BindingDB logo
myBDB logout

899 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
26522950 60 Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).EBI Novartis Institutes for BioMedical Research
26509551 31 Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.EBI Pfizer Inc.
26475522 81 Acyl dihydropyrazolo[1,5-a]pyrimidinones as metabotropic glutamate receptor 5 positive allosteric modulators.EBI Vanderbilt University Medical Center
26396681 58 Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.EBI Novartis Institutes for Biomedical Research
26363868 10 3-Nitrotriazole-based piperazides as potent antitrypanosomal agents.EBI NorthShore University HealthSystem
26428869 7 Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists.EBI Sumitomo Dainippon Pharma Co. Ltd.
26355532 18 Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).EBI Korea University of Science and Technology (UST)
26496070 96 Discovery of a Novel, Potent Spirocyclic Series of┐-Secretase Inhibitors.EBI Merck Research Laboratories
26426481 114 Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in SchizophrenicsEBI Vanderbilt University
26360048 21 (2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands.EBI Jagiellonian University Medical College
26144347 27 Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease.EBI University of California
25978966 65 Development of a novel class of potent and selective FIXa inhibitors.EBI Merck Research Laboratories
26403853 32 Discovery of 4-Aryl-5,6,7,8-tetrahydroisoquinolines as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors: In Vivo Evaluation in Rodents and Cynomolgus Monkeys.EBI Roche Pharma Research and Early Development (pRED)
26384287 65 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI Kangwon National University
26313252 22 Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.EBI AstraZeneca
26288697 41 Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.EBI Merck Research Laboratories
26288692 37 Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.EBI Bristol Myers-Squibb Research and Development
26288683 43 Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.EBI Bristol-Myers Squibb R&D
26335039 320 Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.EBI Vanderbilt University Medical Center
26288685 59 Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
26288682 64 Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.EBI Bristol-Myers Squibb Research& Development
26365710 26 Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors.EBI Shenyang Pharmaceutical University
26299347 4 Optimization of a small molecule probe that restores e-cadherin expression.EBI Vanderbilt University Medical Center
26344593 5 Discovery of potent nitrotriazole-based antitrypanosomal agents: In vitro and in vivo evaluation.EBI NorthShore University HealthSystem
26204510 6 4-Fluoro-3',4',5'-trimethoxychalcone as a new anti-invasive agent. From discovery to initial validation in an in vivo metastasis model.EBI Ghent University
26191360 99 Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.EBI Merck Research Laboratories
26231163 50 Discovery of novel bridged tetrahydronaphthalene derivatives as potent T/L-type calcium channel blockers.EBI Actelion Pharmaceuticals Ltd
26259804 23 Tetrahydropyrrolo-diazepenones as inhibitors of ERK2 kinase.EBI Novartis Institutes for BioMedical Research
26134551 25 Novel benzidine and diaminofluorene prolinamide derivatives as potent hepatitis C virus NS5A inhibitors.EBI Seoul National University
26291341 66 Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.EBI AstraZeneca
26225459 48 Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile).EBI Heptares Therapeutics Ltd.
26191364 10 Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.EBI Bristol-Myers Squibb Research
26191358 105 Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).EBI Euroscreen SA
26267483 83 Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.EBI GlaxoSmithKline Research and Development
26183084 53 Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.EBI Vanderbilt University Medical Center
26037322 100 3-Substituted pyrazoles and 4-substituted triazoles as inhibitors of human 15-lipoxygenase-1.EBI Uppsala University
26181851 26 Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.EBI Novartis Institutes for BioMedical Research
26115573 67 Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.EBI Merck Research Laboratories
26105194 24 Design, synthesis and evaluation of MCH receptor 1 antagonists--Part III: Discovery of pre-clinical development candidate BI 186908.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
26091726 41 Discovery and characterization of a potent and selective EP4 receptor antagonist.EBI Lilly Research Laboratories
26181715 73 Bicyclic [3.3.0]-Octahydrocyclopenta[c]pyrrolo Antagonists of Retinol Binding Protein 4: Potential Treatment of Atrophic Age-Related Macular Degeneration and Stargardt Disease.EBI Columbia University Medical Center
25286150 75 Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.EBI AstraZeneca
23033255 177 Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.EBI Tongji University
22328583 132 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.EBI Pfizer Inc.
22205779 11 Cyclosporine A- and tacrolimus-mediated inhibition of CYP3A4 and CYP3A5 in vitro.EBI University of Oslo
25677656 7 A novel molecule with notable activity against multi-drug resistant tuberculosis.EBI University of Georgia
25655723 27 Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.EBI Teva Branded Pharmaceutical Products R&D, Inc.
25577041 7 Benzimidazole-containing HCV NS5A inhibitors: effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency.EBI Vertex Pharmaceuticals Inc
25082126 34 Discovery of novel pyrimidine and malonamide derivatives as TGR5 agonists.EBI Chung-Ang University
25164763 95 Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.EBI Shanghai Institute of Materia Medica
26039570 100 Design, Synthesis, and Structure-Activity Relationships of Pyridine-Based Rho Kinase (ROCK) Inhibitors.EBI Vertex Pharmaceuticals, Inc.
26101566 14 Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.EBI AbbVie, Inc.
26087021 94 Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.EBI TBA
26052884 1 Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides.EBI Jagiellonian University Medical College
26005536 92 Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
26005524 147 Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.EBI Merck Research Laboratories
25992974 14 Synthesis and Biological Evaluation of Novel Olean-28,13▀-lactams as Potential Antiprostate Cancer Agents.EBI China Pharmaceutical University
25879485 60 Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.EBI Seragon Pharmaceuticals
25990761 66 Novel Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa) from Natural Product Anabaenopeptin.EBI Institute for Infection Research
25893048 25 Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.EBI Janssen Pharmaceutical Company
23355637 14 Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity.EBI GlaxoSmithKline
22517972 40 Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.EBI Amgen, Inc.
22496391 40 Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human.EBI Bristol-Myers Squibb Research
22645092 15 Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.EBI Pfizer Inc.
21149541 5 Casopitant: in vitro data and SimCyp simulation to predict in vivo metabolic interactions involving cytochrome P450 3A4.EBI GlaxoSmithKline
21447734 2 Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.EBI Amgen, Inc.
22930276 25 Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.EBI Amgen, Inc
22106171 9 Stereospecific metabolism of itraconazole by CYP3A4: dioxolane ring scission of azole antifungals.EBI University of Washington
22679214 13 Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.EBI University of Washington
23132334 28 In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.EBI GlaxoSmithKline
21068193 1 Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug.EBI University of Michigan
22531045 2 In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.EBI Amgen Inc.
25941547 12 Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.EBI Roche Innovation Center Shanghai
25850459 46 Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep).EBI TBA
25781223 96 Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.EBI The Scripps Research Institute
25763473 108 The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.EBI EntreMed Inc.
25751283 79 Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.EBI Purdue University
25738882 210 Discovery and optimization of novel antagonists to the human neurokinin-3 receptor for the treatment of sex-hormone disorders (Part I).EBI Euroscreen SA
25827402 54 3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.EBI Teva Global R&D.
25734520 104 Design and synthesis of orally bioavailable aminopyrrolidinone histone deacetylase 6 inhibitors.EBI Roche Innovation Center Shanghai
25711516 118 Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.EBI Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
25671290 106 Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).EBI Boehringer Ingelheim Pharmaceuticals
25838147 75 Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.EBI Actelion Pharmaceuticals Ltd
25723005 111 The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent.EBI TBA
25680029 12 Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen.EBI The Institute of Cancer Research
25603482 54 Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.EBI Array BioPharma Inc
25489882 63 Novel 2,4-disubstituted pyrimidines as potent, selective, and cell-permeable inhibitors of neuronal nitric oxide synthase.EBI Northwestern University
25422861 78 In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.EBI National Institute of Diabetes and Digestive and Kidney Diseases
25868743 1 Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives.EBI Jagiellonian University Medical College
25801932 55 Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter.EBI Vanderbilt University Medical Center
25782742 76 trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.EBI Novartis Pharma AG
25754490 44 trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.EBI Novartis Pharma AG
25708617 29 Minimization of drug-drug interaction risk and candidate selection in a natural product-based class of gamma-secretase modulators.EBI Satori Pharmaceuticals, Inc.
25701253 23 Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.EBI H. Lundbeck A/S
25683622 86 Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).EBI Janssen Research and Development
25655721 51 Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3▀ inhibitors for Alzheimer's disease.EBI Mitsubishi Tanabe Pharma Corporation
25699143 26 Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.EBI Pfizer Inc.
25597006 8 Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: non-symmetric inhibitors with potent activity against genotype 1a and 1b.EBI Vertex Pharmaceuticals Inc.
25577040 54 Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.EBI Merck Research Laboratories
25556090 99 Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.EBI Genentech Inc.
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25369539 116 SAR156497, an exquisitely selective inhibitor of aurora kinases.EBI Sanofi
25255283 88 Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.EBI AstraZeneca
25100568 68 Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.EBI AbbVie Inc.
25089810 79 Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia.EBI National Taiwan University
25050172 32 Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.EBI AstraZeneca
25050169 52 Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11▀-Hydroxysteroid Dehydrogenase Type 1 (11▀-HSD-1).EBI Bristol-Myers Squibb
25050166 58 Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.EBI Novartis Institutes for BioMedical Research
25001129 89 Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.EBI Amgen, Inc.
