Evidence map›Paper›PMID 34560054›Full record

ArticleBiochemical pharmacology2021

Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC).

Nawid Madjroh, Eleni Mellou, Paul A Davies, Pella C Söderhielm, Anders A Jensen

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

Article in Biochemical pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-weighted citation impact, top 43% 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

4 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. The Concise Guide to PHARMACOLOGY 2023/24: Ion channels.British journal of pharmacology · 2023
    Article
  3. Article
  4. 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

5 authors at 2 institutions in 2 countries.

Nawid MadjrohDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen Ø, Denmark.
Eleni MellouDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen Ø, Denmark.
Paul A DaviesDepartment of Neuroscience, Tufts University School of Medicine, Boston, MA, USA.
Pella C SöderhielmDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen Ø, Denmark.
Anders A JensenDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen Ø, Denmark. Electronic address: aaj@sund.ku.dk.
University of Copenhagen · DKTufts University · US

Funding

Novel actions of neurosteroids on GABA (A) receptor traffickingR01MH097446 · NIMH · TUFTS UNIVERSITY BOSTON · PI DAVIES, PAUL ANDREW, MOSS, STEPHEN J · 2013 to 2017
$2.1M
Novel actions of neurosteroids on GABA (A) receptor traffickingR01NS108378 · NINDS · TUFTS UNIVERSITY BOSTON · PI DAVIES, PAUL ANDREW, MOSS, STEPHEN J · 2018 to 2022
$2.0M
Determining the effects of human KCC2 mutations on neuronal excitabilityR21NS111338 · NINDS · TUFTS UNIVERSITY BOSTON · PI DAVIES, PAUL ANDREW · 2019 to 2020
$454k
Sensory Hypersensitivity in Fragile X Syndrome Due to Deficits in Tonic Inhibition Reversed by Neuroactive SteroidsR21NS111064 · NINDS · TUFTS UNIVERSITY BOSTON · PI DAVIES, PAUL ANDREW · 2020 to 2021
$450k
NIMH NIH HHS R01 MH097446NINDS NIH HHS R01 NS108378NINDS NIH HHS R21 NS111064NINDS NIH HHS R21 NS111338
6 · The paper itself

Abstract

The Zinc-Activated Channel (ZAC) is an atypical member of the Cys-loop receptor (CLR) superfamily of pentameric ligand-gated ion channels, with its very different endogenous agonists and signalling properties. In this study, a compound library screening at ZAC resulted in the identification of 2-(5-bromo-2-chlorobenzamido)-4-methylthiazole-5-methyl ester (1) as a novel ZAC antagonist. The structural determinants for ZAC activity in 1 were investigated by functional characterization of 61 analogs at ZAC expressed in Xenopus oocytes by two-electrode voltage clamp electrophysiology, and couple of analogs exerting more potent ZAC inhibition than 1 were identified (IC

Indexed as

AnimalsBenzamidesCysteine Loop Ligand-Gated Ion Channel ReceptorsDrug DiscoveryGene Expression RegulationHEK293 CellsHumansNerve Tissue ProteinsOocytesSmall Molecule LibrariesStructure-Activity RelationshipXenopusBenzamidesCysteine Loop Ligand-Gated Ion Channel ReceptorsNerve Tissue ProteinsSmall Molecule LibrariesZACN protein, humanCys-loop receptor (CLR)Negative allosteric modulator (NAM)N-(thiazol-2-yl)-benzamide analogsPentameric ligand-gated ion channel (pLGIC)State-dependent inhibitionZinc-Activated Channel (ZAC)

Identifiers

PMID34560054
PMCPMC9979163
OpenAlexW3198986985

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.