Evidence map›Paper›PMID 31071238›Full record

ArticleChemMedChem2019

Development of Tetrahydroindazole-Based Potent and Selective Sigma-2 Receptor Ligands.

Iredia D Iyamu, Wei Lv, Neha Malik, Rama K Mishra, Gary E Schiltz

Abstract read
In one paragraph

Article in ChemMedChem, 2019. 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
–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

4 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Review
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.

Iredia D IyamuCenter for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL, 60208, USA.
Wei LvCenter for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL, 60208, USA.
Neha MalikCenter for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL, 60208, USA.
Rama K MishraCenter for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL, 60208, USA.
Gary E SchiltzCenter for Molecular Innovation and Drug Discovery, Northwestern University, Evanston, IL, 60208, USA.ORCID 0000-0003-4180-5051

Funding

Tumor Environment and Metastasis (TEAM) Research ProgramP30CA060553 · NCI · NORTHWESTERN UNIVERSITY AT CHICAGO · PI LEONIDAS C. PLATANIAS · 1993 to 2026
$153.9M
Small molecule CXCR4 modulators as molecular probes for studying AMLR01CA189074 · NCI · NORTHWESTERN UNIVERSITY · PI MILLER, RICHARD J, PLATANIAS, LEONIDAS C. · 2015 to 2017
$1.6M
NCI NIH HHS P30 CA060553NCI NIH HHS R01 CA189074NIMH NIH HHS HHSN271201300017C
6 · The paper itself

Abstract

The sigma-2 receptor has been shown to play important roles in a number of important diseases, including central nervous system (CNS) disorders and cancer. However, mechanisms by which sigma-2 contributes to these diseases remain unclear. The development of new sigma-2 ligands that can be used to probe the function of this protein and potentially as drug discovery leads is therefore of great importance. Herein we report the development of a series of tetrahydroindazole compounds that are highly potent and selective for sigma-2. Structure-activity relationship data were used to generate a pharmacophore model that summarizes the common features present in the potent ligands. Assays for solubility and microsomal stability showed that several members of this compound series possess promising characteristics for further development of useful chemical probes or drug discovery leads.

Indexed as

Drug DesignHumansIndazolesLigandsMicrosomesProtein BindingReceptors, sigmaSigma-1 ReceptorSolubilityStructure-Activity RelationshipIndazolesLigandsReceptors, sigmaSigma-1 Receptorsigma-2 receptorpharmacophoressigma-1sigma-2solubilitytetrahydroindazoles

Identifiers

PMID31071238
PMCPMC6613831

What OpenQuestion holds

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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.