345 articles for thisTarget

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PMID	Data	Article Title	Organization
27721153	18	Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation.	Jagiellonian University Medical College
28043778	3	Neuritogenic activity of bi-functional bis-tryptoline triazole.	Chiang Mai University
27816517	14	Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.	Bristol-Myers Squibb
27104967	1	Pregnane-10,2-carbolactones from a Hawaiian Marine Sponge in the Genus Myrmekioderma.	University Of Hawaii At Manoa
27046190	10	Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.	Tu Dortmund University
27211244	9	Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.	University Of Florida
26978477	25	Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.	Amgen
26985314	23	Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents.	Bristol-Myers Squibb
26937601	55	Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.	Merck Research Laboratories
27102162	1	Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors.	Birla Institute Of Technology
26696252	32	Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3ß Inhibitors.	Alma Mater Studiorum-University Of Bologna
26632651	70	Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.	China Pharmaceutical University
26608551	35	Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.	Korea University Of Science And Technology
26614409	1	Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors.	Birla Institute Of Technology
26378740	37	1,4-Oxazineß-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.	Janssen Pharmaceutica
26497283	68	Macrocyclic prolinyl acyl guanidines as inhibitors ofß-secretase (BACE).	Bristol-Myers Squibb
26264846	15	Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors.	Kyoto Pharmaceutical University
26003339	12	From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.	University Of Bologna
25167370	75	Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.	The Walter And Eliza Hall Institute Of Medical Research
26061085	13	Peptidomimeticß-Secretase Inhibitors Comprising a Sequence of Amyloid-ß Peptide for Alzheimer's Disease.	Instituto De Biologia Experimental E Tecnol£Gica
26003344	48	Isolation of cholinesterase andß-secretase 1 inhibiting compounds from Lycopodiella cernua.	Catholic University Of Daegu
26001341	19	Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.	Eli Lilly
25941546	9	4,6-Diarylaminothiazines as BACE1 Inhibitors and Their Use for the Reduction of Beta-Amyloid Production.	Temple University
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.	The Scripps Research Institute
25695670	35	Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.	Eurofarma Laboratorios
25842365	21	Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.	Fudan University
25782742	76	trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.	Novartis Pharma
25754490	44	trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.	Novartis Pharma
25728416	25	Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.	Merck Research Laboratories
25736996	1	Novelß-amyloid aggregation inhibitors possessing a turn mimic.	Kobe Pharmaceutical University
25699151	57	An Orally Available BACE1 Inhibitor That Affords Robust CNS Aß Reduction without Cardiovascular Liabilities.	Amgen
25613679	79	Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.	Amgen
25088549	47	Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aß aggregation, andß-secretase.	Central China Normal University
25050166	58	Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.	Novartis Institutes For Biomedical Research
25537272	17	Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.	Purdue University
25455483	61	Discovery of potent iminoheterocycle BACE1 inhibitors.	Merck Research Laboratories
25411915	54	8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.	Array Biopharma
25389560	96	Lead optimization and modulation of hERG activity in a series of aminooxazoline xantheneß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.	Amgen
25363711	62	Inhibitors ofß-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).	Amgen
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.	University Of Coimbra
24835197	13	ß-Secretase (BACE1)-inhibiting C-methylrotenoids from Abronia nana suspension cultures.	Kyungpook National University
24780121	19	Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.	Genentech
24704031	69	The evolution of amidine-based brain penetrant BACE1 inhibitors.	Janssen Pharmaceutica
24568372	40	Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents.	Universitat De Barcelona
24763262	8	4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies.	Peking University Health Science Center
24900714	8	?-Secretase Inhibitors for the Treatment of Alzheimer's Disease and Down's Syndrome.	Therachem Research Medilab (India)
23590342	105	ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.	F. Hoffmann-La Roche
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.	Array Biopharma
23480856	22	Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors ofß-secretase (BACE1).	Tehran University Of Medical Sciences
23465612	17	Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.	Elan Pharmaceuticals
24900681	13	Cyclopropyl-Fused 1,3-Thiazepines as BACE1 and BACE2 Inhibitors.	Temple University
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.	Novartis Pharma
23374014	24	Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.	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.	Novartis Pharma
23219701	1	Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease.	Universidad Complutense
23218605	17	Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.	Universit£
22325942	31	Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.	Astrazeneca
21093114	61	Self-organizing molecular field analysis on humanß-secretase nonpeptide inhibitors: 5, 5-disubstituted aminohydantoins.	Sichuan University
21381769	56	Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.	Universite£
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.	University Of Florida
23030502	86	Acyl guanidine inhibitors ofß-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.	Bristol-Myers Squibb Research
23017051	69	New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.	Astrazeneca
