inhibitor for the Treatment of Autoimmune Diseases.
Galapagos NV
Discovery of Small and Bifunctional Molecules Targeting PD-L1/CD73 for Cancer Dual Immunotherapy.
Wenzhou Medical University Lishui Hospital
Explorations of Agonist Selectivity for the α9* nAChR with Novel Substituted Carbamoyl/Amido/Heteroaryl Dialkylpiperazinium Salts and Their Therapeutic Implications in Pain and Inflammation.
University of Florida
Discovery of Oral AMP-Activated Protein Kinase Activators for Treating Hyperlipidemia.
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy.
Southern Medical University
Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer.
Insilico Medicine Shanghai Ltd
Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500).
Repare Therapeutics, Inc.
Design and synthesis of 4-amino-2',4'-dihydroxyindanone derivatives as potent inhibitors of tyrosinase and melanin biosynthesis in human melanoma cells.
University of Grenoble Alpes
HDAC/NAMPT dual inhibitors overcome initial drug-resistance in p53-null leukemia cells.
Ocean University of China
Discovery of a Covalent Inhibitor That Overcame Resistance to Venetoclax in AML Cells Overexpressing BFL-1.
University of Chinese Academy of Sciences
Discovery of Highly Selective, Potent, Covalent, and Orally Bioavailable Factor XIIa Inhibitors for the Treatment of Thrombo-Inflammation.
Hefei University of Technology
Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer.
University of Chinese Academy of Sciences
Improving tumor sensitivity by the introduction of an ester chain to triaryl derivatives targeting PD-1/PD-L1.
China Pharmaceutical University
Plasmodium falciparum topoisomerases: Emerging targets for anti-malarial therapy.
University of Kashmir
Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors.
Pfizer
Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.
Abbott Laboratories
Novel Indane-Containing NBTIs with Potent Anti-Gram-Negative Activity and Minimal hERG Inhibition.
Roche Pharma Research & Early Development
Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors.
University of Bonn
Discovery of Selective and Potent Macrocyclic CDK9 Inhibitors for the Treatment of Osimertinib-Resistant Non-Small-Cell Lung Cancer.
China Pharmaceutical University
Catecholamine Derivatives: Natural Occurrence, Structural Diversity, and Biological Activity.
Shandong University
Development of small molecule inhibitors of natural killer group 2D receptor (NKG2D).
Janssen Research & Development
Discovery of novel indazole derivatives as SOS1 agonists that activate KRAS signaling.
Sun Yat-Sen University
Discovery of novel SOS1 inhibitors using machine learning.
University of Nottingham Ningbo China
Small molecules modulating RNA splicing: a review of targets and future perspectives.
University of Bordeaux
Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1.
China Pharmaceutical University
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
Mirati Therapeutics
Advances in the development of phosphodiesterase-4 inhibitors.
Guangdong Academy of Sciences
Application and synthesis of thiazole ring in clinically approved drugs.
Zhengzhou University
Amide containing NBTI antibacterials with reduced hERG inhibition, retained antimicrobial activity against gram-positive bacteria and in vivo efficacy.
University of Ljubljana
Identification of novel Pyrrolo[2,3-d]Pyrimidine-based KRAS G12C inhibitors with anticancer effects.
Sun Yat-Sen University
Discovery of a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
Takeda Pharmaceutical
Exploration of Janus Kinase (JAK) and Histone Deacetylase (HDAC) Bispecific Inhibitors Based on the Moiety of Fedratinib for Treatment of Both Hematologic Malignancies and Solid Cancers.
China Pharmaceutical University
Acetyl-Click Screening Platform Identifies Small-Molecule Inhibitors of Histone Acetyltransferase 1 (HAT1).
Wayne State University
Advances in Epilepsy: Mechanisms, Clinical Trials, and Drug Therapies.
Sichuan University
Development of Son of Sevenless Homologue 1 (SOS1) Modulators To Treat Cancers by Regulating RAS Signaling.
