The first public molecular recognition database, BindingDB supports research, education and practice in drug discovery, pharmacology and related fields.

BindingDB contains 2.8M data for 1.2M Compounds and 9.2K Targets. Of those, 1,346K data for 622K Compounds and 4.5K Targets were curated by BindingDB curators. BindingDB is a FAIRsharing resource.

If BindingDB was of value to your research, please take a moment to donate to this nonprofit project. Your donation will let us provide you with more data and improved service.

Advanced Search

182 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
Novel approach of fragment-based lead discovery applied to renin inhibitors.EBI
Takeda Pharmaceutical
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.EBI
Takeda Pharmaceutical
Discovery of highly potent renin inhibitors potentially interacting with the S3' subsite of renin.EBI
China Pharmaceutical University
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
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
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
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
Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.EBI
Daiichi Sankyo
Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.EBI
Daiichi Sankyo
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.EBI
F. Hoffmann-La Roche
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
Renin inhibitors. Free-Wilson and correlation analysis of the inhibitory potency of a series of pepstatin analogues on plasma renin.EBI
Sanofi Recherche
An integrated computational workflow for efficient and quantitative modeling of renin inhibitors.EBI
Sanofi Us
 
Retro-Inverso Tripeptide Renin InhibitorsEBI
TBA
Design and discovery of new (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides as potent renin inhibitors.EBI
Daiichi Sankyo
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI
Universite£
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.EBI
TBA
Dual inhibitors for aspartic proteases HIV-1 PR and renin: advancements in AIDS-hypertension-diabetes linkage via molecular dynamics, inhibition assays, and binding free energy calculations.EBI
National Hellenic Research Foundation
Design and optimization of novel (2S,4S,5S)-5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxy-2-isopropylhexanamides as renin inhibitors.EBI
Daiichi Sankyo
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.EBI
TBA
Design and synthesis of potent, isoxazole-containing renin inhibitors.EBI
Merck Frosst Centre For Therapeutic Research
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI
University Of Florida
Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors.EBI
Actelion Pharmaceuticals
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
Excursions in drug discovery.EBI
Merck Research Laboratories
Highly potent, orally active diester macrocyclic human renin inhibitors.EBI
Merck Research Laboratories
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
Determination of dissociation constants of high affinity (pM) human renin inhibitors: application to analogues of ditekiren (U-71,038).EBI
Upjohn Laboratories
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
Novel inhibitors of human renin. Cyclic peptides based on the tetrapeptide sequence Glu-D-Phe-Lys-D-Trp.EBI
Ici Pharmaceuticals Group
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.EBI
Abbott Laboratories
Renin inhibitory peptides. A beta-aspartyl residue as a replacement for the histidyl residue at the P-2 site.EBI
Upjohn
Orally potent human renin inhibitors derived from angiotensinogen transition state: design, synthesis, and mode of interaction.EBI
Kissei Pharmaceutical
Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.EBI
University Of Wisconsin-Madison
Azido glycols: potent, low molecular weight renin inhibitors containing an unusual post scissile site residue.EBI
Abbott Laboratories
Design of rat renin inhibitory peptides.EBI
Massachusetts General Hospital
Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, Leu psi [CH2S]Val, or Leu psi [CH2SO]Val at the P1-P1' cleavage site.EBI
Upjohn
Conformationally constrained renin inhibitory peptides: gamma-lactam-bridged dipeptide isostere as conformational restriction.EBI
Upjohn
Design, structure-activity, and molecular modeling studies of potent renin inhibitory peptides having N-terminal Nin-For-Trp (Ftr): angiotensinogen congeners modified by P1-P1' Phe-Phe, Sta, Leu psi[CH(OH)CH2]Val or leu psi[CH2NH]Val substitutions.EBI
Upjohn
Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.EBI
TBA
alpha-Methylproline-containing renin inhibitory peptides: in vivo evaluation in an anesthetized, ganglion-blocked, hog renin infused rat model.EBI
TBA
Optimization and in vivo evaluations of a series of small, potent, and specific renin inhibitors containing a novel Leu-Val replacement.EBI
Abbott Laboratories
Pepstatin analogues as novel renin inhibitors.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
Inhibition of renin by angiotensinogen peptide fragments containing the hydroxy amino acid residue 5-amino-3-hydroxy-7-methyloctanoic acid.EBI
TBA
Renin inhibitors. Substitution of the leucyl residues of Leu-Leu-Val-Phe-OCH3 with 3-amino-2-hydroxy-5-methylhexanoic acid.EBI
TBA
Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.EBI
TBA
 
