Evidence map›Paper›PMID 29683647›Full record

ArticleACS chemical neuroscience2018

Structure-Activity Relationships of Pan-Gα

Alice E Berizzi, Aaron M Bender, Craig W Lindsley, P Jeffrey Conn, Patrick M Sexton, Christopher J Langmead, Arthur Christopoulos

Abstract read
In one paragraph

Article in ACS chemical neuroscience, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. ACS pharmacology & translational science · 2019
    Article
  7. Analytical Pharmacology: How Numbers Can Guide Drug Discovery.ACS pharmacology & translational science · 2019
    Review
  8. 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

7 authors.

Alice E BerizziDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences , Monash University , Parkville , Victoria 3052 , Australia.
Aaron M BenderDepartments of Pharmacology & Chemistry, Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Craig W LindsleyDepartments of Pharmacology & Chemistry, Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.ORCID 0000-0003-0168-1445
P Jeffrey ConnDepartments of Pharmacology & Chemistry, Vanderbilt Center for Neuroscience Drug Discovery , Vanderbilt University , Nashville , Tennessee 37232 , United States.
Patrick M SextonDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences , Monash University , Parkville , Victoria 3052 , Australia.
Christopher J LangmeadDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences , Monash University , Parkville , Victoria 3052 , Australia.
Arthur ChristopoulosDrug Discovery Biology, Monash Institute of Pharmaceutical Sciences , Monash University , Parkville , Victoria 3052 , Australia.

Funding

Research Project: Sensory and Multisensory Contributions to AutismU54HD083211 · NICHD · VANDERBILT UNIVERSITY MEDICAL CENTER · PI DYKENS, ELISABETH MAY · 2015 to 2019
$7.1M
Safety and tolerability testing of VU0467319: an M1 PAM for clinical developmentU19MH106839 · NIMH · VANDERBILT UNIVERSITY · PI CONN, P JEFFREY · 2015 to 2017
$5.3M
Selective M1 mAChR allosteric modulators for the treatment of schizophreniaR01MH082867 · NIMH · VANDERBILT UNIVERSITY · PI LINDSLEY, CRAIG · 2008 to 2017
$3.7M
Discovery of mAChR5 Modulators for Use in Rodent Models of Drug AddictionR01DA037207 · NIDA · VANDERBILT UNIVERSITY · PI JONES, CARRIE KIMBERLY, LINDSLEY, CRAIG · 2015 to 2017
$1.1M
NICHD NIH HHS U54 HD083211NIDA NIH HHS R01 DA037207NIMH NIH HHS R01 MH082867NIMH NIH HHS U19 MH106839
6 · The paper itself

Abstract

Recent years have seen a large increase in the discovery of allosteric ligands targeting muscarinic acetylcholine receptors (mAChRs). One of the challenges in screening such compounds is to understand their mechanisms of action and define appropriate parameter estimates for affinity, cooperativity and efficacy. Herein we describe the mechanisms of action and structure-activity relationships for a series of "pan-G

Indexed as

Allosteric RegulationAnimalsCHO CellsCholinergic AgentsCricetulusIndazolesMolecular StructureReceptors, G-Protein-CoupledReceptors, MuscarinicStructure-Activity RelationshipSulfonamides1-((1H-Indazol-5-yl)sulfonyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamideCholinergic AgentsIndazolesReceptors, G-Protein-CoupledReceptors, MuscarinicSulfonamidesaffinitycooperativityefficacyMuscarinic acetylcholine receptoroperational modelpositive allosteric modulator

Identifiers

PMID29683647
PMCPMC6106869

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.