Evidence map›Paper›PMID 25499438›Full record

ArticleBioorganic & medicinal chemistry letters2015

Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.

James B Thomas, Angela M Giddings, Srinivas Olepu, Robert W Wiethe, Danni L Harris, Sanju Narayanan, Keith R Warner, Philippe Sarret, Jean-Michel Longpre, Scott P Runyon and 1 more

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 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.4field-weighted citation impact, top 46% 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

2 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. 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

11 authors at 3 institutions in 2 countries.

James B ThomasCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States. Electronic address: jbthomas@rti.org.
Angela M GiddingsCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Srinivas OlepuCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Robert W WietheCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Danni L HarrisCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Sanju NarayananCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Keith R WarnerCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Philippe SarretDepartment of Physiology and Biophysics, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12th Ave. North, Sherbrooke, QC J1H 5N4, Canada.
Jean-Michel LongpreDepartment of Physiology and Biophysics, Faculty of Medicine and Health Sciences, Université de Sherbrooke, 3001, 12th Ave. North, Sherbrooke, QC J1H 5N4, Canada.
Scott P RunyonCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
Brian P GilmourCenter for Organic and Medicinal Chemistry, Research Triangle Institute, PO Box 12194, Research Triangle Park, NC 27709, United States.
RTI International · USResearch Triangle Park Foundation · USUniversité de Sherbrooke · CA

Funding

Synthesis and Testing of Targeted Libraries to Identify Small-molecule Agonists aR33DA029961 · NIDA · RESEARCH TRIANGLE INSTITUTE · PI GILMOUR, BRIAN P, THOMAS, JAMES B. · 2012 to 2014
$1.5M
Synthesis and Testing of Targeted Libraries to Identify Small-molecule Agonists aR21DA029961 · NIDA · RESEARCH TRIANGLE INSTITUTE · PI GILMOUR, BRIAN P, THOMAS, JAMES B. · 2010 to 2011
$937k
NIDA NIH HHS DA029961NIDA NIH HHS R21 DA029961NIDA NIH HHS R33 DA029961
6 · The paper itself

Abstract

Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesic effects in relevant animal models. Using a pharmacophore model based on known NT receptor nonpeptide compounds, we screened commercial databases to identify compounds that might possess activity at NTS2 receptor sites. Modification of our screening hit to include structural features known to be recognized by NTS1 and NTS2, led to the identification of the novel NTS2 selective nonpeptide, N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (9). This compound is a potent partial agonist in the FLIPR assay with a profile of activity similar to that of the reference NTS2 analgesic nonpeptide levocabastine (5).

Indexed as

Drug Partial AgonismCalciumHumansLeucineModels, MolecularMolecular StructureQuinazolinesRadioligand AssayReceptors, NeurotensinStructure-Activity RelationshipCalciumLeucineNTRC-808NTSR2 protein, humanQuinazolinesReceptors, NeurotensinFLIPR assayLevocabastineNeurotensinNTS2 receptorPainSR142948aSR48692

Identifiers

PMID25499438
PMCPMC4296974
OpenAlexW1967959358

What OpenQuestion holds

Textmetadata
LicenceTDM
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.