22989333	43	Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.	Merck Research Laboratories
22984865	43	Spirocyclic sulfamides asß-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.	Pfizer
22954357	29	Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.	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.	Amgen
22924815	97	Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.	Astrazeneca
22468999	20	Discovery and optimization of a novel spiropyrrolidine inhibitor ofß-secretase (BACE1) through fragment-based drug design.	Pfizer
22468684	76	Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.	Amgen
22468639	26	Design and preparation of a potent series of hydroxyethylamine containingß-secretase inhibitors that demonstrate robust reduction of centralß-amyloid.	Amgen
22998419	47	Conformational restriction approach toß-secretase (BACE1) inhibitors: effect of a cyclopropane ring to induce an alternative binding mode.	Shionogi
22506484	6	Structural modifications that alter the P-glycoprotein efflux properties of compounds.	Envoy Therapeutics
23041347	33	Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.	Central China Normal University
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.	Medivir
24900397	18	Compounds and Their Use as BACE Inhibitors: Patent Highlight.	TBA
24900396	8	5-Amino-oxazepine and 5-Amino-thiazepine Compounds as ß-Secretase Antagonists and Methods of Use: Patent Highlight.	TBA
24900395	3	BACE-Inhibitors: Potential Treatment of Alzheimer Disease, Dementia, and Related Neurodegenerative Diseases. C. Spiro-Heterocyclic Derivatives: Patent Highlight.	TBA
24900394	8	BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (B): 3-Amino-4-fluoro-1H-isoindol Derivatives: Patent Highlight.	TBA
24900393	4	BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (A): 5,6-Dihydroimidazo[1,2-a]pyrazin-8-yl-amine Derivatives: Patent Highlight.	TBA
23412139	26	Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aß Reduction.	TBA
24900403	42	A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of ß-Secretase.	TBA
22863204	17	Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potentß-secretase inhibitors.	Purdue University
22727644	43	Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.	University Of South Florida
22409666	4	Modern phenotypic drug discovery is a viable, neoclassic pharma strategy.	Eli Lilly
22726930	7	Novel BACE1 inhibitors possessing a 5-nitroisophthalic scaffold at the P2 position.	Kobe Gakuin University
22704921	34	Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.	University Of Waterloo
22698785	28	Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: design, synthesis and X-ray crystal structures of enzyme inhibitor complexes.	Link£Ping University
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.	Novartis Pharma
24900449	10	BACE1 Inhibitor Peptides: Can an Infinitely Small k cat Value Turn the Substrate of an Enzyme into Its Inhibitor?	TBA
22572583	49	Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.	Envoy Therapeutics
22243648	112	New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, andß-amyloid-reducing properties.	Instituto De Qu£Mica M£Dica
22390835	80	Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.	Merck Research Laboratories
22185619	50	Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.	Universitat De Barcelona
22165820	22	Fragment based drug discovery: practical implementation based on¹¿F NMR spectroscopy.	Amgen
20620068	8	Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.	Zhejiang University
20634069	42	Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.	Elan Pharmaceuticals
20598535	21	beta-Secretase (BACE-1) inhibitory effect of biflavonoids.	Shujitsu University
20579874	150	BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.	Glaxosmithkline
19854048	3	Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening.	University Of Leeds
20045648	39	Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.	Wyeth Research
19715320	87	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.	University Of Florida
19811916	83	Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.	Elan Pharmaceuticals
18565755	8	BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens.	Gyeongsang National University School Of Medicine
18434152	64	Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.	Lg Life Sciences
17980584	72	Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.	Schering-Plough Research Institute
18171614	63	BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).	Glaxosmithkline
18226904	8	Tyramine fragment binding to BACE-1.	F. Hoffmann-La Roche
18249539	6	BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.	Kyoto Pharmaceutical University
18068983	51	Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.	Wyeth Research
18023580	50	Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.	Schering-Plough Research Institute
17998161	19	Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.	University Of Bologna
18181565	71	Multi-target-directed ligands to combat neurodegenerative diseases.	University Of Bologna
17985861	5	Discovery of a novel warhead against beta-secretase through fragment-based lead generation.	Astrazeneca R&D
15341936	17	Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.	Johnson & Johnson Pharmaceutical Research And Development
12747779	13	Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.	Johnson & Johnson Pharmaceutical Research And Development
11784130	42	Design of substrate-based inhibitors of human beta-secretase.	TBA
11405641	8	Secretase targets for Alzheimer's disease: identification and therapeutic potential.	Harvard Medical School
14684336	20	P3 cap modified Phe*-Ala series BACE inhibitors.	Eli Lilly
14684335	21	Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.	Eli Lilly
14643321	31	Design and synthesis of statine-containing BACE inhibitors.	Eli Lilly
22225636	11	The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not aß-secretase inhibitor.	Beijing Institute Of Pharmacology And Toxicology
22178553	10	Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design.	Kobe Gakuin University
22054058	22	Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.	University Of Bologna
22222157	55	Structure-activity relationships for naturally occurring coumarins asß-secretase inhibitor.	Kinki University
22209418	5	A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.	Sissa-Isas
