Evidence map›Paper›PMID 25801932›Full record

ArticleBioorganic & medicinal chemistry letters2015

Synthesis and structure-activity relationships of a series of 4-methoxy-3-(piperidin-4-yl)oxy benzamides as novel inhibitors of the presynaptic choline transporter.

Sean R Bollinger, Darren W Engers, Elizabeth A Ennis, Jane Wright, Charles W Locuson, Craig W Lindsley, Randy D Blakely, Corey R Hopkins

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.6field-weighted citation impact, top 31% of its field
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

1 citing paper in PubMed, 6 citations in OpenAlex.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 1 institution in 1 country.

Sean R BollingerDepartment 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.
Darren W EngersDepartment 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.
Elizabeth A EnnisDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Jane WrightDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Charles W LocusonDepartment 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.
Craig W LindsleyDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, 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.
Randy D BlakelyDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Psychiatry, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
Corey R HopkinsDepartment of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, 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. Electronic address: corey.r.hopkins@vanderbilt.edu.
Vanderbilt University Medical Center · US

Funding

The Vanderbilt Institute for Clinical and Translational Research (VICTR)UL1TR000445 · NCATS · VANDERBILT UNIVERSITY MEDICAL CENTER · PI BERNARD, GORDON RAPHAEL · 2012 to 2016
$41.4M
The Vanderbilt Specialized Chemistry Center for Accelerated Probe DevelopmentU54MH084659 · NIMH · VANDERBILT UNIVERSITY · PI LINDSLEY, CRAIG · 2008 to 2013
$24.1M
TRAINING IN PHARMACOLOGICAL SCIENCEST32GM007628 · NIGMS · VANDERBILT UNIVERSITY · PI BARNETT, JOEY VICTOR, KAVALALI, EGE T · 1985 to 2022
$11.2M
Molecular Analysis of Presynaptic Choline TransportersR37MH073159 · NIMH · VANDERBILT UNIVERSITY · PI BLAKELY, RANDY D. · 2004 to 2013
$3.6M
NCATS NIH HHS UL1 TR000445NCATS NIH HHS UL1TR000445NIGMS NIH HHS GM07628NIGMS NIH HHS T32 GM007628NIMH NIH HHS MH073159NIMH NIH HHS R37 MH073159NIMH NIH HHS U54 MH084659
6 · The paper itself

Abstract

The synthesis and SAR of 4-methoxy-3-(piperidin-4-yl) benzamides identified after a high-throughput screen of the MLPCN library is reported. SAR was explored around the 3-piperidine substituent as well as the amide functionality of the reported compounds. Starting from the initial lead compounds, 1-7, iterative medicinal chemistry efforts led to the identification of ML352 (10m). ML352 represents a potent and selective inhibitor of CHT based on a drug-like scaffold.

Indexed as

AnimalsBenzamidesHalf-LifeHEK293 CellsHumansMembrane Transport ProteinsPiperidinesProtein BindingRatsStructure-Activity RelationshipSymportersTissue DistributionBenzamidescholine transporterMembrane Transport ProteinspiperidinePiperidinesSLC5A7 protein, humanSymportersCholine transporterCHTML352MLPCNStructure–activity relationship

Identifiers

PMID25801932
PMCPMC4385452
OpenAlexW2070822748

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.