China Pharmaceutical University
Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors.
China Pharmaceutical University
Strategies of Targeting CK2 in Drug Discovery: Challenges, Opportunities, and Emerging Prospects.
Sichuan University
Recent Advances on Small-Molecule Bromodomain-Containing Histone Acetyltransferase Inhibitors.
Sichuan University
Discovery of dual-action phenolic 4-arylidene-isoquinolinones with antioxidant and α-glucosidase inhibition activities.
National Autonomous University of Mexico
Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1.
Zhejiang University
Discovery of Novel PD-L1 Inhibitors That Induce the Dimerization, Internalization, and Degradation of PD-L1 Based on the Fragment Coupling Strategy.
China Pharmaceutical University
Discovery of a Dual Tubulin and Neuropilin-1 (NRP1) Inhibitor with Potent In Vivo Anti-Tumor Activity via Pharmacophore-based Docking Screening, Structure Optimization, and Biological Evaluation.
China Pharmaceutical University
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Perha Pharmaceuticals
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Kronos Bio
8-Aza Quinazolines as Brain Penetrant SOS1 Inhibitors for Treating Cancer.
Smith, Gambrell & Russell
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Novartis Institutes For Biomedical Research
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation.
Leipzig University
Receptor Interacting Ser/Thr-Protein Kinase 2 as a New Therapeutic Target.
University of Lille
Discovery of three-dimensional bicyclo[3.3.1]nonanols as novel heat shock protein 90 inhibitors.
Tokyo Institute of Innovative Research
Design, synthesis, and evaluation of PD-1/PD-L1 small-molecule inhibitors bearing a rigid indane scaffold.
China Pharmaceutical University
Targeting VPS34 in autophagy: An update on pharmacological small-molecule compounds.
Southwest Jiaotong University
Design and synthesis of a novel class of PDE4 inhibitors with antioxidant properties as bifunctional agents for the potential treatment of COPD.
China Pharmaceutical University
Clinically approved small-molecule drugs for the treatment of rheumatoid arthritis.
Jilin University
Difluoromethyl-1,3,4-oxadiazoles Are Selective, Mechanism-Based, and Essentially Irreversible Inhibitors of Histone Deacetylase
University of Bonn
Structure-activity relationship studies and biological properties evaluation of peptidic NRP-1 ligands: Investigation of N-terminal cysteine importance.
University of Warsaw
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Genentech
Design, Synthesis, and Activity Evaluation of Novel Dual-Target Inhibitors with Antifungal and Immunoregulatory Properties.
Liaocheng University
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Jinan University
Discovery and Crystallography Study of Novel Biphenyl Ether and Oxadiazole Thioether (Non-Arylmethylamine)-Based Small-Molecule PD-1/PD-L1 Inhibitors as Immunotherapeutic Agents.
Southern Medical University
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
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders.
Bayer
2-Substituted 1,5-benzothiazepine-based HDAC inhibitors exert anticancer activities on human solid and acute myeloid leukemia cell lines.
University of Salerno
Novel Amphibian Bowman-Birk-Like Inhibitor with Antioxidant and Anticoagulant Effects Ameliorates Pancreatitis Symptoms in Mice.
Southern Medical University
Identification of a Protein Arginine Methyltransferase 7 (PRMT7)/Protein Arginine Methyltransferase 9 (PRMT9) Inhibitor.
University of Salerno
Optimizing metabolic stability of phosphodiesterase 5 inhibitors: Discovery of a potent N-(pyridin-3-ylmethyl)quinoline derivative targeting synaptic plasticity.
Columbia University
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bristol-Myers Squibb
Comprehensive coverage on anti-mycobacterial endeavour reported during 2022.
L. M. College of Pharmacy
Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.
University Munster
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.
Zhejiang University
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Perha Pharmaceuticals
PepScaf: Harnessing Machine Learning with In Vitro Selection toward De Novo Macrocyclic Peptides against IL-17C/IL-17RE Interaction.
