Evidence map›Paper›PMID 24462664›Full record

ArticleBioorganic & medicinal chemistry letters2014

Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: development of a [3.3.0]-based series and other piperidine bioisosteres.

Douglas J Sheffler, Michael T Nedelcovych, Richard Williams, Stephen C Turner, Brittany B Duerk, Megan R Robbins, Sataya B Jadhav, Colleen M Niswender, Carrie K Jones, P Jeffrey Conn and 2 more

Erratum issuedAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Article
  3. Discovery of a novel 2,4-dimethylquinoline-6-carboxamide MBioorganic & medicinal chemistry letters · 2017
    Article
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

12 authors.

Douglas J ShefflerDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Apoptosis and Cell Death Research Program and Conrad Prebys Center for Chemical Genomics, Sanford-Burnham Medical Research Institute, 10901 N. Torrey Pines Rd., La Jolla, CA 92037, USA.
Michael T NedelcovychDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Richard WilliamsVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Centre for Cancer Research and Cell Biology, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK.
Stephen C TurnerDepartment of Pharmaceutical Sciences, Lipscomb University, College of Pharmacy and Health Sciences, Nashville, TN 37024-3951, USA.
Brittany B DuerkDepartment of Pharmaceutical Sciences, Lipscomb University, College of Pharmacy and Health Sciences, Nashville, TN 37024-3951, USA.
Megan R RobbinsDepartment of Pharmaceutical Sciences, Lipscomb University, College of Pharmacy and Health Sciences, Nashville, TN 37024-3951, USA.
Sataya B JadhavVanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Colleen M NiswenderDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA.
Carrie K JonesDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
P Jeffrey ConnDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA.
R Nathan DanielsDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Pharmaceutical Sciences, Lipscomb University, College of Pharmacy and Health Sciences, Nashville, TN 37024-3951, USA. Electronic address: nate.daniels@lipscomb.edu.
Craig W LindsleyDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA. Electronic address: craig.lindsley@vanderbilt.edu.

Funding

The Vanderbilt Specialized Chemistry Center for Accelerated Probe DevelopmentU54MH084659 · NIMH · VANDERBILT UNIVERSITY · PI MEILER, JENS · 2008 to 2013
$24.1M
TRAINING IN PHARMACOLOGICAL SCIENCEST32GM007628 · NIGMS · VANDERBILT UNIVERSITY · PI BARNETT, JOEY VICTOR, KAVALALI, EGE T · 1985 to 2022
$11.2M
Vanderbilt NCDDDG for Discovery of Novel Treatments for SchizophreniaU01MH087965 · NIMH · VANDERBILT UNIVERSITY · PI JONES, CARRIE KIMBERLY · 2010 to 2014
$9.3M
NIGMS NIH HHS T32 GM007628NIMH NIH HHS U01 MH08795NIMH NIH HHS U01 MH087965NIMH NIH HHS U54 MH084659
6 · The paper itself

Abstract

This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.

Indexed as

Dose-Response Relationship, DrugGlycine Plasma Membrane Transport ProteinsHumansMolecular StructurePiperidinesStructure-Activity RelationshipSulfonamidesGlycine Plasma Membrane Transport ProteinspiperidinePiperidinesSLC6A9 protein, humanSulfonamidesGlyT1Scaffold hoppingSchizophreniaTransporter

Identifiers

PMID24462664
PMCPMC3951244

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.