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116 articles for Vanderbilt University


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDArticle TitlePublishedDeposition
36966977 Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS. 01-MAY-2023 22-APR-2024
30891122 Discovery of VU2957 (Valiglurax): An mGlu 14-MAR-2019 22-APR-2024
36528230 Persistent challenges in the development of an mGlu 15-JAN-2023 20-APR-2024
36228968 Discovery of a potent M 15-DEC-2022 20-APR-2024
34917258 Ring Size as an Independent Variable in Cyclooligomeric Depsipeptide Antiarrhythmic Activity. 09-DEC-2021 19-APR-2024
US11752138 Treating primary or idiopathic hyperoxaluria with small molecule inhibitors of lactate dehydrogenase 12-SEP-2023 20-OCT-2023
36113671 Discovery of a potent M 15-NOV-2022 26-JUN-2023
35417155 Development of 28-APR-2022 25-JUN-2023
35944850 Development and profiling of mGlu 15-OCT-2022 18-JUN-2023
US11596639 Substituted indole Mcl-1 inhibitors 07-MAR-2023 23-APR-2023
34710625 Discovery of structurally distinct tricyclic M 01-DEC-2021 04-MAR-2023
34413964 Discovery of VU6028418: A Highly Selective and Orally Bioavailable M 12-AUG-2021 24-AUG-2022
34461178 Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds. 15-OCT-2021 24-AUG-2022
33771585 Optimization of ether and aniline based inhibitors of lactate dehydrogenase. 01-JUN-2021 20-AUG-2022
US11319304 Pyridine quinoline compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 03-MAY-2022 07-AUG-2022
US11242342 Isoquinoline amine compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 08-FEB-2022 10-JUN-2022
US11208415 Substituted indole Mcl-1 inhibitors 28-DEC-2021 03-MAY-2022
33556572 Discovery and optimization of a novel CNS penetrant series of mGlu 01-APR-2021 29-MAR-2022
32750526 Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors. 15-SEP-2020 28-MAR-2022
32371100 Synthesis and pharmacological evaluation of bivalent tethered ligands to target the mGlu 01-JUL-2020 28-MAR-2022
32890686 Synthesis and SAR of a series of mGlu 15-NOV-2020 25-MAR-2022
33253881 Lead optimization of the VU0486321 series of mGlu 15-JAN-2021 24-MAR-2022
32944146 Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu 10-SEP-2020 22-MAR-2022
30503632 The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu 15-JAN-2019 21-MAR-2022
US11149022 Antagonists of the muscarinic acetylcholine receptor M4 19-OCT-2021 13-MAR-2022
US10968227 Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 06-APR-2021 09-OCT-2021
US10954193 Substituted indole Mcl-1 inhibitors 23-MAR-2021 28-SEP-2021
31784320 Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M 01-FEB-2020 12-AUG-2021
31787491 Discovery of structurally distinct tricyclic M 15-FEB-2020 12-AUG-2021
32223236 Discovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design. 23-APR-2020 11-AUG-2021
US10844032 Substituted benzofuran, benzothiophene and indole Mcl-1 inhibitors 24-NOV-2020 06-JUL-2021
US10844044 WDR5 inhibitors and modulators 24-NOV-2020 06-JUL-2021
US10807959 WDR5-MLL1 inhibitors and modulators 20-OCT-2020 11-JUN-2021
US10793514 Glutamine transport inhibitors and methods for treating cancer 06-OCT-2020 14-MAY-2021
27503678 Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes. 15-SEP-2016 28-FEB-2021
30728114 Fragment-based screening of programmed death ligand 1 (PD-L1). 15-MAR-2019 27-FEB-2021
31724864 Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5-MYC Protein-Protein Interaction. 26-DEC-2019 26-FEB-2021
30910459 Surveying heterocycles as amide bioisosteres within a series of mGlu 15-MAY-2019 24-FEB-2021
30580918 Novel M 01-FEB-2019 23-FEB-2021
31248774 SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M 15-AUG-2019 23-FEB-2021
30528696 Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes. 15-JAN-2019 22-FEB-2021
31537424 Discovery of a novel 3,4-dimethylcinnoline carboxamide M 01-NOV-2019 22-FEB-2021
