BindingDB logo
myBDB logout

279 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
28591512 114 Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines.EBI GlaxoSmithKline
28230986 7 Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease.EBI FORUM Pharmaceuticals
28038328 17 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
28072531 120 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
28111141 58 The design and synthesis of novel spirocyclic heterocyclic sulfone ROMK inhibitors as diuretics.EBI Merck & Co. Inc
28089699 63 Investigation of piperazine benzamides as human▀EBI Merck & Co. Inc
28337320 21 Discovery and Assessment of Atropisomers of (▒)-Lesinurad.EBI WuXi AppTec
28523106 1 Discovery of Fluorine-Containing Benzoxazinyl-oxazolidinones for the Treatment of Multidrug Resistant Tuberculosis.EBI Peking Union Medical College and Chinese Academy of Medical Sciences
28254166 81 Discovery of novel BTK inhibitors with carboxylic acids.EBI Merck & Co. Inc
28151659 89 Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases.EBI Queen Mary University of London
28064141 12 Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.EBI University of Modena and Reggio Emilia
28523109 79 Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.EBI GlaxoSmithKline
28185720 42 Discovery of phenyl acetamides as potent and selective GPR119 agonists.EBI Merck & Co.
27958732 93 Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes asa7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.EBI Bristol-Myers Squibb Co.
27855359 15 Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease.EBI Korea Institute of Science and Technology
27914948 36 Triazolopyridine ethers as potent, orally active mGluEBI Bristol-Myers Squibb Co.
27517811 12 Synthesis and T-type calcium channel-blocking effects of aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamides for neuropathic pain treatment.EBI Korea Institutes of Science and Technology (KIST)
27769670 5 Bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones: New classes of antibacterial/antifungal agents.EBI University of Kentucky
28105289 51 Development of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes] asa7 Nicotinic Receptor Agonists.EBI Bristol-Myers Squibb Research and Development
27866818 84 The discovery of quinoline based single-ligand human HEBI GlaxoSmithKline
27836401 57 Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.EBI Eli Lilly and Company
27815121 132 Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.EBI Merck & Co.
27994755 18 Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.EBI Merck & Co.
27994747 66 Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.EBI Merck & Co.
27994738 50 Sulfonamides as Selective NaEBI Amgen Inc
27994728 23 Pyrazole Inhibitors of GluN2B NMDA Receptor Subunit.EBI Dart Neuroscience LLC
27789141 58 II. Discovery of a novel series of CXCR3 antagonists with a beta amino acid core.EBI Sanofi Co. Ltd
27780638 65 5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.EBI University of Washington
27769623 21 Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core.EBI Ocean University of China
27769621 109 Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.EBI Amgen Inc
27736063 34 Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists.EBI University of Chinese Academy of Sciences
27564532 3 Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.EBI Bristol-Myers Squibb Research and Development
27933954 122 Discovery of [5-Amino-1-(2-methyl-3H-benzimidazol-5-yl)pyrazol-4-yl]-(1H-indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.EBI Chugai Pharmaceutical Co. Ltd
27709945 62 Design, Synthesis, and Biological Evaluation of Novel Tetrahydroprotoberberine Derivatives (THPBs) as SelectiveaEBI Chinese Academy of Sciences
27690432 75 Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI CHARLES RIVER DISCOVERY RESEARCH SERVICES UK LIMITED
27637151 35 Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 1.EBI Shionogi & Co., Ltd
27583770 82 Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two LockeEBI Bristol-Myers Squibb Research and Development
27548392 76 Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.EBI Janssen Research and Development LLC
27527804 109 Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).EBI Teva Branded Pharmaceutical Products R & D, Inc.
27660692 70 Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-┐ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.EBI Infinity Pharmaceuticals Inc
27634196 60 Discovery of novel 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives as orally bioavailable TRPV4 antagonists for the treatment of pain: Part 2.EBI Shionogi & Co., Ltd
27564135 499 1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists.EBI Aptuit s.r.l
27502700 36 Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.EBI Novartis Institutes of Biomedical Research (NIBR)
27326332 66 Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARa Selective Agonist.EBI Bristol-Myers Squibb Co.
