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939 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27487565 169 Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics.EBI Shanghai Jiao Tong University
27839686 65 Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.EBI Merck Research Laboratories
27749053 56 Sulfamide as Zinc Binding Motif in Small Molecule Inhibitors of Activated Thrombin Activatable Fibrinolysis Inhibitor (TAFIa).EBI Sanofi R&D
27579577 91 Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers.EBI Actelion Pharmaceuticals Ltd.
27190592 24 Discovery of a Selective Series of Inhibitors of Plasmodium falciparum HDACs.EBI IRBM Science Park
27105029 37 2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1 integrase inhibitors: Influence of the alkylcarboxamide substitution of position 4.EBI Universit£ Lille Nord de France
27112449 55 Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.EBI Takeda Pharmaceutical Co., Ltd.
27043173 47 Discovery of small-molecule nonpeptide antagonists of nociceptin/orphanin FQ receptor: The studies of design, synthesis, and structure-activity relationships for (4-arylpiperidine substituted-methyl)-[bicyclic (hetero)cycloalkanobenzene] derivatives.EBI Pfizer Inc.
26965854 96 Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.EBI AstraZeneca
26741166 105 Discovery of (3-(4-(2-Oxa-6-azaspiro[3.3]heptan-6-ylmethyl)phenoxy)azetidin-1-yl)(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)methanone (AZD1979), a Melanin Concentrating Hormone Receptor 1 (MCHr1) Antagonist with Favorable Physicochemical Properties.EBI AstraZeneca
26951753 336 Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors.EBI Novartis Institutes for BioMedical Research
26917221 69 Structure activity relationship studies on chemically non-reactive glycine sulfonamide inhibitors of diacylglycerol lipase.EBI Bristol-Myers Squibb Co.
26852005 82 Novel N-acyl-carbazole derivatives as 5-HT7R antagonists.EBI Yonsei University
26786693 153 Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists.EBI Aptuit s.r.l
26617966 40 Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment.EBI Pfizer Inc.
26707399 45 Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.EBI Janssen Pharmaceutical Research& Development L.L.C.
26522950 60 Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).EBI Novartis Institutes for BioMedical Research
26483200 100 Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics.EBI Huazhong University of Science and Technology
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)
26502160 6 A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.EBI University of Cape Town
26497283 68 Macrocyclic prolinyl acyl guanidines as inhibitors of▀-secretase (BACE).EBI Bristol-Myers Squibb Company
25978966 65 Development of a novel class of potent and selective FIXa inhibitors.EBI Merck Research Laboratories
26384287 65 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors.EBI Kangwon National University
26320624 45 Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.EBI Novartis Institutes for Biomedical Research
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
26322748 7 Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.EBI University of Cape Town
26288685 59 Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.EBI Merck Research Laboratories
26386604 71 Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies.EBI Bristol-Myers Squibb Research and Development
26342544 9 Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.EBI Research Triangle Institute
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
26142947 77 Potent benzoazepinone┐-secretase modulators with improved bioavailability.EBI Merck Research Laboratories
26291341 66 Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.EBI AstraZeneca
26152426 61 Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5).EBI Merck Research Laboratories
26141771 27 Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6).EBI Merck Research Laboratories
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.
26199119 135 Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.EBI Novartis Institutes for BioMedical Research
26191359 19 Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.EBI AstraZeneca
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
26099534 72 Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.EBI Janssen Pharmaceutical Research& Development L.L.C.
26048804 57 Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.EBI Merck Research Laboratories
26211462 71 Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors.EBI The Walter and Eliza Hall Institute of Medical Research
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
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
26078010 28 Discovery of an 8-methoxytetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain without CYP inhibition liability.EBI Astellas Pharma Inc.
26077492 92 Design, synthesis and evaluation of MCH receptor 1 antagonists--Part II: Optimization of pyridazines toward reduced phospholipidosis and hERG inhibition.EBI Boehringer Ingelheim Pharma GmbH& Co. KG
26048791 93 Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series.EBI Arena Pharmaceuticals
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
25677662 3 Synthesis and biological evaluation of aryl isoxazole derivatives as metabotropic glutamate receptor 1 antagonists: a potential treatment for neuropathic pain.EBI Yonsei University
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
25147603 39 Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.EBI Pharmacokinetics
25007124 6 N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds.EBI AstraZeneca
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
25826710 21 Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.EBI National Institute on Drug Abuse-Intramural Research Program
26005541 33 Design, Synthesis, and Pharmacological Evaluation of Fused▀-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.EBI Chinese Academy of Sciences
26005540 14 Design of Pyridopyrazine-1,6-dione┐-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.EBI Pfizer Inc.