25043312 104 Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.EBI University Health Network
25037916 185 Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.EBI Genentech
25036791 56 Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.EBI National Taiwan University
24980053 153 Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.EBI Bristol-Myers Squibb Company
24974340 90 Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.EBI Korea University
24969015 118 Discovery of VU0431316: a negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.EBI Vanderbilt University Medical Center
24948565 20 Design and optimization of highly-selective fungal CYP51 inhibitors.EBI Viamet Pharmaceuticals Inc.
24939756 28 Strategies for the modulation of phase II metabolism in a series of PKCe inhibitors.EBI Vertex Pharmaceuticals
24867403 156 The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.EBI EntreMed Inc.
24422519 31 Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.EBI Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
25589934 125 Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.EBI Sanofi R&D
25589928 37 Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.EBI Novartis Institutes for Biomedical Research
25575658 83 Selective CB2 receptor agonists. Part 3: the optimization of a piperidine-based series that demonstrated efficacy in an in vivo neuropathic pain model.EBI Boehringer Ingelheim Pharmaceuticals
25556092 85 Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
25516794 71 (7-Benzyloxy-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic Acids as S1P1 Functional Antagonists.EBI Arena Pharmaceuticals, Inc.
25516791 177 Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.EBI Boehringer Ingelheim Pharmaceuticals
25516790 37 Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.EBI Arena Pharmaceuticals, Inc.
25499880 51 Identification of a highly potent and selective CB2 agonist, RQ-00202730, for the treatment of irritable bowel syndrome.EBI RaQualia Pharma Inc
25499431 4 Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein.EBI University of Waterloo
25455487 4 Serendipitous discovery of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine derivatives as novel HIV-1 replication inhibitors.EBI Institut Pasteur Korea
25454273 52 Anilinotriazoles as potent gamma secretase modulators.EBI Janssen Research& Development
25453808 101 Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.EBI Bristol-Myers Squibb Company
25441013 49 Discovery of N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide (VX-770, ivacaftor), a potent and orally bioavailable CFTR potentiator.EBI Vertex Pharmaceuticals Inc
25423411 28 Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).EBI Vanderbilt University School of Medicine
25409491 83 A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.EBI Zhejiang University
25393851 10 Discovery of BI 207524, an indole diamide NS5B thumb pocket 1 inhibitor with improved potency for the potential treatment of chronic hepatitis C virus infection.EBI Boehringer Ingelheim (Canada) Ltd.
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
25330343 49 Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.EBI Translational Research Institute
25310383 50 Potent nonimmunosuppressive cyclophilin inhibitors with improved pharmaceutical properties and decreased transporter inhibition.EBI Novartis Institutes for Biomedical Research
25249180 146 The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.EBI GlaxoSmithKline R&D
25248679 85 Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia.EBI Merck Research Laboratories
25221667 66 Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.EBI Vanderbilt University
25221665 33 Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.EBI Janssen Pharmaceutica NV
25221656 116 Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-a-Oxyazetidine.EBI Korea University
25210858 96 Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.EBI Albany Molecular Research
25193232 32 Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.EBI Genentech Inc.
25179681 81 Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.EBI Chinese Academy of Sciences
25176194 69 The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Na(v)1.7.EBI Xenon Pharmaceuticals Inc.
25148100 9 Discovery of novel highly potent hepatitis C virus NS5A inhibitor (AV4025).EBI Alla Chem LLC
24914612 36 Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).EBI Vanderbilt University Medical Center
24870926 50 Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.EBI Institut Pasteur Korea
24835202 68 Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.EBI AstraZeneca
24139169 175 Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.EBI Nerviano Medical Sciences
24944749 21 Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.EBI Boehringer Ingelheim (Canada)
24914738 43 Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.EBI AstraZeneca
24900882 30 Pivotal Role of an Aliphatic Side Chain in the Development of an HDM2 Inhibitor.EBI Merck Research Laboratories
24900876 56 Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.EBI AstraZeneca
24900870 4 Novel carboline derivatives as potent antifungal lead compounds: design, synthesis, and biological evaluation.EBI Second Military Medical University
24899257 71 Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.EBI Saarland University
24874895 42 Lead optimization of 1,4-azaindoles as antimycobacterial agents.EBI AstraZeneca
24874438 42 Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.EBI Chinese Academy of Sciences
24842618 56 The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.EBI AMRI
24815509 51 Discovery of camphor-derived pyrazolones as 11▀-hydroxysteroid dehydrogenase type 1 inhibitors.EBI Hoffmann-La Roche Inc.
24794746 168 Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy.EBI Aurigene Discovery Technologies Limited
24793360 29 Investigation of a novel series of 2-hydroxyisoquinoline-1,3(2H,4H)-diones as human immunodeficiency virus type 1 integrase inhibitors.EBI Universit£ Lille Nord de France
24785301 83 Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.EBI AstraZeneca
24814197 63 Discovery of novel 2-((pyridin-3-yloxy)methyl)piperazines asa7 nicotinic acetylcholine receptor modulators for the treatment of inflammatory disorders.EBI Critical Therapeutics, Inc.
24786585 200 Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-▀ type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.EBI Ewha Womans University
24779514 128 Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.EBI Gilead Sciences, Inc.
24775307 42 Highly-selective 4-(1,2,3-triazole)-based P450c17a 17,20-lyase inhibitors.EBI Viamet Pharmaceuticals, Inc.
24758746 36 Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.EBI Janssen Research& Development
24755431 59 The discovery of diazepinone-based 5-HT3 receptor partial agonists.EBI AMRI
24755427 107 The discovery of potent and selective non-steroidal glucocorticoid receptor modulators, suitable for inhalation.EBI AstraZeneca
24712661 47 Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor▀ agonist in clinical trials for the treatment of dyslipidemia.EBI Madrigal Pharmaceuticals, Inc.
24689770 4 Optimization of an imidazopyridazine series of inhibitors of Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1).EBI MRC Technology
24685542 67 Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.EBI Bristol-Myers Squibb Research and Development
24182233 57 Reductions in log P improved protein binding and clearance predictions enabling the prospective design of cannabinoid receptor (CB1) antagonists with desired pharmacokinetic properties.EBI Bristol-Myers Squibb
24164628 186 Adenosine A2A receptor as a drug discovery target.EBI Merck Research Laboratories
24630411 38 Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.EBI Merck Research Laboratories
24601644 113 Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.EBI Amgen Inc.
24520947 87 Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.EBI Hoffmann-La Roche Inc.
24512187 69 Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.EBI Pfizer Inc.
24666203 124 Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.EBI Genomics Institute of the Novartis Research Foundation
24641103 104 Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.EBI Amgen Inc.
24630562 58 Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.EBI Merck Research Laboratories
24387221 150 Discovery and optimization of pyrimidone indoline amide PI3K▀ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.EBI Sanofi
24294923 65 Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase.EBI Amgen Inc.
24021582 52 Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.EBI Novartis Institutes for Biomedical Research
24042009 89 Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.EBI Genentech Inc.
23855836 147 1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.EBI Newcastle University
23869452 67 Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.EBI Saarland University
23831134 72 Discovery and optimisation of 1-hydroxyimino-3,3-diphenylpropanes, a new class of orally active GPBAR1 (TGR5) agonists.EBI F. Hoffmann-La Roche AG
23726345 41 Design, synthesis and biological evaluation of novel aminothiazoles as antiviral compounds acting against human rhinovirus.EBI Boehringer Ingelheim (Canada) Ltd.
23726034 117 Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.EBI Novartis Institutes for BioMedical Research
23590342 105 ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.EBI F. Hoffmann-La Roche Ltd
23586711 4 Pyridine-substituted desoxyritonavir is a more potent inhibitor of cytochrome P450 3A4 than ritonavir.EBI University of California
23498916 4 VBP15: preclinical characterization of a novel anti-inflammatory delta 9,11 steroid.EBI ReveraGen BioPharma, Inc.
23466233 20 Synthesis and evaluation of non-dimeric HCV NS5A inhibitors.EBI Veterans Affairs Medical Center
23350847 169 Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.EBI Hoffmann-La Roche Inc.
23570561 80 Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.EBI The Scripps Research Institute
23570514 120 Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3.EBI Sirtris a GSK Company
23560650 46 Synthesis and biological evaluation of a new series of hexahydro-2H-pyrano[3,2-c]quinolines as novel selectives1 receptor ligands.EBI Esteve
23473235 21 Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).EBI Genentech
23402880 51 The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.EBI Bristol-Myers Squibb Research& Development
23317570 42 Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.EBI Merck Research Laboratories
23294830 88 Discovery of INT131: a selective PPAR¿ modulator that enhances insulin sensitivity.EBI Amgen, Inc.
23206863 7 Sulfonylpiperidines as novel, antibacterial inhibitors of Gram-positive thymidylate kinase (TMK).EBI AstraZeneca
23200256 54 Discovery of N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)-4-piperidyl]methyl]-3,5-dichloro-benzamide as a selective T-type calcium channel (Cav3.2) inhibitor.EBI AstraZeneca
23473363 12 Structural basis and SAR for G007-LK, a lead stage 1,2,4-triazole based specific tankyrase 1/2 inhibitor.EBI Oslo University Hospital
23445448 33 Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.EBI Vanderbilt University Medical Center
23394205 106 Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.EBI AstraZeneca
23380375 48 Design, synthesis, and SAR of N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1.EBI AMRI
23379595 55 Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.EBI Merck& Co., Inc.
23374868 76 1-(4-Phenylpiperazin-1-yl)-2-(1H-pyrazol-1-yl)ethanones as novel CCR1 antagonists.EBI ChemoCentryx, Inc.
