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218 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review

PMID
Data
Article Title
Organization
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor.EBI
Takeda Pharmaceutical
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI
Charles River Discovery Research Services
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.EBI
Takeda Pharmaceutical
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.EBI
University of Florida
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.EBI
Amgen
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
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.EBI
Korea University of Science and Technology
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
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.EBI
Eli Lilly
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
Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.EBI
Eurofarma Laboratorios
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
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
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.EBI
Merck Research Laboratories
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.EBI
Amgen
Structure-based optimization of non-peptidic Cathepsin D inhibitors.EBI
Merck
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.EBI
Novartis Institutes For Biomedical Research
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.EBI
Purdue University
Discovery of potent iminoheterocycle BACE1 inhibitors.EBI
Merck Research Laboratories
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).EBI
Amgen
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.EBI
University of Bonn
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
Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.EBI
Latvian Institute of Organic Synthesis
Discovery of 7-tetrahydropyran-2-yl chromans:ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloidß-protein (Aß) in the central nervous system.EBI
Array Biopharma
Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position.EBI
Kyoto Pharmaceutical University
The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations.EBI
Novartis Institutes For Biomedical Research
Discovery of cyclic sulfoxide 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
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.EBI
Elan Pharmaceuticals
Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity.EBI
Amgen
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.EBI
Elan Pharmaceuticals
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.EBI
F. Hoffmann-La Roche
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
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
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.EBI
Novartis Pharma
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
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.EBI
Purdue University
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
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
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.EBI
TBA
Antiplasmodial activities of 4-aminoquinoline-statine compounds.EBI
University of Milan
Total synthesis of grassystatin A, a probe for cathepsin E function.EBI
Fudan University
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.EBI
University of South Florida
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
Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.EBI
Envoy Therapeutics
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.EBI
Glaxosmithkline
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University of Florida
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.EBI
Elan Pharmaceuticals
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.EBI
Ewha Womans University
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.EBI
Lg Life Sciences
Identification of acridinyl hydrazides as potent aspartic protease inhibitors.EBI
University of Karachi
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.EBI
Schering-Plough Research Institute
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).EBI
Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.EBI
Wyeth Research
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.EBI
Schering-Plough Research Institute
Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors.EBI
Institute of Medicinal and Aromatic Plants
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.EBI
Universitat Pompeu Fabra
Protease inhibitors: current status and future prospects.EBI
University of Queensland
Non-peptide renin inhibitors containing 2-(((3-phenylpropyl)phosphoryl)oxy)alkanoic acid moieties as P2-P3 replacements.EBI
E. Merck Darmstadt
Potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme identified in rat lung.EBI
Abbott Laboratories
Specific inhibition of HIV-1 protease by boronated porphyrins.EBI
University of California
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.EBI
Parke-Davis Pharmaceutical Research Division of Warner-Lambert
Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.EBI
Warner-Lambert
Renin inhibitors containing esters at the P2-position. Oral activity in a derivative of methyl aminomalonate.EBI
Warner-Lambert
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics.EBI
Merck Sharp and Dohme Research Laboratories
Substrate analogue renin inhibitors containing replacements of histidine in P2 or isosteres of the amide bond between P3 and P2 sites.EBI
E. Merck Darmstadt
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.EBI
Kissei Pharmaceutical
Inhibition of cathepsin D by substrate analogues containing statine and by analogues of pepstatin.EBI
TBA
Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.EBI
TBA
Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone, and related analogues.EBI
TBA
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine.EBI
TBA
Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.EBI
TBA
Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors.EBI
Bayer
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.EBI
Pharmacopeia
 
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability propertiesEBI
TBA
New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships.EBI
University of Karachi
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.EBI
Merck Research Laboratories
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.EBI
Pfizer
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.EBI
Novartis Institutes For Biomedical Research
Design and synthesis of potent macrocyclic renin inhibitors.EBI
Medivir
Direct renin inhibitors as a new therapy for hypertension.EBI
Novartis Pharmaceuticals
Triazolyl tryptoline derivatives asß-secretase inhibitors.EBI
Mahidol University
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI
Pfizer
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.EBI
Elan Pharmaceuticals
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.EBI
Elan Pharmaceuticals
Fragment-based discovery and optimization of BACE1 inhibitors.EBI
Evotec
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.EBI
Merck Research Laboratories
Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents.EBI
Wayne State University
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.EBI
Wyeth Research
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.EBI
University of Montreal
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
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.EBI
Link£Ping University
Design and synthesis of potent and selective BACE-1 inhibitors.EBI
Stockholm University
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
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.EBI
Novartis Institutes For Biomedical Research
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.EBI
Wyeth Research
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
alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases.EBI
Uppsala University
The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.EBI
Nagasaki International University
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.EBI
Uppsala University
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.EBI
Novartis Institutes For Biomedical Research
 