Zhejiang University
New and promising type of leukotriene B4 (LTB4) antagonists based on the 1,4-benzodioxine structure.
Sultan Moulay Slimane University
Synthetic α-glucosidase inhibitors as promising anti-diabetic agents: Recent developments and future challenges.
Quaid-I-Azam University
A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities.
Shanghai Institute of Materia Medica
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Abbott Laboratories
Diaporaustalides A-L, Austalide Meroterpenoids from a Plant Endophytic
Huazhong University of Science and Technology
A silicon-containing aryl/penta-1,4-dien-3-one/amine hybrid exhibits antiproliferative effects on breast cancer cells by targeting the HSP90 C-terminus without inducing heat-shock response.
Yunnan University
Synthesis, in vitro Α-Glucosidase, and acetylcholinesterase inhibitory activities of novel Indol-Fused Pyrano[2,3-D]Pyrimidine compounds.
Vietnam Academy of Science and Technology
The Zinc-Binding Group Effect: Lessons from Non-Hydroxamic Acid Vorinostat Analogs.
Ghent University
Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors.
Verseon
Identification of novel piperazine-tethered phthalazines as selective CDK1 inhibitors endowed with in vitro anticancer activity toward the pancreatic cancer.
Kafrelsheikh University
Discovery of pimozide derivatives as novel T-type calcium channel inhibitors with little binding affinity to dopamine D
Kindai University
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.
Shenyang Pharmaceutical University
Novel cudraisoflavone J derivatives as potent neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/HO-1 signaling.
Dongguk University-Seoul
Design, synthesis, and biological evaluation of novel dual inhibitors of heat shock protein 90/mammalian target of rapamycin (Hsp90/mTOR) against bladder cancer cells.
Sichuan University
Discovery of Novel d-(+)-Biotin-Conjugated Resorcinol Dibenzyl Ether-Based PD-L1 Inhibitors for Targeted Cancer Immunotherapy.
Zunyi Medical University
Structure-Activity Relationships of Alanine Scan Mutants αO-Conotoxins GeXIVA[1,2] and GeXIVA[1,4].
Guangxi University
Discovery of the First Irreversible HDAC6 Isoform Selective Inhibitor with Potent Anti-Multiple Myeloma Activity.
Shandong University
Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.
Sun Yat-Sen University
Design, synthesis and biological evaluation of dual Topo II/HDAC inhibitors bearing pyrimido[5,4-b]indole and pyrazolo[3,4-d]pyrimidine motifs.
Hebei University
Discovery of orally effective and safe GPR40 agonists by incorporating a chiral, rigid and polar sulfoxide into β-position to the carboxylic acid.
Soochow University
Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemia.
Anhui Medical University
Discovery of novel and bioavailable histone deacetylases and cyclin-dependent kinases dual inhibitor to impair the stemness of leukemia cells.
Nankai University
1,2,4-Amino-triazine derivatives as pyruvate dehydrogenase kinase inhibitors: Synthesis and pharmacological evaluation.
University of Palermo
Rational design of novel nucleoside analogues reveals potent antiviral agents for EV71.
Swansea University
Indole-containing pharmaceuticals: targets, pharmacological activities, and SAR studies.
Tianjin University
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Galapagos
Discovery of 2-(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase-3 (GSK-3) Inhibitors.
Biocon-Bristol Myers Squibb Research and Development Center
Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery.
Sichuan University
Carbohydrate Strengthens the Immunotherapeutic Effect of Small-Molecule PD-L1 Inhibitors.
Zhejiang University
A Molecular Toolbox of Positron Emission Tomography Tracers for General Anesthesia Mechanism Research.
Xiamen University
Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and Perspectives.
Hefei University of Technology
METTL3 from Target Validation to the First Small-Molecule Inhibitors: A Medicinal Chemistry Journey.
Sapienza University of Rome
Discovery of α-Amidobenzylboronates as Highly Potent Covalent Inhibitors of Plasma Kallikrein.
