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152 articles for thisTarget

The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27774132 20 Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.EBI Takeda Pharmaceutical Company Limited
27690432 75 Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI CHARLES RIVER DISCOVERY RESEARCH SERVICES UK LIMITED
27687967 17 Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.EBI Takeda Pharmaceutical Company Ltd
27211244 9 Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.EBI University of Florida
26978477 25 Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of▀-Secretase.EBI Amgen, Inc.
26670264 73 Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV.EBI Latvian Institute of Organic Synthesis
26608551 35 Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.EBI Korea University of Science and Technology
25167370 75 Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.EBI The Walter and Eliza Hall Institute of Medical Research
26001341 19 Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.EBI Lilly 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
25695670 35 Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.EBI Eurofarma Laboratorios S.A.
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
25728416 25 Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.EBI Merck Research Laboratories
25613679 79 Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious▀-secretase inhibitors for the potential treatment of Alzheimer's disease.EBI Amgen Inc.
25086681 57 Structure-based optimization of non-peptidic Cathepsin D inhibitors.EBI Merck KGaA
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
25537272 17 Structure-based design, synthesis and biological evaluation of novel▀-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.EBI Purdue University
25455483 61 Discovery of potent iminoheterocycle BACE1 inhibitors.EBI Merck Research Laboratories
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.
25313316 20 3-Cyano-3-aza-▀-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.EBI University of Bonn
24921156 6 Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease.EBI University of Coimbra
24900843 60 Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.EBI Latvian Institute of Organic Synthesis
24397738 41 Discovery of 7-tetrahydropyran-2-yl chromans:▀-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid▀-protein (A▀) in the central nervous system.EBI Array BioPharma
23993670 2 Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.EBI Kyoto Pharmaceutical University
24054120 5 The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations.EBI Novartis Institutes for Biomedical Research
23981898 20 Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective▀-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid▀-peptides.EBI Novartis Pharma AG
23856050 28 Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.EBI Elan Pharmaceuticals
23769639 17 Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.EBI Amgen Inc.
23570791 2 Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.EBI Elan Pharmaceuticals
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
23537249 165 Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.EBI Array BioPharma
23425156 24 The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.EBI Novartis Pharma AG
23360239 19 A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.EBI Novartis Pharma AG
23181502 57 Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.EBI University of Florida
22954357 29 Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.EBI Purdue University
22928914 104 Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.EBI Amgen Inc.
23010268 32 Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates.EBI Medivir AB
24900544 8 Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.EBI TBA
22884991 9 Antiplasmodial activities of 4-aminoquinoline-statine compounds.EBI Universit£ degli Studi di Milano
22748705 2 Total synthesis of grassystatin A, a probe for cathepsin E function.EBI Fudan University
22727644 43 Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.EBI University of South Florida
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
22572583 49 Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.EBI Envoy Therapeutics
20579874 150 BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.EBI GlaxoSmithKline R&D
20045648 39 Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
19811916 83 Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.EBI Elan Pharmaceuticals
19419206 77 Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.EBI Ewha Womans University
18434152 64 Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.EBI LG Life Sciences
18417344 6 Identification of acridinyl hydrazides as potent aspartic protease inhibitors.EBI University of Karachi
17980584 72 Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.EBI Schering-Plough Research Institute
18171614 63 BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).EBI GlaxoSmithKline R&D
18068983 51 Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.EBI Wyeth Research
18023580 50 Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.EBI Schering-Plough Research Institute
16797987 11 Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors.EBI Institute of Medicinal and Aromatic Plants
15139758 50 Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.EBI Universitat Pompeu Fabra
10669559 180 Protease inhibitors: current status and future prospects.EBI University of Queensland
1527792 55 Specific inhibition of HIV-1 protease by boronated porphyrins.EBI University of California
2002469 80 Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.EBI Merck Sharp and Dohme Research Laboratories
3906131 61 Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.EBI TBA
10498202 43 Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.EBI Bayer Corporation
9873534 36 Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.EBI Pharmacopeia, Inc.
 37 Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability propertiesEBI TBA
22204908 22 New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships.EBI University of Karachi
22130130 19 Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.EBI Merck Research Laboratories
21835615 165 New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.EBI Pfizer Inc.