31358468 Further exploration of an N-aryl phenoxyethoxy pyridinone-based series of mGlu 15-SEP-2019 20-FEB-2021
31938459 Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy. 09-JAN-2020 19-FEB-2021
30247901 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 10-JAN-2019 18-FEB-2021
US10538491 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators 21-JAN-2020 09-NOV-2020
US10533010 Substituted indole Mcl-1 inhibitors 14-JAN-2020 02-NOV-2020
US10501466 WDR5 inhibitors and modulators 10-DEC-2019 12-OCT-2020
US10508105 Indazole compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 17-DEC-2019 12-OCT-2020
US10487087 Positive allosteric modulators of the GLP-1 receptor 26-NOV-2019 20-SEP-2020
23687559 The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor. 09-MAY-2013 01-SEP-2020
24060487 Exploring the molecular determinants of substrate-selective inhibition of cyclooxygenase-2 by lumiracoxib. 01-NOV-2013 01-SEP-2020
US10399948 Negative allosteric modulators of metabotropic glutamate receptor 3 03-SEP-2019 24-AUG-2020
29958762 Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu 15-AUG-2018 17-AUG-2020
29705142 Discovery of 6-(pyrimidin-5-ylmethyl)quinoline-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5. 01-JUN-2018 16-AUG-2020
29037946 Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M 15-NOV-2017 15-AUG-2020
29057060 Discovery of VU6005649, a CNS Penetrant mGlu 12-OCT-2017 04-JUL-2020
29856609 Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling. 26-JUL-2018 24-JUN-2020
29259756 VU6010608, a Novel mGlu 14-DEC-2017 23-JUN-2020
US10294214 Positive allosteric modulators of human melanocortin-4 receptor 21-MAY-2019 10-MAR-2020
28958625 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. 01-NOV-2017 25-JAN-2020
28866269 Discovery of a novel, CNS penetrant M 15-SEP-2017 19-JAN-2020
US10239887 Positive allosteric modulators of the muscarinic acetylcholine receptor M4 26-MAR-2019 30-DEC-2019
US10227343 Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 12-MAR-2019 27-DEC-2019
28428041 Structure of a Myeloid cell leukemia-1 (Mcl-1) inhibitor bound to drug site 3 of Human Serum Albumin. 15-JUN-2017 30-NOV-2019
US10221175 Substituted pyrrolo[3,4-e]indolizines, imidazo[1,2-a]pyrrolo[3,4-e]pyridines, pyrrolo[3,4-e][1,2,4]triazolo[1,5-a]pyridines and pyrrolo[3,4-e][1,2,4]triazolo[4,3-a]pyridines as positive allosteric modulators of muscarinic acetylcholine receptor M1 05-MAR-2019 27-OCT-2019
US10221172 Benzothiazole and benzisothiazole-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 05-MAR-2019 27-OCT-2019
US10189805 Metabolism probes for therapy and diagnosis 29-JAN-2019 25-MAY-2019
28103022 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. 23-FEB-2017 01-MAY-2019
US9550778 Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5 24-JAN-2017 18-SEP-2018
US9676782 Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of metabotropic glutamate receptor 3 13-JUN-2017 07-AUG-2018
27353534 New structure-activity relationships of N-acetamide substituted pyrazolopyrimidines as pharmacological ligands of TSPO. 19-JUL-2016 06-OCT-2017
US9453017 Antiviral therapies with phospholipase D inhibitors 27-SEP-2016 05-SEP-2017
27080176 Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists. 16-JUN-2016 14-JUL-2017
US9346803 Indomethacin analogs for the treatment of castrate-resistant prostate cancer 24-MAY-2016 05-JUN-2017
24047900 Complexes of Trypanosoma cruzi sterol 14a-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity. 01-NOV-2013 25-FEB-2017
US9255103 Substituted pyrazolo[1,5-a]pyrazines as mGluR5 receptor modulators 09-FEB-2016 20-DEC-2016
26426481 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 22-OCT-2015 14-DEC-2016
US9192603 Heterocyclic sulfone mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 24-NOV-2015 19-SEP-2016