26071372 89 Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.EBI Astellas Pharma Inc.
26071371 26 Discovery of a 1-isopropyltetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain.EBI Astellas Pharma Inc.
26125327 93 Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers.EBI Leiden University
26101568 51 Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.EBI Pfizer Inc.
26022839 11 Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.EBI Bristol-Myers Squibb Research and Development
25953512 74 Discovery of (1R,2S)-2-{[(2,4-Dimethylpyrimidin-5-yl)oxy]methyl}-2-(3-fluorophenyl)-N-(5-fluoropyridin-2-yl)cyclopropanecarboxamide (E2006): A Potent and Efficacious Oral Orexin Receptor Antagonist.EBI Eisai Co., Ltd.
26102506 40 Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.EBI Celgene Corporation
26087021 94 Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.EBI TBA
26083478 66 Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.EBI Celgene Corporation
26005524 147 Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.EBI Merck Research Laboratories
26005523 37 Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.EBI Shanghai Institute of Materia Medica
25992974 14 Synthesis and Biological Evaluation of Novel Olean-28,13▀-lactams as Potential Antiprostate Cancer Agents.EBI China Pharmaceutical University
25906200 6 A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides.EBI University of Helsinki
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
25893046 77 Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.EBI Bristol-Myers Squibb Company
25893043 36 Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.EBI Pfizer Inc.
25087753 240 Prediction of Thorough QT study results using action potential simulations based on ion channel screens.EBI University of Oxford
21300721 90 Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.EBI University of Oxford
25790336 93 Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.EBI AstraZeneca
25978963 70 Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3).EBI Merck Research Laboratories
25911300 58 Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4).EBI Merck Research Laboratories
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
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
25494650 8 CNS drug design: balancing physicochemical properties for optimal brain exposure.EBI Eli Lilly and Company
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.
25686153 73 Design, synthesis, and biological evaluation of novel matrix metalloproteinase inhibitors as potent antihemorrhagic agents: from hit identification to an optimized lead.EBI University of Navarra
25658964 69 Synthesis and structure-activity relationship study of a new series of selectives(1) receptor ligands for the treatment of pain: 4-aminotriazoles.EBI Esteve
25633969 96 Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents.EBI University of Illinois at Chicago
25633741 67 Discovery and profiling of a selective and efficacious Syk inhibitor.EBI Novartis Institutes for Biomedical Research
25625541 58 Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.EBI Merck & Co., Inc.
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
25599836 14 Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.EBI Boehringer Ingelheim (Canada) Ltd
25594740 33 Identification of novel aminothiazole and aminothiadiazole conjugated cyanopyridines as selective CHK1 inhibitors.EBI Cairo University
25565255 49 Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.EBI Roche Pharmaceutical Research and Early Development
25557493 109 Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.EBI Jagiellonian University Collegium Medicum
25514658 182 Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3K▀ and PI3Kd for the treatment of PTEN-deficient cancers.EBI AstraZeneca
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
25851938 27 Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).EBI Merck Research Laboratories
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
25746816 3 Synthesis of 3-azabicyclo[3.2.2]nonanes and their antiprotozoal activities.EBI Karl-Franzens-University
25728416 25 Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.EBI Merck Research Laboratories
25614114 1 Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis.EBI CSIR-Central Drug Research Institute
25699151 57 An Orally Available BACE1 Inhibitor That Affords Robust CNS A▀ Reduction without Cardiovascular Liabilities.EBI Amgen Inc.
25699143 26 Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.EBI Pfizer Inc.
25613679 79 Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious▀-secretase inhibitors for the potential treatment of Alzheimer's disease.EBI Amgen 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.
25597005 86 The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.EBI Amgen Inc.