22130130	19	Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.	Merck Research Laboratories
21452857	6	On a possible neutral charge state for the catalytic dyad inß-secretase when bound to hydroxyethylene transition state analogue inhibitors.	Universidad De Santiago De Compostela
22019465	28	Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.	Zhejiang University
22071305	24	Rational design and synthesis of aminopiperazinones asß-secretase (BACE) inhibitors.	Research Informatics & Integrative Genomics
22044119	84	Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads.	University Of Sharjah
21992804	1	Daedalols A-C, fungal-derived BACE1 inhibitors.	University Of Hawaii At Manoa
21782431	95	Monosubstituted¿-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors ofß-secretase (BACE).	Bristol-Myers Squibb
21974952	31	Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.	Bristol-Myers Squibb Research And Development
21986588	19	Carbazole-containing arylcarboxamides as BACE1 inhibitors.	Universit£
21835615	165	New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.	Pfizer
21707077	54	From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).	Amgen
21803585	12	Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.	Kyoto Pharmaceutical University
21798635	32	Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.	Institut F£R Molekulare Physiologie
21621412	6	Triazole-linked reduced amide isosteres: an approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors.	Virginia Tech
19447035	16	Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay.	Singapore Polytechnic
21511472	13	Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on β-secretase (BACE-1).	Gyeongsang National University
21388807	45	Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.	Novartis Institutes For Biomedical Research
21441028	18	Synthesis and evaluation of arylquinones as BACE1 inhibitors,β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils.	Universidad Complutense
21112780	30	Design and synthesis of potent macrocyclic renin inhibitors.	Medivir
21183353	27	Investigation ofa-phenylnorstatine anda-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors.	Uppsala University
20934348	8	BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides.	University Of Pisa
20943389	2	Triazolyl tryptoline derivatives asß-secretase inhibitors.	Mahidol University
20880704	200	Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.	Pfizer
20850315	17	Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors.	Singapore Polytechnic
20833041	40	Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.	Elan Pharmaceuticals
20822903	87	Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.	Elan Pharmaceuticals
20806907	1	Topsentinols, 24-isopropyl steroids from the marine sponge Topsentia sp.	University Of Hawaii At Manoa
20656487	45	Fragment-based discovery and optimization of BACE1 inhibitors.	Evotec
20420456	6	Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.	University Of Bologna
20503979	9	Xestosaprols from the Indonesian marine sponge Xestospongia sp.	University Of Hawaii At Manoa
20378363	135	Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.	Applied Science University
20303626	33	Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors.	Institute Of Science And Technology
20462757	15	Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.	Pukyong National University
20399652	22	Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.	Johnson & Johnson Pharmaceutical Research & Development
20381362	8	Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.	Kyoto Pharmaceutical University
20347593	76	Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.	Merck Research Laboratories
20153560	10	Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase.	Peking University
20223661	48	Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.	Wyeth
20202842	47	Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.	Wyeth Research
20176482	42	SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.	Merck Research Laboratories
20172717	35	Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.	Universit£
20036448	20	Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.	Link£Ping University
19939683	7	Biotransformation of isoimperatorin and imperatorin by Glomerella cingulata and beta-secretase inhibitory activity.	Kinki University
20128595	24	Design and synthesis of potent and selective BACE-1 inhibitors.	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.	Stockholm University
19963375	30	Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.	Novartis Institutes For Biomedical Research
19959359	46	Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.	Wyeth Research
19968289	201	Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.	Wyeth Research
19640712	5	A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.	Merck Research Laboratories
19757823	98	Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.	Wyeth Research
20043700	5	Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.	Schering-Plough Research Institute
20043696	17	Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.	Schering-Plough Research Institute
19995674	17	P2'-truncated BACE-1 inhibitors with a novel hydroxethylene-like core.	Stockholm University
19788239	8	Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors.	University Of Sharjah
19576765	15	Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.	Uppsala University
19523824	3	Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).	Technische Universit£T M£Nchen
19375914	116	Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.	Bristol-Myers Squibb Research And Development
19195887	18	Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.	Novartis Institutes For Biomedical Research
19409780	11	Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.	Merck Research Laboratories
19345096	10	Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.	Kyoto Pharmaceutical University
19323561	11	Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.	Purdue University
19162488	57	Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.	Chinese Academy Of Sciences
19013792	37	Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.	University Of Illinois At Chicago
19013073	2	Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.	Zhejiang University
