Evidence map›Paper›PMID 35557491›Full record

ArticleChemMedChem2022

Further Exploration of the Benzimidazole Scaffold as TRPC5 Inhibitors: Identification of 1-Alkyl-2-(pyrrolidin-1-yl)-1H-benzo[d]imidazoles as Potent and Selective Inhibitors.

Swagat Sharma, Juan L Pablo, Kirsten T Tolentino, Wacey Gallegos, Jennifer Hinman, Madison Beninato, MacKenzie Asche, Anna Greka, Corey R Hopkins

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ChemMedChem, 2022. 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
–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

1 citing paper in PubMed.

  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

9 authors.

Swagat SharmaDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
Juan L PabloDepartment of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, 02115, USA.
Kirsten T TolentinoDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
Wacey GallegosDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
Jennifer HinmanDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
Madison BeninatoDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
MacKenzie AscheDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.
Anna GrekaDepartment of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, 02115, USA.
Corey R HopkinsDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, 68198, USA.ORCID 0000-0003-4958-1697

Funding

Optimization of novel inhibitors of TRPC5 as anti-proteinuric therapeuticsR01DK103658 · NIDDK · VANDERBILT UNIVERSITY · PI HOPKINS, COREY R. · 2014 to 2018
$1.7M
NIDDK NIH HHS R01 DK103658
6 · The paper itself

Abstract

The transient receptor potential cation channel 5 (TRPC5) plays an important role in numerous cellular processes. Due to this, it has gained considerable attention over the past few years as a potential therapeutic target. Recently, TRPC5 has been shown to be involved in the regulation of podocyte survival, indicating a potential treatment option for chronic kidney disease. In addition, a recent study has shown TRPC5 to be expressed in human sensory neurons and suggests that TRPC5 inhibition could be an effective treatment for spontaneous and tactile pain. To understand these processes more fully, potent and selective tool compounds are needed. Herein we report further exploration of the 2-aminobenzimidazole scaffold as a potent TRPC5 inhibitor, culminating in the discovery of 16 f as a potent and selective TRPC5 inhibitor.

Indexed as

ImidazolesTRPC Cation ChannelsBenzimidazolesCationsHumansBenzimidazolesCationsImidazolesTRPC5 protein, humanTRPC Cation Channelsbenzimidazolechronic kidney diseasepaintransient receptor potential cation channel 5TRPC5

Identifiers

PMID35557491
PMCPMC9308755

What OpenQuestion holds

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LicenceCC BY-NC-ND
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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.