27078757 121 Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).EBI AstraZeneca
27096048 80 Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders.EBI Peking Union Medical College and Chinese Academy of Medical Sciences
27256912 36 Discovery of hydroxyl 1,2-diphenylethanamine analogs as potent cholesterol ester transfer protein inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
27190600 48 Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.EBI Merck Research Laboratories
26999509 7 Discovery of Potent Benzofuran-Derived Diapophytoene Desaturase (CrtN) Inhibitors with Enhanced Oral Bioavailability for the Treatment of Methicillin-Resistant Staphylococcus aureus (MRSA) Infections.EBI East China University of Science and Technology
27096041 27 Core Replacements in a Potent Series of VEGFR-2 Inhibitors and Their Impact on Potency, Solubility, and hERG.EBI Novartis Institutes for BioMedical Research
27038498 33 Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.EBI Gilead Sciences Inc
26985319 36 Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.EBI AstraZeneca
27229618 30 Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold.EBI Saint Petersburg State University
27173799 97 Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics.EBI Shanghai Institute of Materia Medica
27106708 130 The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.EBI Merck Research Laboratories
27003636 51 Synthesis and Biological Evaluation of Novels1 Receptor Ligands for Treating Neuropathic Pain: 6-Hydroxypyridazinones.EBI Huazhong University of Science and Technology
26985317 20 Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.EBI Bristol-Myers Squibb Research & Development
26985314 23 Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain A▀ Reduction in Rodents.EBI Bristol-Myers Squibb Co.
26985309 8 Astemizole Derivatives as Fluorescent Probes for hERG Potassium Channel Imaging.EBI Shandong University
27117428 50 1-Sulfonyl-6-Piperazinyl-7-Azaindoles as potent and pseudo-selective 5-HT6 receptor antagonists.EBI Selvita S.A.
26937601 55 Structure-Based Design of an Iminoheterocyclic▀-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central A▀ in Nonhuman Primates.EBI Merck Research Laboratories
26924461 45 Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.EBI Bristol-Myers Squibb Research and Development
27117261 31 Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.EBI Takeda Pharmaceutical Co., Ltd
27017115 77 Differentiation of ROMK potency from hERG potency in the phenacetyl piperazine series through heterocycle incorporation.EBI Merck Research Laboratories
26876931 36 Optimization of N'-(arylsulfonyl)pyrazoline-1-carboxamidines by exploiting a novel interaction site in the 5-HT6 antagonistic binding pocket.EBI Abbott Healthcare Products BV
26756222 70 Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.EBI Pfizer Inc
26951750 59 Identification of a 5-[3-phenyl-(2-cyclic-ether)-methylether]-4-aminopyrrolo[2,3-d]pyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26923695 43 Novel 2,4-diaminopyrimidines bearing tetrahydronaphthalenyl moiety against anaplastic lymphoma kinase (ALK): Synthesis, in vitro, ex vivo, and in vivo efficacy studies.EBI Chungbuk National University
27055939 2 Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.EBI GlaxoSmithKline
26852363 72 Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.EBI Merck KGaA
26951894 376 1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists.EBI Aptuit s.r.l
26898814 154 SAR exploration at the C-3 position of tetrahydro-▀-carboline sstr3 antagonists.EBI Merck Research Laboratories
26819673 55 Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.EBI AstraZeneca
26900657 1 New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold.EBI University of Ljubljana
26935940 23 Emerging targets and new small molecule therapies in Parkinson's disease treatment.EBI School of Medicine of University of Electronic Science and Technology of China
26751273 92 Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.EBI GlaxoSmithKline
26736071 79 Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.EBI Takeda Pharmaceutical Co., Ltd
26713112 36 Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.EBI Genentech
26704965 229 Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models.EBI University of Illinois at Chicago
26700945 68 Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome.EBI National Institute of Biological Sciences, Beijing
26709102 142 Discovery of Vibegron: A Potent and Selective▀3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.EBI Merck Research Laboratories
26804230 48 Optimization of tetrahydronaphthalene inhibitors of Raf with selectivity over hERG.EBI Takeda Pharmaceutical Co., Ltd