University of Nottingham
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
Galapagos
Development, validation, and evaluation of a deep learning model to screen cyclin-dependent kinase 12 inhibitors in cancers.
Peking Union Medical College
Design, Synthesis, and Biological Evaluation of 2-Hydroxy-4-phenylthiophene-3-carbonitrile as PD-L1 Antagonist and Its Comparison to Available Small Molecular PD-L1 Inhibitors.
University Medical Center Groningen
Discovery of BRD4-HDAC Dual Inhibitors with Improved Fungal Selectivity and Potent Synergistic Antifungal Activity against Fluconazole-Resistant
East China University of Science & Technology
Nanomolar β-glucosidase and β-galactosidase inhibition by enantiomeric α-1-C-alkyl-1,4-dideoxy-1,4-imino-arabinitol derivatives.
Chinese Academy of Sciences
Solubilizer Tag Effect on PD-L1/Inhibitor Binding Properties for
Jagiellonian University
Chloroacetamide fragment library screening identifies new scaffolds for covalent inhibition of the TEAD·YAP1 interaction.
Indiana University School of Medicine 635 Barnhill Drive
Synthesis and pharmacological evaluation of 1,3-diaryl substituted pyrazole based (thio)urea derivatives as potent antimicrobial agents against multi-drug resistant
National Institute of Pharmaceutical Education and Research (NIPER)
Thiourea derivatives containing 4-arylthiazoles and d-glucose moiety: design, synthesis, antimicrobial activity evaluation, and molecular docking/dynamics simulations.
Vietnam National University
Discovery of a Potent and Selective Tyrosine Kinase 2 Inhibitor: TAK-279.
Nimbus Therapeutics
Identification of small-molecule inhibitors of human MUS81-EME1/2 by FRET-based high-throughput screening.
Fuzhou University
What We Have Gained from Ibogaine: α3β4 Nicotinic Acetylcholine Receptor Inhibitors as Treatments for Substance Use Disorders.
University of Illinois At Chicago
Evolution of Slow-Binding Inhibitors Targeting Histone Deacetylase Isoforms.
Osaka University
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
Zhejiang University
Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Discovery of a Series of Indane-Containing NBTIs with Activity against Multidrug-Resistant Gram-Negative Pathogens.
Roche Pharma Research & Early Development
Synthesis of the Purported Structure of Glyphaeaside C and Proposed Revisions to the Structures of the Glyphaeaside Alkaloids.
University of Wollongong
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Pfizer
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.
Guangxi University
Discovery and Characterization of the Topical Soft JAK Inhibitor CEE321 for Atopic Dermatitis.
Novartis
Discovery of Novel Indazole Chemotypes as Isoform-Selective JNK3 Inhibitors for the Treatment of Parkinson's Disease.
Sichuan University
Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against
University of Ljubljana
Mechanistic Insight of Synthesized 1,4-Dihydropyridines as an Antidiabetic Sword against Reactive Oxygen Species.
Tanta University
Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment.
China Pharmaceutical University
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
Revolution Medicines
Subnanomolar Affinity and Selective Antagonism at α7 Nicotinic Receptor by Combined Modifications of 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624).
University of Milan
Current advances in Vibrio harveyi quorum sensing as drug discovery targets.
Zhejiang University
Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5- a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction.
Zhengzhou University
Recent advances in small molecule based cancer immunotherapy.
Southern Medical University
Enzyme inhibitory activities an insight into the structure-Activity relationship of biscoumarin derivatives.
Quaid-I-Azam University
Chemical Constituents of Bryophytes: Structures and Biological Activity.
Tokushima Bunri University
An overview on the recent developments of 1,2,4-triazine derivatives as anticancer compounds.
Universita Degli Studi Di Palermo
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Genentech
Isoxazole ring as a useful scaffold in a search for new therapeutic agents.
Wroclaw University
Therapeutic journey of 2,4-thiazolidinediones as a versatile scaffold: An insight into structure activity relationship.