23317569 57 Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors.EBI OSI Pharmaceuticals, LLC
23294255 114 Development of new cyclic plasmin inhibitors with excellent potency and selectivity.EBI Philipps University Marburg
23253441 3 The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.EBI Merck Research Laboratory
23227781 119 Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.EBI AstraZeneca
23182090 92 Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.EBI Janssen Research and Development, LLC
22921279 2 Armeniaspiroles, a new class of antibacterials: Antibacterial activities and total synthesis of 5-chloro-Armeniaspirole A.EBI Sanofi Research& Development
22765894 223 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.EBI Exelixis
22545772 100 Use of small-molecule crystal structures to address solubility in a novel series of G protein coupled receptor 119 agonists: optimization of a lead and in vivo evaluation.EBI AstraZeneca
22094028 31 Lead optimisation of pyrazoles as novel FPR1 antagonists.EBI AstraZeneca
21955939 49 Discovery of pyrazoles as novel FPR1 antagonists.EBI AstraZeneca
21907579 22 Effect of lipophilicity modulation on inhibition of human rhinovirus capsid binders.EBI AstraZeneca
21669521 44 Selective non zinc binding inhibitors of MMP13.EBI AstraZeneca
19772287 67 p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.EBI GlaxoSmithKline
21414782 178 Phenoxyacetic acids as PPARd partial agonists: synthesis, optimization, and in vivo efficacy.EBI GlaxoSmithKline Pharmaceuticals
16248836 154 Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.EBI F. Hoffmann-La Roche Ltd.
20627722 89 Identification of a sulfonamide series of CCR2 antagonists.EBI GlaxoSmithKline Medicines Research Centre
20097073 68 Synthesis and structure-activity relationships of a series of 3-aryl-4-isoxazolecarboxamides as a new class of TGR5 agonists.EBI GlaxoSmithKline Pharmaceuticals
19664922 35 2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2',3':4,5]thieno[2,3-b]pyridine derivatives as selective progesterone receptor agonists.EBI GlaxoSmithKline
19902954 19 Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.EBI GlaxoSmithKline Pharmaceuticals
18768319 53 N-alkyl-5H-pyrido[4,3-b]indol-1-amines and derivatives as novel urotensin-II receptor antagonists.EBI GlaxoSmithKline
18798607 27 Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
18680280 34 Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.EBI GlaxoSmithKline
23141912 30 Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N1-arylsulfonyl indole derivatives as 5-HT6 receptor ligands.EBI Suven Life Sciences Limited
23107482 82 Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.EBI Genentech
23079519 86 In vivo activity of an azole series of CCR2 antagonists.EBI GlaxoSmithKline Research and Development
23043539 60 Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.EBI The Institute of Cancer Research
22727372 14 Novel retinoic acid 4-hydroxylase (CYP26) inhibitors based on a 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-(4-(phenylamino)phenyl)propyl scaffold.EBI Cardiff University
22651823 57 Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.EBI Pfizer Inc.
22607673 34 Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.EBI Vanderbilt University Medical Center
21486038 177 Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.EBI H. Lundbeck A/S
21604762 152 Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphEBI S*BIO Pte. Ltd.
23153230 8 Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.EBI Bristol-Myers Squibb Research& Development
23116186 68 Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).EBI AstraZeneca
23098566 17 Aminopiperidine sulfonamide Cav2.2 channel inhibitors for the treatment of chronic pain.EBI Merck Research Laboratories
23075267 85 Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.EBI Bristol-Myers Squibb Company
23072213 32 Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.EBI Janssen-Cilag S.A.
23061660 92 Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.EBI Genentech
23061376 63 Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.EBI Roche R&D Center-China Ltd.
23009245 53 Orally active metabotropic glutamate subtype 2 receptor positive allosteric modulators: structure-activity relationships and assessment in a rat model of nicotine dependence.EBI Sanford-Burnham Medical Research Institute
23006002 35 Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor antagonists.EBI Suven Life Sciences Ltd.
22989333 43 Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.EBI Merck Research Laboratories
22849725 28 Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV).EBI Boehringer Ingelheim (Canada) Ltd.
22650177 12 Design and synthesis of a novel series of bicyclic heterocycles as potent¿-secretase modulators.EBI Pharmaceutical Companies of Johnson& Johnson
22533986 181 Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.EBI ArQule Inc.
22468684 76 Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.EBI Amgen Inc.
22437115 66 Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).EBI GlaxoSmithKline R&D
22409598 28 Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.EBI Pfizer Inc.
22924734 87 Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment ofEBI Pfizer Inc.
22905713 9 Identification, synthesis, and biological evaluation of 6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one (AS1940477), a potent p38 MAP kinase inhibitor.EBI Astellas Pharma Inc.
22861813 42 Novelß-amino acid derivatives as inhibitors of cathepsin A.EBI Sanofi-Aventis Deutschland GmbH
22803959 196 Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.EBI Boehringer Ingelheim Pharmaceuticals
22784008 100 Synthesis and biological evaluation of the 1-arylpyrazole class ofs(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862).EBI Esteve
22277094 59 Optimization of hydroxybenzothiazoles as novel potent and selective inhibitors of 17ß-HSD1.EBI Saarland University
23010262 46 Discovery of phosphoinositide 3-kinases (PI3K) p110ß isoform inhibitor 4-[2-hydroxyethyl(1-naphthylmethyl)amino]-6-[(2S)-2-methylmorpholin-4-yl]-1H-pyrimidin-2-one, an effective antithrombotic agent without associated bleeding and insulin resistance.EBI AstraZeneca
23006603 5 Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity.EBI Actelion Pharmaceuticals Ltd
22861193 60 Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.EBI Saarland University& Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)
22801646 49 4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.EBI GlaxoSmithKline R&D
22793372 66 Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor.EBI Vanderbilt University Medical Center
22626259 59 Discovery of novel PI3-kinased specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.EBI Genentech
22497444 55 Discovery and characterization of an inhibitor of glucosylceramide synthase.EBI Exelixis
22191331 6 ADME-guided design and synthesis of aryloxanyl pyrazolone derivatives to block mutant superoxide dismutase 1 (SOD1) cytotoxicity and protein aggregation: potential application for the treatment of amyotrophic lateral sclerosis.EBI Northwestern University
23040895 37 Adamantyl carboxamides and acetamides as potent human 11ß-hydroxysteroid dehydrogenase type 1 inhibitors.EBI University of Bath
22708876 106 Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes.EBI Merck Research Laboratories
22698084 99 Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.EBI Genentech
22697905 21 N'-substituted-2'-O,3'-N-carbonimidoyl bridged macrolides: novel anti-inflammatory macrolides without antimicrobial activity.EBI GlaxoSmithKline Research Centre Zagreb
22039836 188 Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).EBI Johnson& Johnson Pharmaceutical Research& Development
22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
22087535 20 Comparative study of the affinity and metabolism of type I and type II binding quinoline carboxamide analogues by cytochrome P450 3A4.EBI Washington State University
21797275 139 Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.EBI Novartis Institutes for BioMedical Research
22981333 103 Preparation and optimization of new 4-(morpholin-4-yl)-(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives as PI3Kß inhibitors.EBI Sanofi
22975301 128 Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators.EBI Lundbeck Research USA
22642300 160 Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors.EBI Kyoto Prefectural University of Medicine
22938786 86 Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.EBI Dainippon Sumitomo Pharma Co., Ltd
22884988 49 Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus.EBI Amgen Inc.
22858142 121 Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.EBI AstraZeneca
22853998 164 Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles.EBI Shionogi& Co., Ltd.
22850208 60 Dipeptidyl peptidase-4 inhibitor withß-amino amide scaffold: synthesis, SAR and biological evaluation.EBI Dong-A Pharm. Co., Ltd
22832311 75 N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators.EBI Lundbeck Research USA, Inc.
22185670 73 Oxadiazoles in medicinal chemistry.EBI AstraZeneca
22594690 80 A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779.EBI Cephalon, Inc.
22524426 281 Discovery and optimization of new benzimidazole- and benzoxazole-pyrimidone selective PI3Kß inhibitors for the treatment of phosphatase and TENsin homologue (PTEN)-deficient cancers.EBI Sanofi Research& Development
22524250 12 Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.EBI Genomics Institute of the Novartis Research Foundation
22500954 99 Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).EBI GlaxoSmithKline
22765892 48 Benzoxazole and benzothiazole amides as novel pharmacokinetic enhancers of HIV protease inhibitors.EBI Janssen Infectious Diseases BVBA
22732695 26 Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.EBI Bristol-Myers Squibb R&D
22727645 42 The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.EBI Bristol-Myers Squibb Research& Development
22727639 24 Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe.EBI Vanderbilt University School of Medicine
22726929 118 Novel 2-(2-(benzylthio)-1H-benzo[d]imidazol-1-yl)acetic acids: discovery and hit-to-lead evolution of a selective CRTh2 receptor antagonist chemotype.EBI Actelion Pharmaceuticals Ltd
22704887 12 Synthesis and evaluation of novel potent HCV NS5A inhibitors.EBI Emory University School of Medicine
22652255 50 C-Aryl 5a-carba-ß-d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.EBI Chugai Pharmaceutical Co. Ltd
22633692 51 Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.EBI Arena Pharmaceuticals
22380629 174 Discovery of cyclic sulfone hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloidß-peptides.EBI Novartis Pharma AG
22749190 23 Wake-promoting agents: search for next generation modafinil: part IV.EBI Cephalon (France)
22497764 3 Preclinical metabolism of LB42908, a novel farnesyl transferase inhibitor, and its effects on the cytochrome P450 isozyme activities.EBI LG Life Sciences R&D Center
22364528 412 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.EBI Merck Research Laboratories
22608963 109 The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity.EBI AstraZeneca
22608962 59 Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.EBI AstraZeneca
22578490 35 Synthesis and evaluation of 4- and 5-pyridazin-3-one phenoxypropylamine analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22542012 155 The design, synthesis, and biological evaluation of PIM kinase inhibitors.EBI Exelixis
22450133 64 Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists.EBI Cephalon, Inc.