26652717 96 Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent.EBI BioMarin Pharmaceutical Inc
26761776 62 Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent.EBI Sungkyunkwan University
26747393 4 Discovery and preclinical evaluation of potent, orally bioavailable, metabolically stable cyclopropylindolobenzazepine acylsulfonamides as thumb site 1 inhibitors of the hepatitis c virus NS5B RNA-dependent, RNA polymerase.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
26653180 61 Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors.EBI Eli Lilly and Company
26640981 3 Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?EBI University of Belgrade
26684851 86 Preliminary investigation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4-one derivatives as a novel series of mGlu5 receptor positive allosteric modulators with efficacy in preclinical models of schizophrenia.EBI Janssen Pharmaceutica NV
 29 Synthesis and structure-activity relationships of novel 3′-Hty-substituted pneumocandinsEBI TBA
28156111 214 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
28152427 1 Discovery of 1-(3-(benzyloxy)pyridin-2-yl)-3-(2-(piperazin-1-yl)ethyl)urea: A new modulator for amyloid beta-induced mitochondrial dysfunction.EBI Korea Institute of Science and Technology (KIST)
28106991 136 Discovery of a Phosphoinositide 3-Kinase (PI3K) ?/? Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3K? Potency in a PI3K?-Selective Template by Targeting Nonconserved Asp856.EBI Gilead Sciences, Inc.
27017549 15 Design and synthesis of new potent anticancer benzothiazole amides and ureas featuring pyridylamide moiety and possessing dual B-Raf(V600E) and C-Raf kinase inhibitory activities.EBI Korea Institute of Science and Technology (KIST)
26996374 75 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
26590100 42 Discovery of benzamides as potent human ?3 adrenergic receptor agonists.EBI Merck and Co.
26568411 68 Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration.EBI Novartis Institutes for BioMedical Research
26505898 123 Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.EBI Novartis Institutes for Biomedical Research
26547056 36 Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.EBI Gwangju Institute of Science and Technology (GIST)
26519929 3 Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel.EBI Leiden University
26509640 234 Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.EBI AbbVie Bioresearch Center
26363507 88 Synthesis and SAR of Imidazo[1,5-a]pyridine derivatives as 5-HT4 receptor partial agonists for the treatment of cognitive disorders associated with Alzheimer's disease.EBI Suven Life Sciences Ltd.
26561979 42 Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.EBI Merck & Co., Inc.
26546213 56 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.EBI Corcept Therapeutics
26531152 23 Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.EBI Eisai Limited
26212776 69 Discovery of novel triazolobenzazepinones as ?-secretase modulators with central A?42 lowering in rodents and rhesus monkeys.EBI Merck Research Laboratories Boston
24513046 28 Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel.EBI AstraZeneca
24410637 86 Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.EBI AstraZeneca
24900814 2 Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.EBI Seoul National University
24099149 7 Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.EBI University of Cape Town
24521299 2 Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.EBI Bristol-Myers Squibb Research and Development
24446664 6 2,4-Diaminothienopyrimidines as orally active antimalarial agents.EBI University of Cape Town
24224729 4 Imidazopyridazine hepatitis C virus polymerase inhibitors. Structure-activity relationship studies and the discovery of a novel, traceless prodrug mechanism.EBI GlaxoSmithKline Research & Development
24462667 28 New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.EBI Merck Research Laboratories
24412109 18 Successful reduction of off-target hERG toxicity by structural modification of a T-type calcium channel blocker.EBI The Catholic University of Korea
24900603 3 Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties.EBI Merck Serono
24224763 51 Removal of human ether-Ó-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues.EBI Leiden University
23795771 94 Selective cannabinoid receptor type 2 (CB2) agonists: optimization of a series of purines leading to the identification of a clinical candidate for the treatment of osteoarthritic pain.EBI Lilly Research Laboratories
24071446 39 Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors.EBI China Pharmaceutical University
24063433 72 Structure-activity relationships and discovery of a G protein biased ? opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain.EBI Trevena, Inc.
