189 articles for thisTarget
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Adamantyl Antiestrogens with Novel Side Chains Reveal a Spectrum of Activities in Suppressing Estrogen Receptor Mediated Activities in Breast Cancer Cells.
The Scripps Research Institute
Synthesis of novel steroidal agonists, partial agonists, and antagonists for the glucocorticoid receptor.
The Scripps Research Institute
Discovery and Structure-Activity Relationships of the Neoseptins: A New Class of Toll-like Receptor-4 (TLR4) Agonists.
The Scripps Research Institute
Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.
The Scripps Research Institute
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
Synthesis and structure-activity relationships of pteridine dione and trione monocarboxylate transporter 1 inhibitors.
The Scripps Research Institute
Discovery libraries targeting the major enzyme classes: the serine hydrolases.
The Scripps Research Institute
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1).
The Scripps Research Institute
Benzoquinones as inhibitors of botulinum neurotoxin serotype A.
The Scripps Research Institute
Dual protonophore-chitinase inhibitors dramatically affect O. volvulus molting.
The Scripps Research Institute
a-Ketoheterocycle inhibitors of fatty acid amide hydrolase: exploration of conformational constraints in the acyl side chain.
The Scripps Research Institute
Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of a/ß-hydrolase domain containing 6 (ABHD6).
The Scripps Research Institute
Design, synthesis, and characterization ofa-ketoheterocycles that additionally target the cytosolic port Cys269 of fatty acid amide hydrolase.
The Scripps Research Institute
Identification of clinically viable quinolinol inhibitors of botulinum neurotoxin A light chain.
The Scripps Research Institute
Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.
The Scripps Research Institute
Synthesis and activity of substituted heteroaromatics as positive allosteric modulators fora4ß2a5 nicotinic acetylcholine receptors.
The Scripps Research Institute
Synthesis/biological evaluation of hydroxamic acids and their prodrugs as inhibitors for Botulinum neurotoxin A light chain.
The Scripps Research Institute
Targeting botulinum A cellular toxicity: a prodrug approach.
The Scripps Research Institute
Efforts toward broadening the spectrum of arylomycin antibiotic activity.
The Scripps Research Institute
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
The Scripps Research Institute
Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.
The Scripps Research Institute
Evaluation of adamantane hydroxamates as botulinum neurotoxin inhibitors: synthesis, crystallography, modeling, kinetic and cellular based studies.
The Scripps Research Institute
The C-terminus of Botulinum A Protease Has Profound and Unanticipated Kinetic Consequences Upon the Catalytic Cleft.
The Scripps Research Institute
SAR analysis of novel non-peptidic NPBWR1 (GPR7) antagonists.
The Scripps Research Institute
Small molecule amides as potent ROR-¿ selective modulators.
The Scripps Research Institute
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7).
The Scripps Research Institute
Discovery and optimization of sulfonyl acrylonitriles as selective, covalent inhibitors of protein phosphatase methylesterase-1.
The Scripps Research Institute
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erba.
The Scripps Research Institute
Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists.
The Scripps Research Institute
Synthesis and SAR of tetrahydroisoquinolines as Rev-erba agonists.
The Scripps Research Institute
Discovery of potent and selective histone deacetylase inhibitors via focused combinatorial libraries of cyclic alpha3beta-tetrapeptides.
The Scripps Research Institute
Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling.
The Scripps Research Institute
Noxious compounds activate TRPA1 ion channels through covalent modification of cysteines.
The Scripps Research Institute
Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs.
The Scripps Research Institute
Small-molecule synergist of the Wnt/beta-catenin signaling pathway.
The Scripps Research Institute
Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.
The Scripps Research Institute
Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.
The Scripps Research Institute
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
The Scripps Research Institute
High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays.
The Scripps Research Institute
Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.
The Scripps Research Institute
Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonists.
The Scripps Research Institute
Formulating a new basis for the treatment against botulinum neurotoxin intoxication: 3,4-Diaminopyridine prodrug design and characterization.
The Scripps Research Institute
Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-II).
The Scripps Research Institute
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.
The Scripps Research Institute
Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors.
The Scripps Research Institute
Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I).
The Scripps Research Institute
Discovery, synthesis and SAR analysis of novel selective small molecule S1P4-R agonists based on a (2Z,5Z)-5-((pyrrol-3-yl)methylene)-3-alkyl-2-(alkylimino)thiazolidin-4-one chemotype.
The Scripps Research Institute
The development of N-a-(2-carboxyl)benzoyl-N(5)-(2-fluoro-1-iminoethyl)-l-ornithine amide (o-F-amidine) and N-a-(2-carboxyl)benzoyl-N(5)-(2-chloro-1-iminoethyl)-l-ornithine amide (o-Cl-amidine) as second generation protein arginine deiminase (PAD) inhibitors.
