PMID

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Article Title

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Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Core.

Vanderbilt University

New structure-activity relationships of N-acetamide substituted pyrazolopyrimidines as pharmacological ligands of TSPO.

Vanderbilt University

Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.

Vanderbilt University

Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics

Vanderbilt University

Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition.

Vanderbilt University

Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.

Vanderbilt University

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Vanderbilt University

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Vanderbilt University

Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.

Vanderbilt University

Rational Design of Novel Pyridinol-Fused Ring Acetaminophen Analogues.

Vanderbilt University

Improving the affinity of SL0101 for RSK using structure-based design.

Vanderbilt University

Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein.

Vanderbilt University

3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators.

Vanderbilt University

Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors.

Vanderbilt University

(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors.

Vanderbilt University

A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.

Vanderbilt University

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.

Vanderbilt University

Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.

Vanderbilt University

A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.

Vanderbilt University

Synthesis and characterization of a pegylated derivative of 3-(1,2,3,6-tetrahydro-pyridin-4yl)-1H-indole (IDT199): a high affinity SERT ligand for conjugation to quantum dots.

Vanderbilt University

2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery.

Vanderbilt University

Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.

Vanderbilt University

Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.

Vanderbilt University

Discovery of VU2957 (Valiglurax): An mGlu

Vanderbilt University

Persistent challenges in the development of an mGlu

Vanderbilt University

Discovery of a potent M

Vanderbilt University

Ring Size as an Independent Variable in Cyclooligomeric Depsipeptide Antiarrhythmic Activity.

Vanderbilt University

Discovery of a potent M

Vanderbilt University

High affinity inhibitors of the dopamine transporter (DAT): novel biotinylated ligands for conjugation to quantum dots.

Vanderbilt University

Development of

Vanderbilt University

Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots.

Vanderbilt University

Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1.

Vanderbilt University

Development and profiling of mGlu

Vanderbilt University

Discovery of structurally distinct tricyclic M

Vanderbilt University

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M

Vanderbilt University

Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.

Vanderbilt University

Optimization of ether and aniline based inhibitors of lactate dehydrogenase.

Vanderbilt University

Discovery and optimization of a novel CNS penetrant series of mGlu

Vanderbilt University

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.

Vanderbilt University

Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu

Vanderbilt University

Synthesis and SAR of a series of mGlu

Vanderbilt University

Lead optimization of the VU0486321 series of mGlu

Vanderbilt University

Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu

Vanderbilt University

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu

Vanderbilt University

Discovery of structurally distinct tricyclic M

Vanderbilt University

Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M

Vanderbilt University

Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design.

Vanderbilt University

Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes.

Vanderbilt University

Fragment-based screening of programmed death ligand 1 (PD-L1).

Vanderbilt University

Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction.

Vanderbilt University

Surveying heterocycles as amide bioisosteres within a series of mGlu

Vanderbilt University

SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M

Vanderbilt University

Novel M

Vanderbilt University

Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes.

Vanderbilt University

Discovery of a novel 3,4-dimethylcinnoline carboxamide M

Vanderbilt University

Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu

Vanderbilt University

Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy.

Vanderbilt University

Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu

Vanderbilt University

Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib.

Vanderbilt University

Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors.

Vanderbilt University

The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor.

Vanderbilt University

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu

Vanderbilt University

Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Vanderbilt University

Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M

Vanderbilt University

Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

Vanderbilt University

Discovery of VU6005649, a CNS Penetrant mGlu

Vanderbilt University

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.

Vanderbilt University

VU6010608, a Novel mGlu

Vanderbilt University

Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.

Vanderbilt University

Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.

Vanderbilt University

Discovery of a novel, CNS penetrant M

Vanderbilt University

Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.

Vanderbilt University

Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin.

Vanderbilt University

PRPK INHIBITORS

Dana-Farber Cancer Institute

RIP1K inhibitors

Rigel Pharmaceuticals

Azabenzimidazoles and their use as AMPA receptor modulators

Janssen Pharmaceutica

Substituted sulfoximine compounds

Cadila Healthcare

Dual MAGL and FAAH inhibitors

Abide Therapeutics

Modulators of the sigma-2 receptor and their method of use

Temple University

Inhibitors of Hepatitis C virus polymerase

Cocrystal Pharma

Thienopyridines and benzothiophenes useful as IRAK4 inhibitors

Bristol-Myers Squibb

Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor

Chia Tai Tianqing Pharmaceutical Group

Pyrazolyl pyrrolo[2,3-b]pyrmidine-5-carboxylate analogs and methods of making the same

Aclaris Therapeutics

Therapeutic inhibitory compounds

Attune Pharmaceuticals

Inhibitors of protein kinases

Portola Pharmaceuticals

Certain chemical entities, compositions, and methods

Neupharma

Nitrogen-containing tricyclic derivatives having HIV replication inhibitory activity

Shionogi

Compounds that inhibit MPS1 kinase

Cancer Research Technology

Aminopyrimidinyl compounds

Pfizer

Inhibitors of the IRE-1/XBP-1 pathway and methods of using thereof

H. Lee Moffitt Cancer Center and Research Institute

Heterocyclic GLP-1 agonists

Gasherbrum Bio

Bacterial topoisomerase I inhibitors with antibacterial activity

The Florida International University Board of Trustees

Indoline compounds as aldosterone synthase inhibitors

Merck Sharp & Dohme

Oxoazetidine derivatives, process for the preparation thereof and use thereof in human medicine and in cosmetics

Galderma Research & Development

Spiro ring compound as hepatitis C virus (HCV) inhibitor and uses thereof

Sunshine Lake Pharma

Cyclopropanecarboxamido-substitute aromatic compounds as anti-tumor agents

Crown Bioscience Inc. (Taiwan)

Indazole derivatives useful as ERK inhibitors

Merck Sharp & Dohme

Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists

Merck Sharp & Dohme

Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity

Boehringer Ingelheim International

2′-cyano substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases

Merck Sharp & Dohme

2-(Hetero(aryl)methylene)hydrazine-1-carbothioamides as potent urease inhibitors.

Quaid-I-Azam University

An efficient synthesis of SK-658 and its analogs as potent histone deacetylase inhibitors.

Kyushu Institute of Technology

Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors

Boehringer Ingelheim International

Inhibitors of Bruton's tyrosine kinase

Pharmacyclics

 

Synthesis of 3,5-disubstituted isoxazolines as protein tyrosine phosphatase 1B inhibitors

Central Drug Research Institute

Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo.

Case Western Reserve University

Identification of biologically active PDE11-selective inhibitors using a yeast-based high-throughput screen.

Boston College

A natural product ligand of the oxysterol receptor, liver X receptor.

Eli Lilly

The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound.

Janssen Research Foundation

Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist.

Sanofi Recherche

Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells.

Janssen Research Foundation

Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS.

Cytopia Research

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.

Ambit