22420844 86 First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain.EBI NeurAxon Inc.
22339472 148 Discovery of the macrocycle (9E)-15-(2-(pyrrolidin-1-yl)ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5).1(14,18)]hexacosa-1(24),2,4,9,14(26),15,17,20,22-nonaene (SB1578), a potent inhibitor of janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) for the treatment of rheumatoid arthEBI S BIO Pte. Ltd.
22239250 59 Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.EBI GlaxoSmithKline Research and Development
22617490 23 Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.EBI Cephalon, Inc.
22560567 82 Discovery of XL413, a potent and selective CDC7 inhibitor.EBI Exelixis
22168626 32 Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.EBI Ambit Biosciences
22248262 101 Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.EBI The Beatson Institute for Cancer Research
22503453 59 The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.EBI GlaxoSmithKline
22503248 61 Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.EBI GlaxoSmithKline
22497760 144 Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.EBI AstraZeneca
22465635 95 Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.EBI Abbott Laboratories
22450130 87 Design and synthesis of potent, isoxazole-containing renin inhibitors.EBI Merck Frosst Centre for Therapeutic Research
22429469 2 Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active¿-secretase modulators.EBI Pfizer Inc.
22386529 38 From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.EBI GlaxoSmithKline
22260203 73 [1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.EBI Novartis Institutes for Biomedical Research
22239545 287 Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.EBI Amgen Inc.
22214363 78 Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.EBI Exelixis
22401864 61 Discovery of oxazole-based PDE4 inhibitors with picomolar potency.EBI Merck Research Laboratories
22366657 39 A novel series of benzimidazole NR2B-selective NMDA receptor antagonists.EBI GlaxoSmithKline R&D
22365751 45 Synthesis and evaluation of a new series of 1'-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4'-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists.EBI Cephalon, Inc.
22361135 29 Indolyl and dihydroindolyl N-glycinamides as potent and in vivo active NPY5 antagonists.EBI Lundbeck Research USA
22306122 90 The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR.EBI Amgen Inc.
22148957 8 Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.EBI Merck Research Laboratories
22148921 48 Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-cEBI Cephalon, Inc.
22061639 54 Discovery, optimisation and in vivo evaluation of novel GPR119 agonists.EBI Astrazeneca U K Ltd
21923116 40 Discovery of N-(3-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indol-6-yl) thiophene-2-carboximidamide as a selective inhibitor of human neuronal nitric oxide synthase (nNOS) for the treatment of pain.EBI NeurAxon Inc.
21906941 94 Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H3 receptor antagonists.EBI Cephalon, Inc.
21782432 62 Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.EBI Cephalon, Inc.
21824776 31 Amine-constrained pyridazinone histamine H3 receptor antagonists.EBI Cephalon Inc.
21634396 55 Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.EBI Cephalon, Inc.
21608528 166 Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.EBI Merck Research Laboratories
21438541 45 Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrEBI Pfizer Inc.
21441024 74 Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.EBI Sanofi-aventis
21316976 62 17,20-lyase inhibitors. Part 4: design, synthesis and structure-activity relationships of naphthylmethylimidazole derivatives as novel 17,20-lyase inhibitors.EBI Takeda Pharmaceutical Company, Ltd
21218783 117 Identification of diaryl ether-based ligands for estrogen-related receptora as potential antidiabetic agents.EBI Johnson& Johnson Pharmaceutical Research and Development
21210664 74 Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.EBI H. Lundbeck A/S
21138310 17 Cytochrome P450 3A4 inhibitory constituents of the wood of Taxus yunnanensis.EBI University of Toyama
21105682 1 Human cytochrome P450 liability studies of trans-dihydronarciclasine: a readily available, potent, and selective cancer cell growth inhibitor.EBI McMaster University
21666860 14 Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor.EBI Pfizer Inc.
20724153 31 Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.EBI Korea Institute of Science and Technology
20672820 92 Discovery of novel cyanodihydropyridines as potent mineralocorticoid receptor antagonists.EBI Pfizer Inc.
20614889 71 Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.EBI GlaxoSmithKline
20579874 150 BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.EBI GlaxoSmithKline R&D
20550118 69 Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.EBI Saarland University
20527970 29 6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor.EBI GlaxoSmithKline Medicines Research Centre
20491477 91 Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.EBI F. Hoffmann-La Roche Ltd.
20570147 25 Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.EBI Johnson& Johnson Pharmaceutical Research& Development
20471260 146 Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.EBI Pfizer Global Research and Development
20565112 55 Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.EBI Institute of Cancer Research
20408551 13 Lessons learned from herbal medicinal products: the example of St. John's Wort (perpendicular).EBI Westfalische Wilhelms-Universitat
20429511 6 Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.EBI University of Washington
20420387 118 Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.EBI GlaxoSmithKline
20188553 66 Tetrahydroindolizinone NK1 antagonists.EBI Merck Research Laboratories
20188547 152 Novel benzothiophene H1-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
20000469 179 Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.EBI Boehringer Ingelheim Pharmaceuticals
19703774 56 C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II.EBI Wyeth Research
19821562 34 Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.EBI Bristol-Myers Squibb Research and Development
19778024 31 Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.EBI Bristol-Myers Squibb Co
19645482 245 Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.EBI Merck Research Laboratories
19284751 26 Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable"back-up" compound for N-tert-butyl isoquine.EBI University of Liverpool
19217790 68 Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.EBI Matrix Laboratories Limited
19191554 43 Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.EBI GlaxoSmithKline
18752960 48 Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition.EBI Astellas Pharma. Inc.
18462007 7 Selective inhibition of aromatase by a dihydroisocoumarin from Xyris pterygoblephara.EBI Universidade Federal de Minas Gerais
15679319 40 Potent CYP3A4 inhibitory constituents of Piper cubeba.EBI Toyama Medical and Pharmaceutical University
16562853 22 Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.EBI Tom's of Maine
18420409 4 2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.EBI GlaxoSmithKline
18417343 62 Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity.EBI Pfizer Inc.
18395443 37 Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.EBI Bristol-Myers Squibb
18502123 68 Development of potent and selective small-molecule human Urotensin-II antagonists.EBI GlaxoSmithKline Pharmaceuticals
18374569 65 Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 3. New potent non-competitive metabotropic glutamate receptor 2/3 antagonists.EBI F. Hoffmann-La Roche Ltd.
18359226 50 Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.EBI Bristol-Myers Squibb Research and Development
18345609 57 Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.EBI The Institute of Cancer Research
18324761 65 Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.EBI Amgen Inc.
18313294 68 [4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.EBI Pfizer Inc.
17983756 55 Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.EBI OSI Pharmaceuticals, Inc.
18221875 59 Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
18272363 7 Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.EBI Johnson& Johnson Pharmaceutical Research& Development
18462938 12 Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.EBI GlaxoSmithKline
18324762 20 Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.EBI Saarland University
18032036 17 The discovery of GSK221149A: a potent and selective oxytocin antagonist.EBI GlaxoSmithKline Research and Development
18249540 28 2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability.EBI Neurocrine Biosciences
18247554 134 Histone deacetylase inhibitors: from bench to clinic.EBI Menarini Ricerche
18291645 108 Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.EBI Bristol-Myers Squibb Research and Development
18247547 6 Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.EBI Cephalon, Inc.
18288793 24 Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215EBI Bristol-Myers Squibb Research and Development
18282707 56 Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
18061443 34 Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.EBI Merck Research Laboratories
18308567 44 Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.EBI Johnson& Johnson Pharmaceutical Research and Development
18267361 56 Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.EBI Novartis Institutes for BioMedical Research
18243692 85 Imidazopyridines: a novel class of hNav1.7 channel blockers.EBI Merck Research Laboratories
18052318 30 4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.EBI GlaxoSmithKline Medicines REsearch Centre
17630726 32 Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.EBI Novartis Institutes for BioMedical Research
17118654 21 Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite.EBI Ono Pharmaceutical Co., Ltd
17113292 73 Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.EBI TargeGen, Inc.
16950620 36 N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists.EBI Merck Sharp& Dohme Research Laboratories
17201408 91 Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.EBI Wyeth Research
16750363 101 Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.EBI Pfizer Global Research and Development
15634016 232 5-substituted, 6-substituted, and unsubstituted 3-heteroaromatic pyridine analogues of nicotine as selective inhibitors of cytochrome P-450 2A6.EBI Human BioMolecular Research Institute
15582422 43 Aminothiazole inhibitors of HCV RNA polymerase.EBI NeoGenesis Pharmaceuticals Inc.
12699389 152 Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.EBI F. Hoffmann-LaRoche Ltd.