The Scripps Research Institute
High affinity sialoside ligands of myelin associated glycoprotein.
The Scripps Research Institute
SAR analysis of innovative selective small molecule antagonists of sphingosine-1-phosphate 4 (S1P4) receptor.
The Scripps Research Institute
Medicinal chemistry as a conduit for the modulation of quorum sensing.
The Scripps Research Institute
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
The Scripps Research Institute
Discovery, design and synthesis of the first reported potent and selective sphingosine-1-phosphate 4 (S1P4) receptor antagonists.
The Scripps Research Institute
Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.
The Scripps Research Institute
Reversible competitivea-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics.
The Scripps Research Institute
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Synthesis and evaluation of library of betulin derivatives against the botulinum neurotoxin A protease.
The Scripps Research Institute
Reduced histone deacetylase 7 activity restores function to misfolded CFTR in cystic fibrosis.
The Scripps Research Institute
Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects.
The Scripps Research Institute
Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo.
The Scripps Research Institute
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
The Scripps Research Institute
Chemoselective small molecules that covalently modify one lysine in a non-enzyme protein in plasma.
The Scripps Research Institute
Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9).
The Scripps Research Institute
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
The Scripps Research Institute
Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists.
The Scripps Research Institute
Benzylidene cyclopentenediones: First irreversible inhibitors against botulinum neurotoxin A's zinc endopeptidase.
The Scripps Research Institute
X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.
The Scripps Research Institute
Design and synthesis of novel hybrid benzamide-peptide histone deacetylase inhibitors.
The Scripps Research Institute
Toward optimization of the second aryl substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.
The Scripps Research Institute
Toward optimization of the linker substructure common to transthyretin amyloidogenesis inhibitors using biochemical and structural studies.
The Scripps Research Institute
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
The Scripps Research Institute
Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase.
The Scripps Research Institute
Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
The Scripps Research Institute
Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition.
The Scripps Research Institute
Reversine increases the plasticity of lineage-committed mammalian cells.
The Scripps Research Institute
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors.
The Scripps Research Institute
"Magic Chloro": Profound Effects of the Chlorine Atom in Drug Discovery.
The Scripps Research Institute
Consensus screening for a challenging target: the quest for P-glycoprotein inhibitors.
The Scripps Research Institute
Structure-Activity Relationship and Biological Investigation of a REV-ERBα-Selective Agonist SR-29065 (
The Scripps Research Institute
Dose-Response Activity-Based DNA-Encoded Library Screening.
The Scripps Research Institute
Structure-activity relationships, and drug metabolism and pharmacokinetic properties for indazole piperazine and indazole piperidine inhibitors of ROCK-II.
The Scripps Research Institute
Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ.
The Scripps Research Institute
Rapid discovery and structure-activity profiling of novel inhibitors of human immunodeficiency virus type 1 protease enabled by the copper(I)-catalyzed synthesis of 1,2,3-triazoles and their further functionalization.
The Scripps Research Institute
A review of salvinorin analogs and their kappa-opioid receptor activity.
The Scripps Research Institute
Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response.
The Scripps Research Institute
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization.
The Scripps Research Institute
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
The Scripps Research Institute
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
The Scripps Research Institute
Virtual screening of human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase against the NCI diversity set by use of AutoDock to identify novel nonfolate inhibitors.
The Scripps Research Institute
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.
The Scripps Research Institute
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists.
The Scripps Research Institute
Identification of Slow-Binding Inhibitors of the BoNT/A Protease.
The Scripps Research Institute
Assessment of NR4A Ligands That Directly Bind and Modulate the Orphan Nuclear Receptor Nurr1.
The Scripps Research Institute
Discovery of Potent Coumarin-Based Kinetic Stabilizers of Amyloidogenic Immunoglobulin Light Chains Using Structure-Based Design.
The Scripps Research Institute
Modulators of immunoregulatory exonucleases PLD3 and PLD4 identified by high-throughput screen.
The Scripps Research Institute
Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group.
The Scripps Research Institute
Irreversible inhibition of BoNT/A protease: proximity-driven reactivity contingent upon a bifunctional approach.
The Scripps Research Institute
Structure-Activity Relationship and Biological Investigation of SR18292 (
The Scripps Research Institute
Engineering of a Potent, Long-Acting NPY2R Agonist for Combination with a GLP-1R Agonist as a Multi-Hormonal Treatment for Obesity.
The Scripps Research Institute
alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution.
