Evidence map›Paper›PMID 33859803›Full record

ArticleACS medicinal chemistry letters2021

Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.

Wuqing Deng, Xiaojuan Chen, Kaili Jiang, Xiaojuan Song, Minhao Huang, Zheng-Chao Tu, Zhang Zhang, Xiaojing Lin, Raquel Ortega, Adam V Patterson and 5 more

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

Article in ACS medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.5field-weighted citation impact, top 18% 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

3 citing papers in PubMed, 23 citations in OpenAlex.

  1. Article
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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

15 authors at 4 institutions in 2 countries.

Wuqing DengSchool of Pharmacy, Jinan University, #601 Huangpu Avenue West, Guangzhou 510632, China.
Xiaojuan ChenDepartment of Oncology, NHC Key Laboratory of Cancer Proteomics and Laboratory of Structural Biology, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China.
Kaili JiangSchool of Pharmacy, Jinan University, #601 Huangpu Avenue West, Guangzhou 510632, China.
Xiaojuan SongGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
Minhao HuangGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
Zheng-Chao TuGuangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
Zhang ZhangSchool of Pharmacy, Jinan University, #601 Huangpu Avenue West, Guangzhou 510632, China.
Xiaojing LinAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Raquel OrtegaAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Adam V PattersonMaurice Wilkins Centre for Molecular Biodiscovery, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Jeff B SmaillMaurice Wilkins Centre for Molecular Biodiscovery, University of Auckland, Private Bag 92019, Auckland 1142, New Zealand.
Ke DingSchool of Pharmacy, Jinan University, #601 Huangpu Avenue West, Guangzhou 510632, China.
Suming ChenYancheng Dafeng People's Hospital, #139 Xingfu East Road, Dafeng District,Yancheng 224100, China.
Yongheng ChenDepartment of Oncology, NHC Key Laboratory of Cancer Proteomics and Laboratory of Structural Biology, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China.
Xiaoyun LuSchool of Pharmacy, Jinan University, #601 Huangpu Avenue West, Guangzhou 510632, China.
Jinan University · CNUniversity of Auckland · NZGuangzhou Institutes of Biomedicine and Health · CNCentral South University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Covalent kinase inhibitors are rapidly emerging as a class of therapeutics with clinical benefits. Herein we report a series of selective 2-aminopyrimidine-based fibroblast growth factor receptor 4 (FGFR4) inhibitors exploring different types of cysteine-targeting warheads. The structure-activity relationship study revealed that the chemically tuned warheads α-fluoro acrylamide, vinylsulfonamide, and acetaldehyde amine were suitable as covalent warheads for the design of selective FGFR4 inhibitors. Compounds

Identifiers

PMID33859803
PMCPMC8040253
OpenAlexW3136550777

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.