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteresEBI
TBA
 
Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosetsEBI
TBA
 
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV proteaseEBI
TBA
 
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin DEBI
TBA
 
Novel pseudosymmetric inhibitors of HIV-1 proteaseEBI
TBA
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
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.EBI
Purdue University
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.EBI
LinköPing University
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.EBI
Schering-Plough Research Institute
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1.EBI
Ambrilia Biopharma
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.EBI
Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.EBI
Wyeth Research
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI
Merck Research Laboratories
Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent EBI
Latvian Institute of Organic Synthesis
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.EBI
Pfizer
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).EBI
Technische UniversitäT MüNchen
Discovery of quinazolin-4-one-based non-covalent inhibitors targeting the severe acute respiratory syndrome coronavirus 2 main protease (SARS-CoV-2 MEBI
China Pharmaceutical University
Structure-guided design of direct-acting antivirals that exploit the gem-dimethyl effect and potently inhibit 3CL proteases of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2) and middle east respiratory syndrome coronavirus (MERS-CoV).EBI
Wichita State University
Design of potent inhibitors of human beta-secretase. Part 1.EBI
Pfizer
Discovery of S-217622, a Noncovalent Oral SARS-CoV-2 3CL Protease Inhibitor Clinical Candidate for Treating COVID-19.EBI
Shionogi
Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability.EBI
Fudan University
Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.EBI
Uppsala University
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.EBI
Merck
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
Small molecules targeting γ-secretase and their potential biological applications.EBI
Shenyang Pharmaceutical University
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.EBI
Kalvista Pharmaceuticals
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of EBI
Ucb
Synthesis of the Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor NB-360.EBI
TBA
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious β-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.EBI
Novartis Pharma
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid β In Vivo.EBI
Janssen Research & Development
Re-emerging Aspartic Protease Targets: Examining EBI
Institute of Organic Chemistry and Biochemistry of The Czech Academy of Sciences
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.EBI
Lilly Research Laboratories
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.EBI
Janssen Research & Development
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.EBI
Galapagos
Rational design and synthesis of selective BACE-1 inhibitors.EBI
Merck Research Laboratories
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based β-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.EBI
Janssen Research & Development
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.EBI
Amgen
Identification and structure-activity relationship studies of small molecule inhibitors of the human cathepsin D.EBI
Aten Porus Lifesciences
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.EBI
Pfizer
Molecular dynamics and free energy analyses of cathepsin D-inhibitor interactions: insight into structure-based ligand design.EBI
University of California
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.EBI
Novartis Institutes For Biomedical Research
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.EBI
Eli Lilly
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.EBI
Roche Pharma Research and Early Development
Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II.EBI
University of California
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.EBI
Pharmacopeia
Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).EBI
University of Zambia
Exploiting Structural Dynamics To Design Open-Flap Inhibitors of Malarial Aspartic Proteases.EBI
Latvian Institute of Organic Synthesis
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.EBI
TBA
New evolutions in the BACE1 inhibitor field from 2014 to 2018.EBI
Janssen Research & Development
Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D.EBI
Latvian Institute of Organic Synthesis
Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis.EBI
Czech Academy of Sciences
Renin inhibitors containing a pyridyl amino diol derived C-terminus.EBI
Hoechst
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
SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.EBI
Harvard University
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.EBI
