261 articles for thisTarget
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Thiazolidinones as cellular anandamide uptake inhibitors and their use in the treatment of psychiatric or neurological disorders and inflammation, in particular neuroinflammation
Universitat Bern
1H-pyrrolo[2,3,c]pyridin-7(6H)-ones and pyrazolo[3,4-c]pyridin-7(6H)-ones as inhibitors of BET proteins
Incyte
N-(2-cyano heterocyclyl) pyrazolo pyridones as janus kinase inhibitors
Merck Sharp & Dohme
3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
St. Chuan University
Inhibitor of FLT3 kinase and use thereof
Hefei Institutes of Physical Science, Chinese Academy of Sciences
Carboxy substituted (hetero) aromatic ring derivatives and preparation method and uses thereof
Sunshine Lake Pharma
Condensed-ring pyrimidylamino derivative, preparation method therefor, and intermediate, pharmaceutical composition and applications thereof
Guangzhou Maxinovel Pharmaceuticals
Pyridone derivatives as rearranged during transfection (RET) kinase inhibitors
Glaxosmithkline
Bicyclic heterocyclic derivatives as MNK1 and MNK2 modulators and uses thereof
Agency For Science, Technology and Research
Apoptosis signal-regulating kinase 1 inhibitors and methods of use thereof
Enanta Pharmaceuticals
Derivatives of 2-aminopyridine as adenosine A2B receptor antagonists and ligands of the melatonin MT3 receptors
Palobiofarma
N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators
Novartis
Benzenesulfonamide compounds and their use as therapeutic agents
Xenon Pharmaceuticals
1,2-dithiolane and dithiol compounds useful in treating mutant EGFR-mediated diseases and conditions
Sabila Biosciences
Polysubstituted pyridine compound, preparation method, use and pharmaceutical composition
Peking University Founder Group
N-pyrrolidinyl,N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
Array Biopharma
Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
Amgen
Methods for treating pulmonary emphysema using substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
Boehringer Ingelheim International
Substituted pyrido[3,4-d]pyrimidines and pyrido[4,3-d]pyrimidines as p70S6K inhibitors
Merck Patent
Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use therof
Pfizer
Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
Vanderbilt University
Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors
Bristol-Myers Squibb
Benzoxazolone derivatives as acid ceramidase inhibitors, and their use as medicaments
University of California
Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation
Bristol-Myers Squibb
SHP2 inhibitors and methods of treating autoimmune and/or glomerulonephritis-associated diseases using SHP2 inhibitors
Indiana University Research and Technology
N-acyl-(3-substituted)-(8-methyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a] pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders
Oged
Substituted oxopyridine derivatives and use thereof in the treatment of cardiovascular disorders
Bayer Pharma Aktiengesellschaft
Tetrahydronaphthyridine, benzoxazine, aza-benzoxazine and related bicyclic compounds for inhibition of RORgamma activity and the treatment of disease
Lycera
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
Zhejiang Hisun Pharmaceutical
Amantadine nitrate compounds with neural protective effect, and preparation and medical use thereof
TBA
Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
Hoffmann-La Roche
Tetrahydropyridopyrimidines and tetrahydropyridopyridines for the treatment and prophylaxis of hepatitis B virus infection
Hoffmann-La Roche
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) ureas as P38 MAP knase inhibitors
Respivert
Phosphonate compounds for treatment of complement mediated disorders
Achillion Pharmaceuticals
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors
Leo Pharma
Hexosaminidase inhibitors as new drug candidates for the therapy of osteoarthritis.
The Scripps Research Institute
Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase.
Northwestern University
Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.
Intervet Innovation
Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor.
Astrazeneca
Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold.
Genentech
Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger).
Johnson & Johnson Pharmaceutical
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor acti
Bristol-Myers Squibb
Extra Binding Region Induced by Non-Zinc Chelating Inhibitors into the S(1)' Subsite of Matrix Metalloproteinase 8 (MMP-8) (dagger).
Universita Degli Studi
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.
Gsk
Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Gsk
Tricyclic HIV integrase inhibitors: VI. SAR studies of 'benzyl flipped' C3-substituted pyrroloquinolines.
Gilead Sciences
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.
Gsk
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling.
Fujisawa Pharmaceutical
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.
Deltagen Research Laboratories
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Johnson & Johnson Pharmaceutical
Synthesis and pharmacological evaluation of novel gamma-aminobutyric acid type B (GABAB) receptor agonists as gastroesophageal reflux inhibitors.