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability propertiesEBI
TBA
3,4-Diarylpiperidines as potent renin inhibitors.EBI
Merck Frosst Center For Therapeutic Research
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.EBI
Merck Research Laboratories
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.EBI
Merck Frosst Centre For Therapeutic Research
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.EBI
Merck Frosst Centre For Therapeutic Research
Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors.EBI
Deutschland
Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds.EBI
Sanofi-Aventis Deutschland
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.EBI
Vitae Pharmaceuticals
Synthesis, biological evaluation and docking studies of octane-carboxamide based renin inhibitors with extended segments toward S3' site of renin.EBI
China Pharmaceutical University
Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of pyridone-substituted piperidines.EBI
Merck Frosst Centre For Therapeutic Research
Potential virtual lead identification in the discovery of renin inhibitors: application of ligand and structure-based pharmacophore modeling approaches.EBI
Gyeongsang National University (Gnu)
The discovery and synthesis of potent zwitterionic inhibitors of renin.EBI
Merck Frosst Centre For Therapeutic Research
Design and synthesis of potent macrocyclic renin inhibitors.EBI
Medivir
Direct renin inhibitors as a new therapy for hypertension.EBI
Novartis Pharmaceuticals
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI
Pfizer
Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors.EBI
Sanofi-Aventis Deutschland
Piperidine-based renin inhibitors: upper chain optimization.EBI
Actelion Pharmaceuticals
Design and optimization of new piperidines as renin inhibitors.EBI
Actelion Pharmaceuticals
Identification of a new biaryl scaffold generating potent renin inhibitors.EBI
Merck Frosst Center For Therapeutic Research
Addressing time-dependent CYP 3A4 inhibition observed in a novel series of substituted amino propanamide renin inhibitors, a case study.EBI
Merck Frosst Centre For Therapeutic Research
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.EBI
Merck Frosst Centre For Therapeutic Research
New classes of potent and bioavailable human renin inhibitors.EBI
Actelion Pharmaceuticals
Optimization of orally bioavailable alkyl amine renin inhibitors.EBI
Vitae Pharmaceuticals
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
Synthesis and evaluation of A-seco type triterpenoids for anti-HIV-1protease activity.EBI
University Of Toyama
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 novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides as in vitro potent peptidomimetic inhibitors of human reninEBI
TBA
 
Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosetsEBI
TBA
 
Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitorsEBI
TBA
 
Synthesis of α-hydroxy statine through a facially selective osmylation of a chiral α-amido crotonateEBI
TBA
 
Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 sidechainsEBI
TBA
 
CP-71,362, an unusually potent inhibitor of rat and dog reninEBI
TBA
 
Tetrahydroisoquinoline as a phenylalanine replacement in renin inhibitorsEBI
TBA
 
Preparation of a novel series of phosphonate norstatine renin inhibitorsEBI
TBA
 
Design and synthesis of a prototypical non-peptidic inhibitor model for the enzme reninEBI
TBA
 
The identification of a novel renin inhibitor of equivalent efficacy following oral or intravenous administration.EBI
TBA
 
Novel pseudosymmetric inhibitors of HIV-1 proteaseEBI
TBA
 
Diol sulfonamides: A potent and novel class of inhibitors of human reninEBI
TBA
 
Peptidomimetic inhibitors of renin incorporating topographically modified isosteres spanning the P1(→ P3)-P1' sitesEBI
TBA
 
