Evidence map›Paper›PMID 42258344›Full record

ArticleJournal of medicinal chemistry2026

Structure-Based Design and Optimization of Novel, Potent and Selective Covalent FGFR2/3 Inhibitors with a Tricyclic Core.

Xuzhi Lu, Zhaodi Tian, Xueqiang Li, Xiaojuan Chen, Jean Ching-Yi Tien, Yayuan Yang, Yue Yin, Qingrun Li, Weixue Huang, Fengtao Zhou and 10 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

20 authors.

Xuzhi LuInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, China.
Zhaodi TianState Key Laboratory of Chemical Biology and Shanghai Hongkong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Xueqiang LiKinoTeck Therapeutics Co., Ltd, 35 Sicheng Road, Tianhe District, Guangzhou 510663, China.
Xiaojuan ChenDepartment of Oncology, NHC Key Laboratory of Cancer Proteomics & State Local Joint Engineering Laboratory for Anticancer Drugs, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China.
Jean Ching-Yi TienMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yayuan YangInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, China.
Yue YinNational Facility for Protein Science in Shanghai, Shanghai Advanced Research Institute, Chinese Academy of Science, Shanghai 201210, China.
Qingrun LiNational Facility for Protein Science in Shanghai, Shanghai Advanced Research Institute, Chinese Academy of Science, Shanghai 201210, China.
Weixue HuangState Key Laboratory of Chemical Biology and Shanghai Hongkong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.ORCID 0000-0003-4884-6585
Fengtao ZhouInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, China.ORCID 0000-0003-2518-7855
Jinwei ZhangState Key Laboratory of Chemical Biology and Shanghai Hongkong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Xiaomei RenState Key Laboratory of Chemical Biology and Shanghai Hongkong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.
Dan LiuState Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.ORCID 0000-0002-1077-5884
Abigail J ToddMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Shuqin LiMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Yongheng ChenDepartment of Oncology, NHC Key Laboratory of Cancer Proteomics & State Local Joint Engineering Laboratory for Anticancer Drugs, National Clinical Research Center for Geriatric Disorders, Xiangya Hospital, Central South University, Changsha, Hunan 410008, China.ORCID 0000-0001-8139-6892
Arul M ChinnaiyanMichigan Center for Translational Pathology, University of Michigan, Ann Arbor, Michigan 48109, United States.
Shaohua ChangKinoTeck Therapeutics Co., Ltd, 35 Sicheng Road, Tianhe District, Guangzhou 510663, China.
Ke DingInternational Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Discovery of Chinese Ministry of Education (MOE), Guangzhou City Key Laboratory of Precision Chemical Drug Development, College of Pharmacy, Jinan University, 855 Xingye Avenue East, Guangzhou 511400, China.ORCID 0000-0001-9016-812X
Zhen WangState Key Laboratory of Chemical Biology and Shanghai Hongkong Joint Laboratory in Chemical Synthesis, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, #345 Lingling Rd., Shanghai 200032, China.ORCID 0000-0001-8762-6089

Funding

Howard Hughes Medical Institute
6 · The paper itself

Abstract

Fibroblast growth factor receptors 2 and 3 (FGFR2/3) are attractive therapeutic targets in multiple human cancers. Here, we report the discovery of a series of tricyclic 1-(4-amino-5-ethynyl-8,9-dihydropyrazino[1',2':1,5]pyrrolo[2,3-

Indexed as

Antineoplastic AgentsDrug DesignProtein Kinase InhibitorsPyrimidinesReceptor, Fibroblast Growth Factor, Type 2Receptor, Fibroblast Growth Factor, Type 3AnimalsCell Line, TumorCell ProliferationCrystallography, X-RayHumansMiceRatsStructure-Activity RelationshipAntineoplastic AgentsFGFR2 protein, humanFGFR3 protein, humanProtein Kinase InhibitorsPyrimidinesReceptor, Fibroblast Growth Factor, Type 2Receptor, Fibroblast Growth Factor, Type 3

Identifiers

PMID42258344
PMCPMC13643868

What OpenQuestion holds

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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.