Astrazeneca
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.
Kalypsys
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Wyeth Research
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).
Wyeth Research
Synthesis and structure activity relationships of novel non-peptidic metallo-aminopeptidase inhibitors.
Enscmu
Structure-based design, synthesis, and study of potent inhibitors of beta-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents.
Quorex Pharmaceuticals
Amphipathic benzoic acid derivatives: synthesis and binding in the hydrophobic tunnel of the zinc deacetylase LpxC.
University of San Francisco
Identification of novel chemical inhibitors for ubiquitin C-terminal hydrolase-L3 by virtual screening.
Waseda University
Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase.
Nestle Research Center
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.
Gilead Sciences
Design, synthesis, and biological activity of novel polycyclic aza-amide FKBP12 ligands.
Pfizer
Synthesis of ketone analogues of prolyl and pipecolyl ester FKBP12 ligands.
Guilford Pharmaceuticals
Binding mode of new (thio)hydantoin inhibitors of fatty acid amide hydrolase: comparison with two original compounds, OL-92 and JP104.
Fundp
Structure-based virtual screening against SARS-3CL(pro) to identify novel non-peptidic hits.
University of Mississippi
A refined pharmacophore identifies potent 4-amino-7-chloroquinoline-based inhibitors of the botulinum neurotoxin serotype A metalloprotease.
National Cancer Institute At Frederick
Synthesis and structure-activity relationships of second-generation hydroxamate botulinum neurotoxin A protease inhibitors.
The Scripps Research Institute
Identification of a potent botulinum neurotoxin a protease inhibitor using in situ lead identification chemistry.
The Scripps Research Institute
An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists.
The Scripps Research Institute
Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity.
University of Bristol
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.
University of Mississippi
Substrate specificity analysis and inhibitor design of homoisocitrate dehydrogenase.
Tokyo Institute of Technology
Thiahomoisocitrate: a highly potent inhibitor of homoisocitrate dehydrogenase involved in the alpha-aminoadipate pathway.
Tokyo Institute of Technology
Naturally Occurring Pentacyclic Triterpenes as Inhibitors of Glycogen Phosphorylase: Synthesis, Structure-Activity Relationships, and X-ray Crystallographic Studies.
China Pharmaceutical University
Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate.
Mitsubishi Pharma
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.
University of Cape Town
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
NAD+-dependent DNA ligase (Rv3014c) from Mycobacterium tuberculosis: novel structure-function relationship and identification of a specific inhibitor.
India Central Drug Research Institute
NAD+-dependent DNA Ligase (Rv3014c) from Mycobacterium tuberculosis. Crystal structure of the adenylation domain and identification of novel inhibitors.
India Central Drug Research Institute
Structure-based design and synthesis of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors.
Fujisawa Pharmaceutical
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
Fujisawa Pharmaceutical
Structure-based de novo design of non-nucleoside adenosine deaminase inhibitors.
Fujisawa Pharmaceutical
Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.
Vrije Universiteit Amsterdam
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
Irbm-Mrl
Structural basis of enantioselective inhibition of cyclooxygenase-1 by S-alpha-substituted indomethacin ethanolamides.
Michigan State University
2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice.
Biovitrum
Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.
University of Notre Dame
Identification and structure-activity relationship of phenolic acyl hydrazones as selective agonists for the estrogen-related orphan nuclear receptors ERRbeta and ERRgamma.
Gsk
Structure-guided synthesis of tamoxifen analogs with improved selectivity for the orphan ERRgamma.
Gsk
Crystal structure of human estrogen-related receptor alpha in complex with a synthetic inverse agonist reveals its novel molecular mechanism.
Novartis
Synthesis and structure-activity relationship studies of 1,3-diarylprop-2-yn-1-ones: dual inhibitors of cyclooxygenases and lipoxygenases.
University of Alberta
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.
Bristol-Myers Squibb
SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.
Merck Research Laboratories
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3.
Merck Research Laboratories
Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.
University of California San Francisco
Targeting plague virulence factors: a combined machine learning method and multiple conformational virtual screening for the discovery of Yersinia protein kinase A inhibitors.
Rockefeller University
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
Universita Di Pisa
Structural basis for dipeptide amide isoform-selective inhibition of neuronal nitric oxide synthase.
University of California Irvine
Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds.
Astrazeneca
Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.
Bayer Healthcare Pharmaceuticals
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors.
Millennium Pharmaceuticals
Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity.
