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104 articles for thisTarget


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

PMID
Data
Article Title
Organization
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.EBI
University of Pennsylvania
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.EBI
University of Pennsylvania
Synthesis and evaluation of N8-acetylspermidine analogues as inhibitors of bacterial acetylpolyamine amidohydrolase.EBI
University of Pennsylvania
A new single-photon emission computed tomography (SPECT) imaging agent for serotonin transporters: [(125)I]Flip-IDAM, (2-((2-((dimethylamino)methyl)-4-iodophenyl)thio)phenyl)methanol.EBI
University of Pennsylvania
Identification of a novel family of BRAF(V600E) inhibitors.EBI
University of Pennsylvania
Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17ß-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships.EBI
University of Pennsylvania
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.EBI
University of Pennsylvania
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.EBI
University of Pennsylvania
Hydrophobic effect and hydrogen bonds account for the improved activity of a complement inhibitor, compstatin.EBI
University of Pennsylvania
F-18 stilbenes as PET imaging agents for detecting beta-amyloid plaques in the brain.EBI
University of Pennsylvania
Replacement of Phe6, Phe7, and Phe11 of D-Trp8-somatostatin-14 with L-pyrazinylalanine. Predicted and observed effects on binding affinities at hSST2 and hSST4. An unexpected effect of the chirality of Trp8 on NMR spectra in methanol.EBI
University of Pennsylvania
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.EBI
University of Pennsylvania
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.EBI
University of Pennsylvania
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.EBI
University of Pennsylvania
Secondary interactions significantly removed from the sulfonamide binding pocket of carbonic anhydrase II influence inhibitor binding constants.EBI
University of Pennsylvania
Derivatives of 4-(2'-methoxyphenyl)-1-[2'-(N-2"-pyridinyl-p-iodobenzamido)ethyl]pipera zine (p-MPPI) as 5-HT1A ligands.EBI
University of Pennsylvania
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand.EBI
University of Pennsylvania
R2 C-terminal peptide inhibition of mammalian and yeast ribonucleotide reductase.EBI
University of Pennsylvania
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography.EBI
University of Pennsylvania
Synthesis of (R,S)-trans-8-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'-propenyl)amino]tetral in (trans-8-OH-PIPAT): a new 5-HT1A receptor ligand.EBI
University of Pennsylvania
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.EBI
University of Pennsylvania
Synthesis and characterization of iodobenzamide analogues: potential D-2 dopamine receptor imaging agents.EBI
University of Pennsylvania
Dopamine D-2 receptor imaging radiopharmaceuticals: synthesis, radiolabeling, and in vitro binding of (R)-(+)- and (S)-(-)-3-iodo-2-hydroxy-6-methoxy-N- [(1-ethyl-2-pyrrolidinyl)methyl]benzamide.EBI
University of Pennsylvania
Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.EBI
University of Pennsylvania
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.EBI
University of Pennsylvania
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.EBI
University of Pennsylvania
Synthesis of new (-)-bestatin-based inhibitor libraries reveals a novel binding mode in the S1 pocket of the essential malaria M1 metalloaminopeptidase.EBI
University of Pennsylvania
Discovery of substituted 3-(phenylamino)benzoic acids as potent and selective inhibitors of type 5 17ß-hydroxysteroid dehydrogenase (AKR1C3).EBI
University of Pennsylvania
2-aminoimidazole amino acids as inhibitors of the binuclear manganese metalloenzyme human arginase I.EBI
University of Pennsylvania
Iodophenyl tagged sphingosine derivatives: synthesis and preliminary biological evaluation.EBI
University of Pennsylvania
2-(2'-((dimethylamino)methyl)-4'-(fluoroalkoxy)-phenylthio)benzenamine derivatives as serotonin transporter imaging agents.EBI
University of Pennsylvania
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.EBI
University of Pennsylvania
Creation of a Peptide Antagonist of the GFRAL-RET Receptor Complex for the Treatment of GDF15-Induced Malaise.EBI
University of Pennsylvania
Focused Libraries for Epigenetic Drug Discovery: The Importance of Isosteres.EBI
University of Pennsylvania
Synthesis of biphenyltrienes as probes for beta-amyloid plaques.EBI
University of Pennsylvania
Design, synthesis, and structure-activity relationship of novel thiophene derivatives for beta-amyloid plaque imaging.EBI
University of Pennsylvania
Design, synthesis, and evaluation of octahydropyranopyrrole-based inhibitors of mammalian ribonucleotide reductase.EBI
University of Pennsylvania
2-(2-(dimethylaminomethyl)phenoxy)-5-iodophenylamine: an improved serotonin transporter imaging agent.EBI
University of Pennsylvania
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.EBI
University of Pennsylvania
Identification of gp120 Residue His105 as a Novel Target for HIV-1 Neutralization by Small-Molecule CD4-Mimics.EBI
University of Pennsylvania
Effects of heterocyclic aromatic substituents on binding affinities at two distinct sites of somatostatin receptors. Correlation with the electrostatic potential of the substituents.EBI
University of Pennsylvania
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.EBI
University of Pennsylvania
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).EBI
University of Pennsylvania
Isomerization of (Z,Z) to (E,E)1-bromo-2,5-bis-(3-hydroxycarbonyl-4-hydroxy)styrylbenzene in strong base: probes for amyloid plaques in the brain.EBI
University of Pennsylvania
Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates.EBI
University of Pennsylvania
Structural determinants of affinity and selectivity in the binding of inhibitors to histone deacetylase 6.EBI
University of Pennsylvania
Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor.EBI
University of Pennsylvania
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine DEBI
University of Pennsylvania
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.EBI
University of Pennsylvania
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.EBI
University of Pennsylvania
Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.EBI
University of Pennsylvania
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.EBI
University of Pennsylvania
Specificity of diastereomers of [99mTc]TRODAT-1 as dopamine transporter imaging agents.EBI
University of Pennsylvania
Isoindol-1-one analogues of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridyl)-p-iodobenzamido]ethyl]pipera zine (p-MPPI) as 5-HT1A receptor ligands.EBI
University of Pennsylvania
Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.EBI
University of Pennsylvania
Exploring Structural Determinants of Inhibitor Affinity and Selectivity in Complexes with Histone Deacetylase 6.EBI
University of Pennsylvania
Synthesis and characterization of technetium-99m-labeled tropanes as dopamine transporter-imaging agents.EBI
University of Pennsylvania
Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases.EBI
University of Pennsylvania
Synthesis and optical resolution of (R)- and (S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand.EBI
University of Pennsylvania
Fluorinated and iodinated dopamine agents: D2 imaging agents for PET and SPECT.EBI
University of Pennsylvania
Iodinated 2-aminotetralins and 3-amino-1-benzopyrans: ligands for dopamine D2 and D3 receptors.EBI
University of Pennsylvania
The β-Amyloid Hypothesis in Alzheimer's Disease: Seeing Is Believing.EBI
University of Pennsylvania
Multidentate (18)F-polypegylated styrylpyridines as imaging agents for Aβ plaques in cerebral amyloid angiopathy (CAA).EBI
University of Pennsylvania
Identification of triazinoindol-benzimidazolones as nanomolar inhibitors of the Mycobacterium tuberculosis enzyme TDP-6-deoxy-d-xylo-4-hexopyranosid-4-ulose 3,5-epimerase (RmlC).EBI
University of Pennsylvania
18F stilbenes and styrylpyridines for PET imaging of A beta plaques in Alzheimer's disease: a miniperspective.EBI
University of Pennsylvania
Synthesis and evaluation of indolinyl- and indolylphenylacetylenes as PET imaging agents for beta-amyloid plaques.EBI
University of Pennsylvania
Radioiodinated aza-diphenylacetylenes as potential SPECT imaging agents for beta-amyloid plaque detection.EBI
University of Pennsylvania
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.EBI
University of Pennsylvania
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques.EBI
University of Pennsylvania
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.EBI
University of Pennsylvania
N-(7-Cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide (TAK632) Promotes Inhibition of BRAF through the Induction of Inhibited Dimers.EBI
University of Pennsylvania
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.EBI
University of Pennsylvania
Preparation and biodistribution of 1-[2-(3-[125I]iodo-4-aminophenyl)ethyl]-4-[3-(trifluoromethyl) phenyl]piperazine and 1-[2-(3-[125I]iodo-4-azidophenyl)ethyl]-4-[3-(trifluoromethyl)phenyl] piperazine.EBI
University of Pennsylvania
Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.EBI
University of Pennsylvania
Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.EBI
University of Pennsylvania
(+/-)-7-chloro-8-hydroxy-1-(4'-[125I]iodophenyl)-3-methyl-2,3,4,5- tetrahydro-1H-3-benzazepine: a potential CNS D-1 dopamine receptor imaging agent.EBI
University of Pennsylvania
Highly Selective Dopamine DEBI
University of Pennsylvania
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.EBI
University of Pennsylvania
N-arylmethyl sulfonamide negative modulators of NR2ABDB
Luc Therapeutics
Histone deacetylase inhibitorsBDB
Biomarin Pharmaceutical
Indazolecarboxamides, processes for their preparation, pharmaceutical preparations comprising them and their use for producing medicamentsBDB
Bayer Pharma Aktiengesellschaft
Heterocyclic compounds as LSD1 inhibitorsBDB
Incyte
Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereofBDB
Shanghai Yingli Pharmaceutical
Substituted oxopyridine derivativesBDB
Bayer Pharma Aktiengesellschaft
Imide and acylurea derivatives as modulators of the glucocorticoid receptorBDB
Bristol-Myers Squibb
Guanine analogs as telomerase substrates and telomere length affectorsBDB
Geron
Isoxazole derivative as mutant isocitrate dehydrogenase 1 inhibitorBDB
Daiichi Sankyo
1,3,4-thiadiazole compounds and their use in treating cancerBDB
Astrazeneca
Cyclic sulfonamides as sodium channel blockersBDB
Purdue Pharma
Pyrimidine derivatives as protein kinase inhibitorsBDB
Cyclacel
Inhibitors of Burton's tyrosine kinaseBDB
Roche Palo Alto
Triazine derivative and pharmaceutical composition comprising the sameBDB
Shionogi
N-substituted-5-substituted phthalamic acids as sortilin inhibitorsBDB
H. Lundbeck
Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.BDB
Boehringer Ingelheim Pharmaceuticals
Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors.BDB
Universita Di Pisa
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.BDB
Kudos Pharmaceuticals
Fragment-based substrate activity screening method for the identification of potent inhibitors of the Mycobacterium tuberculosis phosphatase PtpB.BDB
University of California Berkeley
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride SynthesisBDB
Wyeth Research
Identification of BRAF inhibitors through in silico screening.BDB
University of Pennsylvania