25415535 118 Inhibitors of c-Jun N-terminal kinases: an update.EBI Eberhard Karls Universit£t T£bingen
25133923 13 Design, synthesis, and biological evaluation of (3R)-1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) analogues: in vitro pharmacology and ADME profile.EBI Research Triangle Institute
25127154 24 Novel thienopyrimidinones as mGluR1 antagonists.EBI Yonsei University
25127101 26 Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.EBI Dainippon Sumitomo Pharma. Co. Ltd
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
25050161 112 Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.EBI AMRI
25050159 71 Investigation of Cardiovascular Effects of Tetrahydro-▀-carboline sstr3 antagonists.EBI Merck Research Laboratories
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
25017034 1 Confronting the challenges of discovery of novel antibacterial agents.EBI SBS Pharma Consulting LLC
25017033 148 Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.EBI University of Kansas Specialized Chemistry Center
25000588 72 Discovery of selective and orally bioavailable protein kinase C┐ (PKC┐) inhibitors from a fragment hit.EBI AbbVie Bioresearch Center
24974340 90 Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.EBI Korea University
24950374 9 2',6'-Dihalostyrylanilines, pyridines, and pyrimidines for the inhibition of the catalytic subunit of methionine S-adenosyltransferase-2.EBI University of Kentucky
24937104 30 GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.EBI AstraZeneca
24881566 140 Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).EBI GlaxoSmithKline
24856064 9 Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
25589932 60 Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.EBI Astex Pharmaceuticals, Inc.
25589928 37 Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.EBI Novartis Institutes for Biomedical Research
25589927 36 Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.EBI Novartis Institutes for Biomedical Research
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.
25488844 154 Discovery of 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamides as potent and selective CB2 receptor agonists.EBI Arena Pharmaceuticals
25456079 18 Discovery of novel tetrahydroisoquinoline derivatives as orally active N-type calcium channel blockers with high selectivity for hERG potassium channels.EBI Astellas Pharma Inc.
25454273 52 Anilinotriazoles as potent gamma secretase modulators.EBI Janssen Research& Development
25452001 19 Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists.EBI Korea Research Institute of Chemical Technology
25423286 26 Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes.EBI Pfizer Inc.
25420090 66 Synthesis and biological evaluation of novel sigma-1 receptor antagonists based on pyrimidine scaffold as agents for treating neuropathic pain.EBI Huazhong University of Science and Technology
25412409 51 Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.EBI University of Dundee
25389560 96 Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene▀-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.EBI Amgen Inc.
25369270 93 Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.EBI Galapagos NV
25363711 62 Inhibitors of▀-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).EBI Amgen, Inc.
25349648 29 Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.EBI Merck Research Laboratories
25343529 221 Targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors for developing effective antipsychotics: synthesis, biological characterization, and behavioral studies.EBI Universit£ degli Studi di Siena
25313449 8 Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.EBI University of Cape Town
25271963 93 Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.EBI AstraZeneca
25255433 2 Design, synthesis, in silico molecular docking and biological evaluation of novel oxadiazole based thiazolidine-2,4-diones bis-heterocycles as PPAR-┐ agonists.EBI Jamia Hamdard (Hamdard University)
25238555 3 Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.EBI University of Rochester Medical Center
25221656 116 Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-a-Oxyazetidine.EBI Korea University
25208139 40 Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.EBI Departments of Discovery Chemistry, Metabolic Diseases, Lead Evaluation, Computer-Assisted Drug Design, Discovery Toxicology, Exploratory Clinical and Translational Research, and Pharmaceutical Candi
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
25155913 32 Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.EBI AstraZeneca
25149506 20 Discovery and pharmacological profile of new hydrophilic 5-HT(4) receptor antagonists.EBI University of Oslo
24890090 1 Thiazolidine-2,4-diones derivatives as PPAR-┐ agonists: synthesis, molecular docking, in vitro and in vivo antidiabetic activity with hepatotoxicity risk evaluation and effect on PPAR-┐ gene expression.EBI Jamia Hamdard (Hamdard University)
24944750 24 Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.EBI Merck Research Laboratories
24914738 43 Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.EBI AstraZeneca
24904961 27 Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.EBI Qilu Pharmaceutical Co, Ltd
24900889 2 Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.EBI Merck Research Laboratories
24900876 56 Discovery of the Fibrinolysis Inhibitor AZD6564, Acting via Interference of a Protein-Protein Interaction.EBI AstraZeneca
24900864 21 Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.EBI Pfizer Inc.