TBA
2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.EBI
Latvian Institute of Organic Synthesis
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.EBI
Abbott Laboratories
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.EBI
Abbott Laboratories
Synthesis and biological activity of some transition-state inhibitors of human renin.EBI
Ciba-Geigy
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
Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.EBI
TBA
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.EBI
Pfizer
Izenamides A and B, Statine-Containing Depsipeptides, and an Analogue from a Marine Cyanobacterium.EBI
Keio University
Grassystatins D-F, Potent Aspartic Protease Inhibitors from Marine Cyanobacteria as Potential Antimetastatic Agents Targeting Invasive Breast Cancer.EBI
University of Florida
New inhibitors of human renin that contain novel replacements at the P2 site.EBI
Warner-Lambert
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.EBI
The Scripps Research Institute
Renin inhibitory pentols showing improved enteral bioavailability.EBI
Hoechst
Renin inhibitors containing alpha-heteroatom amino acids as P2 residues.EBI
Warner-Lambert
Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts.EBI
Merck
Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'.EBI
E. Merck Darmstadt
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.EBI
Purdue University
IRAK4 PROTACSBDB
Astrazeneca
Phenothiazine derivatives and uses thereofBDB
Camp4 Therapeutics
Pyridazinones as PARP7 inhibitorsBDB
Ribon Therapeutics
Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic diseaseBDB
Shy Therapeutics
KDM1A inhibitors for the treatment of diseaseBDB
Imago Biosciences
Phenylate derivative, preparation method therefor, and pharmaceutical composition and uses thereofBDB
Institute of Materia Medica, Chinese Academy of Medical Sciences
Substituted pyrrolizine compounds and uses thereofBDB
Gilead Sciences
Inhibiting agents for Bruton's tyrosine kinaseBDB
Biogen Ma
Factor IXa inhibitorsBDB
Merck Sharp & Dohme
Substituted pyridines as inhibitors of human immunodeficiency virus replicationBDB
Viiv Healthcare UK (NO.5)
N-substituted pyrazolo [3,4-D] pyrimidine ketone compound, and preparation process and use thereofBDB
Sun Yat-Sen University
Rho kinase inhibitors and methods of useBDB
H. Lee Moffitt Cancer Center and Research Institute
Inhibitors of lysine specific demethylase-1BDB
Celgene Quanticel Research
Substituted benzene compoundsBDB
Epizyme
Inhibitors of lysine specific demethylase-1BDB
Celgene Quanticel Research
Substituted piperazine compounds and methods of use thereofBDB
Sunshine Lake Pharma
Heterocyclic compounds and methods of their useBDB
Novartis
Quinazoline derivatives as kinases inhibitors and methods of use thereofBDB
Teligene
Synthesis and preliminary biological assay of uridine glycoconjugate derivatives containing amide and/or 1,2,3-triazole linkers.BDB
Silesian University of Technology
Key mutations alter the cytochrome P450 BM3 conformational landscape and remove inherent substrate bias.BDB
University of Manchester
Serine/threonine kinase inhibitorsBDB
Array Biopharma
Heterocyclic derivative and pharmaceutical composition comprising the sameBDB
Shionogi
Triazolopyridine compoundsBDB
Novartis
Synthesis of Novel Hybrids Inspired from Bromopyrrole Alkaloids Inhibiting MMP-2 and -12 as Antineoplastic Agents.BDB
University of Kwazulu-Nata
Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitorsBDB
Merck Sharp & Dohme
Hybrid cholinesterase inhibitorsBDB
Uniwersytet Warszawski
Galactoside inhibitors of galectinsBDB
Galecto Biotech
Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivativesBDB
Pfizer
2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating painBDB
Purde Pharma
3-substituted-2-(arlyalkyl)-1-azabicycloalkanes and methods of use thereofBDB
Targacept
Interactive binding between the substrate and allosteric sites of carbamoyl-phosphate synthetase.BDB
Pennsylvania State University
Indolequinone inhibitors of NRH:quinone oxidoreductase 2. Characterization of the mechanism of inhibition in both cell-free and cellular systems.BDB
University of Colorado Denver
Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro.BDB
Eli Lilly
Discovery of novel heterocyclic factor VIIa inhibitors.BDB
Celera
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.BDB
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones.BDB
Ohio State University
1,7-annulated indolocarbazoles as cyclin-dependent kinase inhibitors.BDB
Eli Lilly
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.BDB
Bristol-Myers Squibb
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.BDB
Glaxosmithkline
Cyclic HIV-1 protease inhibitors derived from mannitol: synthesis, inhibitory potencies, and computational predictions of binding affinities.BDB
Uppsala University
Stereospecific synthesis, structure-activity relationship, and oral bioavailability of tetrahydropyrimidin-2-one HIV protease inhibitors.BDB
Dupont Pharmaceuticals