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272 articles for thisTarget


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

PMID
Data
Article Title
Organization
Quinazoline derivatives as selective CYP1B1 inhibitors.EBI
Birla Institute Of Technology
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.EBI
Sun Yat-Sen University
Sulfonamides as Selective NaEBI
Amgen
Discovery and Pre-Clinical Characterization of Third-Generation 4-H Heteroaryldihydropyrimidine (HAP) Analogues as Hepatitis B Virus (HBV) Capsid Inhibitors.EBI
Roche Innovation Center Shanghai
Effects of 6-paradol, an unsaturated ketone from gingers, on cytochrome P450-mediated drug metabolism.EBI
Hanyang University
Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.EBI
Forum Pharmaceuticals
Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.EBI
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-HTEBI
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.EBI
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).EBI
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.EBI
Arena Pharmaceuticals
BMS-933043, a Selectivea7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia.EBI
Bristol-Myers Squibb
Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin.EBI
Global Blood Therapeutics
New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.EBI
Pontif£Cia Universidade Cat£Lica Do Rio Grande Do Sul
Discovery and Assessment of Atropisomers of (±)-Lesinurad.EBI
Wuxi Apptec
Identification and optimization of a novel series of indoleamine 2,3-dioxygenase inhibitors.EBI
Bristol-Myers Squibb Research And Development
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DPEBI
Novartis Institutes For Biomedical Research
Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.EBI
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.EBI
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.EBI
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.EBI
Rapt Therapeutics
Discovery of Highly Selective Inhibitors of Calmodulin-Dependent Kinases That Restore Insulin Sensitivity in the Diet-Induced Obesity EBI
University Of Nottingham
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.EBI
Janssen Research & Development
Discovery of Vixotrigine: A Novel Use-Dependent Sodium Channel Blocker for the Treatment of Trigeminal Neuralgia.EBI
Convergence Pharmaceuticals
Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.EBI
Ontario Institute For Cancer Research
Identification and Optimization of Pyrrolidine Derivatives as Highly Potent Ghrelin Receptor Full Agonists.EBI
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.EBI
Astellas Pharma
Exploration of Alternative Scaffolds for P2YEBI
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of 3-Quinazolin-4(3EBI
Luoxin Pharmaceutical (Shanghai) Co.
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of ROR?t.EBI
Phenex Pharmaceuticals
Discovery of CPI-1612: A Potent, Selective, and Orally Bioavailable EP300/CBP Histone Acetyltransferase Inhibitor.EBI
Constellation Pharmaceuticals
Discovery of BMS-986251: A Clinically Viable, Potent, and Selective ROR?t Inverse Agonist.EBI
Bristol Myers Squibb
Discovery of 6-Phenylhexanamide Derivatives as Potent Stereoselective Mitofusin Activators for the Treatment of Mitochondrial Diseases.EBI
The First Affiliated Hospital Of Xi'An Jiao Tong University
Discovery of a lead series of potent benzodiazepine 5-HTEBI
Arena Pharmaceuticals
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.EBI
Haisco Pharmaceutical Group
5,6-Dihydroxypyrimidine Scaffold to Target HIV-1 Nucleocapsid Protein.EBI
Irbm
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.EBI
Sun Yat-Sen University
Novel Autotaxin Inhibitor for the Treatment of Idiopathic Pulmonary Fibrosis: A Clinical Candidate Discovered Using DNA-Encoded Chemistry.EBI
X-Chem
Structure-Based Drug Discovery of EBI
Sosei Heptares
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.EBI
Biogen
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors.EBI
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).EBI
Astrazeneca
Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis.EBI
Washington University School Of Medicine
Discovery of the First Vitamin K Analogue as a Potential Treatment of Pharmacoresistant Seizures.EBI
Ocean University Of China
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.EBI
University Of Washington
Discovery and SARs of 5-Chloro-EBI
Anhui Medical University
Design, synthesis, and enzymatic characterization of quinazoline-based CYP1A2 inhibitors.EBI
University Of Florida
Discovery of Second Generation ROR? Inhibitors Composed of an Azole Scaffold.EBI
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.EBI
De Montfort University
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.EBI
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.EBI
Northwest Agriculture & Forestry University
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.EBI
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.EBI
Arqule
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors.EBI
Amgen
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.EBI
Shenyang Pharmaceutical University
Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research.EBI
Shenyang Pharmaceutical University
SAR Studies and Biological Characterization of a Chromen-4-one Derivative as an Anti-EBI
University Of Modena And Reggio Emilia
Design and Synthesis of Orally Bioavailable 4-Methyl Heteroaryldihydropyrimidine Based Hepatitis B Virus (HBV) Capsid Inhibitors.EBI
Roche Innovation Center Shanghai
Profiling of Flavonol Derivatives for the Development of Antitrypanosomatidic Drugs.EBI
University Of Modena And Reggio Emilia
Discovery of AZD2716: A Novel Secreted Phospholipase AEBI
Astrazeneca
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.EBI
Boehringer Ingelheim (Canada)
Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine ?-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.EBI
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).EBI
Bristol-Myers Squibb Research And Development
Design and synthesis of aminothiazole modulators of the gamma-secretase enzyme.EBI
University Of California
Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors.EBI
Takeda California
Synthesis, structure-activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators.EBI
Sumitomo Dainippon Pharma
N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.EBI
Jagiellonian University Medical College
Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).EBI
Bristol-Myers Squibb
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.EBI
Shionogi
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).EBI
The Scripps Research Institute
Design of Novel Inhibitors of Human Thymidine Phosphorylase: Synthesis, Enzyme Inhibition, in Vitro Toxicity, and Impact on Human Glioblastoma Cancer.EBI
Universidade Federal Do Pampa
Novel non-xanthine antagonist of the AEBI
Bayer Pharmaceuticals
Development of Robust 17(EBI
University Of Texas Southwestern
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaEBI
Xenon Pharmaceuticals
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.EBI
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.EBI
Recordati
Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1 H-pyrrolyl)(phenyl)methyl-1 H-imidazole Derivatives as Antiprotozoal Agents.EBI
"Sapienza" Universit£
Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.EBI
Chung-Ang University
Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.EBI
University Of Toronto
Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.EBI
University Of Washington
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human AEBI
Medical College Of Wisconsin
Discovery of Potent and Selective Non-Nucleotide Small Molecule Inhibitors of CD73.EBI
Arcus Biosciences
Discovery of 8-Methyl-pyrrolo[1,2-EBI
Chinese Academy Of Sciences
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.EBI
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.EBI
Lindsley F. Kimball Research Institute
Identification of Novel Resorcinol Amide Derivatives as Potent and Specific Pyruvate Dehydrogenase Kinase (PDHK) Inhibitors.EBI
Korea University
Discovery and lead optimisation of a potent, selective and orally bioavailable RAR? agonist for the potential treatment of nerve injury.EBI
King'S College
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.EBI
Janssen Research & Development
Benzothiazole-based compounds as potent endothelial lipase inhibitors.EBI
Bristol-Myers Squibb
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.EBI
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.EBI
TBA
Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists.EBI
Japan Tobacco
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as ROR?t inverse agonists.EBI
Bristol-Myers Squibb
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.EBI
Biogen
Design and synthesis of a novel series of cyanoindole derivatives as potent ?-secretase modulators.EBI
Janssen Research & Development
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.EBI
Sabila Biosciences
Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.EBI
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.EBI
Sun Yat-Sen University
Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.EBI
Peking Union Medical College And Chinese Academy Of Medical Sciences
CN128: A New Orally Active Hydroxypyridinone Iron Chelator.EBI
Zhejiang University
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.EBI
Shandong University
Discovery of BAY-985, a Highly Selective TBK1/IKK? Inhibitor.EBI
Bayer
Synthesis and structure-activity relationship studies of ?-naphthoflavone derivatives as CYP1B1 inhibitors.EBI
Shanghai Jiao Tong University
Isolation, Structural Identification, Synthesis, and Pharmacological Profiling of 1,2-EBI
University Of Oxford
Discovery of the Oral Leukotriene C4 Synthase Inhibitor (1EBI
Orexo
Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.EBI
TBA
Novel MEBI
Vanderbilt University
Synthesis and evaluation of thieno[3,2-d]pyrimidine derivatives as novel FMS inhibitors.EBI
Chung-Ang University
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.EBI
Advinus Therapeutics
Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.EBI
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 HEBI
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.EBI
Shandong University
Discovery of Clinical Candidate (1EBI
Newlink Genetics
Discovery of a Potent and Selective CCR4 Antagonist That Inhibits TEBI
Rapt Therapeutics
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.EBI
Shanghai Hengrui Pharmaceutical
Discovery of BNC375, a Potent, Selective, and Orally Available Type I Positive Allosteric Modulator of ?7 nAChRs.EBI
Bionomics
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.EBI
Astrazeneca
Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.EBI
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.EBI
Shanghai Hengrui Pharmaceutical
Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties.EBI
Shandong University
Design and Identification of a Novel, Functionally Subtype Selective GABAEBI
Pfizer
Novel Chemical Series of 5-Lipoxygenase-Activating Protein Inhibitors for Treatment of Coronary Artery Disease.EBI
TBA
Discovery and pharmacological evaluation of indole derivatives as potent and selective ROR?t inverse agonist for multiple autoimmune conditions.EBI
Advinus Therapeutics
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.EBI
Japanese Foundation For Cancer Research
Identification of Isoform 2 Acid-Sensing Ion Channel Inhibitors as Tool Compounds for Target Validation Studies in CNS.EBI
Promidis
Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active ROR?t Inverse Agonists.EBI
Bristol-Myers Squibb
1EBI