24874895 42 Lead optimization of 1,4-azaindoles as antimycobacterial agents.EBI AstraZeneca
24871036 13 4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.EBI AstraZeneca
24852118 7 Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists.EBI Dainippon Sumitomo Pharma Co., Ltd
24809953 28 Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.EBI AstraZeneca
24805037 380 Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia.EBI Adamed Ltd.
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23149230 22 The discovery of a novel series of glucokinase activators based on a pyrazolopyrimidine scaffold.EBI AstraZeneca
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22931505 69 Chemokine receptor antagonists.EBI National Heart and Lung Institute
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22938049 29 Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.EBI Korea Institute of Science and Technology
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.
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23046966 43 Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development.EBI AstraZeneca
22809456 2 Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.EBI Hoffmann-La Roche Inc.
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22779702 53 Discovery of potent inhibitors of human and mouse fatty acid amide hydrolases.EBI Universit£ degli Studi di Siena
22779424 31 Novel N-linked aminopiperidine inhibitors of bacterial topoisomerase type II with reduced pK(a): antibacterial agents with an improved safety profile.EBI AstraZeneca
22770500 219 3-Oxoisoindoline-1-carboxamides: potent, state-dependent blockers of voltage-gated sodium channel Na(V)1.7 with efficacy in rat pain models.EBI AstraZeneca
22335555 43 1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate.EBI NeurAxon Inc.
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23018093 41 Targeting conserved water molecules: design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization.EBI Vernalis Ltd.
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22708838 13 Lead optimization of antimalarial propafenone analogues.EBI St. Jude Children's Research Hospital
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
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22548342 210 Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase¿ inhibitors.EBI Exelixis
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22540945 19 Rational evolution of a novel type of potent and selective proviral integration site in Moloney murine leukemia virus kinase 1 (PIM1) inhibitor from a screening-hit compound.EBI The University of Tokyo
22078216 146 2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.EBI Novartis Institutes for BioMedical Research
22985961 99 Synthesis and pharmacological investigation of azaphthalazinone human histamine H(1) receptor antagonists.EBI GlaxoSmithKline Medicines Research Centre
22939696 85 Phenethyl nicotinamides, a novel class of Na(V)1.7 channel blockers: structure and activity relationship.EBI AstraZeneca
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
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22858142 121 Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.EBI AstraZeneca
22858141 113 Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes.EBI Pfizer Inc.
22853997 3 Orally available pyridinylpyrimidine derivatives as novel RANKL-induced osteoclastogenesis inhibitors.EBI Astellas Pharma Inc.
22832315 85 Structure and activity relationship in the (S)-N-chroman-3-ylcarboxamide series of voltage-gated sodium channel blockers.EBI AstraZeneca
22832311 75 N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators.EBI Lundbeck Research USA, Inc.
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22185670 73 Oxadiazoles in medicinal chemistry.EBI AstraZeneca
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22677319 64 Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.EBI H. Lundbeck A/S
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22633692 51 Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease.EBI Arena Pharmaceuticals
22455383 16 Computational design and discovery of"minimally structured" hERG blockers.EBI University of Bologna
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19648007 3 Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.EBI Merck Research Laboratories
19646865 45 Discovery of a novel azepine series of potent and selective 5-HT2C agonists as potential treatments for urinary incontinence.EBI Pfizer Global Research and Development
19632840 43 Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists.EBI Tsukuba Research Institute
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
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
19616429 32 Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists.EBI GlaxoSmithKline Pharmaceuticals
19553115 96 Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.EBI Neurocrine Biosciences
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
19694468 136 Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) benzamide (ADL5747).EBI Adolor Corporation
19663387 29 Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.EBI Neurocrine Biosciences
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
19606870 53 Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).EBI Merck Research Laboratories
19604695 49 Synthesis and biological evaluation of imidazole derivatives as novel NOP/ORL1 receptor antagonists: exploration and optimization of alternative pyrazole structure.EBI Banyu Tsukuba Research Institute
19596193 72 Design, synthesis and evaluation of a novel cyclohexanamine class of neuropeptide Y Y1 receptor antagonists.EBI Tsukuba Research Institute