12930139 22 Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15177483 33 SAR of benzoylpyridines and benzophenones as p38alpha MAP kinase inhibitors with oral activity.EBI Novartis Institutes for BioMedical Research
14552748 8 Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4).EBI University of Basel
22342630 2 Biotransformations of 6',7'-dihydroxybergamottin and 6',7'-epoxybergamottin by the citrus-pathogenic fungi diminish cytochrome P450 3A4 inhibitory activity.EBI Agricultural Research Service
22341942 18 Wake-promoting agents: search for next generation modafinil: part II.EBI Cephalon, Inc.
22330635 25 Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.EBI Janssen Research& Development
22325948 52 Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.EBI Arena Pharmaceuticals Inc.
22318159 36 3,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase (nNOS) inhibitors.EBI NeurAxon Inc.
22107017 47 Optimization of 5-pyridazin-3-one phenoxypropylamines as potent, selective histamine H3 receptor antagonists with potent cognition enhancing activity.EBI Cephalon, Inc.
22297111 32 Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.EBI Cephalon, Inc.
22290075 60 4-phenoxypiperidine pyridazin-3-one histamine H(3) receptor inverse agonists demonstrating potent and robust wake promoting activity.EBI Cephalon, Inc.
22284817 82 ¿-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.EBI AstraZeneca R&D Montreal
22266039 119 Hit to lead evaluation of 1,2,3-triazolo[4,5-b]pyridines as PIM kinase inhibitors.EBI Spanish National Cancer Research Centre (CNIO)
22266038 55 Balancing hERG affinity and absorption in the discovery of AZD5672, an orally active CCR5 antagonist for the treatment of rheumatoid arthritis.EBI AstraZeneca
22264487 5 Aß-tryptase inhibitor with a tropanylamide scaffold to improve in vitro stability and to lower hERG channel binding affinity.EBI Sanofi Pharmaceuticals
22264486 62 Imidazopyridines as selective CYP3A4 inhibitors.EBI The Scripps Research Institute
22227212 58 Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.EBI Merck Research Laboratories
22226656 75 Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test.EBI Cephalon, Inc.
22209458 114 Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.EBI Vernalis (R&D) Ltd
22177783 122 Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.EBI Argenta Discovery Ltd.
22196117 48 Identification of triazolopyridazinones as potent p38a inhibitors.EBI Amgen Inc.
22148278 132 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinaseEBI S BIO Pte. Ltd.
22070604 150 Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor¿ (PPAR¿) modulators.EBI Merck Research Laboratories
22153941 140 Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.EBI AstraZeneca
22130135 55 Discovery of potent and specific CXCR3 antagonists.EBI Amgen Inc.
22017539 75 Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.EBI Boehringer Ingelheim Pharmaceuticals Inc
22172695 28 Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).EBI Arena Pharmaceuticals
22153937 52 Novel brain penetrant benzofuropiperidine 5-HT6 receptor antagonists.EBI Cephalon, Inc.
22153347 111 Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H¿?-antihistamines for insomnia.EBI Neurocrine Biosciences
22153342 60 Synthesis and evaluation of 4-alkoxy-[1'-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4'-piperidine)] analogues as histamine-3 receptor antagonists.EBI Cephalon, Inc.
22142542 73 4,5-dihydropyridazin-3-one derivatives as histamine H3 receptor inverse agonists.EBI Cephalon, Inc.
22100140 10 Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans.EBI University of Eastern Finland
22061640 5 Discovery of 4-aminomethylphenylacetic acids as¿-secretase modulators via a scaffold design approach.EBI Biogen Idec Inc.
22041175 74 Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors.EBI Genkyotex S.A.
22019046 35 Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.EBI Sanwa Kagaku Kenkyusho Co. Ltd
22014550 337 Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).EBI Ansaris
22106937 83 Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ulimorelin (TZP-101) from hit to clinic.EBI Tranzyme Pharma Inc.
22071301 115 Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.EBI Merck Frosst Centre for Therapeutic Research
22059882 206 5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.EBI Amira Pharmaceuticals
22030028 55 Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.EBI Merck Research Laboratories
22018461 41 Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).EBI Bristol-Myers Squibb Research and Development
22014551 33 Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists.EBI Cephalon, Inc.
21978946 45 Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer.EBI Takeda Pharmaceutical Company, Ltd.
21966889 61 Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinEBI Vanderbilt University Medical Center
21852130 69 Discovery and characterization of potent and selective 4-oxo-4-(5-(5-phenyl-1,2,4-oxadiazol-3-yl)indolin-1-yl)butanoic acids as S1P¿? agonists.EBI Arena Pharmaceuticals
21699209 75 Design, synthesis, and biological evaluation of 3,4-dihydroquinolin-2(1H)-one and 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors.EBI NeurAxon Inc.
21958540 95 Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.EBI Amira Pharmaceuticals
21944855 30 Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H3 receptor antagonists with robust wake-promoting activity.EBI Cephalon, Inc.
21944852 79 Substituted indole-1-acetic acids as potent and selective CRTh2 antagonists-discovery of AZD1981.EBI AstraZeneca R&D Charnwood
21930376 92 Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.EBI Vanderbilt University Medical Center
21924610 3 Aminothiazoles as¿-secretase modulators.EBI F. Hoffmann-La Roche Ltd
21996520 149 7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.EBI Bristol-Myers Squibb Research and Development
21974949 57 Discovery of a new class of glucosylceramide synthase inhibitors.EBI Exelixis
21958544 31 Indolin-2-one p38a inhibitors III: bioisosteric amide replacement.EBI Rhône-Poulenc Rorer
21924902 43 5-(2'-Pyridyl)-2-aminothiazoles: alkyl amino sulfonamides and sulfamides as potent NPY(5) antagonists.EBI Lundbeck Research USA, Inc.
21641209 120 Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.EBI Merck Frosst Centre for Therapeutic Research
21942426 113 Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.EBI Merck& Co.
21936542 143 Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.EBI Novartis Institute for BioMedical Research
21917454 159 Design, synthesis and SAR of indazole and benzoisoxazole containing 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists.EBI Johnson& Johnson Pharmaceutical Research and Development
21899332 1 P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.EBI Abbott Laboratories
21885275 65 Discovery of PF-184563, a potent and selective V1a antagonist for the treatment of dysmenorrhoea. The influence of compound flexibility on microsomal stability.EBI Pfizer Inc.
21873051 31 Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
21838322 37 Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P¿? and S1P5 receptors efficacious at low oral dose.EBI GlaxoSmithKline
21782428 61 Discovery of Lu AA33810: a highly selective and potent NPY5 antagonist with in vivo efficacy in a model of mood disorder.EBI Lundbeck Research USA, Inc.
21899292 76 Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.EBI AstraZeneca
21838328 35 Synthesis and biological evaluation of 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-[4-(naphthalen-2-ylamino)phenyl]propyl derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26).EBI Cardiff University
21786805 130 Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.EBI Vitae Pharmaceuticals
21634430 218 Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile.EBI S*BIO Pte Ltd.
21859094 61 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.EBI Cephalon, Inc.
21823597 373 Design and synthesis of novel arylpiperazine derivatives containing the imidazole core targeting 5-HT(2A) receptor and 5-HT transporter.EBI Green Cross Corporation
21803580 115 Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.EBI Merck Research Laboratories Rome
21798739 6 Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPAR¿ partial agonist.EBI GlaxoSmithKline
21798738 44 Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).EBI Biogen Idec Inc.
21783360 52 Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series.EBI Bioprojet-Biotech
21865048 29 2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.EBI Dainippon Sumitomo Pharma Co. Ltd
21550808 25 1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: further insights into a class of triple re-uptake inhibitors.EBI GlaxoSmithKline Medicines Research Centre
21515056 61 Design of small molecule inhibitors of acetyl-CoA carboxylase 1 and 2 showing reduction of hepatic malonyl-CoA levels in vivo in obese Zucker rats.EBI AstraZeneca Research and Development
21739935 62 Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.EBI Sunovion Pharmaceuticals
21737263 63 Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.EBI Merck Research Laboratories Rome
21658961 72 Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.EBI Ono Pharmaceutical Co. Ltd
20800486 16 Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences
21742496 85 The design, synthesis and structure-activity relationships of novel isoindoline-based histone deacetylase inhibitors.EBI Novartis Institutes for Biomedical Research
21724392 3 Rigidized 1-aryl sulfonyl tryptamines: synthesis and pharmacological evaluation as 5-HT6 receptor ligands.EBI Suven Life Sciences Ltd.
21705217 60 Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38a MAP kinase inhibitors.EBI Bristol-Myers Squibb
20931971 155 Discovery of dual inducible/neuronal nitric oxide synthase (iNOS/nNOS) inhibitor development candidate 4-((2-cyclobutyl-1H-imidazo[4,5-b]pyrazin-1-yl)methyl)-7,8-difluoroquinolin-2(1H)-one (KD7332) part 2: identification of a novel, potent, and selective series of benzimidazole-quinolinone iNOS/nNOEBI Kalypsys, Inc
20634071 41 Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.EBI GlaxoSmithKline
21644570 25 Imidazolopiperazines: hit to lead optimization of new antimalarial agents.EBI Genomics Institute of the Novartis Research Foundation
21080647 27 Discovery of 2-(6-{[(6-fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex-3-yl)-N-hydroxypyrimidine-5-carboxamide (CHR-3996), a class I selective orally active histone deacetylase inhibitor.EBI Chroma Therapeutics Ltd.
21621998 110 Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.EBI Merck Frosst Centre for Therapeutic Research
19447034 76 Discovery of selective PDE4B inhibitors.EBI Asahi Kasei Pharma Corporation
21536437 219 Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis.EBI AstraZeneca
21507633 77 The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.EBI Genzyme Corp.