23927720 2 Cell-based medicinal chemistry optimization of high-throughput screening (HTS) hits for orally active antimalarials. Part 1: challenges in potency and absorption, distribution, metabolism, excretion/pharmacokinetics (ADME/PK).EBI Calibr
23927599 1 Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries.EBI University of Cape Town
23968823 8 Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.EBI GlaxoSmithKline
23930994 67 Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).EBI AstraZeneca
23978358 28 N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.EBI H. Lundbeck A/S
23842474 53 Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507.EBI AstraZeneca
23816371 6 Identification of N-substituted 8-azatetrahydroquinolone derivatives as selective and orally active M(1) and M(4) muscarinic acetylcholine receptors agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
23743277 38 Potent MCH-1 receptor antagonists from cis-1,4-diaminocyclohexane-derived indane analogs.EBI Hoffmann-La Roche Inc.
23711922 19 The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.EBI Takeda Pharmaceutical Company Limited
23711770 4 Synthesis and pharmacological properties of a new hydrophilic and orally bioavailable 5-HT4 antagonist.EBI Drug Discovery Laboratory AS
23566515 23 Synthesis and structure-activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors.EBI Penn State University College of Medicine
23566517 69 Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.EBI Pfizer Inc.
23126626 76 Core refinement toward permeable ?-secretase (BACE-1) inhibitors with low hERG activity.EBI AstraZeneca
21055935 2 Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.EBI AstraZeneca
16337790 53 Aminoalkyl phenyl sulfones--a novel series of 5-HT7 receptor ligands.EBI Merck Sharp and Dohme Research Laboratories
30130718 21 Design, synthesis and biological evaluation of novel thiazolidinedione derivatives as irreversible allosteric IKK-? modulators.EBI Korea Institute of Science and Technology (KIST)
30383372 190 Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.EBI Huazhong University of Science and Technology
30339387 114 6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CBEBI Janssen Research & Development
30196060 39 Structure-based drug design: Synthesis and biological evaluation of quinazolin-4-amine derivatives as selective Aurora A kinase inhibitors.EBI Sun Yat-sen University
30098482 1 Pyrazinyl ureas revisited: 1-(3-(Benzyloxy)pyrazin-2-yl)-3-(3,4-dichlorophenyl)urea, a new blocker of A?-induced mPTP opening for Alzheimer's disease.EBI Korea Institute of Science and Technology (KIST)
30006171 2 Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.EBI Sanwa Kagaku Kenkyusho Co., Ltd.
30429950 98 Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.EBI Merck & Co.
30429949 59 Discovery and Pharmacology of a Novel Somatostatin Subtype 5 (SSTR5) Antagonist: Synergy with DPP-4 Inhibition.EBI Merck & Co.
30346772 124 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
30344914 37 Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel.EBI GlaxoSmithKline
30177375 16 Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPAR? derived from the AT1R antagonist, Fimasartan.EBI Boryung Pharmaceuticals Co. Ltd.
30143425 12 Design and synthesis of tetrahydropyridopyrimidine based Toll-Like Receptor (TLR) 7/8 dual agonists.EBI Janssen Infectious Diseases
28918096 47 A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.EBI Nirma University
30429097 29 PPAR?-sparing thiazolidinediones as insulin sensitizers. Design, synthesis and selection of compounds for clinical development.EBI SPTanis PharmaChem Consulting LLC
30392954 57 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
30278333 40 Development of high potent and selective Bcl-2 inhibitors bearing the structural elements of natural product artemisinin.EBI Shanghai Institute of Materia Medica (SIMM)
30243592 23 Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.EBI EMD Serono Research & Development Institute, Inc.
30457865 7 Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.EBI GlaxoSmithKline
30431269 41 Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.EBI Pfizer Inc.
30407821 21 Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA).EBI Novartis Institutes for BioMedical Research
30337231 47 Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (CaEBI Janssen Research & Development, L.L.C.
