PMID
Data
Article Title
Organization
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.

Smithkline Beecham Pharmaceuticals
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.

Smithkline Beecham Pharmaceuticals
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.

Novartis Institutes For Biomedical Research
Discovery and profiling of a selective and efficacious Syk inhibitor.

Novartis Institutes For Biomedical Research
Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group.

University of Pennsylvania
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.

University of Pennsylvania
Syk inhibitors with high potency in presence of blood.

Novartis Institutes For Biomedical Research
One-step semisynthesis of oleacein and the determination as a 5-lipoxygenase inhibitor.

University of Athens
Design, synthesis, and evaluation of inhibitors of cathepsin L: Exploiting a unique thiocarbazate chemotype.

University of Pennsylvania
Identification and synthesis of a unique thiocarbazate cathepsin L inhibitor.

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.

University of Pennsylvania
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.

Clinical Research Institute of Montr£Al
Synthesis of a substance P antagonist with a somatostatin scaffold: factors affecting agonism/antagonism at GPCRs and the role of pseudosymmetry.

University of Pennsylvania
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.

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.

University of Pennsylvania
Structure-based design and synthesis of HIV-1 protease inhibitors employing beta-D-mannopyranoside scaffolds.

University College Dublin
Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists.

University of Pennsylvania
Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening.

Bryn Mawr College
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.

Novartis
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.

University of Pennsylvania
Studies towards the identification of a new generation of atypical antipsychotic agents.

Uk. Vinc
Design, synthesis, and evaluation of octahydropyranopyrrole-based inhibitors of mammalian ribonucleotide reductase.

University of Pennsylvania
Identification of gp120 Residue His105 as a Novel Target for HIV-1 Neutralization by Small-Molecule CD4-Mimics.

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.

University of Pennsylvania
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.

University of Pennsylvania
Optimization of Small Molecules That Sensitize HIV-1 Infected Cells to Antibody-Dependent Cellular Cytotoxicity.

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.

University of Pennsylvania
Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases.

University of Pennsylvania
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.

Glaxosmithkline Pharmaceuticals
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.

University of Pennsylvania
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research
Cyclic sulfonamides as sodium channel blockers

Purdue Pharma
Bicyclic sulfonamide compounds as sodium channel inhibitors

Amgen
Biochemical and structural analysis of inhibitors targeting the ADC-7 cephalosporinase of Acinetobacter baumannii.

Grand Valley State University
Triazolopyridine compounds as PIM kinase inhibitors

Array Biopharma
Triazine derivative and pharmaceutical composition comprising the same

Shionogi
N-substituted-5-substituted phthalamic acids as sortilin inhibitors

H. Lundbeck