272 articles for thisTarget
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Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.
Roche Innovation Center Shanghai
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism.
Hanyang University
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.
Forum Pharmaceuticals
Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.
De Montfort University
Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT
Suven Life Sciences
Discovery and Preclinical Characterization of 3-((4-(4-Chlorophenyl)-7-fluoroquinoline-3-yl)sulfonyl)benzonitrile, a Novel Non-acetylenic Metabotropic Glutamate Receptor 5 (mGluR5) Negative Allosteric Modulator for Psychiatric Indications.
Gedeon Richter
Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3).
East China University Of Science And Technology
Discovery of 2-(((1r,4r)-4-(((4-Chlorophenyl)(phenyl)carbamoyl)oxy)methyl)cyclohexyl)methoxy)acetate (Ralinepag): An Orally Active Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.
Arena Pharmaceuticals
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.
Bristol-Myers Squibb
Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.
Global Blood Therapeutics
New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
Pontif£Cia Universidade Cat£Lica Do Rio Grande Do Sul
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.
Bristol-Myers Squibb Research And Development
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP
Novartis Institutes For Biomedical Research
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.
University Of Modena And Reggio Emilia
Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.
Vanderbilt University
Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome.
National Institute Of Biological Sciences
Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.
Rapt Therapeutics
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity
University Of Nottingham
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.
Janssen Research & Development
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia.
Convergence Pharmaceuticals
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.
Ontario Institute For Cancer Research
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.
Astrazeneca
Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for ?-secretase modulators with oral efficacy against cognitive deficits in Alzheimer's disease model mice.
Astellas Pharma
Exploration of Alternative Scaffolds for P2Y
National Institute Of Diabetes And Digestive And Kidney Diseases
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t.
Phenex Pharmaceuticals
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.
Constellation Pharmaceuticals
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.
Bristol Myers Squibb
Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases.
The First Affiliated Hospital Of Xi'An Jiao Tong University
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.
Haisco Pharmaceutical Group
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.
Sun Yat-Sen University
Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.
X-Chem
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.
Biogen
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.
University College London
Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Astrazeneca
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis.
Washington University School Of Medicine
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures.
Ocean University Of China
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
University Of Washington
Design, synthesis, and enzymatic characterization of quinazoline-based CYP1A2 inhibitors.
University Of Florida
Discovery of Second Generation ROR? Inhibitors Composed of an Azole Scaffold.
Kyoto Prefectural University Of Medicine
Cink4T, a quinazolinone-based dual inhibitor of Cdk4 and tubulin polymerization, identified via ligand-based virtual screening, for efficient anticancer therapy.
De Montfort University
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.
Janssen Research & Development
Development of a Series of (1-Benzyl-3-(6-methoxypyrimidin-3-yl)-5-(trifluoromethoxy)-1H-indol-2-yl)methanols as Selective Protease Activated Receptor 4 (PAR4) Antagonists with in Vivo Utility and Activity Against ?-Thrombin.
Northwest Agriculture & Forestry University
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.
University Of Dundee
Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
Arqule
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.
Amgen
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.
Shenyang Pharmaceutical University
Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research.
Shenyang Pharmaceutical University
SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-
University Of Modena And Reggio Emilia
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.
Roche Innovation Center Shanghai
Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.
University Of Modena And Reggio Emilia
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.
Boehringer Ingelheim (Canada)
Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine ?-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.
Bristol-Myers Squibb
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
Bristol-Myers Squibb Research And Development
Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme.
University Of California
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.
Takeda California
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators.
Sumitomo Dainippon Pharma
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.
Jagiellonian University Medical College
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).
Bristol-Myers Squibb
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Shionogi
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
The Scripps Research Institute
Design of Novel Inhibitors of Human Thymidine Phosphorylase: Synthesis, Enzyme Inhibition, in Vitro Toxicity, and Impact on Human Glioblastoma Cancer.
Universidade Federal Do Pampa
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na
Xenon Pharmaceuticals
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
TBA
Evaluation of Amides, Carbamates, Sulfonamides, and Ureas of 4-Prop-2-ynylidenecycloalkylamine as Potent, Selective, and Bioavailable Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5.
Recordati
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.
"Sapienza" Universit£
Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.
Chung-Ang University
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.
University Of Toronto
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
University Of Washington
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College Of Wisconsin
Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73.
Arcus Biosciences
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University Of Chinese Medicine
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.
Lindsley F. Kimball Research Institute
Identification of Novel Resorcinol Amide Derivatives as Potent and Specific Pyruvate Dehydrogenase Kinase (PDHK) Inhibitors.
Korea University
Discovery and lead optimisation of a potent, selective and orally bioavailable RAR? agonist for the potential treatment of nerve injury.
King'S College
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.
Janssen Research & Development
Benzothiazole-based compounds as potent endothelial lipase inhibitors.
