PMID

Data

Article Title

Organization

Discovery of benzimidazole derivatives as modulators of mitochondrial function: A potential treatment for Alzheimer's disease.

Korea Institute of Science and Technology

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT

National Institute of Diabetes and Digestive and Kidney Diseases

Synthesis and evaluation of aporphine analogs containing C1 allyl isosteres at the h5-HT(2A) receptor.

City University of New York

First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).

University of New South Wales

C4 phenyl aporphines with selective h5-HT(2B) receptor affinity.

City University of New York

Ether analogues of DPA-714 with subnanomolar affinity for the translocator protein (TSPO).

Stanford University School of Medicine

Discovery of a neuroprotective chemical, (S)-N-(3-(3,6-dibromo-9H-carbazol-9-yl)-2-fluoropropyl)-6-methoxypyridin-2-amine [(-)-P7C3-S243], with improved druglike properties.

University of Texas Southwestern Medical Center

Synthesis and evaluation in monkey of [(18)F]4-fluoro-N-methyl-N-(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([(18)F]FIMX): a promising radioligand for PET imaging of brain metabotropic glutamate receptor 1 (mGluR1).

National Institute of Mental Health

Identification of a novel benzoxazolone derivative as a selective, orally active 18 kDa translocator protein (TSPO) ligand.

Dainippon Sumitomo Pharma

Discovery of ML314, a Brain Penetrant Non-Peptidic?-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.

Sanford-Burnham Medical Research Institute

Genetic neural networks for quantitative structure-activity relationships: improvements and application of benzodiazepine affinity for benzodiazepine/GABAA receptors.

Harvard University

Synthesis of 6-[¹8F]fluoro-PBR28, a novel radiotracer for imaging the TSPO 18 kDa with PET.

Cea

TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT.

TBA

Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.

National Institute of Mental Health

Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.

Emory University

Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.

Abbott Laboratories

From hit to lead. Analyzing structure-profile relationships.

Universities of Lille

(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.

Virginia Commonwealth University

1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.

Tibotec

Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.

National Institute of Mental Health

Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.

National Institute of Mental Health

Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.

National Institute of Mental Health

Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.

University of Nebraska Medical Center

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.

Predix Pharmaceuticals

Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.

Columbia University College of Physicians and Surgeons

The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.

Niddk

Glioblastoma: Current Status, Emerging Targets, and Recent Advances.

Taipei Medical University

An update into the medicinal chemistry of translocator protein (TSPO) ligands.

University of Pisa

Structure-Activity Studies of 1

National Institute of Diabetes and Digestive and Kidney Diseases

Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y

National Institute of Diabetes and Digestive and Kidney Diseases

Selective A

National Institute of Diabetes and Digestive and Kidney Diseases

Structure-Activity Relationship of Heterocyclic P2Y

National Institute of Diabetes and Digestive and Kidney Diseases

Discovery, structure-activity relationship study and biological evaluation of 2-thioureidothiophene-3-carboxylates as a novel class of C-X-C chemokine receptor 2 (CXCR2) antagonists.

University of Michigan

[18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).

National Institute of Radiological Sciences

Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.

Faculty of Science and The University of Sydney

Reversing binding sensitivity to A147T translocator protein.

The University of Sydney

Exploration of Alternative Scaffolds for P2Y

National Institute of Diabetes and Digestive and Kidney Diseases

Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.

Palack£

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A

Medical College of Wisconsin

Design and in Vivo Characterization of A

Medical College of Wisconsin

First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.

Macquarie University

Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against A?-induced neurotoxicity.

Korea Institute of Science & Technology (Kist)

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

Abbvie

Oximinoarylsulfonamides as potent HIV protease inhibitors.

Abbott Laboratories