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81 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
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
26061085 13 Peptidomimetic▀-Secretase Inhibitors Comprising a Sequence of Amyloid-▀ Peptide for Alzheimer's Disease.EBI Instituto de Biologia Experimental e Tecnol£gica
26001341 19 Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.EBI Lilly Research Laboratories
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
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
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.
24704031 69 The evolution of amidine-based brain penetrant BACE1 inhibitors.EBI Janssen Research and Development
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
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
23374014 24 Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.EBI University of Leeds
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
23017051 69 New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.EBI AstraZeneca
22954357 29 Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.EBI Purdue University
22924815 97 Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.EBI AstraZeneca
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
23412139 26 Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS A▀ Reduction.EBI TBA
22390835 80 Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.EBI Merck Research Laboratories
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
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
18023580 50 Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.EBI Schering-Plough Research Institute
14684335 21 Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.EBI Lilly Research Laboratories
22130130 19 Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.EBI Merck Research Laboratories
22044119 84 Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads.EBI University of Sharjah
21835615 165 New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.EBI Pfizer Inc.
20880704 200 Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI Pfizer Inc.
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
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
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
19323561 11 Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.EBI Purdue University
19013792 37 Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.EBI University of Illinois at Chicago
18468890 69 Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.EBI Schering-Plough Research Institute
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
17433698 6 Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).EBI Technische Universität München
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
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
17034121 20 Acylguanidines as small-molecule beta-secretase inhibitors.BDB Wyeth Research
15588077 15 Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).BDB Merck Research Laboratories
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