21592791 61 Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.EBI AstraZeneca R&D Charnwood
21570283 29 Discovery of DA-1229: a potent, long acting dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes.EBI Dong-A Pharm. Co., Ltd
21565499 32 Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.EBI Pfizer Inc.
21550240 9 From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons.EBI Boehringer Ingelheim (Canada) Ltd
21536438 74 Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.EBI Merck Research Laboratories
21524576 69 2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.EBI AstraZeneca Pharmaceuticals
21515053 58 New indole amide derivatives as potent CRTH2 receptor antagonists.EBI Merck Frosst
21514825 81 3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.EBI Amgen, Inc.
21514824 91 3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.EBI Merck Research Laboratories
21195614 56 Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.EBI Pfizer Inc.
21429754 75 17,20-Lyase inhibitors. Part 3: Design, synthesis, and structure-activity relationships of biphenylylmethylimidazole derivatives as novel 17,20-lyase inhibitors.EBI Takeda Pharmaceutical Company, Ltd
21428449 27 Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates.EBI Cardiff University
21413799 63 Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes.EBI Hoffmann-La Roche Inc.
21413798 174 Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents.EBI Vertex Pharmaceuticals (Europe) Ltd.
21381763 52 The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.EBI GlaxoSmithKline Medicines Research Centre
21375347 5 Pyrimidine-2,4,6-trione derivatives and their inhibition of mutant SOD1-dependent protein aggregation. Toward a treatment for amyotrophic lateral sclerosis.EBI Northwestern University
21375264 77 Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitorsEBI Roche Palo Alto LLC
21388809 76 Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.EBI Roche Research Center
21376585 120 Discovery of 3-aryl-5-acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor.EBI Euroscreen SA
21354795 95 1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.EBI Boehringer Ingelheim Pharmaceuticals
21334894 218 Substituted phenyl triazoles as selective inhibitors of 11 β-Hydroxysteroid Dehydrogenase Type 1.EBI Merck& Co
21439819 49 Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1.EBI Sanofi-aventis R&D,
21429746 88 The discovery and synthesis of potent zwitterionic inhibitors of renin.EBI Merck Frosst Centre for Therapeutic Research
21411321 28 Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.EBI Merck Research Laboratories
21324691 24 N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors.EBI Pfizer Inc.
21324688 36 1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes.EBI Pfizer Inc.
21316218 5 Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent.EBI Chugai Pharmaceutical Co., Ltd
21310612 99 Discovery of N-methyl-1-(1-phenylcyclohexyl)ethanamine, a novel triple serotonin, norepinephrine and dopamine reuptake inhibitor.EBI Sunovion Pharmaceuticals Inc.
21300546 129 The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.EBI AstraZeneca
21295478 81 Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.EBI Incyte Corporation
21295471 4 A new structural alert for benzimidazoles: 2,6-dimethylphenyl substituents increase mutagenic potential and time-dependent CYP3A4 inhibition risk.EBI Global Discovery Chemistry
21277198 71 II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.EBI Ligand Pharmaceuticals
21256005 51 Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.EBI GlaxoSmithKline
21269824 112 Optimization of a novel class of benzimidazole-based farnesoid X receptor (FXR) agonists to improve physicochemical and ADME properties.EBI F. Hoffmann-La Roche Ltd
21256008 44 Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.EBI Ono Pharmaceutical Co., Ltd
21251824 24 Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy.EBI OSI Pharmaceuticals, Inc.
21232954 75 Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.EBI Neurocrine Biosciences
21211972 6 The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.EBI Array BioPharma, 3200 Walnut Street, Boulder, CO 80301, USA.
21211969 42 Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.EBI USA.
21189020 54 New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17ß-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.EBI Saarland University
19289530 25 Novel S-adenosylmethionine decarboxylase inhibitors for the treatment of human African trypanosomiasis.EBI Genzyme Corporation
21095126 60 Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.EBI Sunovion Pharmaceuticals Inc
21093273 154 Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.EBI Sepracor Inc.
21074994 46 Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.EBI Cephalon, Inc
21147532 82 Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.EBI Merck Research Laboratories
21146988 26 Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.EBI AMRI
21134749 31 Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists.EBI Suven Life Sciences Ltd
21134748 59 Stereospecific synthesis and structure-activity relationships of unsymmetrical 4,4-diphenylbut-3-enyl derivatives of nipecotic acid as GAT-1 inhibitors.EBI GlaxoSmithKline
21106375 198 Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.EBI Merck Frosst Centre for Therapeutic Research
21195616 26 A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain.EBI Merck Research Laboratories
21185722 74 Azaindoles as potent CRTH2 receptor antagonists.EBI Merck Frosst Centre for Therapeutic Research
20971004 126 Synthesis and characterization of 1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: Part 4. In vivo active potent and selective non-competitive metabotropic glutamate receptor 2/3 antagonists.EBI F. Hoffmann-La Roche Ltd
21106456 35 Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.EBI Merck Research Laboratories
21105711 79 Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection.EBI Pfizer Inc.
20974532 57 Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.EBI F. Hoffmann-La Roche Ltd
21074434 4 Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.EBI Merck Research Laboratories
21074430 53 Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.EBI Dainippon Sumitomo Pharma Co., Ltd
21055936 14 Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists.EBI GlaxoSmithKline Medicines Research Centre
21036042 7 Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.EBI Pfizer Inc.
21035336 42 5-amino-pyrazoles as potent and selective p38a inhibitors.EBI Bristol-Myers Squibb Research and Development
20961756 61 5-(pyridinon-1-yl)indazoles and 5-(furopyridinon-5-yl)indazoles as MCH-1 antagonists.EBI AMRI
20952195 62 Tetrahydrocarboline analogs as MCH-1 antagonists.EBI AMRI
20951036 47 Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.EBI AMRI
20942472 88 Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders.EBI GlaxoSmithKline
20942471 79 First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis.EBI Genkyotex, S.A.
20801551 34 Synthesis and evaluation of novel stearoyl-CoA desaturase 1 inhibitors: 1'-{6-[5-(pyridin-3-ylmethyl)-1,3,4-oxadiazol-2-yl]pyridazin-3-yl}-3,4-dihydrospiro[chromene-2,4'-piperidine] analogs.EBI Daiichi Sankyo Co., Ltd.
20731374 65 Direct renin inhibitors as a new therapy for hypertension.EBI Novartis Pharmaceuticals Corp
21033679 6 Electron density guided fragment-based lead discovery of ketohexokinase inhibitors.EBI Johnson& Johnson Pharmaceutical Research and Development
20934334 16 Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.EBI Boehringer Ingelheim Pharmaceuticals Inc.
20933414 25 Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as¿-secretase inhibitors.EBI Merck Research Lab.
20933413 74 2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.EBI GlaxoSmithKline Medicines Research Centre
20933409 50 Arylpiperazine-containing pyrimidine 4-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI Green Cross Corporation
20926294 65 3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists.EBI GlaxoSmithKline Pharmaceuticals
20889341 59 Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.EBI AMRI
20888225 17 Discovery of a vorapaxar analog with increased aqueous solubility.EBI Merck Research Laboratories
20880704 200 Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI Pfizer Inc.
20864344 110 Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.EBI Vitae Pharmaceuticals
20850301 68 Inhibitors of the tyrosine kinase EphB4. Part 3: identification of non-benzodioxole-based kinase inhibitors.EBI AstraZeneca
20843687 60 Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.EBI Merck Research Laboratories
20843686 99 Design and optimization of new piperidines as renin inhibitors.EBI Actelion Pharmaceuticals Ltd
20833041 40 Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.EBI Elan Pharmaceuticals
20839775 60 Exploration of the amine terminus in a novel series of 1,2,4-triazolo-3-yl-azabicyclo[3.1.0]hexanes as selective dopamine D3 receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
20832301 6 Isoform-selective inhibition of chrysin towards human cytochrome P450 1A2. Kinetics analysis, molecular docking, and molecular dynamics simulations.EBI Sun Yat-Sen University
20801030 106 Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.EBI F Hoffmann-La Roche Ltd
20797855 63 PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.EBI Pfizer Inc.
20729082 59 Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.EBI Merck Research Laboratories
20804198 29 Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases.EBI Bristol-Myers Squibb Research and Development
20690643 68 Investigation of the histamine H3 receptor binding site. Design and synthesis of hybrid agonists with a lipophilic side chain.EBI Meiji Seika Kaisha, Ltd.
20590088 124 Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).EBI GlaxoSmithKline
20709552 36 Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.EBI Merck Research Laboratories
20709545 31 Substituted biaryl pyrazoles as sodium channel blockers.EBI Merck Research Laboratories
20685118 97 The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H3 antagonists.EBI Merck Research Laboratories
20673729 60 Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist.EBI Green Cross Corporation
20673718 5 Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.EBI Merck Frosst Centre for Therapeutic Research
20667729 86 Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.EBI Evotec (UK) Ltd
20684610 73 Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.EBI Saarland University
19933795 12 SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.EBI Scynexis, Inc.