19564110 31 Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist.EBI Tsukuba Research Institute
19539471 130 Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.EBI Merck& Co. 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
19500979 74 Optimization of 2-piperidin-4-yl-acetamides as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Designing out hERG inhibition.EBI AstraZeneca R&D M£lndal
19487123 31 Optimization of a series of 2,4-diaminopyridines as neuropeptide Y Y1 receptor antagonists with reduced hERG activity.EBI Tsukuba Research Institute
19581086 37 The identification and optimisation of novel and selective diamide neuropeptide Y Y2 receptor antagonists.EBI GlaxoSmithKline
19556128 8 Tetrahydrocarbazole amides with potent activity against human papillomaviruses.EBI GlaxoSmithKline Research& Development
19331340 1 Rhynchophylline from Uncaria rhynchophylla functionally turns delayed rectifiers into A-Type K+ channels.EBI China Medical University
19359175 132 4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.EBI Pfizer Global Research and Development
19588934 71 Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.EBI Abbott Laboratories
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
19410451 31 The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.EBI Pfizer Global Research and Development
19199480 6 Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators.EBI Sirtris Pharmaceuticals
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
19492813 56 Antagonists of the calcium receptor I. Amino alcohol-based parathyroid hormone secretagogues.EBI GlaxoSmithKline
19459652 56 Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.EBI Tsukuba Research Institute
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
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
19327989 40 Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.EBI Pfizer Global R&D
19320488 171 1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.EBI Merck Research Laboratories
19297154 88 Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.EBI Millennium Pharmaceuticals, Inc
19290642 14 Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.EBI Johnson & Johnson Pharmaceutical R&D
19285862 30 Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes.EBI Pfizer Global Research and Development
19282174 85 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.EBI Pfizer Global Research and Development
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
19269173 81 7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.EBI Pfizer Global Research and Development
19231185 44 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.EBI Pfizer Global Research and Development
19231183 44 5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.EBI AstraZeneca
19208472 52 Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.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
19167884 16 The design and discovery of novel amide CCR5 antagonists.EBI Pfizer Global Research and Development
19121937 4 Discovery and SAR of benzyl phenyl ethers as inhibitors of bacterial phenylalanyl-tRNA synthetase.EBI Pfizer Global Research and Development
19097777 55 Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.EBI Merck Research Laboratories
19072656 110 Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.EBI University of Siena
19053768 64 Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.EBI Novartis Institutes for BioMedical Research
19036582 45 Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain.EBI GlaxoSmithKline
19014886 83 Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.EBI GlaxoSmithKline
19010676 28 Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.EBI Bristol-Myers Squibb Company
19006669 82 The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.EBI GlaxoSmithKline
18986805 39 Imidazole pyrimidine amides as potent, orally bioavailable cyclin-dependent kinase inhibitors.EBI AstraZeneca Pharmaceuticals
18954985 111 Novel 3,3-disubstituted pyrrolidines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.EBI Roche Palo Alto LLC
18954983 12 Identification of KD5170: a novel mercaptoketone-based histone deacetylase inhibitor.EBI Kalypsys, Inc.
18952421 60 Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18951790 109 SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).EBI Merck Research Laboratories
18948001 179 Quantitative structure-activity relationship of phenoxyphenyl-methanamine compounds with 5HT2A, SERT, and hERG activities.EBI Pfizer Global Research and Development
18841880 82 Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18835163 41 Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.EBI Merck Frosst Center for Therapeutic Research
18817368 57 Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.EBI Merck Research Laboratories
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.
18783943 35 Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.EBI Novartis Institutes for BioMedical Research
18768318 37 Synthesis and evaluation of a spiro-isobenzofuranone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18752953 111 Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.EBI F. Hoffmann-La Roche Ltd
18752952 31 Benzimidazole-substituted (3-phenoxypropyl)amines as histamine H3 receptor ligands.EBI The Schering Plough Research Institute
18701276 97 Highly functionalized 7-azaindoles as selective PPAR gamma modulators.EBI Merck Research Laboratories
18682323 58 Discovery of 1,3-disubstituted-1H-pyrrole derivatives as potent melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.EBI AstraZeneca R&D Mölndal
18640038 74 Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2.EBI Amgen Inc.