30265805 71 Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases.EBI SIB Swiss Institute of Bioinformatics
29541366 64 Novel Staphyloxanthin Inhibitors with Improved Potency against Multidrug Resistant EBI East China University of Science and Technology
29335214 10 Inávivo potent BM635 analogue with improved drug-like properties.EBI Sapienza University of Rome
29324345 122 Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.EBI Shanghai Institute of Materia Medica
29291438 46 Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HTEBI Shanghai Institute of Pharmaceutical Industry
30234300 70 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
30215258 228 Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic ?EBI University of Strathclyde
30207721 58 A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.EBI University of Dundee
30122225 25 Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.EBI EMD Serono Research & Development Institute, Inc.
30104093 5 2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas' disease.EBI University of Dundee
30054191 66 Synthesis and evaluation of an orally available "Y"-shaped biaryl peroxisome proliferator-activated receptor ? agonist.EBI Daegu-Gyeongbuk Medical Innovation Foundation
29871847 26 Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety.EBI The Ohio State University
29688015 67 Blocking Alcoholic Steatosis in Mice with a Peripherally Restricted Purine Antagonist of the Type 1 Cannabinoid Receptor.EBI RTI International
29681484 16 Design, synthesis, and structure-activity relationships of novel imidazo[4,5-c]pyridine derivatives as potent non-nucleoside inhibitors of hepatitis C virus NS5B.EBI Shenyang Pharmaceutical University
29655612 10 Practical application of ligand efficiency metrics in lead optimisation.EBI AstraZeneca
29576271 47 2,4-Diamino-8-quinazoline carboxamides as novel, potent inhibitors of the NAD hydrolyzing enzyme CD38: Exploration of the 2-position structure-activity relationships.EBI GlaxoSmithKline Research and Development
29482950 43 Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.EBI University of Auckland
29452839 82 Development of selective inhibitors for the treatment of rheumatoid arthritis: (R)-3-(3-(Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile as a JAK1-selective inhibitor.EBI Seoul National University
30216722 77 Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.EBI Carna Biosciences, Inc.
30204441 1 Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.EBI AstraZeneca
30189136 5 Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines.EBI AstraZeneca
30149709 33 Discovery of Indole Derivatives as Novel and Potent Dengue Virus Inhibitors.EBI Cistim Leuven vzw
30148362 36 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
30137981 53 Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.EBI Novartis Institutes for BioMedical Research
30128072 68 Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.EBI AstraZeneca
30034607 60 Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.EBI Shanghai Haiyan Pharmaceutical Technology Co. Ltd.
30034595 7 MK-7622: A First-in-Class MEBI Merck & Co.
30034586 90 Design of Selective sPLAEBI AstraZeneca
29494843 29 Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists.EBI Soochow University
29459274 69 Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.EBI Shanghai HaiHe Pharmaceutical, Co. Ltd
29407968 28 Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.EBI University of Modena and Reggio Emilia
29952567 107 Discovery of a Potent, Orally Bioavailable PI4KIII? Inhibitor (UCB9608) Able To Significantly Prolong Allogeneic Organ Engraftment in Vivo.EBI UCB Pharma
29944371 79 Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.EBI Pfizer Inc.
29890830 112 Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces.EBI WuXi Apptec (Tianjin) Co. Ltd.
29886732 300 Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.EBI Dart NeuroScience LLC
29733614 47 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
28938137 30 Synthesis and biological evaluation of novel 6,11-dihydro-5H-benzo[e]pyrimido- [5,4-b][1,4]diazepine derivatives as potential c-Met inhibitors.EBI Shanghai Institute of Pharmaceutical Industry
28835799 28 Discovery of Potent EV71 Capsid Inhibitors for Treatment of HFMD.EBI WuXi AppTec (Shanghai) Co. Ltd
29767973 260 Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.EBI National Center for Advancing Translational Sciences
29767967 74 Structure-Guided Modification of Heterocyclic Antagonists of the P2YEBI National Institute of Diabetes and Digestive and Kidney Diseases
29763304 60 Synthesis, Structure-Activity Relationships, and Preclinical Evaluation of Heteroaromatic Amides and 1,3,4-Oxadiazole Derivatives as 5-HTEBI Suven Life Sciences Limited
29429832 77 Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships.EBI Beijing University of Technology
29153425 69 Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [EBI University of Kentucky
28818461 67 Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.EBI Nestl� Skin Health R&D
29613789 138 Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.EBI Pfizer Inc.