Jamia Hamdard
Design, synthesis and bioactivity evaluations of 8-substituted-quinoline-2-carboxamide derivatives as novel histone deacetylase (HDAC) inhibitors.
Shandong University
Synthesis and biological evaluation of novel pteridin-7(8H)-one derivatives as potent CDK2 inhibitors.
Jiangnan University
Siderophores: Chemical tools for precise antibiotic delivery.
Universidade De Santiago De Compostela
Total Synthesis and Biological Evaluation of the Anti-Inflammatory (13
Johannes Gutenberg-University
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.
Vanderbilt University
Accelerated Discovery of Macrocyclic CDK2 Inhibitor QR-6401 by Generative Models and Structure-Based Drug Design.
Tencent Ai Lab
Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN.
University of Shizuoka
Anagrelide: A Clinically Effective cAMP Phosphodiesterase 3A Inhibitor with Molecular Glue Properties.
The Baruch S. Blumberg Institute
Quinazolinone-1,2,3-triazole-acetamide conjugates as potent α-glucosidase inhibitors: synthesis, enzyme inhibition, kinetic analysis, and molecular docking study.
Tehran University of Medical Sciences Tehran Iran
Development of sulfonium tethered peptides conjugated with HDAC inhibitor to improve selective toxicity for cancer cells.
Tongji Medical College Huazhong University of Science and Technology
Design, synthesis and biological evaluation of novel N-(methyl-d
Nanjing University of Science and Technology
Dual Kinase-Bromodomain Inhibitors in Anticancer Drug Discovery: A Structural and Pharmacological Perspective.
University of Modena and Reggio Emilia
2015 Philip S. Portoghese Medicinal Chemistry Lectureship. Curing Hepatitis C Virus Infection with Direct-Acting Antiviral Agents: The Arc of a Medicinal Chemistry Triumph.
Bristol-Myers Squibb Research & Development
Discovery and development of kibdelomycin, a new class of broad-spectrum antibiotics targeting the clinically proven bacterial type II topoisomerase.
Sbs Pharma Consulting
Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors.
Guru Nanak Dev University
Discovery of Isonicotinamides as Highly Selective, Brain Penetrable, and Orally Active Glycogen Synthase Kinase-3 Inhibitors.
Bristol-Myers Squibb Research & Development
A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Novartis Institutes For Biomedical Research
Novel Concept for Super-Soft Topical Drugs: Deactivation by an Enzyme-Induced Switch into an Inactive Conformation.
Novartis Institutes For Biomedical Research
New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate
University of Ljubljana
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Perha Pharmaceuticals
Design, synthesis and anticancer evaluation of selective 2,4-disubstituted pyrimidine CDK9 inhibitors.
Southeast University
C-6 fluorinated casuarines as highly potent and selective amyloglucosidase inhibitors: Synthesis and structure-activity relationship study.
Beijing National Laboratory For Molecular Sciences
Novel alpha6 preferring GABA-A receptor ligands based on loreclezole.
University of Vienna
Improved Selective Class I HDAC and Novel Selective HDAC3 Inhibitors: Beyond Hydroxamic Acids and Benzamides.
IRBM Science Park
Geminal Diheteroatomic Motifs: Some Applications of Acetals, Ketals, and Their Sulfur and Nitrogen Homologues in Medicinal Chemistry and Drug Design.
Bristol Myers Squibb Research and Early Development
Aldose reductase and protein tyrosine phosphatase 1B inhibitors as a promising therapeutic approach for diabetes mellitus.
Aristotle University of Thessaloniki
Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery.
China Pharmaceutical University
Artemisinin-derived hybrids and their anticancer activity.
Qilu University of Technology (Shandong Academy of Sciences)
Thiazole-containing compounds as therapeutic targets for cancer therapy.
Kurukshetra University
A comprehensive review on xanthone derivatives as α-glucosidase inhibitors.
Polytechnic Institute of Braganca
Recent developments of quinolone-based derivatives and their activities against Escherichia coli.