18632269 18 Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.EBI Abbott Laboratories
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
18625556 20 Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.EBI Institute of Science and Technology
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
18617397 21 Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.EBI AstraZeneca Pharmaceuticals
18598020 75 Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists.EBI Tsukuba Research Institute
18578472 16 Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.EBI Merck Research Laboratories
18550373 97 The design and synthesis of potent and cell-active allosteric dual Akt 1 and 2 inhibitors devoid of hERG activity.EBI Merck Research Laboratories
18547806 100 Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.EBI AstraZeneca R&D Boston
18540666 8 Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.EBI Merck Research Laboratories
18539028 81 Discovery of potent, orally active benzimidazole glucagon receptor antagonists.EBI Merck Research Laboratories
18537234 55 A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.EBI Tsukuba Research Institute
18515099 12 Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine.EBI Tsukuba Research Institute
18329269 77 Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.EBI Neurocrine Biosciences
18313293 26 Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.EBI Centre de Recherches
18164199 34 Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.EBI Merck Research Laboratories
18160289 119 1-Aminoindanes as novel motif with potential atypical antipsychotic properties.EBI Pfizer Global Research and Development
18060775 67 Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).EBI Merck Research Laboratories
18020391 12 From astemizole to a novel hit series of small-molecule somatostatin 5 receptor antagonists via GPCR affinity profiling.EBI F. Hoffmann-La Roche Ltd.
18020390 37 Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.EBI F. Hoffmann-La Roche Ltd.
17977724 83 Design and synthesis of potent amido- and benzyl-substituted cis-3-amino-4-(2-cyanopyrrolidide)pyrrolidinyl DPP-IV inhibitors.EBI Pfizer Global Research and Development
17976986 80 Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.EBI Pfizer Global Research & Development
17867665 41 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.EBI GlaxoSmithKline Medicine Research Centre
17851076 77 4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.EBI Merck Research Laboratories
17804233 29 Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.EBI Merck Research Laboratories
17804227 28 Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.EBI Merck Research Laboratories
17768047 33 Discovery of novel and orally active NR2B-selective N-methyl-D-aspartate (NMDA) antagonists, pyridinol derivatives with reduced HERG binding affinity.EBI Pfizer Global Research & Development
17766107 25 Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation.EBI Pfizer Global Research & Development
17766106 45 Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.EBI Pfizer Global Research & Development
17761419 16 Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.EBI Merck Research Laboratories
17761416 53 The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.EBI Merck Research Laboratories
17562364 150 Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.EBI Merck Research Laboratories
17498953 17 A new class of histamine H3 receptor antagonists derived from ligand based design.EBI F. Hoffmann-La Roche Ltd
17425296 161 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.EBI Abbott Laboratories
17418570 141 CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17395460 13 Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.EBI Merck Research Laboratories
17350253 51 Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.EBI Abbott Laboratories
17303420 24 The synthesis and biological evaluation of novel series of nitrile-containing fluoroquinolones as antibacterial agents.EBI Pfizer Global Research and Development
17267217 76 N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.EBI Pfizer Global Research and Development
17266208 104 Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.EBI Millennium Pharmaceuticals
17257843 35 A novel, non-substrate-based series of glycine type 1 transporter inhibitors derived from high-throughput screening.EBI Pfizer Inc.
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
17236777 28 The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.EBI Procter & Gamble Pharmaceuticals
17234405 34 An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.EBI Abbott Laboratories
17188866 17 Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.EBI Abbott Laboratories
17178222 29 Quinazoline and benzimidazole MCH-1R antagonists.EBI Argenta Discovery Limited
17125262 42 Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1.EBI GlaxoSmithKline
17125248 24 Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.EBI Merck Research Laboratories
17107796 26 Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG.EBI Procter & Gamble Pharmaceuticals
17107791 50 Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.EBI Procter & Gamble Pharmaceuticals
17098428 21 Core exploration in optimization of chemokine receptor CCR4 antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
17064075 107 Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.EBI Abbott Laboratories
16950617 50 N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II.EBI Merck Sharp & Dohme Research Laboratories
16942878 8 Discovery and synthesis of tetrahydroindolone-derived carbamates as Kv1.5 blockers.EBI Procter and Gamble Pharmaceuticals
16942874 10 Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers.EBI Procter & Gamble Pharmaceuticals
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
16814542 51 Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.EBI Neurocrine Biosciences Inc.
16789733 41 Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
16789729 25 A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.EBI Neurocrine Biosciences Inc.
16757170 40 Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.EBI F. Hoffmann-La Roche Ltd
16753297 29 Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.EBI Schering-Plough Research Institute
16722631 87 An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.EBI Predix Pharmaceuticals Ltd.