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.EBI
TBA
 
Conformationally restricted peptide isosteres. 2.1 Synthesis and in vitro potency of dipeptide renin inhibitors employing a 2-alkylsulfonyl-3-phenylcyclopropane carboxamide as a P3 amino acid replacementEBI
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
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI
Merck Research Laboratories
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.EBI
Pfizer
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.EBI
Pfizer
Rational design and synthesis of selective BACE-1 inhibitors.EBI
Merck Research Laboratories
Piperidine-renin inhibitors compounds with improved physicochemical properties.EBI
F. Hoffmann-La Roche
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.EBI
F. Hoffmann-La Roche
Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-725EBI
Abbott Laboratories
Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides.EBI
Abbott Laboratories
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
Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors.EBI
Warner-Lambert
Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog.EBI
Abbott Laboratories
Time-resolved ligand exchange reactions: kinetic models for competitive inhibitors with recombinant human renin.EBI
Boehringer Ingelheim Pharmaceuticals
alpha-Hydroxy phosphinyl-based inhibitors of human renin.EBI
Bristol-Myers Squibb Pharmaceutical Research Institute
N-(alpha-Hydroxyalkanoyl) derivatives of Leu-Val-Phe-OCH3 as inhibitors of renin.EBI
TBA
Synthesis of analogues of the carboxyl protease inhibitor pepstatin. Effects of structure on inhibition of pepsin and renin.EBI
TBA
Inhibition of renin by substrate analogue inhibitors containing the olefinic amino acid 5(S)-amino-7-methyl-3(E)-octenoic acid.EBI
TBA
A uniquely potent renin inhibitor and its unanticipated plasma binding component.EBI
TBA
Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analogue inhibitor.EBI
TBA
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.EBI
Abbott Laboratories
Renin inhibitors. Statine-containing tetrapeptides with varied hydrophobic carboxy termini.EBI
Merck Sharp & Dohme Research Laboratories
alpha,alpha-Difluoro-beta-aminodeoxystatine-containing renin inhibitory peptides.EBI
Upjohn
Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond.EBI
Abbott Laboratories
Fluoro ketone containing peptides as inhibitors of human renin.EBI
TBA
New inhibitors of human renin that contain novel Leu-Val replacements.EBI
TBA
Analysis of structure-activity relationships in renin substrate analogue inhibitory peptides.EBI
TBA
Renin inhibitors. Design of angiotensinogen transition-state analogues containing novel. (2R,3R,4R,5S)-5-amino-3,4-dihydroxy-2-isopropyl-7-methyloctanoic acid.EBI
TBA
Renin inhibitors containing psi[CH2O] pseudopeptide inserts.EBI
Upjohn
New inhibitors of human renin that contain novel Leu-Val replacements. Examination of the P1 site.EBI
Abbott Laboratories
Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogues of angiotensinogen.EBI
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability.EBI
Abbott Laboratories
Renin inhibitors. Dipeptide analogues of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency.EBI
Abbott Laboratories
Synthesis and biological activity of some transition-state inhibitors of human renin.EBI
Ciba-Geigy
New human renin inhibitors containing an unnatural amino acid, norstatine.EBI
Kissei Pharmaceutical
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
Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency.EBI
Merck Sharp & Dohme Research Laboratories
Renin inhibitors. Synthesis of transition-state analogue inhibitors containing phosphorus acid derivatives at the scissile bond.EBI
Ciba-Geigy Pharmaceuticals Division
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites.EBI
Warner-Lambert
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.EBI
Abbott Laboratories
Inhibitors of human renin. Cyclic peptide analogues containing a D-Phe-Lys-D-Trp sequence.EBI
Ici Pharmaceuticals Group
Thermodynamics of the interaction of inhibitors with the binding site of recombinant human renin.EBI
Upjohn
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.EBI
Abbott Laboratories
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 2. Synthesis, biological properties and molecular modeling of hydroxyethylene isostere derivatives.EBI
Ici Pharmaceuticals Group
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 1. Synthesis and biological properties of alkyl alcohol and statine derivatives.EBI
Ici Pharmaceuticals Group
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.EBI
Abbott Laboratories
Renin inhibitory peptides. Incorporation of polar, hydrophilic end groups into an active renin inhibitory peptide template and their evaluation in a human renin infused rat model and in conscious sodium-depleted monkeys.EBI
Upjohn
Design of a well-absorbed renin inhibitor.EBI
Abbott Laboratories
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3.1 Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives.EBI
Ici Pharmaceuticals Group
New inhibitors of human renin that contain novel replacements at the P2 site.EBI
Warner-Lambert
Design and synthesis of P2-P1'-linked macrocyclic human renin inhibitors.EBI
Merck Sharp And Dohme Research Laboratories
Renin inhibitory pentols showing improved enteral bioavailability.EBI
Hoechst
Renin inhibitors containing C-termini derived from mercaptoheterocycles.EBI
Merck Sharp & Dohme Research Laboratories
C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.EBI
Abbott Laboratories
Nonpeptide renin inhibitors employing a novel 3-aza(or oxa)-2,4-dialkyl glutaric acid moiety as a P2/P3 amide bond replacement.EBI
Abbott Laboratories
1,2,3-trisubstituted cyclopropanes as conformationally restricted peptide isosteres: application to the design and synthesis of novel renin inhibitors.EBI
University Of Texas
Renin inhibitors containing alpha-heteroatom amino acids as P2 residues.EBI
Warner-Lambert
Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.EBI
Merck Sharp And Dohme Research Laboratories
New modified heterocyclic phenylalanine derivatives. Incorporation into potent inhibitors of human renin.EBI
Wyeth-Ayerst Research
Inhibitors of human renin with C-termini derived from amides and esters of alpha-mercaptoalkanoic acids.EBI
Merck Research Laboratories
Renin inhibitors containing new P1-P1' dipeptide mimetics with heterocycles in P1'.EBI
E. Merck Darmstadt
Structural determinants of Tau aggregation inhibitor potency.BDB
The Ohio State University
Kainate receptors are involved in synaptic plasticity.BDB
University Of Bristol
I. NGD 94-1: identification of a novel, high-affinity antagonist at the human dopamine D4 receptor.BDB
Neurogen
Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.BDB
Massachusetts Institute Of Technology