20630754 33 Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.EBI GlaxoSmithKline
20615692 52 The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-beta-hydroxylase.EBI Novartis Institutes for BioMedical Research
20598880 48 Discovery of novel sphingosine kinase-1 inhibitors. Part 2.EBI Genzyme Corporation
20598534 105 Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.EBI Bristol-Myers Squibb
20594842 90 Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.EBI GlaxoSmithKline
20594839 4 Synthesis and pharmacological evaluation of aryl aminosulfonamide derivatives as potent 5-HT(6) receptor antagonists.EBI Suven Life Sciences Ltd
20573506 39 A specific and direct comparison of the trifluoromethyl and pentafluoro sulfanyl groups on the selective dopamine D(3) antagonist 3-(3-{[4-methyl-5-(4-methyl-1,3-oxazol-5-yl)-4H-1,2,4-triazol-3-yl]thio}propyl)-1-phenyl-3-azabicyclo[3.1.0]hexane template.EBI GlaxoSmithKline Medicines Research Centre
20566292 6 5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.EBI Amira Pharmaceuticals
20481485 1 Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules.EBI Sanford-Burnham Medical Research Institute
20465278 27 Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).EBI Amgen Inc.
20405922 53 Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).EBI Bristol-Myers Squibb Research and Development
20399649 41 Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.EBI Bristol-Myers Squibb Company
20384344 42 Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.EBI Meiji Seika Kaisha, Ltd.
20380377 70 Discovery of novel and potent leukotriene B4 receptor antagonists. Part 1.EBI Roche Research Center
20359891 13 A prodrug approach towards the development of tricyclic-based FBPase inhibitors.EBI Daiichi Sankyo Co., Ltd
20347297 61 The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.EBI Neurocrine Biosciences
20423086 93 Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.EBI Merck Research Laboratories
20236824 4 Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.EBI Merck Research Laboratories
20227880 144 Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
20223663 100 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.EBI Wyeth Research
20223662 174 Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.EBI Yangji Chemicals
20218621 131 Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).EBI Bristol-Myers Squibb
20218619 44 Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc.
20206513 35 Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.EBI Merck Frosst Centre for Therapeutic Research
20189807 32 Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics.EBI Sanofi-aventis
20189386 4 Potent and selective inhibition of human cytochrome P450 3A4 by seco-pancratistatin structural analogs.EBI McMaster University
20096577 42 Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.EBI Merck Research Laboratories
19694467 1 Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.EBI Wyeth Research
20185309 15 Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.EBI Boehringer Ingelheim (Canada) Ltd
20184326 40 Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.EBI Merck Research Laboratories
20153189 51 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.EBI Bristol-Myers Squibb Co.
20149649 133 Arylpiperazine-containing pyrrole 3-carboxamide derivatives targeting serotonin 5-HT(2A), 5-HT(2C), and the serotonin transporter as a potential antidepressant.EBI Green Cross Corporation
20138761 30 Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc.
19891474 131 1,2,4-Triazolyl azabicyclo[3.1.0]hexanes: a new series of potent and selective dopamine D(3) receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
19853442 35 New classes of potent and bioavailable human renin inhibitors.EBI Actelion Pharmaceuticals Ltd
19846298 119 Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs).EBI GlaxoSmithKline R&D
19804969 109 The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.EBI GlaxoSmithKline
19689106 4 Minor furanocoumarins and coumarins in grapefruit peel oil as inhibitors of human cytochrome P450 3A4.EBI University of Sao Paulo State
19682899 211 Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.EBI Merck Research Laboratories
19679477 38 Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.EBI Abbott Laboratories
19647430 104 N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.EBI Pfizer Global Research and Development
20045321 85 An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter.EBI Pfizer Global Research& Development
20022752 94 Tricyclic dihydroquinazolinones as novel 5-HT2C selective and orally efficacious anti-obesity agents.EBI Bristol-Myers Squibb Co
20170186 49 1-(Aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors.EBI GlaxoSmithKline Medicine Research Centre
20153655 3 Selective benzimidazole inhibitors of the antigen receptor-mediated NF-kappaB activation pathway.EBI Human BioMolecular Research Institute
20151677 67 Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).EBI Institute of Cancer Research
20089400 27 Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors.EBI Johnson& Johnson Pharmaceutical Research and Development
20064717 64 Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.EBI Vitae Pharmaceuticals
20006500 60 Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.EBI GlaxoSmithKline
20005102 34 2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.EBI GlaxoSmithKline
20004097 36 Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438).EBI Merck Frosst Centre for Therapeutic Research
19962893 3 The comparative antimalarial properties of weak base and neutral synthetic ozonides.EBI University of Nebraska Medical Center
19945870 10 Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.EBI Boehringer Ingelheim (Canada) Ltd
19914828 37 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.EBI Amira Pharmaceuticals
19914064 9 Synthesis and antiplasmodial activity of novel 2,4-diaminopyrimidines.EBI Institute Infectious Diseases Initiative
19957930 126 Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent thatEBI deCODE Chemistry, Inc.
19883100 3 Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.EBI Merck Research Laboratory
19819693 50 Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.EBI Amgen Inc.
19769332 49 Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment. 5. An evolution from indole to azaindoles leading to the discovery of 1-(4-benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a drug candidate that demonstrates antiviral activityEBI Bristol-Myers Squibb Research and Development
19743867 51 Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.EBI GlaxoSmithKline
19699641 145 Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum.EBI Institute Infectious Diseases Initiative
19683918 36 Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.EBI Pfizer Global Research and Development
19679475 6 A novel class of highly potent multidrug resistance reversal agents: disubstituted adamantyl derivatives.EBI Chung-Ang University
19632830 47 Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.EBI Merck Research Laboratories
19713107 7 Structure-activity studies on seco-pancratistatin analogs: potent inhibitors of human cytochrome P450 3A4.EBI McMaster University
19888755 43 Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.EBI Wyeth Research
19831396 84 New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity.EBI Saarland University
19810674 93 Discovery of a novel class of potent coumarin monoamine oxidase B inhibitors: development and biopharmacological profiling of 7-[(3-chlorobenzyl)oxy]-4-[(methylamino)methyl]-2H-chromen-2-one methanesulfonate (NW-1772) as a highly potent, selective, reversible, and orally active monoamine oxidase B EBI Universita degli Studi di Bari
19783143 65 Special ergolines are highly selective, potent antagonists of the chemokine receptor CXCR3: discovery, characterization and preliminary SAR of a promising lead.EBI Novartis Institutes for BioMedical Research
19553115 96 Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
19524437 31 Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.EBI Hoffmann-La Roche Ltd
19500982 93 Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.EBI AstraZeneca R&D M£lndal
19739647 52 5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).EBI Amira Pharmaceuticals
19616432 176 Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.EBI Pfizer Global Research and Development
19608418 95 Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.EBI Amira Pharmaceuticals
19592244 61 7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.EBI Novartis Institutes of Biomedical Research
19574047 42 Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc
19541481 57 Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.EBI Bristol-Myers Squibb Company
19520574 49 Synthesis, structure-activity relationships, and biological profiles of a dihydrobenzoxathiin class of histamine H(3) receptor inverse agonists.EBI Tsukuba Research Institute
19211174 15 Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls.EBI Saarland University
19128860 24 Comparative chemometric modeling of cytochrome 3A4 inhibitory activity of structurally diverse compounds using stepwise MLR, FA-MLR, PLS, GFA, G/PLS and ANN techniques.EBI Jadavpur University
19719241 55 Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.EBI Wyeth Research
19552431 104 Novel small molecule bradykinin B2 receptor antagonists.EBI Jerini AG
19537798 22 Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.EBI Tsukuba Research Institute
19481450 121 Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors.EBI Schering-Plough Research Institute
19428250 5 Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids.EBI McMaster University
19209845 12 Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor.EBI Pfizer Global Research and Development
19222165 36 Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.EBI University of Liverpool
19481932 164 Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.EBI Merck Research Laboratories
19467868 131 Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs).EBI GlaxoSmithKline R&D
19441819 17 Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.EBI Merck Research Laboratories
19419866 24 Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).EBI Bristol-Myers Squibb Pharmaceutical Research and Development
19419141 23 Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.EBI Abbott Laboratories
19364658 113 Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).EBI Wyeth Research
19354254 24 Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.EBI Merck Research Laboratories
19341281 32 Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones.EBI University College London
19339177 127 The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.EBI Schering-Plough Research Institute
19332369 43 Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.EBI GlaxoSmithKline
19323562 14 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.EBI Abbott Laboratories
19320488 171 1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.EBI Merck Research Laboratories
19275964 64 (3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.EBI Pfizer Global Research & Development
19256507 5 Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.EBI Celgene Corporation
19246199 3 Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists.EBI Pfizer Global Research and Development
19239254 6 Rational modification of a candidate cancer drug for use against Chagas disease.EBI University of Washington
19231183 44 5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.EBI AstraZeneca
19208473 7 Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.EBI Novartis Institutes for BioMedical Research
19181519 71 Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).EBI TBA
19140664 82 N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.EBI Neurocrine Biosciences
19119007 34 Novel imidazole-based histamine H3 antagonists.EBI Johnson & Johnson Pharmaceutical Research & Development
19053768 64 Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.EBI Novartis Institutes for BioMedical Research
19049427 98 In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.EBI Saarland University
19036582 45 Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.EBI GlaxoSmithKline
19019676 94 Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.EBI Medicines Research Centre
19014886 83 Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.EBI GlaxoSmithKline
19010671 28 Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.EBI GlaxoSmithKline PLC
19006669 82 The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.EBI GlaxoSmithKline
19006286 37 Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.EBI Neurocrine Biosciences, Inc.
18990568 15 Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
18954983 12 Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.EBI Kalypsys, Inc.
18823779 27 5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).EBI Johnson & Johnson Pharmaceutical Research and Development
18817364 41 3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase.EBI Amgen Inc.
18809327 6 Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.EBI GlaxoSmithKline
18805008 133 Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.EBI F. Hoffmann-La Roche Ltd.