16640325 41 Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).EBI Millennium Pharmaceuticals
16632354 61 A new class of selective, non-basic 5-HT2A receptor antagonists.EBI Merck Sharp & Dohme
16631366 26 Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.EBI AstraZeneca
16574413 28 NK1 antagonists based on seven membered lactam scaffolds.EBI Merck Sharp and Dohme Research Laboratories
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
16529931 139 SAR studies: designing potent and selective LXR agonists.EBI Merck Research Laboratories
16524729 72 Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.EBI Millennium Pharmaceuticals, Inc.
16480279 71 A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinone.EBI Institute of Medical Research Biotechnology Centre
16458508 52 Identification and structure-activity relationships of a new series of Melanocortin-4 receptor antagonists.EBI Millennium Pharmaceuticals, Inc.
16458504 37 Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.EBI Columbia University College of Physicians and Surgeons
16439122 16 Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.EBI Merck Research Laboratories
16413782 20 1-Phenyl-8-azabicyclo[3.2.1]octane ethers: a novel series of neurokinin (NK1) antagonists.EBI Merck Sharp & Dohme Research Laboratories
16392798 46 Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.EBI Columbia University College of Physicians and Surgeons
16384700 24 Novel lactam NK1 antagonists with anti-emetic activity.EBI Merck Sharp & Dohme Research Laboratories
16361098 70 Synthesis and biological evaluation of novel hexahydro-pyrido[3',2':4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT(2C) receptor agonists.EBI F. Hoffmann-La Roche Ltd
16307878 25 Synthesis and structure-activity relationships of 8-azabicyclo[3.2.1]octane benzylamine NK1 antagonists.EBI Merck Sharp & Dohme Research Laboratories
16161992 29 Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.EBI Abbott Laboratories
16102966 55 Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.EBI Merck Research Laboratories
15993598 55 4-Fluorosulfonylpiperidines: selective 5-HT2A ligands for the treatment of insomnia.EBI Merck Sharp and Dohme
15878274 33 Discovery of potent and use-dependent sodium channel blockers for treatment of chronic pain.EBI Merck Research Laboratories
15837299 11 NMDA-NR2B subtype selectivity of stereoisomeric 2-(1,2,3,4-tetrahydro-1-isoquinolyl)ethanol derivatives.EBI Ludwig-Maximilians-Universität München
15808483 30 Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.EBI Merck Research Laboratories
15771419 134 Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.EBI Johnson & Johnson Pharmaceutical Research & Development
15686947 1 Discovery and structure-activity relationships of 2-benzylpyrrolidine-substituted aryloxypropanols as calcium-sensing receptor antagonists.EBI Bristol-Myers Squibb Pharmaceutical Research Institute
15615511 8 Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.EBI Abbott Laboratories
15546728 15 Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.EBI Aventis Pharmaceuticals
15380217 87 Potent and selective proline derived dipeptidyl peptidase IV inhibitors.EBI Merck & Co. Inc.
15012999 166 Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.EBI Merck Research Laboratories
14980678 88 Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.EBI Merck Research Laboratories
14684294 79 4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.EBI Merck & Co. Inc.
12773045 27 Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.EBI Merck Frosst Centre for Therapeutic Research
12067555 31 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.EBI Merck Sharp & Dohme Research Laboratories
11334570 103 3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.EBI Merck Sharp and Dohme
9397166 25 Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.EBI Merck Research Laboratories
28135068 9 Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease.BDB Exonate Ltd
17221184 55 Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.BDB Columbia University
16352709 44 Antidepressant-like activity and modulation of brain monoaminergic transmission by blockade of anandamide hydrolysis.BDB McGill University
12176106 20 A comparison of the receptor binding and HERG channel affinities for a series of antipsychotic drugs.BDB Aventis Pharmaceuticals, Inc.
19398200 45 Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.BDB Banyu Pharmaceutical Co.
19394217 14 2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists.BDB Banyu Pharmaceutical Co.
19447610 39 Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists.BDB Banyu Pharmaceutical Co.
18588282 63 Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.BDB Johnson & Johnson Pharmaceutical
17766111 17 Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.BDB Merck Research Laboratories
16603356 27 Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.BDB Merck Research Laboratories
16439123 25 Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.BDB Merck Research Laboratories
18307293 75 2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.BDB Neuroscience