Bristol-Myers Squibb
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
National Institute Of Biological Sciences (Nibs)
Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease.
TBA
Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists.
Japan Tobacco
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.
Bristol-Myers Squibb
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
Biogen
Design and synthesis of a novel series of cyanoindole derivatives as potent ?-secretase modulators.
Janssen Research & Development
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
Sabila Biosciences
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.
University Of Modena And Reggio Emilia
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.
Sun Yat-Sen University
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
Peking Union Medical College And Chinese Academy Of Medical Sciences
Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
Shandong University
Synthesis and structure-activity relationship studies of ?-naphthoflavone derivatives as CYP1B1 inhibitors.
Shanghai Jiao Tong University
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-
University Of Oxford
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.
TBA
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.
Chung-Ang University
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Advinus Therapeutics
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
Astrazeneca
Discovery and Development of N-[4-(1-Cyclobutylpiperidin-4-yloxy)phenyl]-2-(morpholin-4-yl)acetamide Dihydrochloride (SUVN-G3031): A Novel, Potent, Selective, and Orally Active Histamine H
Suven Life Sciences
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
Shandong University
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.
Shanghai Hengrui Pharmaceutical
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of ?7 nAChRs.
Bionomics
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
Astrazeneca
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
Chinese Academy Of Medical Sciences And Peking Union Medical College
Discovery of Imidazoisoindole Derivatives as Highly Potent and Orally Active Indoleamine-2,3-dioxygenase Inhibitors.
Shanghai Hengrui Pharmaceutical
Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.
Shandong University
Novel Chemical Series of 5-Lipoxygenase-Activating Protein Inhibitors for Treatment of Coronary Artery Disease.
TBA
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.
Advinus Therapeutics
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.
Japanese Foundation For Cancer Research
Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS.
Promidis
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists.
Bristol-Myers Squibb
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.
Bristol-Myers Squibb Research & Development
Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.
Korea Research Institute Of Chemical Technology
Rationally Designed, Conformationally Constrained Inverse Agonists of ROR?t-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Bristol-Myers Squibb
Maximizing ER-? Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.
Seragon Pharmaceuticals
Discovery of new indole-based acylsulfonamide Na
Bristol-Myers Squibb Research And Development
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Gwangju Institute Of Science And Technology
Discovery of potent and selective PPAR?/? dual antagonists and initial biological studies.
Inception Sciences
Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure.
Japan Tobacco
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Bayer
Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1.
Birla Institute Of Technology
Adaptable Small Ligand of CYP1 Enzymes for Use in Understanding the Structural Features Determining Isoform Selectivity.
Seoul National University
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD-1).
Bristol-Myers Squibb
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.
Ube Industries
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.
West China Hospital Of Sichuan University
Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.
Bayer
Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria.
Chinese Academy Of Sciences
Design and synthesis of selective CYP1B1 inhibitor via dearomatization of ?-naphthoflavone.
Showa Pharmaceutical University
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu
Vanderbilt University
Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.
Abide Therapeutics
Fragment Based Optimization of Metabotropic Glutamate Receptor 2 (mGluR2) Positive Allosteric Modulators in the Absence of Structural Information.
Gedeon Richter
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.
Astrazeneca
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor ?/? Agonist for the Treatment of Primary Biliary Cirrhosis.
Wuxi Apptec (Shanghai) Co.
Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation.
University Of South Australia
Re-exploration of the mGlu? PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.
Vanderbilt University Medical Center
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.
Astrazeneca
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-?-D-ribose 2'-oxidase.
Astrazeneca
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
Eli Lilly
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
Modification and Biological Evaluation of a Series of 1,5-Diaryl-1,2,4-triazole Compounds as Novel Agents against Pancreatic Cancer Metastasis through Targeting Myoferlin.
East China Normal University
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB
Janssen Research & Development
Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents.
Bristol-Myers Squibb Research And Development
Discovery and Characterization of AZD6738, a Potent Inhibitor of Ataxia Telangiectasia Mutated and Rad3 Related (ATR) Kinase with Application as an Anticancer Agent.
Astrazeneca
Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity.
Japan Tobacco
Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists.
Janssen Infectious Diseases
Cell-Active Small Molecule Inhibitors of the DNA-Damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides.
The University Of Manchester
Design and optimization of 2,3-dihydrobenzo[b][1,4]dioxine propanoic acids as novel GPR40 agonists with improved pharmacokinetic and safety profiles.
Chinese Academy Of Sciences
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).
Marquette University
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNa
Xenon Pharmaceuticals
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.
Keimyung University
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.
University Of Chinese Academy Of Sciences
In vitro and in vivo pharmacokinetic and pharmacodynamic study of MBRI-001, a deuterium-substituted plinabulin derivative as a potent anti-cancer agent.