29596745 13 Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.EBI Sanofi R&D
29116786 265 Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.EBI Idorsia Pharmaceuticals Ltd.
29107541 16 Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.EBI University of Auckland
29074257 115 Discovery and evaluation of CaEBI Idorsia Pharmaceuticals Ltd.
29042223 8 Astemizole analogues with reduced hERG inhibition as potent antimalarial compounds.EBI KU Leuven
29037948 70 Discovery of aminocyclohexene analogues as selective and orally bioavailable hNav1.7 inhibitors for analgesia.EBI WuXi AppTec (Shanghai) Co. Ltd
29029933 45 Highly potent and selective NaEBI Pfizer Inc.
29017786 35 Identification of novel PI3K inhibitors through a scaffold hopping strategy.EBI Spanish National Cancer Research Centre (CNIO)
28445047 46 Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis.EBI Novartis Institutes for BioMedical Research
28287730 89 Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.EBI Wuxi AppTec
30350997 111 Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic ? Receptor Ligands with Exocyclic Amino Moiety.EBI Universit£t M£nster
30091600 48 A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-oneEBI Astex Pharmaceuticals
30052039 172 Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties.EBI Emory University
29683659 127 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
30080045 42 Discovery of Novel Aminotetralines and Aminochromanes as Selective and Competitive Glycine Transporter 1 (GlyT1) Inhibitors.EBI AbbVie Deutschland GmbH & Co. KG
29927604 90 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
29328999 4 Discovery of novel piperonyl derivatives as diapophytoene desaturase inhibitors for the treatment of methicillin-, vancomycin- and linezolid-resistant Staphylococcus aureus infections.EBI East China University of Science and Technology
29906396 10 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
29456800 47 Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors.EBI Pfizer Inc.
29456796 51 Discovery of Tetralones as Potent and Selective Inhibitors of Acyl-CoA:Diacylglycerol Acyltransferase 1.EBI GlaxoSmithKline
29259755 55 Discovery of JTZ-951: A HIF Prolyl Hydroxylase Inhibitor for the Treatment of Renal Anemia.EBI Japan Tobacco Inc.
29259753 70 Discovery of APD371: Identification of a Highly Potent and Selective CBEBI Arena Pharmaceuticals
29259752 1 Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.EBI Merck KGaA (Darmstadt, Germany)
29259743 52 Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.EBI Boehringer Ingelheim Pharma GmbH & Co. KG
29965759 26 2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.EBI Janssen Infectious Diseases-Diagnostics BVBA
29909635 160 Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.EBI AstraZeneca
29809004 50 Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.EBI Janssen Pharmaceutica NV
29152045 74 Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.EBI Shenyang Pharmaceutical University
28987606 3 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.EBI Shanghai Institute of Materia Medica
29057044 13 6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis.EBI University of Auckland
28947942 55 Discovery of an Isothiazole-Based Phenylpropanoic Acid GPR120 Agonist as a Development Candidate for Type 2 Diabetes.EBI Janssen Research and Development LLC
29889526 4 Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.EBI University of Cape Town
29878763 27 Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents.EBI Pfizer Inc
29847724 25 Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase? (PI3K?) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS).EBI Vertex Pharmaceuticals Inc
29852070 101 Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.EBI Pharmaron-Beijing Co., Ltd
29752182 52 Discovery of a bicyclo[4.3.0]nonane derivative DS88790512 as a potent, selective, and orally bioavailable blocker of transient receptor potential canonical 6 (TRPC6).EBI Daiichi Sankyo Co., Ltd
28729057 11 Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HTEBI University of Science and Technology
28720503 146 Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.EBI Merck & Co.