The Scripps Research Institute
Design, synthesis, and biological evaluation of HIV/FIV protease inhibitors incorporating a conformationally constrained macrocycle with a small P3' residue.
The Scripps Research Institute
Modifications of a Nanomolar Cyclic Peptide Antagonist for the EphA4 Receptor To Achieve High Plasma Stability.
The Scripps Research Institute
Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.
The Scripps Research Institute
Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140).
The Scripps Research Institute
Structural Basis of Altered Potency and Efficacy Displayed by a Major in Vivo Metabolite of the Antidiabetic PPARγ Drug Pioglitazone.
The Scripps Research Institute
Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12).
The Scripps Research Institute
N-Acyl pyrazoles: Effective and tunable inhibitors of serine hydrolases.
The Scripps Research Institute
Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.
The Scripps Research Institute
Exploiting the Polypharmacology of ß-Carbolines to Disrupt O. volvulus Molting.
The Scripps Research Institute
Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.
The Scripps Research Institute
Discovery, design and synthesis of a selective S1P(3) receptor allosteric agonist.
The Scripps Research Institute
3-Hydroxy-1-alkyl-2-methylpyridine-4(1H)-thiones: Inhibition of the Pseudomonas aeruginosa Virulence Factor LasB.
The Scripps Research Institute
Histone deacetylase inhibitors reverse gene silencing in Friedreich's ataxia.
The Scripps Research Institute
Synthesis and biological evaluation of penem inhibitors of bacterial signal peptidase.
The Scripps Research Institute
A copper(I)-catalyzed 1,2,3-triazole azide-alkyne click compound is a potent inhibitor of a multidrug-resistant HIV-1 protease variant.
The Scripps Research Institute
Identification of potent RORβ modulators: Scaffold variation.
The Scripps Research Institute
Synthetic molecules for disruption of the MYC protein-protein interface.
The Scripps Research Institute
Covalent inhibitors of nicotinamide N-methyltransferase (NNMT) provide evidence for target engagement challenges in situ.
The Scripps Research Institute
O6C-20-nor-salvinorin A is a stable and potent KOR agonist.
The Scripps Research Institute
Identification of an aminothiazole series of RORβ modulators.
The Scripps Research Institute
Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.
The Scripps Research Institute
Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.
The Scripps Research Institute
Selective Irreversible Inhibitors of the Wnt-Deacylating Enzyme NOTUM Developed by Activity-Based Protein Profiling.
The Scripps Research Institute
HTS and Structure Based Optimization of Indazole-Derived ULK1 Inhibitors.
The Scripps Research Institute
Cyclic tetrapeptide HDAC inhibitors as potential therapeutics for spinal muscular atrophy: Screening with iPSC-derived neuronal cells.
The Scripps Research Institute
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
The Scripps Research Institute
Newly Designed Quinolinol Inhibitors Mitigate the Effects of Botulinum Neurotoxin A in Enzymatic, Cell-Based, and ex Vivo Assays.
The Scripps Research Institute
Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor.
The Scripps Research Institute
Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPARγ-Targeted Antidiabetics.
The Scripps Research Institute
IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
Dana-Farber Cancer Institute
QUINAZOLINONES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USING THE SAME
Repare Therapeutics
Hypoxia inducible factor-2(alpha) inhibitors and their use in the treatment of diseases
Nikang Therapeutics
Benzofuran derivative, preparation method thereof and use thereof in medicine
Jiangsu Hengrui Medicine
Substituted bicycle heterocyclic derivatives useful as ROMK channel inhibitors
Bristol-Myers Squibb
Imidazole derivative having JNK inhibitory activity and use thereof
Samjin Pharmaceutical
Antitumor compound targeting IDH2 mutation and method of use thereof
Chia Tai Tianqing Pharmaceutical Group
Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity
Boehringer Ingelheim International
Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors
Chong Kun Dang Pharmaceutical
Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators
Purdue Pharma
The pharmacological profile of (R)-3,4-dihydro-N-isopropyl-3-(N-isopropyl-N-propylamino)-2H-1-benzopyran-5-carboxamide, a selective 5-hydroxytryptamine(1A) receptor agonist.
Astrazeneca R&D
[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
Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies.
Gliatech
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
Wyeth Research
Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.
Abbott Laboratories
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.
Vertex Pharmaceuticals
Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors.
Glaxosmithkline
Specificity and affinity of natural product cyclopentapeptide inhibitors against A. fumigatus, human, and bacterial chitinases.
University of Dundee
1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.
Chemical Diversity Research Institute
Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.
Chemical Diversity Research Institute
Development and evaluation of a pharmacophore model for inhibitors of aldosterone synthase (CYP11B2).
Saarland University
Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.
Glaxosmithkline