Abbott Laboratories
Synthesis, Cannabinoid Receptor Affinity, and Molecular Modeling Studies of Substituted 1-Aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.
Sapienza University of Rome
Derivatives of 4-Amino-6-hydroxy-2-mercaptopyrimidine as Novel, Potent, and Selective A3 Adenosine Receptor Antagonists.
Universita Di Napoli
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.
Neuroscience
Synthesis of Stable and Potent delta/mu Opioid Peptides: Analogues of H-Tyr-c[d-Cys-Gly-Phe-d-Cys]-OH by Ring-Closing Metathesis.
Universita Degli Studi
A Structure-Activity Relationship Study and Combinatorial Synthetic Approach of C-Terminal Modified Bifunctional Peptides That Are delta/mu Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists.
University of Arizona Tucson
Exploring inhibitor binding at the s' subsites of cathepsin L.
National Research Council Canada
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
Bristol-Myers Squibb
2-Aryloxy-4-alkylaminopyridines: Discovery of Novel Corticotropin-Releasing Factor 1 Antagonists.
Pfizer
Synthesis and SAR of 2-Aryloxy-4-alkoxy-pyridines as Potent Orally Active Corticotropin-Releasing Factor 1 Receptor Antagonists.
Pfizer
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Amgen
Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
Biogen Idec
7'-substituted benzothiazolothio- and pyridinothiazolothio-purines as potent heat shock protein 90 inhibitors.
Conforma Therapeutics
Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.
Novartis Pharmaceuticals
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Abbott Laboratories
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Seoul National University
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues.
Seoul National University
Selective chemical probe inhibitor of Stat3, identified through structure-based virtual screening, induces antitumor activity.
University of Central Florida College of Medicine
An oxazole-based small-molecule Stat3 inhibitor modulates Stat3 stability and processing and induces antitumor cell effects.
University of Central Florida College of Medicine
Isoform selective inhibition of STAT1 or STAT3 homo-dimerization via peptidomimetic probes: structural recognition of STAT SH2 domains.
Yale University
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.
University of Michigan
Investigation of the binding determinants of phosphopeptides targeted to the SRC homology 2 domain of the signal transducer and activator of transcription 3. Development of a high-affinity peptide inhibitor.
The University of Texas At Houston
Discovery of substituted maleimides as liver X receptor agonists and determination of a ligand-bound crystal structure.
Glaxosmithkline
Biochemical and biophysical characterization of inhibitor binding to caspase-3 reveals induced asymmetry.
Wyeth Research
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Gnf
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
Gnf
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
Gnf
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin.
University of California Davis
Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa.
Bristol-Myers Squibb
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Bristol-Myers Squibb
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.
Karo Bio
Chiral nonsteroidal affinity ligands for the androgen receptor. 1. Bicalutamide analogues bearing electrophilic groups in the B aromatic ring.
University of Tennessee At Memphis
Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.
University of Tennessee At Memphis
Novel 2,7-Dialkyl-Substituted 5(S)-Amino-4(S)-hydroxy-8-phenyl-octanecarboxamide Transition State Peptidomimetics Are Potent and Orally Active Inhibitors of Human Renin.
Novartis Pharmaceuticals
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with omega-carboxyalkoxy or omega-carboxy-1-alkynyl substitution in the side chain.
Harvard Medical School
Influence of side-chain structure of aliphatic amino acids on binding to isoleucyl-tRNA synthetase from Escherichia coli MRE 600.
Gesellschaft Fur Molekularbiolische Forschung Mbh
Thermodynamic characterization of the binding of nucleotides to glycyl-tRNA synthetase.
Medical College of Ohio
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists.
Daiichi Pharmaceutical
Discovery of the HCV NS3/4A protease inhibitor (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) II. Key steps in structure-based optimization.
Schering-Plough Research Institute
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.
Morphochem
Serendipitous discovery of novel bacterial methionine aminopeptidase inhibitors.
The Procter & Gamble Pharmaceuticals
Elucidation of the function of type 1 human methionine aminopeptidase during cell cycle progression.
Johns Hopkins University
Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.
Berlex Biosciences
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Bristol-Myers Squibb Pharmaceutical Research Institute
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
National Health Research Institutes
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
Istituto Di Cristallografia
Crystal structures of multidrug binding protein TtgR in complex with antibiotics and plant antimicrobials.
Imperial College
Effector-repressor interactions, binding of a single effector molecule to the operator-bound TtgR homodimer mediates derepression.
Estacion Experimental Del Zaidin