Medical School of Nanjing University
β-Carboline alkaloid monomers and dimers: Occurrence, structural diversity, and biological activities.
Northwest A&F University
Current anti-diabetic agents and their molecular targets: A review.
University of Kwazulu-Natal
2-Anilino-4-(1-methyl-1H-pyrazol-4-yl)pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation.
University of South Australia
A concise review on marine bromopyrrole alkaloids as anticancer agents.
University of Kwazulu-Natal (Westville)
A comprehensive review of BET-targeting PROTACs for cancer therapy.
Xinxiang Medical University
Insights into the recent progress in the medicinal chemistry of pyranopyrimidine analogs.
Mansoura University
Non-steroidal anti-inflammatory drugs: recent advances in the use of synthetic COX-2 inhibitors.
Leibniz Institute For Plasma Science and Technology (Inp Greifswald)
Discovery of a Dual Tubulin and Poly(ADP-Ribose) Polymerase-1 Inhibitor by Structure-Based Pharmacophore Modeling, Virtual Screening, Molecular Docking, and Biological Evaluation.
China Pharmaceutical University
A comprehensive overview of β-carbolines and its derivatives as anticancer agents.
Xinyang Normal University
Research progress of dual inhibitors targeting crosstalk between histone epigenetic modulators for cancer therapy.
Xinxiang Medical University
Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets.
University of Palermo
Inhibitors of BCL2A1/Bfl-1 protein: Potential stock in cancer therapy.
China Pharmaceutical University
Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators.
IQM-CSIC
Novel α7 nicotinic acetylcholine receptor modulators as potential antitussive agents.
Philip Morris International
Bioactive Aurones, Indanones, and Other Hemiindigoid Scaffolds: Medicinal Chemistry and Photopharmacology Perspectives.
Universite Grenoble Alpes
An overview of the development of EED inhibitors to disable the PRC2 function.
University of Jinany
Imidazo[1,2-b]pyridazine as privileged scaffold in medicinal chemistry: An extensive review.
Universite de Tours
An overview of hydroxypyranone and hydroxypyridinone as privileged scaffolds for novel drug discovery.
Guizhou Medical University
β-Carboline as a Privileged Scaffold for Multitarget Strategies in Alzheimer's Disease Therapy.
Univ. Grenoble Alpes
Anticancer fungal natural products: Mechanisms of action and biosynthesis.
Sun Yat-Sen University
β-Lactams as promising anticancer agents: Molecular hybrids, structure activity relationships and potential targets.
Beijing University of Chinese Medicine
Resveratrol - A comprehensive review of recent advances in anticancer drug design and development.
Mazandaran University of Medical Sciences
Recent advances in DNA gyrase-targeted antimicrobial agents.
Queensland University of Technology
Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: A review.
Jadavpur University
Discovery and development of plasma kallikrein inhibitors for multiple diseases.
Hefei University of Technology
Diarylamides in anticancer drug discovery: A review of pre-clinical and clinical investigations.
University of Sharjah
Recent developments of chalcones as potential antibacterial agents in medicinal chemistry.
Weifang Medical University
Recent advance in the development of novel, selective and potent FGFR inhibitors.
China Pharmaceutical University
Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules.
China Pharmaceutical University
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.
Northwest University
From Hit Seeking to Magic Bullets: The Successful Union of Epigenetic and Fragment Based Drug Discovery (EPIDD + FBDD).
University of S£O Paulo
Synthesis and Biological Evaluation of Celastrol Derivatives with Improved Cytotoxic Selectivity and Antitumor Activities.
China Pharmaceutical University
Natural spirocyclic alkaloids and polyphenols as multi target dementia leads.
Rmit University
Computational methods-guided design of modulators targeting protein-protein interactions (PPIs).
Shanghai Jiao Tong University
Hydroxamic acid hybrids as the potential anticancer agents: An Overview.
Huaihe Hospital of Henan University
A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents.
