91 articles for thisTarget
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Discovery of Potent and Orally Bioavailable GPR40 Full Agonists Bearing Thiophen-2-ylpropanoic Acid Scaffold.
Shanghai Institute of Materia Medica
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.
Shanghai Institute of Materia Medica
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.
Shanghai Institute of Materia Medica
Design, synthesis, structure-activity relationships, and docking studies of pyrazole-containing derivatives as a novel series of potent glucagon receptor antagonists.
Shanghai Institute of Materia Medica
Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors.
Shanghai Institute of Materia Medica
Discovery of novel 2-phenyl-imidazo[1,2-a]pyridine analogues targeting tubulin polymerization as antiproliferative agents.
Shanghai Institute of Materia Medica
Design, synthesis and biological evaluation of bisthiazole-based trifluoromethyl ketone derivatives as potent HDAC inhibitors with improved cellular efficacy.
Shanghai Institute of Materia Medica
Design, synthesis and in vitro activity of phidianidine B derivatives as novel PTP1B inhibitors with specific selectivity.
Shanghai Institute of Materia Medica
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.
Shanghai Institute of Materia Medica
Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization.
Shanghai Institute of Materia Medica
Discovery of Anilinopyrimidines as Dual Inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and Cellular Activity.
Shanghai Institute of Materia Medica
Discovery of novel inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 by docking and pharmacophore modeling.
Shanghai Institute of Materia Medica
Asymmetric synthesis and biological evaluation of N-cyclohexyl-4-[1-(2,4-dichlorophenyl)-1-(p-tolyl)methyl]piperazine-1-carboxamide as hCB1 receptor antagonists.
Shanghai Institute of Materia Medica
AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.
Shanghai Institute of Materia Medica
Discovery of Imidazo[1,2-a]pyrazine Derivatives as Potent ENPP1 Inhibitors.
Shanghai Institute of Materia Medica
Targeting Thyroid-Stimulating Hormone Receptor: A Perspective on Small-Molecule Modulators and Their Therapeutic Potential.
Shanghai Institute of Materia Medica
Discovery of pyrrolo[2,3-d]pyrimidin-4-one derivative YCH3124 as a potent USP7 inhibitor for cancer therapy.
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of 2,4-Diaminopyrimidine Derivatives as Potent CDK7 Inhibitors.
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of Potent and Selective PROTAC Degraders of Oncogenic KRASG12D.
Shanghai Institute of Materia Medica
Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma.
Shanghai Institute of Materia Medica
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
Discovery of Potent and Selective G9a Degraders for the Treatment of Pancreatic Cancer.
Shanghai Institute of Materia Medica
Discovery of Pyrido[2,3-d]pyrimidin-7-one Derivatives as Highly Potent and Efficacious Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (ENPP1) Inhibitors for Cancer Treatment.
Shanghai Institute of Materia Medica
Discovery of PVD-06 as a Subtype-Selective and Efficient PTPN2 Degrader.
Shanghai Institute of Materia Medica
Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
Shanghai Institute of Materia Medica
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
Discovery and Structural Optimization of Covalent ZAP-70 Kinase Inhibitors against Psoriasis.
Shanghai Institute of Materia Medica
A chemical perspective on the modulation of TEAD transcriptional activities: Recent progress, challenges, and opportunities.
Shanghai Institute of Materia Medica
Design and synthesis of cantharidin derivative DCZ5418 as a TRIP13 inhibitor with anti-multiple myeloma activity in vitro and in vivo.
Shanghai Institute of Materia Medica
Discovery of Novel 5,6-Dihydro-1,2,4-triazine Derivatives as Efficacious Glucagon-Like Peptide-1 Receptor Agonists.
Shanghai Institute of Materia Medica
Design and exploration of gut-restricted bifunctional molecule with TGR5 agonistic and DPP4 inhibitory effects for treating ulcerative colitis.
Shanghai Institute of Materia Medica
Discovery of a potent and selective proteolysis targeting chimera (PROTAC) degrader of NSD3 histone methyltransferase.
Shanghai Institute of Materia Medica
Discovery of a Novel Bifunctional Steroid Analog, YXG-158, as an Androgen Receptor Degrader and CYP17A1 Inhibitor for the Treatment of Enzalutamide-Resistant Prostate Cancer.
Shanghai Institute of Materia Medica
Discovery of 7H-Pyrrolo[2,3-d]pyrimidine Derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Shanghai Institute of Materia Medica
Selective degradation of cellular BRD3 and BRD4-L promoted by PROTAC molecules in six cancer cell lines.
Shanghai Institute of Materia Medica
Development of a series of quinazoline-2,5-diamine derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors.