18842420	44	Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.	LinköPing University
18468890	69	Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.	Schering-Plough Research Institute
18457385	41	Recent developments in fragment-based drug discovery.	Astex Therapeutics
18334299	6	Tetramic and tetronic acids: an update on new derivatives and biological aspects.	University Of Bayreuth
18261904	10	Novel non-peptidic and small-sized BACE1 inhibitors.	Kyoto Pharmaceutical University
18180160	17	Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.	Purdue University
18166458	90	BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.	Glaxosmithkline
18162398	43	Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.	Wyeth Research
17985862	45	Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.	Astrazeneca Pharmaceuticals
17827011	12	Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.	Merck Research Laboratories
17761418	16	Thiophene substituted acylguanidines as BACE1 inhibitors.	Wyeth Research
17583334	13	Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.	TBA
17482814	37	Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.	Merck Research Laboratories
17434734	28	Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.	Pfizer
17433698	6	Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).	Technische UniversitäT MüNchen
17049233	82	Design of potent inhibitors of human beta-secretase. Part 2.	Pfizer
17046251	38	Design of potent inhibitors of human beta-secretase. Part 1.	Pfizer
16757166	4	beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.	Kyoto Pharmaceutical University
16481167	8	Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.	Kyoto Pharmaceutical University
16412632	17	BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.	University Of The Mediterranean
16078830	12	Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.	University Of ZüRich
15582441	5	Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.	Kyoto Pharmaceutical University
15582431	1	Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.	National Institute Of Health Sciences
15509178	37	Efficient evaluation of binding free energy using continuum electrostatics solvation.	University Of ZüRich
15177452	13	Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.	Wyeth Research
15006396	4	KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.	Kyoto Pharmaceutical University
14741251	12	Rational design and synthesis of selective BACE-1 inhibitors.	Merck Research Laboratories
14643307	1	KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.	Kyoto Pharmaceutical University
14592472	15	Green tea catechins as a BACE1 (beta-secretase) inhibitor.	Kyungpook National University
14561080	9	Human beta-secretase (BACE) and BACE inhibitors.	Elan Pharmaceuticals
12723942	38	Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.	Elan Pharmaceuticals
28749667	10	BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.	University Of Dundee
28539221	1	Lodopyridones B and C from a marine sediment-derived bacterium Saccharomonospora sp.	Ewha Womans University
28537720	5	Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances.	University Of Porto
28427814	24	Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.	Purdue University
22994801	7	Synthesis and paroxonase activities of novel bromophenols.	Atatürk University
21067438	10	Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.	Instituto Superior Técnico
20939763	15	Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors.	Sun Yat-Sen University
28134508	18	Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.	Syracuse University
9225287	174	RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.	Roche Bioscience
9223586	8	[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors.	Georgetown University
9223553	16	[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.	Institut De Recherches Servier
7616392	5	Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells.	Sanofi Recherche
6325601	52	Cholecystokinin receptors: biochemical demonstration and autoradiographical localization in rat brain and pancreas using [3H] cholecystokinin8 as radioligand.	F. Hoffmann-La Roche
6317122	20	Ligand binding to thromboxane receptors on human platelets: correlation with biological activity.	University Of Edinburgh
1738111	26	Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release.	University Of Texas
12498885	9	Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.	Massachusetts Institute Of Technology
11410378	50	Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase.	Northwestern University
11182316	22	Energetic, structural, and antimicrobial analyses of beta-lactam side chain recognition by beta-lactamases.	Northwestern University
18785742	18	A novel class of small molecule inhibitors of Hsp90.	Yale University
18408713	2	Identification of RIP1 kinase as a specific cellular target of necrostatins.	Tufts University
18835174	17	Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.	Astellas Pharma
17349580	6	Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.	Harvard Medical School
17049248	19	Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.	Astellas Pharma
17601739	30	Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.	Astellas Pharma
18412317	23	(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor with Reduced Myotoxicity Potential.	Bristol-Myers Squibb
12773033	17	A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.	Pfizer
17004721	49	Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor	Schering-Plough Research Institute
16033281	19	Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.	Bristol-Myers Squibb Pharmaceutical Research Institute
10794700	40	1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.	Universitat Des Saarlandes
16279787	14	Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.	University Of Bologna
15653343	20	Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.	Uppsala University
7518523	90	Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.	Pfizer
15239657	30	Novel azapeptide inhibitors of hepatitis C virus serine protease.	Boehringer Ingelheim (Canada)
7504733	33	Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.	Glaxo Group Research
12699382	4	An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study.	Academy Of Sciences Of The Czech Republic