Ocean University Of China
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu
Vanderbilt University
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Jagiellonian University Medical College
Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy.
Shionogi
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.
Shenyang Pharmaceutical University
Discovery of {4-[4,9-bis(ethyloxy)-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl]-2-fluorophenyl}acetic acid (GSK726701A), a novel EP
Glaxosmithkline
Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists.
Taisho Pharmaceutical
Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors.
Cistim Leuven
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Astrazeneca
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Shanghai Haiyan Pharmaceutical Technology
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.
Shanghai Haihe Pharmaceutical
Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.
University Of Modena And Reggio Emilia
Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.
Dart Neuroscience
Rational Design of Novel 1,3-Oxazine Based ?-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust A? Reduction in the Brain.
TBA
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Vanderbilt University
Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure.
Japan Tobacco
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.
Frost Biologic
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.
Janssen Infectious Diseases Diagnostics
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.
King'S College
Glycyrrhiza glabra extract and quercetin reverses cisplatin resistance in triple-negative MDA-MB-468 breast cancer cells via inhibition of cytochrome P450 1B1 enzyme.
Csir-Indian Institute Of Integrative Medicine
(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.
De Montfort University
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Idorsia Pharmaceuticals
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.
Wuxi Apptec (Shanghai)
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
Sunshine Lake Pharma
Design and Activity of Specific Hypoxia-Inducible Factor-2? (HIF-2?) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).
Peloton Therapeutics
Design, synthesis, structure-activity relationships study and X-ray crystallography of 3-substituted-indolin-2-one-5-carboxamide derivatives as PAK4 inhibitors.
Shenyang Pharmaceutical University
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Astrazeneca
Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition.
Washington State University
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.
Chinese Academy Of Medical Sciences And Peking Union Medical College
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Bristol-Myers Squibb Research And Development
Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).
Janssen Pharmaceutical Companies Of Johnson & Johnson
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.
Glaxosmithkline
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.
Japan Tobacco
Discovery of APD371: Identification of a Highly Potent and Selective CB
Arena Pharmaceuticals
Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.
TBA
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
Astrazeneca
Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Janssen Pharmaceutica
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors.
Roche Innovation Center Shanghai
Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.
Tsinghua University
Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.
East China University Of Science And Technology
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.
Pfizer
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Janssen Research And Development
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
University Of Liverpool
The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.
Bristol-Myers Squibb Research And Development
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.
Mitsubishi Tanabe Pharma
Discovery of dimethyl pent-4-ynoic acid derivatives, as potent and orally bioavailable DGAT1 inhibitors that suppress body weight in diet-induced mouse obesity model.
Wuxi Apptec (Shanghai)
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.
Shenyang Pharmaceutical University
Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.
Iteos Therapeutics
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).
Genentech
Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.
Mitsubishi Tanabe Pharma
Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.
Mitsubishi Tanabe Pharma
Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance.
De Montfort University
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Janssen Research And Development
Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).
Pharmakea Therapeutics
Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.
Corcept Therapeutics
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.
Csir-Indian Institute Of Integrative Medicine
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Vanderbilt University
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H
Glaxosmithkline
Synthesis and optimization of 4,5,6,7-tetrahydrooxazolo[4,5-c]pyridines as potent and orally-active metabotropic glutamate receptor 5 negative allosteric modulators.
Sumitomo Dainippon Pharma
Neuroactive Steroids. 2. 3?-Hydroxy-3?-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5?-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (?-Aminobutyric Acid)
Sage Therapeutics
Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.
Experimental Therapeutics Centre
Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation.
Vanderbilt University Institute Of Imaging Science
Therapeutic potentials of baicalin and its aglycone, baicalein against inflammatory disorders.
Tripura University
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Janssen Research And Development
Discovery of an Orally Bioavailable Benzofuran Analogue That Serves as a?-Amyloid Aggregation Inhibitor for the Potential Treatment of Alzheimer's Disease.
Medifron Dbt
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
Janssen Pharmaceutica
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
Hec Pharma Group
In Vitro Pharmacokinetic Optimizations of AM2-S31N Channel Blockers Led to the Discovery of Slow-Binding Inhibitors with Potent Antiviral Activity against Drug-Resistant Influenza A Viruses.
The University Of Arizona
Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.
National Health Research Institutes
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
East China University Of Science And Technology
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin
Wuxi Apptec
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88
Astrazeneca
Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.
Galapagos
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Genentech
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).
Celgene
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.
Wuxi Apptec (Shanghai)
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.
Mochida Pharmaceutical
Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity.
University Of Waterloo
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.
Wuxi Apptec (Shanghai)
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
Emory University
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.
Bayer
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.
Bristol-Myers Squibb
Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11?-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.
Bristol-Myers Squibb
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours.
Astrazeneca
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Wyeth Research