Shanghai Institute of Materia Medica
An Update on Poly(ADP-ribose)polymerase-1 (PARP-1) Inhibitors: Opportunities and Challenges in Cancer Therapy.
Shanghai Institute of Materia Medica
Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers.
Shanghai Institute of Materia Medica
Structural Optimization of Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
Shanghai Institute of Materia Medica
Discovery of Highly Potent and Selective Thyroid Hormone Receptor β Agonists for the Treatment of Nonalcoholic Steatohepatitis.
Shanghai Institute of Materia Medica
Targeted Drugs for Treatment of Pulmonary Arterial Hypertension: Past, Present, and Future Perspectives.
Shanghai Institute of Materia Medica
Structure-Based Discovery of Potent CARM1 Inhibitors for Solid Tumor and Cancer Immunology Therapy.
Shanghai Institute of Materia Medica
Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells.
Shanghai Institute of Materia Medica
Discovery of the First-in-Class Agonist-Based SOS1 PROTACs Effective in Human Cancer Cells Harboring Various KRAS Mutations.
Shanghai Institute of Materia Medica
Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors.
Shanghai Institute of Materia Medica
Phosphodiesters as GPR84 Antagonists for the Treatment of Ulcerative Colitis.
Shanghai Institute of Materia Medica
In silico screening-based discovery of novel covalent inhibitors of the SARS-CoV-2 3CL protease.
Shanghai Institute of Materia Medica
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
Shanghai Institute of Materia Medica
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate.
Shanghai Institute of Materia Medica
Design, Synthesis, and Structure-Activity Relationship Studies of Bisamide Derivatives of Amphotericin B with Potent Efficacy and Low Toxicity.
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer.
Shanghai Institute of Materia Medica
Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR
Shanghai Institute of Materia Medica
Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-
Shanghai Institute of Materia Medica
Discovery of selective HDAC/BRD4 dual inhibitors as epigenetic probes.
Shanghai Institute of Materia Medica
Automated design and optimization of multitarget schizophrenia drug candidates by deep learning.
Shanghai Institute of Materia Medica
Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer.
Shanghai Institute of Materia Medica
Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1).
Shanghai Institute of Materia Medica
Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors.
Shanghai Institute of Materia Medica
Discovery of an Inhibitor for the TREK-1 Channel Targeting an Intermediate Transition State of Channel Gating.
Shanghai Institute of Materia Medica
Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors.
Shanghai Institute of Materia Medica
Discovery of 2-substituted-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-1,2,3,4-tetrahydroisoquinoline-6-carboxamide as potent and selective protein arginine methyltransferases 5 inhibitors: Design, synthesis and biological evaluation.
Shanghai Institute of Materia Medica
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Shanghai Institute of Materia Medica
Discovery and biological evaluation of vinylsulfonamide derivatives as highly potent, covalent TEAD autopalmitoylation inhibitors.
Shanghai Institute of Materia Medica
Design of cell-permeable stapled peptides as HIV-1 integrase inhibitors.
Shanghai Institute of Materia Medica
Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.
Shanghai Institute of Materia Medica
Design, synthesis and biological evaluation of 4,7,12,12a-tetrahydro-5H-thieno[3',2':3,4]pyrido[1,2-b]isoquinolines as novel adenosine 5'-monophosphate-activated protein kinase (AMPK) indirect activators for the treatment of type 2 diabetes.
Shanghai Institute of Materia Medica
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrido[4,3-c]azepin-5-one-based novel chemotype CCR2 antagonists via scaffold hopping strategy.
Shanghai Institute of Materia Medica
Quinone skeleton as a new class of irreversible inhibitors against Staphylococcus aureus sortase A.
Shanghai Institute of Materia Medica
SUBSTITUTED N-CYANOPYRROLIDINES WITH ACTIVITY AS USP30 INHIBITORS
Mission Therapeutics
Pyrido[3,2-d]pyrimidine compounds uses thereof for treating a proliferative disease
Université
Benzothiophene-based selective estrogen receptor downregulator compounds
University of Illinois
FUSED POLYCYCLIC SUBSTITUTED 5-CARBOXYLIC ACID THIENOPYRIMIDINE DIONE COMPOUND AND USE THEREOF
Soter Biopharma
Substituted benzodiazoles and use thereof in therapy
Thomas Helledays Stiftelse FÖR Medicinsk Forskning
INHIBITORS OF MYCOBACTERIUM TUBERCULOSIS LIPOAMIDE DEHYDROGENASE
Cornell University
QUINAZOLINE-2,4-DIAMINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER COMPRISING SAME AS ACTIVE INGREDIENT
The Asean Foundation
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Merck Research Laboratories
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Sphinx Laboratories