28720324 7 Synthesis and diabetic neuropathic pain-alleviating effects of 2N-(pyrazol-3-yl)methylbenzo[d]isothiazole-1,1-dioxide derivatives.EBI Korea University of Science and Technology (UST)
28684121 60 Discovery of a biarylamide series of potent, state-dependent NaEBI Amgen Inc
28493698 56 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 LLC
28426996 21 Design, synthesis, SAR discussion, inávitro and inávivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants.EBI Nanjing Normal University
28481112 2 Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.EBI Shandong University
28459575 5 7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis.EBI University of Auckland
28414242 22 Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary FibEBI Galapagos SASU
28406300 3 Synthesis and Characterization of Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Antibacterial Activity against Gram-Negative Bacteria.EBI Actelion Pharmaceuticals Ltd
28304162 1 Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis.EBI University of Liverpool
28252959 116 Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.EBI Merck & Co. Inc
29627981 45 Discovery of a Novel Small-Molecule Modulator of C-X-C Chemokine Receptor Type 7 as a Treatment for Cardiac Fibrosis.EBI Pfizer Inc
29617572 45 Toward?-Secretase-1 Inhibitors with Improved Isoform Selectivity.EBI AstraZeneca
28431879 123 Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores.EBI Merck & Co.
29381358 65 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
29300474 45 Identification of Morpholino-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-ones as Nonsteroidal Mineralocorticoid Antagonists.EBI Pfizer Inc
29243920 134 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
29211475 65 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
29185748 3 4-Aminoquinoline Antimalarials Containing a Benzylmethylpyridylmethylamine Group Are Active against Drug Resistant Plasmodium falciparum and Exhibit Oral Activity in Mice.EBI University of Cape Town
29172502 96 Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88EBI AstraZeneca
29148763 6 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 NV
28209465 124 Identification of highly potent and selective PI3K? inhibitors.EBI Bristol-Myers Squibb Co.
29461823 2 Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.EBI University of Auckland
29457982 80 Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.EBI Genentech
29283260 113 Targeting Acidic Mammalian chitinase Is Effective in Animal Model of Asthma.EBI OncoArendi Therapeutics SA
28994286 2 Novel Derivative of Bardoxolone Methyl Improves Safety for the Treatment of Diabetic Nephropathy.EBI Crystal Pharmatech Co., Ltd.
28415011 54 Design and synthesis of novel xanthine derivatives as potent and selective AEBI Advinus Therapeutics Ltd
28892629 74 Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1.EBI University of Manchester
28873303 1 Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription.EBI Shanghai Institute of Materia Medica (SIMM)
28408226 51 Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.EBI Mochida Pharmaceutical Co., Ltd
28385504 52 The discovery of tetrahydropyridine analogs as hNav1.7 selective inhibitors for analgesia.EBI WuXi AppTec (Shanghai) Co. Ltd
28385503 19 Novel small molecule guanidine Sigma1 inhibitors for advanced prostate cancer.EBI Drexel University College of Medicine
28574690 98 Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups.EBI Heinrich-Heine-Universit£t D£sseldorf
28541707 119 Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase? (PI3K?) Inhibitor for the Treatment of Immunological Disorders.EBI Bristol-Myers Squibb Co.
28537728 43 Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures.EBI Laboratorium f�r Organische Chemie, ETH Zurich , Vladimir-Prelog-Weg 3, 8093 Zurich, Switzerland.
28498658 47 Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.EBI Pfizer Inc
28489379 165 Hydroxy-Substituted Heteroarylpiperazines: Novel Scaffolds for?-Arrestin-Biased DEBI Friedrich-Alexander University Erlangen-Nuernberg
28430437 19 Discovery of a Hepatitis C Virus NS5B Replicase Palm Site Allosteric Inhibitor (BMS-929075) Advanced to Phase 1 Clinical Studies.EBI Bristol-Myers Squibb Research and Development
28418664 32 Selective IEBI Bristol-Myers Squibb Co.
28347666 45 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