Evidence map›Paper›PMID 29277458›Full record

ArticleBioorganic & medicinal chemistry letters2018

Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors.

Andrii Monastyrskyi, Simon Bayle, Victor Quereda, Wayne Grant, Michael Cameron, Derek Duckett, William Roush

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. 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

7 authors.

Andrii MonastyrskyiDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Simon BayleDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Victor QueredaDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Wayne GrantDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Michael CameronDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
Derek DuckettDepartment of Molecular Medicine, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
William RoushDepartment of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States. Electronic address: roush@scripps.edu.

Funding

Development of in vivo active small molecule selective inhibitors of ASK1R01GM122109 · NIGMS · SCRIPPS FLORIDA · PI BANNISTER, THOMAS D, DUCKETT, DEREK RONALD · 2017 to 2019
$1.6M
NIGMS NIH HHS R01 GM122109
6 · The paper itself

Abstract

The development of a new series of apoptosis signal-regulating kinase 1 (ASK1) inhibitors is described. Starting from purine, pyrimidine and quinazoline scaffolds identified by high throughput screening, we used tools of structure-based drug design to develop a series of potent kinase inhibitors, including 2-arylquinazoline derivatives 12 and 23, with submicromolar inhibitory activities against ASK1. Kinetic analysis demonstrated that the 2-arylquinazoline scaffold ASK1 inhibitors described herein are ATP competitive.

Indexed as

Drug DiscoveryAnimalsCell LineDose-Response Relationship, DrugHumansMAP Kinase Kinase 6MAP Kinase Kinase Kinase 5Models, MolecularMolecular StructurePhosphorylationProtein Kinase InhibitorsQuinazolinesRatsStructure-Activity RelationshipTumor Necrosis Factor-alphaMAP3K5 protein, humanMAP Kinase Kinase 6MAP Kinase Kinase Kinase 5Protein Kinase InhibitorsQuinazolinesTumor Necrosis Factor-alphaApoptosis signal-regulating kinase (ASK1)High throughput screeningInhibitorKinaseStructure-based drug design

Identifiers

PMID29277458
PMCPMC5999544

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.