US9180192 mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 10-NOV-2015 15-AUG-2016
US9163015 Pyrazolopyridine, pyrarolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction 20-OCT-2015 18-JUL-2016
US9127005 Isoform selective phospholipase D inhibitors 08-SEP-2015 09-MAY-2016
25466173 Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition. 03-DEC-2014 17-MAR-2016
25221667 Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity. 15-SEP-2014 08-MAR-2016
US9040694 Compounds and methods useful for directing stem cell differentiation 26-MAY-2015 21-DEC-2015
25384256 Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes. 20-FEB-2015 15-OCT-2015
US8796295 Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same 05-AUG-2014 12-JAN-2015
24164599 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). 27-NOV-2013 25-JUL-2014
US8598345 Substituted heteroarylamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same 03-DEC-2013 14-APR-2014
24482730 Rational Design of Novel Pyridinol-Fused Ring Acetaminophen Analogues. 08-AUG-2013 13-APR-2014
23916258 Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators. 23-AUG-2013 13-APR-2014
24050755 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). 24-OCT-2013 13-APR-2014
US8569308 Substituted heteroarylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same 29-OCT-2013 24-FEB-2014
23519677 Improving the affinity of SL0101 for RSK using structure-based design. 14-FEB-2012 24-SEP-2013
11964599 Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein. 19-APR-2002 22-MAY-2013
20732812 3D-QSAR CoMFA study of benzoxazepine derivatives as mGluR5 positive allosteric modulators. 13-SEP-2010 22-MAY-2013
7861418 Binding of 5H-dibenzo[a,d]cycloheptene and dibenz[b,f]oxepin analogues of clozapine to dopamine and serotonin receptors. 21-MAR-1995 31-OCT-2012
3172140 (S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[125I]iodo- 2-methoxybenzamide hydrochloride, a new selective radioligand for dopamine D-2 receptors. 18-NOV-1988 16-OCT-2012
8278895 Evaluation of 5-[18F]fluoropropylepidepride as a potential PET radioligand for imaging dopamine D2 receptors. XX-XXX-1993 02-JAN-2012
3139864 Putative selective 5-HT-2 antagonists block serotonin 5-HT-1c receptors in the choroid plexus. XX-XXX-1988 24-NOV-2011
18022567 Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth. XX-NOV-2007 04-AUG-2011
19136975 Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. XX-FEB-2009 25-FEB-2011
20020776 In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors. 19-FEB-2010 11-FEB-2011
19443215 A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. 29-MAY-2009 25-AUG-2010
19299128 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. 03-APR-2009 11-JAN-2010
18800848 Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential. 27-OCT-2008 11-JAN-2010
18674906 A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride. 11-AUG-2008 11-JAN-2010
8064797 Binding of 5H-dibenzo[b,e][1,4]diazepine and chiral 5H-dibenzo[a,d]cycloheptene analogues of clozapine to dopamine and serotonin receptors. 22-SEP-1994 10-NOV-2009
17766114 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. 18-SEP-2007 10-NOV-2009
16183285 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. 19-OCT-2005 10-NOV-2009
16784853 High affinity inhibitors of the dopamine transporter (DAT): novel biotinylated ligands for conjugation to quantum dots. 31-JUL-2006 10-NOV-2009
15887968 Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1. 12-MAY-2005 10-NOV-2009
1694546 Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors. 06-AUG-1990 10-NOV-2009
1967652 Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. 09-MAR-1990 10-NOV-2009
2571728 Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. 01-NOV-1989 10-NOV-2009
19354253 Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase. 14-MAY-2009 08-JUN-2009