21388807 45 Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.EBI Novartis Institutes for BioMedical Research
21112780 30 Design and synthesis of potent macrocyclic renin inhibitors.EBI Medivir AB
20731374 65 Direct renin inhibitors as a new therapy for hypertension.EBI Novartis Pharmaceuticals Corp
20943389 2 Triazolyl tryptoline derivatives asß-secretase inhibitors.EBI Mahidol University
20880704 200 Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI Pfizer Inc.
20833041 40 Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.EBI Elan Pharmaceuticals
20822903 87 Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.EBI Elan Pharmaceuticals
20656487 45 Fragment-based discovery and optimization of BACE1 inhibitors.EBI Evotec UK Ltd
20347593 76 Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.EBI Merck Research Laboratories
20438064 14 Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents.EBI Wayne State University
20223661 48 Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.EBI Princ
20202842 47 Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.EBI Wyeth Research
20172717 35 Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.EBI Universit£ de Montr£al
20102207 7 Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.EBI China Medical University
20036448 20 Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.EBI Link£ping University
20128595 24 Design and synthesis of potent and selective BACE-1 inhibitors.EBI Stockholm University
20122837 21 Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core.EBI Stockholm University
19963375 30 Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.EBI Novartis Institutes for BioMedicalResearch
19959359 46 Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19968289 201 Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19757823 98 Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
20043696 17 Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.EBI Schering-Plough Research Institute
19635672 35 alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.EBI Uppsala University
19576765 15 Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.EBI Uppsala University
19195887 18 Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.EBI Novartis Institutes for BioMedical Research
 10 Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteresEBI TBA
 6 Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV proteaseEBI TBA
 25 Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin DEBI TBA
 22 Novel pseudosymmetric inhibitors of HIV-1 proteaseEBI TBA
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
19323561 11 Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.EBI Purdue University
18842420 44 Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.EBI Linköping University
18468890 69 Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.EBI Schering-Plough Research Institute
17638694 2 In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.EBI Ambrilia Biopharma, Inc.
18166458 90 BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.EBI GlaxoSmithKline R&D
18162398 43 Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.EBI Wyeth Research
17482814 37 Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI Merck Research Laboratories
17434734 28 Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.EBI Pfizer Global Research and Development
17433698 6 Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).EBI Technische Universität München
17046251 38 Design of potent inhibitors of human beta-secretase. Part 1.EBI Pfizer Inc.
16162010 78 Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.EBI Uppsala University
15974592 68 Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II.EBI Linköping University
14741251 12 Rational design and synthesis of selective BACE-1 inhibitors.EBI Merck Research Laboratories
11906282 6 Molecular dynamics and free energy analyses of cathepsin D-inhibitor interactions: insight into structure-based ligand design.EBI University of California
10212129 20 Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.EBI University of California
9873703 4 Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.EBI Pharmacopeia, Inc.
8410992 35 Renin inhibitors containing a pyridyl amino diol derived C-terminus.EBI Hoechst AG
8410973 75 Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation.EBI University of Florida
3126296 43 Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases.EBI University of Wisconsin
1738148 16 Renin inhibitory pentols showing improved enteral bioavailability.EBI Hoechst AG
28427814 24 Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.EBI Purdue University
20063996 12 Characterisation of hydrazides and hydrazine derivatives as novel aspartic protease inhibitors.BDB University of Karachi
16892342 10 Unexpected novel binding mode of pyrrolidine-based aspartyl protease inhibitors: design, synthesis and crystal structure in complex with HIV protease.BDB Philipps-Universitńt Marburg
9195867 15 Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D.BDB University of California Berkeley
19406640 58 Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.BDB GSK
19477642 87 Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.BDB GSK
19428244 60 Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.BDB GSK
19195886 22 Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.BDB Novartis
18171615 69 BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.BDB GSK
18457381 36 Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.BDB GSK
17850059 195 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase.BDB Montana State University
17685503 6 2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead.BDB Johnson & Johnson Pharmaceutical
17034121 20 Acylguanidines as small-molecule beta-secretase inhibitors.BDB Wyeth Research
17432843 22 Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.BDB Purdue University
16620080 15 Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.BDB Purdue University
16854060 58 Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).BDB Universite de Montreal at Succursale Centre-Ville
16078837 34 Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.BDB Universite de Montreal at Succursale Centre-Ville
12857114 102 High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II.BDB Uppsala University
12593654 48 Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.BDB Uppsala University
14695825 67 Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.BDB Uppsala University
15189032 66 Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs.BDB Linkoping University