Mizoram University
Recent advances in steroid amino acid conjugates: Old scaffolds with new dimensions.
Panjab University
Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry.
William S. Middleton Veterans Hospital
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
Polycomb Repressive Complex 2 Modulation through the Development of EZH2-EED Interaction Inhibitors and EED Binders.
University of Naples "Federico Ii
Rational Multitargeted Drug Design Strategy from the Perspective of a Medicinal Chemist.
Shandong University
Source and exploration of the peptides used to construct peptide-drug conjugates.
China Pharmaceutical University
Targeting Nuclear Receptors in Neurodegeneration and Neuroinflammation.
Goethe University Frankfurt
Advances in Cyclic Nucleotide Phosphodiesterase-Targeted PET Imaging and Drug Discovery.
Massachusetts General Hospital
Fused-azepinones: Emerging scaffolds of medicinal importance.
National Institute of Pharmaceutical Education and Research (NIPER)
Small-Molecule Inhibitors Targeting the Canonical WNT Signaling Pathway for the Treatment of Cancer.
Ocean University of China
The long and winding road of designing phosphodiesterase inhibitors for the treatment of heart failure.
Rural Federal University of Rio De Janeiro
Mercaptoacetamide: A promising zinc-binding group for the discovery of selective histone deacetylase 6 inhibitors.
Scripps Research
Natural heat shock protein 90 inhibitors in cancer and inflammation.
Oswaldo Cruz Foundation
Design, synthesis, and biological evaluation of novel N-Benzyl piperidine derivatives as potent HDAC/AChE inhibitors for Alzheimer's disease.
Shandong University
4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione inhibitors of the checkpoint kinase Wee1. Structure-activity relationships for chromophore modification and phenyl ring substitution.
University of Auckland
Recent advances toward the development of Hsp90 C-terminal inhibitors.
University of Notre Dame
Structure, Function, and Inhibitors of the Mitochondrial Chaperone TRAP1.
Ewha Womans University
Targeting the PI3K/AKT/mTOR Signaling Pathway in the Treatment of Human Diseases: Current Status, Trends, and Solutions.
South China University of Technology
Biphenyl-based small molecule inhibitors: Novel cancer immunotherapeutic agents targeting PD-1/PD-L1 interaction.
Acharya & Bm Reddy College of Pharmacy
Homobivalent, Trivalent, and Covalent PROTACs: Emerging Strategies for Protein Degradation.
Second Military Medical University
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Abbott Laboratories
Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
University of Regensburg
High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.
Hadassah Hebrew University
Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.
Johnson & Johnson Pharmaceutical Research & Development
2-Hydroxy-4,6-diamino-[1,3,5]triazines: a novel class of VEGF-R2 (KDR) tyrosine kinase inhibitors.
Johnson & Johnson Pharmaceutical Research and Development
Targeting Small GTPases and Their Prenylation in Diabetes Mellitus.
Lodz University of Technology
Orally active anti-proliferation agents: novel diphenylamine derivatives as FGF-R2 autophosphorylation inhibitors.
Kirin Brewery
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
Aventis Pharmaceuticals
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.
Aventis Pharmaceuticals
Macrocyclic bisindolylmaleimides as inhibitors of protein kinase C and glycogen synthase kinase-3.
Johnson & Johnson Pharmaceutical Research & Development
Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck.
Abbott Bioresearch Center
Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.
Merck Research Laboratories
Substituted 5,7-diphenyl-pyrrolo[2,3d]pyrimidines: potent inhibitors of the tyrosine kinase c-Src.
Novartis Pharma
Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.
Novartis
Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors.
Warner-Lambert
Dianilinophthalimides: potent and selective, ATP-competitive inhibitors of the EGF-receptor protein tyrosine kinase.
Ciba-Geigy
5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.
Sterling Winthrop Pharmaceuticals Research Division
A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives.
RhôNe-Poulenc Rorer
Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Shenyang Pharmaceutical University
Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
Korea Research Institute of Chemical Technology