18793848 20 Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.EBI GlaxoSmithKline
18752953 111 Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.EBI F. Hoffmann-La Roche Ltd
18701276 97 Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI Merck Research Laboratories
18672861 91 Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.EBI Saarland University
18667310 49 Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.EBI Neurocrine Biosciences, Inc.
18665579 21 Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficEBI Bristol-Myers Squibb Research & Development
18662879 54 Discovery of piperidine carboxamide TRPV1 antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
18632268 8 Discovery and optimization of pyridazinone non-nucleoside inhibitors of HIV-1 reverse transcriptase.EBI Roche Palo Alto LLC
18625557 60 N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.EBI Pfizer Global Research and Development
18625554 2 Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase.EBI Roche Palo Alto LLC
18621528 133 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.EBI Pfizer Global Research and Development
18614366 97 Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.EBI GlaxoSmithKline R&D
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18583127 1 Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).EBI Albert Einstein College of Medicine
18572407 75 Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.EBI Bristol-Myers Squibb Co.
18539454 47 Imidazopyridines as VLA-4 integrin antagonists.EBI UCB
18539028 81 Discovery of potent, orally active benzimidazole glucagon receptor antagonists.EBI Merck Research Laboratories
18524591 62 Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.EBI GlaxoSmithKline Pharmaceuticals
18479916 24 Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.EBI Bristol-Myers Squibb Research and Development
18455394 34 The discovery of fused pyrrole carboxylic acids as novel, potent D-amino acid oxidase (DAO) inhibitors.EBI Merck Sharp & Dohme
18442910 53 Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.EBI Neurocrine Biosciences, Inc.
18249473 97 Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues.EBI Vrije Universiteit
15568772 3 Isolation of cytochrome P450 inhibitors from strawberry fruit, Fragaria ananassa.EBI Kanazawa University
15270556 37 Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.EBI Toyama Medical and Pharmaceutical University
18329269 77 Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.EBI Neurocrine Biosciences
18180160 17 Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.EBI Purdue University
17994701 12 Cytochrome P3A4 inhibitors and other constituents of Fibraurea tinctoria.EBI National Cheng Kung University
17994683 55 Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
17988864 29 Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.EBI Schering-Plough Research Institute
17937987 83 Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.EBI Centre de Recherches
17933533 36 Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.EBI Institute of Cancer Research
17918824 39 Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.EBI Neurocrine Biosciences, Inc.
17890085 22 Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.EBI Schering-Plough Research Institute
17869105 42 Synthesis and biological evaluation of phenyl piperidine derivatives as CCR2 antagonists.EBI Johnson & Johnson Pharmaceutical Research and Development
17855089 25 Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17822895 110 Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.EBI Neurocrine Biosciences, Inc.
17761416 53 The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.EBI Merck Research Laboratories
17723300 55 Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.EBI Merck Research Laboratories
17722903 57 Novel substituted (pyridin-3-yl)phenyloxazolidinones: antibacterial agents with reduced activity against monoamine oxidase A and increased solubility.EBI AstraZeneca Discovery
17705360 76 Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.EBI Wyeth Research
17629698 36 Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.EBI GlaxoSmithKline
17531480 51 2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.EBI Novartis Institutes of Biomedical Research
17524641 69 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.EBI GlaxoSmithKline
17477516 115 Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.EBI GlaxoSmithKline
17428043 5 Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.EBI P. Angeletti S.p.A. (Merck Research Laboratories
17418568 50 1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.EBI F. Hoffmann-La Roche Ltd
17400460 2 Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit.EBI Texas A&M University
17399990 45 In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).EBI Université Laval
17398093 72 Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17368019 46 Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.EBI The Scripps Research Institute
17352462 90 Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1).EBI Via Zambeletti 25
17350839 52 Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).EBI Neurocrine Biosciences Inc.
17315987 268 Discovery of (R)-9-ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a selective, orally active agonist of the 5-HT(2C) receptor.EBI Pharmaceutical Research Institute
17276061 6 In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.EBI Pfizer Inc.
17266208 104 Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.EBI Millennium Pharmaceuticals
17249648 64 Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.EBI Merck Research Laboratories
17234405 34 An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.EBI Abbott Laboratories
17188869 53 Thienopyridine urea inhibitors of KDR kinase.EBI Abbott Laboratories
17107790 40 Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.EBI Argenta Discovery Ltd
17084080 15 Studies towards the identification of a new generation of atypical antipsychotic agents.EBI UK. Vinc
17055721 80 Discovery of potent and selective PKC-theta inhibitors.EBI Boehringer Ingelheim Pharmaceuticals
17027263 42 Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.EBI Merck Research Laboratories
16950617 50 N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.EBI Merck Sharp & Dohme Research Laboratories
16908150 59 Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.EBI Novo Nordisk A/S
16843659 5 Identification of novel pyrazole acid antagonists for the EP1 receptor.EBI GlaxoSmithKline
16821776 13 2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.EBI Cardiovascular and Urogenital Centre of Excellence for Drug Discovery
16806913 6 N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.EBI GlaxoSmithKline
16759855 130 1,4-Dihydroindeno[1,2-c]pyrazoles as novel multitargeted receptor tyrosine kinase inhibitors.EBI Abbott Laboratories
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Global Research & Development
16686533 89 Evolution of the thienopyridine class of inhibitors of IkappaB kinase-beta: part I: hit-to-lead strategies.EBI Boehringer Ingelheim Pharmaceuticals
16647256 16 Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.EBI Arpida A/S
16640325 41 Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).EBI Millennium Pharmaceuticals
16631366 26 Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.EBI AstraZeneca
16570908 39 Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.EBI Pharmaceutical Research Institute
16504501 54 3-[6-(2-Dimethylamino-1-imidazol-1-yl-butyl)-naphthalen-2-yloxy]-2,2-dimethyl-propionic acid as a highly potent and selective retinoic acid metabolic blocking agent.EBI OSI Pharmaceuticals, Inc.
16503138 15 Discovery of novel biaryl heterocyclic EP1 receptor antagonists.EBI GlaxoSmithKline
16495056 23 Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2.EBI Universite Paris 5 René Descartes
16297617 87 Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl]piperidine series of histamine H3 receptor antagonists.EBI The Schering Plough Research Institute
16134939 67 Synthesis and biological activity of flurbiprofen analogues as selective inhibitors of beta-amyloid(1)(-)(42) secretion.EBI Chiesi Farmaceutici S.p.A.
16134929 22 Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.EBI Bristol-Myers Squibb Co
16107158 60 Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors.EBI Boehringer Ingelheim (Canada) Ltd.
16061379 32 Analogs of a potent maxi-K potassium channel opener with an improved inhibitory profile toward cytochrome P450 isozymes.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15943473 136 Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15837312 66 Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.EBI Celltech R&D Ltd
15801819 23 Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.EBI Eli Lilly and Co.
15745819 64 Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).EBI OSI Pharmaceuticals, Inc.
15177482 86 Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.EBI Novartis Institutes for BioMedical Research
15177477 2 An aminomethylpyrimidine DPP-IV inhibitor with improved properties.EBI F. Hoffmann-La Roche Ltd
15139756 221 Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.EBI Actelion Pharmaceuticals Ltd.
14998324 190 Design and synthesis of new templates derived from pyrrolopyrimidine as selective multidrug-resistance-associated protein inhibitors in multidrug resistance.EBI Xenova Ltd.
14998323 79 Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance.EBI Xenova Ltd.
14698201 47 New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties.EBI CV Therapeutics
14698153 46 Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors.EBI Taisho Pharmaceutical Co., Ltd
14640550 132 Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors.EBI Taisho Pharmaceutical Co, Ltd
14584934 15 Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
12643913 55 The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.EBI GlaxoSmithKline
12643910 5 Identification of a novel series of selective 5-HT7 receptor antagonists.EBI GlaxoSmithKline
12593666 30 Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI Senju Pharmaceutical Co.
12182870 53 The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.EBI GlaxoSmithKline
12161148 17 Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.EBI Merck Research Laboratories
11859012 85 2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.EBI Merck Research Laboratories
11714595 43 Discovery of a N'-hydroxyphenylformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor.EBI Taisho Pharmaceutical Co., Ltd.
11327589 11 In vitro metabolism considerations, including activity testing of metabolites, in the discovery and selection of the COX-2 inhibitor etoricoxib (MK-0663).EBI Merck Frosst Centre for Therapeutic Research
10737744 146 Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.EBI SmithKline Beecham Pharmaceuticals
9934466 7 Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.EBI Abbott Laboratories
9925723 10 5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.EBI SmithKline Beecham Pharmaceuticals
9357513 15 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.EBI SmithKline Beecham Pharmaceuticals
8340925 18 Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.EBI Syntex Discovery Research
1495014 36 Stereoisomers of ketoconazole: preparation and biological activity.EBI Syntex Research
23746300 12 Dissecting cytochrome P450 3A4-ligand interactions using ritonavir analogues.BDB University of California at Irvine
22686946 12 Cytotoxic and potent CYP1 inhibitors from the marine algae Cymopolia barbata.BDB University of the West Indies
18763755 20 Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor actiBDB Bristol-Myers Squibb Company
18620382 41 Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.BDB GSK
18672868 76 Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.BDB Saarland University
17948978 29 Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.BDB Wyeth Research
18311908 42 Characterization of Type II Ligands in CYP2C9 and CYP3A4.BDB AstraZeneca
17125252 60 Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.BDB Human BioMolecular Research Institute