Janssen Research & Development
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.EBI
Bristol-Myers Squibb Research & Development
Discovery of a New Sulfonamide Hepatitis B Capsid Assembly Modulator.EBI
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.EBI
Bristol-Myers Squibb
Maximizing ER-? Degradation Maximizes Activity in a Tamoxifen-Resistant Breast Cancer Model: Identification of GDC-0927.EBI
Seragon Pharmaceuticals
Discovery of new indole-based acylsulfonamide NaEBI
Bristol-Myers Squibb Research And Development
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.EBI
Gwangju Institute Of Science And Technology
Discovery of potent and selective PPAR?/? dual antagonists and initial biological studies.EBI
Inception Sciences
Lead generation and optimization of novel GPR119 agonists with a spirocyclic cyclohexane structure.EBI
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.EBI
Bayer
Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1.EBI
Birla Institute Of Technology
Adaptable Small Ligand of CYP1 Enzymes for Use in Understanding the Structural Features Determining Isoform Selectivity.EBI
Seoul National University
Discovery of Clinical Candidate BMS-823778 as an Inhibitor of Human 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD-1).EBI
Bristol-Myers Squibb
Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl.EBI
Ube Industries
Discovery and Characterization of the Potent and Selective P2X4 Inhibitor EBI
Bayer
Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.EBI
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.EBI
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.EBI
Chinese Academy Of Sciences
Targeting DNA Repair in Tumor Cells via Inhibition of ERCC1-XPF.EBI
University Of Alberta
Design and synthesis of selective CYP1B1 inhibitor via dearomatization of ?-naphthoflavone.EBI
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 (mGluEBI
Vanderbilt University
Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders.EBI
Abide Therapeutics
Fragment Based Optimization of Metabotropic Glutamate Receptor 2 (mGluR2) Positive Allosteric Modulators in the Absence of Structural Information.EBI
Gedeon Richter
Building Bridges in a Series of Estrogen Receptor Degraders: An Application of Metathesis in Medicinal Chemistry.EBI
Astrazeneca
Discovery of a Novel Selective Dual Peroxisome Proliferator-Activated Receptor ?/? Agonist for the Treatment of Primary Biliary Cirrhosis.EBI
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.EBI
University Of South Australia
Re-exploration of the mGlu? PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.EBI
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.EBI
Astrazeneca
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-?-D-ribose 2'-oxidase.EBI
Astrazeneca
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.EBI
Eli Lilly
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.EBI
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.EBI
East China Normal University
6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CBEBI
Janssen Research & Development
Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents.EBI
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.EBI
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.EBI
Japan Tobacco
Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists.EBI
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.EBI
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.EBI
Chinese Academy Of Sciences
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-? agonists (SERBAs).EBI
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 hNaEBI
Xenon Pharmaceuticals
Design, synthesis, and biological evaluation of a series of resorcinol-based N-benzyl benzamide derivatives as potent Hsp90 inhibitors.EBI
Keimyung University
Structure-Based Design of 1-Heteroaryl-1,3-propanediamine Derivatives as a Novel Series of CC-Chemokine Receptor 5 Antagonists.EBI
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.EBI
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 mGluEBI
Vanderbilt University
Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.EBI
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.EBI
Shionogi
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.EBI
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 EPEBI
Glaxosmithkline
Design, synthesis and biological evaluation of novel 7-azaspiro[3.5]nonane derivatives as GPR119 agonists.EBI
Taisho Pharmaceutical
Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors.EBI
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.EBI
Sun Yat-Sen University
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.EBI
Astrazeneca
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.EBI
Shanghai Haiyan Pharmaceutical Technology
Design of Selective sPLAEBI
Astrazeneca
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.EBI
Shanghai Haihe Pharmaceutical
Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.EBI
University Of Modena And Reggio Emilia
Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.EBI
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.EBI
TBA
Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.EBI
Vanderbilt University
Discovery of Potent and Selective AEBI
Advinus Therapeutics
Design and synthesis of novel and potent GPR119 agonists with a spirocyclic structure.EBI
Japan Tobacco
Pharmacology and in vivo efficacy of pyridine-pyrimidine amides that inhibit microtubule polymerization.EBI
Frost Biologic
Discovery of selective 2,4-diaminoquinazoline toll-like receptor 7 (TLR 7) agonists.EBI
Janssen Infectious Diseases Diagnostics
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist.EBI
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.EBI
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.EBI
De Montfort University
Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.EBI
Idorsia Pharmaceuticals
Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.EBI
Wuxi Apptec (Shanghai)
Highly potent and selective NaEBI
Pfizer
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).EBI
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).EBI
Peloton Therapeutics
Design, synthesis, structure-activity relationships study and X-ray crystallography of 3-substituted-indolin-2-one-5-carboxamide derivatives as PAK4 inhibitors.EBI
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).EBI
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.EBI
Washington State University
Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-Kinase Inhibitors for Cancer Treatment.EBI
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.EBI
Bristol-Myers Squibb Research And Development
Aminoisoxazoles as Potent Inhibitors of Tryptophan 2,3-Dioxygenase 2 (TDO2).EBI
Genentech
Discovery of EBI
Cytokinetics
Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV).EBI
Janssen Pharmaceutical Companies Of Johnson & Johnson
Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.EBI
Glaxosmithkline
Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.EBI
Japan Tobacco
Discovery of APD371: Identification of a Highly Potent and Selective CBEBI
Arena Pharmaceuticals
Discovery of VU6005649, a CNS Penetrant mGluEBI
Vanderbilt University
Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.EBI
TBA
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.EBI
Astrazeneca
Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.EBI
Janssen Pharmaceutica
Design and Synthesis of EBI
Vanderbilt University School Of Medicine
Discovery of methylsulfonyl indazoles as potent and orally active respiratory syncytial Virus(RSV) fusion inhibitors.EBI
Roche Innovation Center Shanghai
Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.EBI
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.EBI
East China University Of Science And Technology
Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.EBI
Pfizer
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.EBI
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.EBI
University Of Liverpool
The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor.EBI
Bristol-Myers Squibb Research And Development
Discovery of evocalcet, a next-generation calcium-sensing receptor agonist for the treatment of hyperparathyroidism.EBI
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.EBI
Wuxi Apptec (Shanghai)
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.EBI
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.EBI
Iteos Therapeutics
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).EBI
Genentech
Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.EBI
Mitsubishi Tanabe Pharma
Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3? inhibitors.EBI
Mitsubishi Tanabe Pharma
Synthesis and biological evaluation of pyrrole-based chalcones as CYP1 enzyme inhibitors, for possible prevention of cancer and overcoming cisplatin resistance.EBI
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.EBI
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).EBI
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.EBI
Corcept Therapeutics
Discovery and Preclinical Development of IIIM-290, an Orally Active Potent Cyclin-Dependent Kinase Inhibitor.EBI
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.EBI
Vanderbilt University
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine HEBI
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.EBI
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)EBI
Sage Therapeutics
Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.EBI
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.EBI
Vanderbilt University Institute Of Imaging Science
Therapeutic potentials of baicalin and its aglycone, baicalein against inflammatory disorders.EBI
Tripura University
Challenges in the development of an MEBI
Vanderbilt University School Of Medicine
Inhibitors of cytochrome P450 (CYP) 1B1.EBI
Universit£
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.EBI
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.EBI
Medifron Dbt
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.EBI
Janssen Pharmaceutica
Optimization of MEBI
Vanderbilt University Medical Center
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.EBI
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.EBI
The University Of Arizona
Development of Stem-Cell-Mobilizing Agents Targeting CXCR4 Receptor for Peripheral Blood Stem Cell Transplantation and Beyond.EBI
National Health Research Institutes
Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.EBI
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-dihydroisoquinEBI
Wuxi Apptec
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88EBI
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.EBI
Galapagos
Identification of highly potent and selective PI3K? inhibitors.EBI
Bristol-Myers Squibb
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.EBI
Genentech
Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).EBI
Celgene
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.EBI
Wuxi Apptec (Shanghai)
Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.EBI
Mochida Pharmaceutical
Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity.EBI
University Of Waterloo
The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.EBI
Wuxi Apptec (Shanghai)
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.EBI
Emory University
Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure.EBI
Bayer
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.EBI
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.EBI
Bristol-Myers Squibb
Selective IEBI
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.EBI
Astrazeneca
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.BDB
Wyeth Research
Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity.BDB
Pfizer